This document summarizes the development and evaluation of an in situ gelling system for the treatment of periodontitis using tinidazole as the model drug. Tinidazole was incorporated into gellan gum and poloxamer 407 polymer matrices using a 32 full factorial design to optimize the formulation variables. Nine formulations were developed varying the concentration of gellan gum (0.5-1.5% w/v) and poloxamer 407 (10-20% w/v). The formulations were characterized for appearance, gelling capacity, pH, viscosity, gelation temperature, drug content, syringeability and in vitro drug release. The optimized formulation with maximum desirability contained 0.5% w/
This topic include all the drugs that are locally applied in periodontal pocket so that their levels in GCF should be more than blood.
Advantages:
Can attain higher concentrations at base of pocket
Can use drugs that are not suitable for systemic administration
Patient compliance is not required
Alternative for patients predisposed to adverse drug reactions from systemic administration.
Reduced risk for drug resistant microbe development
Lower total drug dose
INDICATIONS:
As an adjunct to mechanical therapy in pockets of 5 mm or greater depth
In patients who are systemically compromised & cannot undergo periodontal flap surgery
Localized recurrent pockets with supportive periodontal therapy
In refractory periodontitis (that is resistant to treatment)
This is an Engg Biotechnology project based on medicinal plant i.e singapore cherry or jamaican cherry tree (scientific name Muntingia calabure ), we did in 2013 in GMIT college Davangere, karanataka, India. i have complete project detail what we did..,
This topic include all the drugs that are locally applied in periodontal pocket so that their levels in GCF should be more than blood.
Advantages:
Can attain higher concentrations at base of pocket
Can use drugs that are not suitable for systemic administration
Patient compliance is not required
Alternative for patients predisposed to adverse drug reactions from systemic administration.
Reduced risk for drug resistant microbe development
Lower total drug dose
INDICATIONS:
As an adjunct to mechanical therapy in pockets of 5 mm or greater depth
In patients who are systemically compromised & cannot undergo periodontal flap surgery
Localized recurrent pockets with supportive periodontal therapy
In refractory periodontitis (that is resistant to treatment)
This is an Engg Biotechnology project based on medicinal plant i.e singapore cherry or jamaican cherry tree (scientific name Muntingia calabure ), we did in 2013 in GMIT college Davangere, karanataka, India. i have complete project detail what we did..,
GC-MS analysis of phytocomponents in Vernonia amygdalina.Del leaves and its c...iosrjce
IOSR Journal of Agriculture and Veterinary Science (IOSR-JAVS) is a double blind peer reviewed International Journal edited by the International Organization of Scientific Research (IOSR). The journal provides a common forum where all aspects of Agricultural and Veterinary Sciences are presented. The journal invites original papers, review articles, technical reports and short communications containing new insight into any aspect Agricultural and Veterinary Sciences that are not published or not being considered for publication elsewhere.
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.
The IOSR Journal of Pharmacy (IOSRPHR) is an open access online & offline peer reviewed international journal, which publishes innovative research papers, reviews, mini-reviews, short communications and notes dealing with Pharmaceutical Sciences( Pharmaceutical Technology, Pharmaceutics, Biopharmaceutics, Pharmacokinetics, Pharmaceutical/Medicinal Chemistry, Computational Chemistry and Molecular Drug Design, Pharmacognosy & Phytochemistry, Pharmacology, Pharmaceutical Analysis, Pharmacy Practice, Clinical and Hospital Pharmacy, Cell Biology, Genomics and Proteomics, Pharmacogenomics, Bioinformatics and Biotechnology of Pharmaceutical Interest........more details on Aim & Scope).
All manuscripts are subject to rapid peer review. Those of high quality (not previously published and not under consideration for publication in another journal) will be published without delay.
DOI: 10.21276/ijlssr.2016.2.3.16
ABSTRACT- The present research article was described about the hypotriglycerdemic activity of Withania coagulans
bud extract. Withania coagulans Dunal belonging to the family Solanaceae is a small bush which is widely spread in
South Asia. The biological activity of with anolides from Withania coagulans has antihyperglycaemic activity and the
plant is commonly called as Indian cheese maker due to the milk coagulation characteristics of the bud. The present study
was to investigate preliminary studies shows satisfactory result. The chromatographic studies like TLC, HPTLC and
HPLC show good spot. HPTLC shows maximum height and area of 18.83%.HPLC shows maximum peak at 1.867
minutes having area coverage of 87.4%.The free radical scavenging activity of chloroform fraction (CF) of a crude drug
shows 510μg/ml of scavenging activity. The IC50 value for MTT assay was found to be 84.7μg/ml. The GLUT4 study
shows significant uptake of glucose. PPAR gamma activity regulation of glucose disposal and insulin sensitivity in the
skeletal muscles shows concentration dependence response using standard Pioglitazone. The bud of Withania coagulants
will be a promising medicine for more ailments.
Key-words- Withania coagulants, Hypotriglycerdemic, HPLC, HPTLC, GLUT-4, MTT assay
In recent years, there is increased number of active pharmaceutical ingredients with high therapeutic activity, but very low water solubility. Thus, a great challenge for pharmaceutical technology is to manufacture successful formulations and efficient drug delivery systems to overcome these dissolution problems. In case of poorly water soluble drugs, dissolution is the rate limiting step in the process of drug absorption. So, bioavailability problems are associated with extremely hydrophobic drugs (aqueous solubility < 0.1 mg / ml at 370C)
In Vivo Assay of Analgesic Activity of Methanolic and Petroleum Ether Extract...IOSR Journals
Abstract: Aims: The main objective of this work was to observe the analgesic activity of Vitex negundo (leaves) on mice. Study Design: Present study was designed to isolate pure compounds as well as to observe pharmacological activities of the isolated pure compounds with crude extracts of the plant Vitex negundo (leaves). The study protocol consisted of the following steps:
Cold extraction at room temperature of the whole plant with distilled methanol.
Filtration of the crude petroleum ether and methanolic extracts by using the Markin cotton cloth and subsequently through the filter paper and solvent evaporation.
Screening of analgesic activity of crude extracts on Swiss Albino mice.
Place and Duration of Study: The study of analgesic activity of Vitex negundo (leaves) on mice was take place in the laboratory of Department of Pharmacy, Southeast University, Bangladesh, between January 2011 and July 2011. Methodology: The analgesic activity was investigated for its peripheral pharmacological actions using acetic acid-induced writhing test in mice. Results: The methanolic and petroleum ether extracts, at the dose of 200 mg/kg body weight, displayed 82.60% & 74.66% pain inhibition which was significant (p<0.001) compared to control. These results indicate that the extracts possess strong analgesic activity. Conclusion: The present study tends to suggest the analgesic activities of the crude methanolic and petroleum ether extract of the leaves of Vitex negundo and justify its use in folkloric remedies
Membrane Stabilizing And Antimicrobial Activities Of Caladium Bicolor And Che...IOSR Journals
The crude methanol extracts of whole plant of Caladium bicolor (Aiton) Vent. and leaf of Chenopodium album L. as well as their pet-ether, carbon tetrachloride, chloroform and aqueous soluble fractions were evaluated for membrane stabilizing and antimicrobial activities. At concentration 1.0 mg/ml, the carbon tetrachloride soluble fraction of C. bicolor inhibited 43.92±1.63% and 38.08±0.83 % hypotonic solution and heat induced haemolysis of RBCs, respectively. Among the extractives of C. album, the aqueous soluble fraction inhibited 47.11±0.49 % and 36.73±0.76 % hypotonic solution and heat induced haemolysis of RBCs as compared to 72.79 % and 42.12 % by acetyl salicylic acid (0.10 mg/ml), respectively. C. bicolor test samples demonstrated zone of inhibition ranging from 6.0 to 20.0 mm. The chloroform soluble fraction showed the highest zone of inhibition (20.0 mm) against Staphylococcus aureus. The test samples of C. album displayed zone of inhibition ranging from 7.0 to 13.0 mm. The highest zone of inhibition (13.0 mm) was showed by the chloroform soluble fraction against Salmonella paratyphi
GC-MS analysis of phytocomponents in Vernonia amygdalina.Del leaves and its c...iosrjce
IOSR Journal of Agriculture and Veterinary Science (IOSR-JAVS) is a double blind peer reviewed International Journal edited by the International Organization of Scientific Research (IOSR). The journal provides a common forum where all aspects of Agricultural and Veterinary Sciences are presented. The journal invites original papers, review articles, technical reports and short communications containing new insight into any aspect Agricultural and Veterinary Sciences that are not published or not being considered for publication elsewhere.
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.
The IOSR Journal of Pharmacy (IOSRPHR) is an open access online & offline peer reviewed international journal, which publishes innovative research papers, reviews, mini-reviews, short communications and notes dealing with Pharmaceutical Sciences( Pharmaceutical Technology, Pharmaceutics, Biopharmaceutics, Pharmacokinetics, Pharmaceutical/Medicinal Chemistry, Computational Chemistry and Molecular Drug Design, Pharmacognosy & Phytochemistry, Pharmacology, Pharmaceutical Analysis, Pharmacy Practice, Clinical and Hospital Pharmacy, Cell Biology, Genomics and Proteomics, Pharmacogenomics, Bioinformatics and Biotechnology of Pharmaceutical Interest........more details on Aim & Scope).
All manuscripts are subject to rapid peer review. Those of high quality (not previously published and not under consideration for publication in another journal) will be published without delay.
DOI: 10.21276/ijlssr.2016.2.3.16
ABSTRACT- The present research article was described about the hypotriglycerdemic activity of Withania coagulans
bud extract. Withania coagulans Dunal belonging to the family Solanaceae is a small bush which is widely spread in
South Asia. The biological activity of with anolides from Withania coagulans has antihyperglycaemic activity and the
plant is commonly called as Indian cheese maker due to the milk coagulation characteristics of the bud. The present study
was to investigate preliminary studies shows satisfactory result. The chromatographic studies like TLC, HPTLC and
HPLC show good spot. HPTLC shows maximum height and area of 18.83%.HPLC shows maximum peak at 1.867
minutes having area coverage of 87.4%.The free radical scavenging activity of chloroform fraction (CF) of a crude drug
shows 510μg/ml of scavenging activity. The IC50 value for MTT assay was found to be 84.7μg/ml. The GLUT4 study
shows significant uptake of glucose. PPAR gamma activity regulation of glucose disposal and insulin sensitivity in the
skeletal muscles shows concentration dependence response using standard Pioglitazone. The bud of Withania coagulants
will be a promising medicine for more ailments.
Key-words- Withania coagulants, Hypotriglycerdemic, HPLC, HPTLC, GLUT-4, MTT assay
In recent years, there is increased number of active pharmaceutical ingredients with high therapeutic activity, but very low water solubility. Thus, a great challenge for pharmaceutical technology is to manufacture successful formulations and efficient drug delivery systems to overcome these dissolution problems. In case of poorly water soluble drugs, dissolution is the rate limiting step in the process of drug absorption. So, bioavailability problems are associated with extremely hydrophobic drugs (aqueous solubility < 0.1 mg / ml at 370C)
In Vivo Assay of Analgesic Activity of Methanolic and Petroleum Ether Extract...IOSR Journals
Abstract: Aims: The main objective of this work was to observe the analgesic activity of Vitex negundo (leaves) on mice. Study Design: Present study was designed to isolate pure compounds as well as to observe pharmacological activities of the isolated pure compounds with crude extracts of the plant Vitex negundo (leaves). The study protocol consisted of the following steps:
Cold extraction at room temperature of the whole plant with distilled methanol.
Filtration of the crude petroleum ether and methanolic extracts by using the Markin cotton cloth and subsequently through the filter paper and solvent evaporation.
Screening of analgesic activity of crude extracts on Swiss Albino mice.
Place and Duration of Study: The study of analgesic activity of Vitex negundo (leaves) on mice was take place in the laboratory of Department of Pharmacy, Southeast University, Bangladesh, between January 2011 and July 2011. Methodology: The analgesic activity was investigated for its peripheral pharmacological actions using acetic acid-induced writhing test in mice. Results: The methanolic and petroleum ether extracts, at the dose of 200 mg/kg body weight, displayed 82.60% & 74.66% pain inhibition which was significant (p<0.001) compared to control. These results indicate that the extracts possess strong analgesic activity. Conclusion: The present study tends to suggest the analgesic activities of the crude methanolic and petroleum ether extract of the leaves of Vitex negundo and justify its use in folkloric remedies
Membrane Stabilizing And Antimicrobial Activities Of Caladium Bicolor And Che...IOSR Journals
The crude methanol extracts of whole plant of Caladium bicolor (Aiton) Vent. and leaf of Chenopodium album L. as well as their pet-ether, carbon tetrachloride, chloroform and aqueous soluble fractions were evaluated for membrane stabilizing and antimicrobial activities. At concentration 1.0 mg/ml, the carbon tetrachloride soluble fraction of C. bicolor inhibited 43.92±1.63% and 38.08±0.83 % hypotonic solution and heat induced haemolysis of RBCs, respectively. Among the extractives of C. album, the aqueous soluble fraction inhibited 47.11±0.49 % and 36.73±0.76 % hypotonic solution and heat induced haemolysis of RBCs as compared to 72.79 % and 42.12 % by acetyl salicylic acid (0.10 mg/ml), respectively. C. bicolor test samples demonstrated zone of inhibition ranging from 6.0 to 20.0 mm. The chloroform soluble fraction showed the highest zone of inhibition (20.0 mm) against Staphylococcus aureus. The test samples of C. album displayed zone of inhibition ranging from 7.0 to 13.0 mm. The highest zone of inhibition (13.0 mm) was showed by the chloroform soluble fraction against Salmonella paratyphi
Dissolution Enhancement of BCS Class 4 Dssrugs Using Quality by Design Approa...inventionjournals
Solid dispersion is one of the vastly accepted and practically economical processes in bioavailability enhancement study. The present investigation deals mostly with increase in solubility and dissolution rate of BCS class 4 drugs for enhancement of oral bioavailability. For the same solid dispersion were prepared and analyzed for appropriate concentration of drug polymer ratio by phase solubility analysis. The solvent evaporation study widely accepted due to its efficient solid dispersion in lesser efforts. The study designs were prepared with specific concentration of drug and polymer ratio with the help of high throughput model i.e. Central Composite Design (by Design Expert trial copy) by specific design of experiment with full factorial design (DOE). The fixed variables were concentration of polymers and dependant variables were dissolution and permeability across bio-membrane in in-vitro model. The prepared dispersion investigated for dissolution and permeability improvement using USP Type II apparatus and modified everted gut sac model which leads to improvement of quality of whole formulation with Quality by design efficiently.
Design and Development of Effervescent Floating Tablet Dapagliflozinijtsrd
The objective of the present study was to formulate and evaluate Effervescent Floating Tablet of Dapagliflozin for the treatment of antidepressant agent. Tablets were prepared by direct compression using directly compressible polymers such as HPMC K4M, and Carbopol 934 were evaluated for drug excipient compatibility, density, buoyancy test, swelling study, drug content and In Vitro release profile. Sodium bicarbonate and citric acid were used producing effervescent base for buoyancy of tablets. Analysis of drug release from tablet indicates drug release by zero order, first order rate kinetics. No significant change was observed in physical appearance, drug content, floatability or in vitro dissolution pattern after storage at 450C 750C RH for three months. Samadhan Mali | Shweta Gedam | Swati Talele | Anil Jadhav "Design and Development of Effervescent Floating Tablet Dapagliflozin" Published in International Journal of Trend in Scientific Research and Development (ijtsrd), ISSN: 2456-6470, Volume-4 | Issue-5 , August 2020, URL: https://www.ijtsrd.com/papers/ijtsrd31674.pdf Paper Url :https://www.ijtsrd.com/pharmacy/pharmaceutics/31674/design-and-development-of-effervescent-floating-tablet-dapagliflozin/samadhan-mali
ABSTRACT The purpose of this study was to prepare and evaluate immediate release itraconazole pellets and comprehensive studies of the same. The itraconazole pellets is prepared using fluid bed processer with different concentration of HPMC (Hydroxy Propyl Methyl Cellulose). The physicochemical compatibility of the drug and the excipient studied by differential scanning calorimetry. The prepared pellets were physically evaluated with size, shape, bulk density, tapped density, compressibility index, hausners ratio, angle of repose, sieve analysis, surface roughness, density, moisture content, assay and drug release etc. The in vitro drug release profile from pellets shows that all the formulation release more than 75% drug within 90min. Optimized formulations were found to have HPMC concentration 2-5% of total weight of pellets to maximize high-quality surface, desired release, and size distribution within the range. These results indicate that pellets containing 10 % HPMC of total weight of pellets give better quality of itraconazole pellets for immediate release. Key Words: Itraconazole, Hydroxyl propyl methyl cellulose and Immediate release.
Solubility enhancement technique of BCS Class II drug by Solvent EvaporatiomKaustav Dey
I am very happy to share with you my B.Pharm Final semester Presentation. The topic of the presentation was “SOLUBILITY ENHANCEMENT TECHNIQUE OF BCS CLASS II DRUG BY SOLVENT EVAPORATION TECHNIQUE – FORMULATION & EVALUATION" which i have done under the esteemed guidance of Dr. Goutam Kumar Jena. It was a great experience to deliver this topic infront of the expert jury. I would also like thank all my teammates especially Agniv Masanta for his efforts. I hope everyone of you will like presentation and the research and efforts behind it.Thank you for giving your precious time. #research #science #thankyou #experience #share
Formulation, Development and Evaluation of Fast Disintegrating Tablet of Piro...ijtsrd
The solubility behavior of drugs remains one of the most exigent aspects in formulation development. With the advent of combinatorial chemistry and high throughput screening, the number of poorly water soluble compounds has dramatically increased. Among all the newly discovered chemical entities, about 40 45 drugs fail to reach market due to their poor water solubility. Because of solubility problem, bioavailability of drugs gets affected and hence solubility enhancement becomes necessary. In present study the attempts have been made to increase the dissolution of BCS class 2 drug Piroxicam using hydrophilic polymers namely polyethylene glycol PEG 6000 and sodium lauryl sulphate as a surfactant by using solid dispersion technique. In solid dispersion microwave induced solid dispersion and conventional fusion method is compared. Drug polymer complex was prepared using batch method. Maximum dissolution rate was obtained of the complex prepared from Piroxicam PEG6000 SLS . A successful solubility enhancement of drug complex was confirmed by taking drug release in phosphate buffer pH 6.8. The drug was characterized according to different compendial methods, on the basis of identification by UV spectroscopy, organoleptic properties and other tests. After that among the all formulation batches, solid dispersion F16 was selected for further tablet formulation batches, nine formulations were developed and studied. The values of pre compression parameters was evaluated, results were within prescribed limits and indicated good free flowing properties. The data obtained of post compression parameters such as weight variation, hardness, friability, wetting time, water absorption ratio, content uniformity, disintegration time and dissolution was found to superior over conventional formulation. The F9 batch with disintegrating time 10 ± 0.52 second and dissolution 93.20 ± 0.61 was selected as optimized formulation and was found superior over other formulation. Batch F9 was also subjected to stability studies for three months and was tested for its disintegrating time, drug contents and dissolution behavior monthly. F9 formulation after stability study was found to be stable. Mr. Yennuwar Dhiresh Pramod | Mr. Sujit Kakade | Mrs. Trusha Shangrapawar | Dr. Ashok Bhosale "Formulation, Development and Evaluation of Fast Disintegrating Tablet of Piroxicam using Solid Dispersion Technique" 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/ijtsrd50422.pdf Paper URL: https://www.ijtsrd.com/pharmacy/pharmaceutics/50422/formulation-development-and-evaluation-of-fast-disintegrating-tablet-of-piroxicam-using-solid-dispersion-technique/mr-yennuwar-dhiresh-pramod
PREPARATION AND IN-VITRO EVALUATION OF ITRACONAZOLE LOADED NANOSPONGES FOR T...Mahewash Sana Pathan
Itraconazole is an imidazole derivative and used for the treatment of local and systemic fungal infections. It is a BCS Class II drug having very low solubility in water i.e. 1-4ng/ml. The oral use of Itraconazole is not much recommended as it has many side effects. The present research has been undertaken with the aim to develop a topical hydrogel formulation of Itraconazole loaded nanosponges to increase the solubility, permeability and stability of itraconazole. Itraconazole loaded nanosponge was prepared by emulsion solvent diffusion method by using different concentrations of ethyl cellulose as a polymer, Polyvinyl alcohol as surfactant and dichloromethane as cross linking agent. Physical characteristics of the nanosponges as well as the drug entrapment efficiency, percentage drug content, Percent yield, drug polymer compatibility, solubility studies of the nanosponges were investigated. Particle size analysis and surface morphology of nanosponges were performed. The scanning electron microscopy of nanosponges showed that they were spherical in shape and spongy in nature. Drug entrapment efficiency was found to be in the range of 42.75 % to 73.10 %. The optimized nanosponge formulation was loaded into hydrogel using carbopol 940 and studied for pH, viscosity, in vitro drug release. Of the nanosponge formulations prepared, F4 was found to show drug release of 70.62%. It was concluded that Itraconazole nanosponge hydrogel may have increased solubility and drug release
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
ABSTRACT
Overactive bladder (OAB) is a prevalent condition which has an adverse effect on quality of life. The presence
of urgency incontinence confers significant morbidity above and beyond that of OAB sufferers who are
continent. The primary treatment for OAB and urgency incontinence is a combination of behavioral measures
and antimuscarinic drug therapy. The ideal antimuscarinic agent should effectively relieve the symptoms of
OAB, with the minimum of side effects; it should be available as a once-daily sustained release formulation
and in dosage strength that allows easy dose titration for the majority of sufferers. Solifenacin succinate was
launched in 2005 and has been shown in both short and long term clinical trials to fulfill these requirements.
Solifenacin is a competitive M3 receptor antagonist with a long half-life (45-68 hours). It is available in two
dosage strengths namely a 5 or 10 mg once-daily tablet. The efficacy and tolerability of solifenacin for the
treatment of all symptoms of OAB has been evaluated in a number of large, placebo controlled, randomized
trials. Long-term safety, efficacy, tolerability and persistence with treatment have been established in an open
label 40 week continuation study.
KEYWORDS
Solifenacin, Urinary incontinence, Overactive bladder and Wet granulation method.
Background: The main objective of present research work is to formulate the Carbamazepine Fast Dissoving tablets. Carbamazepine, an
antiepileptic, belongs to BCS Class-II and used to control some types of seizures in the treatment of epilepsy and Neuropathic Pain by
blocking use-dependent sodium channels. Methods: The Fast Dissoving tablets of Carbamazepine were prepared employing different
concentrations of Crospovidone and Croscarmellose sodium in different combinations as a Sperdisintegrants by Direct Compression technique
using 32
factorial design. The concentration of Crospovidone and Croscarmellose sodium was selected as independent variables, X1
and X2 respectively whereas, wetting time, Disintegration time, t
50% ,t90%were selected as dependent variables. Results and Discussion:
Totally nine formulations were designed and are evaluated for hardness, friability, thickness, Assay, Wetting time, Disintegration time, Invitro
drug release. From the Results 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 (a), slope (b) &
regression coefficient (r) were calculated. Polynomial equations were developed for Wetting time, Disintegration time, t50%, t90%. Validity of
developed polynomial equations were verified by designing 2 check point formulations (C1
, C2
). According to SUPAC guidelines the
formulation (F5
) containing combination of 9.375% Crospovidone and 9.375% Croscarmellose, is the most similar formulation (similarity factor
f
2
=82.675, dissimilarity factor f1
= 2.049 & No significant difference, t= 0.041) to marketed product (TEGRETOL-100). Conclusion: The
selected formulation (F5
) follows First order, Higuchi’s kinetics, mechanism of drug release was found to be Non-Fickian Diffusion (n= 0.665).
KEYWORDS: Carbamazepine, 3
2Factorial Design, Crospovidone , croscarmellose Sodium, Wetting Time, Disintegration Time.
Evaluating the Effects of Different Molecular Weights of Polymers in Stabiliz...
(2102 2112) nd14
1. International Journal of PharmTech Research
CODEN (USA): IJPRIF ISSN : 0974-4304
Vol.6, No.7, pp 2102-2112, November 2014
Development and Evaluation of in Situ Gelling System for
Treatment of Periodontitis
Khushbu S. Patel1
*, Dr.K.R.Vadalia2
, Dr. J. K. Patel3
1
School of Pharmacy, RK University, Rajkot, India, Nootan Pharmacy College,
Visnagar, Gujarat, India.
2
Department of Pharmaceutical Analysis, Atmiya institute of pharmacy,
Rajkot, Gujarat, India.
3
Department of Pharmaceutics, Nootan Pharmacy College,
Visnagar, Gujarat, India
*Corres.author : khushbus_patel@yahoo.com
Tel.:+91-2765-233103, Mobile phone: +91-9426305648
Abstract: Tinidazole is well reported for the treatment of periodontal disease, they have better penetration into
periodontal tissues, minimal bacterial resistance as compared to many of the other drugs used for the treatment.
In situ gel-forming systems are viscous liquids that shift to a gel phase upon exposure to physiological
conditions. Tinidazole periodontal gel was prepared by different concentrations of gellan gum, poloxamer 407.
32
full factorial design was applied for optimization. Selected dependent variables were concentration of gellan
gum (X1) and poloxamer 407 (X2). Selected independent variables were viscosity (Y1) release at 1 hour (Y2),
release at 8 hour (Y3). All the prepared formulations were evaluated for appearance, pH, viscosity, % drug
content, syringeability, % drug release and effect of sterilization. By compatibility study drug was found to be
compatible with formulation excipients. Gelation temperature and pH of all formulation found to be in the range
of 29-40ºC and 5.34-6.83 respectively. Viscosity of all prepared formulations was found in the range of 310-
692 centipoise. Both the independent variable had the significant effect on the entire three response variable (P<
0.05). All the formulations were developed using combination of gellan gum and poloxamer 407. The
developed formulations showed satisfactory results for in-vitro gelling capacity, rheology and other physical
properties. Based on maximum desirability and cost effectiveness formulation containing 0.5%w/v of gellan
gum and 15 %w/v of poloxamer 407 was consider as an optimized batch.
Keywords: In situ gel; Periodontitis; Gellan gum; Poloxamer 407; Ion sensitive; Thermo-sensitive.
Introduction:
Periodontitis is an inflammatory response to the overgrowth of anaerobic organisms such as spirochetes
and bactericides and in some cases, micro aerophillic organisms in the subgingival plaque. Periodontal disease,
if unchecked result in the destruction of the bone and soft tissue supporting the tooth which causes tooth loss.
The clinical sign of Periodontitis is changes in morphology of gingival tissues, gingival bleeding as well as
periodontal pocket formation. This pocket provides an ideal environment for the growth and proliferation of
anaerobic pathogenic bacteria1-3
.
Distinguishing from preformed hydrogels, in situ forming gels are formulations, applied as a solution,
which undergoes gelation after instillation due to physicochemical changes inherent to the biological fluids. In
this way, the polymers which show sol-gel phase transition and thus trigger drug release in response to external
stimuli are the most investigated. In situ hydrogels are providing such “sensor” properties and can undergo
reversible sol-gel phase transitions upon changes in the environmental condition. These “intelligent” or “smart”
polymers play important role in drug delivery since they may dictate not only where a drug is delivered, but
2. Khushbu S. Patel et al /Int.J. PharmTech Res.2014,6(7),pp 2102-2112. 2103
also when and with which interval it is released. In situ gels are polymeric networks that absorb large quantities
of water while remaining insoluble in aqueous solutions due to chemical or physical cross linking of individual
polymer chains. They resemble natural living tissue more than any other class of synthetic biomaterials due to
their high water content; furthermore, the high water content of the materials contributes to their
biocompatibility In situ gels show minimal tendency to adsorb proteins from body fluids because of their low
interfacial tension. Further, the ability of molecules of different sizes to diffuse into (drug loading) and out of
(drug release) in situ gels allow the possible use of dry or swollen polymeric networks as drug delivery systems
for oral, nasal, buccal, rectal, vaginal, ocular and parenteral routes of administration. Preformed in situ gels can
be defined as simple viscous solutions which do not undergo any modifications after administration 4-7
.
Figure 1 Healthy and Periodontal Disease
A polymer used to prepare in situ gels should have following characteristics:
It should be biocompatible.
It should be capable of adherence to mucus.
It should have pseudo plastic behavior.
It should have good tolerance and optical clarity.
It should influence the tear behavior.
It should be capable of decreasing the viscosity with increasing shear rate there by offering lowered
viscosity during blinking and stability of the tear film during fixation.
Tinidazole may be related to action of free nitro radical generated as a result of reduction by cell
extracts. Tinidazole also causes DNA base changes in bacterial cells and DNA strand breakage in mammalian
cells. Tinidazole is an antiprotozoal, antibacterial agent. The nitro- group of tinidazole is reduced by cell
extracts of Trichomonas. The free nitro- radical generated as a result of this reduction may be responsible for
the antiprotozoal activity. Chemically reduced tinidazole was shown to release nitrites and cause damage to
purified bacterial DNA in vitro. Additionally, the drug caused DNA base changes in bacterial cells and DNA
strand breakage in mammalian cells. The mechanism by which tinidazole exhibits activity against Giardia and
Entamoeba species is not known8
.
The main aim of research work is developed and evaluated of in situ gelling system for the treatment of
Periodontitis for controlled drug delivery systems. The dose of tinidazole is 2oomg. In situ gel formulations
prepared by using carbopol 934, sodium citrate, methyl paraben and propyl paraben by cold process method.
Thus the study aims to improve patient compliance, increase bioavilibility and sustained drug release9
.
Experimental
Materials
Tinidazole was obtained as a gift samples from cadila pharmaceutical Pvt. Ltd. Ahmedabad. Gellan
gum and poloxamer 407 were obtained as a gift sample from corel pharmaceutical Pvt. Ltd. Ahmedabad.
Methyl paraben, propyl paraben and sodium citrate were obtained from Seva fine chem. Ahmedabad. All other
ingredients used were of analytical grade.
3. Khushbu S. Patel et al /Int.J. PharmTech Res.2014,6(7),pp 2102-2112. 2104
Methods
Preformulation study 10-12
Preformulation testing is the first step in rational development of dosage forms of a drug substance.
Preformulation study is the process of optimizing the delivery of drug through determination of
physicochemical properties of the new compound that could affect drug performance and development of an
efficacious, stable and safe dosage form. It gives the information needed to define the nature of the drug
substance and provide a frame work for the drug combination with pharmaceutical excipients in the dosage
form. Hence, Preformulation studies were performed for the obtained sample of drug for identification and
compatibility studies.
1. Determination of melting point
Melting point of drug was determined by capillary method & compare with the reported value.
2. Drug-interaction study
Differential Scanning Calorimetry (DSC)
Differential Scanning Calorimetry (DSC) technique has been used to study the physical and chemical
interaction between drug and excipients. Firstly DSC of a drug is taken and after a physical mixture of
Tinidazole: Gellan gum: Poloxamer 407 was performed using a Shimadzu DSC-60. Samples were taken, sealed
in aluminum pans, and analyzed in an atmosphere of air at flow rate of 25 mL/min. A temperature range of
50°C to 200°C is to be used, and the heating rate is 20°C/min.
3. Spectrophotometric Estimation of Tinidazole
Determination of λmax of Tinidazole
Tinidazole solution was prepared in phosphate buffer pH 6.8 and then dilute suitably. The UV
spectrums of the solutions were taken on Shimanzu UV Spectrophotometer (Japan). The solutions exhibited UV
maxima at 318.0nm in phosphate buffer pH 6.8.
Preparation of Standard curve of Tinidazole (UV)
Accurately weighed 100mg of tinidazole was transferred to a 100ml volumetric flask and dissolved in
100ml phosphate buffer pH 6.8 to prepared stock solution (1000µg/ml). Then 10ml of above solution was taken
and diluted it with 100ml phosphate buffer pH 6.8 in 100ml volumetric flask to prepare the solution
(100µg/ml). Then 10ml of above solution was taken and diluted it with 100ml phosphate buffer pH 6.8 in
100ml volumetric flask to prepare the solution (10µg/ml). Aliquots of working solution of tinidazole (4-
24µg/ml) were transferred in to a series of 10 ml volumetric flask and volume was making up to the mark with
phosphate buffer pH 6.8. Absorbance of the resulting solutions was measured at 318.0 nm against a reagent
blank solution prepared similarly without drug using Shimanzu UV Spectrophotometer (Japan). Calibration
curve was prepared by plotting concentration versus absorbance graph.
Preliminary study for selection of polymer
This study was done to get idea about the appearance, gelling capacity, pH, viscosity, gelation
temperature, drug content uniformility, syringe ability and in vitro release study of the drug formulation. This
study was aimed to select proper concentration of Gellan gum and poloxamer 407 were used as gelling agent.
Preparation of In situ gel formulations 13-15
For the preparation of in situ gel formulations, Gellan gum was first added to distilled water with
continuous stirring. Gellan gum was dissolved by warming the solution at 80 ºC for 15 min with continue
stirring. poloxamer 407 was slowly added to cold water separately with continuous stirring and stirred until it
completely mixed. The partially dissolved Poloxamer 407 solutions were stored in a refrigerator and stirred
periodically until clear homogenous solutions were obtained (approximately 24 hrs).Then gellan gum
formulations and poloxamer 407 formulations were mixed uniformly by stirring. Tinidazole was dissolved in
required quantity of distilled water separately and then it was added to polymer solutions under constant stirring
until a uniform solution was obtained. Finally Sodium citrate, Propyl paraben and Methyl paraben were added
4. Khushbu S. Patel et al /Int.J. PharmTech Res.2014,6(7),pp 2102-2112. 2105
to the formulation under constant stirring until a uniform solution was obtained. Different concentrations of
polymer were used to prepare in situ gel as per the composition shown in (Table 1).
Table -1: Composition Of Drug And Excipients In Factorial Batches Of Periodontal In Situ Gel Of
Tinidazole
Ingredients
(%w/v)
Formulations
F1 F2 F3 F4 F5 F6 F7 F8 F9
Tinidazole 2 2 2 2 2 2 2 2 2
Gellan gum 0.5 1 1.5 0.5 1 1.5 0.5 1 1.5
Poloxamer 407 10 10 10 15 15 15 20 20 20
Sodium Citrate 0.1 0.1 0.1 0.1 0.1 0.1 0.1 0.1 0.1
Methyl paraben 0.15 0.15 0.15 0.15 0.15 0.15 0.15 0.15 0.15
Propyl paraben 0.02 0.02 0.02 0.02 0.02 0.02 0.02 0.02 0.02
Distilled water q.s. q.s. q.s. q.s. q.s. q.s. q.s. q.s. q.s.
Table - 2: Selection Of Levels For Independent Variables
Level Variable
X 1 (Concentration of
Gellan gum) %w/v
X 2 (Concentration of Poloxamer 407)
%w/v
Low -1 0.5 10
Medium 0 1.0 15
High +1 1.5 20
Experimental design
A 32
randomized full factorial design was employed in the present study. In this design 2 factors were
evaluated, each at 3 levels, and experimental trials were performed for all 9 possible combinations. The
Concentration of Gellan gum (X1) and concentration of Poloxamer 407 (X2) were chosen as independent
variables and viscosity, % cumulative drug release at 1 h. (Q1) and % cumulative drug release at 8 h. (Q8) were
taken as dependent variables Shown in (Table 2 and 3).
Table - 3: Formulation Layout For 32
Factorial Batches
Batches
Coded value Actual value
X1 X2
X 1 (Concentration of
Gellan gum)
X 2 (Concentration of
Poloxamer 407)
F1 -1 -1 0.5 10
F2 0 -1 1 10
F3 +1 -1 1.5 10
F4 -1 0 0.5 15
F5 0 0 1 15
F6 +1 0 1.5 15
F7 -1 +1 0.5 20
F8 0 +1 1 20
F9 +1 +1 0.5 20
5. Khushbu S. Patel et al /Int.J. PharmTech Res.2014,6(7),pp 2102-2112. 2106
Characterization of in situ gel 16,17
1. Appearance
All developed formulations were evaluated from the visual inspection.
2. Gelling Capacity
All formulations were evaluated for gelling capacity in order to identify the compositions suitable for
use as in situ gelling systems. The gelling capacity were determined by placing a drop of the system in a vial
containing 2 ml of phosphate buffer pH 6.8 freshly prepared and equilibrated at 37o
C and visually assessing gel
formation and noting the time for gelation and the time taken for the gel formed to dissolve.
3. pH
pH is one of the most important parameter involved in the periodontal formulation. The two area of
critical importance are the effect of pH on solubility and stability. The formulations were evaluated for pH by
using digital pH meter.
4. Viscosity
The viscosity of all prepared formulations was measured using Digital Brookfield viscometer (DV-
II+Pro, USA). The measurements were carried out using spindle no.02 at the speed of a 10 rpm in the sample.
5. Gelation temperature
Ten milliliters of the sample solution and a magnetic bead were put into a 30 ml transparent vial that
was placed in a low temperature digital water bath. A thermometer was placed in the sample solution. The
solution was heated at the rate of 1°C/min with the continuous stirring at lower rpm. The temperature was
determined as gelation temperature.
6. Drug content uniformity
Accurately weighed amount gel equivalent to 2mg of drug was taken in a 100ml volumetric flask.
Phosphate buffer (pH 6.8) was added to it and kept on magnetic stirrer to dissolve the drug. The volume was
made to 100ml with Phosphate buffer (pH 6.8) and filtered using 0.45μm filter paper. 10ml aliquot of the above
solution will be taken and diluted to 100ml with Phosphate buffer (pH 6.8). The absorbance of sample solution
was determined at 318 nm against Phosphate buffer (pH 6.8) by using UV-Visible Spectrophotometer-1800
(Shimadzu, Japan).
7. Syringeability
All prepared formulations were transferred into an identical 5 ml syringe placed with 20 gauge needle
to a constant volume (1 ml). The solutions which were easily passed from syringe was termed as pass and
difficult to pass were termed as fail.
8. In vitro Drug Release Studies
The in vitro release of Tinidazole from the formulations was studied through cellophane membrane
using a modified USP II dissolution testing apparatus. The dissolution medium was phosphate buffer (pH 6.8).
Cellophane membrane, previously soaked overnight in the dissolution medium, was tied to one end of a
specifically designed glass cylinder (open at both ends and of 5 cm diameter). A selected volume of the
formulation was accurately pipette into this assembly. The cylinder was attached to the metallic driveshaft and
suspended in 50 ml of dissolution medium maintained at 37± 0.5°C so that the membrane just touched the
receptor medium surface. The dissolution medium was stirred at required 50 rpm using magnetic stirrer.
Aliquots, a sample was withdrawn at regular intervals and replaced by an equal volume of the receptor medium.
The aliquots were diluted with the receptor medium and were analyzed by UV-VIS spectrophotometer.
9. Sterility Testing
The sterility test was performed according to Indian Pharmacopoeia. Direct inoculation method was
preferred to use. 2 ml of liquid from test container was removed with a sterile pipette or with a sterile syringe or
6. Khushbu S. Patel et al /Int.J. PharmTech Res.2014,6(7),pp 2102-2112. 2107
a needle. The test liquid was aseptically transferred to fluid thioglycolate medium (20 ml) and soyabeancasein
digest medium (20 ml) separately. The liquid was mixed with the media. The inoculated media was incubated
for not less than 14 days at 30°C to 35°C in the case of fluid thioglycolate medium and 20°C to 25°C in the case
of soyabean-casein digest medium.
Result and Discussion:
Preformulation Study
1. Determination of melting point
The melting point of Tinidazole was found to be 124-128 ºC which was similar with the reported value Shown
in (Table 4).
Table - 4: Melting Point Of Tinidazole
Drug
Practically
obtained
Theoretical range
Tinidazole 124-128 ºC 124-130ºC
2. Drug- interaction study
Differential Scanning Calorimetry (DSC)
The DSC results provided both qualitative and quantitative information about the physicochemical state
of the drug present in formulation. The thermograph of pure Tinidazole showed a melting endothermic peak at
1280
C while in the thermograph of mixture peaks it was observed at 1280
C. The DSC thermo grams of the
mixture showed distinct endothermic peaks for Tinidazole and the polymer. This corresponds to the peaks of
individual drug and polymer without exhibiting any modification which indicates that the drug did not interact
with excipients used in the tablets. This confirmed that the presence of other excipients did not affect the drug
stability.
Figure 2 Dsc Of Tinidazole
7. Khushbu S. Patel et al /Int.J. PharmTech Res.2014,6(7),pp 2102-2112. 2108
Figure 3 Dsc Of Tinidazole With Polymer Mixture
3. Spectrophotometric Estimation of Tinidazole
Determination of λmax of Tinidazole
The wavelength maximum for Tinidazole was found to be 318.0 nm (shown in figure: 4).
Figure 4 λmax OF TINIDAZOLE
Preparation of Standard curve of Tinidazole (UV)
The linear regression data obtained for the calibration curve showed a good linear relationship over the
concentration range 4-24 µg/ml with respect to Absorbance shown in (Table 5).
Table - 5: Standard Plot Of Tinidazole In Phosphate Buffer (Ph 6.8) At λmax 318nm
Concentration(µg/ml) Absorbance
0 0.000
4 0.121
8 0.248
12 0.362
16 0.485
20 0.589
24 0.743
8. Khushbu S. Patel et al /Int.J. PharmTech Res.2014,6(7),pp 2102-2112. 2109
Figure 5 Regressed Calibration Curve For Tinidazole, Ph 6.8
Characterization of 32
full factorial batches
In the present study, 32
factorial design was applied in which Gellan gum and Poloxamer 407 polymer
in combination were fixed from the preliminary trials. In this design two factors were evaluated, each at three
levels, and experimental trials were carried out at all nine possible combinations. The factors were selected
based on preliminary study. The concentration of Gellan gum (X1) and concentration of Poloxamer 407 (X2)
were selected as independent variables. Viscosity (cps), Drug release at 1 h. (Q1) (%) and Drug release at 8 h.
(Q8) (%) were selected as dependent variables. The evaluation of factorial batches (F1 to F9) has been shown in
(Table 6).
Table - 6: Evaluation Of Factorial Batches F1-F9
Batch Clarity
Gelling
capacity
pH
Gelation
temperature
(o
c)
Viscosity
(in cps)
Drug
Content
(%)
Syringeability
F1 Clear + 6.37 37 503.4 ± 4.3 97.25 ±0.12 Pass
F2 Clear ++ 6.21 32 710.2 ± 3.6 94.83± 0.23 Pass
F3 Clear ++ 6.08 31 1045.9 ±5.3 96.68± 0.15 Fail
F4 Clear +++ 6.28 33 607.3 ±6.6 95.82±0.26 Pass
F5 Clear +++ 6.12 29 753.0 ±5.4 97.08±0.26 Pass
F6 Clear +++ 6.02 31 1093.2± 3.8 97.30± 0.31 Fail
F7 Clear ++ 5.92 36 670 ± 2.9 97.93± 0.31 Pass
F8 Clear +++ 5.72 33 845 ± 3.8 95.73± 0.14 Pass
F9 Clear +++ 5.61 28 1070± 4.6 96.24± 0.24 Fail
1. Appearance
All the formulations were checked for the appearance. From batch F1 to F9, all other batches were
found to be clear
2. Gelling Capacity
The gelling capacity o all the formulations were shown in (Table 6). The gelling capacity of all
formulation was found to be satisfactory.
3. pH
The formulations were evaluated for pH as per described in material and methods. pH of all the
formulations was shown in (Table 6). The pH of the formulations was in the range of 5.34 - 6.83 which was
satisfactory.
4. Gelation temperature
It was determined as described in material and methods. Gelation temperature of all the formulations
was shown in (Table 6). The satisfactory results were found which is quite beneficial for gelation.
9. Khushbu S. Patel et al /Int.J. PharmTech Res.2014,6(7),pp 2102-2112. 2110
5. Viscosity
Viscosity of all formulations was measured using Brookfield digital Viscometer DV-II+ Pro
viscometer. The gel under study was placed in the spindle S61 at 50 RPM for liquid formulations and gels.
Viscosity of batch E1 to E9 was 503.4 ± 4.3, 710.2 ± 3.6, 1045.9 ± 5.3, 607.3 ± 6.6, 753.0 ± 5.4, 1093.2 ± 3.8,
659.2 ± 2.9, 875 ± 3.8, 1065.2 ± 4.6 respectively. Highest viscosity was found in batch F9. Figure 6 shows that
increase in concentration of polymer causes increase in viscosity of the formulation.
Figure 6 Viscosity Of All Formulations
6. Drug content
Drug content of all factorial batches were found to be 97.25 ±0.12, 94.83 ± 0.23, 96.68 ± 0.15, 95.82±
0.26, 97.08± 0.26, 97.30 ± 0.31, 97.93 ± 0.31, 95.73 ± 0.14 and 96.24 ± 0.24 for batch F1 to F9 respectively.
This indicates the uniformity of drug content.
7. Syringeability
Syringe ability of the formulations was determined as per material and methods. Syringe ability of all
the formulations was shown in (Table 6). In that F3, F6 and F9 batches are fail and all other batches were
passed the syringe ability.
8. In vitro drug release studies
The in vitro release of Tinidazole from the formulations was studied and evaluated. Shown in (Table
7).
Figure 7 % Drug Release Profile Of Factorial Batches Of Periodontal In-Situ Gel
10. Khushbu S. Patel et al /Int.J. PharmTech Res.2014,6(7),pp 2102-2112. 2111
The release profile of a drug predicts how a delivery system might function and gives valuable insight
into its in vivo behavior. The in vitro release of Tinidazole from the formulations was studied as described in
the material and methods. In vitro release profile of the selected formulations was shown in (Table 7). The in
vitro release profile represented that the in situ gelling formulation could provide sustained and controlled
release of drug. The comparison of release profile of factorial batches shows there were significant effect of
both the factors concentration of Gellan gum and Poloxamer 407. The release pattern also showed that the
concentration of Gellan gum is more significant than the concentration of Poloxamer 407 on the variable %
drug release. So the controlled release of Tinidazole is more significant on the concentration of Gellan gum.
Table - 7: % Drug Release Of Factorial Batches Of Periodontal In-Situ Gel
Batch
code --> F1 F2 F3 F4 F5 F6 F7 F8 F9
Time (hour)
0 0 0 0 0 0 0 0 0 0
1 17.37 15.84 11.02 15.31 13.21 10.41 14.22 12.07 10.02
2 26.31 22.69 16.22 27.44 20.14 15.07 25.88 18.22 23.21
3 39.86 34.52 31.04 37.17 30.24 26.31 41.35 30.2 36.57
4 48.52 46.36 44.34 46.21 44.61 46.69 52.14 41.64 44.2
5 61.78 57.77 52.35 59.67 57.34 55.28 60.27 54.44 52.39
6 76.47 74.32 72.21 74.37 73.22 64.31 72.89 66.54 60.04
7 89.17 84.96 80.39 83.28 80.42 77.21 81.29 76.25 71.02
8 95.64 93.83 89.31 93.48 91.47 88.35 92.27 89.07 85.31
9. Sterility testing
As Per the material and methods sterility testing was determined. Formulation F4 passed the sterility
test as there was no appearance of turbidity and hence no evidence of microbial growth when incubated for a
period of not less than 7 days at 30-35°C in case of fluid thioglycolate medium and at 20-25°C in the case of
soya bean casein digest medium.
Kinetic Modeling of Dissolution Data
Based on the r2
-value, the best-fit model was selected. The n value was 0.5-1 so the drug transport
mechanism was non Fickian diffusion. The highest R2
value was obtained in the Higuchi model so the release
kinetics followed by higuchi model as best fit model shown in (Table 8).
Table - 8: Kinetic Modeling Of Drug Release Data
Batch
no.
Higuchi Zero order First order K-Peppas
r2
r2
r2
r2
F4 0.994 0.963 0.9504 0.9818
Discussion:
Tinidazole is well reported for the treatment of periodontal disease, they have better penetration into
periodontal tissues, minimal bacterial resistance as compared to many of the other drugs used for the treatment.
The excipients used in this present work are Gellan gum and Poloxamer 407 as gelling agent which form
immediate gel. The Methyl paraben and Propyl paraben is used as preservatives. Preformulation studies were
carried out in order to establish the compatibility between the drug and polymers by DSC. The studies revealed
that drug and polymers were compatible. From the results, two factors were selected i.e. concentration of Gellan
gum (X1) and concentration of Poloxamer 407 (X2) as independent variables for 32
full factorial design.
Dependent variables selected were Viscosity (CPS), Drug release after 1hr (%) and Drug release after 8hrs (%).
The prepared formulations were evaluated for different parameters like pH, appearance, drug content, in vitro
gelation study, viscosity, in vitro release study, and sterility testing. From the in vitro study, it was found that
the developed formulation was provided sustained release of the drug over 8 hrs. On the bases of Desirability
11. Khushbu S. Patel et al /Int.J. PharmTech Res.2014,6(7),pp 2102-2112. 2112
approach, formulation containing Gellan gum and Poloxamer 407 in concentration of 0.5 and 15% respectively
was selected as optimized batch. The release profile of the formulation follows Higuchi order model (r2
=0.994)
and release mechanism was non-Fickian diffusion. By doing compatibility study, drug was found to be
compatible with formulation excipients, it is concluded that the selected polymers are likely to be suitable for
preparation of in situ periodontal gel formulation. The developed formulations shows satisfactory results for
gelation time, gelation temperature, Viscosity, Syringeability and other physical properties. Based on maximum
desirability the formulation containing 0.5%w/v of Gellan gum and 15%w/v of Poloxamer 407 was consider as
an optimized formulation. The developed formulation was therapeutically efficacious, stable and provided
sustained release of the drug over extended period of time.
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