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Device and method for treatment of dysmenorrhea

A medicament and a selected technology are applied in the field of devices for treating dysmenorrhea, and can solve the problems of obtaining analgesics, restricting administration, failing to successfully relieve dysmenorrhea symptoms, and the like

Inactive Publication Date: 2000-08-16
UNIVERSITY OF MINNESOTA DULUTH
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

In general, systemic administration of analgesics to patients via the oral route has not been successful in alleviating dysmenorrhea symptoms in many women, and dosing is often limited by side effects
We believe this failure is due to the inability to obtain effective dose levels of analgesics in the uterine muscle

Method used

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  • Device and method for treatment of dysmenorrhea
  • Device and method for treatment of dysmenorrhea
  • Device and method for treatment of dysmenorrhea

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0098] Preparation of Verapamil Vaginal Suppository

[0099] The dose of verapamil (Sigma / Aldrich, St. Louis, MO) was 0.15-0.6 mg / kg body weight. Radiolabeled verapamil (4-7 μCi) was added to the unlabeled compound. Pessaries were formulated and prepared 24 hours prior to each test. The three basic components used in suppositories are: SUPPOCIRE® AS2 (Gattefosse, Westwood, NJ) (75% by weight); hydroxypropyl methylcellulose (e.g. METHOCEL® K, HPMC K15M) (Michigan Dow Chemical Company, Midland) (10% by weight), a mucoadhesive; and TRANSCUTOL(R) (Gattefosse) (15% by weight). To make 8 suppositories, weigh 4.5g SUPPOCIRE, 600mg HPMC, 900mg TRANSCUTOL, calculate the dose of the drug, and its labeled counterpart. The SUPPOCIRE was melted in a single-use 100ml polypropylene beaker suspended in water at 50°C. The solution was stirred until completely molten. Then HPMC and TRANSCUTL were added and mixed. Finally, unlabeled drug and radiolabeled drug are added to ...

Embodiment 2

[0101] Preparation of indomethacin vaginal suppository

[0102] 14 C-Indomethacin was obtained from Amersham Life Science, Arlington Hts., IL. The dose of frozen indomethacin (Sigma / Aldrich) was 0.2 mg / kg body weight. Labeled indomethacin (4-7 μCi) was added to the cooled compound. All other steps in the preparation of indomethacin suppositories are the same as in Example 1, but indomethacin is used instead of verapamil.

Embodiment 3

[0104] Pharmacokinetic test of verapamil

[0105] 3 H-Verapamil was obtained from Dupont / NEN (Boston, MA). Cold verapamil (Sigma / Aldrich, St. Louis, Missouri) (0.15–0.6 mg / kg body weight, i.v.) was dissolved in 0.5 ml of dimethylsulfoxide (Syntex, West Des Moines, IA) prior to intravenous injection . Labeled verapamil (4-7 μCi) was then added to the cold compound prior to iv injection.

[0106] Female New Zealand White rabbits weighing 2.8-3.5 kg were obtained from Myrtle Rabbitry (Thompson Station, TN). Rabbits were housed in a National Institute of Health (NIH) approved facility and acclimatized for at least 48 hours prior to each test.

[0107] Pharmacokinetic studies of the drug were performed using two models of intravenous and intravaginal administration. In the first series of experiments, the intravenous route was used to determine the initial half-life of the test compound. In a second series of experiments, intravenous and intravaginal administra...

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PUM

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Abstract

Methods, devices, and compositions for treatment of dysmenorrhea comprise an intravaginal drug delivery system containing an appropriate pharmaceutical agent incorporated into a pharmaceutically acceptable carrier whereby the pharmaceutical agent is released into the vagina and absorbed through the vaginal mucosa to provide relief of dysmenorrhea. The drug delivery system can be a tampon device (42), vaginal ring, pessary, tablet, suppository, vaginal sponge, bioadhesive tablet, bioadhesive microparticle, cream lotion, foam, ointment, paste solution, or gel. The system delivers a higher concentration to the muscle of the uterus, the primary site for the dyskinetic muscle contraction, which is the pathophysiologic cause of dysmenorrhea.

Description

field of invention [0001] The present invention relates to devices, methods and compositions for treating dysmenorrhea by vaginally administering therapeutic and / or relieving drugs to the uterus. Background of the invention [0002] Primary or secondary dysmenorrhea are painful uterine cramps that occur during menstruation. In secondary dysmenorrhea, visible pelvic damage can explain such pain, but primary dysmenorrhea is caused solely by biochemical imbalances. Primary dysmenorrhea affects 50 percent of postpubertal women and is estimated to cost an estimated 600 million hours of work or more than $2 billion annually during periods of severe dysmenorrhea. Therefore, effective, simple and safe treatment of primary dysmenorrhea within a few days of menstrual period can not only improve the quality of life of dysmenorrhea patients, but also produce positive economic benefits. [0003] The pain of dysmenorrhea originates from the uterus. Typically, syst...

Claims

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Application Information

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IPC IPC(8): A61F6/08A61F13/20A61K9/00A61M31/00A61K9/02A61K9/08A61K31/192A61K31/21A61K31/27A61K31/405A61K45/00A61P15/00
CPCA61K9/0036A61F6/08A61K9/0034A61P15/00A61P15/02
Inventor 唐纳德·C·哈里森詹姆士·H·廖沃尔夫冈·A·里切尔罗杰·A·斯特恩
Owner UNIVERSITY OF MINNESOTA DULUTH
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