Improving dissolution and oral bioavailability of pranlukast hemihydrate by particle surface modification with surfactants and homogenization.
Drug Des Devel Ther
; 9: 3257-66, 2015.
Article
in En
| MEDLINE
| ID: mdl-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 12 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 â 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.
Key words
Full text:
1
Collection:
01-internacional
Database:
MEDLINE
Main subject:
Surface-Active Agents
/
Chromones
/
Leukotriene Antagonists
Type of study:
Prognostic_studies
Limits:
Animals
Language:
En
Journal:
Drug Des Devel Ther
Journal subject:
FARMACOLOGIA
/
TERAPIA POR MEDICAMENTOS
Year:
2015
Document type:
Article