{"title":"姜黄素的溶解度和稳定性增强:改善天然色素的药物性能","authors":"MJ Ansari, R. Parveen","doi":"10.4103/2394-6555.191166","DOIUrl":null,"url":null,"abstract":"Aim: Water insolubility, low potency, and instability are inherent problems of several herbal medicines. Identity, strength, quality, and purity of herbal products are further compromised during manufacturing and storage. The aim of present work was to evaluate solubility and stability of curcumin, a pigment obtained from dried rhizomes of plant Cucrcuma longa. Materials and Methods: The stoichiometric ratios for inclusion complexation of curcumin with various cyclodextrins (CDs) were determined by phase solubility analysis. Grinding, kneading, and freeze-drying were employed to determine optimum complexation. Complexes were evaluated for drug inclusion, solubility, and stability. Results: Stability constants were 11200 M−1 , 1557 M−1 , 2858 M−1 , and 2206 M−1 for α-, β-, γ-CD, and dimethyl β-CD (DIMEB), respectively, thus indicating good complex formation. Theoretical amounts of curcumin in binary products were between 80% and 97% with a maximum of 96.8% in curcumin-β-CD freeze-dried product. The complexation resulted in a marked improvement in the solubility of curcumin up to 60, 55, 56, and 1500 folds by α-, β-, γ-CD, and DIMEB, respectively. Inclusion complexation protected the drug from hydrolytic degradations as only 20-40% degradation was observed at the end of 8 h as opposed to >70% for pure curcumin. Conclusion: A significant improvement in the solubility and stability was observed with curcumin-CD complex as compared to pure curcumin.","PeriodicalId":11347,"journal":{"name":"Drug Development and Therapeutics","volume":null,"pages":null},"PeriodicalIF":0.0000,"publicationDate":"2016-07-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":"6","resultStr":"{\"title\":\"Solubility and stability enhancement of curcumin: Improving drug properties of natural pigment\",\"authors\":\"MJ Ansari, R. Parveen\",\"doi\":\"10.4103/2394-6555.191166\",\"DOIUrl\":null,\"url\":null,\"abstract\":\"Aim: Water insolubility, low potency, and instability are inherent problems of several herbal medicines. Identity, strength, quality, and purity of herbal products are further compromised during manufacturing and storage. The aim of present work was to evaluate solubility and stability of curcumin, a pigment obtained from dried rhizomes of plant Cucrcuma longa. Materials and Methods: The stoichiometric ratios for inclusion complexation of curcumin with various cyclodextrins (CDs) were determined by phase solubility analysis. Grinding, kneading, and freeze-drying were employed to determine optimum complexation. Complexes were evaluated for drug inclusion, solubility, and stability. Results: Stability constants were 11200 M−1 , 1557 M−1 , 2858 M−1 , and 2206 M−1 for α-, β-, γ-CD, and dimethyl β-CD (DIMEB), respectively, thus indicating good complex formation. Theoretical amounts of curcumin in binary products were between 80% and 97% with a maximum of 96.8% in curcumin-β-CD freeze-dried product. The complexation resulted in a marked improvement in the solubility of curcumin up to 60, 55, 56, and 1500 folds by α-, β-, γ-CD, and DIMEB, respectively. Inclusion complexation protected the drug from hydrolytic degradations as only 20-40% degradation was observed at the end of 8 h as opposed to >70% for pure curcumin. Conclusion: A significant improvement in the solubility and stability was observed with curcumin-CD complex as compared to pure curcumin.\",\"PeriodicalId\":11347,\"journal\":{\"name\":\"Drug Development and Therapeutics\",\"volume\":null,\"pages\":null},\"PeriodicalIF\":0.0000,\"publicationDate\":\"2016-07-01\",\"publicationTypes\":\"Journal Article\",\"fieldsOfStudy\":null,\"isOpenAccess\":false,\"openAccessPdf\":\"\",\"citationCount\":\"6\",\"resultStr\":null,\"platform\":\"Semanticscholar\",\"paperid\":null,\"PeriodicalName\":\"Drug Development and Therapeutics\",\"FirstCategoryId\":\"1085\",\"ListUrlMain\":\"https://doi.org/10.4103/2394-6555.191166\",\"RegionNum\":0,\"RegionCategory\":null,\"ArticlePicture\":[],\"TitleCN\":null,\"AbstractTextCN\":null,\"PMCID\":null,\"EPubDate\":\"\",\"PubModel\":\"\",\"JCR\":\"\",\"JCRName\":\"\",\"Score\":null,\"Total\":0}","platform":"Semanticscholar","paperid":null,"PeriodicalName":"Drug Development and Therapeutics","FirstCategoryId":"1085","ListUrlMain":"https://doi.org/10.4103/2394-6555.191166","RegionNum":0,"RegionCategory":null,"ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":null,"EPubDate":"","PubModel":"","JCR":"","JCRName":"","Score":null,"Total":0}
引用次数: 6
摘要
目的:中药不溶于水、效力低、不稳定是中药的固有问题。草药产品的特性、强度、质量和纯度在生产和储存过程中进一步受到损害。本文研究了姜黄素的溶解度和稳定性。姜黄素是一种从蓖麻干根茎中提取的色素。材料与方法:采用相溶解度法测定了姜黄素与不同环糊精包合的化学计量比。研磨、揉捏和冷冻干燥是确定最佳配位的方法。评估配合物的药物包裹性、溶解度和稳定性。结果:α-、β-、γ-CD和二甲基β- cd (DIMEB)的稳定常数分别为11200 M−1、1557 M−1、2858 M−1和2206 M−1,表明配合物形成良好。姜黄素-β-CD冻干产品中姜黄素理论含量在80% ~ 97%之间,最高可达96.8%。通过α-、β-、γ-CD和DIMEB络合,姜黄素的溶解度分别提高了60倍、55倍、56倍和1500倍。包合物保护药物免于水解降解,因为在8小时结束时仅观察到20-40%的降解,而纯姜黄素的降解率>70%。结论:与纯姜黄素相比,姜黄素- cd复合物在溶解度和稳定性方面有显著改善。
Solubility and stability enhancement of curcumin: Improving drug properties of natural pigment
Aim: Water insolubility, low potency, and instability are inherent problems of several herbal medicines. Identity, strength, quality, and purity of herbal products are further compromised during manufacturing and storage. The aim of present work was to evaluate solubility and stability of curcumin, a pigment obtained from dried rhizomes of plant Cucrcuma longa. Materials and Methods: The stoichiometric ratios for inclusion complexation of curcumin with various cyclodextrins (CDs) were determined by phase solubility analysis. Grinding, kneading, and freeze-drying were employed to determine optimum complexation. Complexes were evaluated for drug inclusion, solubility, and stability. Results: Stability constants were 11200 M−1 , 1557 M−1 , 2858 M−1 , and 2206 M−1 for α-, β-, γ-CD, and dimethyl β-CD (DIMEB), respectively, thus indicating good complex formation. Theoretical amounts of curcumin in binary products were between 80% and 97% with a maximum of 96.8% in curcumin-β-CD freeze-dried product. The complexation resulted in a marked improvement in the solubility of curcumin up to 60, 55, 56, and 1500 folds by α-, β-, γ-CD, and DIMEB, respectively. Inclusion complexation protected the drug from hydrolytic degradations as only 20-40% degradation was observed at the end of 8 h as opposed to >70% for pure curcumin. Conclusion: A significant improvement in the solubility and stability was observed with curcumin-CD complex as compared to pure curcumin.