吡喹酮制剂的挑战和已证实的建议

IF 2.1 4区 医学 Q3 PHARMACOLOGY & PHARMACY Journal of Clinical Pharmacy and Therapeutics Pub Date : 2023-10-16 DOI:10.1155/2023/3976392
Deryl Nii Okantey Kuevi, Francis Asiedu Acquah, Amy Amuquandoh, Andrew Papa Abbey
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引用次数: 0

摘要

背景。血吸虫病是世界上仅次于疟疾的重要寄生虫感染之一,截至2019年,感染人数接近2.4亿。吡喹酮是一种口服驱虫药,是治疗血吸虫病的一线药物。虽然该药物安全有效,但配方片剂存在一些局限性,如生物利用度低和苦味。本文献综述旨在提供有关如何改善吡喹酮制剂相关的溶解度、低生物利用度和苦味问题的信息,并随后有助于提高患者的依从性。材料与方法。为了收集本综述中有关吡喹酮配方改进的所有相关数据,使用了以下数据库:Google Scholar、Science Direct、Scopus、PubMed、Springer Link、Elsevier和Wiley在线图书馆。结果。文献显示,在提高吡喹酮的生物利用度方面,在药物中加入氢化蓖麻油固体脂质纳米颗粒可有效延长口服给药后7.6至95.9小时的体循环。此外,采用融合方法的固体分散技术将吡喹酮的生物利用度提高了约两倍。此外,在制剂中加入超崩解剂或一种以上崩解剂可增强吡喹酮的释放。添加羟丙基-β-环糊精(HP-β-CD)和三氯蔗糖作为甜味剂可以掩盖吡喹酮的苦味。结论。本文综述的配制方法可大大提高吡喹酮的溶解度、生物利用度和口感。虽然改进吡喹酮配方的几种技术已经得到了广泛的研究,但还需要进一步研究吡喹酮的释放特性以及与其他赋形剂的相容性。
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Challenges and Proven Recommendations of Praziquantel Formulation
Background. Schistosomiasis, ranked second to malaria as one of the crucial parasitic infections in the world, infects close to 240 million people as at 2019. Praziquantel, an oral anthelmintic, is the first-line drug for the treatment of schistosomiasis. Although the drug is safe and effective, the formulated tablets come with some limitations such as low bioavailability and bitter taste. This literature review aims to provide information on how to improve the issues of solubility, low bioavailability, and bitter taste associated with the praziquantel formulation and, subsequently, to be helpful in improving patient’s compliance. Materials and Methods. For gathering all pertinent data in this review on improving the praziquantel formulation, the following databases were used: Google Scholar, Science Direct, Scopus, PubMed, Springer Link, Elsevier, and Wiley online library. Results. Literature revealed that in improving the bioavailability of praziquantel, loading the drug with hydrogenated castor oil solid lipid nanoparticles has shown to be effective in prolonging systemic circulation from 7.6 to 95.9 hours after oral administration. Moreover, employing the solid dispersion technique using the fusion method increases the bioavailability of praziquantel about twice as much. Furthermore, incorporating a superdisintegrant or more than one disintegrant to the formulation can enhance the release of praziquantel. The addition of hydroxypropyl-beta-cyclodextrin (HP-β-CD) and sucralose as sweeteners can mask the bitter taste of praziquantel. Conclusion. The formulation approaches outlined in this review can be employed to greatly enhance the solubility, bioavailability, and taste of praziquantel. Although several techniques to improve praziquantel formulation have been widely studied, further studies on the release profile and compatibility studies with other excipients need to be investigated.
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来源期刊
CiteScore
4.10
自引率
5.00%
发文量
226
审稿时长
6 months
期刊介绍: The Journal of Clinical Pharmacy and Therapeutics provides a forum for clinicians, pharmacists and pharmacologists to explore and report on issues of common interest. Reports and commentaries on current issues in medical and pharmaceutical practice are encouraged. Papers on evidence-based clinical practice and multidisciplinary collaborative work are particularly welcome. Regular sections in the journal include: editorials, commentaries, reviews (including systematic overviews and meta-analyses), original research and reports, and book reviews. Its scope embraces all aspects of clinical drug development and therapeutics, including: Rational therapeutics Evidence-based practice Safety, cost-effectiveness and clinical efficacy of drugs Drug interactions Clinical impact of drug formulations Pharmacogenetics Personalised, stratified and translational medicine Clinical pharmacokinetics.
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