Dual Activity of Hydroxypropyl-β-Cyclodextrin and Water-Soluble Carriers on the Solubility of Carvedilol

被引:13
|
作者
Zoghbi, Abdelmoumin [1 ,2 ]
Geng, Tianjiao [1 ]
Wang, Bo [1 ]
机构
[1] China Pharmaceut Univ, Dept Pharmaceut, 639 Longmian Ave, Nanjing 211198, Jiangsu, Peoples R China
[2] Ferhat Abbas Univ, Dept Pharm, Setif 19000, Algeria
来源
AAPS PHARMSCITECH | 2017年 / 18卷 / 08期
关键词
carvedilol; inclusion complex; solid dispersion; solubility; bioavailability; INCLUSION COMPLEX; SOLID DISPERSIONS; IN-VITRO; PHYSICOCHEMICAL PROPERTIES; ORAL DELIVERY; DISSOLUTION; DRUGS; SYSTEMS; ACID; BIOAVAILABILITY;
D O I
10.1208/s12249-017-0769-2
中图分类号
R9 [药学];
学科分类号
1007 ;
摘要
Carvedilol (CAR) is a non-selective alpha and beta blocker categorized as class II drug with low water solubility. Several recent studies have investigated ways to overcome this problem. The aim of the present study was to combine two of these methods: the inclusion complex using hydroxypropyl-beta-cyclodextrin (HP beta CD) with solid dispersion using two carriers: Poloxamer 188 (PLX) and Polyvinylpyrrolidone K-30 (PVP) to enhance the solubility, bioavailability, and the stability of CAR. Kneading method was used to prepare CAR-HP beta CD inclusion complex (KD). The action of different carriers separately and in combination on Carvedilol solubility was investigated in three series. CAR-carrier and KD-carrier solid dispersions were prepared by solvent evaporation method. In vitro dissolution test was conducted in three different media: double-distilled water (DDW), simulative gastric fluid (SGF), and PBS pH 6.8 (PBS). The interactions between CAR, HP beta CD, and different carriers were explored by Fourier transform infrared spectroscopy (FTIR), powder X-ray diffractometry (XRD), and differential scanning colorimetry (DSC). The results showed higher solubility of CAR in KD-PVP solid dispersions up to 70, 25, and 22 fold compared to pure CAR in DDW, SGF, and PBS, respectively. DSC and XRD analyses indicated an improved degree of transformation of CAR in KD-PVP solid dispersion from crystalline to amorphous state. This study provides a new successful combination of two polymers with the dual action of HP beta CD and PLX/PVP on water solubility and bioavailability of CAR.
引用
收藏
页码:2927 / 2935
页数:9
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