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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.
Introduction
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, 25°C) 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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