title: Physical and dissolution characterization of cilostazol solid dispersions prepared by hot melt granulation (HMG) and thermal adhesion granulation (TAG) methods.
abstract: A growing number of poorly water-soluble drug have been discovered, but the poor bioavailability is a critical problem. In this study, physical properties and dissolution profiles of cilostazol solid dispersions prepared by hydrophilic/lipophilic excipients (Kollidon(®) VA64, tocopheryl polyethylene glycol succinate (TPGS), vitamine E) with hot-melt and thermal adhesion granulation (TAG) method to adsorb Fujicalin(®) and Microcel(®) were characterized. Results demonstrate the angle of repose in formulations with Fujicalin(®) was improved than those with Microcel(®), but the difference disappeared when more TPGS or vitamin E was added. Compared the formulation made by hot-melt and TAG method, both improved flowability. The hardness decreased with the increased amount of TPGS and vitamin E. The formulations with Microcel(®) had lower hardness than those with Fujicalin(®), because Microcel(®) has weaker adsorption ability and cannot afford much TPGS and vitamin E, leading to lower hardness. Furthermore, the solubility was almost three-fold higher than that of Pletaal(®) (7.68 ± 0.20 μg/mL) in compositions containing TPGS and vitamin E made by hot-melt or TAG method, in which a controlled drug release pattern was demonstrated. There is no significant difference on dissolution profile between hot-melt and TAG method. However, the procedure of TAG is easier, indicating its potential pharmaceutical use.
authors.affiliation: School of Pharmacy, College of Pharmacy, Taipei Medical University, Taipei, Taiwan, ROC.
authors.forename: Ying-Chen
authors.initials: YC
authors.lastname: Chen
authors.affiliation: School of Pharmacy, College of Pharmacy, Taipei Medical University, Taipei, Taiwan, ROC.
authors.forename: Hsiu-O
authors.initials: HO
authors.lastname: Ho
authors.affiliation: School of Pharmacy, College of Pharmacy, Taipei Medical University, Taipei, Taiwan, ROC.
authors.forename: Jiun-Da
authors.initials: JD
authors.lastname: Chiou
authors.affiliation: School of Pharmacy, College of Pharmacy, Taipei Medical University, Taipei, Taiwan, ROC; Clinical Research Center and Traditional Herbal Medicine Research Center, Taipei Medical University Hospital, Taipei, Taiwan, ROC. Electronic address: mingsheu@tmu.edu.tw.
authors.forename: Ming-Thau
authors.initials: MT
authors.lastname: Sheu
mesh_terms: D001546:Bentonite / Q000737:chemistry; D002130:Calcium Phosphates / Q000737:chemistry; D002152:Calorimetry, Differential Scanning; D002364:Caseins / Q000737:chemistry; D002482:Cellulose / Q000737:chemistry; D000077407:Cilostazol; D004339:Drug Compounding / Q000379:methods; D006244:Hardness; D006358:Hot Temperature; D011092:Polyethylene Glycols / Q000737:chemistry; D011759:Pyrrolidines / Q000737:chemistry; D012995:Solubility; D013607:Tablets; D013777:Tetrazoles / Q000737:chemistry*; D014753:Vinyl Compounds / Q000737:chemistry; D014810:Vitamin E / Q000031:analogs & derivatives / Q000737:chemistry
chemical_list: D002130:Calcium Phosphates; D002364:Caseins; D011759:Pyrrolidines; D013607:Tablets; D013777:Tetrazoles; D014753:Vinyl Compounds; C452280:fujicalin; C402301:poly(vinylpyrrolidone-co-vinyl-acetate); D001546:Bentonite; D014810:Vitamin E; D011092:Polyethylene Glycols; D002482:Cellulose; D000077407:Cilostazol; C014225:tocophersolan
keywords: Cilostazol; Solid dispersion; Thermal adhesion granulation; Tocopheryl polyethylene glycol succinate (TPGS)