title: Improving dissolution and oral bioavailability of pranlukast hemihydrate by particle surface modification with surfactants and homogenization.
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.
authors.affiliation: College of Pharmacy, Pusan National University, Busan, Republic of Korea.
authors.forename: Eun-Sol
authors.initials: ES
authors.lastname: Ha
authors.affiliation: College of Pharmacy, Kyungsung University, Busan, Republic of Korea.
authors.forename: In-hwan
authors.initials: IH
authors.lastname: Baek
authors.affiliation: College of Pharmacy, Pusan National University, Busan, Republic of Korea.
authors.forename: Jin-Wook
authors.initials: JW
authors.lastname: Yoo
authors.affiliation: College of Pharmacy, Pusan National University, Busan, Republic of Korea.
authors.forename: Yunjin
authors.initials: Y
authors.lastname: Jung
authors.affiliation: College of Pharmacy, Pusan National University, Busan, Republic of Korea.
authors.forename: Min-Soo
authors.initials: MS
authors.lastname: Kim
mesh_terms: D000284:Administration, Oral; D000818:Animals; D019540:Area Under Curve; D001682:Biological Availability; D002626:Chemistry, Pharmaceutical; D002867:Chromones / Q000008:administration & dosage* / Q000097:blood / Q000737:chemistry / Q000493:pharmacokinetics*; D018360:Crystallography, X-Ray; D065347:Hypromellose Derivatives / Q000737:chemistry; D020024:Leukotriene Antagonists / Q000008:administration & dosage* / Q000097:blood / Q000737:chemistry / Q000493:pharmacokinetics*; D008297:Male; D008855:Microscopy, Electron, Scanning; D033362:Powder Diffraction; D017207:Rats, Sprague-Dawley; D012995:Solubility; D013395:Sucrose / Q000031:analogs & derivatives / Q000737:chemistry; D013499:Surface Properties; D013501:Surface-Active Agents / Q000737:chemistry*; D013678:Technology, Pharmaceutical / Q000379:methods; D014867:Water / Q000737:chemistry
chemical_list: D002867:Chromones; D020024:Leukotriene Antagonists; D013501:Surface-Active Agents; D014867:Water; C018152:sucrose monolaurate; D065347:Hypromellose Derivatives; D013395:Sucrose; C047681:pranlukast
keywords: cellulose; solubility; sucrose laurate; wettability