scholarly journals An Investigation into the Influence of Experimental Conditions on In Vitro Drug Release from Immediate-Release Tablets of Levothyroxine Sodium and Its Relation to Oral Bioavailability

2011 ◽  
Vol 12 (3) ◽  
Author(s):  
Ivana Kocic ◽  
Irena Homsek ◽  
Mirjana Dacevic ◽  
Jelena Parojcic ◽  
Branislava Miljkovic
Keyword(s):  
Drug Release ◽  
Oral Bioavailability ◽  
Immediate Release ◽  
Levothyroxine Sodium ◽  
Experimental Conditions ◽  
In Vitro Drug Release

scholarly journals Optimizing the Role of Polymer Blend in the Preparation of Acyclovir Controlled-Release Tablets: An Approach for Better Patient Compliance

2018 ◽  
Author(s):  
Barkat Khan ◽  
Faheem Haider ◽  
Kifayat Shah ◽  
Bushra Uzair ◽  
Kaijian Hou ◽  
...  
Keyword(s):  
Controlled Release ◽  
Drug Release ◽  
Release Kinetics ◽  
Immediate Release ◽  
Matrix Tablets ◽  
Release Mechanism ◽  
In Vitro Drug Release ◽  
Solubility Study ◽  
Release Data

This study was carried out to formulate and evaluate controlled release (CR) matrix tablets of Acyclovir using combination of hydrophilic and hydrophobic polymers. Acyclovir is a guanine derivative and is its half-life is short hence administered five times a day using immediate release tablets. Six formulations (F1-F6) were developed using Ethocel and Carbopol in equal combinations at drug-polymer (D:P) ratio of 10:5, 10:6, 10:7, 10:8, 10:9 and 10:10. Solubility study was performed using six different solvents. The compatibility studies were carried out using FTIR and DSC. According to USP, Quality Control and dimensional tests (hardness, friability, disintegration and thickness) were executed. In-vitro drug release studies of Acyclovir was carried out in dissolution apparatus using using 0.1 N HCl medium at constant temperature of 37 ± 0.5 ºC. In order to analyze the drug release kinetics, five different mathematical models were applied to the release data. The results showed that there was no incompatibility between drug and polymers. Physical QC tests were found within limits of USP. The release was retarded upto 24 hrs and non-fickian in-vitro drug release mechanism was found. A formulation developed using blend of polymers, showed excellent retention and desired release profiles thus providing absolute control for 24 hrs.

scholarly journals Formulation, Characterisation and Evaluation of the Ethosuximide Oral Immediate Release Tablets

2020 ◽  
Vol 11 (2) ◽  
pp. 1807-1813
Author(s):  
Naga Sujan M ◽  
Kunal K Mehta ◽  
Amit B Patil ◽  
Anusha Vajhala
Keyword(s):  
Drug Release ◽  
Dosage Form ◽  
Immediate Release ◽  
Rice Starch ◽  
Wet Granulation ◽  
Drug Release Profile ◽  
Disintegration Time ◽  
In Vitro Drug Release ◽  
Release Studies

The present study is aimed to formulate, characterization, and evaluate oral immediate-release tablets of Ethosuximide. It is employed as an anti-epileptic agent used in the treatment of epilepsy, in all the age groups who were≥ 1 year. The dosage form is formulated by directly compressing the blend and granulating the powder blend by wet granulation methods. The optimized formulation is achieved by the trial and error method by changing the concentration of lactose monohydrate and di-basic calcium phosphate dehydrate as diluents, sodium starch glycolate as Super-dis-integrant, rice Starch as an intra-granular binder, hydroxypropyl cellulose as binder talc as a lubricant. Evaluation parameters such as micrometric properties, disintegration time along with in-vitro drug release studies were performed for characterizing the dosage form. In-vitro drug release studies were carried out using 0.1 N HCl as dissolution media with 75 rpm and temperature of 370C ± 50C by employing USP apparatus II (Paddle type). Estimation of the % drug release of the tablet was carried out using the UV method. The prepared formulation and the marketed formulation were tested for the in-vitro drug release profile and the prepared formulation was compared with the marketed formulation. All the evaluated result was found to be within the specifications. Therefore, from the obtained evaluation results F6 trail was selected as the best formulation.

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 In Vitro Methods for Evaluating Drug Release of Vaginal Ring Formulations—A Critical Review

Pharmaceutics ◽  
2019 ◽  
Vol 11 (10) ◽  
pp. 538 ◽  
Author(s):  
Tietz ◽  
Klein
Keyword(s):  
Drug Delivery ◽  
Drug Release ◽  
Immediate Release ◽  
Discriminatory Power ◽  
Current Status ◽  
Predictive Capacity ◽  
In Vitro Drug Release ◽  
In Vitro Methods

The vagina is a promising site for both local and systemic drug delivery and represents an interesting administration route for compounds with poor oral bioavailability. Whereas most of the currently marketed dosage forms were designed as immediate release formulations, intravaginal rings (IVRs) offer the possibility of a controlled vaginal drug delivery over several weeks or months. For a long time, the development of IVRs was limited to steroid-releasing formulations. Recently, IVRs have witnessed a surge of new interest as promising delivery systems for microbicides. Therefore, various novel IVR designs have been introduced. To ensure that only safe and effective IVRs will be administered to patients, it is important to properly distinguish between IVRs with desired and undesired release performance. In vitro methods for evaluating drug release of IVRs that present with sufficient predictive capacity for in vivo drug release, and discriminatory power with regard to IVRs quality, are an essential tool for this purpose. The objective of the present review article is to present the current status of in vitro drug release testing of IVRs and to critically discuss current compendial and non-official in vitro drug release methods with regard to their discriminatory power and in vivo predictivity.

Improved oral bioavailability of capsaicin via liposomal nanoformulation: preparation, in vitro drug release and pharmacokinetics in rats

2014 ◽  
Vol 38 (4) ◽  
pp. 512-521 ◽  
Author(s):  
Yuan Zhu ◽  
Miaomiao Wang ◽  
Jiajia Zhang ◽  
Wei Peng ◽  
Caleb Kesse Firempong ◽  
...  
Keyword(s):  
Drug Release ◽  
Oral Bioavailability ◽  
In Vitro Drug Release ◽  
Pharmacokinetics In Rats

scholarly journals DEVELOPMENT OF ORALLY DISINTEGRATING TABLETS OF MEMANTINE HYDROCHLORIDE-A REMEDY FOR ALZHEIMER’S DISEASE

2019 ◽  
pp. 147-152
Author(s):  
IMRAN S. GHOGARI ◽  
PRITAM S. JAIN
Keyword(s):  
Alzheimer’S Disease ◽  
Alzheimer's Disease ◽  
Drug Release ◽  
Immediate Release ◽  
Tablet Formulation ◽  
Disintegration Time ◽  
In Vitro Drug Release ◽  
Orally Disintegrating Tablet ◽  
Accelerated Stability

Objective: The study is directed towards the development of an orally disintegrating drug delivery system of memantine hydrochloride which can be commercially exploited for the well-being of society for the treatment of Alzheimer’s disease, which is a most common form of dementia. Methods: Orally disintegrating immediate-release tablets of memantine hydrochloride were prepared and optimized for disintegration time and in vitro drug release. The top spray granulation method was used for the preparation of granules. Subsequently, these granules were compressed to tablets. The levels of diluent, disintegrant and taste-masking agents were optimized using the design of experiments. The resulting tablets were evaluated for disintegration time and in vitro drug release. The optimized formulation was subjected to accelerated stability study for 3 mo. Results: The optimized orally disintegrating tablet formulation exhibited a disintegration time of 2-3 min and complete drug release i.e. more than 85 % drug release within 10 min while performing in vitro drug release study. This is a prerequisite for faster action in the case of patients suffering from Alzheimer’s disease. Accelerated stability studies indicated good physical and chemical stability of the optimized formulation. Conclusion: Developed orally disintegrating tablet formulation of memantine hydrochloride could release the drug faster compared to conventional immediate-release tablets which is useful in paediatric, geriatric and psychiatric patients.

scholarly journals Novel ion exchange resin-based combination drug-delivery system for treatment of gastro esophageal reflux diseases

2010 ◽  
Vol 46 (2) ◽  
pp. 335-342 ◽  
Author(s):  
Mangesh Ramesh Bhalekar ◽  
Nitin Madhukar Kadam ◽  
Nilam Hindurao Patil ◽  
Nitin Somnath Gawale ◽  
Ashwini Madgulkar
Keyword(s):  
Ion Exchange ◽  
Drug Release ◽  
Sustained Release ◽  
Immediate Release ◽  
Esophageal Reflux ◽  
In Vitro Drug Release ◽  
Combination Tablet ◽  
Tablet Properties ◽  
Release Form

The present study involves preparation and characterization of a combination tablet of ranitidine in immediate release form and domperidone in sustained release form, using ion exchange resins. Ranitidine lowers acid secretion, while domperidone release over a prolonged period improves gastric motility thus justifying this combination in gastro esophageal reflux diseases (GERD) and ensuring patient compliance. Drug loading was carried out by batch method & resinates were characterized using FTIR, XRPD. Resinates were formulated as a combination tablet and evaluated for tablet properties & in vitro drug release. Resinates provided sustained release of domperidone and immediate release of ranitidine. IR and X-ray studies indicate complexation of drug and resin along with monomolecular distribution of drugs in amorphous form in the resin matrix. The tablets of resinate combination showed good tablet properties. In-vitro drug release gave desired release profiles and ex-vivo drug absorption studies carried out by placing everted rat intestine in dissolution medium indicated statistically significant similarity in absorption from test and marketed formulation. The novelty of this study is that the retardation in release of domperidone from resinates is achieved by presence of weak resin in the formulation.

FORMULATION AND EVALUATION OF THYROID HORMONE (T4) IMMEDIATE RELEASE TABLETS

2022 ◽  
Vol 2 (1) ◽  
pp. 389-393
Author(s):  
Madhivardhana P ◽  
Rajalakshmi A N ◽  
Padmapriya S
Keyword(s):  
Thyroid Hormone ◽  
Drug Release ◽  
Research Work ◽  
Immediate Release ◽  
Flow Property ◽  
Direct Compression ◽  
Disintegration Time ◽  
In Vitro Drug Release ◽  
Good Flow

The aim of this research work is to formulate and evaluate Levothroxine sodium immediate release tablets prepared by direct compression method . Five formulations were evaluated for different pre and post compression parameter and in vitro drug release studies.The results of pre compression parameters of formluation 1 to 5 were compared with prescribed limits. It showed that formulation 1 to 5 powder blend exhibit good flow property and compressibility property. The disintegration time of all formulation was found to be in the range 2mins 09 secsto 4mins 03 secs.Thus, based on evaluation of different parameters it was concluded that formulation of immediate release tablet Levothyroxine sodium was successfully done and F-5 showed almost 93% drug release at 45 mins in Alkaline borate buffer( pH 10). Keywords: Thyroid hormone (T4), Immediate release tablets, Direct compression, Dissolution.

scholarly journals Enhancement of Aqueous Solubility, Dissolution Profile, and Oral Bioavailability of Pentoxifylline by Microsponges

2021 ◽  
Author(s):  
Anil Raosaheb Pawar ◽  
Nikhil Arun Shete ◽  
Priyanka Vitthal Jadhav ◽  
Vinayak Kashinath Deshmukh ◽  
Jaswandi Sameer Mehetre
Keyword(s):  
Drug Release ◽  
Oral Bioavailability ◽  
Aqueous Solubility ◽  
Diffusion Method ◽  
Dissolution Profile ◽  
Scanning Calorimetry ◽  
In Vitro Drug Release ◽  
Pure Drug

Microsponge, a novel drug delivery system, is designed to deliver a pharmaceutically active ingredient efficiently at the minimum dose. Microsponge plays an important role in enhancing drug stability, reducing side effects, and modifying drug release profiles. It is mostly used for transdermal delivery. Recent studies also explored their use for oral administration. This study aimed to explore the potential use of the microsponge technique in improving the aqueous solubility and dissolution profile of pentoxifylline (PTX). In this study, microsponges were prepared by a quasi-emulsion solvent diffusion method by varying concentrations of carriers. Nine different ratios of the PTX:Eudragit E-100 with varying amounts of dichloromethane were used. All formulated microsponges were evaluated for %production yield, compatibility of drug excipient, encapsulation efficiency, in vitro drug release, and in vivo bioavailability, as well as recorded by scanning electron microscopy (SEM) and differential scanning calorimetry(DSC). Our data suggested that the aqueous solubility of PTX microsponges was four times greater than that of pure drug. The in vitro drug release of selected microsponges (M8) was found to be 70%; furthermore, the in vivo study suggested that the selected formulation significantly enhanced drug concentration in the plasma (9,219 ng/mL in 12 hours) in comparison to pure drug PTX (2,476 ng/mL in 12 hours). SEM showed that the prepared microsponges were spherical with porous nature. Fourier-transform infrared spectroscopy and DSC studies confirmed an absence of incompatibility among drugs and selected excipients. The pH of the selected gel was found to be 6.8, which was compatible with those of skin and oral formulations also. All above data suggested a highly successful and beneficial use of the microsponge technique in enhancing aqueous solubility, dissolution profile, and oral bioavailability of PTX. Microsponge-based delivery of PTX may represent an alternative strategy to improve the bioavailability of the drug.

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