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Method of promoting cervical and vaginal secretions

A cervical and vaginal technology, applied in the directions of medical preparations, pharmaceutical formulations, organic active ingredients, etc. containing active ingredients, can solve the problems of danger and poor vaginal drying effect, etc.

Inactive Publication Date: 2002-05-08
INSPIRE PHARMA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0008] Because current treatments for vaginal dryness are ineffective and dangerous, medical researchers have developed alternative treatments

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0110] Example 1: Short circuit in vitro (I sc ) Determination

[0111] Through in vitro evaluation (the method is to administer UTP to tissue culture so that the UTP concentration on the mucosa reaches approximately 10 -7 To 10 -1 Mol / L), the compound UTP was found to be P2Y in cervical and vaginal tissue preparations 2 And / or P2Y 4 A potent agonist of purinergic receptors (Rojanasakul, Y. et al., Pharm. Res. 9: 1029-34 (1992); Bechgaard, E., et al., Int. J. Pharm. 106: 237-242 ( 1994); Gipson, I., et al., Biol. Reprod. 56:999-1011 (1997)). Specifically, ovariectomized female New Zealand white rabbit albino bodies were sacrificed, and vaginal tissues were taken out. Fix the tissue on the support ring and clamp it in the Ussing chamber. Measure the I flowing from the tissue epithelial side to the chorionic side sc . About half of this current value corresponds to chloride moving through the membrane, so this is an accurate measure of the corresponding fluid movement.

Embodiment 2

[0112] Example 2: Using non-isotopic in situ hybridization to determine P2Y in monkey endocervical and vaginal epithelial tissues 2 Cell location of nucleotide receptor gene expression

[0113] organization. The research organization was obtained from Tulane Regional Primate Research Center (Covington, LA). The tissues included in the study are vagina and cervix. The tissue taken out immediately after death of the 3.25-year-old Indian rhesus monkey was quickly frozen in O.C.T. embedding medium. Frozen tissues are shipped overnight on dry ice and stored at -80°C before cryosectioning. The tissue was cut into 5 micron sections and fixed on a microscope slide for hematoxylin and eosin (H&E) staining, Alcian blue / periodic acid transfer (AB / PAS) staining and in situ hybridization (ISH).

[0114] Evaluation of tissue sections. H&E stained tissue sections were prepared to evaluate the quality and orientation of the studied tissues. H&E slide inspection showed that all tissues are suitabl...

Embodiment 3

[0119] Example 3. P2Y 2 Effects of agonists on the health of vaginal mucosa in ovariectomized rabbits

[0120] The purpose of this experiment is to study U 2 P 4 And dCP 4 The effect of U on the health of the vaginal mucosa was evaluated by clinical and pathological indicators in a female animal model under the condition of removing estrogen and estrogen replacement.

[0121] Evaluation

[0122] Daily evaluation. According to Hubbard et al. (Lab Anim. Sci. 47: 36-39 (1997); Bachman et al., (Clin. Pract. Sexual 8: 12-17 (1992)), by one hour after daily administration The vaginal pH, vaginal lubricity and vaginal stain were measured at the same time to evaluate the health of the mucous membrane. The baseline measurement of vaginal pH was recorded with a digital pH meter (Sandhill Scientific). The vaginal lubricity was evaluated with a specially designed tampon weighed in advance, and Fixation, staining, and visual inspection by a pathologist to evaluate vaginal stains.

[0123] Peri...

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PUM

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Abstract

The present invention provides a method of stimulating cervical and vaginal secretions in a mammal by treatment with P2Y2, and / or P2Y4 purinergic receptor agonists. Treatment of vaginal dryness associated with menopause, chemotherapy, and various disease states as well as the treatment of vulvar pain is discussed. Suitable purinergic receptor agonists include nucleotide triphosphates such as uridine 5-triphosphate, cytidine 5'-triphosphate and adenosine 5'-triphosphate; dinucleotide polyphosphates such as P<1>, P<4>-di(uridine-5') tetraphosphate; and their analogs. These purinergic receptor agonists are useful in stimulating cervical and vaginal secretions and treating vaginal dryness in mammals.

Description

Background of the invention [0001] The mucus that covers the surface of the female reproductive tract is important in its defense and reproductive functions. Mucus gel is mainly secreted by the epithelium in the cervix. It provides a barrier to the penetration of sperm and pathogens into the uterine mucosa, and is a protective covering of the vaginal epithelium. The hydration of vagina and cervical mucus prevents atrophy, provides lubrication during intercourse, helps surface defense against pathogens, and mediates sperm entry into the uterus (see Gipson IK, et al., Biology of Reproduction, 60, 58-64 (1999) ). [0002] The vaginal and ectocervix epithelium are squamous epithelium (similar to skin) without ciliated cells. The vaginal epithelium falls off at certain stages of the menstrual cycle. The lower endocervical epithelium contains submucosal glands composed of columnar epithelial cells that secrete mucin, but it does not have ciliated cells. The inner lining of the upper cer...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07H19/10A61K31/00A61K31/7042A61K31/7052A61K31/7064A61K31/7068A61K31/7072A61K31/7076A61K31/708A61K31/7084A61P15/02C07H19/20C07H19/207C07H21/00
CPCA61K31/00C07H21/00A61P15/02A61K31/7064
Inventor W·彭德格斯特S·R·谢弗D·J·德鲁兹J·L·赖德奥特
Owner INSPIRE PHARMA
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