Article(id=1321426292726158320, tenantId=1146029695717560320, journalId=1235980733773295621, issueId=1321426285826519296, articleNumber=null, orderNo=null, doi=10.20251/j.cnki.1003-3734.2026.16.012, 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=1762099200000, acceptedDateStr=2025-11-03, onlineDate=1792982179099, onlineDateStr=2026-10-26, pubDate=1788019200000, pubDateStr=2026-08-30, doiRegisterDate=null, doiRegisterDateStr=null, onlineIssueDate=1792982179099, onlineIssueDateStr=2026-10-26, onlineJustAcceptDate=null, onlineJustAcceptDateStr=null, onlineFirstDate=null, onlineFirstDateStr=null, sourceXml=null, magXml=null, createTime=1792982179099, creator=13701087609, updateTime=1792982179099, updator=13701087609, issue=Issue{id=1321426285826519296, tenantId=1146029695717560320, journalId=1235980733773295621, year='2026', volume='35', issue='16', pageStart='1681', pageEnd='1792', issueExtLink='null', onlineDate='null', pubDate='1788019200000', pubDateStr='2026-08-30', beforeIssueId=null, nextIssueId=null, price=null, status=1, issueComplete=1, articleOrder=1, issueType=-1, specialIssue=null, createTime=1792982177454, creator='13701087609', updateTime=1792982881356, updator='13701087609', preIssue=null, nextIssue=null, articleTotal=null, ext={EN=IssueExt(id=1321429238297776921, tenantId=1146029695717560320, journalId=1235980733773295621, issueId=1321426285826519296, language=EN, specialIssueTitle=, coverIllustrator=null, specialIssueEditor=, specialIssueAbout=), CN=IssueExt(id=1321429238297776922, tenantId=1146029695717560320, journalId=1235980733773295621, issueId=1321426285826519296, language=CN, specialIssueTitle=, coverIllustrator=null, specialIssueEditor=, specialIssueAbout=)}, issueFiles=null, downloadFileDto=null}, startPage=1770, endPage=1777, ext={EN=ArticleExt(id=1321426294533903345, articleId=1321426292726158320, tenantId=1146029695717560320, journalId=1235980733773295621, language=EN, title=Preparation, evaluation and bioavailability study of abiraterone acetate-loaded lipid nanoemulsion, columnId=null, journalTitle=Chinese Journal of New Drugs, columnName=null, runingTitle=null, highlight=null, articleAbstract=
Objective: To improve the oral bioavailability of abiraterone acetate (ABA), reduce the administered dose, and eliminate its significant food effect.
Methods: ABA-loaded lipid nanoemulsion (ABA-NE) was prepared by high-pressure homogenization. The formulation and process parameters were optimized through single-factor tests and orthogonal experimental design. The prepared ABA-NE was characterized for particle size, polydispersity index (PDI), zeta potential, and entrapment efficiency. A pharmacokinetic study in beagle dogs was conducted to compare the bioavailability of ABA-NE with that of the reference tablets.
Results: The optimized ABA-NE appeared as a white, homogeneous emulsion with average particle size of (195.61±3.12) nm, PDI of (0.05±0.01), Zeta potential of -(48.17±2.64) mV, encapsulation efficiency of (95.76±1.59)% and drug loading capacity of (39.84±0.23) mg·mL-1. The pharmacokinetic study demonstrated that compared with the reference formulation, ABA-NE significantly increased the maximum plasma concentration (Cmax) and the area under the concentration-time curve (AUC). The oral relative bioavailability of ABA-NE was 16.06-fold higher than that of the reference tablets.
Conclusion: ABA-NE can significantly improve the oral bioavailability of ABA, which is expected to reduce the clinical dosage. It also provides a potential strategy for eliminating the effect of food. However, further experiments after meals are needed to verify this hypothesis.
, authors=Tian-tian GONG
1, Jian-feng ZUO
2, Ming ZHAO
1, Yong QIN
2, *, authorsList=Tian-tian GONG, Jian-feng ZUO, Ming ZHAO, Yong QIN, authorCompany=null, correspAuthors=Yong QIN, authorNote=null, correspAuthorsNote=null, copyrightStatement=null, copyrightOwner=null, extLink=null, articleAbsUrl=null, sourceXml=null, magXml=null, pdfUrl=null, pdf=null, pdfFileSize=null, pdfExtLink=null, richHtmlUrl=null, mobilePdfUrl=null, reviewReport=null, pdfFirstPage=null, abstractGraph=null, abstractGraphContent=null, abstractVideo=null, citation=null, cebUrl=null, magXmlContent=null, mapNumber=null, fund=null), CN=ArticleExt(id=1321426294810727410, articleId=1321426292726158320, tenantId=1146029695717560320, journalId=1235980733773295621, language=CN, title=醋酸阿比特龙脂质纳米乳的制备、评价与生物利用度研究, columnId=1236330556003242277, journalTitle=中国新药杂志, columnName=实验研究, runingTitle=null, highlight=null, articleAbstract=
目的: 提高醋酸阿比特龙(abiraterone acetate, ABA)的口服生物利用度,减少给药剂量,消除其严重的食物效应。
方法: 采用高压均质法制备醋酸阿比特龙脂质纳米乳(ABA-loaded lipid nanoemulsion, ABA-NE),通过单因素实验与正交设计优化处方与工艺参数,并对制剂的粒径、多分散指数(polydispersity index, PDI)、Zeta电位及包封率进行表征。以比格犬为模型动物,进行体内药动学研究,比较ABA-NE与原研片剂的生物利用度。
结果: 优化所得ABA-NE呈白色均一乳状,平均粒径为(195.61±3.12) nm,PDI为(0.05±0.01),Zeta电位为-(48.17±2.64) mV,包封率达(95.76±1.59)%,载药量为(39.84±0.23) mg·mL-1。药动学结果表明,与醋酸阿比特龙原研片剂相比,ABA-NE的Cmax和AUC显著提高,口服相对生物利用度为原研片剂的16.06倍。
结论: ABA-NE能显著提高ABA的口服生物利用度,有望降低临床给药剂量,同时为消除食物效应提供了潜在策略,未来需要进一步通过餐后实验验证。
, authors=宫甜甜
1, 佐建锋
2, 赵明
1, 秦勇
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