Article(id=1212692430252589841, tenantId=1146029695717560320, journalId=1190317699101192196, issueId=1212692423956939344, articleNumber=1001-2494(2024)17-1590-07, orderNo=null, doi=10.11669/cpj.2024.17.006, pmid=null, cstr=null, oa=null, hot=null, price=null, onlineType=0, articleFormat=0, articleType=null, articleTypeStr=research-article, receivedDate=1677513600000, receivedDateStr=2023-02-28, revisedDate=null, revisedDateStr=null, acceptedDate=null, acceptedDateStr=null, onlineDate=1767058006108, onlineDateStr=2025-12-30, pubDate=1725724800000, pubDateStr=2024-09-08, doiRegisterDate=null, doiRegisterDateStr=null, onlineIssueDate=1767058006108, onlineIssueDateStr=2025-12-30, onlineJustAcceptDate=null, onlineJustAcceptDateStr=null, onlineFirstDate=null, onlineFirstDateStr=null, sourceXml=null, magXml=null, createTime=1767058006108, creator=13701087609, updateTime=1767058006108, updator=13701087609, issue=Issue{id=1212692423956939344, tenantId=1146029695717560320, journalId=1190317699101192196, year='2024', volume='59', issue='17', pageStart='1553', pageEnd='1664', issueExtLink='null', onlineDate='null', pubDate='null', beforeIssueId=null, nextIssueId=null, price=null, status=1, issueComplete=1, articleOrder=1, issueType=-1, specialIssue=null, createTime=1767058004596, creator=13701087609, updateTime=1767058886858, updator=13701087609, preIssue=null, nextIssue=null, ext={EN=IssueExt(id=1212696124457140722, tenantId=1146029695717560320, journalId=1190317699101192196, issueId=1212692423956939344, language=EN, specialIssueTitle=, coverIllustrator=null, specialIssueEditor=, specialIssueAbout=), CN=IssueExt(id=1212696124457140723, tenantId=1146029695717560320, journalId=1190317699101192196, issueId=1212692423956939344, language=CN, specialIssueTitle=, coverIllustrator=null, specialIssueEditor=, specialIssueAbout=)}, issueFiles=null}, startPage=1590, endPage=1596, ext={EN=ArticleExt(id=1212692430713963304, articleId=1212692430252589841, tenantId=1146029695717560320, journalId=1190317699101192196, language=EN, title=Research Progress of Transdermal Delivery of Anti-Vomiting Drug 5-HT₃ Receptor Antagonist, columnId=null, journalTitle=Chinese Pharmaceutical Journal, columnName=null, runingTitle=null, highlight=null, articleAbstract=

Chemotherapy induced nausea and vomiting (CINV) is the most common adverse reaction in cancer patients during chemotherapy. 5-HT₃ receptor antagonists are recommended as the first-line drugs against CINV. However, the commonly used clinical dosage forms of 5-HT₃ receptor antagonists are mainly oral and intravenous administration, among which intravenous administration is easy to produce adverse reactions and requires professional medical operation. Oral administration has first-pass effect, especially for patients with severe vomiting after chemotherapy, so the commonly used clinical dosage forms have certain defects and limited clinical application. Transdermal drug delivery system has the advantages of avoiding gastrointestinal first-pass effect, less toxic and side effects, and good patient compliance, so the transdermal drug delivery system of anti-tumor nausea and vomiting drugs has been widely concerned and studied. In this paper, the research status of transdermal delivery of 5-HT₃ receptor antagonists at home and abroad is reviewed, which provides reference for the research and development of new preparations and new delivery routes of these drugs.

, correspAuthors=Yuan XU, 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, authorCompany=null, fund=null, authors=null, authorsList=Xu ZHANG, Xiurong GAO, Qianru WANG, Taomin HU, Qin CAI, Xingxing WU, Tao ZHANG, Yuan XU), CN=ArticleExt(id=1212692432299410313, articleId=1212692430252589841, tenantId=1146029695717560320, journalId=1190317699101192196, language=CN, title=抗呕吐药5-HT₃受体拮抗剂的经皮给药制剂研究进展, columnId=1190352408384471863, journalTitle=中国药学杂志, columnName=综述, runingTitle=null, highlight=null, articleAbstract=

化疗所致恶心呕吐(chemotherapy induced nausea and vomiting, CINV)是肿瘤患者化疗过程中最常见的不良反应。5-HT₃受体拮抗剂类药物被推荐为抗CINV的一线用药。但5-HT₃受体拮抗剂药物目前临床常用剂型以口服和静脉给药为主,其中静脉注射给药易产生不良反应且需要专业医护操作,口服给药有首过效应,尤其是化疗后严重呕吐患者无法口服用药,所以目前临床常用剂型具有一定的缺陷,临床应用受到限制。经皮给药系统具有避免胃肠道首过效应、毒副作用小、病人依从性好等优点,所以抗肿瘤所致恶心呕吐药物的经皮给药系统受到人们的广泛关注和研究。本研究就5-HT₃受体拮抗剂类药物的经皮给药制剂国内外研究现状进行综述,为该类药物的新制剂和新给药途径研发提供借鉴和参考。

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张旭,女,硕士,主管药师 研究方向:临床药学及药物新制剂研究

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张旭,女,硕士,主管药师 研究方向:临床药学及药物新制剂研究

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1-格拉司琼微乳;2-格拉司琼混悬剂;3-格拉司琼凝胶;4-格拉司琼水溶液。

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CINV种类	分类依据
急性	发生在给予化疗药物24 h内,并在给药后5~6 h达高峰,多在24 h内缓解
延迟性	发生在给予化疗药物24 h之后,用药后48~72 h达到最高峰,可持续6~7 d
预期性	患者在前一次化疗时经历了难以控制的CINV,在下一次化疗开始前即发生的恶心呕吐
爆发性	指即使充分使用了预防恶心呕吐的药物,仍出现的恶心呕吐和(或)需要进行解救性止吐治疗
难治性	指以往的化疗周期中使用预防性和(或)解救性止吐治疗失败,而在后续化疗周期中仍然出现的恶心呕吐

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化疗所致恶心呕吐(CINV)的种类和分类依据

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CINV种类	分类依据
急性	发生在给予化疗药物24 h内,并在给药后5~6 h达高峰,多在24 h内缓解
延迟性	发生在给予化疗药物24 h之后,用药后48~72 h达到最高峰,可持续6~7 d
预期性	患者在前一次化疗时经历了难以控制的CINV,在下一次化疗开始前即发生的恶心呕吐
爆发性	指即使充分使用了预防恶心呕吐的药物,仍出现的恶心呕吐和(或)需要进行解救性止吐治疗
难治性	指以往的化疗周期中使用预防性和(或)解救性止吐治疗失败,而在后续化疗周期中仍然出现的恶心呕吐

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代表药物	剂量和给药途径
昂丹司琼	8~16 mg静脉注射;16~24 mg口服
阿扎司琼	10 mg静脉注射;口服
多拉司琼	100 mg口服
格拉司琼	3 mg静脉注射;2 mg口服;或3.1 mg透皮贴
莫雷司琼	0.3 mg静脉注射
帕洛诺司琼	0.25 mg静脉注射;0.5 mg口服
托烷司琼	5 mg静脉注射;口服

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临床常用的5-羟色胺3(5-HT₃)受体拮抗剂代表性药物及用量

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代表药物	剂量和给药途径
昂丹司琼	8~16 mg静脉注射;16~24 mg口服
阿扎司琼	10 mg静脉注射;口服
多拉司琼	100 mg口服
格拉司琼	3 mg静脉注射;2 mg口服;或3.1 mg透皮贴
莫雷司琼	0.3 mg静脉注射
帕洛诺司琼	0.25 mg静脉注射;0.5 mg口服
托烷司琼	5 mg静脉注射;口服

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药物	相对分子质量	logP值	熔点/℃
昂丹司琼	293.15	2.07[13]	231~232
阿扎司琼	349.81	1.91	301~303
多拉司琼	324.37	2.46	278
格拉司琼	315.43	3.45	290~292
莫雷司琼	279.30	3.69	244~246
帕洛诺司琼	296.41	2.53	91[14]
托烷司琼	284.35	3.55	201~202

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5-HT₃受体拮抗剂代表性药物的主要理化性质

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药物	相对分子质量	logP值	熔点/℃
昂丹司琼	293.15	2.07[13]	231~232
阿扎司琼	349.81	1.91	301~303
多拉司琼	324.37	2.46	278
格拉司琼	315.43	3.45	290~292
莫雷司琼	279.30	3.69	244~246
帕洛诺司琼	296.41	2.53	91[14]
托烷司琼	284.35	3.55	201~202

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