Purpose

Dextromethorphan (DXM) is exceptionally bitter, yet the most widely used antitussive agents worldwide. It belongs to BCS class-II of pharmaceutical agents because of its poor water solubility; this is why it is only available in its hydrobromide salt form either in liquid or in solid formulations in the market. This water-soluble salt of the drug releases its content to a greater extent in salivary pH, which increases bitterness perception. This study aimed at designing a more palatable chocolate formulation of DXM, which releases the minimum drug in salivary pH.

Methodology

DXM nano-emulsion prepared using lecithin and Tween-80 was dried and incorporated in placebo chocolates, poured into silicon molds, and refrigerated to have medicated chocolates.

Results

Medicated chocolates had an average weight of 1.757 ± 0.006 g, a thickness of 7.606 ± 0.0175 mm, and hardness of 2.007 ± 0.0102 Kp. The average drug content was 98.707 ± 0.012%. The average particle size of optimized nano-emulsion was 101.145 ± 2.906 nm with an encapsulation efficiency of 75.866 ± 0.543%. Scanning electron microscopy (SEM) revealed the spherical structure of nanoparticles. Fourier transform infrared (FTIR) spectra and differential scanning calorimetry (DSC) thermograms showed no drug-excipient interaction, and X-ray diffraction (XRD) analysis confirmed the amorphous form of the drug in nano-emulsion. The minimal drug was released at salivary pH from chocolate formulation compared to the standard. The Human Panel taste evaluation confirmed better palatability of chocolate than marketed syrup and tablet formulations of DXM.

Conclusion

The novel medicated chocolate of DXM was proven to have a better palatability profile than its marketed formulations.

中文翻译：

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右美沙芬新型口感药用巧克力的设计与优化

目的

右美沙芬（Dextromethorphan，DXM）异常苦涩，但却是全球使用最广泛的镇咳药。由于其水溶性差，属于BCS II类药剂。这就是为什么它只能以氢溴酸盐的形式在市场上以液体或固体制剂形式获得的原因。药物的这种水溶性盐在唾液pH值中更大程度地释放其含量，从而增加了苦味感。这项研究旨在设计一种更美味的DXM巧克力配方，该配方在唾液pH中释放的药物最少。

方法

将使用卵磷脂和Tween-80制备的DXM纳米乳液干燥，并掺入安慰剂巧克力中，倒入硅模中，然后冷藏制成含药巧克力。

结果

药用巧克力的平均重量为1.757±0.006 g，厚度为7.606±0.0175 mm，硬度为2.007±0.0102 Kp。平均药物含量为98.707±0.012％。优化后的纳米乳液的平均粒径为101.145±2.906 nm，包封效率为75.866±0.543％。扫描电子显微镜（SEM）揭示了纳米颗粒的球形结构。傅里叶变换红外（FTIR）光谱和差示扫描量热法（DSC）热谱图显示没有药物-赋形剂相互作用，X射线衍射（XRD）分析证实了纳米乳液中药物的无定形形式。与标准品相比，巧克力配方在唾液pH值下释放的药物极少。人类专家小组的口味评估证实，巧克力的可口性比市售的DXM糖浆和片剂更佳。

结论

事实证明，DXM的新型药用巧克力比其市售配方具有更好的适口性。