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Design and Optimization of Novel Taste-Masked Medicated Chocolates of Dextromethorphan with In vitro and In vivo Taste Evaluation

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Abstract

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.

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Acknowledgments

We highly acknowledge Mr. Muhammad Mohsin, Prof. Dr. Shahiq-Uz-Zaman, and Dr. Humaira from the Riphah Institute of Pharmaceutical Sciences for their support and lab facilities. We also endorse Abbasi Chemicals Lahore, Paramount Pharmaceuticals, Islamabad, for their chemicals as gift samples used in this project. We are thankful to Dr. Zia-Ur-Rahman and Miss. Humaira Khalid from Pakistan Council of Scientific and Industrial Research for Karl Fischer Analysis.

Funding

We express our thanks to the office of the Dean, Biological Sciences, Quaid-i-Azam University, who funded this project under URF (University Research Fund; NO. DFBS/2019-3693).

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Authors and Affiliations

  1. Department of Pharmacy, Quaid-i-Azam University, Islamabad, Pakistan

    Rahat Fatima Naqvi, Ahmad Khan & Muhammad Farooq Umer

  2. Drug Regulatory Authority of Pakistan, Ministry of National Regulations and Services Islamabad, Islamabad, Pakistan

    Obaidullah Malik

  3. Faculty of Pharmacy, University of Balochistan, Quetta, Pakistan

    Nisar Ahmad Shahwani

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  1. Rahat Fatima Naqvi
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Correspondence to Ahmad Khan.

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Naqvi, R.F., Khan, A., Umer, M.F. et al. Design and Optimization of Novel Taste-Masked Medicated Chocolates of Dextromethorphan with In vitro and In vivo Taste Evaluation. J Pharm Innov 17, 376–390 (2022). https://doi.org/10.1007/s12247-020-09511-8

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