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Methods of Treating Wounds With Gonyautoxins

Inactive Publication Date: 2007-12-06
PHYTOTOX LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Benefits of technology

[0073] Thus, as Table 6 demonstrates, GTX provides a safer treatment regiment for healing acute and chronic anal fissures than the current therapeutic methods such as BoTox or surgery. GTX treatment does not produce the inconveniences of flatus or fecal incontinence, nor does it require 5 to 7 weeks healing time. GTX treatment does not produce permanent sphincter damage resulting in long term hospitalization.
[0074] One unit of activity corresponds to an amount of the composition of the invention necessary to block the muscular contractions of the crural biceps of a 20 gram CF1 albino strain mous

Problems solved by technology

The high toxicity of these phycotoxins is due to reversible binding to a receptor site on the voltage-gated sodium channel on excitable cells, thus blocking the influx of sodium ions and preventing nerve and muscle cells from producing action potentials, thereby blocking neuronal transmission and causing death in mammals via respiratory arrest and cardiovascular shock.
This common problem causes substantial morbidity with nearly equal incidence in both sexes and is difficult to heal without intervention.
In many cases, bright blood may appear on the toilet paper.
The fundamental problem with this surgical procedure is permanent changes in the control of gas, mucus and stool.
Recurrence is a frequent problem in both ointment treatments with 31% relapse occurrence in nitroglycerine treated patients having relapse and 42% relapse occurrence in nifedipine patients.

Method used

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  • Methods of Treating Wounds With Gonyautoxins
  • Methods of Treating Wounds With Gonyautoxins

Examples

Experimental program
Comparison scheme
Effect test

example 1

[0048] Ten healthy male adults between 24 and 48 years old with normal sphincter tone (pressure at rest less than 72 mmHG as determined by anorectal manometry) were studied. The test subjects had no anorectal pathologies like hemorrhoids, fistula or abscesses. Before intervention, tests were performed including anorectal manometry, electromyography, a hemogram, a basic metabolic panel and a urinalysis.

[0049] A dosage of 100 units of activity of a combination of GTX-2 and GTX-3, in approximately a 2:1 ratio, in a total volume of 1.0 ml was locally infiltrated into both sides of the anal internal sphincter (0.5 ml each side) with an insulin syringe (25 gauge). The mixture of GTX-2 and GTX-3 was purified from shellfish collected in the Chilean Patagonia fjord that was found to be highly-contaminated with PSP toxins using standard purification methods.

[0050] Two minutes post injection an anorectal manometry was performed. Resting and voluntary contraction pressures were measured and r...

example 2

[0059] Fifty adults between the ages of 18 and 70 with symptomatic anal fissures were evaluated for inclusion in a study to test the effects of GTX local infiltration efficacy in the treatment of anal fissure via the reduction of anal tone to promote the healing process and eliminate the need for surgical intervention as well as provide a safe and effective alternative to ointment treatments.

[0060] Patients were evaluated for the following inclusion criteria: evidence of anterior, posterior or both circumscribed ulcers, induration at the edges and posterior of horizontal fibers of the interior anal sphincter, with symptoms of post defecatory or permanent pain, bleeding or both. Patients with an anal fissure history of two or month duration were considered to be chronic. Table 3 contains a detail of the patients selected for study. Patients younger than 18 or older than 70 years of age were excluded from this study as were those patients that were pregnant or had anal fissure associ...

example 3

[0074] One unit of activity corresponds to an amount of the composition of the invention necessary to block the muscular contractions of the crural biceps of a 20 gram CF1 albino strain mouse leg for 1.5 to 2.0 hours. The toxin was intramuscularly injected in the crural biceps of the mouse right leg in a volume of 0.5 ml. The left leg is used as a control. This was done in three mice and the paralyzing effect was tested every 30 minutes for the first two hours, and then every 2, 4, 8 hours and overnight. Depending on the dose injected, the paralyzing effect can last 24 hours or longer. This example confirms the reversible nature of the effect of the toxins of the present invention and demonstrates that the duration of the effect can be controlled by varying the dosage of the toxins.

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Abstract

Pharmaceutical compositions comprising tricyclic 3,4-propinoperhydropurines and uses thereof for blocking neuronal transmission which are useful in treating anal fissure and other wounds and muscle disorders are provided. Also provided are methods of treating wounds and muscle disorders by administering the composition of the invention to a muscle or in the vicinity of a muscle either topically or by injection.

Description

FIELD OF THE INVENTION [0001] This invention relates to pharmaceutical compositions containing heterocyclic guanidine-type compounds and uses thereof for treating wounds. More specifically, this invention relates to tricyclic 3,4-propinoperhydropurines and uses thereof for treating wounds, particularly in for use in treating anal fissure and other ailments. BACKGROUND OF THE INVENTION [0002] Paralytic shellfish poisoning (PSP) results from a mixture of phycotoxins that bind reversibly to a receptor site on the voltage-gated sodium channel found in excitable cells. The primary clinical symptom is an acute paralytic illness. Phycotoxins or algal toxins are produced by microscopic planktonic algae. These toxins accumulate on filter feeders such as bivalves. Consumption of phycotoxin-contaminated shellfish results in six diseases in humans: PSP, diarrhetic shellfish poisoning (DSP), amnesic shellfish poisoning (ASP), neurotoxic shellfish poisoning (NSP), ciguatera poisoning (CP) and cya...

Claims

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Application Information

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IPC IPC(8): A61K31/522A61K36/02A61K45/00A61F2/00A61K31/505
CPCA61K31/505A61P1/00A61P1/04A61P9/14A61P13/10A61P15/00A61P17/00A61P17/02A61P19/00A61P19/02A61P19/10A61P21/00A61P21/02A61P23/00A61P25/00A61P25/02A61P25/04A61P25/06A61P25/08A61P27/02A61P29/00Y02A50/30
Inventor WILSON, NESTOR
Owner PHYTOTOX LTD
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