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用于临床研究的3D粉末床打印药物片剂

3D-Powder-Bed-Printed Pharmaceutical Drug Product Tablets for Use in Clinical Studies.

作者信息

van den Heuvel Korinde A, Berardi Alberto, Buijvoets Lisa B, Dickhoff Bastiaan H J

机构信息

DFE Pharma, Klever Strasse 187, 47568 Goch, Germany.

出版信息

Pharmaceutics. 2022 Oct 28;14(11):2320. doi: 10.3390/pharmaceutics14112320.

Abstract

Printing of phase 1 and 2a clinical trial formulations represents an interesting industrial application of powder bed printing. Formulations for clinical trials are challenging because they should enable flexible changes in the strength of the dosage form by varying the active pharmaceutical ingredient (API) percentage and tablet mass. The aim of this study was to investigate how powder bed 3D printing can be used for development of flexible platforms for clinical trials, suitable for both hydrophilic and hydrophobic APIs, using only conventional tableting excipients. A series of pre-formulation and formulation studies were performed to develop two platform formulations for clinical trials using acetaminophen and diclofenac sodium as model compounds and lactose and starch as excipients. The results showed that the type of starch used as the formulation binder must be optimized based on the type of API. Moreover, powder blend flow and liquid penetration ability proved to be critical material attributes (CMAs) that need to be controlled, particularly at high drug loading. Optimization of these CMAs was performed by selecting the appropriate particle size of the API or by addition of silica. A critical process parameter that had to be controlled for production of tablets of good quality was the quantity of the printing ink. After optimization of both the formulation and process parameters, two platform formulations, that is, one for each API, were successfully developed. Within each platform, drug loading from 5 up to 50% w/w and tablet mass from 50 to 500 mg were achieved. All 3D-printed tablets could be produced at tensile strength above 0.2 MPa, and most tablets could enable immediate release (i.e., >80% w/w within 30 min).

摘要

1期和2a期临床试验制剂的打印是粉末床打印一项有趣的工业应用。临床试验制剂具有挑战性,因为它们应通过改变活性药物成分(API)百分比和片剂质量,实现剂型强度的灵活变化。本研究的目的是研究如何利用粉末床3D打印技术,开发适用于亲水性和疏水性API的临床试验灵活平台,且仅使用常规压片辅料。进行了一系列处方前研究和处方研究,以开发两种用于临床试验的平台制剂,使用对乙酰氨基酚和双氯芬酸钠作为模型化合物,乳糖和淀粉作为辅料。结果表明,用作制剂粘合剂的淀粉类型必须根据API类型进行优化。此外,粉末混合物流动性和液体渗透能力被证明是需要控制的关键物料属性(CMA),特别是在高载药量时。通过选择合适的API粒径或添加二氧化硅来优化这些CMA。生产高质量片剂时必须控制的一个关键工艺参数是印刷油墨的用量。在优化了制剂和工艺参数后,成功开发了两种平台制剂,即每种API一种。在每个平台内,实现了5%至50% w/w的载药量和50至500 mg的片剂质量。所有3D打印片剂的拉伸强度均可达到0.2 MPa以上,且大多数片剂可实现速释(即30分钟内>80% w/w)。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/e53b/9699453/d077610226a2/pharmaceutics-14-02320-g001.jpg

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