Ahmed M, Ramadan W, Rambhu D, Shakeel F
Department of Pharmaceutical Chemistry, Faculty of Pharmacy, Alarab Medical Sciences University, Benghazi, Libya.
Pharmazie. 2008 Nov;63(11):806-11.
The aim of the present study was to develop, characterize and evaluate nanoemulsion formulations for intravenous delivery of rifampicin (RIF). Different oil-in-water (o/w) nanoemulsions were prepared by the aqueous phase titration method. Prepared nanoemulsions were subjected to thermodynamic stability tests for phase separation, creaming, cracking, coalescence or phase inversion and dispersibility test for dilution capacity. Nanoemulsion formulations which passed these tests were characterized in terms of droplet size, viscosity, entrapment efficiency, homogeneity and pH. The selected formulations were subjected to in vitro dissolution studies using a dissolution apparatus-XXIII in dialysis bag. Best results were obtained with the formulation which consisted of 150 mg of RIF, 15% w/w of Sefsol 218, 18.75% w/w of Tween 80, 6.25% w/w of Tween 85 and 60% w/w of normal saline. The optimized formulation was also subjected to stability studies according to the ICH guidelines. The formulation was found to be stable for more than19 months. These results indicated the potential of nanoemulsions for intravenous delivery of RIF.
本研究的目的是开发、表征和评估用于利福平(RIF)静脉给药的纳米乳剂制剂。通过水相滴定法制备了不同的水包油(o/w)纳米乳剂。对制备的纳米乳剂进行相分离、乳析、破裂、聚结或相转变的热力学稳定性测试以及稀释能力的分散性测试。通过这些测试的纳米乳剂制剂在液滴大小、粘度、包封率、均匀性和pH值方面进行表征。使用透析袋中的溶出度装置-XXIII对所选制剂进行体外溶出研究。由150 mg RIF、15% w/w的Sefsol 218、18.75% w/w的吐温80、6.25% w/w的吐温85和60% w/w的生理盐水组成的制剂获得了最佳结果。根据ICH指南对优化后的制剂进行稳定性研究。发现该制剂在超过19个月的时间内是稳定的。这些结果表明纳米乳剂用于RIF静脉给药的潜力。