Sustained-release progesterone vaginal suppositories 1--development of sustained-release granule--.
Progesterone (P) is an important hormone for the establishment of pregnancy, and its administration is useful for luteal insufficiency. Considering the problems of commercially available oral and injection drugs, hospital-formulated vaginal suppositories are clinically used. However, since the half-life of P suppositories is short, it is difficult to maintain its constant blood concentration. To sustain drug efficacy and prevent side-effects, we are attempting to develop sustained-release suppositories by examining the degree of sustained-release of active ingredients. In this study, we examined the combinations of granulation methods and release systems for the preparation of sustained-release granules of P, and produced 13 types of sustained-release granules. We also examined the diameter, content, and dissolution of each type of granules, and confirmed that the sustained-release of all types of granules was satisfactory. Among the sustained-release granules, we selected granules with a content and a degree of sustained-release suitable for sustained-release suppositories.
Nakayama
Ayako
A
Department of Pharmacy, Hoshigaoka Maternity Hospital, Nagoya, Japan. hoshiya@toukeikai.com
Sunada
Hisakazu
H
Okamoto
Hirokazu
H
Furuhashi
Kaoru
K
Ohno
Yukiko
Y
Ito
Mikio
M
D000180:Acrylic Resins; D002626:Chemistry, Pharmaceutical; D003692:Delayed-Action Preparations; D004339:Drug Compounding; D005079:Excipients; D010316:Particle Size; D011208:Powders; D011374:Progesterone / Q000008:administration & dosage*; D012967:Sodium Dodecyl Sulfate; D012995:Solubility; D013488:Suppositories
D000180:Acrylic Resins; D003692:Delayed-Action Preparations; D005079:Excipients; D011208:Powders; D013488:Suppositories; C050528:Eudragit RS; D012967:Sodium Dodecyl Sulfate; D011374:Progesterone