GB1561037A - Composition for the treatment and prevention of skin eye and mucosal inflammation - Google Patents

Description

(54) COMPOSITION FOR THE TREATMENT AND PREVENTION OF SKIN, EYE AND MUCOSAL INFLAMMATION (71) We, EUGENE LAPINET, of 1517 Galerie Vivienne 75002 Paris, France and GEORGES CEHOVIC of 7 residence de la Vallee 91120 Paliseau, France both citizens of France, and THEODORE POSTERNAK, of 25 Athenee 1206, Geneve Switzerland, a citizen of Switzerland, do hereby declare the invention for which we pray that a patent may be granted to us, and the method by which it is to be performed, to be particularly described in and by the following statement:- The invention relates to compositions for the treatment and prevention of skin conditions, eye and mucosal inflammation on humans and animals. This invention may be used to treat or prevent irritation of skin or eye or mucosa of humans and animals such as dogs and cats especially, but not exclusively, by external, topical application.

This invention may be used to treat inflammation and alleviate skin conditions such as sun and weather induced damages, skin disorders producing swelling (edema), redness, irritation, itching, allergic reactions such as those produced by chemical agents, scalding, toxic substances of chemical or biological origin, poison oak (dermatitis venenata), acid, poison ivy, insect bites or burns and other inflammatory skin reactions of bacterial or fungal origin or produced by irradiation such as ultra-violet or infra-red irradiation. The composition may be used both in curing a function for skin, mucosa or eye after a subject has been exposed to conditions leading to inflammation or irritation as well as in a prophylatic function prior to any such exposure.

According to this invention, there is provided a composition in the form of a cream, a solution, a lotion or a spray for the treatment (including remedial and preventative treatment) of skin, eye or mucosa irritations or inflammations comprising, in a suitable pharmaceutical carrier, as an active ingredient from 0.01 to 1% by weight of a compound of the following formula:

this compound may be used as such or in the form of any pharmaceutically acceptable salt of the same and a phosphodiesterase inhibiting amount of aminophylline.

The compound of the formula is 3',5'adenosine monophosphate or cAMP.

The compositions prepared with these compounds have been shown also to decrease the skin histamme level. these compositions, when applied in pharmaceutically active amounts 1 to 3 times daily, decrease oedema arising from scalds or burns, inflammations produced by chemical compounds or organic agents, and improve or prevent itching, redness, swelling, which are caused by scalding, burning or various skin mucosal or eye irritations.

Compositions prepared with these compounds in the form of solutions or ointment are useful for treatment or prevention of acute eye inflammation produced by foreign bodies, chemicals or burns. The composition with these compounds can be used especially topically for treatment of different kinds of inflammatory processes of skin, mucosa, of ear, throat and mouth and rectal and genital mucosa.

cAmp may be made as set out in publications of the inventors (Posternak et al., Bioch. Bioph., Acta 65, 558, 1962, and Cehovic et al., Adv. Cyclic Nucleotides Res., vol. 1, 521, 1972, Raven Press, N.Y.).

A pharmaceutically effective amount of the cAMP ingredient may be admixed, together with the phosphodiesterase inhibitor aminophylline as desired and with a non-toxic carrier suitable for human external use. For example, suitable carriers include combinations of petroleum; waxes, stearin, glycerol, lanolin, sesame oil, lanette wax or propylene glycol.

The effective amount of the active ingredient may vary with the severity of the inflammation.

The preferred method of application is once, twice, or three times daily using enough of the composition to lightly cover the area to be treated. In the case of different kinds of inflammation of the skin or mucosa, it is important to apply the cream as soon as possible after the appearance of inflammation and to repeat the cream application 2 to 3 hours later. For persons suffering from allergic reactions a preventive topical application of the cream on the skin or in the eye is recommended 2 to 3 hours before exposure to chemical or biological substances which are suspected to produce an allergic reaction.

Improved results are obtained if the cream or the lotion is applied 1 to 2 hours before exposure to sunshine or unfavourable weather conditions. In case of eye irritation produced by foreign bodies or chemical or burns or irradiation, the preferred method is the treatment by irrigation of the eye and consecutive frequent instillations or applications or active compound in form of ointment or cream.

For experimental studies on eye inflammation, the active compound was diluted in physiological solution (NaCI 0.9%) and pH adjusted at 7.3.

Example 1 illustrates a formulation without limiting the invention for dermatological use.

Percentage Example 1 by weight Stearic acid 15.0 Lanolin anhydrous 4.0 Beeswax 2.0 Mineral Oil 23.0 Tween (Registered Trade Mark) 85 1.0 Arlacel (Registered Trade Mark) 85 1.0 Sorbitol 11.5 Distilled water 42.0 Aminophylline 0.4 3',5'-adenosine cyclic monophosphate 0.1 WHAT WE CLAIM IS: 1. A composition in the form of a cream, a lotion, a solution or a spray for treatment of irritation or inflammation of skin, eye or mucosa comprising in a suitable pharmaceutical carrier as an active ingredient from 0.01 to 1% by weight of a compound of the following formula:

or a pharmaceutical acceptable salt of the compound and a phosphodiesterase inhibiting amount of aminophylline.

2. A composition according to claim 1 which contains 3',5'-adenosine monophosphate in a concentration or 0.1% by weight and aminophylline in a concentration of 0.4% by weight.

3. A composition for treatment of irritation or inflammation of skin, eye and mucosa substantially as described in the Example.

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

Claims (3)

**WARNING** start of CLMS field may overlap end of DESC **. Res., vol. 1, 521, 1972, Raven Press, N.Y.). A pharmaceutically effective amount of the cAMP ingredient may be admixed, together with the phosphodiesterase inhibitor aminophylline as desired and with a non-toxic carrier suitable for human external use. For example, suitable carriers include combinations of petroleum; waxes, stearin, glycerol, lanolin, sesame oil, lanette wax or propylene glycol. The effective amount of the active ingredient may vary with the severity of the inflammation. The preferred method of application is once, twice, or three times daily using enough of the composition to lightly cover the area to be treated. In the case of different kinds of inflammation of the skin or mucosa, it is important to apply the cream as soon as possible after the appearance of inflammation and to repeat the cream application 2 to 3 hours later. For persons suffering from allergic reactions a preventive topical application of the cream on the skin or in the eye is recommended 2 to 3 hours before exposure to chemical or biological substances which are suspected to produce an allergic reaction. Improved results are obtained if the cream or the lotion is applied 1 to 2 hours before exposure to sunshine or unfavourable weather conditions. In case of eye irritation produced by foreign bodies or chemical or burns or irradiation, the preferred method is the treatment by irrigation of the eye and consecutive frequent instillations or applications or active compound in form of ointment or cream. For experimental studies on eye inflammation, the active compound was diluted in physiological solution (NaCI 0.9%) and pH adjusted at 7.3. Example 1 illustrates a formulation without limiting the invention for dermatological use. Percentage Example 1 by weight Stearic acid 15.0 Lanolin anhydrous 4.0 Beeswax 2.0 Mineral Oil 23.0 Tween (Registered Trade Mark) 85 1.0 Arlacel (Registered Trade Mark) 85 1.0 Sorbitol 11.5 Distilled water 42.0 Aminophylline 0.4 3',5'-adenosine cyclic monophosphate 0.1 WHAT WE CLAIM IS:

1. A composition in the form of a cream, a lotion, a solution or a spray for treatment of irritation or inflammation of skin, eye or mucosa comprising in a suitable pharmaceutical carrier as an active ingredient from 0.01 to 1% by weight of a compound of the following formula:

or a pharmaceutical acceptable salt of the compound and a phosphodiesterase inhibiting amount of aminophylline.

2. A composition according to claim 1 which contains 3',5'-adenosine monophosphate in a concentration or 0.1% by weight and aminophylline in a concentration of 0.4% by weight.

3. A composition for treatment of irritation or inflammation of skin, eye and mucosa substantially as described in the Example.