基于磺丁基-β-环糊精包合技术的姜黄素舌下片的制备及质量评价
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摘要
目的以磺丁基-β-环糊精(sulfobutyl ether-β-cyclodextrin, SBE-β-CD)为原料制备姜黄素(Curcumin, CUR)包合物,并考察包合物对CUR水溶性的提高作用。方法采用饱和水溶液法制备CUR-SBE-β-CD包合物,设计正交试验优化制备工艺,以直接压片技术制备舌下片,并对其进行质量考察。结果正交试验表明,最佳制备工艺为投料比(CUR∶SBE-β-CD) 1∶1,包合温度45℃,包合时间1.5 h,乙醇浓度60%。CUR溶解度达到15.892μg/ml,所制舌下片半小时内可溶出完全。结论采用SBE-β-CD包合后可显著提高CUR水溶性。
Objective To prepare the Curcumin(CUR) inclusion complex by using Sulfobutyl-β-cyclodextrin(SBE-β-CD) as raw material, and explore the optimal conditions for the preparation. Further evaluate the effect of inclusion complex on the water solubility of CUR. Methods The saturated aqueous solution method is carried out to prepare CUR-SBE-β-CD inclusion complex. The technology is optimized by orthogonal design method. The CUR-SBE-β-CD clathrate sublingual tablets are prepared by direct compression method, the quality evaluation then is carried out. Results The optimal technology are as follows: the ratio of CUR to SBE-β-CD is 1 : 1, the concentration of ethanol is 60 %, inclusion temperature is 45 °C and inclusion time is 1.5 h. The solubility reaches 15.892 μg/ml which is improved significantly. The sublingual tablet can be completely dissolved within 30 min. Conclusion The water solubility of the CUR can be significantly improved by the use of SBE-β-CD inclusion.
Objective To prepare the Curcumin(CUR) inclusion complex by using Sulfobutyl-β-cyclodextrin(SBE-β-CD) as raw material, and explore the optimal conditions for the preparation. Further evaluate the effect of inclusion complex on the water solubility of CUR. Methods The saturated aqueous solution method is carried out to prepare CUR-SBE-β-CD inclusion complex. The technology is optimized by orthogonal design method. The CUR-SBE-β-CD clathrate sublingual tablets are prepared by direct compression method, the quality evaluation then is carried out. Results The optimal technology are as follows: the ratio of CUR to SBE-β-CD is 1 : 1, the concentration of ethanol is 60 %, inclusion temperature is 45 °C and inclusion time is 1.5 h. The solubility reaches 15.892 μg/ml which is improved significantly. The sublingual tablet can be completely dissolved within 30 min. Conclusion The water solubility of the CUR can be significantly improved by the use of SBE-β-CD inclusion.
引文
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[2]Sanidad K Z,Zhu J,Wang W,et al.Effects of Stable Degradation Products of Curcumin on Cancer Cell Proliferation and Inflammation[J].J Agr Food Chem,2016,64(48):9189-9195.
[3]Santos A C,Costa G,Veiga F,et al.Advance in methods studying the pharmacokinetics of polyphenols[J].Curr Drug Metab,2014,15(1):96-115.
[4]Stohs S J,Ji J,Bucci L R,et al.A Comparative Pharmacokinetic Assessment of a Novel Highly Bioavailable Curcumin Formulation with 95%Curcumin:A Randomized,Double-Blind,Crossover Study[J].J Am Cull Nutr,2017,37(1):1-9.
[5]Sharma R A,Steward W P,Gescher A J,et al.Pharmacokinetics and pharmacodynamics of curcumin[J].Adv Exp Med Biol,2007,595(6):453.
[6]梁硕,李超英.舌下给药研究进展[J].长春中医药大学学报,2016,6(32):1309-1311.
[7]谢捷,杜君琛,朱兴一,等.磺丁基醚-β-环糊精对葛根素的增溶作用及其包合物的研制[J].中成药,2012,34(3):454-458.
[8]张芹,钱芳.清肠化湿颗粒中肉桂挥发油的提取及β-环糊精包合工艺研究[J].现代中药研究与实践,2016,152(5):43-45.
[9]章雪辉,钟玲,姜小丽.环维黄杨D舌下片的制备工艺研究[J].科学技术创新,2014(27):94-95.
[10]Rawasqalaji M M,Simons F E,Simons K J.Fast-disintegrating sublingual tablets:effect of epinephrine load on tablet characteristics[J].AAPS Pharm Sci Tech,2006,7(2):72-78.
[11]何瑶阮,李卓恒,王丽娟,等.卡前列甲酯-羟丙基-β-环糊精包合物舌下片的制备及质量评价[J].中国药房,2017,28(34):4860-4863.
[12]章建芳.九里香叶总黄酮-羟丙基-β-环糊精包合物的研究[D].杭州:浙江大学,2010.
[13]苏柘僮,杨明,吴品江,等.胆酸-羟丙基-β-环糊精包合物的物相鉴别及体外鼻黏膜渗透评价[J].中草药,2009,40(6):878-882.