Novel Pharmaceutical Cocrystals of Tegafur: Synthesis, Performance, and Theoretical Studies

Mei, Haoran; Wang, Na; Wu, Di; Rong, Qi; Bai, Xue; Huang, Xin; Zhou, Lina; Wang, Ting; Hao, Hongxun

doi:10.1007/s11095-024-03668-4

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“…In the pharmaceutical industry, the solid-state form of a drug is crucial for its solubility, dissolution, bioavailability, stability, and therapeutic effectiveness [1,2]. Among the various solid states that drugs can possess, the amorphous state is particularly significant due to its superior properties [3,4].…”

Section: Introductionmentioning

confidence: 99%

“…Figure 9. Accelerated stability test: (a) PXRD patterns of the samples S1 and S2 with different storage times in the drug stability test chamber; (b) PDF traces (The NNN represents the next nearest neighbor atoms in the nilotinib free base solid samples); (c) GNNN values (n = 3); (d) PCA scores plot (The R2 represents the goodness of fit, while the Q 2 represents the goodness of prediction, the crystalline Form A was used as a reference sample). (0(S1), 3(S1), and 6(S1) represent the sample S1 stored for 0, 3, and 6 months, respectively; 0(S2), 3(S2), and 6(S2) represent the sample S2 stored for 0, 3, and 6 months, respectively).…”

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An Investigation of the Impact of Precipitation Temperature and Filter Cake Thickness on the Physical Stability of Amorphous Solids: A Case Study

Li,

Liao,

Gong

et al. 2024

Molecules

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The purpose of this study was to resolve the issue of physical instability in amorphous solid drugs, which can result in unwanted crystallization, affecting solubility and dissolution rates. The focus was on precipitating physically stable amorphous forms of the nilotinib free base, an anticancer drug, by monitoring preparation conditions such as precipitation temperature and filter cake thickness. A comprehensive set of characterization techniques, including powder X-ray diffraction (PXRD), differential scanning calorimetry (DSC), thermogravimetric analysis (TGA), and focused beam reflectance measurement (FBRM), were used. These were supplemented by advanced data analysis methods that incorporated pair distribution function (PDF), reduced crystallization temperature (Rc), and principal component analysis (PCA) to evaluate the physical stability of the amorphous samples. Results emphasized that optimal physical stability was achieved when amorphous solids were prepared at a precipitation temperature of 10 °C and a filter cake thickness of 4 cm. Moreover, the integration of PDF analysis with Rc values was confirmed as an innovative approach for assessing physical stability, thus offering enhanced efficiency and accuracy over conventional accelerated stability testing methods.

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