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喷雾干燥对乙酰氨基酚/聚乙烯吡咯烷酮无定形固体分散体：第一部分——粉末和片剂的稳定性

Spray-Dried Paracetamol/Polyvinylpyrrolidone Amorphous Solid Dispersions: Part I-Stability of Powders and Tablets.

作者信息

Ritters Lena, Tian Yuanyuan, Reichl Stephan

机构信息

Institut für Pharmazeutische Technologie und Biopharmazie, Technische Universität Braunschweig, Mendelssohnstraße 1, D-38106 Braunschweig, Germany.

Zentrum für Pharmaverfahrenstechnik (PVZ), Franz-Liszt-Straße 35a, D-38106 Braunschweig, Germany.

出版信息

Pharmaceutics. 2021 Nov 16;13(11):1938. doi: 10.3390/pharmaceutics13111938.

DOI:10.3390/pharmaceutics13111938
PMID:34834353
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC8621994/
Abstract

The formulation of active pharmaceutical ingredients (APIs) in amorphous solid dispersions (ASDs) is a promising approach to improve the bioavailability of poorly soluble compounds. However, problems often arise in the production of tablets from ASDs regarding the compressibility and recrystallization of the API. In the present study, the preparation of spray-dried ASDs of paracetamol (PCM) and four different types of polyvinylpyrrolidone (PVP) and their further processing into tablets were investigated. The influence of PVP type on the glass transition temperature (T) and the physical stability of ASD powders were characterized by differential scanning calorimetry (DSC) and powder X-ray diffraction (XRD). ASD powders with 10 to 30% PCM were stable for at least 48 weeks. PCM contents of 40 to 50% led to recrystallization of the amorphous PCM within a few days or weeks. ASD with PVP/vinyl acetate (VA) copolymer (PVP/VA) was the most unstable and tended to recrystallize in PCM polymorphic form II. This formulation was therefore used for tablet studies. The influence of compression force on recrystallization, crushing strength, and drug release was investigated. Even high compression forces did not affect the stability of the ASD. However, the ASD tablets led to slow release of the API.

摘要

将活性药物成分（API）制成无定形固体分散体（ASD）是提高难溶性化合物生物利用度的一种很有前景的方法。然而，由ASD制备片剂时，在API的可压性和重结晶方面经常会出现问题。在本研究中，对扑热息痛（PCM）与四种不同类型聚乙烯吡咯烷酮（PVP）的喷雾干燥ASD的制备及其进一步压片过程进行了研究。通过差示扫描量热法（DSC）和粉末X射线衍射（XRD）对PVP类型对ASD粉末玻璃化转变温度（T）和物理稳定性的影响进行了表征。含10%至30%PCM的ASD粉末至少48周内稳定。40%至50%的PCM含量会导致无定形PCM在几天或几周内重结晶。含PVP/醋酸乙烯酯（VA）共聚物（PVP/VA）的ASD最不稳定，倾向于重结晶为PCM多晶型II。因此，该制剂用于片剂研究。研究了压力对重结晶、抗压强度和药物释放的影响。即使是高压力也不会影响ASD的稳定性。然而，ASD片剂导致API的缓释。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/3918/8621994/dc8c198ed182/pharmaceutics-13-01938-g011.jpg
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https://cdn.ncbi.nlm.nih.gov/pmc/blobs/3918/8621994/e626b9b9a575/pharmaceutics-13-01938-g010.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/3918/8621994/dc8c198ed182/pharmaceutics-13-01938-g011.jpg

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