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Patent Searching and Data

Document Type and Number:
WIPO Patent Application WO/2006/092151
Kind Code:
Topical corticosteroid formulations are the mainstay in treatment of psoriasis, eczema, burns and ulcers, the conventional formulations have the disadvantage of adverse effects both locally and systemically due to high dose, long duration of treatment and /or large area of application. The presen invention relates to a topical corticosteroid co-formulated with acetic acid, vanillin, rose oil and lemon oil. This formula has been proved to be highly effective in treating psoriasis, eczema, burns and ulcers with an excellent tolerability and minimal adverse effects, in addition to long lasting remissions and low percentage relapses as compared to available standard concentration corticosteroids alone or with other conventional medications for psoriasis and other related conditions.

El Masri, Mohamed Zakaria Ahmed (El Sayadela Building, Galal El Dosoky St. Wabour El May, Bab Sharky Alexandria, EG)
Application Number:
Publication Date:
September 08, 2006
Filing Date:
February 28, 2006
Export Citation:
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El Masri, Mohamed Zakaria Ahmed (El Sayadela Building, Galal El Dosoky St. Wabour El May, Bab Sharky Alexandria, EG)
International Classes:
A61K31/573; A61K31/055; A61K31/085
Foreign References:
Other References:
See also references of EP 1863493A1
Download PDF:
1. Patent of pharmaceutical formulation containing 5 ingradients . Acetic acid , Thymol , Vanillin , very small dose of one of High potency corticosteroid for example ( clobetasole . propionate , betamethasone propionate . etc ) Rose oil or lemon oil , in addition to trace of antioxidant , vitamines this patent is manufactured in the form of Cream .ointment , Emulsion , Lotion , solution and spray . this patent indicated for , all forms of Psoriasis ,all forms of Eczema, all forms of ulceration ( leg ulcer, bed ulcer ) all forms of Burns. acetic acid 96% : its dose from 0.5% to 2% gm in each 100 gm w/w of ointment (ointment , cream , solution , lotion , emultion ,spray), it has anti inflammatory , anti pruritic , keratolytic as well as bactericidal and fungicidal action. vanillin is a potent fungicidal and anti inflammatory its dose from 0.5% to 3% gm in each lOOgm w/w (ointment , cream , solution , lotion , emultion .spray). Rose oil or lemon oil is soothing agent and lubricant its dose from 0.5 gm to 4gm in each 100 gm w/w of (ointment , cream . solution , lotion , emultion ,spray).
2. High potency corticosteroid for ex .( clobetasole. Propionate , betamethasome dipropionate etc . ) it is anti inflammatory, anti pruritic its dose from.
3. mg to 7 mg in each 100 gram w\w (ointment , cream , solution , lotion , emultion .spray). Thymol it is antiseptic and anti inflammatory its dose from 25 mg to 150 mg in each 100 gram w\w (ointment , cream , solution , lotion , emultion ,spray).

Technical field

Pharmaceutical preparation patent for dermatological use only

Background art

Topical treatment

Treatments applied directly to the skin are sometimes effective in clearing psoriasis.

Sunlight -daily- regular, short doses of sunlight without burning clears psoriasis in many people with the disease


UV light from the sun stimulates production of vitamin D by the skin which slows the overproduction of skin cells that causes scaling, daily , short , nonburning exposure to sunlight clears or improves psoriasis in some people therefore : sunlight may be included among initial treatments for the disease . A more controlled artificial light treatment may be used in mild psoriasis ( UVB phototherapy or in more server or extensive psoriasis ( psoralen and ultraviolet PUVA therapy ) .

UVB phototherapy - artificial sources of UVB light are similar to sunlight . some physicians will start with UVB treatments instead of topical agents. UVB phototherapy also is used to treat widespread psoriasis and lesions that resist topical treatment . This type of phototherapy is normally administered in a doctor's office by using a light panel or light box . Although with a doctor's guidance , some patients can use UVB light boxes at home .

Corticosteroids- available in different strengths, corticosteroids

( cortisone ) are usually applied twice each day . short-term treatment is often effective . if less than 10 percent of the body's skin is involved . some doctors will begin treatment with a high-potency corticosteroid ointment ( for example , diprolene . temovate, ultravate or psorcon ) .

high-potency steroids may also be used for treatment resistant plaques, particularly those on the hands or feet .

Calcipotriene - this drugs is a synthetic form of vitamins D3 (this is not the same as vitamins D supplements) application of calcipotriene ointment (for example, dovonex ) twice daily controls the excessive production of skin cells in psoriasis

Coal tar - coal tar may be applied directly to the skin, used in a bath solution, or used as a shampoo for the scalp, it is available in different strengths

Anthralin-doctors sometimes use a 15- to 30- minute application of anthralin ointment, cream, or paste to treat chronic psoriasis lesions .

Salicylic acid - used to remove scales, salicylic acid is usually more effective when combined with topical steroids, anthralin , or coal tar .

Bath solutions - people with psoriasis may find that bathing in water with oil added then applying a moisturizer, can soothe the skin , scakes can be removed and itching reduced by soaking 15 minutes in water containing coal tar solution , oiled oatmeal , Epsom salts , or dead sea salts .

Moisturizers: when applied regularly over a long period, moisturizers have cosmetic and soothing effect . Preparations that are thick and greasy usually work best because they lock water into the skin

Systemic treatment

Doctors sometimes prescribe medicines that are taken internally for more severe forms of psoriasis , particularly when more than 10 percent of the body is involved .

Retinoids - these drugs are derived from vitamin A and include etretinate

( tegison ) and isotretinoin ( accutane ) . etretinate is most effective against pustular psoriasis .

Methotrexate - this treatment , which can be taken by pill or injection ,

Hydroxyurea ( hydrea ) - compared with methotrexate . hydroxyurea is less toxic but also less effective . hydroxyurea is sometimes combined

PUVA or retinoids .


Sunlight may be included among initial treatment for the disease

UVB phototherapy

It is associated with more side effects, including nausea .headache , fatigue , burning , and itching . long -term treatment is associated with irregular skin pigmentation . Corticosteroids

Long-term use or overuse of high-potency corticosteroids can lead to thinning of skin , internal side effects , resistance to the treatment's benefits, and worsening of the psoriasis the international dose from the high- potency is 50 m/g for each 100g/m of ointment w/w for example ( dermovite ointment or cream each 100g/m provides 5OnVg high potency clobetasole propionate , each lOOgm of elcon cream or ointment provides 100 mg high- potency corticosteroids w/w , each lOOgm . ointment of diprosalic provides 50m.g w/w of Beta methasone dipropionat (high- potency corticosteroids ) Calcipotriene - The safety of using the drugs for psoriasis affecting more than 20 percent of the body's skin is unknown : use on widespread - area of skin may raise the amount of calcium in the body to unhealthy levels Coal tar : Less effective and thus is not popular with many patients . other drawbacks include its failure to provide long-term help for most patients , it's strong ouder , and its tendency to stain skin . Anthralin

This treatment often fails to adequately clear lesions , it irritates the skin , and it stains skin and clothing brown or purple . in additions unsuitable for acute or actively inflamed eruptions Salicylic acid : Overuse cause salicyism

Systemic treatment

Retinoids : And include etertinate ( tegison ) and isortetinoin ( accutane )

Both drug can cause birth defects and are not recommende for women of childbearing age , at high doses , etretinete can effect liver function , therefore it is often combined with UVB phototherapy PUVA so that a lower , less toxic , does can be taken . Methotrexate - this treatment , which can be taken by pill or injection , slows down cell production and suppresses the immune system . patients taking methorexate must be closely carrying red blood cells , infection - fighting white blood cells , and clot-enhancing platelets . as a precaution , doctors do not prescribe the drug for people with long term livers disease or anemia . also , methotrexate should not be used by pregnant women , by women who are planning to get pregnant , or by their male partners

Disclosure of invention

Composition: active ingredients, acetic acid , thymol , vanillin , high potency corticosteroid for example ( clobetasole propionate , betamethasone dipropionate .

!0 etc ) rose oil or lemon oil and antioxidant trace. High potency corticosteroids actions has anti inflammatory, anti pruritic, Acetic acid has keratolytic as well as bactericidal and fungicidal actions . Vanillin has potent fungicidal and falvouring agent . Thymol has antiseptic propriety . rose oil or lemon oil has soothing effect for skin . the patent demonstrates these actions in a sustained manners there by

:5 permitting twice a day application . Indications and usage :

The patent is indicated for the relief of the inflammatory manifestations of hyper keratolytic and dry corticosteroid - responsive dermatoses such as psoriasis , chronic a topic dermatitis , new dermatitis ( lichen simplex chronicus ) licken planus ,

30 eczyma ( including nummular eczema , hard eczema , eczematous dermatitis , dysludrosis seborrhaic dermatitis of tiie scalp ichthyosis vulgaris and other ichthyolic conditions . it is also indicated for relief of scaling and flaking associated with skin conditions . also indicated for bed ulcer , leg ulcer , all forms of burns and ulceration

5 Dosage and administration :

In form of ( ointment ,cream , solution , lotion , emultion , spray ) a thin film should be applied to cover completely the affected area twice daily in the morning and at night

In form of ( spray ) shaken it before use and spray just to cover the affective area

0 with a fine coat products twice daily .

The patent provides in each 100 gram of ( ointment , cream , solution , lotion , emultion ,spray) from 2mg to 7 mg w\w high potency corticosteroid consequently adverse reactions that have been reported with the use of topical corticosteroids ( include . burning , itching . irritation , dryness , eruptions , hypopigmentation ,

5 dermatitis ) completely disappear and therefore must be born in mind when long- term continouse therapy is very safe . where no possible particularly in infants and children as adrenal suppression can occur . use these patent for treating such conditions as psoriasis , discoid lupus erythematosus and sever eczyma is also very

0 safe