Study on the Role of the Inclusion Complexes with 2-Hydroxypropyl-β-cyclodextrin for Oral Administration of Amiodarone

被引：20

作者：

Creteanu, Andreea ^{[1
]}

Pamfil, Daniela ^{[2
]}

Vasile, Cornelia ^{[2
]}

Tantaru, Gladiola ^{[3
]}

Ghiciuc, Cristina Mihaela ^{[4
]}

Ochiuz, Lacramioara ^{[1
]}

Ghilan, Alina ^{[2
]}

Macsim, Ana Maria ^{[2
]}

机构：

[1] Grigore T Popa Univ Med & Pharm Iasi, Fac Pharm, Dept Pharmaceut Technol, 16 Univ Str, Iasi 700115, Romania

[2] Petru Poni Inst Macromol Chem, Phys Chem Polymers Dept, 41A Gr Ghica Voda Alley, RO-700487 Iasi, Romania

[3] Grigore T Popa Univ Med & Pharm, Fac Pharm, Dept Analyt Chem, 16 Univ Str, Iasi 700115, Romania

[4] Grigore T Popa Univ Med & Pharm, Fac Med, Dept Pharmacol, 16 Univ Str, Iasi 700115, Romania

来源：

INTERNATIONAL JOURNAL OF POLYMER SCIENCE | 2019年 / 2019卷

关键词：

HYDROXYPROPYL-BETA-CYCLODEXTRIN; DRUG-DELIVERY; IN-VITRO; SOLUBILITY; BIOAVAILABILITY; HYDROCHLORIDE; FORMULATIONS; DERIVATIVES; PHARMACOKINETICS; DISSOLUTION;

D O I：

10.1155/2019/1695189

中图分类号：

O63 [高分子化学（高聚物）];

学科分类号：

070305 ; 080501 ; 081704 ;

摘要：

The aim of this study was to improve the solubility of amiodarone hydrochloride (AMD) and the drug release using its inclusion complexes with 2-hydroxypropyl-beta-cyclodextrin (HP-beta-CD). The inclusion complexes were prepared by coprecipitation and freeze-drying. The solubility enhancement of AMD/HP-beta-CD inclusion complexes by 4-22 times was evaluated by the phase solubility method. The inclusion complexes were studied both in solution and in solid state by spectroscopic methods, dynamic light scattering (DLS) and zeta potential analysis, SEM, and DSC. The formulations of AMD/HP-beta-CD inclusion complexes both as powdered form and as matrix tablets showed superior pharmacokinetic performance in improving loading and release properties in respect of those of the insoluble AMD drug. In vitro kinetic study reveals a complex mechanism of release occurring in three steps: the first one being attributed to a burst effect and the other two to different bonding existing in inclusion complexes. An in vivo test on matrix tablets containing Kollidon (R) and chitosan also reveals a multiple (at least two) peaks release diagram because of both structures of the inclusion complexes and also of different sites of absorption in biological media (digestive tract).

引用

页数：23

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