scholarly journals FORMULATION AND EVALUATION OF GASTRORETENTIVE TABLETS OF ANTIULCER DRUG

2016 ◽  
Vol 9 (6) ◽  
pp. 48
Author(s):  
Pranali Shivaji Salunkhe
Keyword(s):  
Drug Release ◽  
Extended Period ◽  
Lag Time ◽  
In Vitro Dissolution ◽  
Content Uniformity ◽  
In Vitro Drug Release ◽  
Gastric Residence Time ◽  
Target Drug ◽  
Weight Variation

ABSTRACTGastroretentive floating drug delivery system is utilised to target drug release in the stomach or to the upper part of intestine. Lansoprazole is proton pump inhibitor intended for oral administration used as antiulcer agent. The present investigation involved formulation and evaluation of Gastroretentive floating tablets of Lansoprazole for prolongation of gastric residence time with a view to deliver the drug at sustained and controlled manner in gastrointestinal tract. The tablets of Lansoprazole were prepared by direct compression method using gas generating agent and different polymer combinations (HPMCK4M, HPMC K100M, Psyllium husk) . The prepared tablets of Lansoprazole were evaluated for hardness, thickness, friability, weight variation, drug content uniformity, buoyancy lag time, total floating time, swelling index, in-vitro dissolution study. The varying concentration of gas generating agent and polymers were found to affect on in-vitro drug release, floating lag time and swelling index. In vitro drug release of floating Gastroretentive tablet of Lansoprazole shown that the formulation F2 was found to be the best formulation as it releases 97.9% Lansoprazole in a controlled manner for extended period of time (upto 12 hrs.)Keywords: Lansoprazole, Gastroretentive, floating tablet, total floating time.

scholarly journals Development and evaluation of miconazole mucoadhesive tablets for oropharyngeal candidiasis

2017 ◽  
Vol 16 (10) ◽  
pp. 2325-2330
Author(s):  
Qiong Jin ◽  
Wei Chen ◽  
Wan Wu
Keyword(s):  
Drug Release ◽  
Factorial Design ◽  
Hydroxypropyl Methylcellulose ◽  
Extended Period ◽  
Content Uniformity ◽  
Oropharyngeal Candidiasis ◽  
In Vitro Drug Release ◽  
Weight Variation ◽  
Mucoadhesive Tablets

Purpose: To develop mucoadhesive tablets containing miconazole (MCZ) for the treatment of oropharyngeal candidiasis, using chitosan and hydroxypropyl methylcellulose (HPMC) as mucoadhesive polymers.Methods: Mucoadhesive tablets were formulated and optimized using a 23 factorial design and direct compression method. The independent variables were compression force and concentrations of chitosan and HPMC, while mucoadhesion time and in vitro drug release were dependent variables. Tablet characterization was carried out by evaluating hardness, thickness, tablet weight variation, content uniformity, friability and in vitro drug release at salivary pH (pH 6.8).Results: The tablets showed good mucoadhesion for an extended period (8 h), and their physical characteristics were within acceptable ranges. Drug release ranged from 60.5 % to 80.8 %.Conclusion: These results indicate that the mucoadhesive MCZ tablets formulated with chitosan and HPMC possess potential for the development of therapeutic preparations for management of oropharyngeal candidiasis.Keywords: Miconazole, Oropharyngeal candidiasis, Factorial design, Mucoadhesion, Chitosan, Drug release

scholarly journals Formulation Development and Evaluation of Sustain Release Gastroretentive Floating Tablets of Prochlorperazine Dimaleate

2019 ◽  
Vol 9 (4-s) ◽  
pp. 445-450
Author(s):  
Bharti Patle ◽  
Vivek Jain ◽  
Shradha Shende ◽  
Prabhat Kumar Jain
Keyword(s):  
Drug Delivery ◽  
Drug Release ◽  
Extended Period ◽  
Lag Time ◽  
In Vitro Dissolution ◽  
Compression Method ◽  
In Vitro Drug Release ◽  
Floating Tablets ◽  
Gastro Retentive

Floating drug delivery systems are the gastroretentive forms that precisely control the release rate of target drug to a specific site which facilitate an enormous impact on health care. The purpose of this research was to develop a novel gastro retentive drug delivery system based on direct compression method for sustained delivery of active agent to improve the bioavailability, reduce the number of doses and to increase patient compliance. Gastro retentive floating tablets of Prochlorperazine dimaleate (PCZ) were prepared by direct compression method using altered concentrations of HPMC K4, HPMC K15 and PVP K30 as polymers. The prepared tablets of PCZ were evaluated for hardness, thickness, friability, weight variation, drug content uniformity, buoyancy lag time, total floating time, in-vitro dissolution study, etc. All the compositions were resulted in adequate Pharmacopoeial limits. Compatibility studies was execution during FTIR shown that there was absence of probable chemical interaction between pure drug and excipients. The varying concentration of gas generating agent and polymers was found to affect on in-vitro drug release and floating lag time. In vitro drug release of floating gastro retentive tablet of PCZ shown that the formulation F9 was found to be the best formulation as it releases 98.89% in a controlled manner for an extended period of time (up to 12 hrs). The release data was fitted to various mathematical models such as Higuchi, Korsmeyer-Peppas, First order and Zero order to evaluate the kinetics and mechanism of the drug release. The optimized formulation (F9) showed no significant change in physical appearance, drug content, floating lag time, in vitro dissolution studies after 75%±5% RH at 40±20C relative humidity for 6 months.  Prepared floating tablets of PCZ may prove to be a potential candidate for safe and effective controlled drug delivery over an extended period of time for gastro retentive drug delivery system. Keywords: Prochlorperazine dimaleate, Floating tablet, Gastro retentive, Total floating time.

scholarly journals Formulation design, optimization & in vitro evaluation of novel orodissolving tablets of efavirenz for hiv infections

2015 ◽  
Vol 49 (3) ◽  
pp. 173-180
Author(s):  
T Ayyappan ◽  
C Poojitha ◽  
T Vetrichelvan
Keyword(s):  
Drug Release ◽  
In Vitro Dissolution ◽  
Dissolution Time ◽  
Disintegration Time ◽  
In Vitro Drug Release ◽  
Drug Content ◽  
Sodium Starch Glycolate ◽  
Weight Variation ◽  
Wetting Time

In the present work, orodissolving tablets of Efavirenz were prepared by direct compression method with a view to enhance patient compliance. A 23 full factorial design was applied to investigate the combined effect of three formulation variables. Amount of crospovidone, croscarmellose sodium and sodium starch glycolate were used as superdisintegrant material along with direct compressible mannitol to enhance mouth feel. The prepared batches of tablets were evaluated for hardness, friability, weight variation, disintegration time, wetting time, drug content and in-vitro dissolution studies. Based on wetting time, disintegration time, the formulation containing crospovidone (5% w/v), carscarmellose sodium (5% w/v) and sodium starch glycolate (8% w/v) was found to be promising and tested for in-vitro drug release pattern (in 0.1 N HCl), short term stability and drug- superdisintegrants interaction. Surface response plots are presented to graphically represent the effect of independent variables (conc. of superdisintegrants) on the in-vitro dissolution time. The validity of the generated mathematical model was tested by preparing extra-design check point formulation. The formulation showed nearly faster drug release compared to the conventional commercial tablet formulation. Stability studies on the optimized formulation indicated that there was no significant change found in physical appearance, hardness, disintegration time, drug content and in-vitro drug release. DOI: http://dx.doi.org/10.3329/bjsir.v49i3.22131 Bangladesh J. Sci. Ind. Res. 49(3), 173-180, 2014

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 Evaluation of Floating Matrix Tablets of Sacubitril and Valsartan

2019 ◽  
Vol 9 (4-s) ◽  
pp. 298-309
Author(s):  
Sudhakar Pathak ◽  
Harish Pandey ◽  
Sunil Kumar Shah
Keyword(s):  
Drug Delivery ◽  
Drug Release ◽  
Lag Time ◽  
Matrix Tablets ◽  
In Vitro Dissolution ◽  
Potential Candidate ◽  
In Vitro Drug Release ◽  
Gastric Emptying Rate ◽  
Floating Tablets

Floating Drug Delivery Systems (FDDS) have a bulk density lower than gastric fluids and thus remain buoyant in the stomach for a prolonged period of time, without affecting the gastric emptying rate. While the system is floating on the gastric contents, the drug is released slowly at a desired rate from the system. These floating tablets mainly prepared for reduction of lag time and release the drug up to 12 hours and may also increase the bioavailability of the drugs by utilizing the drug to full extent avoiding unnecessary frequency of dosing. The purpose of this research was to develop and evaluated floating matrix tablets of sacubitril and valsartan. The floating matrix tablets of sacubitril and valsartan were prepared by direct compression method using altered concentrations of HPMC K4M, HPMC K100M, sodium alginate as polymers and sodium bicarbonate, citric acid as gas generating agent. FTIR, DSC studies conformed that there was no incompatibility between the polymers and the drug. Tablet preformulation parameters were within the pharmacopoeias limit. Tablets were evaluated by different parameters such as weight uniformity, content uniformity, thickness, hardness, in vitro release studies, buoyancy determination and kinetic analysis of dissolution data. The varying concentration of gas generating agent and polymers was found to affect on in-vitro drug release and floating lag time. Tablet showed ≤ 1min lag time, continuance of buoyancy for >12 h. The in-vitro drug release pattern of sacubitril and valsartan optimized floating tablets (F16) was fitted to different kinetic models which showed highest regression (r2 = 0.9838) for Higuchi model. The Optimized formulation (F16) showed no significant change in physical appearance, drug content, floating lag time, in vitro dissolution studies after 75%±5% RH at 40±20C relative humidity for 6 months.  Prepared floating tablets of sacubitril and valsartan may prove to be a potential candidate for safe and effective controlled drug delivery over an extended period of time for gastro retentive drug delivery system.  

Design and Evaluation of Rectal Suppositories of Carvedilol

2009 ◽  
Vol 2 (3) ◽  
pp. 654-660
Author(s):  
P. V. Swamy ◽  
Laeeq Farhana ◽  
S. B. Shirsand ◽  
Md.Younus Ali ◽  
Ashokgoud Patil
Keyword(s):  
Drug Release ◽  
Significant Degree ◽  
Water Soluble ◽  
In Vitro Dissolution ◽  
Physical Parameters ◽  
Content Uniformity ◽  
Drug Content ◽  
Weight Variation ◽  
Rectal Suppositories

Carvedilol (non-cardio selective b-blocker) is an antihypertensive used in management of hypertension, angina pectoris and heart failure.  But its oral bioavailability is about 25-35% only due to significant degree of first pass metabolism.  It has gastrointestinal side effects such as diarrhea, gastric pain and irritation.  Hence, rectal suppositories of carvedilol were developed by using different water-soluble polymeric bases like gelatin and agar-agar using propylene glycol as plasticizer. The gelatin suppositories were disintegrating/dissolving type while gelatin–agar based suppositories were non-disintegrating/non-melting. All the formulations were evaluated for various physical parameters like weight variation,  drug content uniformity, liquefaction time, micro-melting range, in vitro dissolution, short-term stability and drug-excipient interaction (FTIR).  The mechanism of drug release was diffusion controlled and follows first order kinetics in majority of cases. The results suggested that when gelatin is replaced up to 25% w/w with agar, liquefaction time and drug release were not appreciably affected; higher proportions of agar exhibited incomplete and slow release.  Stability studies conducted at 25±3º C and 60±5% relative humidity for three months indicated that the formulations were stable in the drug-content and in vitro drug release rate (p<0.05).

Design, in vitro and in vivo Evaluation of Gemifloxacin Mesylate Floating Matrix Tablets

1970 ◽  
Vol 9 (1) ◽  
pp. 3143-3149
Author(s):  
Sushma Appala ◽  
Ramesh Bomma ◽  
Kishan Veerabrahma
Keyword(s):  
Helicobacter Pylori ◽  
Drug Release ◽  
Lag Time ◽  
Matrix Tablets ◽  
In Vivo Evaluation ◽  
In Vitro Drug Release ◽  
Weight Variation ◽  
Gastro Retentive

Objective of the investigation was to develop gastro retentive dosage form of gemifloxacin mesylate for local action in the stomach as it has antibacterial activity against Helicobacter pylori. Gemifloxacin mesylate is a synthetic broad-spectrum antibacterial agent for oral administration, having 7 hrs half-life and 71% oral bioavailability. In present study, gemifloxacin mesylate floating matrix tablets were prepared by direct compression method using polymers (HPMC K4M, HPMC K15M and polyox WSR 1105) and evaluated for various parameters like drug content, floating behavior (floating lag time and total floating time), in vitro drug release, swelling index, weight variation, friability, hardness and thickness. Sodium bicarbonate was incorporated as gas generating agent in all formulations. Drug-excipients compatibility was studied by Differential Scanning Calorimetry. Results have shown that the amount of polymer in the formulation affected the drug release. Optimized formulation (F8 containing polyox WSR1105 as release retarding agent) was selected based on in vitro drug release, floating lag time, floating time and other parameters. This formulation followed zero order kinetics and non-Fickian mechanism of drug release. In vivo radiographic study was conducted in healthy human volunteers using tablets containing BaSO4 as radio opaque agent. The average residence time was found to be 4.5± 0.86 h (n=3). This design of gastro retentive drug delivery system helps in increasing the local delivery of drug in patients with Helicobacter pylori infection

Theoritical Uses of Pramipexole dihydrochloride in Parkinson's Resistance Depression

2017 ◽  
Vol 1 (2) ◽  
pp. 01-03
Author(s):  
Samuel Langhorne
Keyword(s):  
Drug Release ◽  
Dopamine D2 Receptor ◽  
In Vitro Dissolution ◽  
Molecular Formula ◽  
Dissolution Profile ◽  
Drug Release Profile ◽  
In Vitro Drug Release ◽  
Weight Variation ◽  
Pramipexole Dihydrochloride

Pramipexole dihydrochloride monohydrate is an antiparkinson’s agent which is known as dopamine D2 receptor agonist. It is structurally different from the ergot-derived drugs, e.g. bromocriptine or pergolide. Pramipexole is designated chemically as (S)-2-Amino-4, 5, 6, and 7-tetrahydro-6-(propylamino) benzothiazole and has the molecular formula C10H17N3S. It comes under class I of Biopharmaceutical Classification System. The purpose of this study was to develop and evaluate pramipexole dihydrochloride monohydrate extended release tablets by wet granulation method using different proportions of polymers and binder. Pre-formulation studies were done initially and the results were found to be within the limits. All the mentioned batches were prepared and granules were evaluated for pre-compression parameters such as loss on drying, bulk density, tapped density and compressibility index. Tablets were evaluated for weight variation, thickness, hardness, friability; disintegration time and assay were found to be within the limits. In vitro dissolutions were performed with 0.05M 6.8 PH phosphate buffer and effect of various polymers were explored. Final selection of formulation was based on dissolution profile, from dissolution studies formulation 9 showed 80% drug release within 20 hours, so it will be compared with innovator. Similarity and difference factors which revealed that formulation (F 9) containing HPMC K 200, Eudragit L100 and binder are most successful as it exhibited in vitro drug release that matched with innovator product. In vitro drug release profile reveals that with increased concentration of Eudragit L 100. Accelerated stability studies were performed for the optimized batch which indicated that there were no changes in drug content and in vitro dissolution.

scholarly journals Preparation and in-Vitro Evaluation of Cinnarizine Raft Forming Chewable Tablets

2019 ◽  
pp. 42-53
Keyword(s):  
Drug Release ◽  
Water Solubility ◽  
Content Uniformity ◽  
Compression Method ◽  
Basic Drug ◽  
In Vitro Drug Release ◽  
Weight Variation ◽  
Chewable Tablets ◽  
Optimum Formula

Cinnarizine is an anti-histaminic drug and is mainly used to treat symptoms accompanying motion sickness like vomiting and dizziness. It has low and variable bioavailability due to its low water solubility. Cinnarizine (weakly basic drug) is formulated as raft forming chewable Tablets to allow its complete dissolution at the stomach to be absorbed at the upper part of small intestine. Raft forming chewable Tablets are formulated by direct compression method using sodium alginate or pectin as raft forming agents. The prepared Tablets were evaluated for their pre and post- compression parameters and they have shown desirable results regarding evaluation of hardness, thickness, % friability, weight variation, content uniformity, raft strength, weight and volume, in addition to in-vitro drug release. Out of all the prepared formulas F1 selected as the optimum formula with 488.1mg raft strength and 92.34% drug release after 24hrs that is promising for the formulation of the raft system.

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.

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