Development of novel fast-dissolving tacrolimus solid dispersion-loaded prolonged release tablet

Title
Development of novel fast-dissolving tacrolimus solid dispersion-loaded prolonged release tablet
Author(s)
용철순조정현김용일김동욱[김동욱]Abid M. Yousaf[Abid M. Yousaf]김종오우종수[우종수]최한곤[최한곤]
Keywords
SPRAY-DRYING TECHNIQUE; DRUG-DELIVERY; BEAGLE DOGS; PHYSICOCHEMICAL CHARACTERIZATION; ORAL BIOAVAILABILITY; FORMULATION; PHARMACOKINETICS; SOLUBILITY; DISSOLUTION; CLASSIFICATION
Issue Date
201404
Publisher
ELSEVIER SCIENCE BV
Citation
EUROPEAN JOURNAL OF PHARMACEUTICAL SCIENCES, v.54, pp.1 - 7
Abstract
The goal of this research was to develop a novel prolonged release tablet bioequivalent to the commercial sustained release capsule. A number of tacrolimus-loaded fast-dissolving solid dispersions containing various amounts of DOSS were prepared using the spray drying technique. Their solubility, dissolution and pharmacokinetics in rats were studied. DOSS increased drug solubility and dissolution in the solid dispersions. Compared with the drug powder, the solubility, dissolution and bioavailability of tacrolimus with the fast-dissolving solid dispersion containing tacrolimus/HP-beta-CD/DOSS in the weight ratio of 5:40:4 were boosted by approximately 700-, 30- and 2-fold, respectively. Several tablet formulations were accomplished with this solid dispersion in combination with various ratios of HPMC/ethylcellulose. The release behaviour and pharmacokinetic studies in beagle dogs were assessed compared with the commercial prolonged release capsule. A decrease in HPMC/ethylcellulose ratios reduced the dissolution of tacrolimus from the tablets. Particularly, the tacrolimus-loaded prolonged release tablet consisting of fast-dissolving tacrolimus solid dispersion, HPMC, ethylcellulose and talc at the weight ratio of 20:66:112:2 exhibited a dissolution profile similar to that produced by the commercial prolonged release capsule. Furthermore, there were no significant differences in the AUC, C-max, T-max and MRT values between them in beagle dogs. Consequently, this tacrolimus-loaded prolonged release tablet might be bioequivalent to the tacrolimus-loaded commercial capsule. (C) 2013 Elsevier B.V. All rights reserved.
URI
http://hdl.handle.net/YU.REPOSITORY/32515http://dx.doi.org/10.1016/j.ejps.2013.12.016
ISSN
0928-0987
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약학대학 > 약학부 > Articles
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