Enhanced diuretic action of furosemide by complexation with β-cyclodextrin in the presence of sodium lauryl sulfate

Green Processing and Synthesis

article

Ramadan I. Al-Shdefat¹ 

[1] Department of Pharmaceutical Sciences, Faculty of Pharmacy, Jadara University

关键词: furosemide;    cyclodextrin;    complex;    solubility;    diuretic activity;   

DOI  :  10.1515/gps-2020-0069

来源: De Gruyter

【 摘 要 】

Preparation of inclusion complex using cyclodextrins is a well-known formulation strategy to elevate the solubility of drugs. However, often cyclodextrins alone may not bring a considerable improvement in the solubility of low solubility drugs. In this study, the inclusion complexation of furosemide (FSM) was tried with β-cyclodextrin (β-CD) either with the use or without the use of sodium lauryl sulfate (SLS), which is a surfactant. By using the kneading method, the binary complex of FSM/β-CD in the equal molar ratio was used. FSM and β-CD were kneaded continuously until a thick past was achieved, which was evaporated for a period of about 24 h. The solid complexed product was then crushed and stored in airtight container until use. Phase solubility studies confirmed a stoichiometric ratio of 1:1 (FSM/β-CD and FSM/β-CD with SLS). The apparent stability constant and complexation efficiencies of significantly enhanced in the presence of SLS. The prepared complexes were evaluated for DSC, PXRD, 1 H NMR, and in vitro release studies. The results exhibited a significant enhancement in diuresis in rats. It is evident that the addition of SLS with β-CD significantly enhances the solubilizing efficiencies and hence bioavailability of FSM.

【 授权许可】

CC BY