期刊
INTERNATIONAL JOURNAL OF PHARMACEUTICS
卷 428, 期 1-2, 页码 18-24出版社
ELSEVIER SCIENCE BV
DOI: 10.1016/j.ijpharm.2012.02.041
关键词
Tacrolimus; Solid dispersion; Solubilization; Eudragit (R) E; Supersaturation; Reprecipitation inhibitor
资金
- Grants-in-Aid for Scientific Research [20106004] Funding Source: KAKEN
The aim of this study was to investigate the effect of Eudragit E (R)/HCl (E-SD) on the reprecipitation of a poorly water-soluble drug, tacrolimus. To evaluate the inhibition of reprecipitation of E-SD, reprecipitation studies on tacrolimus were conducted using a dissolution test method. Solubility of tacrolimus was measured at regular intervals in a dissolution media, in which tacrolimus was dissolved in ethanol, and the test media contained additives for inhibiting precipitation. Supersaturation profiles of tacrolimus were observed, and were maintained for 24 h only with E-SD. Solid dispersion formulations of tacrolimus prepared with hydroxypropylmethylcellulose (HPMC) or E-SD in different drug/carrier ratios were also investigated. Solid dispersions prepared with E-SD showed higher solubility of tacrolimus compared with that of HPMC. In the E-SD formulation, the drug solubility influences to drug/carrier ratio. The formulation of drug/E-SD (1/5) showed the highest drug solubility. Thus, it may be inferred that a definite drug/carrier ratio exists to increase drug solubility. Further, by mixing E-SD the solid dispersion prepared with HPMC showed enhanced drug solubility. (C) 2012 Elsevier B.V. All rights reserved.
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