In this study an attempt was made to prepare mucoadhesive microcapsules of Clerodendrum phlomidis extract using alginate polymers for prolonged release. Encapsulation of extract into sodium alginate polymer was done by ionic-gelation technique. In vivo testing of the mucoadhesive microcapsules in diabetic albino rats demonstrated significant antidiabetic effect of extract. The hypoglycemic effect obtained by mucoadhesive microcapsules was for more than 16 h whereas plain CP extract produced an antidiabetic effect for only 4 h suggesting that mucoadhesive microcapsules are a valuable system for the long term delivery of CP extract. In-vivo data obtained over a 120-h period indicate that CP extract loaded alginate microspheres from batch F7 showed the better glycemic control than control and a commercial brand of the drug.
ABSTRACT
Hyperglycemia is the technical term for high blood glucose (sugar). It
happens when the body has too little or not enough insulin or when the
body can‘t use insulin properly. The main objective of the present
research work was to develop a bilayer tablet of immediate release
Pioglitazone and controlled release Metformin Hydrochloride, which is
used as an Anti-hyperglycemic agent. Metformin Hydrochloride has
biological half-life nearly about 6 hours, so, an attempt was made in
the direction of preparation and optimization of a combination of
sustained release and immediate release in a single tablet. In controlled
release layer natural gums like xanthum gum, gum trgacanth and guar
gum were used as retarding materials and in immediate release laye
croscarmellose sodium was used as a superdisintegrent to give the faster release of
pioglitazone. The tablets were prepared by wet granulation method and by direct
compression. Granules were evaluated for precompression parameters and the tablets were
evaluated for post compression parameters.
Key Words: Bilayer tablets, Metformin Hydrochloride, pioglitazone, xanthum gum, guar
gum, gum tragacanth and crosscarmellose sodium.
In the present study, a gastro retentive micro particulate system was formulated with different Polymers by using
solvent evaporation technique. A series of 8 formulations was prepared based on 23 Design of experiments. The
formulated microspheres were evaluated flow characteristics, Practical yield (up to 80 %) and Encapsulation
efficiency (up to 94%). Scanning electron Microscopy confirmed their porous and spherical structure and the
particles were of the Size range of (65-525 μm). The release of drug at 1 hour and 8 hours’ time points were
taken as the measurable parameters for running the DOE experiments. According to design space Hollow
Microspheres formulated with Drug in the range of 50 to 70 mg/unit, Ethyl cellulose 7 cps in the range of 145 to
150 mg/unit and HPMC 5 cps in the range of 0.4 to 2 mg/unit were observed to have the best floating
characteristics and in vitro dissolution profile as per the preset target product profile. Stability studies showed no
significant change in the drug content in the formulations at 3 months accelerated condition. In this study
concluded that a micro particulate floating dosage form of an anti-infective drug can be successfully designed to
give controlled release and improved oral bioavailability.
KEYWORDS
Gastro retentive system, Ciprofloxacin Hcl, Ethyl Cellulose 7 cps, HPMC 5cps, Hollow microspheres.
Design expert software assisted development and evaluation of cefpodoxime pro...Makrani Shaharukh
Cefpodoxime Proxetil is third generation, broad-spectrum Cephalosporin Antibiotic & it has an oral bioavailability of only 50% and biological half life 2 h so to improve it’s bioavailability sustain release matrix formulation was designed. Sustained release matrix tablets of Cefpodoxime Proxetil prepared by direct compression method based on combination of natural Acacia gum & Karaya gum polymers. 32 full factorial designs optimization study was carried out by using Design Expert Software to find the effect of independent variables, i.e., Acacia gum (X1) and Karaya gum (X2) concentration on dependent variables i.e., Hardness & % CDR. The drug excipient mixtures were subjected to preformulation studies. The tablets were subjected to physicochemical studies, in-vitro drug release, kinetic studies and stability studies. FTIR and DSC studies shown there was no interaction between drug and polymers. Matrix tablet of Cefpodoxime Proxetil were formulated well in term of hardness 5.07 ± 0. 5.93 ± 0.03 kg/cm2, thickness 2.25 ± 0.1 mm to 3.33 ± 0.3 mm, weight variation were within limits. In-vitro release studies show that almost 90 % of drug was release from all the formulation were within 12 h. Formulation F5 selected as a optimized one since it showed optimum hardness & sustained drug release within 12 h in comparison to other formulation. The F5 optimized formulations were subjected to stability studies and shown there were no significant changes in drug content, physicochemical parameters and release pattern. 32 full factorial design optimization technique was successfully used in this research work. Developed matrix tablets of Cefpodoxime Proxetil produced a sustained and effective drug release over a prolonged time frame that led to greater therapeutic efficacy.
This presentation deals with they proposal of my M Pharm research project topic briefly. It consist of various areas which needs to answer during the course of project.
ABSTRACT
Hyperglycemia is the technical term for high blood glucose (sugar). It
happens when the body has too little or not enough insulin or when the
body can‘t use insulin properly. The main objective of the present
research work was to develop a bilayer tablet of immediate release
Pioglitazone and controlled release Metformin Hydrochloride, which is
used as an Anti-hyperglycemic agent. Metformin Hydrochloride has
biological half-life nearly about 6 hours, so, an attempt was made in
the direction of preparation and optimization of a combination of
sustained release and immediate release in a single tablet. In controlled
release layer natural gums like xanthum gum, gum trgacanth and guar
gum were used as retarding materials and in immediate release laye
croscarmellose sodium was used as a superdisintegrent to give the faster release of
pioglitazone. The tablets were prepared by wet granulation method and by direct
compression. Granules were evaluated for precompression parameters and the tablets were
evaluated for post compression parameters.
Key Words: Bilayer tablets, Metformin Hydrochloride, pioglitazone, xanthum gum, guar
gum, gum tragacanth and crosscarmellose sodium.
In the present study, a gastro retentive micro particulate system was formulated with different Polymers by using
solvent evaporation technique. A series of 8 formulations was prepared based on 23 Design of experiments. The
formulated microspheres were evaluated flow characteristics, Practical yield (up to 80 %) and Encapsulation
efficiency (up to 94%). Scanning electron Microscopy confirmed their porous and spherical structure and the
particles were of the Size range of (65-525 μm). The release of drug at 1 hour and 8 hours’ time points were
taken as the measurable parameters for running the DOE experiments. According to design space Hollow
Microspheres formulated with Drug in the range of 50 to 70 mg/unit, Ethyl cellulose 7 cps in the range of 145 to
150 mg/unit and HPMC 5 cps in the range of 0.4 to 2 mg/unit were observed to have the best floating
characteristics and in vitro dissolution profile as per the preset target product profile. Stability studies showed no
significant change in the drug content in the formulations at 3 months accelerated condition. In this study
concluded that a micro particulate floating dosage form of an anti-infective drug can be successfully designed to
give controlled release and improved oral bioavailability.
KEYWORDS
Gastro retentive system, Ciprofloxacin Hcl, Ethyl Cellulose 7 cps, HPMC 5cps, Hollow microspheres.
Design expert software assisted development and evaluation of cefpodoxime pro...Makrani Shaharukh
Cefpodoxime Proxetil is third generation, broad-spectrum Cephalosporin Antibiotic & it has an oral bioavailability of only 50% and biological half life 2 h so to improve it’s bioavailability sustain release matrix formulation was designed. Sustained release matrix tablets of Cefpodoxime Proxetil prepared by direct compression method based on combination of natural Acacia gum & Karaya gum polymers. 32 full factorial designs optimization study was carried out by using Design Expert Software to find the effect of independent variables, i.e., Acacia gum (X1) and Karaya gum (X2) concentration on dependent variables i.e., Hardness & % CDR. The drug excipient mixtures were subjected to preformulation studies. The tablets were subjected to physicochemical studies, in-vitro drug release, kinetic studies and stability studies. FTIR and DSC studies shown there was no interaction between drug and polymers. Matrix tablet of Cefpodoxime Proxetil were formulated well in term of hardness 5.07 ± 0. 5.93 ± 0.03 kg/cm2, thickness 2.25 ± 0.1 mm to 3.33 ± 0.3 mm, weight variation were within limits. In-vitro release studies show that almost 90 % of drug was release from all the formulation were within 12 h. Formulation F5 selected as a optimized one since it showed optimum hardness & sustained drug release within 12 h in comparison to other formulation. The F5 optimized formulations were subjected to stability studies and shown there were no significant changes in drug content, physicochemical parameters and release pattern. 32 full factorial design optimization technique was successfully used in this research work. Developed matrix tablets of Cefpodoxime Proxetil produced a sustained and effective drug release over a prolonged time frame that led to greater therapeutic efficacy.
This presentation deals with they proposal of my M Pharm research project topic briefly. It consist of various areas which needs to answer during the course of project.
Formulation and evaluation of oral biphasic drug delivery system of Metronida...inventionjournals
In the present study, a newly innovative drug delivery system of biphasic Metronidazole (MTZ) tablet has been studied. An attempt was made to improve the patient’s adherence and the potential clinical outcomes by reducing the dosing frequency by formulating bilayer tablets containing Metrodinazole. Each bilayer tablet is composed of a sustained release (SR) layer and an immediate release (IR) layer for rapid drug release. Five different formulations of bilayer tablets were formulated using HPMC as hydrophilic polymer to retarded the drug release and the effect of Starch and MCC on the release profile were evaluated. Wet granulation method was used to prepare granules of the immediate and sustained release layers. The tablets were evaluated for their physical parameters and all valuesobtained found to be within the acceptable limits. The dissolution test has been carried out using the USP type II rotating paddle. Collected samples were analyzed using the high performance liquid chromatography. The mechanisms of Metrodinazole release from the sustained release layer were fitted into zero-order, first order, Higuchi, Hixon- Crowell model and Korsmeyer-Peppas release model. The results of the dissolution profiles showed that the drug release from the sustained release layer varied depending on the amount of HPMC and the presence of Starch or MCC. The kinetics of the release of MTZ from the different formulations showed good fitting with Higuchi model with correlation coefficients (R2) of 0.9965 - 0.9985. From values obtained for the diffusional exponent, n, Korsmeyer-Peppas equation observed that for all the formulations n value ranged from 0.4662 to 0.5370, and this demonstrates that the release mechanism followed non-Fickian type of release ( anomalous transport).
Development and evaluation of a novel twice daily cup core metformin hydrochl...SriramNagarajan19
The study was undertaken with an aim to formulate develop and evaluation of a novel twice daily core cup of Metformin hydrochloride(Antidiabetic drug) tablets using different grades and weight of HPMC polymers as release retarding agent. Granules were evaluated for tests Bulk density, tapped density, Hausner ratio before being punched as tablets. Tablets were tested for weight variation, thickness, hardness and friability as per official procedure. F-2 was found to be 73.90. From the above results and discussion it is concluded that formulation of Cup core tablet of containing Metformin hydrochloride HPMC K 4M & 215: 230 (in mg) can be taken as an ideal or optimized formulation of sustained release tablets for 12hour release as it fulfills all the requirements for sustained release tablet and our study encourages for the further clinical trials on this formulation. The core in cup tablets of Metformin hydrochloride were prepared by wet granulation method, they were evaluated for weight variation, friability, hardness, and thickness for all batches (F1 – F9). No significant difference was observed in the weight of individual tablets from the average weight. The weight variation tests were performed according to the procedure given in the pharmacopoeia. In a weight variation test, pharmacopoeial limit of tablet for percentage deviation is 5%. The average percentage deviation of all tablet formulation was found to be within the pharmacopoeial limit and hence all formulation passed the test for uniformity of weight.
The main objective of present research investigation is to formulate
the sustained release tablet of Doxofylline using 32 factorial design.
Doxofylline, an anti-Asthmatic agent, belongs BCS class-III agent.
The SR tablets of Doxofylline were prepared employing different
concentrations of HPMC K100M and Chitosan in different
combinations by Direct Compression technique using 32 factorial
design. The concentration of Polymers, HPMC K100M and
Chitosan required to achieve the desired drug release was selected as
independent variables, X1 and X2 respectively whereas, time required
for 10% of drug dissolution (t10%), 50% (t50%), 75% (t75%) and 90%
(t90%) were selected as dependent variables. Totally nine formulations
were designed, Formulated and are evaluated for hardness, friability,
thickness, % drug content, In-vitro drug release. From the Results
it was concluded that all the formulation were found to be with
in the Pharmacopoeial limits and the In-vitro dissolution profiles
of all formulations were fitted in to different Kinetic models, the
statistical parameters like intercept, slope & regression coefficient
were calculated. Polynomial equations were developed for t10%,
t50%, t75%, t90%. Validity of developed polynomial equations were
verified by designing 2 check point formulations (C1, C2). According
to SUPAC guidelines the formulation (F4) containing combination
of 10% HPMC K100M and 15% Chitosan, is the most similar
formulation (similarity factor f2= 64.501, dissimilarity factor f1=
6.862 & No significant difference, t= 0.23001) to marketed product
(DOXOLIN). The selected formulation (F4) follows Zero order,
Higuchi’s kinetics, and the mechanism of drug release was found to be Non-Fickian Diffusion anomalous Super Case-II Transport (n= 0.963).
Formulation and Evaluation of Floating Tablet of Metoprolol Succinateijtsrd
The aim of the present work is Formulation and Evaluation of Floating Tablet of Metoprolol Succinate. Metoprolol Succinate is a BCS class I drug used in the treatment of Angina pectoric, Heart attack, Hypertension and has short half life 3 7hours. In the present study it was planned to prepare sustained release floating tablets of Metoprolol succinate by using HPMC E5 and Gum Karaya excipients. The procured sample of drug was authenticated by pre formulation study like melting point, IR spectra, UV analysis were done. Results of pre formulation studies show that Metoprolol Succinate was pure and complies with standard. Prior to compression, the powder blend were evaluated for angle of repose, bulk density, tapped density, compressibility index, Hausners ratio. Results of pre formulation studies show that Metoprolol Succinate was pure and complies with standard. Formulations were evaluated for various evaluation parameters like hardness, thickness, weight variation, friability, drug content, floating lag time, floating time, swelling index and in vitro drug release. From the results of evaluation parameters it was observed that formulation F6 shows best results for floating lag time 4min floating time up to 12 hours and consistent drug release 96.15 as compared to other formulations. So formulation F6 was finalized as a optimized formulation for further study. On the basic of above finding it was concluded that sustained release floating drug delivery system was successfully achieved. Neeta. V. Jadhav | Prof. Mr. Prashant Khade | Dr. Ashok Bhosale "Formulation and Evaluation of Floating Tablet of Metoprolol Succinate" Published in International Journal of Trend in Scientific Research and Development (ijtsrd), ISSN: 2456-6470, Volume-6 | Issue-5 , August 2022, URL: https://www.ijtsrd.com/papers/ijtsrd50409.pdf Paper URL: https://www.ijtsrd.com/pharmacy/pharmaceutics/50409/formulation-and-evaluation-of-floating-tablet-of-metoprolol-succinate/neeta-v-jadhav
A new precise accurate and reliable validated method for the determination of Capecitabine was developed by using
reverse phase high performance liquid chromatography in pharmaceutical dosage forms. Spectrophotometer
determination was carried out at an absorption maximum of 240nm by using methanol. The linearity was over the
concentration range of 20-120 μg/ml with correlation coefficient 0.999. Chromatographic separation was carried
out by using a mobile phase of methanol: Acetonitrile: water (80:20:80 V/V) on Waters 2487 dual absorbance
column in an isocratic mode at a flow rate of 1.1 ml/min with UV detection at 240 nm. The developed methods were
found to be precise and accurate for the estimation of Capecitabine in pharmaceutical dosage forms and could be
used for routine analysis.
Keywords: Capecitabine, RP-HPLC, Spectrophotometry, Waters 2487 dual absorbance detector, Nova pack 300 ×
3.9mm 5μ as column, 240nm
Formulation and evaluation of oral biphasic drug delivery system of Metronida...inventionjournals
In the present study, a newly innovative drug delivery system of biphasic Metronidazole (MTZ) tablet has been studied. An attempt was made to improve the patient’s adherence and the potential clinical outcomes by reducing the dosing frequency by formulating bilayer tablets containing Metrodinazole. Each bilayer tablet is composed of a sustained release (SR) layer and an immediate release (IR) layer for rapid drug release. Five different formulations of bilayer tablets were formulated using HPMC as hydrophilic polymer to retarded the drug release and the effect of Starch and MCC on the release profile were evaluated. Wet granulation method was used to prepare granules of the immediate and sustained release layers. The tablets were evaluated for their physical parameters and all valuesobtained found to be within the acceptable limits. The dissolution test has been carried out using the USP type II rotating paddle. Collected samples were analyzed using the high performance liquid chromatography. The mechanisms of Metrodinazole release from the sustained release layer were fitted into zero-order, first order, Higuchi, Hixon- Crowell model and Korsmeyer-Peppas release model. The results of the dissolution profiles showed that the drug release from the sustained release layer varied depending on the amount of HPMC and the presence of Starch or MCC. The kinetics of the release of MTZ from the different formulations showed good fitting with Higuchi model with correlation coefficients (R2) of 0.9965 - 0.9985. From values obtained for the diffusional exponent, n, Korsmeyer-Peppas equation observed that for all the formulations n value ranged from 0.4662 to 0.5370, and this demonstrates that the release mechanism followed non-Fickian type of release ( anomalous transport).
Development and evaluation of a novel twice daily cup core metformin hydrochl...SriramNagarajan19
The study was undertaken with an aim to formulate develop and evaluation of a novel twice daily core cup of Metformin hydrochloride(Antidiabetic drug) tablets using different grades and weight of HPMC polymers as release retarding agent. Granules were evaluated for tests Bulk density, tapped density, Hausner ratio before being punched as tablets. Tablets were tested for weight variation, thickness, hardness and friability as per official procedure. F-2 was found to be 73.90. From the above results and discussion it is concluded that formulation of Cup core tablet of containing Metformin hydrochloride HPMC K 4M & 215: 230 (in mg) can be taken as an ideal or optimized formulation of sustained release tablets for 12hour release as it fulfills all the requirements for sustained release tablet and our study encourages for the further clinical trials on this formulation. The core in cup tablets of Metformin hydrochloride were prepared by wet granulation method, they were evaluated for weight variation, friability, hardness, and thickness for all batches (F1 – F9). No significant difference was observed in the weight of individual tablets from the average weight. The weight variation tests were performed according to the procedure given in the pharmacopoeia. In a weight variation test, pharmacopoeial limit of tablet for percentage deviation is 5%. The average percentage deviation of all tablet formulation was found to be within the pharmacopoeial limit and hence all formulation passed the test for uniformity of weight.
The main objective of present research investigation is to formulate
the sustained release tablet of Doxofylline using 32 factorial design.
Doxofylline, an anti-Asthmatic agent, belongs BCS class-III agent.
The SR tablets of Doxofylline were prepared employing different
concentrations of HPMC K100M and Chitosan in different
combinations by Direct Compression technique using 32 factorial
design. The concentration of Polymers, HPMC K100M and
Chitosan required to achieve the desired drug release was selected as
independent variables, X1 and X2 respectively whereas, time required
for 10% of drug dissolution (t10%), 50% (t50%), 75% (t75%) and 90%
(t90%) were selected as dependent variables. Totally nine formulations
were designed, Formulated and are evaluated for hardness, friability,
thickness, % drug content, In-vitro drug release. From the Results
it was concluded that all the formulation were found to be with
in the Pharmacopoeial limits and the In-vitro dissolution profiles
of all formulations were fitted in to different Kinetic models, the
statistical parameters like intercept, slope & regression coefficient
were calculated. Polynomial equations were developed for t10%,
t50%, t75%, t90%. Validity of developed polynomial equations were
verified by designing 2 check point formulations (C1, C2). According
to SUPAC guidelines the formulation (F4) containing combination
of 10% HPMC K100M and 15% Chitosan, is the most similar
formulation (similarity factor f2= 64.501, dissimilarity factor f1=
6.862 & No significant difference, t= 0.23001) to marketed product
(DOXOLIN). The selected formulation (F4) follows Zero order,
Higuchi’s kinetics, and the mechanism of drug release was found to be Non-Fickian Diffusion anomalous Super Case-II Transport (n= 0.963).
Similar to Formulation and invivo evaluation of mucoadhesive microspheres embedded clerodendrum phlomidis (cp) extract for prolonged antidiabetic activity
Formulation and Evaluation of Floating Tablet of Metoprolol Succinateijtsrd
The aim of the present work is Formulation and Evaluation of Floating Tablet of Metoprolol Succinate. Metoprolol Succinate is a BCS class I drug used in the treatment of Angina pectoric, Heart attack, Hypertension and has short half life 3 7hours. In the present study it was planned to prepare sustained release floating tablets of Metoprolol succinate by using HPMC E5 and Gum Karaya excipients. The procured sample of drug was authenticated by pre formulation study like melting point, IR spectra, UV analysis were done. Results of pre formulation studies show that Metoprolol Succinate was pure and complies with standard. Prior to compression, the powder blend were evaluated for angle of repose, bulk density, tapped density, compressibility index, Hausners ratio. Results of pre formulation studies show that Metoprolol Succinate was pure and complies with standard. Formulations were evaluated for various evaluation parameters like hardness, thickness, weight variation, friability, drug content, floating lag time, floating time, swelling index and in vitro drug release. From the results of evaluation parameters it was observed that formulation F6 shows best results for floating lag time 4min floating time up to 12 hours and consistent drug release 96.15 as compared to other formulations. So formulation F6 was finalized as a optimized formulation for further study. On the basic of above finding it was concluded that sustained release floating drug delivery system was successfully achieved. Neeta. V. Jadhav | Prof. Mr. Prashant Khade | Dr. Ashok Bhosale "Formulation and Evaluation of Floating Tablet of Metoprolol Succinate" Published in International Journal of Trend in Scientific Research and Development (ijtsrd), ISSN: 2456-6470, Volume-6 | Issue-5 , August 2022, URL: https://www.ijtsrd.com/papers/ijtsrd50409.pdf Paper URL: https://www.ijtsrd.com/pharmacy/pharmaceutics/50409/formulation-and-evaluation-of-floating-tablet-of-metoprolol-succinate/neeta-v-jadhav
A new precise accurate and reliable validated method for the determination of Capecitabine was developed by using
reverse phase high performance liquid chromatography in pharmaceutical dosage forms. Spectrophotometer
determination was carried out at an absorption maximum of 240nm by using methanol. The linearity was over the
concentration range of 20-120 μg/ml with correlation coefficient 0.999. Chromatographic separation was carried
out by using a mobile phase of methanol: Acetonitrile: water (80:20:80 V/V) on Waters 2487 dual absorbance
column in an isocratic mode at a flow rate of 1.1 ml/min with UV detection at 240 nm. The developed methods were
found to be precise and accurate for the estimation of Capecitabine in pharmaceutical dosage forms and could be
used for routine analysis.
Keywords: Capecitabine, RP-HPLC, Spectrophotometry, Waters 2487 dual absorbance detector, Nova pack 300 ×
3.9mm 5μ as column, 240nm
Formulation and Evaluation of Colon Targeted Suppository of Mesalazineijtsrd
The aim of the present investigation was to formulate and evaluate of Colon Targeted Suppository of Mesalazine. The attempts have been made to increase the dissolution of BCS class IV drug Mesalazine using Cocoa butter, Polyethylene Glycol 6000, Polyethylene Glycol 9000 as base which was prepared by Fusion Method. Base combinations was prepared. Total three formulations of each combinations of base Cocoa butter Polyethylene Glycol 6000 and Cocoa butter Polyethylene Glycol 9000 were prepared in the ratio of 1 9 to 9 1.Cocoa butter was taken alone and used as standard. These base combinations were evaluated for optimization of base using parameters like melting point and liquefaction time. The optimized base Cocoa butter Polyethylene Glycol 6000 with ratio of1 9 and Cocoa butter Polyethylene Glycol 9000 with ratio of1 9 was then formulated into Colon Targeted Suppository of Mesalazine. Polyethylene glycol 400 was added in combination of bases which was used as plasticizer to increase its flexibility which was added in the concentration of 15, 30 and 45 . Displacement value was then calculated to formulate suppository. These formulated colon targeted Mesalazine suppository were evaluated with parameters such as weight variation, hardness, melting point, liquefaction time, content uniformity, and dissolution test. The F3 batch was selected as optimized formulation and was found superior. The F3 formulation shows high drug release of 94.31 and less dissolution time of 30 minutes from six formulation batches Hence showing better results than other formulations. When F3 formulation was compared with marketed formulation, it gives highest percent drug release than marketed formulation. The results of stability studies showed that F3 has no significant change in drug content, melting point, hardness, liquefaction time and dissolution profile of suppositories after storing them for 90 days at refrigeration temperature. Shrutika S. Kamble | Mrs. Trusha P. Shangrapawar | Dr. Ashok Bhosale "Formulation and Evaluation of Colon Targeted Suppository of Mesalazine" Published in International Journal of Trend in Scientific Research and Development (ijtsrd), ISSN: 2456-6470, Volume-6 | Issue-5 , August 2022, URL: https://www.ijtsrd.com/papers/ijtsrd50411.pdf Paper URL: https://www.ijtsrd.com/pharmacy/pharmaceutics/50411/formulation-and-evaluation-of-colon-targeted-suppository-of-mesalazine/shrutika-s-kamble
Research by Mahendra Kumar Trivedi - Evaluation of the Impact of Biofield Tre...john henrry
Research on Trivedi Effect - In the present study, the influence of biofield treatment on physical and thermal properties of Casein Enzyme Hydrolysate (CEH) and Casein Yeast Peptone (CYP) were investigated. The control and treated samples were characterized by Fourier transform infrared (FT-IR) spectroscopy, differential scanning calorimetry (DSC), Thermo Gravimetric Analysis (TGA), particle size and surface area analysis.to read more visit http://www.academicroom.com/article/evaluation-impact-biofield-treatment-physical-and-thermal-properties-casein-enzyme-hydrolysate-and-casein-yeas-t-peptone
Research by Mahendra Kumar Trivedi - Evaluation of the Impact of Biofield Tre...Abby Keif
http://works.bepress.com/mahendra_trivedi/54/ - Research on Trivedi Effect - In the present study, the influence of biofield treatment on physical and thermal properties of Casein Enzyme Hydrolysate (CEH) and Casein Yeast Peptone (CYP) were investigated. The control and treated samples were characterized by Fourier transform infrared (FT-IR) spectroscopy, differential scanning calorimetry (DSC), Thermo Gravimetric Analysis (TGA), particle size and surface area analysis.
Neuro Quantology is an international, interdisciplinary, open-access, peer-reviewed journal that publishes original research and review articles on the interface between quantum physics and neuroscience. The journal focuses on the exploration of the neural mechanisms underlying consciousness, cognition, perception, and behavior from a quantum perspective. Neuro Quantology is published monthly.
MICROBALLOONS: A NOVEL APPROACH IN GASTRO-RETENTION FLOATING DRUG DELIVERY SY...Snehal Patel
ABSTRACT
Oral controlled release dosage forms face several physiological restriction like inability to retain
and position the controlled drug delivery system within the targeted region of the gastrointestinal
tract (GIT) due to fluctuation in gastric emptying. This results in non uniform absorption
pattern, inadequate medication release and shorter residence time of the dosage form in the
stomach. As the fallout of this episode there is inadequate absorption of the drug having
absorption window predominantly, in the upper area of GIT. These contemplations have
provoked to the development of oral controlled release dosage forms with gastroretentive
properties. Microballoons (Hollow microspheres) hold certification as one of the potential
approaches for gastric retention. Microballoons are spherical empty particles without core and
can remain in the gastric region for delayed periods. They significantly increase the gastric
residence time of medication, thereby enhance bioavailability, improves patient compliance by
reducing dosing frequency, lessen the medication waste, enhance retention of medication which
solubilize only in stomach, enhance solubility for medications that are less soluble at a higher pH
environment. The present review preparation methods, characterization, advantages,
disadvantages, mechanism of drug release from microballoons, applications and list of the drugs
formulated as microballoons are discussed.
KEYWORDS: Microballoons, Gastro-retention, Floating drug delivery system (FDDS).
Ten Reliable Sources to Learn About Journal of Nano Medicine and Nanotechnologyscience journals
The nano medicine Journal enjoys reputation and popularity among the medical practitioners, as a novice technology in the biomedical research that offers innovative therapeutic practices. Nanotechnology as a medical application offers plethora of opportunities for the practitioners to explore innovative ways of drug delivery systems, therapies and In vivo imaging techniques.
In-vitro anti-inflammatory activity of oral poly herbal formulations rashmi y...thepharmacyjournal
Aim: To evaluate the In-vitro anti-inflammatory activity of Oral poly herbal formulations.
Methodology: The In-vitro anti-inflammatory activity was investigated by protein denaturation method using Egg's albumin and Bovine serum albumin. The Hydro-alcoholic extracts of the plants used for the preparation of six poly herbal formulations. In-vitro anti-inflammatory activity of all poly herbal formulations were estimated by protein denaturation method using Egg's albumin and Bovine serum albumin at 50 - 250 μg/ml concentrations. The result was assessed UV spectrophotometer at 660nm and compared with the diclofenac sodium as standard drug.
Result: The result revealed that the all six oral poly herbal formulations possessed significant anti-inflammatory activity. But the formulations F5 and F6 exhibited the maximum percentage inhibition of Protein denaturation at 200μg/ml concentration 86.07% (using Egg's albumin) and 85.14% (using Bovine serum albumin) as compared to others formulations. The standard drug diclofenac sod. showed 98.06, 97.91% inhibition for Bovine serum and Egg's albumin methods, respectively.
Conclusion: The study concluded that the formulations is an effective inhibitor of protein denaturation and showed potent anti- inflammatory activity.
Prophylactic role of coenzyme Q10 and Cynara scolymus L on doxorubicin-indu...Prof. Hesham N. Mustafa
Objective: The study aims to evaluate the protective effects of coenzyme Q10 (CoQ10) and Cynara scolymus L (CS) on doxorubicin (dox)-induced toxicity.
Materials and Methods: Sixty male rats were divided into six groups. Group 1 as a control. Group 2 received dox (10 mg/kg) intraperitoneally. Group 3 received CoQ10 (200 mg/kg). Group 4 received CS (500 mg/kg). Group 5 received CoQ10 (200 mg/kg) and dox (10 mg/kg). Group 6 received CS (500 mg/kg) and dox (10 mg/kg). The rats were then evaluated biochemically and immunohistochemically.
Results: Dox produced a significant deterioration of hepatic and renal functional parameters. Moreover, an upsurge of oxidative stress and nitrosative stress markers. The expression of alpha-smooth muscle actin (α-SMA) was increased and proliferating cell nuclear antigen (PCNA) expression was decreased. Administration of CoQ10 and CS resulted in a significant improvement of hepatic and renal functional parameters, and an improvement of both α-SMA and PCNA.
Conclusion: It is concluded that pretreatment with CoQ10 and CS is associated with up-regulation of favorable protective enzymes and down-regulation of oxidative stress. That can be advised as a supplement to dox-treated patients.
Keywords: Alpha-smooth muscle actin, doxorubicin, nitrosative, oxidative, proliferating cell nuclear antigen
Hepatoprotective Effect of Cestrum parqui L. aerial parts and Phytochemical ...Jing Zang
This study deals with the investigation of hepatoprotective effect of 70% methanolic extract from Cestrum parqui aerial parts and determination of the bioactive components of the plant. The hepatoprotective effect of Cestrum parqui methanol extract (100, 500, 1000 mg/kg) was analysed on carbon tetrachloride (CCl4)-induced acute liver injury. The administration of a single dose of 40% CCl4 (1ml/kg b.w.) causes an increase in the activities of serum alanine aminotransferase (ALT) and aspirate aminotransferase (AST) enzymes and so pretreated orally of a dose from Cestrum parqui methanol extract (100, 500, 1000 mg/kg) and silymarin (200 mg/kg) for three consecutive days prior to The administration of a single dose of CCl4 significantly prevented the increase in the activities of these enzymes. Histological analysis showed that Cestrum parqui methanol extract at doses of 500 and 1000 mg/kg and silymarin reduced the incidence of liver lesions including vacuole formation, neutrophil infiltration and necrosis of hepatocytes induced by CCl4. The extract cause a negative result on the antioxidative enzymes, superoxide dismutase (SOD), glutathione peroxidase (GPx), glutathione reductase (GRd) and decreased malondialdehyde (MDA) level in liver, as compared to those in the CCl4-treated group and this suggests that the hepatoprotective activity of the extract is due to the antioxidant effect of the extract. Phytochemical analysis of the methanol extract from Cestrum parqui aerial parts showed that it contained different phytoconstituents, flavonoids, tannins, saponins, alkaloids, terpenes and carbohydrates.
IOSR Journal of Pharmacy and Biological Sciences(IOSR-JPBS) is an open access international journal that provides rapid publication (within a month) of articles in all areas of Pharmacy and Biological Science. The journal welcomes publications of high quality papers on theoretical developments and practical applications in Pharmacy and Biological Science. Original research papers, state-of-the-art reviews, and high quality technical notes are invited for publications.
ABSTRACT Human platelet-derived growth factor-BB (hPDGF-BB), a proliferation factor, has been successfully manufactured and approved by FDA as the treatment for diabetic foot ulcer and self bone grafting. There have been no reports on the storage of the recombinant hPDGF-BB (rhPDGF-BB) in the Pichia pastoris fermentation broth although during the research of process development and the production manufacture it needs to be stored at low temperature. The concentration of rhPDGF-BB protein in the fed-batch fermentation broth of P. pastoris was stable during 3-week storage at -20oC, but its bioactivity was reduced by 20%. The addition of a mixture of 50% glycerol with either 1 mM EDTA or 1 mM PMSF into the fermentation broth could fully preserve the bioactivity of rhPDGF-BB until 3 weeks at -20oC. The addition of 50% glycerol with either 1 mM EDTA or 1 mM PMSF was found no affection on the protein purification process.
Key-words: rhPDGF-BB, Pichia pastoris, Fed-batch fermentation, Protein stability, Bioactivity, Storage
Similar to Formulation and invivo evaluation of mucoadhesive microspheres embedded clerodendrum phlomidis (cp) extract for prolonged antidiabetic activity (20)
A new RP -HPLC method development and validation for simultaneous estimation ...SriramNagarajan19
A simple, accurate, precise method was developed for the simultaneous estimation of the Aspirin and Omeprazole in Tablet dosage form. Chromatogram was run through Discovery 250 x 4.6 mm, 5m. Mobile phase containing Buffer and Acetonitrile in the ratio of 70:30 v/v was pumped through column at a flow rate of 1 ml/min. Temperature was maintained at 30°C. Optimized wavelength for Aspirin and Omeprazole was 241 nm. Retention time of Aspirin and Omeprazole were found to be 2.454 min and 3.168 min %RSD of the Aspirin and Omeprazole were and found to be 1.1 and 0.8 respectively. Percentage recovery was obtained as 99.50% and 99.57%for Aspirin and Omeprazole. LOD, LOQ values were obtained from regression equations of Aspirin and Omeprazole were 0.26ppm, 0.80ppm and 0.06ppm, 0.17ppm respectively. Regression equation of Aspirin is y = 3524x + 3853, and of Omeprazole is y = 10438x+542.2.
Nutrease powder; a natural plant based nutritional shake with co-factors & co...SriramNagarajan19
Nutrease powder is an effective natural vitamin and minerals Nutritional supplementation to improve metabolism. Nutrease powder just ½ serving (1 scoop) Provides 150 calories,18 grams of protein, 12 grams of fiber, and 1 gram of sugar per day. Nutrease powder Supports effective weight management, Reduces hunger and cravings, Promotes energy and positive mood, Promotes loss of fat and preservation of lean body mass, Improves metabolism and insulin sensitivity. This article reviews the current available scientific literature regarding the effect of nutrease powder as an effective supplementation for daily energy needs.
Analytical method development and validation for the estimation of quinapril ...SriramNagarajan19
A simple and selective LC method is described for the determination of Quinapril and Tolcapone tablet dosage forms. Chromatographic separation was achieved on a c18 column using mobile phase consisting of a Mixed Phosphate buffer (KH2PO4 +K2HPO4): Acetonitrile 40:60, with detection of 239 nm. Linearity was observed in the range 50 - 150 µg /ml for Quinapril (r2 =0.995) and 62.5- 187.5µg /ml for Tolcapone (r2 =0.999) for the amount of drugs estimated by the proposed methods was in good agreement with the label claim.
The proposed methods were validated. The accuracy of the methods was assessed by recovery studies at three different levels. Recovery experiments indicated the absence of interference from commonly encountered pharmaceutical additives. The method was found to be precise as indicated by the repeatability analysis, showing %RSD less than 2. All statistical data proves validity of the methods and can be used for routine analysis of pharmaceutical dosage form.
Method development and validation of simultaneous estimation of paracetamol &...SriramNagarajan19
A drug may be defined as a substance meant for diagnosis, cure, mitigation, prevention or treatment of diseases in human beings or animals or for alternating any structure or function of the body of human being or animals. Pharmaceutical chemistry is a science that makes use of general laws of chemistry to study drugs i.e. their preparation, chemical natures, composition, structure, influence on an organism and studies the physical and chemical properties of drugs, the methods of quality control and the conditions of their storage etc. the family of drugs may be broadly classified as.
1. Pharmacodynamic agents.
2. Chemotherapeutic agents.
It is necessary to find the content of each drug either in pure or single, combined dosage forms for purity testing. It is also essential to know the concentration of the drug and it’s metabolites in biological fluids after taking the dosage form for treatment.
The scope of developing and validating analytical methods is to ensure a suitable method for a particular analyte more specific, accurate and precise. The main objective for that is to improve the conditions and parameters, which should be followed in the development and validation.
WELLIA-R tablets; helps to protect brain tissue in cerebral edemaSriramNagarajan19
Boswellia serrate extract in Wellia- R gained significant importance in treatment of cerebral edema in patients with brain tumors, colon cancer, lung cancer, blood cancer, skin cancer, breast cancer, renal cancer, fibro sarcoma, prostate cancer and pancreatic cancer. The medicinal properties of Boswellia serrate extract in Wellia- R have been known and utilized since antiquity. Its current potential as an anti inflammatory and anticancer agent are being investigated and hold great promise. This article reviews the current available scientific literature regarding the effect of wellia-R tablets, from Boswellia serrate extract that Provides long lasting cerebral protection in brain tumor patients
Brian stroke memory impairment and treatment strategiesSriramNagarajan19
A brain stroke occurs when one of the brain parts are deprived form oxygen-rich blood due to various mechanism. Usually a brain stroke occurs when one of the arteries is blocked either because of narrowing of small arteries with in the brain or the hardening of the arteries that lead to atherosclerosis strokes can be either ischemic (85%) or Hemorrhagic (15%). Forget fullness is a common complaint among older people. Age –related memory changes are not the same thing as dementia. Preventing memory loss is by exercise regularly staying social, manage stress, get plenty of sleep and don’t smoke. Eat plenty of fruits and vegetable and take food contain antioxidant in abundance; will reduce your risk of stroke. Walking regularly is an easy to fight memory loss and also brain exercises to prevent loss and boost brainpower. Research is going no to enhance memory power in brain in patient with brain stroke.
A new analytical method development and validation for the estimation of lenv...SriramNagarajan19
A simple and selective LC method is described for the determination of Lenvatinib dosage forms. Chromatographic separation was achieved on a c18 column using mobile phase consisting of a mixture of Phosphate buffer (KH2PO4): Acetonitrile (80:20) with detection of 240nm. Linearity was observed in the range 60-140 µg /ml for Lenvatinib (r2 =0.996) for the amount of drug estimated by the proposed methods was in good agreement with the label claim.
The proposed methods were validated. The accuracy of the methods was assessed by recovery studies at three different levels. Recovery experiments indicated the absence of interference from commonly encountered pharmaceutical additives. The method was found to be precise as indicated by the repeatability analysis, showing %RSD less than 2. All statistical data proves validity of the methods and can be used for routine analysis of pharmaceutical dosage form.
A new analytical method development and validation for the simultaneus estima...SriramNagarajan19
A simple and selective LC method is described for the determination of LEDIPASVIR and SOFOSBUVIR in tablet dosage forms. Chromatographic separation was achieved on a c18 column using mobile phase consisting of a mixture of Mixed Phosphate Buffer:ACN (55:45) with detection of 213 nm. Linearity was observed in the range 60-140 µg/ml for LEDIPASVIR oxalate (r2 =0.999) and 6-14 µg /ml for SOFOSBUVIR (r2 =0.996) for the amount of drugs estimated by the proposed methods was in good agreement with the label claim.
The proposed methods were validated. The accuracy of the methods was assessed by recovery studies at three different levels. Recovery experiments indicated the absence of interference from commonly encountered pharmaceutical additives. The method was found to be precise as indicated by the repeatability analysis, showing %RSD less than 2. All statistical data proves validity of the methods and can be used for routine analysis of pharmaceutical dosage form.
A new analytical method development and validation for the simultaneus estima...SriramNagarajan19
A simple and selective LC method is described for the determination of Ibuprofen and Tramadol in tablet dosage forms. Chromatographic separation was achieved on a c18 column using mobile phase consisting of a mixture of 60 volumes of Triethylamine buffer, 40 volumes of acetonitrile with detection of 227 nm. Linearity was observed in the range 50-150 µg/ml for Ibuprofen (r2 =0.983) and 50-150 µg /ml for Tramadol (r2 =0.985) for the amount of drugs estimated by the proposed methods was in good agreement with the label claim.
The proposed methods were validated. The accuracy of the methods was assessed by recovery studies at three different levels. Recovery experiments indicated the absence of interference from commonly encountered pharmaceutical additives. The method was found to be precise as indicated by the repeatability analysis, showing %RSD less than 2. All statistical data proves validity of the methods and can be used for routine analysis of pharmaceutical dosage form.
Method development and validation of escitalopram and estizolam in tablet dos...SriramNagarajan19
A simple and selective LC method is described for the determination of Escitalopram oxalate and Etizolam in tablet dosage forms. Chromatographic separation was achieved on a c18 column using mobile phase consisting of a mixture of 30 volumes of ammonium acetate buffer, 40 volumes of acetonitrile and 30 volumes of Methanol with detection of 238 nm. Linearity was observed in the range 60-140 µg/ml for Escitalopram oxalate (r2 =0.999) and 6-14 µg /ml for Etizolam (r2 =0.996) for the amount of drugs estimated by the proposed methods was in good agreement with the label claim.
The proposed methods were validated. The accuracy of the methods was assessed by recovery studies at three different levels. Recovery experiments indicated the absence of interference from commonly encountered pharmaceutical additives. The method was found to be precise as indicated by the repeatability analysis, showing %RSD less than 2. All statistical data proves validity of the methods and can be used for routine analysis of pharmaceutical dosage form.
Analytical method development and validation for the estimation of aspirin an...SriramNagarajan19
A simple and selective LC method is described for the determination of Aspirin and Omeprazole in tablet dosage forms. Chromatographic separation was achieved on a c18 column using mobile phase consisting of a mixture of 30 volumes of ammonium acetate buffer, 40 volumes of acetonitrile and 30 volumes of Methanol with detection of 233 nm. Linearity was observed in the range 18-42 µg/ml for Aspirin (r2 =0.983) and 6-14 µg /ml for Omeprazole (r2 =0.970) for the amount of drugs estimated by the proposed methods was in good agreement with the label claim. The proposed methods were validated. The accuracy of the methods was assessed by recovery studies at three different levels. Recovery experiments indicated the absence of interference from commonly encountered pharmaceutical additives. The method was found to be precise as indicated by the repeatability analysis, showing %RSD less than 2. All statistical data proves validity of the methods and can be used for routine analysis of pharmaceutical dosage form.
A new analytical method development and validation for the simultaneus estima...SriramNagarajan19
A simple and selective LC method is described for the determination of Albuterol and Ipratropium Bromide in tablet dosage forms. Chromatographic separation was achieved on a c18 column using mobile phase consisting of a mixture of 80 volumes of methanol and 20 volumes of water with detection of 239 nm. Linearity was observed in the range 36-84 µg /ml for Albuterol (r2 =0.996) and 6-14 µg /ml for Ipratropium Bromide (r2 =0.997) for the amount of drugs estimated by the proposed methods was in good agreement with the label claim.
The proposed methods were validated. The accuracy of the methods was assessed by recovery studies at three different levels. Recovery experiments indicated the absence of interference from commonly encountered pharmaceutical additives. The method was found to be precise as indicated by the repeatability analysis, showing %RSD less than 2. All statistical data proves validity of the methods and can be used for routine analysis of pharmaceutical dosage form.
Formulation and evaluation of rosiglitazone nanosuspensionSriramNagarajan19
The main aim of this study is to formulate and evaluate Rosiglitazone Nano suspension. Nano suspensions are colloidal dispersion of Nano sized drug particles stabilized by surfactants. They can also be defined as a biphasic system consisting of pure drug particles dispersed in an aqueous vehicle in which the diameter of the suspended particle is less than 1micro meter in size. Rosiglitazone is an oral rapid and short –acting anti-diabetic drug from the sulfonylurea class. It is classified as a second generation sulfonylurea, which means that it undergoes enter hepatic circulation. Rosiglitazone Nano suspension was prepared by precipitation technique. After preparation of Nano suspension various characterization studies were done such as drug content, %yield, FTIR, DSC, TEM, and Invitro drug release.PVPK30,polaxomer are used as stabilizers. From the dissolution study F4 formulation which containts PVPK30 as stabilizer was considered as optimized formulation. It showed maximum drug release at 30min.FTIR and DSC studies revealed that good stability in dispersion.
Effect of hydrophilic polymers on solubility of some antihypertentives drugs ...SriramNagarajan19
The main aim of the present study is to carried out to enhance solubility of Felodipine. Felodipine.was selected as model drug and different carriers like Vitamin-E, Polyethylene Glycol 8000, Polyvinyl pyrrolidone K-30 were used in drug to carrier ratio 1:1, 1:2, 1:4 by weight respectively. Solid dispersions were prepared by physical mixing method and solvent evaporation method. Solid dispersions were evaluated by drug content, in-vitro release, FT-IR, DSC and XRD. The obtained data of solid dispersion prepared by solvent evaporation method were compared with physical mixing method. The result showed decrease in melting point change from crystalline to amorphous form and improved dissolution rate as compared to physical mixing as well as pure Felodipine. The finding of present study proposes that solid dispersion approach is beneficial in enhancing solubility of drug and bioavailability as well.
A review on plants act on both antidiabetic and antihyperlipidemic plantsSriramNagarajan19
Since ancient times, plants have been an exemplary source of medicine. Ayurveda and other Indian literature mentioned the use of plants in treatment of various human ailments. Medical plants play an important role in the management of diabetes mellitus especially in developing countries where resources are meager. Oral hypoglycemic agents like sulphonylureas and biguanides are still the major players in the management of the disease but there is growing interest in herbal remedies due to the side effects associated with the oral hypoglycemic agents. Herbal medicines have been the highly esteemed source of medicine throughout human history. Hyperlipidemia has been ranked as one of the greatest risk factors contributing to prevalence and severity of coronary heart diseases. Hyperlipidemia is a condition when abnormally high levels of lipids i.e. the fatty substances are found in the blood. Hypolipidemic drugs are extensively used as prophylactic agents to prevent such atherosclerosis induced disorders. But these hypolipidemic drugs are not free from adverse effects. Many plant derivatives and domestic remedies have been screened for their hypolipidemic action. More than 70 medicinal plants have been documented to have significant hypolipidemic action. During the last decade, an increase in the use of medicinal plants has been observed in metropolitan areas of developed countries. Medicinal plants play a major role in diabetes and hypolipidemic activity. The advantages of herbal medicines reported are effectiveness, safety, affordability and acceptability, this review focus on diabeties and hyperlipidemia and the role of plants used for the treatment of diabeties and hyperlipidemia.
FORMULATION AND CHARACTERISATION OF TRANSDERMAL PATCHES OF PERINDOPRILSriramNagarajan19
Transdermal drug delivery system (TDDS) has been an increased interest in the drug administration via the skin for both local therapeutic effects on diseased skin (topical delivery) as well as for systemic delivery of drugs. The skin as a site of drug delivery, has a number of significant advantages over many other routes of drug administration, including the ability to avoid problems of gastric irritation, pH and emptying rate effects, avoid hepatic first-pass metabolism thereby increasing the bioavailability of drug, reduce the risk of systemic side effects by minimizing plasma concentrations compared to oral therapy, provide a sustained release of drug at the site of application; rapid termination of therapy by removal of the device or formulation, the reduction of fluctuations in plasma levels of drugs, and avoid pain associated with injections. The transdermal delivery can also eliminate pulsed entry into the systemic circulation, which might often cause undesirable side effects. Main objective of formulating the transdermal system was to prolong the drug release time, reduce the frequency of administration and to improve patient compliance. In the present study, five formulations were prepared using single polymer in different ratios, along with plasticizers and penetration enhancer. Finally it was concluded that Some formulations show formation of brittle patch due to insufficient amount of polymer and in some patches texture of patch is not elegant due to plasticizer concentration for patch preparation. So by increasing concentration of polymer and plasticizer, finally formulation-5 was considered as optimized formula for preparing transdermal patch of Perindopril, where it shown best drug release profile.
Intercontinental journal of pharmaceutical Investigations and ResearchSriramNagarajan19
Anti-inflammatory activity of the ethanolic extract of Portulaca quadrifida Linn. was studied in wister rats using the carrageenan induced left hind paw edema, carrageenan induced pleurisy and cotton pellet induced granuloma model. The ethanolic extract (200 mg/kg, p.o.,) produced the inhibition of carrageenan induced rat paw edema. It also showed an inhibitory effect on leukocyte migration and a reduction on the pleural exudates as well as reduction on the granuloma weight in the cotton pellet granuloma method. The results indicated that the ethanolic extract produced significant (P<0.001) anti-inflammatory activity when compared with the standard and untreated control.
ANTI-BACTERIAL ACTIVITY OF EXTRACTS OF TACHYSPERMUM AMMI FRUITSSriramNagarajan19
This study was carried out with an objective to investigate the antibacterial activity of Tachyspermum ammi fruits extracts. In the present study, the anti-bacterial activity of aqueous and ethanolic extracts of Tachyspermum ammi fruits was evaluated for potential antimicrobial activity against medically important bacterial and fungal strains. The antimicrobial activity was determined using agar disc diffusion method. The antibacterial and antifungal activities of extracts were tested against Gram-positive—Staphylococcus aureus and Gram-negative—Escherichia coli human pathogenic bacteria. Zone of inhibition of extracts were compared with that of different standard drugs. The results showed that the remarkable inhibition of the bacterial growth was shown against the tested organisms. The phytochemical analyses of the plants were carried out. The antibacterial activity of the Tachyspermum ammi fruits was due to the presence of various secondary metabolites. Hence, these plants can be used to discover bioactive natural products that may serve as leads in the development of new pharmaceuticals research activities.
Live Longer, Stay healthy, Feel better with AstashinecapsulesSriramNagarajan19
ASTASHINE capsule contains natural astaxanthin from Haematococcus pluvialis Astaxanthin has exceptional antioxidant activity to combat singlet oxygen when compared to other antioxidants. In particular, Astaxanthin can be used to defend against singlet oxygen damage, which are especially susceptible to aging effects.
In this study, Astaxanthin extracted from Haematococcus microalgae powerfully quenched singlet oxygen. Results show that the quenching effect of Astaxanthin is 800 times greater than coenzyme Q10. Astaxanthin was also about 75 times greater than alpha lipoic acid, about 550 times greater than green tea catechins and about 6000 times greater than Vitamin C.the present Article reviews the role of ASTASHINE capsules as World’s most powerful Antioxidant and Anti-aging Nutrient.
Astashine capsules: an excellent choice for eye fatique relieveSriramNagarajan19
Scientists long ago discovered that a class of naturally-occurring pigments called carotenoids held powerful antioxidant properties that are crucial for eye health. This carotenoid is called astaxanthin. Astaxanthin is produced by the microalgae Haematococcus pluvialis when its water supply dries up, forcing it to protect itself from ultraviolet radiation. Astaxanthin is leaps and bounds more powerful than beta-carotene, alpha-tocopherol, lycopene, and lutein--other members of its chemical family. Astaxanthin exhibits very strong free radical scavenging activity, and protects eyes from oxidative damage. Astaxanthin is by far the most powerful carotenoid antioxidant when it comes to free radical scavenging: it is 65 times more powerful than vitamin C, 54 times more powerful than beta-carotene, and 14 times more powerful than vitamin E. Astaxanthin is far more effective than other carotenoids at "singlet oxygen quenching," which is a particular type of oxidation. The damaging effects of sunlight and various organic materials are caused by this less-stable form of oxygen. Astaxanthin is 550 times more powerful than vitamin E and 11 times more powerful than beta-carotene at neutralizing this singlet oxygen. Astaxanthin crosses the blood-brain barrier and the blood-retinal barrier which has huge implications for the health of eyes.
Recomendações da OMS sobre cuidados maternos e neonatais para uma experiência pós-natal positiva.
Em consonância com os ODS – Objetivos do Desenvolvimento Sustentável e a Estratégia Global para a Saúde das Mulheres, Crianças e Adolescentes, e aplicando uma abordagem baseada nos direitos humanos, os esforços de cuidados pós-natais devem expandir-se para além da cobertura e da simples sobrevivência, de modo a incluir cuidados de qualidade.
Estas diretrizes visam melhorar a qualidade dos cuidados pós-natais essenciais e de rotina prestados às mulheres e aos recém-nascidos, com o objetivo final de melhorar a saúde e o bem-estar materno e neonatal.
Uma “experiência pós-natal positiva” é um resultado importante para todas as mulheres que dão à luz e para os seus recém-nascidos, estabelecendo as bases para a melhoria da saúde e do bem-estar a curto e longo prazo. Uma experiência pós-natal positiva é definida como aquela em que as mulheres, pessoas que gestam, os recém-nascidos, os casais, os pais, os cuidadores e as famílias recebem informação consistente, garantia e apoio de profissionais de saúde motivados; e onde um sistema de saúde flexível e com recursos reconheça as necessidades das mulheres e dos bebês e respeite o seu contexto cultural.
Estas diretrizes consolidadas apresentam algumas recomendações novas e já bem fundamentadas sobre cuidados pós-natais de rotina para mulheres e neonatos que recebem cuidados no pós-parto em unidades de saúde ou na comunidade, independentemente dos recursos disponíveis.
É fornecido um conjunto abrangente de recomendações para cuidados durante o período puerperal, com ênfase nos cuidados essenciais que todas as mulheres e recém-nascidos devem receber, e com a devida atenção à qualidade dos cuidados; isto é, a entrega e a experiência do cuidado recebido. Estas diretrizes atualizam e ampliam as recomendações da OMS de 2014 sobre cuidados pós-natais da mãe e do recém-nascido e complementam as atuais diretrizes da OMS sobre a gestão de complicações pós-natais.
O estabelecimento da amamentação e o manejo das principais intercorrências é contemplada.
Recomendamos muito.
Vamos discutir essas recomendações no nosso curso de pós-graduação em Aleitamento no Instituto Ciclos.
Esta publicação só está disponível em inglês até o momento.
Prof. Marcus Renato de Carvalho
www.agostodourado.com
Pulmonary Thromboembolism - etilogy, types, medical- Surgical and nursing man...VarunMahajani
Disruption of blood supply to lung alveoli due to blockage of one or more pulmonary blood vessels is called as Pulmonary thromboembolism. In this presentation we will discuss its causes, types and its management in depth.
New Directions in Targeted Therapeutic Approaches for Older Adults With Mantl...i3 Health
i3 Health is pleased to make the speaker slides from this activity available for use as a non-accredited self-study or teaching resource.
This slide deck presented by Dr. Kami Maddocks, Professor-Clinical in the Division of Hematology and
Associate Division Director for Ambulatory Operations
The Ohio State University Comprehensive Cancer Center, will provide insight into new directions in targeted therapeutic approaches for older adults with mantle cell lymphoma.
STATEMENT OF NEED
Mantle cell lymphoma (MCL) is a rare, aggressive B-cell non-Hodgkin lymphoma (NHL) accounting for 5% to 7% of all lymphomas. Its prognosis ranges from indolent disease that does not require treatment for years to very aggressive disease, which is associated with poor survival (Silkenstedt et al, 2021). Typically, MCL is diagnosed at advanced stage and in older patients who cannot tolerate intensive therapy (NCCN, 2022). Although recent advances have slightly increased remission rates, recurrence and relapse remain very common, leading to a median overall survival between 3 and 6 years (LLS, 2021). Though there are several effective options, progress is still needed towards establishing an accepted frontline approach for MCL (Castellino et al, 2022). Treatment selection and management of MCL are complicated by the heterogeneity of prognosis, advanced age and comorbidities of patients, and lack of an established standard approach for treatment, making it vital that clinicians be familiar with the latest research and advances in this area. In this activity chaired by Michael Wang, MD, Professor in the Department of Lymphoma & Myeloma at MD Anderson Cancer Center, expert faculty will discuss prognostic factors informing treatment, the promising results of recent trials in new therapeutic approaches, and the implications of treatment resistance in therapeutic selection for MCL.
Target Audience
Hematology/oncology fellows, attending faculty, and other health care professionals involved in the treatment of patients with mantle cell lymphoma (MCL).
Learning Objectives
1.) Identify clinical and biological prognostic factors that can guide treatment decision making for older adults with MCL
2.) Evaluate emerging data on targeted therapeutic approaches for treatment-naive and relapsed/refractory MCL and their applicability to older adults
3.) Assess mechanisms of resistance to targeted therapies for MCL and their implications for treatment selection
Report Back from SGO 2024: What’s the Latest in Cervical Cancer?bkling
Are you curious about what’s new in cervical cancer research or unsure what the findings mean? Join Dr. Emily Ko, a gynecologic oncologist at Penn Medicine, to learn about the latest updates from the Society of Gynecologic Oncology (SGO) 2024 Annual Meeting on Women’s Cancer. Dr. Ko will discuss what the research presented at the conference means for you and answer your questions about the new developments.
Title: Sense of Taste
Presenter: Dr. Faiza, Assistant Professor of Physiology
Qualifications:
MBBS (Best Graduate, AIMC Lahore)
FCPS Physiology
ICMT, CHPE, DHPE (STMU)
MPH (GC University, Faisalabad)
MBA (Virtual University of Pakistan)
Learning Objectives:
Describe the structure and function of taste buds.
Describe the relationship between the taste threshold and taste index of common substances.
Explain the chemical basis and signal transduction of taste perception for each type of primary taste sensation.
Recognize different abnormalities of taste perception and their causes.
Key Topics:
Significance of Taste Sensation:
Differentiation between pleasant and harmful food
Influence on behavior
Selection of food based on metabolic needs
Receptors of Taste:
Taste buds on the tongue
Influence of sense of smell, texture of food, and pain stimulation (e.g., by pepper)
Primary and Secondary Taste Sensations:
Primary taste sensations: Sweet, Sour, Salty, Bitter, Umami
Chemical basis and signal transduction mechanisms for each taste
Taste Threshold and Index:
Taste threshold values for Sweet (sucrose), Salty (NaCl), Sour (HCl), and Bitter (Quinine)
Taste index relationship: Inversely proportional to taste threshold
Taste Blindness:
Inability to taste certain substances, particularly thiourea compounds
Example: Phenylthiocarbamide
Structure and Function of Taste Buds:
Composition: Epithelial cells, Sustentacular/Supporting cells, Taste cells, Basal cells
Features: Taste pores, Taste hairs/microvilli, and Taste nerve fibers
Location of Taste Buds:
Found in papillae of the tongue (Fungiform, Circumvallate, Foliate)
Also present on the palate, tonsillar pillars, epiglottis, and proximal esophagus
Mechanism of Taste Stimulation:
Interaction of taste substances with receptors on microvilli
Signal transduction pathways for Umami, Sweet, Bitter, Sour, and Salty tastes
Taste Sensitivity and Adaptation:
Decrease in sensitivity with age
Rapid adaptation of taste sensation
Role of Saliva in Taste:
Dissolution of tastants to reach receptors
Washing away the stimulus
Taste Preferences and Aversions:
Mechanisms behind taste preference and aversion
Influence of receptors and neural pathways
Impact of Sensory Nerve Damage:
Degeneration of taste buds if the sensory nerve fiber is cut
Abnormalities of Taste Detection:
Conditions: Ageusia, Hypogeusia, Dysgeusia (parageusia)
Causes: Nerve damage, neurological disorders, infections, poor oral hygiene, adverse drug effects, deficiencies, aging, tobacco use, altered neurotransmitter levels
Neurotransmitters and Taste Threshold:
Effects of serotonin (5-HT) and norepinephrine (NE) on taste sensitivity
Supertasters:
25% of the population with heightened sensitivity to taste, especially bitterness
Increased number of fungiform papillae
Prix Galien International 2024 Forum ProgramLevi Shapiro
June 20, 2024, Prix Galien International and Jerusalem Ethics Forum in ROME. Detailed agenda including panels:
- ADVANCES IN CARDIOLOGY: A NEW PARADIGM IS COMING
- WOMEN’S HEALTH: FERTILITY PRESERVATION
- WHAT’S NEW IN THE TREATMENT OF INFECTIOUS,
ONCOLOGICAL AND INFLAMMATORY SKIN DISEASES?
- ARTIFICIAL INTELLIGENCE AND ETHICS
- GENE THERAPY
- BEYOND BORDERS: GLOBAL INITIATIVES FOR DEMOCRATIZING LIFE SCIENCE TECHNOLOGIES AND PROMOTING ACCESS TO HEALTHCARE
- ETHICAL CHALLENGES IN LIFE SCIENCES
- Prix Galien International Awards Ceremony
TEST BANK for Operations Management, 14th Edition by William J. Stevenson, Ve...kevinkariuki227
TEST BANK for Operations Management, 14th Edition by William J. Stevenson, Verified Chapters 1 - 19, Complete Newest Version.pdf
TEST BANK for Operations Management, 14th Edition by William J. Stevenson, Verified Chapters 1 - 19, Complete Newest Version.pdf
These lecture slides, by Dr Sidra Arshad, offer a quick overview of physiological basis of a normal electrocardiogram.
Learning objectives:
1. Define an electrocardiogram (ECG) and electrocardiography
2. Describe how dipoles generated by the heart produce the waveforms of the ECG
3. Describe the components of a normal electrocardiogram of a typical bipolar leads (limb II)
4. Differentiate between intervals and segments
5. Enlist some common indications for obtaining an ECG
Study Resources:
1. Chapter 11, Guyton and Hall Textbook of Medical Physiology, 14th edition
2. Chapter 9, Human Physiology - From Cells to Systems, Lauralee Sherwood, 9th edition
3. Chapter 29, Ganong’s Review of Medical Physiology, 26th edition
4. Electrocardiogram, StatPearls - https://www.ncbi.nlm.nih.gov/books/NBK549803/
5. ECG in Medical Practice by ABM Abdullah, 4th edition
6. ECG Basics, http://www.nataliescasebook.com/tag/e-c-g-basics
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Formulation and invivo evaluation of mucoadhesive microspheres embedded clerodendrum phlomidis (cp) extract for prolonged antidiabetic activity
1. Jesindha B K et al, ICJPIR 2017, 4(1), 201-206
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Available online at www.icjpir.com ISSN: 2349-5448
Intercontinental journal of pharmaceutical
Investigations and Research
ICJPIR |Volume 4 | Issue 1 | Jan – Mar- 2017 Research Article
Formulation and invivo evaluation of mucoadhesive microspheres
embedded clerodendrum phlomidis (cp) extract for prolonged antidiabetic
activity
K. Jesindha Beyatricks*, S. Kavimani2
, Habeela Jainab3
, ShivaKumar3
, Bindhu3
*Research scholar, PRIST University, Thanjavur, Tamilnadu
1
Professor, Mother Therasa Post Graduate Institute of Health Sciences, Pondicherry
2
Hillside College of Pharmacy & Research Centre, Bangalore
Corresponding Author: K. Jesindha Beyatricks
Email: jolyjesi@gmail.com
ABSTRACT
In this study an attempt was made to prepare mucoadhesive microcapsules of Clerodendrum phlomidis extract using
alginate polymers for prolonged release. Encapsulation of extract into sodium alginate polymer was done by ionic-
gelation technique. In vivo testing of the mucoadhesive microcapsules in diabetic albino rats demonstrated significant
antidiabetic effect of extract. The hypoglycemic effect obtained by mucoadhesive microcapsules was for more than
16 h whereas plain CP extract produced an antidiabetic effect for only 4 h suggesting that mucoadhesive
microcapsules are a valuable system for the long term delivery of CP extract. In-vivo data obtained over a 120-h
period indicate that CP extract loaded alginate microspheres from batch F7 showed the better glycemic control than
control and a commercial brand of the drug.
Keyword: Mucoadhesive, Ionic gelation technique, Sodium Alginate, Microspheres
INTRODUCTION
Diabetes mellitus is a most common metabolic
disorder of human beings. It is global in
distribution affecting 2 to 6 percent population of
the World [1]. Clerodendrum phlomidis is well
known drug in ayurveda and siddha medicine for
treatment of diabetics. Clerodendrum phlomoidis L.
(Family: Verbenaceae) is commonly known as
Thazhu thaazhai in Tamil and Arni in Hindi [2].
β-Sitosterol is widely distributed in the plant
kingdom and found in Clerodendrum phlomidis [3].
The biochemical effects of cholesterol differ from
those of phytosterols. The major phytosterol
sources in the human diet are vegetable oils,
cereals, fruits, and vegetables [4]. Authors have
reported that β-sitosterol inhibits the growth of HT-
29 human colon cancer cells and induces apoptosis
of human prostate cancer cells. β-Sitosterol also
has the potential to function as an anti-cancer agent
for controlling colon carcinogenesis [5]. Moreover,
2. Jesindha B K et al, ICJPIR 2017, 4(1), 201-206
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β-sitosterol possessed potential anti-diabetic and
anti-oxidant activities in streptozotocin-induced
hyperglycemia models reported [6]. In addition to
their cholesterol-lowering effect, β-sitosterol have
anti-inflammatory, antipyretic, antineoplastic,
immune-modulating and blood sugar-controlling
effects.
In humans, <10% of the total dietary β-
sitosterol consumed is absorbed in the intestine. In
rats, ∼4% of β-sitosterol is absorbed. Human
dietary intake ranges from 40 to 400 mg/d. In
Western diets, phytosterol intake is low, ∼80 mg/d.
Due to poor solubility and bioavailability of
phytosterols, the serum cholesterol-lowering effect
of phytosterols is not consistent, and high dosages
(up to 25 to 50 g/d) are required for efficacy [14].
Plasma concentrations of β-sitosterol ranged
from 0.30 to 1.02 mg/100 ml plasma. Plasma levels
were raised slightly when intakes were increased
greatly, and on fixed intakes they were constant
from week to week. The percentage of esterified β-
sitosterol in the plasma was the same as for
cholesterol. However, the rate of esterification of b-
sitosterol was slower than that for cholesterol. β-
sitosterol were much shorter than for cholesterol
and excreted in bile as free sterol; this excretion
was more rapid than that of cholesterol [7].
Novel drug delivery system has shown improved
pharmacokinetic and pharmacological properties of
phytoconstituents parameters which can be
advantageously be used in the treatment of the
diabetes mellitus [8].
Recently, dosage forms that can precisely
control the release rates and target drugs to a
specific body site have made an enormous impact
in the formulation and development of novel drug
delivery systems [9]. Microparticles are defined as
spherical polymeric particles. These microparticles
are constitutes an important part of these drug
delivery systems, by virtue of their small size and
efficient carrier characteristics [10]. However, the
success of these novel microparticles is limited due
to their short residence time at the site of
absorption. It would, therefore, be advantageous to
have means for providing an intimate contact of the
drug delivery system with the absorbing
membranes. It can be achieved by coupling
bioadhesion characteristics to microparticles and
developing novel delivery systems referred to as
―bioadhesive microparticles‖. Bioadhesive
microparticles include microspheres and
microcapsules (having a core of the drug) of 1–
1000 μm in diameter and consisting either entirely
of a bioadhesive polymer or having an outer
coating of it, respectively. Bioadhesive
microparticles have advantages such as efficient
absorption and enhanced bioavailability of drugs
owing to their high surface to volume ratio, a much
more intimate contact with the mucus layer, and
specific targeting of drugs to the absorption site
[11].
Preparation of Mucoadhesive Microcapsules
containing CP extract
Cross-linking technique [12]
Mucoadhesive microcapsules containing CP
extract were prepared employing sodium alginate
in combination with three mucoadhesive
polymers—sodium CMC, carbopol 934Pand HPMC
as coat materials. Orifice-ionic gelation method
was employed to prepare the microcapsules.
Sodium alginate was dissolved in 50 ml of purified
water to form a homogenous polymer solution. The
active substance CP extract was added to the
polymer solution (in a ratio of CP extract: polymer
solution 1:1) and sonicated to form a viscous
dispersion. The aqueous phase was taken in a
syringe (No. 20) and extruded dropwise in 100 ml
of the external oily phase (liquid paraffin)
containing 0.2% Span®
80 and stirring was carried
out using propeller stirrer (Remi, India) at 1000
rpm. After 15 min, 2.0 ml of calcium chloride was
added drop-by-drop to the emulsion and stirring
was continued. The emulsion was stirred for 1 h
and then centrifuged at 2000 rpm for 15 min. The
microspheres were separated by filtration and
washed with petroleum ether followed by water to
remove the paraffin and excess cross linking agent.
The dried microspheres were then stored at 25°C.
Sodium alginate microspheres were dispersed in
5 ml of 1.5 wt% mucoadhesive polymers—sodium
CMC, carbopol 934P and HPMC in buffer solution
(pH 6.8) for 1 h under stirring of 300 rpm as the
second-step solidification. Finally, the
mucoadhesive polymers coated sodium alginate
microspheres and then dried at 40ºC for 6 Hrs.
3. Jesindha B K et al, ICJPIR 2017, 4(1), 201-206
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Table No. 1 Formulations for CP extract loaded alginate microspheres
S.No. Ingredients (% w/w) F1 F2 F3 F4 F5 F6 F7 F8
1 CP extract 5 5 5 5 5 5 5 5
2 Alginate 0.75 1.5 1.5 1.5 1.5 1.5 1.5 1.5
3 Calcium chloride 2 2 2 2 2 2 2 2
Cross linking time 30 min 30 min 15 min 30 min 45 min 30 min 30 min 30 min
4 Sodium CMC - - - - - 1.5 - -
5 Carbopol 934P - - - - - - 1.5 -
6 HPMC - - - - - - - 1.5
In Vivo study [13]
The animals used for in vivo experiments were
adult Wistar male albino rats (230-250 g) from
Central Animal House of C.L.Baid Metha college
of pharmacy, Chennai, India
(IAEC/XLVI/02/CLB/MCP/2015). The animals
were kept under standard laboratory conditions,
temperature at 25±1º
C and relative humidity (55 ±
5%). The animals were housed in polypropylene
cages, four per cage, with free access to standard
laboratory diet (Lipton feed, Mumbai, India) and
water ad libitum. Guidelines of Institutional
Animal Ethics Committee were followed for in vivo
experiments.
Induction of diabetes and experimental
groups
Diabetes was induced in rats by intraperitoneal
injection of 50 mg ⁄ kg streptozotocin (STZ; Sigma,
St Louis, MO, USA) dissolved in 0.1 mol ⁄L
sodium citrate buffer, pH 4.5. The induction of
diabetes was evaluated 72 h later and rats with
blood glucose levels >250 mg ⁄ dL were used in
subsequent experiments. The nine experimental
groups (n = 9 in each) used in the present study
were as follows.
1. Group I, a vehicle-treated diabetics control group.
2. Group II, diabetic rats treated with CP extracts
1200 mg ⁄ kg per day.
3. Group III, diabetic rats treated with β-sitosterol
10 mg ⁄ kg per day (BS was dissolved in 0.5 mL
olive oil).
4. Group IV, diabetic rats administered
mucoadhesive microcapsules of CP extract at a
dose equivalent to BS 10 mg ⁄ kg per day.
5. Group V, diabetic rats treated with glibenclamide
0.3 mg ⁄ kg per day.
Blood samples were withdrawn by the retro
orbital puncture at predetermined time at 1 hour
intervals up to 24 h, and were analyzed for blood
glucose by glucose oxidase and peroxidise
(GOD/POD) method using commercial glucose kit.
Statistical analysis
Statistical analyses were accomplished using
GraphPad Prism statistical package. Student’s t-test
was used to determine the statistically significant
differences between the results. Results with P
values <0.05 were considered statistically
significant.
Relative pharmacological availability (PA%)
was calculated by using following equation. The
same equation was used in calculation of the
relative bioavailability (F%); however, the AUC
values were substituted instead of the AAC values.
4. Jesindha B K et al, ICJPIR 2017, 4(1), 201-206
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Where, PA is the pharmacological availability
of the CP extract. AAC oral suspension and AACoral
microcapsules are area above the curve of reduction in
blood glucose levels for oral and s.c. administration
respectively. The average standard deviations of
blood glucose levels measured in the six
experimental rats are plotted versus time and the
trapezoid rule is used to calculate the AAC.
RESULTS & DISCUSSION
Formulation of cp extract loaded
microspheres
The formulations were compared for their
release, microencapsulation efficacy, mucoadhesive
property by comparing the concentration of sodium
alginate and mucoadhesive polymers. The
percentage of extract entrapment increased with
increase in polymer concentration. This was
attributed to physical interaction and/or
entanglement of the greater amount of extract
inside the intricate cross-linked calcium alginate
gel network.
One of the ways of changing drug release from
the microspheres is to change the crosslinking
density of the matrix by employing various time of
exposure to crosslinking agent. The effect of the
exposure time to calcium chloride on the release
rate of β-sitosterol has been investigated by varying
the time of exposure to calcium chloride as 15 - 45
min. The results were given in Fig.1, which clearly
indicated that increasing exposure time to CaCl2
decreased the cumulative release of β-sitosterol.
The β-sitosterol release was found more slowly
with the percentage increase of cross-linker
concentrations (CaCl2) in cross-linking solutions,
which can be attributed by high degree of cross-
linking by higher CaCl2 concentration might slower
the drug release from highly cross-linked
microspheres. The higher concentration of cross-
linker used for the preparation of ionically gelled
alginate microspheres might produce a rigid
polymeric structure due to contraction of
microvoids, which could facilitate poor entry of
dissolution medium into the calcium ion induced
ionically gelled extract-loaded alginate polymer
and slow the drug release.
Invivo study
In vivo testing of the mucoadhesive
microcapsules of CP extract in diabetic albino rats
demonstrated significant prolonged antidiabetic
effect compared to plain CP extract. The
percentage reduction of blood glucose level
(pharmacological response) after β-sitosterol at 1 h
time period was found to be (44±4%) and the effect
was maintained only for 6 h. These results are in
good agreement with the findings of an earlier
report.
The hypoglycemic effect obtained by F7
mucoadhesive microcapsules was for more than 16 h
whereas plain CP extract produced an antidiabetic
effect for only 4 h suggesting that mucoadhesive
microcapsules are a valuable system for the long term
delivery of CP extract. Prolonged release formulation
of CP extract is significantly more effective than the
immediate release formulation in reducing blood
glucose levels and side effects.
5. Jesindha B K et al, ICJPIR 2017, 4(1), 201-206
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Fig.No.1 Hypoglycemic effect of control, Beta sitosterol, loaded microspheres, CP extract & standard
Table No. 2 Main pharmacokinetic parameters for plasma glucose levels after administration of
different formulations to rats
Parameters Plain CP extract CP extract mucoadhesive micrsocapsules
CP extract dose (mg) 200 200
Minimum glucose level in % of the initial level 62.13±3.44 75.04±2.76
Time point of minimum glucose level (h) 2 6
AAC0→24 368±7.4 925±5.2*
Relative pharmacological efficacy (PA%) - 2.51±4.1*
Results are expressed as (mean±SD, n = 6). * P<0.05
Pharmacokinetic parameters of glucose levels
after dosing are shown in Table 2. The
mucoadhesive microcapsules of CP extract
produced minimum glucose level 55.21±3.16 % at
6 h and the reduction of glucose levels was
maintained over a prolonged period of time. This
result may be attributed to the improved permeation
in gatrointestinal tract using microspheres carrier
system, which keeps the extract for longer time in
absorption site. Orally administered plain CP
extract solution at the same dose showed slight
reduction in blood glucose level due to poor
permeability in GIT. The relative pharmacological
efficacy for mucoadhesive microcapsules of CP
extract (2.51±4.1%) was almost three-fold higher
than the efficacy of the plain CP extract.
CONCLUSION
The microcapsules containing CP extract
consisting of mucoadhesive polymer alginate could
be prepared by an ionic gelation process. The
microcapsules exhibited good mucoadhesive
properties in an in vitro test. The in vivo study
demonstrated significant blood glucose reducing
activity of mucoadhesive microcapsules of CP
extract. Developed mucoadhesive microcapsules
are suitable for prolonged effect after oral
administration of CP extract.
0
20
40
60
80
100
120
0 1 2 4 6 8 12 16 20 24
PlasmaGlucoseConc(%ofinitial)
Time (Hrs)
control
betasitosterol
10mg/kg
Mucoadhesive
microcapsule of
Methanolic CP
extract( 200mg/kg)
CP extract (200
mg/kg)
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