Meira Rafaela Z C, Biscaia Isabela F B, Nogueira Camila, Murakami Fabio S, Bernardi Larissa S, Oliveira Paulo R
Post Graduation Program in Pharmaceutical Sciences, Department of Pharmacy, Universidade Estadual do Centro-Oeste/UNICENTRO, Guarapuava, PR 85040-080, Brazil.
Department of Pharmacy, Federal University of Paraná, Av. Prefeito Lothário Meissner, 632, Jardim Botânico, Curitiba, PR 80210-170, Brazil.
Materials (Basel). 2019 Sep 27;12(19):3154. doi: 10.3390/ma12193154.
The physical and chemical characterization of the solid-state properties of drugs and excipients is fundamental for planning new formulations and developing new strategies for the treatment of diseases. Techniques such as differential scanning calorimetry, thermogravimetry, X-ray powder diffraction, Fourier transform infrared spectroscopy, and scanning electron microscopy are among the most commonly used techniques for these purposes. Penciclovir and lysine are individually used to treat the herpes virus. As such, the development of a formulation containing both drugs may have therapeutic potential. Solid-state characterization showed that both penciclovir and lysine were crystalline materials with melting points at 278.27 °C and 260.91 °C, respectively. Compatibility studies of penciclovir and lysine indicated a possible interaction between these substances, as evidenced by a single melting point at 253.10 °C. The compatibility of several excipients, including ethylenediaminetetraacetic acid, cetostearyl alcohol, sodium lauryl sulphate, di-tert-butyl methyl phenol, liquid petrolatum, methylparaben, nonionic wax, paraffin, propylene glycol, and propylparaben, was evaluated in ternary (penciclovir-lysine-excipient) mixtures (1:1:1, //) to determine the optimal formulation. The developed formulation was stable under accelerated and ambient conditions, which demonstrated that the interaction between penciclovir and lysine was suitable for the development of a formulation containing both drugs.
药物和辅料固态性质的物理化学表征对于规划新剂型和开发疾病治疗新策略至关重要。差示扫描量热法、热重分析法、X射线粉末衍射法、傅里叶变换红外光谱法和扫描电子显微镜等技术是用于这些目的最常用技术。喷昔洛韦和赖氨酸分别用于治疗疱疹病毒。因此，开发一种包含这两种药物的剂型可能具有治疗潜力。固态表征表明，喷昔洛韦和赖氨酸均为结晶材料，熔点分别为278.27℃和260.91℃。喷昔洛韦和赖氨酸的相容性研究表明这两种物质之间可能存在相互作用，253.10℃处的单一熔点证明了这一点。在三元（喷昔洛韦-赖氨酸-辅料）混合物（1:1:1，//）中评估了几种辅料的相容性，包括乙二胺四乙酸、鲸蜡硬脂醇、月桂基硫酸钠、二叔丁基甲基苯酚、液体石蜡、对羟基苯甲酸甲酯、非离子蜡、石蜡、丙二醇和对羟基苯甲酸丙酯，以确定最佳剂型。所开发的剂型在加速条件和环境条件下均稳定，这表明喷昔洛韦和赖氨酸之间的相互作用适合开发包含这两种药物的剂型。
