Rheological evaluation of thermosensitive and mucoadhesive vaginal gels in physiological conditions

被引:196
作者
Chang, JY
Oh, YK
Choi, HG
Kim, YB
Kim, CK
机构
[1] Seoul Natl Univ, Coll Pharm, Natl Res Lab Drug & Gene Delivery, Seoul 151742, South Korea
[2] Korea Food & Drug Adm, Div Antibiot, Seoul 122704, South Korea
[3] Pochon CHA Univ, Coll Med, Kyonggi Do, South Korea
[4] Pochon CHA Univ, Inst Med Res, Kyonggi Do, South Korea
[5] Yeungnam Univ, Coll Pharm, Kyongsan 712749, South Korea
关键词
rheology; poloxamer; thermosensitive gel; clotrimazole; vaginal formulation;
D O I
10.1016/S0378-5173(02)00232-6
中图分类号
R9 [药学];
学科分类号
1007 ;
摘要
The timely gelation and retention of in situ-gelling vaginal formulations would be fundamental to improve the efficacy of drugs. In this study, various rheological properties of clotrimazole gels were evaluated for predicting their performance in vagina. Two kinds of thermosensitive and mucoadhesive formulations were composed of poloxamer 407 (P407, 15%), polycarbophil (0.2%), and different amounts of P188 (15 vs. 20%). Both formulations were Newtonian at 20 degreesC but non-Newtonian at 37 degreesC. Although both liquid formulations gelled below the vaginal temperature, they differed in gelation time and viscoelastic properties in the presence of vaginal fluid simulant. At body temperature, the formulation with 20% of P188 gelled within 35 s but it took two times longer for the other one gelled. Upon dilution with simulated vaginal fluid, the formulation with 20% of P188 retained the rheology of a gel, but the other one lost the viscoelastic properties typical for a gel. Moreover, after dilution with simulated vaginal fluid, the elastic modulus was orders of magnitude higher in the formulations with 20% of P188 relative to the other one. These results indicate that the rheological evaluation at the physiologic conditions needs to be preceded to develop more effective in situ-gelling vaginal formulations. (C) 2002 Elsevier Science B.V. All rights reserved.
引用
收藏
页码:155 / 163
页数:9
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