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首页> 外文期刊>International Journal of Pharmaceutics >Comparison of the mechanical properties of the crystalline and amorphous forms of a drug substance.
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Comparison of the mechanical properties of the crystalline and amorphous forms of a drug substance.

机译：药物结晶形式和无定形形式的机械性能比较。

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摘要

PURPOSE: To better understand the influence of long-range molecular order on the processing characteristics of an active pharmaceutical ingredient (API). METHODS: Crystalline and amorphous samples of a model drug substance were isolated and their "true" density, crystallinity, melting point, glass transition temperature, particle size distribution, and powder flow characteristics determined. Compacts of a standard porosity were manufactured from each form and their dynamic indentation hardness, quasi-static indentation hardness, tensile strength and "compromised tensile strength" determined. X-ray powder diffraction was used to confirm that no changes were induced by compact formation or testing. RESULTS: The crystalline and amorphous forms of the drug substance had relatively high melting and glass transition temperatures (approximately 271 and 142 degrees C, respectively) and were physically and chemically stable under the conditions of the testing laboratory. Consistent with this there was no evidence of crystallinity in the amorphous samples or vice versa before, during or after testing. The two API lots were effectively equivalent in their particulate properties (e.g. particle size distribution), although differences in their particle morphologies were observed which influenced powder flow behavior. The compacts of the bulk drug samples exhibited moderate ductility, elasticity, and strength, and high brittleness, in keeping with many other drug substance samples. A significantly greater compression stress was required to form the compacts of the crystalline material, and these sample materials were more ductile, less brittle and less elastic than those made from the amorphous API. There were no major differences in the tensile strength or the viscoelasticity of the compacts made from the crystalline and amorphous samples. CONCLUSIONS: The mechanical properties of compacted amorphous and crystalline samples of a drug substance have been measured and the contributions due to the molecular ordering of the crystalline form proposed. Small but significant differences in the mechanical properties were noted which could potentially affect the processing performance of API.
机译：目的：为了更好地理解远程分子顺序对活性药物成分（API）加工特性的影响。方法：分离出模型药物的结晶和无定形样品，并确定其“真实”密度，结晶度，熔点，玻璃化转变温度，粒度分布和粉末流动特性。由每种形式制造标准孔隙率的压块，并确定其动态压痕硬度，准静态压痕硬度，抗张强度和“折中抗张强度”。 X射线粉末衍射用于确认压块的形成或测试不会引起变化。结果：原料药的结晶和无定形形式具有较高的熔融和玻璃化转变温度（分别约为271和142摄氏度），并且在测试实验室的条件下具有物理和化学稳定性。与此相一致，在测试之前，期间或之后，无定形样品中没有结晶性的迹象，反之亦然。尽管观察到了两个API批次的颗粒形态差异会影响粉末的流动行为，但它们的颗粒性质（例如粒度分布）实际上是等效的。与许多其他原料药样品保持一致，原料药样品的压坯显示出适度的延展性，弹性和强度，以及高脆性。形成晶体材料的成形体需要明显更大的压缩应力，并且与由无定形API制成的材料相比，这些样品材料具有更高的延展性，脆性和弹性。由结晶和无定形样品制成的压块的拉伸强度或粘弹性没有重大差异。结论：已测量了致密无定形和结晶性药物样品的机械性能，并提出了由于结晶形式的分子有序化而引起的贡献。注意到机械性能上的微小但显着的差异可能会影响API的加工性能。

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