Abstract

Objective of study was to develop a solid self-nanoemulsifying rosuvastatin drug delivery system (S-SNEDDS) for enhancement of its oral bioavailability and to produce synergistic action with garlic oil for better management of hypertriglyceridemia. Results showed that mean globule size of all reconstituted self-nanoemulsifying drug delivery system (SNEDDS) was found to be in nanometric range (48.32–73.64 nm) with optimum polydispersibility index (PDI) values (0.215–0.448). Rosuvastatin release from SNEDDS formulae in vitro showed that more than 75% of rosuvastatin released in about 30 min. Optimized SNEDDS formulae were selected for use with spray drying technique to develop into S-SNEDDS. Rosuvastatin plasma concentrations in rats treated with S-SNEDDS have been found at all times to be substantially high. When garlic oil-loaded rosuvastatin S-SNEDDS was administered orally to poloxamer-407 (P-407) induced hypertriglyceridemia rats there was significant (p ˂ 0.01) more increase in high-density lipoprotein (HDL) (19.24 ± 0.40 mg/dl) in comparision to rosuvastatin commercial tablet treated group. Rosuvastatin commercial tablet treated group showed significantly (p ˂ 0.01) less PT and APTT as compared to garlic oil loaded rosuvastatin S-SNEDDS treated group. Findings showed that garlic oil loaded rosuvastatin S-SNEDDS might play important role in better management of hypertriglyceridemia.

摘要

研究目的是开发一种固体自纳米乳化罗苏伐他汀给药系统 (S-SNEDDS)，以提高其口服生物利用度，并与大蒜油产生协同作用，以更好地控制高甘油三酯血症。结果表明，发现所有重组自纳米乳化药物递送系统 (SNEDDS) 的平均小球尺寸在纳米范围内 (48.32–73.64 nm)，具有最佳多分散性指数 (PDI) 值 (0.215–0.448)。SNEDDS 配方体外释放的瑞舒伐他汀表明，超过 75% 的瑞舒伐他汀在约 30 分钟内释放。选择优化的 SNEDDS 配方与喷雾干燥技术一起使用以开发成 S-SNEDDS。已发现用 S-SNEDDS 治疗的大鼠中的瑞舒伐他汀血浆浓度始终很高。p˂ 0.01) 与瑞舒伐他汀商业片剂治疗组相比，高密度脂蛋白 (HDL) (19.24 ± 0.40 mg/dl) 增加更多。与负载大蒜油的瑞舒伐他汀 S-SNEDDS 治疗组相比，瑞舒伐他汀商业片剂治疗组的 PT 和 APTT 显着降低 ( p˂ 0.01)。研究结果表明，负载大蒜油的瑞舒伐他汀 S-SNEDDS 可能在更好地管理高甘油三酯血症方面发挥重要作用。