134 results about "Clobetasol propionate" patented technology

Sprayable, anhydrous and physically / chemically stable dermatological / pharmaceutical compositions, well suited for the treatment of a variety of dermatological disorders, notably psoriasis, contain: a) a therapeutically effective amount of a solubilized corticoid, notably dissolved clobetasol propionate; b) a therapeutically effective amount of a solubilized vitamin D derivative, notably dissolved calcitriol; and c) an oily phase which comprises one or more oils; formulated into d), a sprayable and topically applicable, dermatologically / pharmaceutically acceptable vehicle therefor.

Anhydrous sprayable pharmaceutical / dermatological compositions containing, as active pharmaceutical agent, a corticoid, preferably clobetasol propionate, and an oily phase, are formulated in a physiologically acceptable medium, and are useful for the treatment of a variety of conditions and afflictions, notably psoriasis.

The invention discloses a nano-emulsion medicine for treating foot rot. The grain diameter of the nano-emulsion is in a range of 1-100 nanometers and the nano-emulsion is composed of the following raw materials: 0.1-10.0% of pine tar, 0.1-6.0% of cinnamyl aldehyde, 0.1-6.0% of carvacrol, 0.1-5.0% of camphor oil, 0.01-0.1% of clobetasol propionate, 18.0-35.0% of surfactant, 0-7.0% of co-surfactant and residual amount of distilled water; and the sum of the mass percentages of the components is 100%. The nano-emulsion disclosed by the invention has the functions of dissolving cutin, relieving itching, diminishing inflammation, restraining, partially disinfecting and resisting corrosion, accelerating absorption and the like, and is mainly used for treating animal foot rot. According to the nano-emulsion medicine for treating the foot rot, the solubility of the medicine is increased, the medicinal stability and the biological utilization rate are improved, the dosage of the medicine is reduced, the skin transmission rate is higher than that of common preparations including a medicinal extract and the like, and the cost is low, so that the nano-emulsion medicine has a wide market prospect in a veterinary medicine field.

Sprayable, anhydrous and physically / chemically stable dermatological / pharmaceutical compositions, well suited for the treatment of a variety of dermatological disorders, notably psoriasis, contain: a) a therapeutically effective amount of a solubilized corticoid, notably dissolved clobetasol propionate; b) a therapeutically effective amount of a solubilized vitamin D derivative, notably dissolved calcitriol; and c) an alcohol phase; and d) an oily phase which comprises one or more oils; formulated into e), a sprayable and topically applicable, dermatologically / pharmaceutically acceptable vehicle therefor.

Stable, topically applicable, non-greasy and non-tacky oil-in-water (O / W) anti-inflammatory emulsions, useful, e.g., for the treatment of psoriasis, contain: a. a therapeutically effective amount of at least one steroidal anti-inflammatory agent, notably clobetasol propionate; b. a pro-penetrating system which includes at least one pro-penetrating glycol and at least one other pro-penetrating agent; and c. at least one polymeric emulsifier not sensitive to electrolytes, for example not an acrylate / C10-C30 alkyl acrylate copolymer, formulated into a topically applicable, pharmaceutically acceptable vehicle therefor.

The present invention provides a method for treating psoriasis, by spraying onto the skin with psoriasis daily for at least 4 weeks a pharmaceutical composition containing an effective amount of clobetasol propionate. A preferred pharmaceutical composition containing clobetasol propionate, ethyl alcohol, isopropyl myristate, and anionic surfactant.

Topically applicable pharmaceutical compositions useful for the treatment of psoriasis contain respective amounts of calcitriol and clobetasol propionate permitting a once-per-day effective regimen of topical application onto the part or parts of the skin affected by psoriasis.

A new topical formulation is provided, with a high chemical stability, of for example a low dose clobetasol propionate, suitable for the topical treatment of skin and mucous membrane conditions associated with disorders including psoriasis, eczema, and other forms of dermatitis and also topical use associated with the mouth, such as lichen planus. The formulation includes an aqueous vehicle of based on propylene glycol as a solvent and moisture-retaining agent, and macrogol-glycerol hydroxystearate as a non-ionic emulsifier, being capable of holding surprisingly low concentrations of clobetasol. The vehicle holds concentrations about 0.005% to about 0.05% by weight of 17-clobetasol propionate, more preferably about 0.02 to 0.025%, even more preferably 0.025% by weight of 17-clobetasol propionate. The formulation has a good chemical stability, resulting in a long durability.

The invention provides a compound clobetasol propionate liposome and a preparation thereof, which are mainly used for treating diseases such as psoriasis vulgaris, dermatitis, eczema and the like. The liposome prepared from neutral synthetic phospholipids, lipids with positive charges, and cholesterol can coat clobetasol propionate and vitamin A acid simultaneously, and is added with a cream substrate or gel substrate to be prepared into compound clobetasol propionate liposome cream or gel. Compared with the common cream, the liposome preparation has the advantages that: the amount of the medicine retained in skin is larger, the skin penetration rate is lower, the content of the medicine in local skin can be improved, the treatment index is improved, and transdermal absorption dose is reduced, so that the toxic and side effects of the medicine are reduced.

The invention discloses a preparation method of clobetasol and the preparation method of clobetasol propionate. The preparation method of the clobetasol comprises the following steps: by taking a compound I, namely 1,4,9(11)-triene androstane-3,17-diketone as an initial raw material, performing a methylation reaction, a cyan substitution reaction, a siloxy protection reaction, an intramolecular nucleophilic substitution reaction, a bromoepoxy reaction and a fluorination reaction to prepare a compound VII which is clobetasol. The compound VII is subjected to a propyl esterification reaction to prepare a compound VIII which is clobetasol propionate. According to the preparation method disclosed by the invention, since relatively basic initial raw materials which are cheap are used, each step of reaction is relatively easy to implement and high yield is achieved; the operation of multi-step protection and deprotection is simplified; moreover, 21 sites of fluorine are directly arranged in one step during arrangement of a side chain, and multiple steps of reaction for arranging the 21 sites of fluorine in the prior art are directly avoided, so that the synthetic route is greatly shortened, the total yield is increased, the product quality is improved and the production cost is greatly lowered.

Two or three external therapeutic options such as clobetasol propionate spray, calcitriol ointment, and excimer laser phototherapy are used to treat generalized psoriasis with systemic safety and better efficacy than any systemic or biologic agent. Combinations of these agents, for example used in parallel and / or series for specific durations, can achieve a significant result: a PASI 75 response after only four weeks and / or a PASI 95-100 response after only six weeks.

The invention provides a preparation method of an intermediate of a steroidal drug with a 16-beta-methyl. In the method, a steroidal compound I is used as a starting material, and a steroidal compound II of the intermediate of the steroidal drug with the 16-beta-methyl can be prepared through epoxy reaction, ketal reaction, addition reaction and hydrolysis reaction for transformation of Position 3, Position 16, Position 17 and Position 20 or Position 16, Position 17 and Position 20. The steroidal compound II with the 16-beta-methyl is generally applied in preparation of the glucocorticoid drugs commonly used in clinical operation, such as betamethasone, betamethasone sodium phosphate, betamethasone acetate, clobetasol propionate, beclometasone dipropionate, betamethasone valerate and the like. In the formulas of the steroidal compound I and the steroidal compound II, R represents OH or OCOCH3, R1 represents OH, R2 represents CH3, and R3 represents CH3.

The invention provides a compound clobetasol propionate mixed micellar solution. Phosphatide and cholate are mainly utilized to prepare the mixed micellar solution which is used for packaging clobetasol propionate and tretinoin. The mixed micelle solution can be simply prepared, and the medicament stability can be guaranteed in the process of preparation. By preparing a mixed micelle system from the phosphatide and the cholate, the problem of medicament dissolution is solved. Compared with a common ointment, the mixed micelle solution has a higher retention volume on skins, and the quantity of the medicament on local skins and the therapeutic index can be increased. The mixed micelle solution can be further prepared into an ointment and a gel, and is mainly used for treating psoriasis vulgaris, dermatitis, eczema, etc.

The invention provides a preparation method of an intermediate of a steroidal drug with a 16-beta-methyl. In the method, a steroidal compound I is used as a starting material, and a steroidal compound II of the intermediate of the steroidal drug with the 16-beta-methyl can be prepared through epoxy reaction, ketal reaction, hydrogenation reaction, addition reaction and hydrolysis reaction for transformation of Position 3, Position 5, Position 6, Position 16, Position 17 and Position 20 or Position 5, Position 6, Position 16, Position 17 and Position 20. The steroidal compound II with the 16-beta-methyl is generally applied in preparation of the glucocorticoid drugs commonly used in clinical operation, such as betamethasone, betamethasone sodium phosphate, betamethasone acetate, clobetasol propionate, beclometasone dipropionate, betamethasone valerate and the like. In the formulas of the steroidal compound I and the steroidal compound II, R represents OH or OCOCH3, R1 represents OH, R2 represents CH3, and R3 represents CH3.

The invention discloses a preparing method of chlorotestosterone betaprodine, which comprises the following steps: blending betamisong 17-propionic ester sulphonation and anhydrous lithium chloride with the rate at 1: 1-2; dissolving in the DMF to do chloridization reaction; elutriating through icy water; drying through centrifuging to obtain rough product; dissolving rough product in the carbinol or alcohol; adding activated charcoal; decoloring; filtering; recycling activated charcoal; condensing the filtrate; crystallizing; dehydrating; drying to obtain the product.

The invention discloses an externally-used medicament for treating skin mycosis diseases, which is prepared from the raw materials of (by weight percent) terbinafine hydrochloride or miconazole or ketoconazole 0. 5-2%, Clobetasol Propionate 0. 01-0. 2%, neomycin sulphate 0. 3-1%, bee glue 5-25%, and balancing distilled water.

A medicine for treating psoriasis vulgaris contains clobetasol propionate and vitamin A acid. Its preparing process is also disclosed. Its advantages are high curativ effect, and low toxic by-effect.

The invention discloses a solution for removing dandruff and its preparing process, wherein the solution is prepared from rhubarb horsetails, flavescent sophora root, Chinese dittany bark, poria cocos, rough gentian, boneol, menthol, ketoconazole, Clobetasol Propionate, propylene glycol, glycerin, azone, polysorbate -80 and sodium benzoate through charging the first five Chinese herbs into water, boiling, concentrating the filtrate, charging ketoconazole, Clobetasol Propionate, boneol, menthol and auxiliary materials, finally keeping constant volume by charging ethanol.

The invention discloses an oil-in-water compound ketoconazole nano-medicament. The grain diameter of the medicament is 1-100nm. The oil-in-water compound ketoconazole nano medicament comprises the following raw materials in percentage by weight: 0.01-8.0 percent of ketoconazole, 0.01-10 percent of eugenol, 0.001-5.0 percent of clobetasol propionate, 25.0-45.0 percent of surfactant, 0-10.0 percentof cosurfactant, 0.1-25.0 percent of oil and the balance of distilled water. The oil-in-water compound ketoconazole nano-medicament can be used for treating stubborn skin mycotic infection, mycodermatitis, chronic mucocutaneous candidiasis, dermatitis blastomycosis, coccidioidomycosis, histoplasmosis, chromoblastomycosis and paracoccidioidomycosis, and dermatomycosis and tinea versicolor caused by dermatophyte and microzyme as well as trichophyton disease, scytitis and pruritus. The oil-in-water compound ketoconazole nano-medicament has the advantages of strong osmosis, favorable stability, favorable infiltrating property, durable acting time, remarkable effect, low cost, simple preparation method and convenience in popularization and application.

The invention discloses a method for synthesizing clobetasol propionate, which belongs to the technical field of synthesis of steroid medicaments in the pharmaceutical chemistry and comprises the following steps: (1) dissolving betamethasone-17-ester into acetone solution; (2) adding a catalyst and BTC (bis(trichloromethyl) carbonate) for carrying out chloroacetic reaction at the reaction temperature of 30-50DEG C for 2-5 hours; and (3) after reaction, carrying out reduced pressure concentration, elutriation, filtering and drying. Compared with the traditional process, the yield can be improved by 6 percent, the cost is reduced by 20 percent and the quality is remarkably improved. The using amount of original auxiliary materials are reduced by 20 percent, the using amount of a toxic material of methanesulfonyl chloride can be reduced by 1 ton each year, the using amount of DMF (Dimethyl Formamide) can be reduced by 17 tons and the using amount of pyridine can be reduced by 6.3 tons, the economic cost can be totally saved by 366,000 yuan and waste water drain can be reduced by 310tons / year; and in addition, the invention greatly reduces the pressure for protecting the environment and can effectively reduce the hazard on human body and the pollution on the environment.

The invention provides an externally applied medicament for treating vitiligo, which relates to medicaments for treating vitiligo. The medicament consists of dark plum fruits, angelica dahurica roots, green husk, green walnut shells, lithospermum, Chinese arborvitae twig, malaytea scurfpea fruits, green eggplant, Chinese ilex leaves, Chinese dodder seeds, clobetasol propionate, laurocapram, chloroform and 90 percent alcohol. A making process comprises: a, soaking the dark plum fruits and the other 10 raw materials in alcohol for 5 to 7 days and forming Chinese medicinal liquid through filtration; b, dissolving clobetasol propionate with chloroform; c, adding clobetasol propionate solution and laurocapram to the Chinese medicinal liquid; and d, adding distilled water for dilution. In general, the raw medicinal materials cooperate to improve immunity by expanding blood vessels, releasing toxin and dispelling wind; brown pigment of the medicament is fully utilized and absorbed; tyrosinase is generated by stimulating skin so as to regenerate pigment; and the pigment is stabilized through allergy resistance. The medicament has the advantages of capability of treating both primary and secondary symptoms, rapid efficacy, safety, reliability, using convenience and good therapeutic effects. 110 clinical trials show that the total effective rate of the medicament reaches 94.5 percent.

Topically applicable pharmaceutical gel, cream, lotion, solution or ointment compositions contain synergistically effective amounts of a) calcitriol and b) clobetasol propionate, formulated into a topically applicable, pharmaceutically acceptable medium therefor, and are useful for the treatment of such dermatological afflictions or conditions as psoriasis, atopic dermatitis, contact dermatitis and seborrhoeic dermatitis.

A new topical formulation is provided, with a high chemical stability, of for example a low dose clobetasol propionate, suitable for the topical treatment of skin and mucous membrane conditions associated with disorders including psoriasis, eczema, and other forms of dermatitis and also topical use associated with he mouth, such as lichen planus. The formulation includes an aqueous vehicle of based on propylene glycol as a solvent and moisture-retaining agent, and macrogol-glycerol hydroxystearate as a non-ionic emulsifier, being capable of holding surprisingly low concentrations of clobetasol. The vehicle holds concentrations about 0.005% to about 0.05% by weight of 17-clobetasol propionate, more preferably about 0.02 to 0.025%, even more preferably 0.025% by weight of 17-clobetasol propionate. The formulation has a good chemical stability, resulting in a long durability.

A spray foaming dosage form comprising clobetasol propionate, dimethyl isosorbide, propylene glycol, polysorbate, sodium dodecyl sulphate, buffer, optional preservative, optional further excipients, and water.

Seborrheic dermatitis is effectively / safely treated by topically applying a corticosteroid shampoo, notably a clobetasol propionate shampoo, onto the scalp of a human subject afflicted therewith.

The present invention is externally applied emulsion for treating dermatitis and eczema, and the emulsion is prepared with clobetasol propionate in 1 weight portions and borneol in 30-50 weight portions as the effective components and through conventional preparation process. The material for the emulsion includes also excipient of octadecanol, stearic acid, glycerol monostearate, liquid paraffin, glycerin, HR-S1 emulsifier, emulsifying silica oil and ethyl hydroxybenzoate. Animal experiments show that the emulsion of the present invention has the functions of resisting inflammation, resisting eczema, stopping itch and relieving pain, and may be used in clinical experiment.

The invention discloses a method for measuring clobetasol propionate in products used for promoting the growth and the development of hairs; the method comprises the steps of: preparing a sample to be tested; carrying out ultra-high performance liquid chromatography measurement on the sample to be tested; adopting a BEH C18 (2.1*50mm, 1.7mu m) chromatographic column with the column temperature of 35-45 DEG C; taking acetonitrile and water as moving phases, and carrying out gradient elution; controlling the constant flow speed to be 0.3-0.4mL / min; and taking Waters personal digital assistant (PDA) as a detector, wherein the detection wavelength is 230-240nm. After being used for detecting the content of the clobetasol propionate in the products used for promoting the growth and the development of the hairs, the method is low in detection limit, high in degree of accuracy, simple in pretreatment and very suitable for the rapid batch detection of the clobetasol propionate in the products used for promoting the growth and the development of the hairs; and the method provides the important technical support for the quality control and safety monitoring of cosmetic products, and has good economic and social benefits.

The invention provides an acne removing preparation with no side effect and good curative effect. The preparation comprises the following components in percentage by weight: 28-56 percent of ketoconazole and clobetasol propionate cream, 20-28 percent of lincomycin hydrochloride gel, 8-20 percent moroxydine hydrochloride, 4-10 percent of metronidazole and 10-40 percent of traditional Chinese medicinal extract, wherein the traditional Chinese medicinal extract comprises extract of white peony root, white poria, bighead atractylodes rhizome and angelica root. The acne removing preparation is effectively combined with traditional Chinese medicines and western medicines, can be used for quickly removing pox and acne, and has the effect of whitening.