GB2084464A

GB2084464A - Povidone-iodine Powders

Info

Publication number: GB2084464A
Application number: GB8032051A
Authority: GB
Original assignee: Beta Medical Products Ltd
Current assignee: Beta Medical Products Ltd
Priority date: 1980-10-04
Filing date: 1980-10-04
Publication date: 1982-04-15
Also published as: GB2084464B

Abstract

An antiseptic pharmaceutical composition for dispersing or sprinkling onto an area of skin to be treated, broken or intact, comprises povidone-iodine and a suitable inert carrier or diluent powder such as lactose. The composition may also comprise zinc oxide.

Description

SPECIFICATION Antiseptic Compositions This invention concerns antiseptic compositions containing, as active ingredient, povidoneiodine, which is a complex formed by reacting poly( 1 -vinylpyrrolidone) with elemental iodine.

Povidone-iodine is a remarkable substance in that it exhibits the antiseptic and germicidal activities of iodine without having the disadvantages of iodine. For example, solutions of pure iodine, when applied to intact human skin, can irritate, stain and cause allergic reactions. By contrast, povidone-iodine is non-irritant and non-sensitising.

Povidone-iodine is, therefore, a most useful antiseptic having the capacity to kill an extremely wide range of Gram positive and Gram negative bacteria, viruses, protozoa, yeasts and fungi. It is particularly useful since it can be employed for certain topical applications as an alternative to antibiotics, thereby reducing the risk of the useful life of the antibiotics being shortened due to the development of resistant strains of organisms.

Povidone-iodine is mainly formulated as an aqueous solution for application to the skin. There are, however, a number of applications where such formulations are unsuitable. For example, the use of an aqueous solution of povidone-iodine for the treatment or prevention of infection in areas of the body that are very wet, such as varicose ulcers which are exuding wet debris and pus, simply adds more unwanted liquid to the wound.

In first-aid treatment of cuts or burns to the skin using an antiseptic, the presence of blood dilutes and interferes with aqueous solutions. Thus there are many occasions when a dry powder preparation would be preferred.

Hitherto, the only method available of applying povidone-iodine as a dry powder, has been from an aerosol spray, where the povidone-iodine has been suspended in pressurised fluorinated hydrocarbon aerosol propellants. When the aerosol is actuated, the propellants (having a boiling point below ooC) are exhausted to atmosphere in the form of a spray, carrying the povidone-iodine powder.

The powder is deposited at the site to which the spray is directed. This method of applying povidoneiodine as a powder has several disadvantages: 1. Liquid propellant can come into contact with the skin, if the spray is held too close, causing a rapid drop in temperature and possibly "frost-bite".

2. Not all the powder from the spray is deposited on the area requiring treatment. There is a considerable "over spray" where particles of powder can bounce off the skin, or are carried some distance away in the air. This can lead to particles being inhaled by either the patient or other persons in close proximity.

3. There is concern that the presence of fluorinated hydrocarbons in the atmosphere at relatively high concentrations, as could occur when an aerosol is used in an unventilated small room, are potentially injurious to the human body when inhaled.

There would therefore, be an advantage in providing a dry antiseptic in powder formulation which could be dispersed or sprinkled onto an area to be treated.

This method of applying an antiseptic powder onto the skin is used for other substances, e.g.

antibiotics, where starch is used as the bulking agent in which the antiseptic is dispersed.

However, starch has been found to be unsuitable for use with povidon-iodine, since the iodine present produces a characteristic purple colour from reaction with the starch. This is not only undesirable, but reduces or cancels the antibacterial activity of the povidone-iodine.

Povidone-iodine is also very hygroscopic forming a sticky, gelatinous substance, which in the presence of starch powder, would cause particles to agglomerate. The end effect could be that the powder forms lumps, and would not be capable of being dispersed or sprinkled onto an area to be treated.

Accordingly this invention provides a pharmaceutical composition comprising povidone-iodine dispersed in a suitable inert carrier or diluent powder, which composition can be dispersed freely onto skin or wounds to the skin.

In identifying a suitable inert carrier or diluent powder for povidone-iodine, the following properties are desirable:- 1. It should be safe for use on human skin, whether intact or broken, and particularly in cuts to the skin.

2. It should be inert to the presence of iodine, i.e. it should not react with povidone-iodine.

3. It should be free flowing and should not form agglomerates with povidone-iodine which has absorbed water but still remain in powder form.

When investigating sugars, and related compounds, the disaccharide obtained from the whey of milk, (lactose) proved siutable. Finely-divided povidone-iodine mixed with finely-divided lactose powder was found to remain a free flowing powder. Particle sizes of 5 to 1 50 microns are particularly advantageous. Preferably powder compositions of this invention contain 0.01 to 20% by weight of povidone-iodine. The povidone-iodine itself preferably contains from 9 to 12% available iodine and has a molecular weight not exceeding 35,000+5%.

The powder compositions of this invention may also contain other suitable constituents, such as zinc oxide. From a medical point of view zinc oxide possesses mild astringent and antiseptic properties and acts so as to aid the healing of skin wounds. Zinc oxide also improves the powder flow characteristics of the compositions.

The powder compositions of this invention are conveniently dispersed or sprinkled onto an area of skin to be treated from a bottle have a pluraiity of small holes at its outlet, such as the type of bottle generally used for the application of talcum powder. Preferably the bottle used is made of a flexible or resilient material so that the bottle may be squeezed to help expel the powder.

This invention will now be further described by means of the following Examples of antiseptic powder compositions made by mixing of the constituents in the stated amounts.

Example 1 Lactose 90% by weight Povidone-lodine 10% by weight Example 2 Lactose 95% by weight Povidone-lodine 5% by weight Example 3 Lactose 80% by weight Zinc Oxide 10% by weight Povidone-lodine 10% by weight Example 4 Lactose 90% by weight Zinc Oxide 5% by weight Povidone-lodine 5% by weight In the above Examples, povidone-iodine with a molecular weight not exceeding 35,000 (+5%) was used. Higher molecular weight povidone-iodine is retained in the body by lymph nodes or in the reticuloendothelial system.

The compositions of Examples 1 to 4 were tested and evaluated immediateiy and after storage as follows: 1. Appearance The appearance of the powder and the distribution of red/brown povidone iodine particles was noted.

2. Active Agent Content The active agent content was determined using 0.01 N sodium thiosulphate solution.

Approximately 1 g of the composition was weighed accurately and diluted with 1 00ml of distilled water.

The resultant solution was titrated with a fresh 0.01 N solution of sodium thiosulphate. Near the end point of the colour change of red to colourless 3ml of starch solution were added and further sodium thiosulphate solution added to the end point change of blue to colourless.

12.69x0.01 xmls of titrate Available iodine % w/w= Weight of sample in grams 3. Identity About 1.0my of sample were diluted with somas of water and 1 .0ml of starch solution added. A deep blue/purple colour indicated the presence of iodine.

The compositions of the Examples were found to be stable and active after storage trials. If sterilised by gamma radiation (2.3 Med/Rads) they also remained stable and active after storage trials.

It was also found that the compositions of Examples 3 and 4 were improved both medically and physically by the addition of zinc oxide. From a medical point of view, zinc oxide possesses mildly astringent and antiseptic properties, and acts so as aid the healing of a wound to the skin. Furthermore the powder flow characteristics were found to be improved compared with the simple mixture of lactose and povidone-iodine.

Claims (Filed 24 Sept. 1981) 1. A pharmaceutical composition comprising povidone-iodine dispersed in a suitable inert carrier or diluent powder, which composition can be dispersed freely onto skin or wounds to the skin.

2. A composition as claimed in claim 1 wherein the inert carrier or diluent powder is safe for use on human skin whether intact or broken.

**WARNING** end of DESC field may overlap start of CLMS **.

Claims

**WARNING** start of CLMS field may overlap end of DESC **. zinc oxide. From a medical point of view zinc oxide possesses mild astringent and antiseptic properties and acts so as to aid the healing of skin wounds. Zinc oxide also improves the powder flow characteristics of the compositions. The powder compositions of this invention are conveniently dispersed or sprinkled onto an area of skin to be treated from a bottle have a pluraiity of small holes at its outlet, such as the type of bottle generally used for the application of talcum powder. Preferably the bottle used is made of a flexible or resilient material so that the bottle may be squeezed to help expel the powder. This invention will now be further described by means of the following Examples of antiseptic powder compositions made by mixing of the constituents in the stated amounts. Example 1 Lactose 90% by weight Povidone-lodine 10% by weight Example 2 Lactose 95% by weight Povidone-lodine 5% by weight Example 3 Lactose 80% by weight Zinc Oxide 10% by weight Povidone-lodine 10% by weight Example 4 Lactose 90% by weight Zinc Oxide 5% by weight Povidone-lodine 5% by weight In the above Examples, povidone-iodine with a molecular weight not exceeding 35,000 (+5%) was used. Higher molecular weight povidone-iodine is retained in the body by lymph nodes or in the reticuloendothelial system. The compositions of Examples 1 to 4 were tested and evaluated immediateiy and after storage as follows: 1. Appearance The appearance of the powder and the distribution of red/brown povidone iodine particles was noted. 2. Active Agent Content The active agent content was determined using 0.01 N sodium thiosulphate solution. Approximately 1 g of the composition was weighed accurately and diluted with 1 00ml of distilled water. The resultant solution was titrated with a fresh 0.01 N solution of sodium thiosulphate. Near the end point of the colour change of red to colourless 3ml of starch solution were added and further sodium thiosulphate solution added to the end point change of blue to colourless. 12.69x0.01 xmls of titrate Available iodine % w/w= Weight of sample in grams 3. Identity About 1.0my of sample were diluted with somas of water and 1 .0ml of starch solution added. A deep blue/purple colour indicated the presence of iodine. The compositions of the Examples were found to be stable and active after storage trials. If sterilised by gamma radiation (2.3 Med/Rads) they also remained stable and active after storage trials. It was also found that the compositions of Examples 3 and 4 were improved both medically and physically by the addition of zinc oxide. From a medical point of view, zinc oxide possesses mildly astringent and antiseptic properties, and acts so as aid the healing of a wound to the skin. Furthermore the powder flow characteristics were found to be improved compared with the simple mixture of lactose and povidone-iodine. Claims (Filed 24 Sept. 1981)

1. A pharmaceutical composition comprising povidone-iodine dispersed in a suitable inert carrier or diluent powder, which composition can be dispersed freely onto skin or wounds to the skin.

3. A composition as claimed in claim 1 or 2 wherein the inert carrier or diluent powder is inert to

the presence of iodine.

4. A composition as claimed in claim 1, 2 or 3 wherein the inert carrier or diluent powder is free flowing and does not form agglomerates with povidone-iodine which has absorbed water.

5. A composition as claimed in any one of claims 1 to 4 wherein the inert carrier or diluent powder is lactose.

6. A composition as claimed in claim 5 wherein the lactose has a particle size of from 5 to 150 microns.

7. A composition as claimed in any one of claims 1 to 6 comprising 0.01 to 20% by weight of povidone-iodine.

8. A composition as claimed in any one of claims 1 to 7 wherein the povidone-iodine contains from 9 to 12% by weight available iodine.

9. A composition as claimed in any one of claims 1 to 8 wherein the povidone-iodine has a molecular weight not exceeding 35,000+5%.

10. A composition as claimed in any one of claims 1 to 9 further comprising zinc oxide.

11. A pharmaceutical composition as claimed in claim 1 and substantially as hereinbefore described with reference to any one of the Examples.