• 专利附录
  • 专利说明
  • 权利要求
  • 类似技术
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  • 引用文献
  • 法律状态
  • 优先权
    • 专利摘要:
    Topical cream of clobesatol-l7propionate, urea and calendula oil and manufacturing procedure. The topical cream is compact, stable, with anti-inflammatory, antiproliferative and antipruritic properties where the pharmacological action of clobetasol 17-propionate is complemented by the moisturizing action of urea and the epithelizing, decongestant and antiseptic action of calendula oil. (Machine-translation by Google Translate, not legally binding)
    公开号:ES2607630A1
    申请号:ES201600192
    申请日:2016-03-09
    公开日:2017-04-03
    发明作者:Paz LOPEZ PITA
    申请人:Paz LOPEZ PITA；
    IPC主号:
    专利说明:

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    g) Dissolution of urea in water. h) Incorporation of the urea solution in water in the tempered mixture obtained in
    stage f).
    i) Stir until complete homogenization obtaining an emulsion.
    j) Cooling of the emulsion to about 30 ° C.
    k) Wetting clobetasol 17-propionate with propylene glycol.
    l) Incorporation into the emulsion of clobetasol 17-propionate from stage k)
    m) Stir more vigorously until cream consistency is achieved.
    n) 0.2% of essence can be incorporated to give a more organoleptic character
    nice.
    An emulsion is formed with stable droplets of small oily internal phase
    dispersed in the external aqueous phase. Clobetasol 17-native is dissolved in the
    oil phase and depending on the concentration may remain as a fine
    suspension at the base of the cream. Preferred embodiment
    In a preferred embodiment of the topical cream of clobesatol-17 propionate, urea and calendula oil, object of the present invention, the composition for 100 g of cream is as follows:
    Calendula oil ......................................... 5% (p / p )
    Urea ................................................. ................ 5% (p / p)
    Clobetasal17-propionate ......................... 0.1-0.2% (w / w)
    Emulsion Base 0 / A ........................................ csp 100 g
    Essence ................................................. ... 0.2% (p / p)
    The incorporation of the essence aims to give a more organoleptic character
    Creamy Where the composition for 100 g of O / A Emulsion Base is as follows: Self-emulsifying Neo-PCL O / W Base ................. 25% Propylene Glycol ...... .................................................. .... cs Nipagin (preservative) ......................................... 0.2% Purified water ........................................... ... csp 100 g
    7
    The creams are prepared by the method of melting and mixing the phases
    Heat the Neo-PCL O / W base at 65-70º until completely melted and add the calendula oil (Phase A).
    Dissolve the nipagin in water and Heat (reserving a little water to dissolve the urea) at 65-70ºC. (Phase B).
    Incorporate the aqueous phase B over the oil phase while stirring moderately and once tempered the water is incorporated with the urea. Stir until complete homogenization.
    When the emulsion reaches about 30º, incorporate the clobetasol propionate previously moistened with a little propylene glycol and continue stirring more vigorously until reaching the consistency of cream.
    0.2% of essence can be incorporated to give a more pleasant organoleptic character.
    An emulsion is formed with stable droplets of small oily internal phase dispersed in the aqueous external phase. Clobetasol 17-propionate dissolves in the oil phase and depending on the concentration may remain a fine suspension at the base of the cream.
    The result of the formulation is a compact, stable cream with anti-inflammatory, anti-proliferative and anti-pruritic properties where the pharmacological action of clobetasol 17-propionate is complemented by the moisturizing action of urea and the epithelizing, decongestant and antiseptic action of calendula oil .
    It has an acidic pH of 5.5 that respects the balance of the epidermis, an important aspect in case of dermal conditions and that is within the optimal effective range of methylparaben.
    It is an oily aqueous and internal external phase cream, which forms a discontinuous fatty film that allows the perspiration of the skin and where the emollient and moisturizing formulation provide a cooling and soothing effect, reducing the desquamation of erythema and pruritus.
    With very little occlusivity, unlike other preparations consisting of a single phase with hydrophobic excipients like petrolatum, paraffins etc. which reduces the possible local and systemic adverse effects, which do occur with those other preparations that, when spread on the skin, form a lipophilic layer that in many cases has an occlusive character, which increases the local and systemic adverse effects of corticosteroids
    Very extensible allowing the application of very thin layers on the affected skin areas thus favoring the use of small amounts of drug during treatments.
    The change that can bring in the therapy of skin diseases, is to reduce the number of applications and the duration of the treatments, being able to be limited to a single daily application or on alternate days (4 days / week) and even 2 days per week,
    8
    gradually decreasing the corticosteroid trying to avoid the effects of tachyphylaxis and rebound.
    To evaluate the transdermal absorption and penetration of the drug through the skin, an "In Vitro" test was performed to determine the transdermal flow of clobetasol from the creams made using the "Franz cells" and pigskin method. as a substrate, which has shown that the use of the 0 / W cream formulation tested favors the penetration of clobetasol propionate through the skin.
    The results obtained reflect that there is a gradual increase in the diffusion of the drug until 6 hours of testing, from that moment the diffusion stops reaching the maximum concentration. Taking into account the value of the calculated flow and amount of sample used, after 24 hours it diffuses 40% of the dose and after 24 hours of contact the amount of clobetasol propionate found inside the skin constitutes approximately a 10% of the dose of drug used, which would indicate in an indicative manner that after a single application of the pharmaceutical preparation the pharmacological action can be maintained throughout the 24 hours. Indications and uses
    Treatment of inflammatory or allergic skin diseases sensitive to corticosteroids tapestries and for short periods, such as atopic dermatitis, severe contact dermatitis, severe eczema, cutaneous lichen planus, simple lichen, discoid lupus erythematosus, some forms of psoriasis and in general conditions that do not respond satisfactorily to less potent corticosteroids and where the emollient formulation improves the moisture content of the skin.
    In cases of psoriasis in which the patient is being treated with immunomodulators tapestries (tacrolimus, pimecrolimus) systemic immunosuppressants (cyclosporine, methotrexate, hydroxyurea) or biological treatment and in which topical intermittent treatments are required to minimize the dose of such drugs.
    The guidelines and duration of treatment will be conditioned by the pathology, surface and anatomical area to be treated (arms, elbows, hands, trunk, etc.) and should be applied late in the afternoon when endogenous steroid levels are lower (midnight ) taking into account that clobetasol propionate can cause reversible suppression of the hypothalamic-pituitary-adrenal axis (HPA) as a systemic side effect.
    It is recommended that its use is not prolonged, neither in large areas of body surface, nor exceed 25 mg of active substance per week and avoid in folds, face and intertriginous regions and that it is not used in cases of hypersensitivity to the active substance or any of its components. It should not be used in cases of rosacea, impetigo, vincal or fungal infections.
    9
    权利要求:
    Claims (1)
    [1]
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    同族专利:
    公开号 | 公开日
    ES2607630B2|2017-09-25|
    引用文献:
    公开号 | 申请日 | 公开日 | 申请人 | 专利标题
    ES8706027A1|1986-03-24|1987-05-16|Belda Galiana Manuel F|Topical pharmaceutical compositions for treating vitiligo|
    RU2042351C1|1990-06-15|1995-08-27|Владимир Валерианович Гусев|Face and body skin care cream|
    DE19904801A1|1999-02-05|2000-08-10|Klossner Axel|Agent containing urea, sulfur and Calendula extract, useful for topical treatment of skin disorders, especially neurodermatitis|
    EP2705847A1|2012-09-05|2014-03-12|PSoriasis+Creams Sweden AB|Composition for treating psoriasis|
    法律状态:
    2017-09-25| FG2A| Definitive protection|Ref document number: 2607630 Country of ref document: ES Kind code of ref document: B2 Effective date: 20170925 |
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    优先权:
    申请号 | 申请日 | 专利标题
    ES201600192A|ES2607630B2|2016-03-09|2016-03-09|Topical cream of clobetasol-17 propionate, urea and marigold oil and manufacturing procedure|ES201600192A| ES2607630B2|2016-03-09|2016-03-09|Topical cream of clobetasol-17 propionate, urea and marigold oil and manufacturing procedure|
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