This document describes the formulation and characterization of nebivolol floating microspheres for gastroretentive drug delivery. Nebivolol is classified as a class II drug with poor solubility and high permeability. Microspheres were prepared using polymers like ethyl cellulose and HPMC via emulsion solvent diffusion method. The microspheres were characterized for particle size, entrapment efficiency, in vitro drug release and buoyancy studies. The results showed the microspheres had prolonged drug release and remained buoyant for over 12 hours, indicating their potential as a gastroretentive drug delivery system.
Formulation and evaluation of mucoadhesive tablets of carvedilol using natura...Nausheen Fatima
Present work describes formulation and evaluation mucoadhesive tablets of Carvedilol using natural binders such as Chitosan and Guar Gum to reduce the first pass metabolism and frequency of administration.
Formulation and evaluation of Muco adhesive Buccal Tablets of Ramprildoddaapurupa
The buccal mucosa lines the inner cheek and Buccal formulations are placed in the mouth between upper gingiva(gums) and cheek to treat local and systemic conditions.
Drugs which undergoes Extensive first pass metabolism and drug degradation in acidic media, GI tract can be administered through buccal route.
The oral cavity has been used as a site for local and systemic drug delivery.
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
Bioavailability and bioequivalence studyMcpl Moshi
BCS is a scientific framework for classifying drug substances based on their aqueous solubility and intestinal permeability.
It is a drug development tool that allows estimation of solubility, dissolution and intestinal permeability affect that oral drug absorption.
Kashikar V S
PES Modern College of Pharmacy ( for ladies), Moshi Pune
Bioavailability and Bioequivalence studyMcpl Moshi
Bioavailability and Bioequivalence study, BCS is a scientific framework for classifying drug substances based on their aqueous solubility and intestinal permeability.
It is a drug development tool that allows estimation of solubility, dissolution and intestinal permeability affect that oral drug absorption.
Formulation and evaluation of mucoadhesive tablets of carvedilol using natura...Nausheen Fatima
Present work describes formulation and evaluation mucoadhesive tablets of Carvedilol using natural binders such as Chitosan and Guar Gum to reduce the first pass metabolism and frequency of administration.
Formulation and evaluation of Muco adhesive Buccal Tablets of Ramprildoddaapurupa
The buccal mucosa lines the inner cheek and Buccal formulations are placed in the mouth between upper gingiva(gums) and cheek to treat local and systemic conditions.
Drugs which undergoes Extensive first pass metabolism and drug degradation in acidic media, GI tract can be administered through buccal route.
The oral cavity has been used as a site for local and systemic drug delivery.
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
Bioavailability and bioequivalence studyMcpl Moshi
BCS is a scientific framework for classifying drug substances based on their aqueous solubility and intestinal permeability.
It is a drug development tool that allows estimation of solubility, dissolution and intestinal permeability affect that oral drug absorption.
Kashikar V S
PES Modern College of Pharmacy ( for ladies), Moshi Pune
Bioavailability and Bioequivalence studyMcpl Moshi
Bioavailability and Bioequivalence study, BCS is a scientific framework for classifying drug substances based on their aqueous solubility and intestinal permeability.
It is a drug development tool that allows estimation of solubility, dissolution and intestinal permeability affect that oral drug absorption.
Formulation and evaluation of antifungal ketoconazole emulgelShwetaKate3
Formulation and evaluation of ketoconazole Emulgel:Controlled drug delivery ,
Presentation by Gajanan S. Lahade
M.pharm second year,
PDEA'S Seth govind raghunath Sable college of pharmacy, saswad ,pune,India
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.
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.
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.
Formulation and Evaluation of Solid dispersion for Dissolution Enhancement of...Jing Zang
Nifedipine, a calcium channel blocker antihypertensive drug, is a poorly water soluble drug and belongs to BCS class II. The objective of the research work was to formulate and optimize solid dispersions (SDs) of a poorly water soluble drug, nifedipine, with sodium starch glycollate, croscarmellose sodium, eudragit E-100. Solid dispersions were prepared by solvent evaporation techniques in different weight ratios of polymers. The results indicated that homogeneous or heterogeneous conditions during the preparation methods employed governed the internal structures of the polymer matrices while retaining the drug in an amorphous form. The physical mixtures and solid dispersions were subjected to drug content and dissolution test. The best formulation, nifedipine with croscarmellose sodium in 1:7 ratio, among all was further adsorbed on neusilin US2 to form ternary mixture. The increased dissolution was achieved by more than 70percent and 30percent comparatively to the nifedipine API and marketed product respectively. The tablet dosage form prepared from ternary mixture was stable at stressed conditions 40±2°C and 75±5% RH. The release kinetics of drug from formulation and marketed product follows peppas model. The similar factor f2 was within limit for the product at stressed conditions with the product at room temperature at the same time.
Formulation Development and Evaluation of Self Nano Emulsifying Drug Delivery...ijtsrd
The primary objective of the work was to develop a self nano emulsifying drug delivery system of dolutegravir HCL. Self nanoemulsifying drug delivery system is a lipid based formulation which consists of isotropic mixtures of oils, surfactants and co surfactants. It can conveniently develop the emulsion on gentle agitation and offers a considerable surface area for interaction between the SNEDDS formulation and the aqueous gastrointestinal fluid. This may lead to enhanced bioavailability of hydrophobic agents. The Liquid SNEDDS was prepared and after that solidified by aerosil 200. For 10 gm of liquid SNEDDS 5 gm of Aerosil 200 was used and after that product is dried by spray drying method. And 12 gm of product is remaining after the process. The drug excipients interaction studies were carried out using FTIR and DSC. The interaction studies were carried out to check physical and chemical stability of Dolutegravir with other excipients. FTIR spectra showed the characteristic peaks of drug i.e. for C H stretch, N C stretch appear in the spectra of physical mixtures at the same wave number indicating no modification or interaction between drug and the polymers. The liquid SNEDDS formulation C1 showed good thermodynamic stability without any precipitation and having globule size 536.6 nm and zeta potential 29.9. Based on thermodynamic stability, precipitation studies, self emulsification studies, globule size and zeta potential liquid SNEDDS of formulation batch C1 was selected as optimized formulation. Liquid SNEDDS and solid SNEDDS was prepared for Dolutegravir. SEM, IR, and DSC results confirmed that drug was present in an amorphous state in solid SNEDDS. In vitro drug release and drug content of optimized formulation was found to be 98.64 and 99.35 respectively. F3 batch of capsule formulation shows better drug release than marketed formulation. Suresh Mularam Choudhary | Prof S. A Waghmare | Hemant V. Kamble "Formulation Development and Evaluation of Self Nano Emulsifying Drug Delivery System of Dolutegravir" 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/ijtsrd50569.pdf Paper URL: https://www.ijtsrd.com/pharmacy/pharmaceutics/50569/formulation-development-and-evaluation-of-self-nano-emulsifying-drug-delivery-system-of-dolutegravir/suresh-mularam-choudhary
Biopharmaceutical classification system & drug delivery system associated wit...PratikShinde120
Biopharmaceutical classification system & drug delivery system based on BCS.
By Pratik shinde, Mpharm, University department of pharmaceutical sciences, Nagpur
Formulation and evaluation of antifungal ketoconazole emulgelShwetaKate3
Formulation and evaluation of ketoconazole Emulgel:Controlled drug delivery ,
Presentation by Gajanan S. Lahade
M.pharm second year,
PDEA'S Seth govind raghunath Sable college of pharmacy, saswad ,pune,India
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.
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.
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.
Formulation and Evaluation of Solid dispersion for Dissolution Enhancement of...Jing Zang
Nifedipine, a calcium channel blocker antihypertensive drug, is a poorly water soluble drug and belongs to BCS class II. The objective of the research work was to formulate and optimize solid dispersions (SDs) of a poorly water soluble drug, nifedipine, with sodium starch glycollate, croscarmellose sodium, eudragit E-100. Solid dispersions were prepared by solvent evaporation techniques in different weight ratios of polymers. The results indicated that homogeneous or heterogeneous conditions during the preparation methods employed governed the internal structures of the polymer matrices while retaining the drug in an amorphous form. The physical mixtures and solid dispersions were subjected to drug content and dissolution test. The best formulation, nifedipine with croscarmellose sodium in 1:7 ratio, among all was further adsorbed on neusilin US2 to form ternary mixture. The increased dissolution was achieved by more than 70percent and 30percent comparatively to the nifedipine API and marketed product respectively. The tablet dosage form prepared from ternary mixture was stable at stressed conditions 40±2°C and 75±5% RH. The release kinetics of drug from formulation and marketed product follows peppas model. The similar factor f2 was within limit for the product at stressed conditions with the product at room temperature at the same time.
Formulation Development and Evaluation of Self Nano Emulsifying Drug Delivery...ijtsrd
The primary objective of the work was to develop a self nano emulsifying drug delivery system of dolutegravir HCL. Self nanoemulsifying drug delivery system is a lipid based formulation which consists of isotropic mixtures of oils, surfactants and co surfactants. It can conveniently develop the emulsion on gentle agitation and offers a considerable surface area for interaction between the SNEDDS formulation and the aqueous gastrointestinal fluid. This may lead to enhanced bioavailability of hydrophobic agents. The Liquid SNEDDS was prepared and after that solidified by aerosil 200. For 10 gm of liquid SNEDDS 5 gm of Aerosil 200 was used and after that product is dried by spray drying method. And 12 gm of product is remaining after the process. The drug excipients interaction studies were carried out using FTIR and DSC. The interaction studies were carried out to check physical and chemical stability of Dolutegravir with other excipients. FTIR spectra showed the characteristic peaks of drug i.e. for C H stretch, N C stretch appear in the spectra of physical mixtures at the same wave number indicating no modification or interaction between drug and the polymers. The liquid SNEDDS formulation C1 showed good thermodynamic stability without any precipitation and having globule size 536.6 nm and zeta potential 29.9. Based on thermodynamic stability, precipitation studies, self emulsification studies, globule size and zeta potential liquid SNEDDS of formulation batch C1 was selected as optimized formulation. Liquid SNEDDS and solid SNEDDS was prepared for Dolutegravir. SEM, IR, and DSC results confirmed that drug was present in an amorphous state in solid SNEDDS. In vitro drug release and drug content of optimized formulation was found to be 98.64 and 99.35 respectively. F3 batch of capsule formulation shows better drug release than marketed formulation. Suresh Mularam Choudhary | Prof S. A Waghmare | Hemant V. Kamble "Formulation Development and Evaluation of Self Nano Emulsifying Drug Delivery System of Dolutegravir" 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/ijtsrd50569.pdf Paper URL: https://www.ijtsrd.com/pharmacy/pharmaceutics/50569/formulation-development-and-evaluation-of-self-nano-emulsifying-drug-delivery-system-of-dolutegravir/suresh-mularam-choudhary
Biopharmaceutical classification system & drug delivery system associated wit...PratikShinde120
Biopharmaceutical classification system & drug delivery system based on BCS.
By Pratik shinde, Mpharm, University department of pharmaceutical sciences, Nagpur
One of the most developed cities of India, the city of Chennai is the capital of Tamilnadu and many people from different parts of India come here to earn their bread and butter. Being a metropolitan, the city is filled with towering building and beaches but the sad part as with almost every Indian city
Medical Technology Tackles New Health Care Demand - Research Report - March 2...pchutichetpong
M Capital Group (“MCG”) predicts that with, against, despite, and even without the global pandemic, the medical technology (MedTech) industry shows signs of continuous healthy growth, driven by smaller, faster, and cheaper devices, growing demand for home-based applications, technological innovation, strategic acquisitions, investments, and SPAC listings. MCG predicts that this should reflects itself in annual growth of over 6%, well beyond 2028.
According to Chris Mouchabhani, Managing Partner at M Capital Group, “Despite all economic scenarios that one may consider, beyond overall economic shocks, medical technology should remain one of the most promising and robust sectors over the short to medium term and well beyond 2028.”
There is a movement towards home-based care for the elderly, next generation scanning and MRI devices, wearable technology, artificial intelligence incorporation, and online connectivity. Experts also see a focus on predictive, preventive, personalized, participatory, and precision medicine, with rising levels of integration of home care and technological innovation.
The average cost of treatment has been rising across the board, creating additional financial burdens to governments, healthcare providers and insurance companies. According to MCG, cost-per-inpatient-stay in the United States alone rose on average annually by over 13% between 2014 to 2021, leading MedTech to focus research efforts on optimized medical equipment at lower price points, whilst emphasizing portability and ease of use. Namely, 46% of the 1,008 medical technology companies in the 2021 MedTech Innovator (“MTI”) database are focusing on prevention, wellness, detection, or diagnosis, signaling a clear push for preventive care to also tackle costs.
In addition, there has also been a lasting impact on consumer and medical demand for home care, supported by the pandemic. Lockdowns, closure of care facilities, and healthcare systems subjected to capacity pressure, accelerated demand away from traditional inpatient care. Now, outpatient care solutions are driving industry production, with nearly 70% of recent diagnostics start-up companies producing products in areas such as ambulatory clinics, at-home care, and self-administered diagnostics.
The dimensions of healthcare quality refer to various attributes or aspects that define the standard of healthcare services. These dimensions are used to evaluate, measure, and improve the quality of care provided to patients. A comprehensive understanding of these dimensions ensures that healthcare systems can address various aspects of patient care effectively and holistically. Dimensions of Healthcare Quality and Performance of care include the following; Appropriateness, Availability, Competence, Continuity, Effectiveness, Efficiency, Efficacy, Prevention, Respect and Care, Safety as well as Timeliness.
CHAPTER 1 SEMESTER V PREVENTIVE-PEDIATRICS.pdfSachin Sharma
This content provides an overview of preventive pediatrics. It defines preventive pediatrics as preventing disease and promoting children's physical, mental, and social well-being to achieve positive health. It discusses antenatal, postnatal, and social preventive pediatrics. It also covers various child health programs like immunization, breastfeeding, ICDS, and the roles of organizations like WHO, UNICEF, and nurses in preventive pediatrics.
Navigating Challenges: Mental Health, Legislation, and the Prison System in B...Guillermo Rivera
This conference will delve into the intricate intersections between mental health, legal frameworks, and the prison system in Bolivia. It aims to provide a comprehensive overview of the current challenges faced by mental health professionals working within the legislative and correctional landscapes. Topics of discussion will include the prevalence and impact of mental health issues among the incarcerated population, the effectiveness of existing mental health policies and legislation, and potential reforms to enhance the mental health support system within prisons.
Explore our infographic on 'Essential Metrics for Palliative Care Management' which highlights key performance indicators crucial for enhancing the quality and efficiency of palliative care services.
This visual guide breaks down important metrics across four categories: Patient-Centered Metrics, Care Efficiency Metrics, Quality of Life Metrics, and Staff Metrics. Each section is designed to help healthcare professionals monitor and improve care delivery for patients facing serious illnesses. Understand how to implement these metrics in your palliative care practices for better outcomes and higher satisfaction levels.
The Importance of Community Nursing Care.pdfAD Healthcare
NDIS and Community 24/7 Nursing Care is a specific type of support that may be provided under the NDIS for individuals with complex medical needs who require ongoing nursing care in a community setting, such as their home or a supported accommodation facility.
Defecation
Normal defecation begins with movement in the left colon, moving stool toward the anus. When stool reaches the rectum, the distention causes relaxation of the internal sphincter and an awareness of the need to defecate. At the time of defecation, the external sphincter relaxes, and abdominal muscles contract, increasing intrarectal pressure and forcing the stool out
The Valsalva maneuver exerts pressure to expel faeces through a voluntary contraction of the abdominal muscles while maintaining forced expiration against a closed airway. Patients with cardiovascular disease, glaucoma, increased intracranial pressure, or a new surgical wound are at greater risk for cardiac dysrhythmias and elevated blood pressure with the Valsalva maneuver and need to avoid straining to pass the stool.
Normal defecation is painless, resulting in passage of soft, formed stool
CONSTIPATION
Constipation is a symptom, not a disease. Improper diet, reduced fluid intake, lack of exercise, and certain medications can cause constipation. For example, patients receiving opiates for pain after surgery often require a stool softener or laxative to prevent constipation. The signs of constipation include infrequent bowel movements (less than every 3 days), difficulty passing stools, excessive straining, inability to defecate at will, and hard feaces
IMPACTION
Fecal impaction results from unrelieved constipation. It is a collection of hardened feces wedged in the rectum that a person cannot expel. In cases of severe impaction the mass extends up into the sigmoid colon.
DIARRHEA
Diarrhea is an increase in the number of stools and the passage of liquid, unformed feces. It is associated with disorders affecting digestion, absorption, and secretion in the GI tract. Intestinal contents pass through the small and large intestine too quickly to allow for the usual absorption of fluid and nutrients. Irritation within the colon results in increased mucus secretion. As a result, feces become watery, and the patient is unable to control the urge to defecate. Normally an anal bag is safe and effective in long-term treatment of patients with fecal incontinence at home, in hospice, or in the hospital. Fecal incontinence is expensive and a potentially dangerous condition in terms of contamination and risk of skin ulceration
HEMORRHOIDS
Hemorrhoids are dilated, engorged veins in the lining of the rectum. They are either external or internal.
FLATULENCE
As gas accumulates in the lumen of the intestines, the bowel wall stretches and distends (flatulence). It is a common cause of abdominal fullness, pain, and cramping. Normally intestinal gas escapes through the mouth (belching) or the anus (passing of flatus)
FECAL INCONTINENCE
Fecal incontinence is the inability to control passage of feces and gas from the anus. Incontinence harms a patient’s body image
PREPARATION AND GIVING OF LAXATIVESACCORDING TO POTTER AND PERRY,
An enema is the instillation of a solution into the rectum and sig
1. FORMULATION OF POLYMERIC MICROSPHERES OF
NEBIVOLOL FOR GASTRO-RETENTION AND
INVESTIGATION OF IN-VITRO AND IN-VIVO
CHARACTERIZATION
Presented by,
Joel Joshua J
M. Pharm III Sem
Dept. of Pharmaceutics
Nandha College of pharmacy
NANDHA COLLEGE OF PHARMACY
Approved by PCI, Affiliated to The Tamil Nadu
Dr. MGR Medical University
Accredited by NBA, AICTE, New Delhi.
Under the guidance,
S. Punitha, M.Pharm
Associate Professor
Dept. of Pharmaceutics
Nandha college of Pharmacy
2. Contents:
• Introduction
• Review of Literature
• Aim & Objective
• Drug Profile
• Polymer Profile
• Plan of work
• Preformulation study
Organoleptic properties
FT-IR analysis
Determination of Melting point
Solubility analysis
Determination of absorbance maxima (λmax)
Preparation of Calibration curve
2
25-Apr-2023 Nandha College of Pharmacy
• Formulation Design
• Preparation of Nebivolol floating microspheres
• Characterization of Nebivolol microspheres
• Works to be followed
• References
3. Introduction
• Microspheres are micro-sized spherical particles made up of polymeric
substances, in which the drug is dispersed throughout the microsphere
matrix and its size ranges from 1µm to 1000µm.
• Floating microspheres are gastroretentive drug delivery systems these are
spherical empty particles without a core.
• In order to float on the surface of gastric contents the floating dosage
systems or hydrodynamically balanced systems should have lower bulk
density than the gastric fluid to convey buoyancy to the dosage form.
• This property results in delayed transit through the stomach. The drug is
released slowly at desired rate, resulting in increased gastric retention with
reduced fluctuations in plasma drug concentration
• In this study Floating microspheres are formulated by emulsion solvent
diffusion method.
3
25-Apr-2023 Nandha College of Pharmacy
4. Review of Literature
1. Arun Kumar et al., (2021), formulated and evaluated gastroretentive
Tinidazole loaded floating microsphere for sustained release. In this study the
synthesis of gastro-retentive microspheres of Tinidazole by using a variable
drug and ethyl cellulose ratios. They were floated successfully on the fluid
due to their low bulk density.
2. Kauslya Arumugam et al., (2021), formulated and evaluated the floating
microspheres of ciprofloxacin by solvent evaporation method. The microspheres
were formulated by the solvent evaporation method using different ratios of
polymers like carbopol 940, ethylcellulose, and Hydroxy Propyl Methyl Cellulose
K4M. Further. The floating microspheres were prepared successfully and the
results clearly stated that prepared ciprofloxacin microspheres may be safe and
effective controlled drug delivery over an extended period which can increase
bioavailability, patient compliance, and decrease dosing frequency.
3. Abdul Hafeez et al., (2017), formulated and evaluated Cefpodoxime Proxetil
floating microsphere.The microspheres were prepared by solvent diffusion method
using different ratios of Cefpodoxime proxetil, hydroxyl propyl methyl cellulose
(HPMC K15M) and ethyl cellulose. In-vitro release of formulation F7 in pH 1.2
HCl buffer and in simulated gastric fluid were 67.52% and 68.32% respectively.
25-Apr-2023 Nandha College of Pharmacy 4
5. 4. Noopur Pandey et al., (2016) formulated and evaluated the floating microspheres
of nateglinide Floating microspheres were prepared by oil-in-water emulsion
solvent evaporation technique using ethyl cellulose and eudragit S-100 as release
retarding polymers. The prepared microspheres showed prolonged drug release of
12 h and remain buoyant for more than 12 h.
5. Anand Panchakshari Gadad et al., (2016) formulated and evaluated
Gastroretentive Floating Microspheres of Lafutidine a second generation histamine
H2–receptor antagonist were prepared by ionotropic gelation technique by using
sodium alginate, HPMC K4M, ethyl cellulose as polymers, sodium bicarbonate as
gas generating agent and calcium chloride as cross linking agent. The in-vitro
buoyancy was found to be in the range of 67.3%-87% and a total buoyancy time of
more than 10 h. The in-vitro dissolution studies showed a cumulative % release in
the range of 57.15%-87.43%.
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6. AIM & OBJECTIVE
Aim:
Managing hypertension continues to be challenging with the currently
available drugs, since they have poor bioavailability by oral route and due to
toxicity at higher doses. The solubility and dissolution behavior of a drug is the
key determinant to its oral bioavailability. Improvement of oral bioavailability
of poor water soluble drugs remains to be one of the most challenging aspects
of drug development.
Under Biopharmaceutical classification system (BCS), Nebivolol is
classified as classII drug having poor solubility and high permeability.
Hence it considered as rate-limiting step in bioavailability.
This research work aims to increase the bioavailability of Nebivolol by
developing Nebivolol microsphere by emulsion solvent diffusion method
using the different polymers HPMC and ethyl cellulose.
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7. Objective:
The objectives of present study as follows:
• The main objective of the present study is to carryout formulation and
evaluation of microsphere of nebivolol by using suitable polymers to
improve its bioavailability.
• Preformulation studies for selection of suitable excipients to develop the
dosage form based on physiochemical properties of drug and excipients.
• Screening of excipients for compatibility and efficacy for developing the
formulation.
• Carry out preformulation study of Nebivolol drug.
• Preparation of microsphere drug delivery system for enhancing the
solubility and thus bioavailability of drug.
• The characterization of the prepared Nebivolol microsphere.
• In-vitro and In-vivo evaluation of Nebivolol microsphere.
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8. Drug Profile
Nebivolol Hydrochloride
• STUCTURE:
• CHEMICAL NAME:
(1RS,1’RS)-1,1’–[(2RS,2’SR)-bis(6-flurochroman-2-yl)]-2,2’–
iminodiethanol hydrochloride.
• MOLECULAR FORMULA:
C22H25F2NO4, HCl
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,HCl
9. • DESCRIPTION:
A white to off-white powder.
• MOLECULAR WEIGHT:
441.9 g/mol.
• STORAGE:
It is protected from moisture, at a temperature not exceeding 30ºC.
• DOSE:
2.5mg, 5mg, 10mg, 20mg.
• SOLUBILITY:
Sparingly soluble in dimethyl formamide, slightly soluble in methanol
and in DMSO(88 mg/ml at 25°C),
• DRUG CLASS:
Nebivolol is used for treating people with high blood pressure. This
medication belongs to a class of drugs known as beta blockers.
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10. • BCS CLASS:
Class II drug (low solubility and high permeability)
• PHARMACOKINETIC PROPERTIES:
Pharmacokinetics data about Nebivolol HCl are as follow:
Oral bioavailability : 12% due to extensive first pass hepatic metabolism
Bound in plasma : 98% bound to plasma proteins, mostly to serum
albumin.
Urinary excretion : 67%
Half life : approximately 8hrs
Gastric retention time: 2.6min
• MECHANISM OF ACTION:
Nebivolol is a beta blocker which blocks beta adrenergic receptors in
the sympathetic nervous system.
• SIDE EFFECTS:
headache, tiredness, weakness, dizziness, diarrhea, nausea, stomach
pain, difficulty falling asleep or staying asleep
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11. Polymer Profile
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Ethyl Cellulose
• Synonym: Aquacoat, Ethocel, Surlease.
• Chemical name: Cellulose ethyl ether.
• Functional category: Coating agent, tablet binder, viscosity increasing
agent.
• Application in Pharmaceutical formulations:
Ethyl cellulose is widely used in oral and topical pharmaceutical
formulations. The main use of ethyl cellulose in oral formulation it is used as a
hydrophobic coating agent for tablet and granules
• Description:
Ethyl cellulose is tasteless, free flowing, white or light tan coloured
powder.
• Solubility:
Insoluble in glycerine, propylene glycol, and water. Ethyl cellulose
that contains not less than 46.5% 0f ethoxy group is freely soluble in
chloroform, ethanol, ethyl acetate, methanol and toluene.
12. Polymer Profile
• Synonym: Hypermellose, Celacol, Metolose.
• Chemical name: Cellulose hydroxypropyl methyl ether.
• Functional category: Coating agent, tablet binder, viscosity increasing
agent.
• Application in Pharmaceutical formulations:
Ethyl cellulose is widely used in oral and topical pharmaceutical
formulations. In oral formulation Hypermellose is used as a tablet binder, in
film-coating, and as matrix for use in extended-release tablet formulations.
• Description:
Ethyl cellulose is odorless, tasteless, white or creamy-white fibrous or
granular powder.
• Solubility:
It is soluble in cold water and forming a viscous colloidal solution,
practically insoluble in chloroform, ethanol (95%) and ether. But it is soluble
in mixtures of ethanol and dichloromethane
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HPMC
13. Plan of Work
The present work was carried out to prepare and evaluate Nebivolol
microsphere with HPMC and EC as polymers in various proportions. The
following experimental protocol was done therefore to allow a systemic
approach to the study.
Review of literature
Procurement of drug and raw material.
Preformulation study.
Preparation of standard curves.
Formulation of Nebivolol microspheres.
In-vitro evaluation of Nebivolol microspheres.
FT-IR analysis.
Saturation solubility
Buoyancy percentage.
Buoyancy lag time.
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14. Drug Entrapment efficiency.
Percentage yield of microspheres.
Drug content determination.
Surface morphology.
In-vitro drug release study.
Powder X-ray Diffraction.
Differential Scanning Calorimetry.
In-vivo evaluation of prepared Nebivolol microspheres.
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15. Preformulation study
• Organoleptic properties:
Color: A white to off-white powder.
Odour: Odourless.
Appearance: Amorphous powder.
• FT-IR analysis:
The IR absorption spectrum of Nebivolol was obtained using FTIR
spectrophotometer by employing Potassium Bromide (KBR) pellet
technique.
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19. Transition
Absorption wave number (cm-1)
Nebivolol HPMC EC Drug+
HPMC
Drug+EC Drug+
HPMC+EC
(Aromatic)
C=C
1492.80 - - 1493.77 1492.80 1492.80
(Halogen)
F
1215.07 - - 1215.07 1215.07 1258.47
(Lactone)
C-O-C
1258.47 1153.35 1279.68 1142.74 1258.47 1215.07
-OH 3195.83 3392.55 3488.02 3205.41 3207.40 3210.29
NH- 3417.63 - - 3418.59 3468.74 3465.84
-CH2 - 2837.09 2899.78 2924.85 2928.71 2901.70
-CH3 - 2905.56 2873.74 2875.67 2874.70 2977.89
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FT-IR analysis
There was no disappearance and appearance of peaks in combined
spectra that indicated good drug – polymer compatibility and no chemical
interaction between Nebivolol and the polymers.
20. • Melting point(MP) analysis:
Melting point determination of the obtained nebivolol drug was done by
open capillary method.
Nebivolol drug was compacted into capillary tubes each 6mm long and
1mm diameter.
The capillaries were introduced vertically into the equipment, with
heating 10ºC per minute. The reading was performed three times.
Melting point of the drug was noted and compared with the melting
point of reference sample cited in Indian pharmacopeia.
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The melting point of the Nebivolol was found to be in the range of
228℃-230℃ and it was matched with literatures, which assured the identity
of received sample.
• Solubility analysis:
As per I.P. Nebivolol HCl is sparingly soluble in dimethyl formamide,
slightly soluble in methanol.
Nebivolol HCl is soluble in DMSO, Methanol, Acetone,
Dichloromehane, Ethanol
21. • Determination of absorbance maxima (λmax):
The standard stock solution was scanned in range of 200-400nm in UV
spectrophotometer using 0.1N HCl as blank. The absorbance maximum was
found to be 281nm. The absorption maxima of nebivolol was noted and
compared with the λmax of reference sample cited in Indian pharmacopeia.
• Preparation of Calibration curve:
Stock solution is prepared and from the stock solution transfer the 10ml
to 100ml volumetric flask for first dilution make up to 100ml by using
buffer solution to get 100μgml solution.
From this stock solution 1,2,3,4,5,6,7,8,9 and 10ml were withdrawn to
10ml volumetric flask and made up volume with 0.1N HCl buffer to get
a concentration range of 10-100μgml,
The absorbance of these solutions was measured at 281nm using UV
spectrophotometer.
0.1N HCl buffer was used as blank. Then calibration curve was plotted
between concentration and absorbance.
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22. 25-Apr-2023 Nandha College of Pharmacy 22
Calibration curve of Nebivolol HCl
R² = 0.997
0
0.01
0.02
0.03
0.04
0.05
0.06
0 20 40 60 80 100 120
Absorbance
at
281nm
Concentration
24. Preparation of Nebivolol floating microspheres
Emulsion solvent diffusion method.
24
25-Apr-2023 Nandha College of Pharmacy
Drug and Polymer(HPMC and EC) was dispersed in the solvent
(dichloromethane and ethanol in ratio 1:1v/v)
Then the slurry was introduced into 20ml of water containing
(0.75% w/v) PVA , SLS and Tween80
Now this mixture is maintained at a constant temperature of
40ºC with continuous stirring at 1200rpm with mechanical
stirrer for 2hrs
Then the formed microspheres was filtered washed with water
and dried at room temperature on a desiccator for 24hrs
25. Microscopic image of prepared microspheres
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26. • Determination of percentage yeild:
Nebivolol loaded microspheres was weighed after drying. Percentage
yeild was calculated by:
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practical weight of microspheres obtained
Theoretical weight
% yeild =
S.No Formulation code Percentage yeild
1. F1 75.26%
2. F2 68.60%
3. F3 89.77%
4. F4 23.65%
5. F5 74.40%
6. F6 48.85%
7. F7 90.32%
Percentage yeild of microsphere formulations
x 100
27. • Drug content:
The prepared microsphere formulation of Nebivolol was tested for their
drug content. 5mg of prepared formulation was properly mixed with 0.1N
HCl buffer and then the total content was analysed at 281nm by using UV
spectrophotometer.
25-Apr-2023 Nandha College of Pharmacy 27
Drug content =
Sample absorbance
Standard absorbance
x 100
S.No Formulation code % Drug content
1. F1 74.08%
2. F2 71.65%
3. F3 76.51%
4. F4F 60.32%
5. F5 70.85%
6. F6 77.73%
7. F7 87.04%
Drug content of Nebivolol microsphere
30. Works to be followed
Particle size determination.
Drug Entrapment efficiency.
Surface morphology.
In-vitro drug release study.
Powder X-ray Diffraction.
Differential Scanning Calorimetry.
In-vivo evaluation of prepared Nebivolol microspheres
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In-vitro evaluation of prepared Nebivolol microspheres
31. References
1. Swapnila Vanshiv D, Hemant Joshi P, Athul Sherje P, Gastroretentive Drug
Delivery System: Review. Journal of Pharmacy Research 2009; 2:12.
2. Wang HT, Schmitt E, Flanagan DR, Linhardt RJ. Influence of formulation methods
on the In-vitro controlled release of protein from poly (ester) microspheres.
J.Control Rel.1991;17;23-32.
3. Jae HP, Mingli Ye, Kinam Park, Biodegradable polymers for microencapsulation of
drug molecules. 2005, 10:146-61.
4. Kalus JS, Salinitri FD Nebivolol: A beta antagonist with novel pharmacologic
properties. Formulary.2004; 39: 532–541.
5. Rajeswari KR, Sankar GG, Rao AL, Raju DB, Rao JVLNS RP-HPLC method for
the estimation of nebivolol in bulk and pharmaceutical dosage form. Asian J
Chem,2005; 17: 1259–1263.
6. Abdul Hafeez, Ashok Kumar and Shmmon Ahmad: Formulation and in vitro
evaluation of cefpodoxime proxetil gastro retentive microspheres. The Pharma
Innovation Journal 2018; 7(1): 340-345.
7. Kauslya Arumugam, Payal D. Borawake, Jitendra V. Shinde: formulation and
evaluation of floating microspheres of ciprofloxacin by solvent evaporation method
using different polymers International Journal of Pharmacy and Pharmaceutical
Sciences,2021; Vol 13, Issue 7.
31
25-Apr-2023 Nandha College of Pharmacy
32. 8. Noopur pandey*, dr. Archana negi sah, kamal mahara, Formulation and evaluation
of floating microspheres of nateglinide,2016; ISSN : 0975-9492 vol. 7.
9. S.S. Badve, P. Sher, A. Korde, A.P. Pawar, Development of hollow/porous calcium
pectinate beads for floating-pulsatile drug delivery, Eur. J. Biopharmaceut.2007; 65
(1) 85–93.
10. M. Chordiya, H. Gangurde, K. Senthilkumaran, L. Kothari, Formulation
development and in vitro evaluation of gastroretentive hollow microspheres of
famotidine,; Int. J. Pharmaceut. Invest.2011; 1,105
11. Anand Panchakshari Gadad* , Sneha Shripad Naik, Panchaxari Mallappa Dandagi
and Uday Baburao Bolmal, Formulation and evaluation of gastroretentive floating
microspheres of lafutidine indian journal of pharmaceutical education and
research,2016 Vol 50, Issue 2.
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