Jeevana Jyothi B, Sreelakshmi K
Institute of Pharmaceutical Technology, Sri Padmavathi Mahila Viswavidyalayam (Women's University), Tirupati, Andhra Pradesh - 517 502, India.
J Young Pharm. 2011 Jan;3(1):4-8. doi: 10.4103/0975-1483.76413.
Flutamide (FLT) is an antiandrogen drug for the treatment of prostate cancer. It has the drawback of poor water solubility and needs enhancement of its dissolution rate in simulated gastric fluids. Hence, it is prepared as self-nanoemulsifying drug delivery systems (SNEDDS) with an aim to enhance its dissolution rate. The objectives of the study are to develop SNEDDS of FLT and to characterize for particle size, self-nanoemulsification, and dissolution enhancement. Solubility of FLT was determined in various oils, surfactants, and cosurfactants. Sesame oil was selected as an oil phase, Tween 20 as surfactant, and PEG400 as cosurfactant due to their higher solubilization effect. Various formulations were prepared by simple mixing followed by vortexing. From studies, the optimized SNEDDS formulation was composed of FLT (8.04% w/w), sesame oil (24.12% w/w), Tween 20 (53.38% w/w), and PEG400 (14.46% w/w). The selected SNEDDS could be self-emulsified without precipitation upon simple mixing. The mean particle size of the SNEDDS was 148.7 nm and percent drug content was 99.66. The dissolution rate of FLT from SNEDDS was faster and higher in three different dissolution media such as 2% sodium lauryl sulfate (97.85%), simulated gastric fluid (0.1 N HCl containing 0.5% Tween 20) (95.71%), and simulated intestinal fluid (pH 6.8 buffer) (96.21%).
氟他胺（FLT）是一种用于治疗前列腺癌的抗雄激素药物。它存在水溶性差的缺点，需要提高其在模拟胃液中的溶解速率。因此，将其制备成自纳米乳化药物递送系统（SNEDDS），旨在提高其溶解速率。本研究的目的是开发氟他胺的SNEDDS，并对其粒径、自纳米乳化和溶出度增强进行表征。测定了氟他胺在各种油、表面活性剂和助表面活性剂中的溶解度。由于芝麻油、吐温20和聚乙二醇400具有较高的增溶效果，因此分别选择它们作为油相、表面活性剂和助表面活性剂。通过简单混合并涡旋制备了各种制剂。通过研究，优化后的SNEDDS制剂由氟他胺（8.04% w/w）、芝麻油（24.12% w/w）、吐温20（53.38% w/w）和聚乙二醇400（14.46% w/w）组成。所选的SNEDDS在简单混合后可自乳化且无沉淀。SNEDDS的平均粒径为148.7 nm，药物含量百分比为99.66。在三种不同的溶出介质中，氟他胺从SNEDDS中的溶出速率更快且更高，这三种介质分别是2%十二烷基硫酸钠（97.85%）、模拟胃液（含0.5%吐温20的0.1 N HCl）（95.71%）和模拟肠液（pH 6.8缓冲液）（96.21%）。
