Maruho Co., Ltd., Kyoto R&D Center, Drug Discovery Research Laboratories.
Chem Pharm Bull (Tokyo). 2021;69(4):352-359. doi: 10.1248/cpb.c20-00860.
Petrolatum ointment, which is an oleaginous ointment, is generally produced through manufacturing processes such as melting, mixing, and cooling. In this type of semisolid formulation, the manufacturing conditions of each process are empirically known to affect the quality of the resultant preparation; however, in many cases, the details of the factors are unclear. To clearly investigate the influence of the pharmaceutical properties of petrolatum ointments, we manufactured several ointments while changing the conditions of the mixing and cooling process after melting white petrolatum. As a result, the temperature at the termination was determined to influence the pharmaceutical properties of the final product. To investigate these phenomena, each petrolatum ointment sample was examined via digital microscopy and laser Raman analysis, and the distribution of the liquid-solid parts of samples was investigated. The internal structure of the ointment sample manufactured at a mixing-stop temperature of 40 °C, the needle crystals and the spherical aggregates surrounding them appropriately coexisted, while the structure exhibited a state wherein the two were linked in a semisolid phase. Meanwhile, for the ointment sample manufactured under the lowest mixing-stop temperature of 25 °C, the liquid part and the spherical aggregates were clearly separated, indicating that the liquid part was easily separated from ointments. In addition, the distribution of the hydrocarbons among the samples was measured via GC-MS; no significant difference in chemical structure was observed. In conclusion, the internal structure of the petrolatum ointment was changed by the manufacturing conditions, and this affected the pharmaceutical properties.
矿脂软膏是一种油性软膏，通常通过加热融化、混合和冷却等制造工艺生产。在这种半固体制剂中，每个工艺的制造条件都被经验性地认为会影响最终制剂的质量；然而，在许多情况下，这些因素的细节并不清楚。为了清楚地研究矿脂软膏的药物性质的影响，我们在加热融化白矿脂后改变混合和冷却过程的条件来制造几种软膏。结果发现，终止时的温度会影响最终产品的药物性质。为了研究这些现象，我们通过数字显微镜和激光拉曼分析对每个矿脂软膏样品进行了检查，并研究了样品中固液部分的分布。在混合停止温度为 40°C 的软膏样品中，针状晶体和围绕它们的球形聚集体适当共存，而结构呈现出两者在半固态相连接的状态。同时，对于在最低混合停止温度为 25°C 下制造的软膏样品，液体部分和球形聚集体明显分离，表明液体部分容易从软膏中分离出来。此外，我们还通过 GC-MS 测量了样品中的碳氢化合物分布；没有观察到化学结构的显著差异。总之，矿脂软膏的内部结构通过制造条件发生了变化，这影响了其药物性质。
