Inclusion complex of methyl-β-cyclodextrin and olanzapine as potential drug delivery system for schizophrenia

被引：74

作者：

de Freitas, Marcia Rocha ^{[1
]}

Rolim, Larissa Araujo ^{[2
]}

de La Roca Soares, Monica Felts ^{[1
]}

Rolim-Neto, Pedro Jose ^{[2
]}

de Albuquerque, Miracy Muniz ^{[1
]}

Soares-Sobrinho, Jose Lamartine ^{[1
]}

机构：

[1] Univ Fed Pernambuco, Dept Pharmaceut Sci, NCQMC, Core Med & Corelated Qual Control, BR-50740521 Recife, PE, Brazil

[2] Univ Fed Pernambuco, Dept Pharmaceut Sci, Lab Med Technol, LTM, BR-50740521 Recife, PE, Brazil

来源：

CARBOHYDRATE POLYMERS | 2012年 / 89卷 / 04期

关键词：

Olanzapine; Solubility; Stability; Drug delivery; Cyclodextrin; Dissolution rate; SOLUBILITY; WATER;

D O I：

10.1016/j.carbpol.2012.03.072

中图分类号：

O69 [应用化学];

学科分类号：

081704 ;

摘要：

Olanzapine (OLP), the most important atypical antipsychotic drug of the new generation, a high cost drug, has low aqueous solubility, affecting its dissolution and absorption. Its complexation with modified cyclodextrins (CDs) is designed to achieve novel vectorization systems with higher solubility, consequently higher bioavailability. From the CD selection, among beta-CD, methyl-beta-CD (M beta CD) and hydroxypropyl-beta-CD, it was obtained a phase solubility diagram suggesting a 1:1 (mol:mol) OLP-CD stoichiometry and complexation constants of 966.9, 149.4 and 91.1 L/mol, respectively. The M beta CD was selected for the inclusion complexes (IC) attainment, a physical mixture (PM) and a rotatory evaporator product (ROE). The analysis showed differences in the structure, morphology and performance of OLP, M beta CD, PM and ROE, revealing the occurrence of interactions between drug and CD. The ROE presented the higher dissolution efficiency and stability. The results suggest that the IC was formation, being a technological resource efficient and profitable for drug delivery. (C) 2012 Elsevier Ltd. All rights reserved.

引用

页码：1095 / 1100

页数：6

共 20 条

[1] BETA-CYCLODEXTRIN AS AN EXCIPIENT IN SOLID ORAL DOSAGE FORMS - INVITRO AND INVIVO EVALUATION OF SPRAY-DRIED DIAZEPAM-BETA-CYCLODEXTRIN PRODUCTS [J].