Looking for breakthrough ideas for innovation challenges? Try Patsnap Eureka!

Apomorphine and sildenafil composition

A technology of apomorphine and composition, applied in the field of compositions for treating human sexual dysfunction, can solve problems such as death, improper disposal, hypertensive crisis and the like

Inactive Publication Date: 2002-05-22
PENTECH PHARMA
View PDF2 Cites 1 Cited by
  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

In particular, the combination of sildelafil citrate and organic nitrates can lead to hypertensive crisis and, in some patients, death, so administration of any form to those taking organic nitrates such as nitroglycerin Administration of this drug is inappropriate
In addition, the long-term effects of high doses of drugs containing sildiafil are unknown

Method used

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
View more

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0068] Example 1: Sublingual Tablets

[0069] This example illustrates the preparation of a sublingual (SL) tablet dosage form suitable for the simultaneous oral administration of apomorphine and sildeprafil.

[0070] Apomorphine Hydrochloride (mg)

Sildelafil (mg)

tablet#

2

15

10

2

25

10

2

35

10

4

35

5

6

35

5

[0071] This example illustrates the simultaneous oral administration of apomorphine and sildelafil in the form of sublingual (SL) tablets in 4 healthy volunteer patients, aged from 36 to 54 years, in an informal home trial.

[0072] The following tablets, sizes 1-6, were prepared containing the indicated amount of drug for sublingual (SL) or conventional (oral) administration as prescribed:

[0073] Tablet No. 1: Sublingual placebo.

[0074] Tablet No. 2: sublingual administration (2 mg)...

Embodiment 3

[0109] The scores obtained in patients B and C showed that the combined sublingual administration of 2 mg apomorphine and 15 mg sildelafil (tablet number 4) produced optimal erections and satisfaction levels higher than those achieved by sublingual administration of 2 mg apomorphine alone. Results of routinely administered (oral) sildelafil with pomorphine (tablet size 2) or higher (50 mg). Scores obtained from patients B and C also showed that erection / satisfaction with sublingual administration of a smaller dose (20 mg) of sildeprafil (tablets No. 5 and 6) was comparable to that achieved by oral administration of 50 mg number of tablets) reached the same or higher levels. Data from patients C and D showed that sublingual administration of 20 mg sildeprafil containing HPBCD (tablet size 6) resulted in a higher erection / sexual satisfaction score than sublingual administration of 20 mg sildiafil (tablet size 5) alone Enhanced. Data from patient A showed no negative decrease i...

Embodiment 4

[0125] Compositions B and C were prepared according to the procedure of composition A except for the dosage of the ingredients as indicated. Example 4: Wet Granule Composition

[0126] This example illustrates sublingual (SL) tablet compositions D-J prepared by the wet granulation method in Table 3 below.

[0127] Table 3: Wet Granule Composition

[0128] Ingredient (mg / tablet) D E F G H I J Apomorphine Hydrochloride, USP 2 2 2 2 2 2 2 Sildelafil Citrate, USP 15 15 15 15 15 15 15 Ascorbic Acid, USP 3 3 3 3 3 3 3 Citric Acid Anhydrous , NF 2 2 2 2 2 2 2 Microcrystalline Cellulose, NF 40 40 40 40 40 40 40 (Avicel PH 102)

[0129] Magnesium stearate, NF 1 1 1 1 1 1 1 Aspartame 1 1 1 1 1 1 1

[0130] Methyl Esters, USP Mannitol, USP, Powder 42 42 42 42 42 42 42 Carbopol 974P 10 - - - - - -

[0131] Sodium alginate - 5 10 - - - -

[0132] Gelatin, NF - - - 10 - - - Sodium hydroxymethylcellulose - - - - 10 - -

[0133] Tragacanth, NF - - - - - 10 - Hyd...

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
Login to View More

PUM

No PUM Login to View More

Abstract

The treatment of sexual dysfunction in human patients by an oral therapy regimen of administration of apomorphine and sildenafil is disclosed. This treatment optimizes the efficacy of each drug and substantially minimizes the undesirable side effects associated individually therewith. Apomorphine and sildenafil can be co-administered with a combination dosage unit or administered sequentially in separate dosage units, substantially prior to sexual activity. Other erectogenic agents can be administered along with apomorphine and sildenafil.

Description

Field of invention: [0001] The present invention relates to compositions, dosage forms and methods for treating sexual dysfunction in humans. More precisely, the present invention relates to the use of a composition comprising apomorphine and sildelafil. Background of the invention: [0002] Normal erections are the result of coordinated vascular activity in the penis. This is usually triggered by the nervous system, including dilation of blood vessels and relaxation of smooth muscles in the penis and its supply arteries. Arterial inflow causes enlargement of the corpus cavernosum, which in turn restricts venous outflow, allowing blood pressure to remain high enough in the penis to create and maintain penile rigidity. The muscles of the perineum also help create and maintain the firmness of the penis. Erections are induced centrally in the nervous system as a result of sexual thoughts, fantasies, and / or stimuli and can be locally intensified by reflex mechanisms (eg, tact...

Claims

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
Login to View More

Application Information

Patent Timeline
no application Login to View More
IPC IPC(8): A61K47/40A61K31/201A61K31/4164A61K31/437A61K31/473A61K31/505A61K31/517A61K31/522A61K31/568A61K31/5685A61P15/10A61P43/00
CPCA61K31/505A61P15/10A61P43/00A61K31/47A61K2300/00
Inventor R·埃尔-拉施迪
Owner PENTECH PHARMA
Who we serve
  • R&D Engineer
  • R&D Manager
  • IP Professional
Why Patsnap Eureka
  • Industry Leading Data Capabilities
  • Powerful AI technology
  • Patent DNA Extraction
Social media
Patsnap Eureka Blog
Learn More
PatSnap group products

Browse by: Latest US Patents, China's latest patents, Technical Efficacy Thesaurus, Application Domain, Technology Topic, Popular Technical Reports.

© 2024 PatSnap. All rights reserved.Legal|Privacy policy|Modern Slavery Act Transparency Statement|Sitemap|About US| Contact US: help@patsnap.com