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首页> 外文期刊>Crystal growth & design >Effect of Crystal Habit on Intrinsic Dissolution Behavior of Celecoxib Due to Differential Wettability
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Effect of Crystal Habit on Intrinsic Dissolution Behavior of Celecoxib Due to Differential Wettability

机译：结晶习性对差异润湿性对塞来昔布内在溶解行为的影响

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摘要

Intrinsic dissolution rate (IDR) is a useful technique to differentiate the solid forms of a drug. In the present study, the impact of crystal habit and crystal size on IDR of celecoxib (CEL) in different media was assessed. The IDR of plate-shaped CEL crystals (CEL-P) (53.4 ± 6.7 μg/min/cm~2) was 46.3% higher than that of acicular crystals (CEL-A) (36.5 ± 1.7 μg/min/cm~2) in pH 12 phosphate buffer. Contact angle experiments and values of dispersive and polar components of surface free energy indicated better wettability of CEL-P compacts than CEL-A. Higher IDR and better wettability of CEL-P were attributed to favorable exposure of hydrophilic crystal facets on compact surface, due to preferred orientation during compaction. In contrast to native samples, milled CEL-A (MCEL-A) and milled CEL-P (MCEL-P) showed similar IDR. Interestingly, IDR of CEL-A (36.5 ± 1.7 μg/min/cm~2) and MCEL-A (35.64 ± 5.09 μg/min/cm~2) did not show any significant difference (p >0.05). However, IDR of CEL-P (53.4 ± 6.7 μg/min/cm~2) was significantly higher (p < 0.05) than that of MCEL-P (39.15 ± 2.48 μg/min/cm~2). This was ascribed to (i) differential cleavage behavior of CEL-A and CEL-P during milling and (ii) reduced degree of preferred orientation of hydrophilic facets in MCEL-P compacts. This work provides an interesting case study of the impact of particle level properties and surface molecular environment on IDR.
机译：本征溶出度（IDR）是区分药物固体形式的有用技术。在本研究中，评估了晶体习性和晶体大小对塞来昔布（CEL）在不同介质中IDR的影响。平板状CEL晶体（CEL-P）的IDR（53.4±6.7μg/ min / cm〜2）比针状晶体（CEL-A）（36.5±1.7μg/ min / cm〜2）高46.3％ ）在pH 12磷酸盐缓冲液中。接触角实验以及表面自由能的分散和极性组分的值表明，CEL-P压块的润湿性比CEL-A好。更高的IDR和更好的CEL-P润湿性归因于压实过程中的首选取向，使亲水性晶面在致密表面上具有良好的暴露性。与天然样品相比，磨碎的CEL-A（MCEL-A）和磨碎的CEL-P（MCEL-P）显示出相似的IDR。有趣的是，CEL-A（36.5±1.7μg/ min / cm〜2）和MCEL-A（35.64±5.09μg/ min / cm〜2）的IDR没有显示任何显着差异（p> 0.05）。然而，CEL-P的IDR（53.4±6.7μg/ min / cm〜2）明显高于MCEL-P（39.15±2.48μg/ min / cm〜2）（p <0.05）。这归因于（i）在研磨过程中CEL-A和CEL-P的不同裂解行为，以及（ii）MCEL-P压坯中亲水性小面的优选取向度降低。这项工作提供了有关粒子水平特性和表面分子环境对IDR影响的有趣案例研究。

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