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신규 Capsaicin 유도체 DA - 5018 을 함유한 외용진통제의 제제설계 Ⅰ: 평가법 확립 및 외용크림제의 설계
Formulation of Topical Analgesic Preparation for a New Capsaicin Derivative Analgesic , DA - 5018 (Ⅰ) : Establishment of Skin Penetration Evaluation System and Formulation of Topical Cream
차봉진 , 이응두 , 김원배 , 이민화 ( Bong Jin Cha , Eung Doo Lee , Won Bae Kim , Min Hwa Lee )
UCI I410-ECN-0102-2008-510-000813819

To formulate the topical analgesic preparation of a new capsaicin derivative. DA-5018, a skin penetration evaluation system was established and the effect of composition of formulation on skin penetration using this system was evaluated. The effect of massage on hairless mouse skin penetration and inter-day variation of this effect were investigated using test formulations (cream). In massage group, compared with non-massage group, absolute penetration amount of DA-5018 increased and this experimental system was found to be reproducible. The effects of pH of water phase, ratio of oil/water and the concentration of active ingredient in cream on skin penetration were investigated. The permeation of DA-5018 from the cream increased with increasing pH of water phase to 9. But at pH 10, the permeation of DA-5018 decreased, because of the physical instability of the cream. The permeation of DA-5018 from the cream increased with increasing the ratio of oil/water of the cream. The increase of the content of DA-5018 to 0.3% increased the permeation of DA-5018. but at high concentration(1.0%), the permeation of DA-5018 decreased, due to the instability of the cream.

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