Department of Pharmaceutical Sciences, M.D. University, Rohtak, 124001, India.
AAPS PharmSciTech. 2024 Jul 24;25(6):169. doi: 10.1208/s12249-024-02888-6.
Motion sickness also known as kinetosis is a condition in which there exists a disagreement between visually perceived movement and the vestibular system's sense of movement. Nausea, vomiting, dizziness, fatigue, and headache are the most common symptoms of motion sickness. This study mainly focuses on the taste masking of Promethazine Hydrochloride (PMZ) by inclusion complexation method, its formulation development in the chewing gum form by using directly compressible gum base HIG® and its quality and performance testing. Different molar ratios (1:1, 1:2, 1:3 and 1:4) of PMZ-cyclodextrin complexes were prepared by using β-Cyclodextrin (β-CD) as a taste masking agent. These complexes were evaluated for FTIR, DSC, % Entrapment Efficiency, % drug yield, and taste evaluation by E-Tongue. The optimized ratio was further evaluated by sophisticated analytical techniques such as Scanning Electron Microscopy (SEM) and X-Ray Diffraction (XRD). A central composite design (CCD) (3 ^2) was utilized to examine the effects of independent variables (amount of gum-X and amount of plasticizer-X) on dependent variables (%CDRY and hardness Y). The prepared gums were evaluated for drug content, organoleptic properties, in-vitro dissolution testing by fabricated disintegration apparatus, texture analysis, etc. The optimization statistics showed that on decreasing the amount of gum, in- vitro drug release increases and hardness decreases. The optimized batch MCG-2 of Promethazine MCG showed 92.34 ± 0.92% of drug release, whereas for marketed formulation (Phenergan®-25 mg) drug release value was 86.19 ± 1.88%. Results provided evidence that PMZ MCGs could be a better alternative to conventional tablet formulations with improved drug release, palatability and texture.
运动病又称晕动病,是一种视觉感知的运动与前庭系统感知的运动之间存在差异的情况。恶心、呕吐、头晕、疲劳和头痛是运动病的最常见症状。本研究主要集中在通过包合络合方法对盐酸异丙嗪(PMZ)进行味觉掩蔽,以直接可压缩胶基 HIG®为基础开发咀嚼胶形式的配方,并对其质量和性能进行测试。通过β-环糊精(β-CD)作为味觉掩蔽剂,制备了 PMZ-环糊精络合物的不同摩尔比(1:1、1:2、1:3 和 1:4)。通过傅里叶变换红外光谱(FTIR)、差示扫描量热法(DSC)、包封效率(%)、药物产率(%)和电子舌味觉评价对这些络合物进行评价。优化比例进一步通过扫描电子显微镜(SEM)和 X 射线衍射(XRD)等复杂分析技术进行评估。采用中心复合设计(CCD)(3^2)研究独立变量(胶-X 的量和增塑剂-X 的量)对依赖变量(%CDRY 和硬度 Y)的影响。对制备的口香糖进行药物含量、感官特性、通过自制崩解装置的体外溶出度测试、质地分析等评价。优化统计数据表明,随着胶用量的减少,体外药物释放增加,硬度降低。优化后的 PMZ MCG 批 MCG-2 显示 92.34±0.92%的药物释放,而市售制剂(Phenergan®-25 mg)的药物释放值为 86.19±1.88%。结果表明,PMZ MCG 可替代传统片剂制剂,具有改善的药物释放、口感和质地。
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