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Article

Bimodal Release Two-In-One Clonazepam Matrix Lozenge Tablets for Managing Anxiety-Related Disorders: Formulation, Optimization and In Vivo Evaluation

1
Department of Pharmaceutics and Industrial Pharmacy, Faculty of Pharmacy, Zagazig University, Zagazig 44519, Egypt
2
Institute of Medicinal and Pharmaceutical Chemistry, Technische Universität Braunschweig, 38106 Braunschweig, Germany
3
Natural and Medical Sciences Research Center, University of Nizwa, P.O. Box 33, Birkat Al Mauz, Nizwa 616, Oman
4
Pharmaceutical Analytical Chemistry Department, Faculty of Pharmacy, Port-Said University, Port Fuad 42526, Egypt
*
Author to whom correspondence should be addressed.
These authors contributed equally to this work.
Academic Editor: Antoni Camins Espuny
Sci. Pharm. 2022, 90(3), 43; https://doi.org/10.3390/scipharm90030043
Received: 25 April 2022 / Revised: 30 June 2022 / Accepted: 15 July 2022 / Published: 21 July 2022
Clonazepam (CLZ), an antipsychotic drug reported for its efficiency in managing anxiety-related disorders, is being marketed only as conventional tablets. Some patients have abstention to swallow the conventional tablets; therefore, the proposed study was aimed at developing a buccal lozenge tablet by direct compression of two types of optimized granules. Conazepam’s water solubility was first enhanced by a solid dispersion technique for a fast and better dissolution of type 1 granules, while the impact of gelling polymers was investigated on controlled-release type 2 granules. The optimized formulae met the acceptable pharmacopeial limits for tablets’ evaluation. A differential scanning calorimetry study revealed the compatibility between the drug and used excipients. All formulae gave a burst release of CLZ in the first hour of investigation, followed by a sustained release over 24 h. The formula that showed the highest prolonged in vitro release (99.0 + 0.1%), following the Higuchi diffusion model (R2 = 0.99), was then selected for further study. The formula succeeded in controlling the induced stress in a rat model with a significant impact on the behavioral tests throughout the experiment. The results were further confirmed by a pharmacokinetic study that showed a significant increase in Cmax, Tmax, and AUC (1.5, 2, and 3.9 folds), respectively, compared to oral suspension. The newly proposed delivery system has proven a better efficacy with a reduced dosing frequency. View Full-Text
Keywords: Clonazepam; buccal lozenge tablets; bimodal behavior; pharmacokinetic Clonazepam; buccal lozenge tablets; bimodal behavior; pharmacokinetic
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MDPI and ACS Style

Gomaa, E.; El Deeb, S.; Ibrahim, A.E.; Faisal, M.M. Bimodal Release Two-In-One Clonazepam Matrix Lozenge Tablets for Managing Anxiety-Related Disorders: Formulation, Optimization and In Vivo Evaluation. Sci. Pharm. 2022, 90, 43. https://doi.org/10.3390/scipharm90030043

AMA Style

Gomaa E, El Deeb S, Ibrahim AE, Faisal MM. Bimodal Release Two-In-One Clonazepam Matrix Lozenge Tablets for Managing Anxiety-Related Disorders: Formulation, Optimization and In Vivo Evaluation. Scientia Pharmaceutica. 2022; 90(3):43. https://doi.org/10.3390/scipharm90030043

Chicago/Turabian Style

Gomaa, Eman, Sami El Deeb, Adel Ehab Ibrahim, and Mennatullah M. Faisal. 2022. "Bimodal Release Two-In-One Clonazepam Matrix Lozenge Tablets for Managing Anxiety-Related Disorders: Formulation, Optimization and In Vivo Evaluation" Scientia Pharmaceutica 90, no. 3: 43. https://doi.org/10.3390/scipharm90030043

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