Introduction

Preparation of self-microemulsifying drug delivery systems (SMEDDS) is a promising delivery approach for drugs with poor aqueous solubility to enhance their dissolution properties and hence oral bioavailability. The objective of the present study was to define the influence of the oily phase surface properties of meloxicam self-microemulsifying drug delivery systems on the physicochemical properties of the formulation.

Methods

Minitab software was applied for the definition of a response surface experimental design. The shake flask method was used to determine the solubility of Meloxicam in formulation ingredients and prepared formulations. Refractive index, transmittance percentage, particle size and zeta potential, and dissolution behaviour of each formulation were determined.

Results

Meloxicam reveals higher solubility in Capryol PGMC (1.347 mg/ml) and PEG 400 (28.63 mg/ml) respectively. Surface tensions of pure Miglyol 812, Capryol PGMC, Labrasol, PEG 400, PG, and Transcutal P were 36.8, 36, 40.44, 40.22, 41, and 37.34 dyne/cm, and the interfacial tensions of Capryol PGMC and Miglyol 812 against the water were 7 and 12 dyne/cm respectively. In the majority of formulations, the solubility of meloxicam was higher in Capryol-containing formulations compared to Miglyol-containing ones. The lower surface tension of formulations associated with higher solubility of meloxicam, better dissolution, and lower emulsification times. Capryol-Labrasol-PEG 400 containing formulations show higher transmitted percentages. The size of droplets has been increased with an increase in the surface tension of formulations.

Conclusion

Lower surface tensions of SMEDDS excipients, especially oil phases, are associated with better physicochemical characteristics, i.e. higher solubilizing potential, emulsification ability, droplet size, transparency, refractive index, and dissolution behaviour.

中文翻译：

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油相表面性质对美洛昔康自微乳化给药系统理化特性的影响

介绍

自微乳化药物递送系统（SMEDDS）的制备是一种有前途的药物递送方法，用于改善水溶性差的药物，以提高其溶出性能，从而提高口服生物利用度。本研究的目的是确定美洛昔康自微乳化给药系统的油相表面性质对制剂理化性质的影响。

方法

Minitab 软件用于定义响应面实验设计。摇瓶法用于测定美洛昔康在制剂成分和制备制剂中的溶解度。测定了每种制剂的折射率、透光率、粒径和 zeta 电位以及溶出行为。

结果

美洛昔康分别在 Capryol PGMC (1.347 mg/ml) 和 PEG 400 (28.63 mg/ml) 中显示出更高的溶解度。纯 Miglyol 812、Capryol PGMC、Labrasol、PEG 400、PG 和 Transcutal P 的表面张力分别为 36.8、36、40.44、40.22、41 和 37.34 dyne/cm，Capryol PGMC 和 Miglyol 812 对水的界面张力分别为 7 和 12 达因/厘米。在大多数配方中，美洛昔康在含辛醇的配方中的溶解度高于含米格利尔的配方。制剂的较低表面张力与较高的美洛昔康溶解度、较好的溶解度和较低的乳化时间有关。含有 Capryol-Labrasol-PEG 400 的配方显示出更高的透射百分比。随着制剂表面张力的增加，液滴的大小也增加了。

结论

SMEDDS 赋形剂，尤其是油相的较低表面张力与更好的物理化学特性相关，即更高的增溶潜力、乳化能力、液滴大小、透明度、折射率和溶解行为。