奥美沙坦酯载脂纳米粒和混悬剂的研制：制备、表征和比较药代动力学评价。

Development of olmesartan medoxomil lipid-based nanoparticles and nanosuspension: preparation, characterization and comparative pharmacokinetic evaluation.

机构信息

a Laboratory of Nanotechnology, Department of Pharmaceutical Sciences , University college of Pharmaceutical Sciences, Kakatiya University , Warangal , Telangana , India.

出版信息

Artif Cells Nanomed Biotechnol. 2018 Feb;46(1):126-137. doi: 10.1080/21691401.2017.1299160. Epub 2017 Mar 14.

DOI:10.1080/21691401.2017.1299160

PMID:28290712

Abstract

The aim was to enhance the oral bioavailability of olmesartan medoxomil (OM) by preparing solid lipid nanoparticles (SLNs) and comparing with nanosuspension (OM-NS). OM-SLNs and OM-NS were prepared by known methods. Prepared SLNs were evaluated for physical characters and in vivo pharmacokinetic (PK) performance in rats. OM-NS showed more than four-fold increase in the solubility. During DSC and XRD studies, drug incorporated in SLNs was found to be in amorphous form. The relative bioavailability of OM-SLN and OM-NS was 7.21- and 3.52-fold when compared with that of coarse suspension. Further, OM-SLNs also increased the oral bioavailability by two-fold over that of OM-NS.

摘要

目的是通过制备固体脂质纳米粒（SLNs）并与纳米混悬剂（OM-NS）进行比较，来提高奥美沙坦酯（OM）的口服生物利用度。OM-SLNs 和 OM-NS 是通过已知的方法制备的。对制备的 SLNs 进行了物理性质和大鼠体内药代动力学（PK）性能的评价。OM-NS 的溶解度增加了四倍以上。在 DSC 和 XRD 研究中，发现 SLNs 中包封的药物呈无定形状态。与粗混悬剂相比，OM-SLN 和 OM-NS 的相对生物利用度分别提高了 7.21 倍和 3.52 倍。此外，OM-SLNs 还使 OM-NS 的口服生物利用度提高了一倍。