title: Novel method to control release of lipophilic drugs with high potency from silicone.
abstract: Silicone has been utilized as a carrier material for sustained release system of lipophilic drugs. Extensive studies revealed that drug release rate is influenced by factors such as physicochemical properties of the drug and additives.(1-5)) When a lipophilic drug is highly potent at low concentrations, the drug release rate should be strictly controlled so as to avoid side effects. In this study, using vitamin D(3) (VD(3)) as an example of such drugs, we investigated novel method to suppress initial burst and to modify drug release rate from silicone matrix. As a result, it was found that (a). addition of human serum albumin (HSA) suppressed initial burst and enhanced release rate in the later stage, resulting constant release of VD(3), (b). covering a matrix formulation with a membrane of low diffusivity (core-rod formulation) suppressed initial burst and released drug in a constant rate, and (3) using materials for which the drug has high affinity as dissolution solvent (reservoir formulation), the drug release rate was reduced.
authors.affiliation: Research Division, Sumitomo Pharmaceuticals Co, Ltd, Osaka, Japan. kajihara@sumitomopharm.co.jp
authors.forename: Masako
authors.initials: M
authors.lastname: Kajihara
authors.forename: Toshihiko
authors.initials: T
authors.lastname: Sugie
authors.forename: Akihiko
authors.initials: A
authors.lastname: Sano
authors.forename: Keiji
authors.initials: K
authors.lastname: Fujioka
authors.forename: Yosuke
authors.initials: Y
authors.lastname: Urabe
authors.forename: Masao
authors.initials: M
authors.lastname: Tanihara
authors.forename: Yukio
authors.initials: Y
authors.lastname: Imanishi
mesh_terms: D001391:Azo Compounds / Q000737:chemistry / Q000493:pharmacokinetics; D002626:Chemistry, Pharmaceutical; D002762:Cholecalciferol / Q000737:chemistry / Q000493:pharmacokinetics; D004337:Drug Carriers / Q000737:chemistry / Q000493:pharmacokinetics; D008055:Lipids / Q000737:chemistry / Q000493:pharmacokinetics*; D012828:Silicones / Q000737:chemistry / Q000493:pharmacokinetics*; D013678:Technology, Pharmaceutical / Q000379:methods*
chemical_list: D001391:Azo Compounds; D004337:Drug Carriers; D008055:Lipids; D012828:Silicones; D002762:Cholecalciferol; C033003:sudan red