Formulation and Evaluation of Extended Release Trihexyphenidyl Hydrochloride Hard Gelatin Capsules

2011 ◽  
Vol 4 (1) ◽  
pp. 1359-1367
Author(s):  
Madhusudan Rao Y ◽  
Vinay Kumar K ◽  
Jagan Mohan S ◽  
Kiran Kumar V
Keyword(s):  
Drug Release ◽  
Extended Release ◽  
In Vitro Release ◽  
Content Uniformity ◽  
Drug Release Profile ◽  
Coupled Diffusion ◽  
Weight Variation ◽  
Release Studies ◽  
Release Profiles

This work aims at investigating different types and levels of hydrophilic high molecular weight matrix agents, (including HPMC K15M, Metalose-60 SH, Metalose-65 SH and Metalose-90SH-SR), hydrophobic diluent (Talc) and formulation methods (Non-aqueous granulation and direct filling by simple mere mixture) in an attempt to formulate hard gelatin extended release matrix capsules containing Trihexyphenidyl HCl (Benzhexol). The drug release from all the extended release matrix capsules show polymer as well as talc concentration dependent retardation affect. The Metalose 90SH-SR concentration was optimized to approximately 27% w/w of total capsule net content weight. The hydrophobic diluent’s talc concentration was optimized and the useful concentration was approximately 17.45% w/w of the total net capsule content weight. The lactose concentration was also optimized and the effective concentration was found to be approximately 48.36% w/w. The prepared hard gelatin extended release capsules were evaluated for weight variation, Average net content, locked length, content uniformity, assay (drug content) and in-vitro drug release studies. From the in-vitro release studies of the prepared formulations, one formula was optimized from each method. All the formulations showed linear release profiles and extended the release of trihexyphenidyl HCl (Benzhexol) over 10 –12 h. The release profiles of extended release matrix capsules of trihexyphenidyl HCl (THP HCl) from the selected formulations were close to zero order and follow diffusion dependent release. The prepared extended release matrix capsules of trihexyphenidyl HCl (Benzhexol) produced from the optimized formulations ‘NAG-M90SH-SR-5 and DB M90SH-SR-4’ complied with the USP XXVII specifications. The difference factor (f1) and similarity factor (f2) was calculated for all these formulations and found to the below 15 and above 50. Irrespective of the formulation method type and its procedure, the prepared hydrophilic extended release matrix capsules showed non-Fickian anomalous transport (coupled diffusion in the hydrated matrix and polymer relaxation) as the values of release exponent (n) are in between 0.50 and 0.89. Finally it was clear that it is possible to design a formulation with any of the above two methods giving the desired drug release profile suggesting that nonaqueous granulation, Direct filling were good methods for preparing extended release matrix capsules of trihexyphenidyl HCl (Benzhexol).

scholarly journals DESIGN AND IN VITRO EVALUATION OF EXTENDED RELEASE TABLET OF NATEGLINIDE

2018 ◽  
Vol 8 (5-s) ◽  
pp. 235-239
Author(s):  
NILESH M MAHAJAN ◽  
Kalyanee Wanaskar ◽  
Yogesh Bhutada ◽  
Raju Thenge ◽  
Vaibhav Adhao
Keyword(s):  
Drug Release ◽  
Extended Release ◽  
In Vitro Release ◽  
Matrix Tablet ◽  
Direct Compression ◽  
In Vitro Drug Release ◽  
Release Studies ◽  
Tablet Properties ◽  
Vitro Release

The aim of present study is to formulate and evaluate extended release matrix tablet of Nateglinide by direct compression method using different polymer like HPMC K4 and HPMC K15. Matrix tablet of nateglidine were prepared in combination with the polymer HPMC K4, HPMC K15, along with the excipients and the formulations were evaluated for tablet properties and in vitro drug release studies. Nateglinide matrix tablet prepared by using polymer such as HPMC K4 and HPMC K15,  it was found that HPMC K15 having higher viscosity as compare to HPMC K4 therefore different concentration of polymer were studied to extend the drug release up to 12 h. The tablets of Nateglinide prepared by direct compression had acceptable physical characteristics and satisfactory drug release. The study demonstrated that as far as the formulations were concerned, the selected polymers proved to have an acceptable flexibility in terms of in-vitro release profile. In present the study the percent drug release for optimize batch was found to 94.62%.  Hence it can be conclude that Nateglinide extended release matrix tablet can prepared by using HPMC. The swollen tablet also maintains its physical integrity during the drug release study Keywords: Tablet, in-vitro drug release, Nateglinide, HPMC

scholarly journals Dissolution Enhancement of Rosuvastatin Calcium by Liquisolid Compact Technique

2013 ◽  
Vol 2013 ◽  
pp. 1-9 ◽  
Author(s):  
V. J. Kapure ◽  
V. V. Pande ◽  
P. K. Deshmukh
Keyword(s):  
Drug Release ◽  
In Vitro Release ◽  
Water Soluble ◽  
Dissolution Enhancement ◽  
Content Uniformity ◽  
Scanning Calorimetry ◽  
Weight Variation ◽  
Liquisolid Compacts ◽  
Rosuvastatin Calcium

In present investigation liquisolid compact technique is investigated as a tool for enhanced dissolution of poorly water-soluble drug Rosuvastatin calcium (RVT). The model drug RVT, a HMG-Co A reductase inhibitor was formulated in form of directly compressed tablets and liquisolid compacts; and studied for in-vitro release characteristics at different dissolution conditions. In this technique, liquid medications of water insoluble drugs in non-volatile liquid vehicles can be converted into acceptably flowing and compressible powders. Formulated systems were assessed for precompression parameters like flow properties of liquisolid system, Fourior transform infra red spectra (FTIR) analysis, X-ray powder diffraction (XRPD), differential scanning calorimetry (DSC), and post compression parameters like content uniformity, weight variation, hardness and friability, disintegration test, wetting time, in vitro dissolution studies, effect of dissolution volume on drug release rate, and estimation of fraction of molecularly dispersed drug in liquid medication. As liquisolid compacts demonstrated significantly higher drug release rates, we lead to conclusion that it could be a promising strategy in improving the dissolution of poor water soluble drugs and formulating immediate release solid dosage forms.

Formulation and Development of Divalproex Sodium Bi-Layered Tablets using Superdisintegrants and Release Retardant Polymers

2017 ◽  
Vol 10 (2) ◽  
pp. 3669-3675
Author(s):  
Ankit Acharya ◽  
Mohammed Gulzar Ahmed ◽  
Ravi Chaudhari ◽  
Renukaradhya Chitti
Keyword(s):  
Drug Release ◽  
Sustained Release ◽  
In Vitro Release ◽  
Immediate Release ◽  
Physical Parameters ◽  
Content Uniformity ◽  
Divalproex Sodium ◽  
In Vitro Drug Release ◽  
Weight Variation

Divalproex sodium is considered as the most important antiepileptic drug and widely used for treatment of epilepsy and bi-polar disorders and prophylaxis of migraine. The present work has been done to formulate bi-layered tablet of Divalproex sodium containing immediate release layer and sustained release layer. The FTIR study revealed that there was no interaction between drug and polymer and combination. Both layers were prepared by wet granulation technique as poor flow property exhibited by pure drug. The immediate release layer was formulated by using superdisintegrants and evaluated for physical parameters, disintegration time and in vitro drug release. The optimized immediate release layer (IF6) with highest in vitro release of 98.11 was selected for bi-layered tablet formulation. HPMC K4M and HPMC K100M polymer were used to retard the drug release from sustained release layer in different proportion and combination and evaluated for physical parameter along with in vitro drug release studies. The optimized sustained release layer (SF8) which extends the Divalproex sodium release more than 18 hrs was selected. Finally, bi-layered tablets were prepared by double compression of selected sustained release layer and immediate release layer of Divalproex sodium. The tablets were evaluated for hardness, thickness, weight variation, friability, drug content uniformity and in vitro drug release. All the physical parameters were in acceptable limit of pharmacopeial specification. The stability studies, shown the bi-layer tablet was stable at 40oC / 75% RH for a period of 3 months.  

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 Once Daily Sustained-Release Matrix Tablet of Naproxen: Formulation and In Vitro Evaluation

1970 ◽  
Vol 9 (1) ◽  
pp. 47-52 ◽  
Author(s):  
Muhammad Rashedul Islam ◽  
Ishtiaq Ahmed ◽  
Mohiuddin Abdul Quadir ◽  
Md Habibur Rahman
Keyword(s):  
Drug Release ◽  
Sustained Release ◽  
In Vitro Release ◽  
Matrix Tablets ◽  
Matrix Tablet ◽  
Once Daily ◽  
Weight Variation ◽  
Release Studies ◽  
The Matrix

The objective of the present study was to develop once-daily sustained-release matrix tablets of naproxen, one of the most potent non-steroidal anti-inflammatory agents used in the treatment of arthritic pain. The tablets were prepared by direct compression method using hydrophilic matrix materials like Methocel® K4M CR and Methocel® K15M CR. The tablets were subjected to measurement of thickness, diameter, weight variation, drug content, hardness and friability, the results of which were within compendial specification range. In vitro release studies were carried out by the USP basket method and were carried out at pH 7.4 buffer for ten hours. The results of dissolution studies indicated that higher polymer content in the matrix (40%) decreased the release rate of the drug as shown in formulation NMK4MF6 and NMK15MF6 (where lactose content is zero). The most successful formulations of the study, exhibited satisfactory drug release which was very close to the theoretical release profile. All the formulations exhibited diffusion-dominated drug release. Key words: Naproxen; Methocel® K4M CR; Methocel® K15M CR; Sustained release; Matrix tablets DOI: 10.3329/dujps.v9i1.7429 Dhaka Univ. J. Pharm. Sci. 9(1): 47-52 2010 (June)

DESIGN AND CHARACTERIZATION OF ACECLOFENAC FAST DISSOLVING TABLETS USING SUPER DISINTEGRATING AGENTS

INDIAN DRUGS ◽  
2014 ◽  
Vol 51 (01) ◽  
pp. 34-40
Author(s):  
V.L Narasaiah ◽  
◽  
Ch. Praneetha ◽  
P Mallika ◽  
K. Pullamma ◽  
...  
Keyword(s):  
Drug Release ◽  
In Vitro Release ◽  
In Vitro Dissolution ◽  
Wet Granulation ◽  
Content Uniformity ◽  
Disintegration Time ◽  
First Order ◽  
Drug Content ◽  
Weight Variation

The aim of this project was to develop fast dissolving tablets (FDT) of aceclofenac by wet granulation using super disintegrating agents such as cross carmellose sodium (CCS), Crospovidone (CP) and sodium starch glycolate (SSG) were formulated and evaluated. The tablets evaluated for thickness, hardness, friability weight variation, drug content, water absorption ratio, wetting time, disintegration time and in vitro dissolution studies. The in vitro release studies were conducted in pH 7.4 phosphate buffer. Different release models like zero order, first order, Higuchi and Korsmeyer-Peppas were applied to in vitro drug release data in order to evaluate drug release mechanisms and kinetics. The formulation ‘F4’ showed satisfactory physico-chemical properties and drug content uniformity. The formulation ‘F4’ follows first order kinetics and the mechanism of drug release was governed by Higuchi. The ‘n’ value showed between <0.5, it was followed that Fickian transport. The FTIR studies were conducted and it shows that there is no interaction between drug and excipients.

scholarly journals FORMULATION AND EVALUATION OF METOCLOPRAMIDE HCL RECTAL SUPPOSITORIES

2019 ◽  
Author(s):  
Deborah Ejiogu Chioma ◽  
Felix Sunday Yusuf
Keyword(s):  
Drug Release ◽  
Release Kinetics ◽  
Diffusion Mechanism ◽  
In Vitro Release ◽  
Content Uniformity ◽  
Disintegration Time ◽  
Weight Variation ◽  
Rectal Suppositories ◽  
Vitro Release

Metoclopramide hydrochloride is a dopamine receptor antagonist, used mostly for stomach and esophageal problems as it is a prokinetic agent. The aim of the present study was to design and evaluate the suppositories of Metoclopramide HCl.  Six different, rectal suppositories were developed by fusion (pour-moulding) method by employing various hydrophilic and hydrophobic polymeric bases like gelatin, PEG-400 and hydrogenated vegetable oil using propylene glycol as plasticizer and beeswax as hardening agent.  Metoclopramide HCl suppositories were evaluated for appearance, weight variation, drug content uniformity, liquefaction time and temperature, micro-melting range, disintegration and in-vitro release study.  The in-vitro release rate data was evaluated statistically and was found that from all the formulations the drug release is by diffusion mechanism. Optimum formulation of batch S1 has shown 83.427% Metoclopramide HCl in a study of 2 hrs. These drug release results are supported by the disintegration time of suppositories. Lesser the disintegration time faster the drug release. All formulations has shown zero, first and Higuchi release kinetics. The result suggests that the Metoclopramide HCl suppositories can be prepared by employing hydrophilic and hydrophobic polymers.

Cashew Nut Starch as Natural Excipient for Improved Bioavailability of Drugs

2019 ◽  
Vol 12 (4) ◽  
pp. 4616-4622
Author(s):  
Anjali Kushwaha
Keyword(s):  
Drug Release ◽  
In Vitro Release ◽  
Disintegration Time ◽  
Cashew Nut ◽  
Weight Variation ◽  
Release Studies ◽  
The Given

The bioavailability of drug is affected by various excipients present in the formulation. In case of tablets, the role of binders is very important for release of drug and bioavailability. In the present study, starch was extracted from the cashew nuts and used as binding agentat a concentration of 2% w/v, 4% w/v, 6% w/v and 8% w/v. The tablets were formulated by using famotidine drug and they were further evaluated for various parameters like weight variation, hardness, friability, disintegration time, in vitro and in vivo drug release. The results show that all parameters were found within the given Indian Pharmacopeial limits. The in vitro release studies were performed in 0.1 N HCl using dialysis methods. This shows that tablets containing 2 % of cashew starch showed maximum drug release (89%) then other formulations. Then optimized formulation was further used for in vivo study and results shows better bioavailability as compared to marketed products.

scholarly journals DESIGN AND EVALUATION OF GUANFACINE EXTENDED RELEASE FORMULATION

2019 ◽  
pp. 43-48
Author(s):  
SANJEEVANI DESAI ◽  
DURGACHARAN BHAGWAT ◽  
SUNITA SHINDE ◽  
JOHN DISOUZA
Keyword(s):  
Extended Release ◽  
In Vitro Release ◽  
Chemical Properties ◽  
Methyl Cellulose ◽  
Stability Study ◽  
Angle Of Repose ◽  
Content Uniformity ◽  
Release Formulation ◽  
Weight Variation

Objective: The present study was aimed to develop of the Guanfacine Hydrochloride Extended-release tablets for the treatment of Attention Deficit Hyperactivity Disorder (ADHD). The dosage regimen of Guanfacine Hydrochloride is 4 mg at every 6 h. The concentration of Guanfacine in plasma is fluctuating. Hence, to control the plasma fluctuation and to avoid toxicity problem, Guanfacine Hydrochloride was chosen as a drug with an aim to develop an extended release system for 20 to 24 h. Methods: The design of the system was based on the use of pH-dependent polymer (Hydroxypropyl Methyl Cellulose), pH-independent polymer (Eudragit L 100-55), along with microenvironment modifiers such as organic acid (Fumaric acid) were used in the formulation. Drug-excipient compatibility was studied by FTIR. Before compression, the granules were evaluated for precompression parameters such as bulk density, tapped density, an angle of repose, compressibility index and Hausner’s ratio. After compression, evaluation tests of tablets such as general appearance, hardness, thickness, weight variation, friability, content uniformity, in vitro release studies and stability studies were performed. Results: Out of 9 formulations, the drug release was found to be within the innovator formulation F9. The stability study of formulation F9 revealed there was no significant change in physical and chemical properties of drug stored at 40 °C/75 % RH, 30 °C/65 % RH, 25 °C/60 % RH for 2 mo. Conclusion: Optimized formulation batch F9 showed highest F2 value which indicates similarity with innovator product. The study indicates that Guanfacine Hydrochloride Extended-release tablet was successfully developed.

scholarly journals FORMULATION AND EVALUATION OF DUAL-LAYERED OSMOTIC PUMP CONTROLLED-RELEASE TABLETS OF CEFIXIME

2021 ◽  
Vol 12 (6) ◽  
pp. 7-19
Author(s):  
Rahul Tyagi ◽  
Pankaj Kumar Sharma ◽  
Dilip Kumar Gupta
Keyword(s):  
Controlled Release ◽  
Drug Release ◽  
In Vitro Release ◽  
Zero Order ◽  
Release Kinetic ◽  
Content Uniformity ◽  
Release Formulation ◽  
Weight Variation ◽  
Core Tablet

Background: This study aims to formulate, optimize and evaluate the osmotic tablet of cefixime. It improves the site specification and provides the controlled release of drug once – a – day through this drug delivery system. Cefixime assumes a significant part in dissolvability restricts other than dissolvable sort. It might increase the bioavailability of drugs by the preparation of the osmotic tablet. Method: The forming core tablet does a formulation of Controlled Porosity Osmotic Tablets (CP1 – CP9) using an ingredient like sodium chloride, PVP K30, Microcrystalline cellulose various ratios. The coating of the core tablet is done by Cellulose Acetate, PEG 400, with statistical ratios. Result: On depending upon the various evaluation parameters like hardness, diameter, friability, weight variation, content uniformity, In vitro release, CP9 formulation gave better consequence. The percentage of drug release is >95%. The optimized CP9 batch showed a maximum correlation of 0.992 with a zero-order drug release kinetic model. Conclusion: A controlled release formulation of cefixime based on osmotic technology, were developed. The release from the developed formulation was independent of pH and agitational intensity of the release media; the formulation fitted well into zero-order kinetics, indicating the release to be drug load independent. Drug release was directly proportional to the initial pore level but inversely related to the membrane weight. The release was inversely associated with the release media's osmotic pressure, confirming osmotic pumping as the central mechanism of release.

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