scholarly journals DESIGN AND CHARACTERISATION OF TRANSDERMAL PATCHES OF PHENFORMIN HYDROCHLORIDE

2017 ◽  
Vol 9 (6) ◽  
pp. 90
Author(s):  
Pratik Swarup Das ◽  
Puja Saha
Keyword(s):  
Drug Release ◽  
Diffusion Mechanism ◽  
Skin Irritation ◽  
In Vitro Release ◽  
Chemical Properties ◽  
In Vitro Dissolution ◽  
Release Mechanism ◽  
Transdermal Patches ◽  
The Matrix

Objective: In present work was designed to develop suitable transdermal matrix patches of Phenformin hydrochloride using various hydrophilic (HPMC) and hydrophobic (EUDRAGID) polymers as matrix formers.Methods: Transdermal patches containing Phenformin hydrochloride were prepared by the solvent casting evaporation technique.Results: Revealed that prepared patches showed good physical characteristics, no drug-polymer interaction and no skin irritation was observed. The in vitro release study revealed that F3 formulation showed maximum release in 24 h. Formulation F3 was subjected for accelerated stability studies. The F3 formulation was found to be stable as there was no drastic change in the Physico-chemical properties of the patches, which was also confirmed by FTIR.Conclusion: Thus conclusion can be made that stable transdermal patches of Phenformin hydrochloride has been developed. F1, F2, F3, F4 formulations showed highest cumulative percentage drug release of 98.13%, 95.50%, 98.65%, 97.21% were obtained during in vitro drug release studies after 24 h. The release of Phenformin hydrochloride appears to be dependent on lipophilicity of the matrix. Moderately lipophillic matrices showed best release. The predominant release mechanism of drug through the fabricated matrices was believed to be by diffusion mechanism. Based upon the in vitro dissolution data the F3 formulation was concluded as optimized formulation.

Transdermal patch, co-loaded with Pregabalin and Ketoprofen for improved bioavailability; in vitro studies

2021 ◽  
pp. 096739112110045
Author(s):  
Nida Shafique ◽  
Tuba Siddiqui ◽  
Muhammad Zaman ◽  
Zoya Iqbal ◽  
Shahid Rasool ◽  
...  
Keyword(s):  
Drug Release ◽  
Diffusion Mechanism ◽  
Controlled Drug Release ◽  
In Vitro Dissolution ◽  
Release Mechanism ◽  
Transdermal Drug Delivery System ◽  
Hydrophobic Polymers ◽  
The Matrix ◽  
Permeation Studies

The current study was aimed to fabricate a transdermal drug delivery system (TDDS) containing Ketoprofen (KTF) and Pregabalin (PGB) for controlled drug release, avoidance of the first-pass metabolism, and increased patient compliance. TDDS of KTF and PGB were formulated using the solvent casting method. Various ratios of hydrophilic polymer (HPMC) and hydrophobic polymers (Eudragit L-100 and Ethyl Cellulose) were employed for the formulation of transdermal patches. PG and oleic acid were used as a permeation enhancer, and PEG-400 was employed as a plasticizer. Surface morphology has confirmed the uniform distribution of drugs throughout the matrix and the excellent compatibility of the selected ingredients. All the formulation showed folding endurance of more than 300, which exhibited that all patches have suitable mechanical strength. One hundred percent flatness also showed good stability of the patches and suitability of the selected ingredients. In vitro drug permeation studies showed more than 97% and 95% release of PGB and KTF, respectively, during the in vitro dissolution studies. The drug release mechanism investigated with various kinetic models exhibited that the rate of drug release was not dependent on initial concentrations of the drug present in the patches and was following the drug diffusion mechanism.

scholarly journals Formulation and evaluation of bi-layer floating tablets of ziprasidone HCl and trihexyphenidyl HCl

2011 ◽  
Vol 47 (3) ◽  
pp. 545-553 ◽  
Author(s):  
Sathis Kumar Dinakaran ◽  
Santhos Kumar ◽  
David Banji ◽  
Harani Avasarala ◽  
Venkateshwar Rao
Keyword(s):  
Sustained Release ◽  
In Vitro Release ◽  
Chemical Properties ◽  
Matrix Tablets ◽  
In Vitro Dissolution ◽  
Floating Tablets ◽  
Ir Studies ◽  
Weight Variation ◽  
The Matrix

The purpose of this research study was to establish ziprasidone HCl NR 40 mg and trihexyphenidyl HCl SR 4mg in the form of bi-layer sustained release floating tablets. The tablets were prepared using sodium HPMC K4M / HPMC K15M as bio-adhesive polymers and sodium bicarbonate acting as a floating layer. Tablets were evaluated based on different parameters such as thickness, hardness, friability, weight variation, in vitro dissolution studies, content of active ingredient and IR studies. The physico-chemical properties of the finished product complied with the specifications. In vitro release from the formulation was studied as per the USP XXIII dissolution procedure. The formulations gave a normal release effect followed by sustained release for 12 h which indicates bimodal release of ziprasidone HCl from the matrix tablets. The data obtained was fitted to Peppas models. Analysis of n values of the Korsmeyer equation indicated that the drug release involved non-diffusional mechanisms. By the present study, it can be concluded that bi-layer tablets of ziprasidone HCl and trihexyphenidyl HCl will be a useful strategy for extending the metabolism and improving the bioavailability of Ziprasidone HCl and Trihexyphenidyl HCl.

Effect of various Polymers on Drug Release from Mucoadhesive Tablets of Cefixime Trihydrate

2021 ◽  
pp. 167-173
Author(s):  
Kumara Swamy Samanthula ◽  
Agaiah Goud Bairi ◽  
Shobha Rani Satla ◽  
Mahendra Kumar CB
Keyword(s):  
Drug Release ◽  
Diffusion Mechanism ◽  
In Vitro Release ◽  
In Vitro Dissolution ◽  
Content Uniformity ◽  
First Pass Metabolism ◽  
First Pass ◽  
Mucoadhesive Tablets ◽  
Pass Metabolism

Cefixime trihydrate (CT) is a third-generation cephalosporin antibiotic and is used in the management of various infections caused by Gram +ve as well as Gram – ve bacteria. It has a plasma half-life of 3-4 h. It has poor oral bioavailability due to hepatic first pass metabolism. Hence, an attempt was made to develop CT mucoadhesive tablets for buccal delivery to avoid first-pass metabolism and improved oral delivery. CT mucoadhesive tablets developed using HPMC K4M, Na-CMC, guar gum and chitosan as rate controlling polymers and mucoadhesive agent, respectively and compressed by direct compression method. The prepared CT mucoadhesive tablets were evaluated for hardness, weight variation, thickness, friability, drug content uniformity, assay, mucoadhesive strength and in vitro release. From the results, all the evaluated parameters were within the pharmacopoeial limits. The in-vitro dissolution studies indicated that the CTmucoadhesive tablets formulation (F2) showed 99.7±1.4 % of drug release after 8 h and chose as the optimized formulation. The kinetic models suggest that the drug release follows Higuchi’s kinetics and tablets drug release was controlled by a diffusion mechanism.

Grewia asiatica Mucilage: A Smart Gelling Polymeric Material for Pharmaceutical Applications In Vitro Studies

2020 ◽  
Vol 12 (2) ◽  
pp. 117-126
Author(s):  
Nitin Gupta ◽  
Giriraj T. Kulkarni ◽  
Pravin Kumar ◽  
Rajendra Awasthi
Keyword(s):  
Drug Release ◽  
Polymeric Material ◽  
Diclofenac Sodium ◽  
Skin Irritation ◽  
In Vitro Release ◽  
Penetration Enhancers ◽  
Release Mechanism ◽  
Drug Release Profile ◽  
Therapeutic Benefits

Background: Natural plant-based materials have several advantages. They are biodegradable, biocompatible, non-toxic, cost-effective, environment friendly, easily available, and can undergo chemical modification. Objective: Grewia asiatica extracts contain various phytoconstituents and have therapeutic benefits such as antimicrobial and anti-diabetic properties. They form colloidal dispersions and make a highly viscous gel in water. Considering these properties of Grewia asiatica mucilage, the present work was aimed to investigate its application in the formulation of gel for the topical delivery of diclofenac sodium. Method: Gel formulations were prepared with and without penetration enhancers using 1% w/w diclofenac sodium as a model drug. The formulations were subjected to different evaluation tests like physical characterization, pH, spreadability, skin irritation, gel retrogradation, drug content and in vitro drug diffusion. The in vitro diffusion of the drug from different formulations was compared with the in vitro drug release profile of the marketed formulation (Omni gel, Cipla, India). To assess the release mechanism, the in vitro release data was analyzed using Korsmeyers-Peppas’ equation. Results: The mucilage showed good gelling behavior in 5.50, 5.75, 6.00, 6.25 and 6.50% concentrations. All the formulations followed the anomalous transport mechanism of drug release. The formulation BP3 showed 90% of drug release after 5.2h of dissolution study, which was similar to the marketed formulation. Hence, formulation BP3 was ideal among all the formulations. Conclusion: It might be concluded that, the Grewia asiatica mucilage may be used as a natural polymeric material for gel formulation.

scholarly journals Formulation and In vitro Release Behavior of Hydroxypropyl Methylcellulose (HPMC) Matrix Tablet Containing Poorly Soluble Fenofibrate

2020 ◽  
Vol 23 (1) ◽  
pp. 10-16
Author(s):  
Ramesh Kandel ◽  
Tushar Saha ◽  
Zia Uddin Masum ◽  
Jakir Ahmed Chowdhury
Keyword(s):  
Hydroxypropyl Methylcellulose ◽  
In Vitro Release ◽  
Pharmaceutical Journal ◽  
Matrix Tablets ◽  
In Vitro Dissolution ◽  
Release Mechanism ◽  
Matrix Tablet ◽  
Dissolution Profile ◽  
The Matrix

Fenofibrate, a water insoluble drug was used to prepare matrix tablet with four different viscosity grades of Hydroxypropyl Methylcellulose (HPMC) which were Methocel K4M CR, Methocel K15M CR, Methocel K100M CR and Methocel K100LV CR. The concentration of those excipients was 5, 10, 20, and 40% (w/w), respectively. The content of drug in a fixed quantity of powder in every formulation was ranged between 96.47 to 104.78 %. The dissolution study was done by using USP dissolution apparatus II. The kinetics of release was analyzed by using zero-order, first order, Korsmeyer-Peppas, Higuchi and Hixon-crowell equations to explain the drug release mechanism from the matrix tablets. In-vitro dissolution profile of matrix tablets were dependent upon the HPMC concentration and dissolution was rapid for tablets containing lower polymer proportion i.e. 5,10, and 20% Percentage (w/w) HPMC than those containing 40% (w/w) HPMC. Bangladesh Pharmaceutical Journal 23(1): 10-16, 2020

scholarly journals FORMULATION AND EVALUATION OF FLOATING PELLETS OF OMEPRAZOLE BY EXTRUSION SPHERONIZATION METHOD

2020 ◽  
Vol 9 (2) ◽  
Author(s):  
Anusha M ◽  
S T Bhagawati ◽  
K Manjunath
Keyword(s):  
Drug Release ◽  
Bulk Density ◽  
In Vitro Release ◽  
Zero Order ◽  
Angle Of Repose ◽  
In Vitro Dissolution ◽  
Release Mechanism ◽  
Release Kinetic ◽  
Drug Content

Objective: The aim of the present study was design, develop and to evaluate a model of floating sustained release pellets formulations for Omeprazole by extrusion and spheronization technique. Methods: Omeprazole at different drug to polymer ratios were prepared by extrusion and spheronization technique and the release rate of the drug from the pellets was studied. Further, the in-vitro release studies of pellets were carried out in 0.1N HCL for 12 hours. Prepared pellets were subjected to characterization by different techniques such as loose bulk density, tapped bulk density, compressibility index and angle of repose. To optimize the formulation on the basis of acceptable pellet properties friability, drug content, moisture content, and loss on drying and in-vitro drug release tests were done. In addition, the compatibility studies were performed by using FTIR and DSC. Results: These above studies indicated that the drug release can be modulated by varying the concentration of the polymer. The resulting formulation produced robust pellets with acceptable drug content and low friability. Further, 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. Kinetic modeling of in-vitro dissolution profiles revealed the release mechanism ranges from Quasi-Fickian transport to Anomalous (non-Fickian transport), which was only dependent on the type and amount of polymer used. The drug release of the optimized formulation (F5) follows Zero order kinetics and the mechanism was found to be diffusion controlled. The FTIR and DSC studies reveal that there is no interaction between the drug and the polymer/excipients mixture. Keywords:  Floating, Ethyl cellulose, HPMC, Pellets, Omeprazole.

Relevancy of Nizatidine Release from Floating Tablets with Viscosity of Various Cellulose Ethers

Sci ◽  
2019 ◽  
Vol 1 (1) ◽  
pp. 22 ◽  
Author(s):  
Yasser Shahzad ◽  
Namra Ibrar ◽  
Talib Hussain ◽  
Abid Mehmood Yousaf ◽  
Ikram Ullah Khan ◽  
...  
Keyword(s):  
Drug Release ◽  
Fickian Diffusion ◽  
In Vitro Dissolution ◽  
Release Mechanism ◽  
Cellulose Ethers ◽  
Polymer Backbone ◽  
Floating Tablets ◽  
The Matrix ◽  
The Difference

Nizatidine is a gastroprotective drug with a short biological half-life and narrow absorption window. This study aimed at developing floating tablets of nizatidine using various HPMC viscosity grades, namely K4M, E4M, K15 and K200M. Directly compressed tablets revealed an excellent uniformity in hardness, thickness and weight and nizatidine was evenly distributed within the matrix floating tablets. Buoyancy study revealed floating lag time as low as 18–38 s, and tablets remain buoyant for upto 24 h. However, the later depended upon viscosity grade of HPMC and that the higher the viscosity, the less was the total floating time. In vitro dissolution indicated viscosity dependent nizatidine release from the floating tablets. HPMC K4M and E4M based floating tablets released almost 100% drug in 12 h, whilst higher viscosity polymers such as K15 and K200M only released 81.88% and 75.81% drug, respectively. The drug release followed non-Fickian diffusion from tablets formulated with K4M, K15 and K200M, whilst super case II transport was observed with E4M based tablets. More interestingly, K4M and E4M polymers have similar viscosity yet exhibited different drug release mechanism. This was attributed to the difference in degree of substitution of methoxyl- and hydroxypropoxyl- groups on polymer backbone.

scholarly journals Relevancy of Nizatidine’s Release from Floating Tablets with Viscosity of Various Cellulose Ethers

Sci ◽  
2021 ◽  
Vol 3 (2) ◽  
pp. 22
Author(s):  
Yasser Shahzad ◽  
Namra Ibrar ◽  
Talib Hussain ◽  
Abid Mehmood Yousaf ◽  
Ikram Ullah Khan ◽  
...  
Keyword(s):  
Drug Release ◽  
Fickian Diffusion ◽  
In Vitro Dissolution ◽  
Release Mechanism ◽  
Cellulose Ethers ◽  
Polymer Backbone ◽  
Floating Tablets ◽  
The Matrix ◽  
The Difference

Nizatidine is a gastroprotective drug with a short biological half-life and narrow absorption window. This study aimed at developing floating tablets of nizatidine using various HPMC viscosity grades, namely K4M, E4M, K15 and K200M. Directly compressed tablets revealed an excellent uniformity in hardness, thickness and weight and nizatidine was evenly distributed within the matrix floating tablets. Buoyancy study revealed floating lag time as low as 18–38 s, and tablets remain buoyant for upto 24 h. However, the later depended upon viscosity grade of HPMC and that the higher the viscosity, the less was the total floating time. In vitro dissolution indicated viscosity dependent nizatidine release from the floating tablets. HPMC K4M and E4M based floating tablets released almost 100% drug in 12 h, whilst higher viscosity polymers such as K15 and K200M only released 81.88% and 75.81% drug, respectively. The drug release followed non-Fickian diffusion from tablets formulated with K4M, K15 and K200M, whilst super case II transport was observed with E4M based tablets. More interestingly, K4M and E4M polymers have similar viscosity yet exhibited different drug release mechanism. This was attributed to the difference in degree of substitution of methoxyl- and hydroxypropoxyl- groups on polymer backbone.

scholarly journals In vitro Release Kinetics Study of Ranolazine from Swellable Hydrophilic Matrix Tablets

1970 ◽  
Vol 8 (1) ◽  
pp. 31-38 ◽  
Author(s):  
Mohammad Nezab Uddin ◽  
Ishtiaq Ahmed ◽  
Monzurul Amin Roni ◽  
Muhammad Rashedul Islam ◽  
Mohammad Habibur Rahman ◽  
...  
Keyword(s):  
Drug Release ◽  
Sustained Release ◽  
Release Kinetics ◽  
In Vitro Release ◽  
High Viscosity ◽  
Matrix Tablets ◽  
Release Studies ◽  
The Matrix ◽  
Vitro Release

The objective of this study was to design oral sustained release matrix tablets of Ranolazine usinghydroxypropyl methylcellulose (HPMC) as the retardant polymer and to study the effect of formulation factors suchas polymer proportion and polymer viscosity on the release of drug. In vitro release studies were performed usingUSP type II apparatus (paddle method) in 900 mL of 0.1N HCl at 100 rpm for 12 hours. The release kinetics wasanalyzed using the zero-order, first order, Higuchi and Korsmeyer-Peppas equations to explore and explain themechanism of drug release from the matrix tablets. In vitro release studies revealed that the release rate decreasedwith increase in polymer proportion and viscosity grade. Mathematical analysis of the release kinetics indicated thatthe nature of drug release from the matrix tablets was dependent on drug diffusion and polymer relaxation andtherefore followed non-Fickian or anomalous release. The developed controlled release matrix tablets of Ranolazineprepared with high viscosity HPMC extended release up to 12 hours.Key words: Ranolazine; Sustained release; Methocel E50 Premium LV; Methocel K100LV CR; Methocel K4M CR;Methocel K15M CR.DOI: 10.3329/dujps.v8i1.5333Dhaka Univ. J. Pharm. Sci. 8(1): 31-38, 2009 (June)

scholarly journals Formulation and In Vitro Evaluation of Sustained Release Floating Matrix Tablet of Levofloxacin by Direct Compression Method

2019 ◽  
Vol 9 (4-s) ◽  
pp. 398-403
Author(s):  
Nidhi Kumari Pandey ◽  
Sailesh Kumar Ghatuary ◽  
Amit Dubey ◽  
Prabhat Kumar Jain
Keyword(s):  
Drug Release ◽  
Acute Infection ◽  
Methyl Cellulose ◽  
In Vitro Dissolution ◽  
Release Mechanism ◽  
Matrix Tablet ◽  
Direct Compression ◽  
Compression Method ◽  
Weight Variation

The objective of the present work was to develop Gastro retentive dosage forms which would remain in the stomach and upper part or GIT for a prolonged period of time thereby maximizing the drug release at desired site within the time before GRDFs left the stomach and upper part of the GIT, has provoked a great deal of increased interest in the formulation of such drug as floating drug delivery systems. Levofloxacin, (BCS class I) is a fluoroquinolone anti-bacterial agent. The rationale for the formulation of floating matrix tablet are acidic solubility of levofloxacin, residence of Halicobactor pylori mainly in sub region of stomach and the overdosing associated adverse effect due to continuous intake of drug in acute infection. A simple visible spectrophotometric method was employed for the estimation of levofloxacin at 294 nm and Beer’s law is obeyed in the concentration range of 2-10 μg /ml. Floating matrix tablet of levofloxacin was prepared by direct compression method using different polymers like hydroxyl propyl methyl cellulose (HPMC K4) and carbopol 934 as matrix formation polymers, sodium bicarbonate and citric acid was used as gas generating agents. The FTIR spectra of the levofloxacin and other excipients alone and in combination show the compatibility of the drug and excipients. Six formulations of different polymer percentages were formulated (F1-F6). Pre-compression parameters were evaluated. The influence of matrix forming agents and binary mixtures of them on levofloxacin release was investigated. The formulated tablets were characterized by hardness, friability, thickness, weight variation and in vitro drug release. The formulated tablets had acceptable physicochemical characters. The data obtained from the in-vitro dissolution studies of optimized batch F4were fitted in different models. The optimized formulation F4 showed 99.25% drug content and swelling index of 79.85 %. Drug release mechanism was found to be first order kinetics. Levofloxacin floating tablets exhibited increased gastric residence time, there by improved bioavailability and therapeutic effect of the drug.  

Sign in / Sign up

Export Citation Format

Share Document