负载西尼地平的自乳化给药系统的体外脂解、稳定性和药效学研究

IF 0.3 Q4 PHARMACOLOGY & PHARMACY
R. Kadian, Arun Nanda
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引用次数: 0

摘要

这项研究工作的目的是调查西尼地平掺入自乳化给药系统(SEDDS)改善西尼地平溶解度和口服生物利用度的潜在能力。自乳化给药系统(SEDDS)被广泛用于水溶性差的药物,以提高其溶解度和口服生物利用度。为了提高水溶性差的药物的溶解度和口服生物利用度,SEDDS 被经常使用。为了开发西尼地平负载 SEDDS 制剂,使用了菜籽油作为油相,吐温 80 作为表面活性剂,PEG 300 作为辅助表面活性剂。根据 ICH 指南对 SEDDS 制剂进行了稳定性研究、空腹和进食状态下体外脂肪分解研究中的药物沉淀以及 Wistar 大鼠体内药效学研究。药效学研究表明,与西尼地平悬浮剂相比,西尼地平载药 SEDDS 制剂能显著产生快速降压效果(2 小时内),且持续 24 小时。在体外脂肪分解研究中,无论在空腹还是进食状态下,10 分钟后从水相中回收的药物浓度均超过 90%,只有少量药物参与沉淀。在 30±2 °C/65±5%RH 的稳定条件下,SEDDS 制剂在 6 个月内保持稳定。采用自乳化给药方法可以提高 BCS 二类药物的口服生物利用度和溶出度。
本文章由计算机程序翻译,如有差异,请以英文原文为准。
In-vitro Lipolysis, Stability and Pharmacodynamic Study of Cilnidipine Loaded Self-emulsifying Drug Delivery System
The aim of this research work was to investigate the potential ability of cilnidipineloaded- Self-Emulsifying Drug Delivery System (SEDDS) to improve the solubility and oral bioavailability of cilnidipine. The limited oral bioavailability of BCS class II drugs restricts the clinical utility of drugs. Self-emulsifying drug delivery systems (SEDDS) are widely used for poorly water-soluble drugs to enhance their solubility and oral bioavailability. The therapeutic value of drugs is constrained by the low oral bioavailability of BCS class II drugs. In order to improve the solubility and oral bioavailability of poorly water-soluble drugs, SEDDS are frequently utilised. To develop the cilnidipine-loaded-SEDDS formulation, Canola oil as the oil phase, tween 80 as the surfactant, and PEG 300 as the co-surfactant were used. The SEDDS formulation was evaluated based on stability study per ICH guidelines, drug precipitation during in-vitro lipolysis study under fasted and fed state, and in vivo pharmacodynamic study in Wistar rats. The content of the drug was determined by assay of SEDDS formulation using the official method of cilnidipine. The pharmacodynamic study demonstrated that cilnidipine-loaded SEDDS formulation significantly produced a rapid antihypertensive effect (within 2 h) that lasted for 24 h in comparison to drug suspension. During the in vitro lipolysis study, the concentration of the drug recovered from the aqueous phase under both fasted and fed state was more than 90% after 10 minutes, with a minute amount of drug involved in precipitation. At stability conditions of 30±2 °C/65±5%RH for a duration of six months, the SEDDS formulation was found to be stable. The content of cilnidipine in the SEDDS formulation was found to be 98.4%. A BCS class-II drug's oral bioavailability and dissolution might be improved using the self-emulsifying drug delivery method.
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来源期刊
Current Drug Therapy
Current Drug Therapy PHARMACOLOGY & PHARMACY-
CiteScore
1.30
自引率
0.00%
发文量
50
期刊介绍: Current Drug Therapy publishes frontier reviews of high quality on all the latest advances in drug therapy covering: new and existing drugs, therapies and medical devices. The journal is essential reading for all researchers and clinicians involved in drug therapy.
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