scholarly journals OPTIMIZED DELIVERY OF DICLOFENAC SODIUM FORMULATED IN A SUSTAINED RELEASE RAPHIA AFRICANA HYDROCOLLOID MATRIX

2018 ◽  
Vol 10 (1) ◽  
pp. 109
Author(s):  
Musiliu Adedokun ◽  
Clement Nkanta
Keyword(s):  
Drug Release ◽  
Sustained Release ◽  
Diclofenac Sodium ◽  
Research Work ◽  
Fickian Diffusion ◽  
In Vitro Dissolution ◽  
Content Uniformity ◽  
Flow Properties ◽  
Weight Variation ◽  
Significant Difference

Objective: The aim of this research work was to comparatively study various proportions of a natural hydrocolloid-Raphia africana, and polyvinylpyrrolidone (PVP) as release sustaining agents in diclofenac sodium tablet formulation.Methods: The purified hydrocolloid (R. africana) was characterized by evaluating its organoleptic, physicochemical and flow properties. Diclofenac-polymer ratios of 1:0, 1:0.2, 1:0.4, 1:0.6, and 1:0.8 were employed to produce different granule batches using wet granulation method (that is, the drug was formulated with 0, 5, 10, 15 and 20 % w/w of either R. africana hydrocolloid or PVP, and coded DWB-00, DRA-05, DRA-10, DRA-15, DRA-20, DPP-05, DPP-10, DPP-15 and DPP-20, respectively). Flow properties of granules were studied by determining bulk density, tapped density, Carr’s index, and Hausner’s ratio for all the formulations. Compressed tablets were evaluated using various parameters as weight variation, friability, hardness, tablet thickness and diameter, content uniformity and in vitro dissolution evaluated in phosphate buffer (pH 7.3).Results: Flowability, mechanical and release parameters determined were within pharmacopoeial limits. Generally, the values of bulk and tapped densities increase as binder concentrations increase for both PVP and R. africana hydrocolloid. The values were significantly different across the batches (p<0.05). Hardness values obtained varied significantly (p<0.05) and were between 5 and 12 KgF which imply that most of the tablet batches are harder than normal depending on the proportion of the polymer used. All the batches exhibited friability within the standard limit without significant difference in values (p>0.05), indicating that tablet formulated with the experimental binders would not undergo surface abrasion. All the formulations exhibited zero order kinetics except batches DPP-10 and DPP-15 which showed Higuchi mechanism. Formulation batches DRA-05 and DRA-10 showed maximum drug release of 98% and 95% respectively after 6 h. A prolonged drug release was observed on increasing polymer ratio. Significantly higher release rates (p<0.05) were observed in the tablets formulated with PVP than those containing R. africana gum. All the batches followed non-fickian diffusion release mechanism.Conclusion: From the study, purified R. africana hydrocolloid generally appeared to perform better than PVP as sustained release agent.

scholarly journals Formulation and evaluation of sustained release matrix tablet of captopril

2019 ◽  
Vol 9 (4-A) ◽  
pp. 260-268
Author(s):  
SIMRAN SHIVDAS PAWAR ◽  
Prashant S. Malpure ◽  
Santosh S Surana ◽  
Jayashri S Bhadane
Keyword(s):  
Drug Release ◽  
Sustained Release ◽  
Release Kinetics ◽  
Matrix Tablets ◽  
In Vitro Dissolution ◽  
Release Mechanism ◽  
Content Uniformity ◽  
Matrix Tablet ◽  
Compression Technique ◽  
Weight Variation

The objective of the present study was to study the effect of polymers on sustained release of Captopril from tablets. Compatibility was studied by Fourier transform infrared spectroscopy and DSC. The tablets were prepared by direct compression technique using Xanthan gum and Ethyl Cellulose. The prepared matrix tablets were evaluated for their physicochemical parameters such as weight variation, hardness, friability, content uniformity and in-vitro dissolution. Pre and post compression parameters were evaluated and all the parameters were found within the limit. The drug release data were subjected to different models in order to evaluate release kinetics and mechanism of drug release. Formulation F4 was selected as best formulation. The dissolution of formulation F4 can be Shows Non-fickian drug release mechanism.

scholarly journals Formulation Development and Evaluation of Rosuvastatin Sustained Release Tablets

2019 ◽  
pp. 238-247
Author(s):  
Raghavendra Kumar Gunda ◽  
Prasada Rao Manchineni
Keyword(s):  
Drug Release ◽  
Sustained Release ◽  
Drug Dissolution ◽  
Fickian Diffusion ◽  
In Vitro Dissolution ◽  
Polynomial Equations ◽  
Formulation Development ◽  
Sustained Release Formulation ◽  
Significant Difference

Purpose: The main objective of present research investigation is to formulate the sustained release formulation of Rosuvastatin. Rosuvastatin, an antihyperlipidemic agent, belongs BCS class-II agent.Methods: The SR tablets of Rosuvastatin were prepared employing different concentrations of HPMCK4M and SCMC in different combinations by Direct Compression using 32 factorial design. The concentration of Polymers , HPMCK4M and SCMC required to achieve the desired drug release was selected as independent variables, X1 and X2 respectively whereas, time required for 10% of drug dissolution (t10%), 50% (t50%), 75% (t75%) and  90% (t90%)  were selected as dependent variables.Results and Discussion: Totally nine formulations were designed and are evaluated for hardness, friability, thickness, % drug content, In-vitro drug release. From the Results it was concluded that all the formulation were found to be with in the Pharmacopoeial limits and  the In-vitro dissolution profiles of all formulations were fitted in to different Kinetic models, the statistical parameters like intercept, slope & regression coefficient  were calculated. Polynomial equations were developed for dependent variables. Validity of developed polynomial equations were verified by designing 2 check point formulations (C1, C2). According to SUPAC guidelines the formulation (F4) containing 30 mg of HPMCK4M and 40 mg of SCMC, is the most similar formulation (similarity factor f2= 89.561, dissimilarity factor f1= 1.543 & No significant difference, t= 0.0056) to marketed product (CRESTOR).Conclusion: The selected formulation (F4) follows Zero order, Higuchi’s kinetics, and the mechanism of drug release was found to be Non-Fickian Diffusion (n= 0.963).

Fabrication and Evaluation of Mouth Dissolving Strips of Metoclopramide Hydrochloride by Using Novel Film Former

2021 ◽  
pp. 5515-5520
Author(s):  
Hemant A. Deokule ◽  
Smita S. Pimple ◽  
Praveen D. Chaudhari ◽  
Ajit S. Kulkarni
Keyword(s):  
Drug Release ◽  
Research Work ◽  
Systemic Circulation ◽  
In Vitro Dissolution ◽  
Disintegration Time ◽  
Visual Appearance ◽  
Dsc Studies ◽  
Weight Variation ◽  
Metoclopramide Hydrochloride

Fast dissolving strips are used as novel approaches, as it dissolves rapidly in mouth and directly reaches the systemic circulation. In present research work, an attempt has been made to prepare mouth dissolving strips of Metoclopramide hydrochloride by using a novel film former Pullulan by solvent casting method. A33 full factorial design was utilized for the optimization of the effect of independent variables such as the amount of Pullulan, amount of PEF 400, amount of SSG on mechanical properties, and % drug release of strips. The drug compatibility studies using FTIR and DSC studies formulated strips were characterized for their physicochemical parameter like weight variation, visual appearance, folding endurance, thickness, disintegration time, drug content, and in vitro dissolution studies. FTIR and DSC studies revealed that the polymer is compatible with the drug. It was found that the optimum levels of the responses for a fast release strip could be obtained at low levels of Pullulan, PEG400, and SSG. The prepared strip was clear transparent and had a smooth surface. The surface pH was found 4.8 to 5.2 be in the range of to which is close to salivary pH, which indicates that strips may have less potential to irritate the oral mucosa, thereby they are comfortable. The drug release was found to be between 90.94 to 100.5% in 2 min. The in-vitro disintegration time of strips prepared with Pullulan was in the range of 19 to 57 sec. As the concentration of SSG increases the decrease in the disintegration time of strips a decrease. The dissolution rate increased with an increase in the concentration of SSG. Hence, it can be inferred that the fast dissolving oral strips of Metoclopramide hydrochloride may produce rapid action thereby improving bioavailability and enhance the absorption by avoiding the first-pass effect.

scholarly journals FORMUALTION AND DEVELOPMENT OF MUCOADHESIVE SUSTAINED RELEASE BUCCAL TABLETS AND PATCHES OF 5-FLUOROURACIL USING DIFFERENT POLYMERS

2018 ◽  
Vol 11 (5) ◽  
pp. 174
Author(s):  
Nitin Gawai ◽  
Zahid Zaheer
Keyword(s):  
Drug Release ◽  
Sustained Release ◽  
Research Work ◽  
Sodium Deoxycholate ◽  
Content Uniformity ◽  
Design Expert ◽  
Buccal Tablet ◽  
Buccal Tablets

 Objective: The present research study was undertaken to formulate mucoadhesive sustained release buccal tablets and patches of 5-fluorouracil (5-FU).Method: For the research experiment work design expert software version 10, stat-ease, Inc. has been used. A 32 full factorial design was selected for the formulation of the buccal tablet as well as buccal patches. In this research work, formulated tablets and patches using different polymers such as carbopol 974p, polyvinylpyrrolidone-K 30, sodium deoxycholate, microcrystalline cellulose, and polyvinyl alcohol. An after formulation of batches formulated products studied for characterization, namely, Fourier transform infrared (FTIR) and differential scanning calorimeter (DSC). Evaluation parameters studied such as weight uniformity, thickness, hardness, friability, and content uniformity also carried out. For drug release purpose from the formulation of buccal tablet and patches in vitro drug released performed. In vivo drug releases study also carried out using Rabbit for drug reaction point of view.Results: Design expert showed the significant results on independent and dependent variables. The R-Squared 0.9943 for drug release and 0.9985 for swelling index is in reasonable agreement with the formulations. FTIR and DSC indicating compatibility of the drug and polymers in the tablet formulation and patch formulations at the molecular level. The drug release of buccal tablet showed 75.10–99.34% and buccal patches showed 58.41–81.43%. These formulations showed good results when compared to the conventional tablet.Conclusion: Formulation of mucoadhesive sustained release buccal tablets and patches of 5-FU successfully done using different polymers, which would definitely help in increasing bioavailability of the drug.

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 Formulation of Metformin Sustained Release Tablet Using Natural Polymer

2021 ◽  
Vol 11 (2) ◽  
pp. 31-37
Author(s):  
Mehak Siddiqui ◽  
L. K. Omray ◽  
Pushpendra Soni
Keyword(s):  
Drug Release ◽  
Sustained Release ◽  
Guar Gum ◽  
Release Kinetics ◽  
Methyl Cellulose ◽  
Matrix Tablets ◽  
Absolute Bioavailability ◽  
Dissolution Time ◽  
Content Uniformity ◽  
Weight Variation

The overall objective of the present work was to develop an oral sustained-release (SR) Metformin tablet that is prepared by the direct compression method by using hydrophilic hydroxyl propyl methyl cellulose (HPMC) and Guar gum polymer alone as well as in combination at different concentrations. Metformin is a biguanide that has a relatively short plasma half-life. It has low absolute bioavailability. All the properties were evaluated for thickness, weight variation, hardness and drug content uniformity and in vitro drug release. The mean dissolution time is used to characterize the drug release rate from a dosage form that indicates the drug release-retarding efficiency of the polymer. The hydrophilic matrix of HPMC alone could not control the Metformin release effectively for 12 h but when combined with Guar gum, it could slow down the release of drug and, thus, can be successfully employed for formulating Sustain Release matrix tablets. Keywords: Guar gum, hydroxylpropylmethylcellulose, matrix tablets, release kinetics,

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).

Formulation and in vitro Evaluation of Matrix tablets containing Repaglinide

2021 ◽  
pp. 4429-4434
Author(s):  
C.C. Patil ◽  
J. Vekatesh ◽  
S. R Karajgi ◽  
Vijapure Vitthal ◽  
Ashwini G. ◽  
...  
Keyword(s):  
Drug Release ◽  
Sustained Release ◽  
Fourier Transforms ◽  
Methyl Cellulose ◽  
Matrix Tablets ◽  
Differential Scanning Calorimetric ◽  
Content Uniformity ◽  
Drug Content ◽  
Weight Variation

The aim of this project was to develop sustained release matrix tablets of Repaglinide. Sustained release matrix tablets of Repaglinide were prepared by the wet granulation method using polymers like Hydroxy propyl methyl cellulose, Microcrystalline cellulose, Eudragit RS-100 in different ratios. The matrix tablets of Repaglinide were evaluated for hardness, weight variation, friability, drug content uniformity, and in-vitro drug release. In order to determine the drug release mechanisms and kinetics, the data was subjected to zero order, first order, and higuchi and peppas diffusion model. Twelve batches of sustained release matrix tablets of Repaglinide were developed. Among these formulations F4, F8 and F12 formulation showed satisfactory physicochemical properties and drug content uniformity and sustained release of drug for 12 hours with maximum release of 86.95%, 84.91% and 84.91%. The optimized formulations were characterized for Differential scanning calorimetric analysis; Fourier transforms infrared spectroscopy and scanning electron microscopic studies. IR spectroscopic studies indicated that there were no drug-excipient interactions. The prepared sustained release matrix tablets of Repaglinide were successfully developed and evaluated.

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 CHARACTERIZATION OF SUSTAINED RELEASE TABLET USING MARDI GUM

2021 ◽  
pp. 52-55
Author(s):  
MANGESH M KUMARE ◽  
GIRIDHAR R SHENDARKAR
Keyword(s):  
Drug Release ◽  
Sustained Release ◽  
Hydroxypropyl Methylcellulose ◽  
Research Work ◽  
Release Mechanism ◽  
In Vitro Drug Release ◽  
Sustained Release Tablet ◽  
Weight Variation ◽  
Release Tablet

Objective: The present research work was to develop and evaluate alprazolam sustained release tablet using Mardi gum, a comparative study on binding properties of gum and hydroxypropyl methylcellulose (HPMC) was performed. Methods: Formulation of alprazolam tablets (f1–f6) was done by direct compression method using 15%, 30%, and 45% concentration of gum as a natural binder, and HPMC was used as synthetic matrix forming agent. Microcrystalline cellulose was used as diluents, talc, and magnesium stearate as a lubricant and PVP K30 as the binder. The formulated batches were evaluated for parameters such as tablet thickness, % friability, hardness, weight variation, and in vitro drug release characteristics. The release information was fitted into different dynamics models to decide the release mechanism of the drug. Results: The results showed that all the parameters of the developed tablets (f1–f6) were in fulfillment with pharmacopeia limits. In vitro, drug release studies showed that formulation f1 had most controlled and sustained manner releaser with maximum drug release of 97.89±0.52% in 18 h with comparison to f2–f4 and f6 drug release is 98.12±0.55%, 97.24±0.57%, 98.16±0.74%, and 97.26±0.35%, respectively, in 16 h and f5 giving 97.89±0.85% release in 14 h. Conclusion: On the basis of obtained result, it can be concluded that Mardi gum can be used to sustain the drug release as a natural polymer in tablet dosage form.

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