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- Title
Preparation and evaluation of sustained-release diltiazem hydrochloride pellets.
- Authors
Xiaopeng Han; Linan Wang; Yinghua Sun; Xiaohong Liu; Wanjun Liu; Yuqian Du; Lin Li; Jin Sun
- Abstract
In this study, diltiazem hydrochloride (DTZ) pellets were prepared successfully by extrusionespheronization method. Then methacrylic acid and ethylcellulose coating formulations were employed to make the DTZ pellets sustained release. The pellets with different coatings were investigated by in vitro dissolution tests. At last, the pellets with the best coating copolymer were subjected to pharmacokinetic studies in beagle dogs. The dissolution profiles of pellets coated with Eudragit® NE30D were similar to Herbesser®, one of the marketed sustained release capsules. In the bioavailability study, the principal pharmacokinetic parameters of self-made pellets and the marketed ones were comparable; the relative bioavailability of DTZ sustained release capsules compared with Herbesser was 98.5 ± 36.4%. All the data indicated self-made sustained pellets could prolong the release of DTZ, decrease the fluctuation of drug level in vivo, and increase the compliance of patients.
- Subjects
CONTROLLED release drugs; DILTIAZEM; METHACRYLIC acid; ETHYLCELLULOSE; PHARMACOKINETICS; DRUG bioavailability; THERAPEUTICS
- Publication
Asian Journal of Pharmaceutical Sciences, 2013, Vol 8, Issue 4, p244
- ISSN
1818-0876
- Publication type
Article
- DOI
10.1016/j.ajps.2013.09.007