Effect of talc and vitamin E TPGS on manufacturability, stability and release properties of trilaurin-based formulations for hot-melt coating,International Journal of Pharmaceutics

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Effect of talc and vitamin E TPGS on manufacturability, stability and release properties of trilaurin-based formulations for hot-melt coating
International Journal of Pharmaceutics ( IF 5.3 ) Pub Date : 2024-01-28 , DOI: 10.1016/j.ijpharm.2024.123866
Van-Trung-Tin Huynh ₁ , Suenia de Paiva Lacerda ₁ , Fabienne Espitalier ₁ , Eric Beyssac ₂ , Maria-Inês Ré ₁

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This study was focused on one particular case of hot-melt coating with trilaurin – a solid medium-chain monoacid triglyceride. The challenge of using trilaurin as coating agent in melting-based processes is linked to its relatively low melting profile: 15.6 °C (Tm,α), 35.1 °C (Tm,β′) and 45.7 °C (Tm,β). From a process perspective, the only possibility to generate products coated with formulations composed of trilaurin is by setting thermal operational conditions above Tm,α. From a material perspective, this processing possibility depends principally on trilaurin crystallisation which was investigated via a set of analytical techniques including turbidimetry, calorimetry, hot-melt goniometry, and polarised light microscopy. A highly soluble drug model substrate (sodium chloride crystals) was coated with three selected trilaurin-based formulations: (i) trilaurin, (ii) trilaurin plus talc, and (iii) trilaurin plus vitamin E TPGS and talc. Coated salt crystals were then analysed to investigate processing performance, coating quality, stability and release properties under digestion effect. The results show that firstly, talc addition promotes nucleation and crystal growth and, as a consequence, it facilitates the manufacture of trilaurin-based formulations. Secondly, the formulation of a solid triglyceride and a hydrophilic surfactant could potentially cause release instability, but formula (iii) was found to be stabilised by a mechanism whereby trilaurin crystallization enhanced in the presence of talc immobilised vitamin E TPGS in its crystal lattice. Thirdly, talc addition did not significantly influence trilaurin digestion which endows products with an immediate release in lipolytic conditions instead of an extended liberation in pure water. Nor did the addition of one or two additives alter the extent of trilaurin digestion under the conditions studied. These important findings relate to product manufacturability, stability, and release properties. A good understanding of material properties (e.g. crystallisation, polymorphism, digestibility) is essential for melt-processing, lipid coating stabilising and modulation of release profile of solid lipid-coated product, as demonstrated in this case study with trilaurin.

中文翻译：

滑石粉和维生素 E TPGS 对热熔涂料用三月桂酸酯基配方的可制造性、稳定性和释放性能的影响

这项研究的重点是使用三月桂酸甘油酯（一种固体中链单酸甘油三酯）进行热熔包衣的一个特殊情况。在基于熔融的工艺中使用三月桂酸甘油酯作为涂层剂的挑战与其相对较低的熔点有关：15.6 °C （Tm，α）、35.1 °C （Tm，β′）和 45.7 °C （Tm，β）。从工艺角度来看，生产由三月桂酸甘油酯组成的配方包衣的产品的唯一可能性是将热作条件设置为高于 Tm，α。从材料的角度来看，这种加工可能性主要取决于三月桂酸甘油苷结晶，这是通过一系列分析技术进行的研究，包括比浊法、量热法、热熔测角法和偏振光显微镜。高度可溶性药物模型底物（氯化钠晶体）涂有三种选定的基于三月桂酸酯的制剂：（i）三月桂酸甘油酯，（ii）三月桂酸甘油酯加滑石粉，以及（iii）三月桂酸甘油酯加维生素 E TPGS 和滑石粉。然后分析包覆盐晶体，以研究消化作用下的加工性能、包衣质量、稳定性和释放性能。结果表明，首先，滑石粉添加促进了成核和晶体生长，因此，它促进了基于三月桂酸酯的配方的制造。其次，固体甘油三酯和亲水性表面活性剂的配方可能会导致释放不稳定，但发现配方（iii）通过一种机制来稳定，即在其晶格中含有滑石粉固定的维生素 E TPGS 存在下，三月桂酸甘油酸结晶增强。第三，添加滑石粉对三月桂酸甘油酯的消化没有显着影响，这使产品在脂解条件下立即释放，而不是在纯水中延长释放。在所研究的条件下，添加一种或两种添加剂也不会改变三月桂酸甘油酯的消化程度。这些重要发现与产品可制造性、稳定性和释放特性有关。充分了解材料特性（例如结晶、多晶型、消化率）对于固体脂质包衣产品的熔融加工、脂质涂层稳定和释放曲线的调节至关重要，如本 trilaurin 案例研究所示。

更新日期：2024-01-28

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