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Methods and formulations for modulating the human sexual response

A preparation and tablet technology, which is applied in the field of regulating human sexual response and preparation, can solve problems such as danger, infection, and affecting the spontaneity of sexual behavior, and achieve the effect of convenient preparation and method and reducing side effects

Inactive Publication Date: 2010-09-01
REPROS THERAPEUTICS
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Obvious deficits include: pain, risk of infection, inconvenience, and interference with sexual spontaneity
[0016] Sonda et al. (J.Sex & Marital Ther.16(1):15-21(year)) reported that the intake of yohimbine could subjectively improve the erectile ability of 38% of impotent men treated, but only 5% of treated patients reported complete satisfaction

Method used

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  • Methods and formulations for modulating the human sexual response
  • Methods and formulations for modulating the human sexual response
  • Methods and formulations for modulating the human sexual response

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0050] Example 1 discloses a fast dissolving formulation for oral administration of a vasodilator. Example 2 discloses the bioavailability of phentolamine mesylate when administered in a fast dissolving oral formulation. Example 3 discloses the effect of phentolamine mesylate on the erectile capacity of men when administered with a fast-dissolving oral formulation. Example 4 discloses other vasoactive agents that can be used to modulate sexual response in humans. Example 5 discloses the method of the present invention for modulating female erectile response.

[0051] Example 1

[0052] Oral fast-dissolving formulations of vasodilators

[0053] The present invention relates to fast-dissolving oral formulations for the rapid delivery of vasodilators into the circulatory system to enable rapid (on demand) initiation of reactive stimulation to improve erectile capacity. The invention also includes other oral formulations for "on demand" improvement of erectile capacity to sexu...

Embodiment 2

[0072] Bioavailability of tolamine mesylate as a fast-dissolving oral formulation

[0073] A pilot study was conducted to correlate the bioavailability of a single 40 mg dose of phentolamine mesylate administered as an oral fast-dissolving tablet with the bioavailability of phentolamine mesylate administered orally as a standard release hard tablet Compare.

[0074] Fast-dissolving tablets containing 40 mg of phentolamine mesylate were formulated as shown in Table 1. Standard release hard tablets containing 40 mg of phentolamine mesylate were prepared as follows:

[0075] Table 2

[0076] standard release hard tablet

[0077] mg / tablet

[0078] Phentolamine Mesylate, USP 40

[0079] Silica, NF 8

[0080] Stearic acid, NF 4

[0081] Dicalcium Phosphate Dibasic, USP 228

[0082] Microcrystalline Cellulose, NF 120

[0083] Total sheet weight 400

[0084] Tablets are made by direct compression. The physical characteristics of the tablets made in Table 2 included a har...

Embodiment 3

[0168] Effects of fast-dissolving oral preparation of phentolamine mesylate on male erectile ability

[0169] In order to examine the effect of phentolamine mesylate instant oral preparation on erectile ability, a single-blind experiment was carried out.

[0170] All patients had impotence of organic etiology. Patients participating in the trial were selected on the basis of medical history and physical examination results, and all had impotence lasting less than 3-4 years. Two tablets were administered to each patient: a fast-dissolving tablet containing 40 mg of phentolamine mesylate (see Table 1), and a placebo tablet without phentolamine mesylate.

[0171] Patients are asked to take one tablet 20-30 minutes before intercourse. One or more days after taking the first tablet, have the patient repeat the process with the second tablet.

[0172] Advise patients not to drink alcohol before taking the tablet and tell them not to expect an erection without sexual stimulation. ...

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Abstract

The invention is directed to improved methods for modulating the human sexual response by orally administering a vasodilator to the blood circulation, thereby modulating the sexual response on demand.

Description

[0001] This case is a divisional application, and its parent case is an application with an application date of April 26, 1996, an application number of 96194822.1, and an invention titled "Method and Preparation for Regulating Human Sexual Response". technical field [0002] The present application relates to the administration of improved formulations of vasodilators in the human blood circulation to modulate the human sexual response as desired. Background technique [0003] The human sexual response, both male and female, is the result of a complex interplay of psychological, hormonal, and other physiological influences. An important aspect of the human sexual response shared by both men and women is the erectile response, itself a result of the interaction between the autonomic, endocrine, and circulatory systems. [0004] Failure to respond to an erection is most common in men and is therefore called impotence. Impotence is the inability of a man to achieve an erectio...

Claims

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Application Information

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IPC IPC(8): A61K9/20A61K9/46A61K9/14A61K9/48A61K9/10A61K31/417A61K47/36A61K47/38A61K47/32A61P15/10A61P15/00A61K31/00A61K31/135A61K31/137A61K31/138A61K31/21A61K31/222A61K31/277A61K31/341A61K31/415A61K31/4174A61K31/4406A61K31/455A61K31/472A61K31/475A61K31/485A61K31/55A61K45/00A61P13/02
CPCA61K31/472A61K9/2054A61K31/475A61K31/138A61K31/00A61K31/4406A61K31/341A61K31/417A61K31/222A61K31/21A61K31/277A61K31/4174A61P13/02A61P15/00A61P15/10A61P5/24A61K31/135A61K31/22
Inventor F·罗雷
Owner REPROS THERAPEUTICS
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