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Wisam M. Daoud, Mohammed A. Rajab and Nawal A. Rajab*


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<0.05) of drug release for the selected hollow type formula in the comparison with the conventional one (52% drug release). The obtained results demonstrated that the effect of storage on the suppositories prepared from PEG 400:4000(70:30) cause slight increase in melting time and hardness (physical properties) and slight increase in release rate of drug from suppository base. On the other hand, clinical study gave very effective and comfortable contraceptive properties of the prepared propranolol HCl vaginal hollow suppositories. Conclusion: It can be concluded that propranolol HCl can be prepared as a suitable vaginal hollow type suppositories for contraceptive effect through rapid release process of drug and good clinical response.

Keywords: propranolol HCl, hollow type suppositories, contraception, vaginal suppositories.

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