a Department of Pharmaceutics and Industrial Pharmacy , Horus University , New Damietta , Egypt.
b Department of Pharmaceutics and Industrial Pharmacy , Sinai University , North Sinai , Egypt.
Drug Dev Ind Pharm. 2019 Jun;45(6):981-994. doi: 10.1080/03639045.2019.1590392. Epub 2019 Mar 19.
A nanoparticulate system; cubosomes has been suggested to support the controlled release of Telmisartan (TEL), a poorly water-soluble medication. Four distinctive formulae were selected according to the results of three estimated responses. The liquid cubosomes were successfully adsorbed onto Aerosil 380 to form granules. The formulae were evaluated for their flow properties. The best granules were compressed into tablets suitable for oral administration. The tablets were evaluated for its performance. The in vivo study of the best selected cubosomal tablets was checked after oral administration in the blood of albino rabbits utilizing an HPLC method. Results revealed that the highest EE was shown in formulae C5 (59.68 ± 1.3). All the prepared formulae had particle size less than 500 nm with PDI < 0.5 and the highest zeta potential results were observed in C5, C7, C9, C11 and C12 (>30 mv). A7 and A9 prepared using Aerosil 380 showed a perfect flowability. After 1 h of dissolution testing, the commercial product showed a 66% drug release while the release of all cubosomal formulae didn't exceed 35% during the first hour reaching a 85% of the drug released at the end of 24 h. A7 was selected for the in vivo study; T of TEL absorption is increased for cubosomal formula by three folds indicating sustained release pattern. The relative bioavailability is also increased by 2.6 fold. The investigation proposed the rationality of cubosome to figure an effective controlled release tablets to improve its bioavailability and expand its activity.
一种纳米颗粒系统;立方脂质体被认为可以支持替米沙坦(TEL)的控制释放,替米沙坦是一种水溶性差的药物。根据三种估计响应的结果选择了四种不同的配方。成功将液体立方脂质体吸附到 Aerosil 380 上形成颗粒。评估了配方的流动特性。将最好的颗粒压缩成片剂,适合口服。评估了片剂的性能。利用 HPLC 法在白化兔血液中口服后,检查了最佳选择的立方体片剂的体内研究。结果表明,配方 C5 的 EE 最高(59.68±1.3)。所有制备的配方的粒径均小于 500nm,PDI<0.5,最高的 ζ 电位结果观察到在 C5、C7、C9、C11 和 C12(>30mv)。使用 Aerosil 380 制备的 A7 和 A9 表现出完美的流动性。在 1 小时的溶解试验后,市售产品显示出 66%的药物释放,而所有立方体配方在第一个小时内的药物释放不超过 35%,在 24 小时结束时释放了 85%的药物。选择 A7 进行体内研究;TEL 吸收的 T 增加了立方体制剂的三倍,表明其具有持续释放模式。相对生物利用度也增加了 2.6 倍。研究提出了立方体制备有效控制释放片剂以提高其生物利用度并扩大其活性的合理性。