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优化长春西汀冻干片的处方设计与临床研究：口腔固体制剂开发的新策略

Formulation and clinical investigation of optimized vinpocetine lyoplant-tabs: new strategy in development of buccal solid dosage form.

作者信息

Ahmed Tarek A

机构信息

Department of Pharmaceutics, Faculty of Pharmacy, King Abdulaziz University, Jeddah, Kingdom of Saudi Arabia,

Department of Pharmaceutics and Industrial Pharmacy, Faculty of Pharmacy, Al-Azhar University, Cairo, Egypt,

出版信息

Drug Des Devel Ther. 2018 Dec 28;13:205-220. doi: 10.2147/DDDT.S189105. eCollection 2019.

DOI:10.2147/DDDT.S189105
PMID:30643387
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC6312694/
Abstract

BACKGROUND

This work aimed to develop a new solid dosage formulation of vinpocetine (VPN) in the form of buccal freeze-dried pullulan-based tablets (lyoplant-tabs) loaded with physically modified drug binary system.

METHODS

Different polyvinyl pyrrolidone (PVP) grades were studied to prepare an efficient VPN binary system characterized by enhanced equilibrium saturation solubility, solubilization efficiency, thermodynamic stability, and permeation through oral mucosal cell lines. The concentrations of pullulan and swelling-aid polymer that affect the quality attributes of lyoplant-tabs were optimized. Clinical pharmacokinetics study on human volunteers for the optimized lyoplant-tabs compared to marketed product was accomplished.

RESULTS

A promising drug binary system with polyvinyl pyrrolidone vinyl acetate (PVP-VA64) utilizing the lyophilization technique was developed. Solid-state characterization confirmed transformation of VPN completely into the amorphous form. The concentrations of pullulan and swelling-aid polymer were significantly affecting the characteristics of the tablets. Compared to the commercial VPN tablets, pullulan-based buccal tablets demonstrated enhancement in the studied pharmacokinetic parameters with positive impact on the drug bioavailability.

CONCLUSION

These VPN lyoplant-tabs containing lyophilized PVP-VA64-VPN binary system can be considered as an alternative to currently available marketed tablets; however, further preclinical investigations using large number of volunteers are required.

摘要

背景

本研究旨在开发一种新的长春西汀（VPN）固体剂型，即基于普鲁兰多糖的口腔冻干片（冻干片），其负载物理改性药物二元体系。

方法

研究了不同等级的聚乙烯吡咯烷酮（PVP），以制备一种高效的VPN二元体系，其特点是平衡饱和溶解度、增溶效率、热力学稳定性以及通过口腔黏膜细胞系的渗透率均有所提高。优化了影响冻干片质量属性的普鲁兰多糖和助溶聚合物的浓度。完成了针对优化后的冻干片与市售产品在人体志愿者身上的临床药代动力学研究。

结果

利用冻干技术开发了一种有前景的含聚乙烯吡咯烷酮醋酸乙烯酯（PVP-VA64）的药物二元体系。固态表征证实VPN完全转变为无定形形式。普鲁兰多糖和助溶聚合物的浓度对片剂特性有显著影响。与市售VPN片剂相比，基于普鲁兰多糖的口腔片在所研究的药代动力学参数方面有所提高，对药物生物利用度有积极影响。

结论

这些含有冻干PVP-VA64-VPN二元体系的VPN冻干片可被视为现有市售片剂的替代品；然而，需要使用大量志愿者进行进一步的临床前研究。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/294e/6312694/cf439b082516/dddt-13-205Fig6.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/294e/6312694/6f7bfa3bc435/dddt-13-205Fig1.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/294e/6312694/948f431de737/dddt-13-205Fig2.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/294e/6312694/010fc15fea9d/dddt-13-205Fig3.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/294e/6312694/cd0f689400c2/dddt-13-205Fig4.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/294e/6312694/9563c7fd9fb2/dddt-13-205Fig5.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/294e/6312694/cf439b082516/dddt-13-205Fig6.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/294e/6312694/6f7bfa3bc435/dddt-13-205Fig1.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/294e/6312694/948f431de737/dddt-13-205Fig2.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/294e/6312694/010fc15fea9d/dddt-13-205Fig3.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/294e/6312694/cd0f689400c2/dddt-13-205Fig4.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/294e/6312694/9563c7fd9fb2/dddt-13-205Fig5.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/294e/6312694/cf439b082516/dddt-13-205Fig6.jpg

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