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.
