Novel Method to Control Release of Lipophilic Drugs with High Potency from Silicone.
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Accession number;03A0040949
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| Title;Novel Method to Control Release of Lipophilic Drugs with High Potency from Silicone. |
| Author;
KAJIHARA M
(Sumitomo Pharmaceuticals Co., Ltd., Osaka, Jpn)
SUGIE T
(Sumitomo Pharmaceuticals Co., Ltd., Osaka, Jpn)
SANO A
(Sumitomo Pharmaceuticals Co., Ltd., Osaka, Jpn)
FUJIOKA K
(Sumitomo Pharmaceuticals Co., Ltd., Osaka, Jpn)
URABE Y
(Dow Corning Asia Ltd., Tokyo, Jpn)
TANIHARA M
(Nara Inst. Sci. And Technol., Nara, Jpn)
IMANISHI Y
(Nara Inst. Sci. And Technol., Nara, Jpn)
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Journal Title;Chem Pharm Bull
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Journal Code:G0504A
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ISSN:0009-2363
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VOL.51;NO.1;PAGE.11-14(2003)
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| Figure&Table&Reference;FIG.4, REF.9 |
| Pub. Country;Japan |
| Language;English |
| 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. 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 D3 (VD3) 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 VD3, (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. (author abst.) |
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