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

Anti-inflammatory formulations for inflammatory diseases

a technology of inflammatory diseases and formulations, applied in the field of topical formulations, can solve the problems of not being particularly effective at reducing the duration of vital shedding or lesion, not being particularly effective at reducing or treating recurrent disease, and further inflammation, and achieves broad-spectrum antimicrobial activity and prevents transmission

Inactive Publication Date: 2001-07-03
ECOLAB USA INC
View PDF7 Cites 48 Cited by
  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Benefits of technology

The aforementioned therapeutic problems are treated by a strongly antimicrobial and anti-inflammatory formulation wherein the active antimicrobial and/or anti-inflammatory effects are provided by a composition which comprises a chlorine dioxide liberating compound and a protic acid. Preferably, the chlorine dioxide liberating compound is an alkaline metal chlorite. Most preferably, the chlorine dioxide generating compound is sodium chlorite or potassium chlorite. Topical formulations are useful for the topical treatment of dermatologic disorders thought to be caused by overgrowth of pathogenic microorganisms that possibly result in an inflammatory response, or for inflammatory conditions. These dermatologic d...

Problems solved by technology

Although the precise mechanisms are not entirely clear, inflammation and edema in the follicular wall result in follicular rupture, leaking follicular contents into the surrounding dermis and creating further inflammation.
Acyclovir, applied topically, tends to decrease pain of the primary lesions, but it has not proven very effective for decreasing vital shedding or lesion duration.
Topical acyclovir has not been shown to be particularly effective for reducing or treating recurrent disease.
The monophosphate form is converted to an acyclovir triphosphate, which can interfere with vital DNA replication.
The up to eight-times-a-day dosing is a difficult procedure for patients and creates patient compliance problems for dosing in the genital areas throughout the day and throughout the night.
A further problem of acyclovir has been the development resistant strains of herpes simplex, caused by a mutation of the thymidine kinase gene.
Accordingly, no backup treatments are available for acyclovir-resistant herpes simplex infections.
Itching is common and severe.
Griseofulvin is a systemic agent, and ketoconazole is also used systemically but is expensive and is associated with severe side effects.
Side effects of griseofulvin include headaches and abdominal discomfort.
However, no single treatment has yet proven to be successful for a wide variety of cases.
At present, there are no known virucidal chemical barrier preparations available that can be used alone or with a condom for prevention of the spread of HIV during sexual contact.
Steroid drugs have anti-inflammatory activity but also have numerous side effects, including sodium retention, hepatic deposition of glycogen, and dramatic redistribution of body fat.
However, aspirin-like drugs have little or no effect upon the release or activity of histamine, 5-HT, SRS-A, or lysosomal enzymes; and similarly, potent antagonists of 5-HT of histamine have little or no therapeutic effect on inflammation.
Although the classical aspirin-like drugs (salicylates, pyrazolone derivatives, ibuprofen, indomethacin, etc.) block prostaglandin biosysthesis, they do not inhibit the formation of the major chemotactic metabolite of arachidonic acid, HETE, and may even increase concentrations of this compound in tissue.
Paradoxically, the antimicromial properties of PMNs are greatly impaired in the ischemic wound region in vivo because of the lack of molecular oxygen.
However, the optimal times and mode of oxygen therapy still remain clouded.
Although the presence of these oxygen-free radicals is necessary for the oxidative killing of microorganisms, excessive generation of these cytotoxic radicals may be extremely harmful to native tissues.

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

Image

Smart Image Click on the blue labels to locate them in the text.
Viewing Examples
Smart Image
  • Anti-inflammatory formulations for inflammatory diseases
  • Anti-inflammatory formulations for inflammatory diseases
  • Anti-inflammatory formulations for inflammatory diseases

Examples

Experimental program
Comparison scheme
Effect test

example 1

This example illustrates a formulation useful for the topical treatment of genital herpes according to the methods of the present invention. This formulation also can be used for hemorrhoids and has anti-inflammatory activity, as shown in Examples 7-9. There is prepared a two-part topical composition according to the invention, having a first gel with sodium chlorite as the chlorine dioxide liberating agent and a second gel with lactic acid as the activator protic acid. The formulations on a percent weight basis are as follows:

% First Gel Poly (sulfonic acid) 45.0 (16% solution .+-. 1%) Sodium hydroxide 1 N 45.0 Sodium chlorite (80% .+-. 5%) 0.32 Tetrasodium EDTA 0.19 Water q.s. Second Gel Lactic Acid (38% .+-. 5%) 2.64 Natrosol 150 MR 1.75 Isopropyl alcohol U.S.P. 5.0 Poloxamer 188 0.4 Sodium Benroate 0.04 Water q.s.

example 2

The composition of Example 1 was prepared for a clinical trial in a pair of unit dose sachets. A 2-gram quantity of gel containing 0.16% of active chlorite was prepared by mixing the contents of both sachets immediately prior to application. Thirty-five patients (30 males and 5 females) were enrolled. Thirty-four were diagnosed as having active genital herpes. Thirty-one patients complied with the treatment of twice daily dosing for seven days. Three patients received the compositions of Example 1 t.d.s., and one patient defaulted. Patients were examined daily until the lesions were healed (defined as re-epithelialization of the original lesions). The results of the study were compared to a similar study conducted with topical acyclovir and placebo (Fiddian et al, J. Antimicrob. Chem. 12:Suppl. B:67-77, 1983) and are presented together in Table 1 below:

Median Median Duration of Viral Median Recurrence Symptoms Shedding Healing Rate (d) Time (d) Time (d) % Example 1 3* 1** 8 (1-17) 1...

example 3

The following formulation can be used as a dermatologic gel for psoriasis treatment:

% Base Sodium chlorite (80% .+-. 5%) 0.32 Tetrasodium EDTA 0.19 Poly (sulfonic acid) 45.0 (16% solution .+-. 1%) Sodium hydroxide 1 N 40.0 Nacconol 90F 1.8 Water q.s. Activator Propylene glycol U.S.P. 40.0 Salicylic acid U.S.P. 2.0 Poloxamer 188 0.4 Sodium Benzoate 0.04 Natrosol 250 MR 2.1 Isopropyl alcohol U.S.P. 5.0 Water q.s.

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

PropertyMeasurementUnit
Percent by massaaaaaaaaaa
Fractionaaaaaaaaaa
Fractionaaaaaaaaaa
Login to View More

Abstract

There is disclosed a method for treating dermatologic diseases caused by microbial overgrowth or inflammation, such as psoriasis, fungal infections, eczema, dandruff, acne, genital herpes lesions, and leg ulcers. There is further disclosed an antiviral lubricating composition that is effective in preventing the transmission of the HIV virus and other sexually transmitted diseases. There is also disclosed systemic and anti-inflammatory compositions and formulations and a method for reducing tissue inflammation in tissues such as the bowel, muscle, bone, tendon and joints (e.g., arthritis).

Description

TECHNICAL FIELDThis invention relates generally to topical formulations that are useful for treating various dermatologic disorders, including genital herpes lesions, facial and body acne, topical fungal infections, psoriasis, eczema, dandruff, skin ulcers (e.g., decabutus), and other dermatologic diseases associated with microbial proliferation. This invention also relates to the anti-inflammatory properties and uses of pharmaceutical compositions.BACKGROUND OF THE INVENTIONThere are a Large number of dermatological diseases that are thought to be caused by microbial overgrowth somehow result in a dermatologic infection and / or inflammatory reaction. These diseases include acne vulgaris and other pilosebaceous inflammatory disorders, which are thought to be caused in part by an overgrowth of the anaerobic bacterium Propionibacterium acnes (P. acnes), which is normally present in the sebaceous follicles but proliferates in large numbers during acute acne. P. acnes generates a lipase,...

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): A61K33/40A61P17/00A61K33/20A61P29/00A61P31/12A61P31/22
CPCA61K33/40A61P17/00A61P29/00A61P31/12A61P31/22A61K31/60A61K31/19A61K2300/00
Inventor KROSS, ROBERT D.SIFF, ELLIOTT J.
Owner ECOLAB USA INC
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