In situ absorption and relative bioavailability studies of zaleplon loaded self-nanoemulsifying powders

被引：21

作者：

Janga, Karthik Y. ^{[1
]}

Jukanti, Raju ^{[1
]}

Sunkavalli, Sharath ^{[1
]}

Velpula, Ashok ^{[1
]}

Bandari, Suresh ^{[1
]}

Kandadi, Prabhakar ^{[1
]}

Veerareddy, Prabhakar Reddy ^{[1
]}

机构：

[1] St Peters Inst Pharmaceut Sci, Dept Pharmaceut, Warangal, Andhra Pradesh, India

来源：

JOURNAL OF MICROENCAPSULATION | 2013年 / 30卷 / 02期

关键词：

zaleplon; oral delivery; self-nanoemulsifying powder; neusilin US2; in situ perfusion; bioavailability; DRUG-DELIVERY SYSTEM; ORAL BIOAVAILABILITY; LYMPHATIC TRANSPORT; LIPID NANOPARTICLES; CYCLOSPORINE-A; FORMULATION; DESIGN; HALOFANTRINE; RATS; PHARMACOKINETICS;

D O I：

10.3109/02652048.2012.714408

中图分类号：

O69 [应用化学];

学科分类号：

081704 ;

摘要：

Self-nanoemulsifying drug delivery systems (SNEDDSs) offer potential as suitable carriers for improved oral delivery of poorly soluble and low bioavailable drugs. To derive self-nanoemulsifying powders (SNEPs), the optimized Z-SNEDDS formulation was adsorbed onto different carriers and based on micromeritics the formulation loaded onto neusilin US2 (SNEP-N) was selected for further characterization. The solid-state characterization (scanning electron microscopy, differential scanning calorimetry and powder X-ray diffraction) studies unravel the transformation of native crystalline state to amorphous and/or molecular state. The higher predictive effective permeability coefficient and fraction absorbed in humans extrapolated from in situ single-pass intestinal absorption study data in rats provide an insight on the potential of SNEPs for augment in absorption across gastrointestinal barrier. Overall a 3.5-fold enhancement in the extent of absorption of zaleplon from SNEP-N formulation proves the feasibility of SNEPs formulation for improved oral delivery of zaleplon.

引用

页码：161 / 172

页数：12

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