scholarly journals Vaginal delivery of clotrimazole by mucoadhesion for treatment of candidiasis

2021 ◽  
Vol 11 (6) ◽  
pp. 6-14
Author(s):  
Monica RP Rao ◽  
Gajanan Paul
Keyword(s):  
Drug Release ◽  
Ex Vivo ◽  
Solid Dispersions ◽  
Vaginal Candidiasis ◽  
Wet Granulation ◽  
Vaginal Fluid ◽  
Eudragit L100 ◽  
Mucoadhesive Polymers ◽  
Weight Variation

The aim of this study was to prepare mucoadhesive vaginal tablets of clotrimazole for treatment of vaginal candidiasis. A combination of mucoadhesive polymers like HPMC K100M, Sodium CMC, and Eudragit L100 were used in different ratios prepare solid dispersions to enhance its solubility. Tablets were prepared by the wet granulation method. Solid dispersions were evaluated for saturation solubility. All tablet batches were evaluated for weight variation, hardness, friability, drug content, swelling index, in vitro drug release study, ex vivo diffusion and mucoadhesive strength. FTIR spectra showed there was no interaction between the drug and the excipients. HPMC K100 M increased the solubility of clotrimazole in simulated vaginal fluid at pH 4.5. Eudragit L100 was shown to increase the swelling and mucoadhesive strength of the tablet, i.e., 3.03 and 3.29 g. The in vitro and ex vivo release of all 9 batches showed between 61 to 78% release in 8h. Ex vivo diffusion studies using sheep vaginal membrane showed 43 to 59% in 6h in simulated vaginal fluid. The release and flux were nearly comparable to marketed tablet i.e., Candid-V6. The drug release of all batches followed the Korsmeyer-Peppas kinetic model, and the mechanism was found to be non‐Fickian/anomalous. Keywords: Clotrimazole, solid dispersion, HPMC K100M, Eudragit L100, Sodium CMC.

scholarly journals Exploration of neem gum-chitosan and kheri gum-chitosan polyelectrolyte complex based film for transdermal delivery of protein/peptide

2020 ◽  
Vol 10 (4) ◽  
pp. 5860-5868
Keyword(s):  
Drug Release ◽  
Drug Concentration ◽  
Polyelectrolyte Complex ◽  
Ex Vivo ◽  
Extended Period ◽  
In Vitro Drug Release ◽  
Drug Permeation ◽  
Permeation Study ◽  
Weight Variation

Present investigation is continuation of author’s previously published work. In the present investigation, the author has prepared neem gum-chitosan and kheri gum-chitosan polyelectrolyte complex transdermal film for the delivery of protein/peptide drug. Concentration of gum (neem gum and kheri gum) and chitosan was varied in each concentration while drug concentration kept constant. Albumin was used as a model protein drug. Transdermal films were fabricated using a solvent casting method without using any plasticizer and evaluated for various parameters viz. folding endurance, surface pH, weight variation, drug content, percentage moisture content, surface morphology, in vitro drug release and ex vivo drug permeation study. The study showed that films were successfully fabricated with good acceptable physical properties. In vitro drug release study and ex vivo drug permeation study showed that polyelectrolyte films were able to extend drug delivery up to 9 days. It can be easily concluded from the findings of the results that neem gum-chitosan and kheri gum-chitosan polyelectrolyte complex films can be easily prepared without using any plasticizer and able to deliver protein/peptide therapeutic agents for an extended period of time.

scholarly journals Formulation and In-Vitro Evaluation of Sustained Release Matrix Tablets of Domperidone

2020 ◽  
Vol 8 (02) ◽  
pp. 40-45
Author(s):  
Chhitij Thapa ◽  
Roma Chaudhary
Keyword(s):  
Drug Release ◽  
Sustained Release ◽  
Epigastric Pain ◽  
Matrix Tablets ◽  
Angle Of Repose ◽  
In Vitro Dissolution ◽  
Wet Granulation ◽  
In Vitro Drug Release ◽  
Weight Variation

INTRODUCTION Domperidone is a unique compound with gastro kinetic and antiemetic effects. It is used in the management of disorder by impaired motility like gastroesophageal reflux (in some instances), gastroparesis, dyspepsia, heartburn, epigastric pain, nausea, vomiting, and colonic inertia. The sustained release system is a widely accepted approach for slow drug release over an extended period to address the challenges of conventional oral delivery, including dosing frequency, drug safety, and efficacy. The study aims to formulate a domperidone sustained release tablet and compare the dissolution rate with the marketed formulations. MATERIAL AND METHODS Sustained release matrix tablets of domperidone were prepared by wet granulation method using different polymers such as HPMC K4M, ethyl cellulose, Gum acacia. Pre-compression studies like angle of repose, bulk density, tapped density, Carr's index, and Hausner’s ratio, and post-compression studies like weight variation, thickness, hardness, friability, drug content, and in-vitro drug release were evaluated.   RESULTS The release profile of domperidone sustained-release tablets was studied spectrophotometrically. The in-vitro dissolution study suggests the minimum %-cumulative drug release with 98.33% in F5. The %-cumulative drug release was maximum in F3 with 99.69%. The in-vitro drug release of all the formulations was non-significant compared to the marketed formulation (p<0.05), exhibiting the sustained-release property by all the formulations. CONCLUSION The pre-compression study concludes the better flow property of the granules of different formulations. The sustained release domperidone tablets were prepared successfully by the wet granulation method. The post-compression parameters of different formulations were within the acceptable range.

scholarly journals Formulation and evaluation of matrix tablets of Eperisone hydrochloride

2020 ◽  
Vol 1 (4) ◽  
pp. 131-136
Author(s):  
Peruboina Neelima ◽  
Maddula Venkata Ramana
Keyword(s):  
Drug Release ◽  
In Vitro Release ◽  
Hepatic Metabolism ◽  
Magnesium Stearate ◽  
Matrix Tablets ◽  
Spinal Reflexes ◽  
Wet Granulation ◽  
Physical Parameters ◽  
Weight Variation

The aim of the present research is to develop and optimize Eperisone Hydrochloride extended release matrix tablets. Eperisone Hydrochloride is an antispasmodic drug mainly used to relieve pains it acts by relaxing the skeletal and smooth vascular muscles by blocking spinal reflexes drug which has oral bioavailability of 70% due to hepatic metabolism. Sustained release matrix tablets of Eperisone Hydrochloride were prepared through wet granulation technique by using HPMC K4M and EC as polymers, PVPK30 as binder, Magnesium stearate as lubricant and Talc as glidant. The granules of different formulations were determined for pre compression parameters. The prepared granules along with the excipients were then compressed. The formulated tablets were evaluated for physical characteristics viz. Hardness, Thickness, % Weight variation, Friability and the drug content. Furthermore the tablets evaluated for the in vitro release studies. Out of all the 8 formulations F7 showed desired characteristics in the physical parameters and in vitro drug release of 85.48% in 12hrs.The F7 dissolution data was best fitted to the Zero order model. The prepared Eperisone Hydrochloride matrix tablets found to be having a potential extended drug release.

scholarly journals Formulation, Optimization and in vitro Characterization of Stavudine Gastro Retentive Floating Matrix Tablets

2016 ◽  
Vol 8 (03) ◽  
Author(s):  
Mahendar Rupavath ◽  
Kranthi G. ◽  
Chinna Palem ◽  
K. S. K. Patnaik
Keyword(s):  
Drug Release ◽  
Hydroxypropyl Methylcellulose ◽  
Matrix Tablets ◽  
Release Mechanism ◽  
Wet Granulation ◽  
Drug Bioavailability ◽  
In Vitro Drug Release ◽  
Weight Variation

The aim of the present investigation was to develop floating matrix tablets of stavudine to achieve prolong gastric residence time, leading to an increase in drug bioavailability and patient compliance. Floating tablets were prepared by wet granulation technique, using hydroxypropyl methylcellulose (HPMC K15M) as synthetic, pullulan gum as natural rate controlling polymers and optimum amounts of sodium-bicarbonate and citric acid as gas generating agents in suitable ratios to generate optimum buoyancy. Developed formulations were evaluated for weight variation, thickness, hardness, friability, drug content, in vitro drug release, floating lag time and floating buoyancy. All the formulations exhibited acceptable physical properties and the best formulation (F3) was selected based on in vitro characteristics. Further, the optimized formulation was evaluated for in vivo radiographic studies by incorporating BaSO4 as radio opaque substance. All the formulations were studied for in vitro drug release characteristics for 16 h. Optimized formulation showed controlled and prolonged drug release profiles while floating over the dissolution medium. Diffusion followed by erosion drug release mechanism was observed for the formulation, indicating that water diffusion and polymer erosion played an essential role in drug release. In vivo radiographic studies revealed that the tablets remained in the stomach for 8 ± 0.5 h in fasting human volunteers and indicated that gastric retention time was increased by the floating principle, which was considered and desirable for absorption window drugs.

FORMULATION AND EVALUATION OF DARIFENACIN HYDROBROMIDE TRANSDERMAL PATCH

2021 ◽  
pp. 12-14
Author(s):  
Aparna Reddy K ◽  
Latha K ◽  
Naseeb Basha Shaik ◽  
Sushma B ◽  
Haritha T ◽  
...  
Keyword(s):  
Drug Release ◽  
Physicochemical Properties ◽  
Ex Vivo ◽  
Skin Irritation ◽  
Drug Level ◽  
Immediate Release ◽  
Tween 20 ◽  
Transdermal Patch ◽  
Weight Variation

The aim of present study is to formulate and characterize darifenacin hydrobromide transdermal patch and the effects of non-ionic surfactants span 20 and tween 20 on drug permeation were studied. Transdermal patches were prepared by solvent casting method using PVA, PVP, HPMC E5, HPMC E15 polymers. Propylene glycol and Glycerol were used as plasticizers and Span 20 and Tween 20 were used as permeation enhancers. The prepared patches were evaluated for physicochemical properties like drug content, thickness, weight variation, folding endurance, moisture uptake, watervapour transmission studies. Physicochemical properties have shown better. Drug release studies by in-vitro diffusion, ex-vivo permeation as well as skin irritation. Formulations DPAT2, DPLT3 showed better drug release rate, ux and Q when compared to DPAS2, DPLS2. From the results it was concluded that darifenacin hydrobromide transdermal patch 24 (DPAT2) formulation would reduce the administration frequency, side effects and may avoid uctuations of drug level in the blood in comparison to immediate release formulations which might enhance the patient compliance.

Development of Effervescent Tablets of Alendronate Sodium with Improved Intestinal Permeation

2018 ◽  
Vol 11 (1) ◽  
pp. 3990-3997
Author(s):  
Prasad Vure ◽  
Sundeep Chaurasia
Keyword(s):  
Drug Release ◽  
Ex Vivo ◽  
Angle Of Repose ◽  
In Vitro Dissolution ◽  
Alendronate Sodium ◽  
Drug Content ◽  
Weight Variation ◽  
Permeation Studies ◽  
Intestinal Permeation

The aim of the present study is to develop effervescent tablets of alendronate sodium to improve their intestinal permeability to treat osteoporosis. Effervescent tablets of alendronate sodium were developed with different ratios of acid to alkaline components having a pH of about 3 to about 6.5. The tablets were prepared by direct compression method. The physical mixture blend was evaluated for angle of repose, true density, bulk density, compressibility index. The formulated tablets were subjected to thickness, weight variation, hardness, friability, drug content and pH. The in vitro dissolution studies were carried out using the USP Type 2 apparatus. Formulation F14 was considered as optimized formulation because it shows drug release pattern higher than that of the other formulations and conventional marketed formulation. Ex vivo permeation studies were performed for the optimized formulation (F14) and that of the conventional marketed formulation. The drug release of the formulation (F14) was higher than the marketed formulation. Accelerated stability studies of the optimized formulation indicated that there were no signs of visually distinguishable changes, drug content and in vitro dispersion time. Thus, an increase in drug release may enhance absorption, in turn may enhance bioavailability.       

scholarly journals FORMULATION AND EVALUATION OF COLON TARGETED MATRIX TABLET USING NATURAL TREE GUMS

2018 ◽  
Vol 10 (9) ◽  
pp. 92
Author(s):  
Poreddy Srikanth Reddy ◽  
Penjuri Subhash Chandra Bose ◽  
Damineni Saritha ◽  
Vuppula Sruthi
Keyword(s):  
Drug Release ◽  
In Vitro Release ◽  
Wet Granulation ◽  
Average Weight ◽  
Matrix Tablet ◽  
Weight Variation ◽  
Release Studies ◽  
Percentage Weight ◽  
Diltiazem Hcl

Objective: To develop a novel colon targeted tablet formulation using natural polysaccharides such as kondagogu gum and ghatti gum as carriers and diltiazem hydrochloride as a model drug.Methods: The polymer-drug tablets were prepared by wet granulation technique, coated with two layers viz., inulin as an inner coat followed by shellac as outer coat and evaluated for properties such as average weight, hardness and coat thickness. In vitro release studies of prepared tablets were carried out for 2 h in pH 1.2 HCl buffer, 3 h in pH 7.4 phosphate buffer and 6 h in simulated colonic fluid (SCF) in order to mimic the conditions from mouth to colon.Results: Percentage weight variation, percent friability and content of active ingredient for all the formulations were found to be well within United States Pharmacopoeia (USP) limits. Out of both the polymers, the tablets prepared with ghatti gum showed the maximum hardness of 7.1 kg/cm2. The FTIR spectra of pure diltiazem HCl and the formulation KF3 were found to be identical. From the DSC, it was evident that the melting point peak of diltiazem HCl and formulation KF3 were observed at 217.16 and 218.34 °C respectively. In vitro studies revealed that the tablets coated with shellac (2.5% w/w), prevented the drug release in stomach environment and inulin coated tablets (4% w/w) have limited the drug release in the small intestinal environment. The data obtained from in vitro drug release studies were fit into Peppas model and in all the cases the value of A was found to be more than 2, i.e., drug release by a combination of both diffusion and erosion-controlled drug release.Conclusion: The study revealed that polysaccharides as carriers and inulin and shellac as a coating material can be used effectively for colon targeting of drugs for treating local as well as systemic disorders.

scholarly journals STUDYING THE EFFECT OF DIFFERENT VARIABLES ON THE FORMULATION OF MUCOADHESIVE BUCCAL PATCHES OF CAPTOPRIL

2017 ◽  
Vol 9 (2) ◽  
pp. 16
Author(s):  
Zainab Ahmed Sadeq ◽  
Nawal Ayash Rajab
Keyword(s):  
Drug Release ◽  
Ex Vivo ◽  
Methyl Cellulose ◽  
Differential Scanning Calorimetric ◽  
Content Uniformity ◽  
Weight Variation ◽  
Film Forming ◽  
Ex Vivo Permeation Study ◽  
Calorimetric Studies

Objective: The objective of this research was to formulate the captopril as mucoadhesive buccal films for hypertension treatment and studying the effect of different variables on the physical and mechanical behavior of the prepared films.Methods: The bucco-adhesive patches were prepared using hydroxyl propyl methyl cellulose K4 (HPMC) as film forming a polymer with secondary polymer included carbopol 934 and eudragit RL100. The patches were prepared by a solvent casting method and evaluated for the weight variation, surface pH, mechanical properties, content, uniformity, ex-vivo mucoadhesive strength, ex-vivo permeation study and drug release study.Results: Formula F5 containing HPMC as primary polymer with carbopol 934 as secondary polymer was chosen to be the best formulation for the following parameters: surface pH6.44, tensile strength (16.06), percentage elongation at break (34.14), swelling index(18.85), mucoadhesive strength(26.2 gm) and the folding endurance was>300 with an in vitro drug release about 94.73% during 6 h.Fourier transforms infrared spectroscopy (FT-IR) and differential scanning calorimetric studies (DSC) showed no interaction between the drug and polymers.Conclusion: It can be concluded that oral mucoadhesive buccal film of captopril, an antihypertensive agent can be prepared utilizing HPMC as a film forming a polymer with carbopol as a secondary polymer which extended the drug release through the buccal mucosa for 6 h.

scholarly journals Formulation and In-Vitro Evaluation of Taste Masked Fast Disintegrating Tablets of Labetalol Hydrochloride by Wet Granulation Technique

2019 ◽  
Vol 9 (4-A) ◽  
pp. 442-449
Author(s):  
SM Shahidulla ◽  
Tayyaba Jeelani
Keyword(s):  
Solid Dispersions ◽  
Hepatic Metabolism ◽  
Precipitation Method ◽  
Wet Granulation ◽  
Sodium Starch Glycolate ◽  
Weight Variation ◽  
Labetalol Hydrochloride ◽  
Co Precipitation ◽  
Fast Disintegrating Tablets

Labetalol Hydrochloride is a β-blocker generally indicated for the treatment of hypertension, and it is extensively metabolized due to the hepatic metabolism. In the present work, an attempt was made to mask the taste by Solid Dispersion technique, with a formulation into Fast Disintegrating dosage form, using superdisintegrants such as Cross carmellose sodium (CCS), crospovidone (CP) and sodium starch glycolate (SSG). The complexes of Labetalol hydrochloride with HP-β-CD (1:3 ratio) were prepared by Co-precipitation method. Using the drug HP-β-CD complex, Fast Disintegrating tablets were prepared by Wet granulation Technique and evaluated for hardness, friability, weight variation, thickness, disintegrating time (DT), In-vitro dispersion time and  dissolution rate. The results of Direct compression optimized formulation WG9 (Sodium Starch Glycolate 15mg and Starch paste 18mg) has shown the % Drug release of  99.97%, In-vitro Dispersion time of 16 Secs respectively. Keywords: Solid dispersions, fast disintegrating tablets, Labetalol, Crospovidone, Croscarmellose sodium and Sodium starch glycolate.

scholarly journals FORMULATION AND EVALUATION OF ORODISPERSIBLE TABLETS OF DONEPEZIL HYDROCHLORIDE

2020 ◽  
pp. 45-51
Author(s):  
P. V. KAMALA KUMARI ◽  
Y. SRINIVASA RAO
Keyword(s):  
Drug Release ◽  
Hydroxypropyl Methylcellulose ◽  
Wet Granulation ◽  
High Concentration ◽  
Disintegration Time ◽  
In Vitro Drug Release ◽  
Orodispersible Tablets ◽  
Weight Variation ◽  
Donepezil Hydrochloride

Objective: The present study was aimed to develop the formulation and in vitro evaluation of Orodispersible tablets by wet granulation method using Donepezil HCl as a model drug to enhance patient compliance. Methods: In the wet granulation method, a mixture of microcrystalline cellulose and hydroxypropyl methylcellulose were used along with superdisintegrants, i.e., croscarmellose sodium and crospovidone. The prepared granules were subjected to both pre and post-compression evaluation parameters including; FTIR spectroscopy, micromeritics properties, tablet weight variation, hardness, friability, drug content, disintegration time and in vitro drug release. Results: FTIR studies indicated that there was nointeraction between the drug and the excipients used. The formulation containing high concentration of crospovidone and mixture as the best formulation F2 based on in vitro drug release characteristics of tablet formulation. Conclusion: The results of this work suggested that orodispersible tablets of Donepezil hydrochloride with rapid disintegration time, fast drug release and good hardness can be efficiently and successfully formulated by wet granulation method.

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