Abstract
Purpose: To optimize and formulate promethazine theoclate fast-dissolving tablets that offer a suitable approach to the treatment of nausea and vomiting. Method: The solubility of promethazine theoclate was increased by formulating it as a fast-dissolving tablet containing β-cyclodextrin, crospovidone, and camphor, using direct compression method. A 33 full factorial design was used to investigate the combined influence of three independent variables - amounts of camphor, crospovidone and β-cyclodextrin - on disintegration time, friability and drug release after 5 min. Result: The optimization study, involving multiple regression analysis, revealed that optimum amounts of camphor, crospovidone and β-cyclodextrin gave a rapidly disintegrating/dissolving tablet. A checkpoint batch was also prepared to verify the validity of the evolved mathematical model. The optimized tablet should be prepared with an optimum amount of β-cyclodextrin (3.0 mg), camphor (3.29 mg) and crospovidone (2.61 mg) which disintegrated in 30 s, with a friability of 0.60 % and drug release of 89 % in 5 min. Conclusion: The optimized approach aided both the formulation of fast-dissolving theoclate tablets and the understanding of the effect of formulation processing variables on the development of the formulation.Keywords: Fast-dissolving tablet, 33 Factorial design, Promethazine theoclate, Optmization studies.
Highlights
Retention of an administered antiemetic oral dose and its subsequent absorption during therapy is critically affected by recurrent emesis, a process coordinated by the vomiting centre in the lateral reticular formation of the medulla receiving inputs from the chemoreceptor trigger zone and other neural sites [1]
The objective of the present work was to develop fast dissolving tablets of promethazine theoclate based on a small number of experimental runs [12]
A factorial design was employed in order to systematically investigate the factors affecting the formulation and optimize the fast dissolving tablet for a disintegration time of 30 s, friability of < 0.6 %, and drug release of up to 90 %
Summary
Retention of an administered antiemetic oral dose and its subsequent absorption during therapy is critically affected by recurrent emesis, a process coordinated by the vomiting centre in the lateral reticular formation of the medulla receiving inputs from the chemoreceptor trigger zone and other neural sites [1]. For drug with low bioavailability, partial drug loss by emesis will result in therapeutic failure. One such antiemetic drug, promethazine theoclate, after oral dosing, undergoes extensive gastric and first pass effect. Promethazine theoclate, after oral dosing, undergoes extensive gastric and first pass effect This results in low bioavailability which, will not minimize the rate of vomiting [3]
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