發(fā)布時(shí)間：2019-04-19 22:58

【摘要】：目的:考察萜烯類手性促進(jìn)劑芳樟醇和薄荷醇對氟比洛芬(flurbiprofen,FP)經(jīng)皮滲透的對映體選擇性作用。方法:采用Valia-Chien雙室滲透擴(kuò)散池,以大鼠離體皮膚為滲透屏障,以穩(wěn)態(tài)經(jīng)皮滲透速率為評價(jià)指標(biāo),用對映體選擇性高效液相色譜法對FP對映體進(jìn)行濃度測定,考察手性促進(jìn)劑芳樟醇或薄荷醇對FP對映體選擇性的影響。結(jié)果:無論供給液是否含單個(gè)對映體或消旋體,若供給液中不含促透劑,FP經(jīng)大鼠離體皮膚滲透未見對映體選擇性。當(dāng)供給液中含有dl-薄荷醇時(shí),RSFP的穩(wěn)態(tài)滲透速率分別為R-FP、S-FP的1.34,1.27倍,差異有顯著性(P0.05);而供給液中含有l(wèi)-薄荷醇時(shí),FP對映體及消旋體間的皮膚滲透速率無顯著差異(P0.05)。l-薄荷醇和dl-薄荷醇對同一藥物構(gòu)型R-FP或S-FP的促透效果相當(dāng);然而,dl-薄荷醇對RS-FP的促透作用是l-薄荷醇的1.44倍。l-芳樟醇或dl-芳樟醇作為手性促透劑時(shí),未發(fā)現(xiàn)對映體選擇性滲透現(xiàn)象。結(jié)論:dl-薄荷醇對FP的促透作用出現(xiàn)了對映體選擇性,而l-薄荷醇、l-芳樟醇和dl-芳樟醇未引起FP的對映體選擇性滲透,且所有滲透實(shí)驗(yàn)均未發(fā)現(xiàn)對映體轉(zhuǎn)化。
[Abstract]:Aim: to investigate the enantioselectivity of linalool and menthol as chiral promoters of terpene on the percutaneous permeation of flurbiprofen (flurbiprofen,FP). Methods: the concentration of Valia-Chien enantiomers was determined by enantiomeric selective high performance liquid chromatography (HPLC) using Valia-Chien two-compartment osmotic diffusion cell, isolated rat skin as osmotic barrier, steady-state percutaneous permeation rate as the evaluation index, and enantiomeric selective high performance liquid chromatography (HPLC). The effects of chiral promoters linalool or menthol on the enantioselectivity of FP were investigated. Results: no matter whether there was a single enantiomer or racemate in the donor solution, no enantioselective enantioselectivity was found in the FP permeation through the rat skin in vitro if there was no transdermal enhancer in the donor solution. When dl- menthol was contained in the feed solution, the steady-state permeation rate of RSFP was 1.34,1.27 times higher than that of RFP, respectively (P0.05). There was no significant difference in skin penetration rate between FP enantiomers and racemates (P0.05). L-menthol and dl- menthol had the same effect on the penetration of R-FP or S-FP of the same drug configuration. However, the transmissibility of dl- menthol on RS-FP was 1.44 times higher than that of l-menthol. When l-linalool or dl- linalool was used as chiral enhancer, enantiomeric selective permeation was not found. Conclusion: the enantioselective enantioselectivity of dl- menthol on FP was observed, while lmenthol, llinalool and dl- linalool did not induce enantioselective permeation of FP, and no enantiomeric transformation was found in all permeation experiments.
【作者單位】： 浙江省醫(yī)學(xué)科學(xué)院藥物研究所;
【基金】：浙江省科技計(jì)劃項(xiàng)目(編號:2014F10034)
【分類號】：R943

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