期刊
PHARMACEUTICAL DEVELOPMENT AND TECHNOLOGY
卷 5, 期 3, 页码 339-346出版社
MARCEL DEKKER INC
DOI: 10.1081/PDT-100100549
关键词
bimodal release; captopril; furosemide; Polyox; sustained-release capsules; swelling
The powder characteristics and the effect of the molecular weight of polymers as diluents on the release rate of furosemide and captopril from hard gelatin capsules were evaluated. The high molecular weight polymers studied were poly(oxyethylene) homopolymers (Polyox), with molecular weight ranging from 4,000,000 to 7,000,000. Powder characteristics suggested good flowability for these materials and predicted capsule fill weight uniformity. Swelling experiments showed a very high degree of swelling for these materials in both gastric and buffer solution. These polymers can sustain the release rate of both water-soluble and insoluble drugs from drug delivery systems. The low molecular weight polymers have a less pronounced sustained-release effect compared to the high molecular weight polymer material (i.e., those with 7,000,000 molecular weight). An increase in the content of polymer results in a decrease in the release rate of the drug. The solubility of the drugs clearly influenced the release rate. Release kinetics were evaluated and appeared to be influenced by the molecular weight of the polymer, the solubility of drug, and the ration of the drug to polymer in the capsule. Bimodal release kinetics were exhibited by a number of furosemide formulations (i.e., F5 and F8).
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