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Improving Dissolution and Oral Bioavailability of Pranlukast Hemihydrate by Particle Surface Modification With Surfactants and Homogenization

Improving Dissolution and Oral Bioavailability of Pranlukast Hemihydrate by Particle Surface Modification With Surfactants and Homogenization

Eun-Sol Ha, In-hwan Baek, Jin-Wook Yoo, Yunjin Jung, Min-Soo Kim

Drug Des Devel Ther. 2015 Jun 24;9:3257-66.

PMID: 26150699

Abstract:

The present study was carried out to develop an oral formulation of pranlukast hemihydrate with improved dissolution and oral bioavailability using a surface-modified microparticle. Based on solubility measurements, surface-modified pranlukast hemihydrate microparticles were manufactured using the spray-drying method with hydroxypropylmethyl cellulose, sucrose laurate, and water and without the use of an organic solvent. The hydrophilicity of the surface-modified pranlukast hemihydrate microparticle increased, leading to enhanced dissolution and oral bioavailability of pranlukast hemihydrate without a change in crystallinity. The surface-modified microparticles with an hydroxypropylmethyl cellulose/sucrose laurate ratio of 1:2 showed rapid dissolution of up to 85% within 30 minutes in dissolution medium (pH 6.8) and oral bioavailability higher than that of the commercial product, with approximately 2.5-fold and 3.9-fold increases in area under the curve (AUC 0 → 12 h) and peak plasma concentration, respectively. Therefore, the surface-modified microparticle is an effective oral drug delivery system for the poorly water-soluble therapeutic pranlukast hemihydrate.

Chemicals Related in the Paper:

Catalog Number	Product Name	Structure	CAS Number	Price
AP150821037	Pranlukast hemihydrate		150821-03-7	Price

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