Vaginal progesterone tablet

Details Vaginal progesterone tablet Vaginal progesterone tablet

1988-08-30

1992-05-26

Page, Thurman K.

Drug, bio-affecting and body treating compositions

Preparations characterized by special physical form

Implant or insert

424430, 424432, 424434, 424470, 424469, 514843, 514935, 514967, 514177, 514777, A61K 902, A61F 1300

Patent

active

051166194

ABSTRACT:
A vaginal progesterone suppository is provided in the form of a tablet which delivers biologically effective amounts of progesterone for at least about 48 hours, and blood amounts above basal levels for 72 hours. The tablet is formulated to preferably have a hardness on its edge of 8-13 kg, and disintegrates from its surface to form a milky suspension in 6-8 hours after it is inserted in the vaginal vault. The tablet contains, by weight, about 13-20% progesterone, 65-85% lactose, 2-10% corn starch paste binder, 3-10% corn starch disintegrant, and 0.1-0.9% magnesium stearate as a lubricant. The ratio by weight of progesterone to lactose is preferably 1:6, and the ratio of starch paste binder to starch disintegrant is preferably 1:1. This dosage form is an effective treatment for many progesterone deficiency conditions, and provides enhanced bioavailability.

REFERENCES:
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patent: 4585782 (1986-04-01), Plempel et al.
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patent: 4650665 (1987-03-01), Kronenthal et al.
patent: 4814183 (1989-03-01), Zentner
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Fulper, L. D., et al., "Comparison of Serum Progesterone Levels In Dogs After Administration of Progesterone By Vaginal Tablet and Vaginal Suppositories", AM.J. Obstet. Gynecol., 156:253-256 (1987).
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Lebhertz, T. B., et al., "A Comparison of a Three-Day and Seven-Day Clotrimazole Regimen for Vulvovaginal Candidiasis", (citation currently unavailable, but will be provided upon request).
Meyers, E. R., et al., "Serum Progesterone Levels Following Vaginal Administration of Progesterone During the Luteal Phase", Fertility and Sterility, 47-1:71-75 (1987).
Meirik, O., et al., "Plasma Concentrations of Chloroquinaldol (Sterosan.RTM.) after Administration of a Vaginal Tablet", Gynecol. Obstet. Invest., 9:166-169 (1978).
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Excerpt from the U.S. Pharmacoepeia (XXI) p. 1242.
Data sheets listing a variety of abstracts located during a computer search on the present invention.
Morgan, L. R., et al., "A Vaginal Pregesterone Tablet: Its Use in Amenorrhea and Dysfunctional Uterine Bleeding", (Abstract) The Journal of Clinical Pharmacology, Sep. 1987 Issue, vol. 27, No. 9.

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