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S-alkylisothiouronium derivatives for treating uterine hypercontractility disorders

A technique of uterine contraction and overpowering, applied in the direction of application, biocides, diseases, etc., can solve problems such as digestive system disorders and complications

Inactive Publication Date: 2010-12-15
BARKAN FARMA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

Although S-ethylisothiouronium bromide was found to be effective in reducing abnormal uterine bleeding and pelvic pain, it exerted a short-term effect with side effects such as digestive disturbances and complications

Method used

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  • S-alkylisothiouronium derivatives for treating uterine hypercontractility disorders
  • S-alkylisothiouronium derivatives for treating uterine hypercontractility disorders
  • S-alkylisothiouronium derivatives for treating uterine hypercontractility disorders

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0153] Effect of S-Ethylisothiourea Diethyl Phosphate on Abnormal Uterine Bleeding

[0154] Thirty-six women presenting with abnormal uterine bleeding were enrolled in the study. Each woman received one suppository (2 g 100mg of S-ethylisothiouronium diethylphosphate, the suppository base is obtained by esterification of hydrogenated palm oil and hydrogenated palm kernel oil), applied to the posterior vaginal fornix.

[0155] After administration of six suppositories of intravaginally applied S-ethylisothiouronium diethylphosphate (100 mg each), complete disappearance of pathological uterine bleeding was obtained in 87.8% of cases (31 patients).

[0156] Hemostasis was achieved over the course of an average of 40-58 hours from the start of treatment with S-ethylisothiouronium diethylphosphate in vaginal suppository form. The intensity of bleeding was moderately reduced in 5 patients (12.2%), but complete hemostasis was not achieved. The majority (94.4%) of the patients rep...

Embodiment 2

[0158] Effects of S-Ethylisothiourea Diethyl Phosphate on Pain in Rats

[0159] Studies were performed in Wistar male rats (210 g body weight). The experiment was carried out on 30 rats divided into 3 groups of 10 animals each. The presence of pain was determined using the tail test. This method is based on monitoring the reaction time of the commonly used tail withdrawal reflex due to thermal stimulation. First, the temperature (°C) at which the rat's tail was withdrawn was measured, thus identifying the level of heat that caused the pain. One hour later, rats were injected intraperitoneally with S-ethylisothiouronium diethylphosphate in 0.9% NaCl. One group (10 rats) was injected with 5 mg / kg body weight of S-ethylisothiouronium diethylphosphate, while the second and third groups (10 rats each) were injected with 10 mg / kg and 20 mg, respectively S-ethylisothiouronium diethylphosphate / kg body weight.

[0160] The results showed that the critical temperature for untreated...

Embodiment 3

[0166] Effect of S-Ethylisothiouronium Diethyl Phosphate on Primary and Secondary Dysmenorrhea

[0167] Vaginal suppositories containing S-ethylisothiouronium diethylphosphate (100 mg / day each) were applied to 28 women suffering from primary or induced dysmenorrhea. Twenty-four hours after starting the treatment, a significant decrease in the intensity of pain was observed in 60.7% of cases (17 patients), while complete disappearance of pain was noted in 11 patients (39.3%). Forty-eight hours after initiation of treatment, ie after administration of the second suppository containing S-ethylisothiouronium diethylphosphate, pain was completely resolved in all treated women.

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Abstract

The present invention relates to methods for treating uterine hypercontractility disorders. In particular, the present invention relates to methods for treating abnormal uterine bleeding and dysmenorrhea comprising administering to women suffering from such disorders a pharmaceutical composition comprising an S-alkylisothiouronium derivative.

Description

field of invention [0001] The present invention relates to methods for the treatment of uterine hypertonic conditions. In particular, the present invention relates to a method for treating abnormal uterine bleeding and dysmenorrhea comprising administering to a woman suffering from such conditions a pharmaceutical composition comprising an S-alkylisothiourea derivative. Background of the invention [0002] abnormal uterine bleeding [0003] Pathological or abnormal uterine bleeding includes metrorrhagia, menorrhagia and hypermenorrhea. The average blood loss in normal menstruation is about 30 ml over a period lasting an average of 5 days. If the blood loss exceeds 80ml, it is classified as pathological or abnormal. [0004] Metrorrhagia is defined as bleeding that may or may not be accompanied by pain and is not associated with menstruation or cycles. If it persists for more than 7 days, blood loss usually exceeds 80ml. [0005] Menorrhagia is menstruation, which may o...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A01N37/52A61K31/155
CPCA61K31/27A61P15/02
Inventor 拉斐尔·巴坎维克托·吉卡维伊
Owner BARKAN FARMA
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