Formulation study and drug release mechanism of a new theophylline sustained-release preparation

Two matrix theophylline tablets with different release mechanisms were compared. Tablet A was a swelling/disintegration-type wax matrix made of hydrophobic wax granules, consisting of stearic acid, hydrogenated oil and glycerol esters of fatty acids, and hydrophilic polymer granules composed primari...

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Veröffentlicht in:International journal of pharmaceutics 2005-11, Vol.304 (1), p.91-101
Hauptverfasser: Hayashi, Tetsuo, Kanbe, Hideyoshi, Okada, Minoru, Suzuki, Makoto, Ikeda, Yasuo, Onuki, Yoichi, Kaneko, Tetsuo, Sonobe, Takashi
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container_end_page 101
container_issue 1
container_start_page 91
container_title International journal of pharmaceutics
container_volume 304
creator Hayashi, Tetsuo
Kanbe, Hideyoshi
Okada, Minoru
Suzuki, Makoto
Ikeda, Yasuo
Onuki, Yoichi
Kaneko, Tetsuo
Sonobe, Takashi
description Two matrix theophylline tablets with different release mechanisms were compared. Tablet A was a swelling/disintegration-type wax matrix made of hydrophobic wax granules, consisting of stearic acid, hydrogenated oil and glycerol esters of fatty acids, and hydrophilic polymer granules composed primarily of hydroxypropyl methylcellulose (HPMC). We named Tablet A the cluster tablet. Tablet B was a gel matrix made of hydrophobic ethylcellulose granules, consisting of ethylcellulose and hydrogenated oil, and hydrophilic polymer granules consisting of HPMC and hydroxylpropylmethylcellulose acetate succinate (HPMCAS). The formulations were screened in vitro according to their dissolution characteristics. The drug release from each preparation was analyzed using release kinetics theories. In Tablet A, the value of the exponent( n) representing the apparent diffusion mechanism determined from the Korsmeyer–Peppas model equation was about 0.6 and was unlikely to be affected by the rotation speed. In Tablet B, the value of the exponent( n) by the Korsmeyer–Peppas model equation changed with the paddle rotation speed. These results suggested that the drug release mechanism of Tablet B is greatly affected by the extent of physical force in the gastrointestinal tract.
doi_str_mv 10.1016/j.ijpharm.2005.07.022
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subjects Biological and medical sciences
Delayed-Action Preparations
Drug Compounding
Excipients - chemistry
General pharmacology
Hydrophilic polymer
Hydrophobic wax
Kinetics
Matrix tablet
Medical sciences
Pharmaceutical technology. Pharmaceutical industry
Pharmacology. Drug treatments
Polymers - chemistry
Release mechanism
Solubility
Sustained-release
Tablets
Theophylline
Theophylline - chemistry
title Formulation study and drug release mechanism of a new theophylline sustained-release preparation
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