PREPARATION, IN-VITRO CHARACTERIZATION, AND CLINICAL STUDY OF PROPRANOLOL HCl VAGINAL CONTRACEPTIVE HOLLOW-TYPE SUPPOSITORIES
Wisam M. Daoud, Mohammed A. Rajab and Nawal A. Rajab*
Abstract
Objective: Recently discovered that Propranolol Hydrochloride is a
potent inhibitor of human sperm motility and can be used as a
contraceptive drug through local anaesthetic or membrane stabilizing
activity. The aim of this study is to prepare Propranolol Hydrochloride
as vaginal hollow suppositories by using different bases. Method:
Eight formulas of hollow suppositories were prepared and the
influence of different hydrophilic (PEG) and lipophilic (Witepsol H
37) base on drug release and the physical properties were evaluated.
On the other hand, the most appropriate hollow type formula was
compared to the conventional prepared suppositories from the same
base of. The selected formula was stored at 4°C and 28°C for 30 days to study the effect of
storage time and storage temperature on the in vitro drug release and the physical properties.
In clinical study the selected prepared Propranolol Hydrochloride vaginal hollow
suppositories formula was given to ten healthy women (25-30 years) as contraceptive way for
determination its clinical activity. Results: the results showed that F7 which contain PEG
400:4000(70:30) gave the best drug release about 99% with accepted physicochemical
properties. In addition to that a significant increase (P
Keywords: propranolol HCl, hollow type suppositories, contraception, vaginal suppositories.
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