非諾貝特-淀粉源介孔碳載體固體分散體雙層滲透泵控釋片的研究
發(fā)布時(shí)間:2018-06-13 00:33
本文選題:淀粉源介孔碳載體 + 難溶性藥物。 參考:《中國(guó)藥學(xué)雜志》2017年16期
【摘要】:目的用淀粉源介孔碳(SMC)作為載體來(lái)提高非諾貝特(FNB)的溶出速率,并結(jié)合雙層滲透泵技術(shù)使藥物得到控釋釋放,從而提高口服生物利用度。方法通過(guò)吸附法將藥物FNB載入SMC的介孔孔道中制備載藥體系(FNB-SMC)。通過(guò)差示掃描量熱法(DSC)和粉末X射線衍射法(PXDR)對(duì)載藥前后藥物的存在狀態(tài)進(jìn)行表征。體外溶出實(shí)驗(yàn)考察FNB-SMC的溶出速率,并對(duì)雙層滲透泵片進(jìn)行優(yōu)化。通過(guò)體內(nèi)實(shí)驗(yàn)考察自制片的口服生物利用度。結(jié)果表征結(jié)果表明,FNB以無(wú)定型狀態(tài)存在在SMC的介孔孔道中。體外溶出實(shí)驗(yàn)表明,SMC能顯著提高FNB的溶出速率,并且雙層滲透泵技術(shù)使藥物達(dá)零級(jí)釋放。體內(nèi)實(shí)驗(yàn)表明,自制片的口服生物利用度得到明顯改善。結(jié)論淀粉源介孔碳載體和雙層滲透泵技術(shù)的聯(lián)合防止了突釋效應(yīng),明顯改善FNB的口服吸收。
[Abstract]:Objective to improve the dissolution rate of fenofibrate (FNB) by using starch source Kong Tan (SMC) as a carrier, and combine the double osmotic pump technology to release the drug by controlled release, thus improving the oral bioavailability. The drug FNB was loaded into the mesoporous channel of SMC by adsorption method (FNB-SMC). Differential scanning calorimetry (DSC) was used. X ray diffraction (PXDR) was used to characterize the existing state of the drug before and after the drug loading. The dissolution rate of FNB-SMC was investigated in vitro and the double layer osmotic pump was optimized. The oral bioavailability of the homemade tablets was investigated by the experiment in vivo. The results showed that the FNB was in the mesoporous channel of SMC in the amorphous state. The dissolution test in vitro showed that SMC could significantly improve the dissolution rate of FNB, and the double layer osmotic pump technology made the drug release to zero. In vivo experiments showed that the oral bioavailability of the homemade tablets was obviously improved. Conclusion the combination of the starch source Kong Tan carrier and the double layer osmotic pump prevented the sudden release effect and obviously improved the oral absorption of FNB. Accept.
【作者單位】: 錦州醫(yī)科大學(xué);
【基金】:校長(zhǎng)基金-奧鴻博澤基金-醫(yī)藥創(chuàng)新專(zhuān)項(xiàng)資助(XZJJ20130104-07)
【分類(lèi)號(hào)】:R943
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本文編號(hào):2011790
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