缬沙坦固体脂质纳米粒的研究

The Study on Valsartan Solid Lipid Nanoparticles

固体脂质纳米粒(SLN)可用于溶解度差、渗透性好的药物,改造原有剂型,提高生物利用度。文章以单硬脂酸甘油酯为载体材料,采用乳化蒸发-低温固化法制备缬沙坦-SLN,并考察体外释放。以包封率为评价指标,采用正交设计得到的优化处方为:单硬脂酸甘油酯350 mg,大豆磷脂120 mg,泊洛沙姆188(F68)1 g/m L,转速1 200 r/min。优化所得缬沙坦-SLN平均粒径(362.7±8.8)nm,平均包封率(63.9±0.4)%,载药量(1.07±0.016)%;4℃放置30 d,外观、包封率和载药量均无显著变化,粒径略有差异。体外释放研究显示,缬沙坦-SLN混悬液在磷酸盐缓冲液中0~8 h的释放符合零级释放方程。

Solid lipid nanoparticles can be used for poor solubility and good permeability drugs. It can transform the original dosage form and improve the bioavailability of drugs. Valsartan solid lipid nanoparticles were prepared by emulsification evaporation-solidification at low temperature with glycerin monostearate and its release profile in vitro was studied. The orthogonal design was applied to optimize its formula. Technique was evaluated by the encapsulation efficiencies. Optimal formulation was Glyceryl monostearate350 mg,granulesten 120 mg and poloxamer188( F68) 1 g / m L,rotation speed 1 200 r / min. The valsartan solid lipid nanoparticles were sphere-like with a mean diameter of( 362. 7 ± 8. 8) nm. The entrapment efficiency was( 63. 9 ± 0. 4) % and drug-loading rate was( 1. 07 ± 0. 016) %. There were no obvious changes in entrapment efficiency and drug-loading rate when loaded drug at 4 ° C within a month. The results showed that the entrapment efficiency and drug-loading rate had no significant change and particle diameter was a little different. In vitro studies have shown that valsartan-SLN suspension is in accordance with zero-order release in phosphate buffer at 0 ~ 8 h.