Eedara Basanth Babu, Nyavanandi Dinesh, Narala Sagar, Veerareddy Prabhakar Reddy, Bandari Suresh
Department of Pharmaceutics, St. Peter's Institute of Pharmaceutical Sciences, Vidyanagar, Warangal 506001, India.
Pharmaceutics. 2021 Feb 27;13(3):310. doi: 10.3390/pharmaceutics13030310.
The objective of this study was to enhance dissolution and permeation of a low soluble, absorbable fexofenadine hydrochloride (FFH) by preparing solid dispersions using polyethylene glycol 20,000 (PEG 20,000) and poloxamer 188 as carriers. The phase solubility measurement for the supplied FFH revealed a linear increase in the solubility of fexofenadine with increasing carrier concentration in water (1.45 mg/mL to 11.78 mg/mL with 0% to 30% PEG 20,000; 1.45 mg/mL to 12.27 mg/mL with 0% to 30% poloxamer 188). To select the appropriate drug carrier concentration, a series of solid dispersions were prepared in the drug carrier weight ratios of 1:1, 1:2 and 1:4 by fusion method. The solid dispersions composed of drug carrier at 1:4 weight ratio showed highest dissolution with the time required for the release of 50% of the drug <15 min compared to the supplied FFH (>120 min). The intestinal absorption study presented a significant improvement in the absorption of drug from the solid dispersions composed of poloxamer 188 than PEG 20,000. In summary, the solid dispersions of FFH prepared using PEG 20,000 and poloxamer 188 demonstrated improved dissolution and absorption than supplied FFH and could be used to improve the oral bioavailability of fexofenadine.
本研究的目的是通过使用聚乙二醇20000（PEG 20000）和泊洛沙姆188作为载体制备固体分散体，来提高低溶解性、可吸收的盐酸非索非那定（FFH）的溶出度和渗透率。对所提供的FFH进行的相溶解度测定表明，随着载体在水中浓度的增加，非索非那定的溶解度呈线性增加（0%至30% PEG 20000时，溶解度从1.45 mg/mL增加到11.78 mg/mL；0%至30%泊洛沙姆188时，溶解度从1.45 mg/mL增加到12.27 mg/mL）。为了选择合适的药物载体浓度，通过熔融法以药物与载体的重量比1:1、1:2和1:4制备了一系列固体分散体。与所提供的FFH（>120分钟）相比，重量比为1:4的药物载体组成的固体分散体显示出最高的溶出度，药物释放50%所需的时间<15分钟。肠道吸收研究表明，由泊洛沙姆188组成的固体分散体中药物的吸收比由PEG 20000组成的固体分散体有显著改善。总之，使用PEG 20000和泊洛沙姆188制备的FFH固体分散体比所提供的FFH显示出更好的溶出度和吸收，可用于提高非索非那定的口服生物利用度。
