Mazurkevičiūtė Agnė, Matulytė Inga, Ivaškienė Marija, Žilius Modestas
Institute of Pharmaceutical Technologies, Lithuanian University of Health Sciences, 50162 Kaunas, Lithuania.
Department of Clinical Pharmacy, Lithuanian University of Health Sciences, 50162 Kaunas, Lithuania.
Polymers (Basel). 2022 Jul 7;14(14):2783. doi: 10.3390/polym14142783.
Emulsions are thermodynamically unstable systems and it is difficult to produce biphasic formulations with large amounts of oil. The aim of our study was to prepare biphasic formulations containing 1% ciclopirox olamine and to determine the influence of the method of oil incorporation (without and with emulsifier and gelifier) on the physical (pH, particle size, rheological properties), mechanical, and biopharmaceutical properties of the formulations. It was found that the use of a poloxamer 407 gel as the hydrophase could result in a stable formulation when an oil with (EPG) or without an emulsifier (APG) or oleogel (OPG) was used as the oily phase. The results of the studies showed that the addition of an emulsifier (polysorbate 80) led to a decrease in the sol-gel temperature, a slower release of ciclopirox olamine, and a higher stability in the freeze-thaw test. However, regardless of the way the oil is incorporated, the particles are distributed in the same range and the antifungal activity against is the same. It is possible to create a biphasic formulation with a large amount of oil and poloxamer gel, but for greater stability, it is recommended to include an emulsifier in the composition.
乳剂是热力学不稳定体系，制备含大量油相的双相制剂较为困难。本研究的目的是制备含1%环吡酮胺的双相制剂，并确定油相加入方法（不添加和添加乳化剂及胶凝剂）对制剂的物理性质（pH值、粒径、流变学性质）、机械性质和生物药剂学性质的影响。研究发现，当使用含乳化剂（EPG）或不含乳化剂（APG）的油相或油凝胶（OPG）作为油相时，以泊洛沙姆407凝胶作为水相可得到稳定的制剂。研究结果表明，添加乳化剂（聚山梨酯80）会导致溶胶-凝胶温度降低、环吡酮胺释放减慢以及冻融试验中的稳定性更高。然而，无论油相的加入方式如何，颗粒分布范围相同，对……的抗真菌活性相同。使用大量油相和泊洛沙姆凝胶制备双相制剂是可行的，但为了获得更高的稳定性，建议在配方中加入乳化剂。
