Article(id=1236331739832972236, tenantId=1146029695717560320, journalId=1235980733773295621, issueId=1236331736221676464, articleNumber=null, orderNo=null, doi=null, pmid=null, cstr=null, oa=null, hot=null, price=null, onlineType=0, articleFormat=0, articleType=null, articleTypeStr=null, receivedDate=null, receivedDateStr=null, revisedDate=null, revisedDateStr=null, acceptedDate=1682352000000, acceptedDateStr=2023-04-25, onlineDate=1772694056708, onlineDateStr=2026-03-05, pubDate=1699977600000, pubDateStr=2023-11-15, doiRegisterDate=null, doiRegisterDateStr=null, onlineIssueDate=1772694056708, onlineIssueDateStr=2026-03-05, onlineJustAcceptDate=null, onlineJustAcceptDateStr=null, onlineFirstDate=null, onlineFirstDateStr=null, sourceXml=null, magXml=null, createTime=1772694056708, creator=13701087609, updateTime=1772694056708, updator=13701087609, issue=Issue{id=1236331736221676464, tenantId=1146029695717560320, journalId=1235980733773295621, year='2023', volume='32', issue='21', pageStart='2121', pageEnd='2224', issueExtLink='null', onlineDate='null', pubDate='null', beforeIssueId=null, nextIssueId=null, price=null, status=1, issueComplete=1, articleOrder=1, issueType=-1, specialIssue=null, createTime=1772694055848, creator=13701087609, updateTime=1772696903836, updator=13701087609, preIssue=null, nextIssue=null, ext={EN=IssueExt(id=1236343681607856366, tenantId=1146029695717560320, journalId=1235980733773295621, issueId=1236331736221676464, language=EN, specialIssueTitle=, coverIllustrator=null, specialIssueEditor=, specialIssueAbout=), CN=IssueExt(id=1236343681607856367, tenantId=1146029695717560320, journalId=1235980733773295621, issueId=1236331736221676464, language=CN, specialIssueTitle=, coverIllustrator=null, specialIssueEditor=, specialIssueAbout=)}, issueFiles=null}, startPage=2198, endPage=2209, ext={EN=ArticleExt(id=1236331740046881742, articleId=1236331739832972236, tenantId=1146029695717560320, journalId=1235980733773295621, language=EN, title=Preparation and characterization of curcumin nanocrystalline suspension and evaluation of its pharmaceutical properties
in vitro and
in vivo, columnId=null, journalTitle=Chinese Journal of New Drugs, columnName=null, runingTitle=null, highlight=null, articleAbstract=
Objective: In order to improve the oral bioavailability of curcumin, curcumin nanocrystalline suspension (Cur-NCS) was prepared by the high-pressure homogenization method in "top-down" method. Its physical properties, in vitro release, in vivo bioavailability and anti-inflammatory activity were studied.
Methods: The prescription and process parameters were optimized using particle size and zeta potential as evaluation indexes; the sample morphology was characterized by transmission electron microscopy, the in vitro release of curcumin nanocrystallines suspension was determined by HPLC, and the blood concentration of curcumin in rats was measured by LC-MS/MS; the anti-inflammatory activity was investigated in RAW264.7 inflammatory cell model, and curcumin was investigated in a mouse model of bronchial asthma airway inflammation nanosuspension on the therapeutic effect of curcumin on airway inflammation in mice.
Results: Preparation process: curcumin was sheared at high speed for 2 min at 16 000 r·min-1 and cycled 40 times at 800 bar. Prescription: curcumin dosage was 0.2%, TPGS dosage was 0.20% and soy lecithin dosage was 0.16%; the cumulative drug release of API and Cur-NCS was 11.67% and 27.44%, respectively. After gavage in rats, Cur-NCS bioavailability was increased by 1.86-fold after gavage in rats. In an in vitro inflammatory cell model and in vivo bronchial asthma mouse model, Cur-NCS significantly inhibited the expression of inflammatory factors NO, IL-6, TNF-α and the levels of MDA, IgE and ICAM-1, and increased the expression of IL-10 and the level of SOD.
Conclusion: The identified preparation process and prescription can meet the preparation requirements of curcumin nanosuspension, and the in vitro release, in vivo bioavailability and anti-inflammatory activity are significantly better than those of API, and curcumin nanosuspension can provide ideas for subsequent dosage form studies.
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目的: 为提高姜黄素的口服生物利用度,采用“Top-down”法中的高压均质法制备姜黄素纳米晶混悬液(Cur-NCS),并对其进行物性表征、体外释放、体内生物利用度及内外抗炎活性研究。
方法: 以粒径、Zeta电位等为评价指标,优化处方和工艺参数;采用透射电镜对样品形态进行表征,HPLC法测定姜黄素纳米混悬液体外释放,LC-MS/MS法检测大鼠体内姜黄素的血药浓度;RAW264.7炎症细胞模型考察其抗炎活性,支气管哮喘气道炎症小鼠模型考察姜黄素纳米混悬液对小鼠气道炎症的治疗作用。
结果: 制备工艺:姜黄素16 000 r·min-1转速下高速剪切2 min,800 bar循环40次。处方:姜黄素用量为0.2%,维生素E聚乙二醇琥珀酸酯(TPGS)用量为0.20%,大豆卵磷脂用量为0.16%;原料药与Cur-NCS累积释药量分别为11.67%和27.44%;大鼠灌胃后,Cur-NCS生物利用度提高了1.86倍;在体外炎症细胞模型和体内支气管哮喘小鼠模型中,Cur-NCS显著抑制炎症因子NO,IL-6,TNF-α的表达及MDA,IgE和ICAM-1水平,提高IL-10的表达与SOD的水平。
结论: 所确定的制备工艺和处方可满足姜黄素纳米混悬剂的制备需要,且体外释放、体内生物利用度、抗炎活性均显著优于原料药,姜黄素纳米混悬剂可为后续剂型研究提供思路。
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梁新丽,女,副教授,主要从事中药药效物质基础研究。联系电话:(0791)87118658,E-mail: paln7@163.com。
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梁新丽,女,副教授,主要从事中药药效物质基础研究。联系电话:(0791)87118658,E-mail: paln7@163.com。
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梁新丽,女,副教授,主要从事中药药效物质基础研究。联系电话:(0791)87118658,E-mail: paln7@163.com。
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鲁永锋,硕士研究生,主要方向:药物新剂型与新制剂。E-mail: lusan18870954216@163.com。
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鲁永锋,硕士研究生,主要方向:药物新剂型与新制剂。E-mail: lusan18870954216@163.com。
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