【摘要】：目的考察萜類促滲劑的種類、濃度及聯(lián)用對鹽酸普萘洛爾(PPL·HCl)經(jīng)皮滲透的影響,為鹽酸普萘洛爾經(jīng)皮遞藥系統(tǒng)的處方篩選提供依據(jù)。方法采用改良Franz直立式擴散池,離體乳豬皮膚為滲透屏障,以體外經(jīng)皮累積滲透量(Q)和促滲倍數(shù)(ER)為指標(biāo),比較萜類促滲劑對鹽酸普萘洛爾經(jīng)皮滲透的影響。結(jié)果 10種萜類促滲劑對凝膠中鹽酸普萘洛爾體外經(jīng)皮滲透促進作用順序為:法尼醇L-薄荷腦橙花叔醇四氫香葉醇1,4-桉葉素≈香葉醇檸檬烯茴香腦冰片甘草酸二鉀,均符合零級滲透規(guī)律,其中法尼醇、L-薄荷腦、橙花叔醇濃度為3%時具有最高的Q,最大的ER;濃度增至5%,其促滲作用反而降低;與單用3%促滲劑相比,與異丙醇聯(lián)用具有協(xié)同促滲作用(P0.05),而與丙二醇聯(lián)用則顯示拮抗作用(P0.05)。結(jié)論新型萜類促滲劑(除甘草酸二鉀)均能不同程度促進鹽酸普萘洛爾經(jīng)皮滲透,促滲劑為3%法尼醇+10%異丙醇時,鹽酸普萘洛爾體外透皮可達最大吸收,該結(jié)果為鹽酸普萘洛爾經(jīng)皮給藥研究提供了基礎(chǔ)。
[Abstract]:Objective to investigate the effects of terpenoids on the transdermal permeation of propranolol hydrochloride (PPL HCl) in order to provide a basis for screening the prescription of propranolol hydrochloride. Methods the effects of terpenoids on the percutaneous permeation of propranolol hydrochloride were compared by using improved Franz vertical diffusion tank and in vitro porcine skin as the permeation barrier. The in vitro cumulative permeation capacity (Q) and multiple permeability enhancement (ER) were used to compare the effects of terpenoids on the transdermal permeability of propranolol hydrochloride. Results the effects of 10 terpenoids on the percolation of propranolol hydrochloride in the gel in vitro were as follows: Farnitol L- menthol tetrahydrogeraniol 1, 4-eucalyptin 鈮，

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