Formulation and Characterization of Fast Dissolving Tablet Containing Promethazine Theoclate Solid Dispersion with PEG 4000

Shailesh Sharma, G.D. Gupta

Abstract: This article investigates enhancement of the dissolution profile of promethazine Theoclate using solid dispersion with PEG 4000. The article also describes the preparation of fast-dissolving tablets of promethazine Theoclate by using a optimized amount of superdisintegrants. A phase solubility method was used to evaluate the effect of various water-soluble polymers on aqueous solubility of promethazine Theoclate. Polyvinyl pyrrolidone (PEG 4000) was selected and solid dispersions were prepared by the method of fusing. Dissolution studies using the USP paddle method were performed for solid dispersions of promethazine Theoclate. Infrared (IR) spectroscopy, differential scanning calorimetry (DSC), and x-ray diffractometry (XRD) were performed to identify the physicochemical interaction between drug and carrier, hence its effect on dissolution. Tablets were formulated containing solid dispersion products and compared with commercial products. IR spectroscopy, XRD, and DSC showed no change in the crystal structure of promethazine Theoclate. Dissolution of promethazine Theoclate improved significantly in solid dispersion products (< 85% in 5 minutes). Tablets containing solid dispersion exhibited better dissolution profile than commercial tablets. Thus, the solid dispersion technique can be successfully used for improvement of dissolution of promethazine Theoclate.

Promethazine Theoclate, Dimethyl (1-methyl-2-phenothiazin-10-ylethyl)amine salt of 8-chlorotheophylline, a novel Antihistaminic, with antimuscarinic and some serotonin-antagonist properties that is indicated for their antiemetic action in the prevention and treatment of nausea and vomiting in conditions such as motion sickness, drug-induced vomiting, and postoperative vomiting. Although it has excellent oral bioavailability (25%), its poor aqueous solubility (10 μg/mL, 25C) makes its absorption dissolution rate limited and thus delays onset of action. Solid dispersion, which was introduced in the early 1970s, is essentially a multicomponent system, having drug dispersed in and around hydrophilic carrier(s). Solid dispersion technique has been used for improvement of dissolution characteristics and bioavailability of poorly aqueous-soluble drugs. Polyvinylpyrrolidone (PEG 4000) has been used for the preparation of solid dispersion as a component of the binary system.


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