發(fā)布時(shí)間：2018-05-29 05:50

  本文選題：羥丙甲纖維素 + 親水凝膠��； 參考：《中國新藥雜志》2017年09期

【摘要】：目的:通過研究羥丙甲纖維素(HPMC)凝膠對(duì)不同藥物的阻滯作用,考察HPMC緩釋性征參數(shù)的適用性,從相互作用的角度闡明親水凝膠的緩釋機(jī)理。方法:選擇不同性質(zhì)的5種模型藥物(托拉塞米、鹽酸洛美利嗪、布洛芬、鹽酸氨溴索、鹽酸二甲雙胍),用三室滲透模型測定藥物透過親水凝膠的速度,取點(diǎn)時(shí)間為1,3,7,10和24 h,計(jì)算藥物的滲透率及阻滯率,利用Material Studio的blend模塊計(jì)算藥物與HPMC的相互作用能,考察試驗(yàn)結(jié)果與計(jì)算結(jié)果的相關(guān)性。結(jié)果:HPMC的存在對(duì)不同的藥物影響不同,以3個(gè)濃度(5,10,20 mg·mL~(-1))的阻滯率作為表征HPMC對(duì)藥物的緩釋特征參數(shù)可以發(fā)現(xiàn):HPMC對(duì)二甲雙胍和氨溴索的阻滯能力較弱,對(duì)布洛芬和托拉塞米具有較強(qiáng)的吸附作用,對(duì)洛美利嗪也有較大的吸收作用,存在飽和現(xiàn)象。理論計(jì)算的HPMC與藥物相互作用能與24 h阻滯率之間存在明顯的相關(guān)性。結(jié)論:緩釋特征參數(shù)可以通過高濃度和低濃度的阻滯率,明確藥物和輔料的相互作用的方式,幫助藥物選擇適當(dāng)?shù)木忈尣牧?還可以用于保證輔料的本身質(zhì)量的一致性。
[Abstract]:Aim: to study the inhibition effect of HPMC gel on different drugs, to investigate the applicability of HPMC sustained-release characteristic parameters, and to elucidate the slow-release mechanism of hydrophilic gel from the point of view of interaction. Methods: five different kinds of model drugs (Tora, lomerizine hydrochloride, ibuprofen, ambroxol hydrochloride, metformin hydrochloride) were selected. The permeation rate of the drug through hydrophilic gel was determined by a three-compartment osmotic model. The drug permeability and blocking rate were calculated for 10 and 24 hours, and the interaction energy between the drug and HPMC was calculated by blend module of Material Studio. The correlation between the experimental results and the calculated results was investigated. Results the effects of the presence of 1: HPMC on different drugs were different. The blocking rate of 3 concentrations of 5 10 ~ 10 ~ (10) mg / L ~ (-1) of HPMC was used as the characteristic parameter to characterize the sustained release of HPMC to the drug. It was found that the inhibition ability of the two groups to metformin and ambroxol was weak. Ibuprofen and Tora were adsorbed strongly, and lomerizine was also adsorbed and saturated. There was a significant correlation between the calculated HPMC and drug interaction energy and 24 h block rate. Conclusion: the characteristic parameters of slow release can be used to ensure the consistency of the quality of excipients by determining the way of interaction between drugs and excipients at high and low concentration.
【作者單位】： 天津醫(yī)科大學(xué);天津中醫(yī)藥大學(xué);天津藥物研究院釋藥技術(shù)與藥動(dòng)學(xué)國家重點(diǎn)實(shí)驗(yàn)室;天津藥物研究院天津市藥物設(shè)計(jì)與發(fā)現(xiàn)重點(diǎn)實(shí)驗(yàn)室;
【分類號(hào)】：R943

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