Design and Optimization of Novel Taste-Masked Medicated Chocolates of Dextromethorphan with In vitro and In vivo Taste E
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ORIGINAL ARTICLE
Design and Optimization of Novel Taste-Masked Medicated Chocolates of Dextromethorphan with In vitro and In vivo Taste Evaluation Rahat Fatima Naqvi 1
&
Ahmad Khan 1
&
Muhammad Farooq Umer 1 & Obaidullah Malik 2 & Nisar Ahmad Shahwani 3
Accepted: 19 October 2020 # Springer Science+Business Media, LLC, part of Springer Nature 2020
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 nanoemulsion. 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. Keywords Chocolate . Dextromethorphan . Cough . Taste-masking . Antitussive
Introduction Cough is the most common and least concerned presenting complaint worldwide [1, 2]. It is an important symptom
associated with various pulmonary as well as extrapulmonary diseases. Dextromethorphan (DXM), a well-known bitter antitussive agent, is a common ingredient of all cough and cold medicines currently available in the Pakistani market.
Supplementary Information The online version contains supplementary material available at https://doi.org/10.1007/s12247-02009511-8. * Ahmad Khan [email protected]
Nisar Ahmad Shahwani [email protected]
Rahat Fatima Naqvi [email protected]
1
Department of Pharmacy, Quaid-i-Azam University, Islamabad, Pakistan
Muhammad Farooq Umer [email protected]
2
Drug Regulatory Authority of Pakistan, Ministry of National Regulations and Services Islamabad, Islamabad, Pakistan
3
Faculty of Pharmac
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