Sustained-Release Progesterone Vaginal Suppositories 3<br/>—Development and Clinical Feasibility Testing—

Abstract

Although progesterone vaginal suppositories (hospital-formulated) are used for the treatment of infertility, their half-life is so short that multiple doses are required. In this study, we aimed to develop sustained-release vaginal suppositories suitable for clinical use which maintain an eŠective blood concentration by once-a-day treatment, and prepared 7 types of suppository containing the sustained-release progesterone tablets to characterize their sustained-release performance. We selected one candidate suppository among them, taking recovery rate, reproducibility, and hardness, as well as the sustained-release performance into consideration. The shell of the selected suppository is composed of VOSCO S-55 and progesterone for rapid release. The molded progesterone tablets for sustained release were embedded inside. The distribution of the weight and content of the suppository was limited, and the release rate of progesterone was signiˆcantly slower than that of a conventional progesterone suppository prepared in our hospital. The single-dose administration of the selected suppository toˆve healthy volunteers led to signiˆcant extension of the blood concentration. We also conˆrmed the rise of the basic value by multiple administration. The simulation comparison suggested that the blood progesterone concentration is controlled by once-a-day administration of the selected suppository better than twice-a-day administration of the conventional suppository. In conclusion, the sustained-release vaginal suppository prepared in this study was considered to be useful for clinical treatment.

Intravaginal administration of progesterone using a new technique for sustained drug release in goats

“…The high viscosity and retention property of the mixture of HM and silicon fluid formulated in this study resulted in slow release and absorption of P 4 in the vagina. In human medicine, vaginal P 4 suppositories or tablets are used for the treatment of infertility, and must be administered once or twice a day [ 22 , 23 ] due to their short half-life. Although more detailed studies in vitro and in vivo are necessary for clinical application, HM-based vaginal suppositories or tablets may allow a reduced frequency of administration in human as well as veterinary medicine.…”