Sustained-release hydrophilic matrix tablets of zileuton: formulation and in vitro/in vivo studies

Aim: Nateglinide is a quick acting anti-diabetic medication whose potent activity lasts for a short duration. One of the dangerous side effects of nateglinide administration is rapid hypoglycemia, a condition that needs to be monitored carefully to prevent unnecessary fatalities. The aim of the study was to develop a longer lasting and slower releasing formulation of nateglinide that could be administered just once daily. Methods: Matrix tablets of nateglinide were prepared in combination with the polymers hydroxypropylmethylcellulose (HPMC), eudragits, ethyl cellulose and polyethylene oxide and the formulated drug release patterns were evaluated using in vitro and in vivo studies. Conclusion: Of the seventeen formulated matrix tablets tested, only one formulation labelled HA-2 that contained 15% HPMC K4M demonstrated release profile we had aimed for. Further, swelling studies and scanning electron microscopic analysis confirmed the drug release mechanism of HA-2. The optimized formulation HA-2 was found to be stable at accelerated storage conditions for 3 months with respect to drug content and physical appearance. Mathematical analysis of the release kinetics of HA-2 indicated a coupling of diffusion and erosion mechanisms. In-vitro release studies and pharmacokinetic in vivo studies of HA-2 in rabbits confirmed the sustained drug release profile we had aimed for. Keywords: Hydroxypropylmethylcellulose, Matrix tablets, Nateglinide, Sustained release

Download Full-text

In Vitro Conditions for the Study of the In Vivo Performance of Sustained-Release Theophylline Matrix Tablets Administered in Fasted Conditions and with a High-Fat Diet

Drug Development and Industrial Pharmacy ◽

10.1081/ddc-100102288 ◽

1999 ◽

Vol 25 (11) ◽

pp. 1199-1203 ◽

Cited By ~ 2

Author(s):

M. T. Andonaegui ◽

J. L. Barría ◽

A. M. Thielemann ◽

C. Seitz ◽

M. N. Gai

Keyword(s):

Sustained Release ◽

High Fat Diet ◽

Matrix Tablets ◽

High Fat ◽

Sustained Release Theophylline

Download Full-text

Chitosan and Enteric Polymer Based Once Daily Sustained Release Tablets of Aceclofenac: In Vitro and In Vivo Studies

AAPS PharmSciTech ◽

10.1208/s12249-008-9075-3 ◽

2008 ◽

Vol 9 (2) ◽

Cited By ~ 12

Author(s):

Srinivas Mutalik ◽

Krishnan Manoj ◽

Meka Sreenivasa Reddy ◽

Pralhad Kushtagi ◽

Achutha Nayak Usha ◽

...

Keyword(s):

Sustained Release ◽

In Vivo Studies ◽

Once Daily ◽

Sustained Release Tablets ◽

Enteric Polymer

Download Full-text

In vitro and in vivo Studies of a New Sustained Release Formulation of Morphine

Arzneimittelforschung ◽

10.1055/s-0031-1296566 ◽

2011 ◽

Vol 58 (12) ◽

pp. 647-652

Author(s):

Amparo Araíco ◽

Francisca Torres-Molina ◽

Anas Saadeddin ◽

Jaime Cárcel-Trullols ◽

Josefa Alvarez-Fuentes ◽

...

Keyword(s):

Sustained Release ◽

In Vivo Studies ◽

Release Formulation ◽

Sustained Release Formulation

Download Full-text

Formulation of sustained-release microspheres of cefixime with enhanced oral bioavailability and antibacterial potential

Therapeutic Delivery ◽

10.4155/tde-2019-0057 ◽

2019 ◽

Vol 10 (12) ◽

pp. 769-782

Author(s):

Karan Razdan ◽

Nikhil S Sahajpal ◽

Kuldeep Singh ◽

Harmanpreet Singh ◽

Harjeet Singh ◽

...

Keyword(s):

Sustained Release ◽

Entrapment Efficiency ◽

Salmonella Typhi ◽

In Vivo Studies ◽

In Vitro Drug Release ◽

Dosing Frequency ◽

Twofold Decrease ◽

Antibacterial Potential

Aim: The present work focused on the development of sustained-release microsphere formulation of cefixime to provide reduction in dosing frequency, improved antibacterial activity and patient compliance. Methodology & results: Microspheres were prepared by modified emulsion solvent evaporation method and evaluated by in vitro and in vivo studies. Optimized formulation (FK-07) was found to have entrapment efficiency of 81.12 ± 0.93% and particle size of 166.82 ± 0.86 μm. FK-07 sustained release up to 24 h as demonstrated by in vitro drug release and in vivo pharmacokinetic study in rats. FK-07 showed approximately twofold increase in bioavailability and twofold decrease in MIC90 value against Escherichia coli, Klebsiella pneumoniae and Salmonella typhi in comparison to marketed formulation. Conclusion: Sustaining the release of cefixime using microspheres enhanced its bioavailability, antibacterial efficacy and will help in reducing its dosing frequency.

Download Full-text

Design and in vivo Evaluation of Gastro-retentive Floating Capsules of Amlodipine Besylate in Healthy Human Volunteers

International Journal of Pharmaceutical Sciences and Nanotechnology ◽

10.37285/ijpsn.2017.10.6.3 ◽

2017 ◽

Vol 10 (6) ◽

pp. 3891-3899

Author(s):

Bhikshapathi D. V. R. N. ◽

Chenna Madipalli Shalina ◽

Vishnu Pulavarthy ◽

Viswaja Medipally

Keyword(s):

Drug Delivery ◽

Drug Release ◽

Sustained Release ◽

In Vivo Studies ◽

Amlodipine Besylate ◽

In Vivo Evaluation ◽

Healthy Human ◽

Gastro Retentive

The aim of this study was to explore the application of Gelucire 43/01 for the design of sustained release gastro retentive drug delivery system of Amlodipine besylate. Gelucire 43/01 has been used in floating sustained release formulations to prolong gastric residence time and increase its bioavailability. Gelucire 43/01 in combination with HPMC and Polyox was used as a release retarding polymer. HPMC of various viscosity grades HPMC K4M, HPMC K15M and HPMC K100M in combination of Gelucire were tested to obtain optimal total floating time as well as controlled drug release for prolonged period. Melt granulation technique has been used to prepare gastro retentive Amlodipine besylate formulations. All the formulations were evaluated in vitro for their floating ability and drug release. The floating times of all tablet formulations were greater than 12h. HPMC K4M in combination with Gelucire as polymeric matrix enhanced the drug release due to addition of hydrophilic polymer facilitated the swelling and erosion of the tablets. Incorporation of low viscosity polymer HPMC K100 M resulted in optimal floating as well as drug release for longer time. In vivo studies of optimized formulation show floating ability for 6 h in stomach. The results indicate that Gelucire 43/01 in combination with dissolution enhancers HPMC increase the permeability of the wax matrix, which provides improved dissolution thereby bioavailability of Amlodipine besylate and can be considered as a carrier for the development of sustained release floating drug delivery systems.

Download Full-text