Department of Pharmacy, University of Rajshahi, Rajshahi, Bangladesh.
Department of Pharmacy, Islamic University, Kushtia, Bangladesh.
J Pharm Pharmacol. 2020 Jul;72(7):909-915. doi: 10.1111/jphp.13267. Epub 2020 Apr 19.
Hyperlipidaemia is a common phenomenon in diabetes mellitus. Fenofibrate (FF) is a good candidate for the treatment of lipid abnormalities in patients with type 2 diabetes. But the bioavailability as well as therapeutic efficacy of this drug is limited to its dissolution behaviour. Here, the authors assess the therapeutic efficacy of a newly formulated solid dispersion of fenofibrate (SDF) having enhanced dissolution profiles in contrast to pure FF using fructose-induced diabetic rat model.
Fructose-induced diabetic rat model was developed to assess the pharmacological efficacy of the formulated SDF, and the results were compared with the effects of conventional FF therapy.
The 14 days treatment showed better improvement in lipid-lowering potency of SDF than pure FF. SDF containing one-third dose of pure FF showed similar effect in terms of triglyceride, total cholesterol and low-density lipoprotein lowering efficacy, whereas increased high-density lipoprotein at same extent. The similar dose of SDF produced more prominent effect than FF. Histological studies also demonstrated the enhanced lipid clearance from liver by SDF than FF that was concordant with the biochemical results.
This newly formulated SDF would be a promising alternative for conventional fenofibrate in treating hyperlipidaemia.
高脂血症是糖尿病的常见现象。非诺贝特(FF)是治疗 2 型糖尿病患者脂质异常的理想药物。但该药物的生物利用度和治疗效果受其溶解行为的限制。本文作者使用果糖诱导的糖尿病大鼠模型,评估了具有增强溶解特性的新型非诺贝特固体分散体(SDF)的治疗效果,与纯 FF 相比。
建立果糖诱导的糖尿病大鼠模型,以评估所制备 SDF 的药效,并将结果与常规 FF 治疗的效果进行比较。
14 天的治疗显示 SDF 在降低血脂方面的效果优于纯 FF。SDF 中的三分之一剂量的纯 FF 具有相似的降低甘油三酯、总胆固醇和低密度脂蛋白的效果,而高密度脂蛋白的增加程度相同。相同剂量的 SDF 产生的效果比 FF 更显著。组织学研究也表明 SDF 比 FF 更能增强从肝脏清除脂质,这与生化结果一致。
这种新配方的 SDF 将成为治疗高脂血症的常规非诺贝特的一种有前途的替代药物。