復(fù)方莪術(shù)油脂質(zhì)體的制備及質(zhì)量評(píng)價(jià)

陳積 趙小倩 胡姍姍 馬彥巧 劉燕 譚丹楓 陳澤慧 田應(yīng)彪

中圖分類號(hào) R283 文獻(xiàn)標(biāo)志碼 A 文章編號(hào) 1001-0408（2018）05-0615-06

DOI 10.6039/j.issn.1001-0408.2018.05.10

摘 要 目的：制備復(fù)方莪術(shù)油脂質(zhì)體（ZTOC-LPS）并對(duì)其質(zhì)量進(jìn)行評(píng)價(jià)。方法：以復(fù)方莪術(shù)油中莪術(shù)油（以吉馬酮表征）和維A酸的包封率及載藥量等為考察指標(biāo)，篩選ZTOC-LPS的制備方法及處方中大豆卵磷脂（SPC）的加入量、脂質(zhì)中SPC-膽固醇（CH）質(zhì)量比、莪術(shù)油-脂質(zhì)質(zhì)量比、維A酸-脂質(zhì)質(zhì)量比、水浴溫度；并對(duì)最優(yōu)處方制備工藝所制脂質(zhì)體進(jìn)行質(zhì)量評(píng)價(jià)和初步穩(wěn)定性考察。結(jié)果：優(yōu)選的制備方法為乙醇注入法；最優(yōu)處方制備工藝為每1 mL脂質(zhì)體中SPC 4 mg、SPC-CH質(zhì)量比3 ∶ 1、莪術(shù)油-脂質(zhì)質(zhì)量比1 ∶ 9、維A酸-脂質(zhì)質(zhì)量比1 ∶ 70、水浴溫度55 ℃。所制3批脂質(zhì)體中莪術(shù)油和維A酸的平均包封率分別為（64.63±1.00）%和（90.33±0.72）%，載藥量分別為（9.09±0.14）%和（1.43±0.02）%，粒徑為（257.41±7.58） nm，Zeta電位為（-38.77±0.81） mV，多分散系數(shù)為 0.10±0.04；離心加速試驗(yàn)結(jié)果顯示脂質(zhì)體具有良好的物理穩(wěn)定性；脂質(zhì)體樣品在（4±2） ℃條件下放置 1 個(gè)月時(shí)各項(xiàng)考察指標(biāo)均未發(fā)生明顯變化。結(jié)論：建立的制備方法簡(jiǎn)單可行，所制脂質(zhì)體質(zhì)量符合要求，可為后續(xù)復(fù)方莪術(shù)油新劑型的研究提供參考。

關(guān)鍵詞 莪術(shù)油；維A酸；脂質(zhì)體；包封率；載藥量；制備工藝；質(zhì)量評(píng)價(jià)

ABSTRACT OBJECTIVE： To prepare zedoary turmeric oil compound liposomes （ZTOC-LPS） and evaluate its quality. METHODS： The preparation method of liposome， the addition amount of soybean phosphatidylcholine （SPC）， ratio of SPC to cholesterol （CH） in lipid， drug-lipid ratio of zedoary turmeric oil （ZTO）， drug-lipid ratio of tretinoin in formulation， and water bath temperature were screened using encapsulation efficiency and drug-loading amount of ZTO （represented by germacrone） and tretinoin as investigation indexes. Quality evaluation and primary stability investigation were conducted for liposomes prepared by optimal preparation technology. RESULTS： The optimal preparation method was ethanol injection method； The optimal preparation technology were SPC 4 mg in 1 mL lipid， the mass ratio of SPC to CH 3 ∶ 1， the ratio of ZTO to lipid 1 ∶ 9 ， the ratio of tretinoin to lipid 1 ∶ 70， water bath temperature of 55 ℃. Encapsulation efficiencies of ZTO and tretinoin were （64.63±1.00）% and （90.33±0.72）% in 3 batches of ZTOC-LPS， respectively. Drug-loading amount of ZTO and tretinoin were （9.09±0.14）% and （1.43±0.02）%， respectively. Particle size was （257.41±7.58） nm， Zeta potential was （-38.77±0.81） mV， PDI was 0.10±0.04； the results of centrifugal acceleration test showed that the liposomes had good physical stability. No obvious change was found in each investigation index of ZTOC-LPS that stored at （4±2） ℃ for 1 month. CONCLUSIONS： Established preparation technology is simple and feasible， the quality of the prepared ZTOC-LPS conforms to the requirements， and it can provide reference for the following research of ZTOC-LPS.

KEYWORDS Zedoary turmeric oil； Tretinoin； Liposomes； Encapsulation efficiency； Drug-loading amount； Preparation technology； Quality evaluation

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