Production of an extremly low dose procaterol HCl preparation by fluidized-bed coating method: in vitro and in vivo evaluation.
A convenient and reliable method to prepare procaterol HCl oral dosage form at an extremely low dosage (25 microg/cap) is presented in this paper. Procaterol HCl was mixed with the film-forming agent hydroxypropyl methylcellulose in an aqueous solution, which was then spray-coated on sugar spheres (Nu-pareil PG 20/25) to produce procaterol HCl pellets. The IR spectra of coated and noncoated pellets indicated that procaterol HCl was coated on the sugar spheres successfully with a weight increment less than 1%. Most of the coated pellets were able to pass through an 18-mesh screen with no agglomeration. The average weights of coated pellets filled inside of capsules were monitored during the filling process. A simple liquid chromatographic method was developed and validated for the assay and uniformity test of procaterol HCl in different dosage forms. The results of assay and content uniformity test for both in-house product and a commercial product, i.e., Meptin-mini tablet, were satisfied. The data of f(2) function and ANOVA analysis for the dissolution profiles of both procaterol HCl products suggested that they are pharmaceutical equivalent. In an in vivo study (n = 24), a single dose of 75 microg procaterol HCl was administrated to each volunteer and the plasma concentration of procaterol was determined by a LC/MS/MS method, developed by the same authors. There were no significant differences (p > 0.05) in the data of AUC(0-->16 h), AUC(0-->infinity), C(max), and MRT for both preparations. It is confirmed that the pellets capsule produced in this study is bioequivalent with Meptin-mini tablet.
Yu
T-W
TW
School of Pharmacy, College of Medicine, National Taiwan University, Taipei, Taiwan.
Chen
R R-L
RR
Gau
C-S
CS
D000284:Administration, Oral; D000318:Adrenergic beta-Agonists / Q000008:administration & dosage / Q000737:chemistry / Q000493:pharmacokinetics*; D000328:Adult; D002214:Capsules; D002851:Chromatography, High Pressure Liquid; D018592:Cross-Over Studies; D006801:Humans; D008297:Male; D017265:Procaterol / Q000008:administration & dosage / Q000737:chemistry / Q000493:pharmacokinetics*; D011786:Quality Control; D012995:Solubility; D013607:Tablets; D013678:Technology, Pharmaceutical; D013810:Therapeutic Equivalency
D000318:Adrenergic beta-Agonists; D002214:Capsules; D013607:Tablets; D017265:Procaterol