Synthesis, characterization and in vitro release studies of a new acetazolamide-HP-β-CD-TEA inclusion complex

被引：57

作者：

Granero, Gladys E. ^{[1
]}

Maitre, Marcos A. ^{[1
]}

Garnero, Claudia ^{[1
]}

Longhi, Marcela R. ^{[1
]}

机构：

[1] Univ Nacl Cordoba, Fac Ciencias Quim, Dept Farm, RA-5000 Cordoba, Argentina

来源：

EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY | 2008年 / 43卷 / 03期

关键词：

acetazolamide; topical preparation; cyclodextrins; triethanolamine; in vitro release studies;

D O I：

10.1016/j.ejmech.2007.03.037

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

The aim of our work was to develop a multicomponent inclusion complex of acetazolamide (ACZ) in order to investigate the combined effect of hydroxypropyl-beta-cyclodextrin (HP-beta-CD) and triethanolamine (TEA) on the solubility of ACZ and its possibility of ophthalmic delivery. Phase solubility study was used to evaluate the complexation in solution at 25 degrees C. Complex formation was also evaluated by comparing the infrared (FT-IR) spectra of the solid complexes with a simple physical mixture containing the same amount of ACZ. FF-IR experiments provided data indicating that the carbonaraido group of ACZ is involved in the inclusion process. In vitro release data showed that both formulations, containing the freeze-dried ternary complex and the corresponding simple physical mixture of ACZ with HP-beta-CD and TEA presented the fastest release rate of ACZ. These results suggest that the ACZ-HP-beta-CD-TEA complex represents an effective novel formulation to enhance ACZ solubility in water, turning it promising for ophthalmic administration. (c) 2007 Elsevier Masson SAS. All rights reserved.

引用

页码：464 / 470

页数：7

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