Purpose

To investigate the compatibility between hard gelatin and HPMC capsules with a range of different isotropic lipid based formulations containing multiple excipients.

Methods

The miscibility was investigated for 350 systems applying five different oils (Labrafac ™ lipophile WL1349, Maisine® CC, Captex 300 EP/NF, olive oil, and Capmul MCM EP/NF), five different surfactans (Labrasol ® ALF, Labrafil M 2125 CS, Kolliphor ® ELP, Kolliphor ® HS 15, Tween 80) and three different cosolvents (propylene glycol, polyethylene glycol 400, and Transcutol ® HP). For the isotropic systems capsule compatibility was investigated in both gelatin and HPMC capsules at 25°C at 40% and 60% relative humidity by examining physical damages to the capsules and weight changes after storage.

Results

The miscibility of lipid based vehicles was best when the formulation contained monoglycerides and surfactants with a hydrophilic–lipophilic balance value <12. Gelatin capsules in general resulted in a better compatibility when compared to HPMC capsules for the evaluated formulations. Addition of water to the formulation improved the capsule compatibility for both capsule types. The expected capsule mass change could partly be predicted in binary systems using the provided data of the single excipients weighted for its formulation proportion.

Conclusions

The capsule compatibility was driven by the components incorporated into the formulations, where more was compatible with gelatin than HPMC capsules. Prediction of the mass change from individual excipient contributions can provide a good first estimate if a vehicle is compatible with a capsule, however, this needs to be proved experimentally.

中文翻译：

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硬明胶和 HPMC 胶囊中的脂质配方：物理相容性研究

目的

研究硬明胶和 HPMC 胶囊与包含多种赋形剂的一系列不同的各向同性脂质制剂之间的相容性。

方法

对使用五种不同油（Labrafac ™ lipophile WL1349、Maisine® CC、Captex 300 EP/NF、橄榄油和 Capmul MCM EP/NF）、五种不同表面活性剂（Labrasol ® ALF、Labrafil M 2125 CS）的 350 个系统的混溶性进行了研究, Kolliphor ® ELP, Kolliphor ® HS 15, Tween 80) 和三种不同的助溶剂（丙二醇、聚乙二醇 400 和 Transcutol ® HP）。对于各向同性系统，在 25°C、40% 和 60% 相对湿度下，通过检查胶囊的物理损坏和储存后的重量变化，研究了明胶和 HPMC 胶囊的胶囊相容性。

结果

当配方中含有亲水-亲油平衡值<12的甘油单酯和表面活性剂时，脂质载体的混溶性最好。与用于评估配方的 HPMC 胶囊相比，明胶胶囊通常具有更好的相容性。向配方中添加水改善了两种胶囊类型的胶囊相容性。使用所提供的单一赋形剂的配方比例加权数据，可以在二元系统中部分预测预期的胶囊质量变化。

结论

胶囊的相容性是由配方中的成分驱动的，其中与明胶的相容性比 HPMC 胶囊高。如果载体与胶囊兼容，则从单个赋形剂贡献预测质量变化可以提供一个很好的初步估计，但是，这需要通过实验来证明。