CN1210035C - Complex external medicine for treating psoriasis - Google Patents
Complex external medicine for treating psoriasis Download PDFInfo
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- CN1210035C CN1210035C CN 03158379 CN03158379A CN1210035C CN 1210035 C CN1210035 C CN 1210035C CN 03158379 CN03158379 CN 03158379 CN 03158379 A CN03158379 A CN 03158379A CN 1210035 C CN1210035 C CN 1210035C
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- tazarotene
- effective active
- medicine
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Abstract
The present invention relates to a compound medicine for external use for treating psoriasis, which is characterized in that the effective active components (weight percentage) of 0.025 to 0.1% of tazarotene and 0.01 to 0.2% of cortical hormone are contained in a matrix carrier of the compound medicine for external use. The present invention has the advantages that the target site of the tazarotene to the selective action on a receptor is obvious, the stability is improved, the tazarotene is mainly reserved in skin when in local application, the metabolism is rapid, and the tazarotene is penetrated into a system without by skin nearly, the irritation of local skin is light, and adverse reaction of a whole body almost does not exist. The tazarotene has good complementary and synergistic effects on the medicine effect after being combined with the cortical hormone, and the adverse reaction can be balanced out.
Description
Technical field:
The present invention relates to the psoriatic external used medicine of a kind of treatment, the psoriatic compound external-use medicine of especially a kind of treatment.
Background technology:
Psoriasis is the cell-mediated immunity inflammatory disease of the T of polygenes and gene pleiomorphism genetic background, and pathogenesis is very complicated.Activated T cell, inflammatory cell and interact based on the skin tissue cell of keratinocyte form whole body and a series of performances of local skin and each clinical subtype, difficult point and focus that psoriatic treatment problem is domestic and international dermatological studies always.
The therapeutical effect of psoriasis Drug therapy present situation and existing medicine all is can only be at the part in the pathogenesis link of psoriasis complexity, the development of new drug and novel formulation and the effort of clinical therapeutics do not have the breakthrough of matter for a long time, can only make adjustment on benefit-risk ratio, its countermeasure comprises: 1 development targeting, the new drug that selectivity is high; 2 research conjoint therapies, treatment new departure of sequential therapy and rotational therapy; 3 choose reasonable or dual purpose system and topical remedy; 4 optimize externally used compound preparation.Purpose is all and heightens the effect of a treatment and alleviate untoward reaction.At present, this type of medicine all is subjected to intrinsic toxicity itself and optionally restriction, thereby curative effect is limited, and untoward reaction is several can not exempt from, and the polygenic inheritance essence and the Drug therapy of disease can not solve the recurrence problem, makes needs of patients for a long time, repeatedly and even lifelong administration.
Summary of the invention:
The objective of the invention is to: the problem at existing in the psoriatic conventional treatments of treatment provides a kind of new treatment psoriatic compound external-use medicine.The present invention is development and optimizes new local topical compound preparation, is intended to develop distinctive new drug, can strengthen the curative effect of principal agent and the untoward reaction that alleviates principal agent to a certain extent, reaches and improves present psoriatic Therapeutic Method present situation.
The object of the present invention is achieved like this: the psoriatic compound external-use medicine of a kind of treatment, it is characterized in that: contain following effective active composition (percentage by weight) in the medium carrier of compound external-use medicine: tazarotene 0.025～0.1%, 17-hydroxy-11-dehydrocorticosterone 0.01～0.2%, described 17-hydroxy-11-dehydrocorticosterone selects 17 for use, the 21-clobetasol propionate, or 17,21-diflorasone, or 17-betamethasone valerate, or 17,21-beclomethasone, or omcilon, or 17-clobetasone butyrate.
The 17-hydroxy-11-dehydrocorticosterone content that contains in the described medium carrier is: 17,21-clobetasol propionate 0.01～0.1%, or 17,21-diflorasone 0.01～0.1%, or 17-betamethasone valerate 0.05～0.2%, or 17,21-beclomethasone 0.01～0.1%, or omcilon 0.05～0.2%, or 17-clobetasone butyrate 0.01～0.1%.
The effective active composition that described compound external-use medicine contains forms ointment or ointment with after medium carrier mixes
The invention has the advantages that: tazarotene is a third generation tretinoin medicines, it is the tretinoin that local skin is used, compare with first generation tretinoin, it is clear and definite to have the receptor-selective target site, improved stability, topical application mainly retain in skin, metabolism is rapid, and percutaneous penetrates in the system hardly, the local skin zest is lighter relatively, and several no whole bodies have no adverse reaction.Prove that at present its independent local topical treatment psoriasis in plaques is effective, and the independent effect of first generation tretinoin is relatively poor, its drug action comprises regulates the keratinocyte differentiation, antiproliferative, and antiinflammatory action.
General superpower effect, the potent class used of 17-hydroxy-11-dehydrocorticosterone topical therapeutic psoriasis, its mechanism is the abnormal cell factor, adhesion molecule, inflammatory mediator, the chemotactic factor that suppresses epithelial cell proliferation, suppresses T cytoactive, inhibition monokaryon one macrophage, fibroblast, vascular endothelial cell and the inflammatory cell expression of local infiltration, thus inflammation-inhibiting.
Tazarotene and 17-hydroxy-11-dehydrocorticosterone share very strong complementation and synergism on drug effect, make the target spot at the psoriasis pathology link enlarge and strengthen, thereby strengthen clinical efficacy.
The tazarotene external can cause certain skin irritation inflammation in addition, and the long-term external of 17-hydroxy-11-dehydrocorticosterone can cause atrophoderma.And tazarotene has anti-atrophoderma effect, and cortical hormone have anti-inflammatory effect, thereby the untoward reaction that two medicines share this two aspect can be offset.
The specific embodiment:
Below the nonrestrictive part embodiment that the present invention relates to that exemplified.
Embodiment 1:
The effective active composition of present embodiment adopts tazarotene 0.1% (percentage by weight, down together) and 17,21-clobetasol propionate 0.1%, and medium carrier adopts liquid paraffin, wool grease, emulsifying agent, antioxidant, ethanol, propylene glycol and vaseline.
Embodiment 2:
The effective active composition of present embodiment adopts tazarotene 0.025% and 17,21-diflorasone 0.1%, and medium carrier adopts liquid paraffin, wool grease, emulsifying agent, antioxidant, ethanol, propylene glycol and vaseline.
Embodiment 3:
The effective active composition of present embodiment adopts tazarotene 0.1% and 17-betamethasone valerate 0.2%, and medium carrier adopts liquid paraffin, wool grease, emulsifying agent, antioxidant, ethanol, propylene glycol and vaseline.
Embodiment 4:
Earlier two kinds of effective active compositions among embodiment 1 or embodiment 2 or the embodiment 3 are dissolved in the ethanol of total amount 5～10% stand-by; The liquid paraffin of total amount 5～10%, the wool grease of total amount 8～15%, an amount of emulsifying agent, an amount of antioxidant and vaseline are mixed and heated to 70 ℃; After the propylene glycol of total amount 10～20% is heated to 70 ℃, the mixture that adds liquid paraffin, wool grease, emulsifying agent, antioxidant and vaseline stirs, to be cooled during to 60 ℃, add oneself and be dissolved with the ethanol of two kinds of effective active compositions, transfer to the medicine gross weight with an amount of vaseline at last, restir evenly forms ointment.
Embodiment 5:
The effective active composition of present embodiment adopts tazarotene 0.05% and 17,21-beclomethasone 0.05%, medium carrier adopts hexadecanol, vaseline, liquid paraffin, glyceryl monostearate, solubilizing agent, emulsifying agent, glycerol, ethyl hydroxybenzoate and distilled water.
Embodiment 6:
The effective active composition of present embodiment adopts tazarotene 0.1% and omcilon 0.1%, and medium carrier adopts hexadecanol, vaseline, liquid paraffin, glyceryl monostearate, solubilizing agent, emulsifying agent, ethyl hydroxybenzoate and distilled water.
Embodiment 7:
The effective active composition of present embodiment adopts tazarotene 0.1% and 17-clobetasone butyrate 0.1%, and medium carrier adopts hexadecanol, vaseline, liquid paraffin, glyceryl monostearate, solubilizing agent, emulsifying agent, ethyl hydroxybenzoate and distilled water.
Embodiment 8:
Earlier the ethyl hydroxybenzoate with two kinds of effective active compositions among embodiment 5 or embodiment 6 or the embodiment 7 and 0.1% is dissolved in the solubilizing agent; Again the hexadecanol of total amount 8～12%, the vaseline of total amount 5～10%, the liquid paraffin of total amount 8～12%, the glyceryl monostearate and an amount of emulsifier of total amount 5～10% are heated to 80～85 ℃; The glyceride of total amount 0.5～5% and an amount of distilled water are mixed and heated to 80～85 ℃, and with the mixture mixing and emulsifying of itself and above-mentioned hexadecanol, vaseline, liquid paraffin, glyceryl monostearate and emulsifying agent; Mixture after the emulsifying is left thermal source, stir when being cooled to 65 ℃, add the solubilizing agent that is dissolved with two kinds of effective active compositions and ethyl hydroxybenzoate, the formation ointment stirs.
Claims (3)
1, the psoriatic compound external-use medicine of a kind of treatment, it is characterized in that: contain following effective active composition (percentage by weight) in the medium carrier of compound external-use medicine: tazarotene 0.025～0.1%, 17-hydroxy-11-dehydrocorticosterone 0.01～0.2%, described 17-hydroxy-11-dehydrocorticosterone selects 17 for use, the 21-clobetasol propionate, or 17,21-diflorasone, or 17-betamethasone valerate, or 17,21-beclomethasone, or omcilon, or 17-clobetasone butyrate.
2, the psoriatic compound external-use medicine of treatment according to claim 1, it is characterized in that: 17-hydroxy-11-dehydrocorticosterone in the effective active composition that contains in the described medium carrier and content thereof are 17,21-clobetasol propionate 0.01～0.1%, or 17,21-diflorasone 0.01～0.1%, or 17-betamethasone valerate 0.05～0.2%, or 17,21-beclomethasone 0.01～0.1%, or omcilon 0.05～0.2%, or 17-clobetasone butyrate 0.01～0.1%.
3, the psoriatic compound external-use medicine of treatment according to claim 1 is characterized in that: the effective active composition that described compound external-use medicine contains forms ointment or ointment with after medium carrier mixes.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN 03158379 CN1210035C (en) | 2003-09-29 | 2003-09-29 | Complex external medicine for treating psoriasis |
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN 03158379 CN1210035C (en) | 2003-09-29 | 2003-09-29 | Complex external medicine for treating psoriasis |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| CN1528313A CN1528313A (en) | 2004-09-15 |
| CN1210035C true CN1210035C (en) | 2005-07-13 |
Family
ID=34287281
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CN 03158379 Expired - Lifetime CN1210035C (en) | 2003-09-29 | 2003-09-29 | Complex external medicine for treating psoriasis |
Country Status (1)
| Country | Link |
|---|---|
| CN (1) | CN1210035C (en) |
Families Citing this family (5)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| EP2612665A1 (en) | 2012-01-09 | 2013-07-10 | Almirall S.A. | Topical pharmaceutical compositions comprising bexarotene and a corticosteroide |
| CA2857207A1 (en) | 2012-01-09 | 2013-07-18 | Almirall, S.A. | Topical pharmaceutical compositions comprising bexarotene and a corticosteroide |
| AU2016279801B2 (en) * | 2015-06-18 | 2021-09-09 | Valeant Pharmaceuticals North America | Topical compositions comprising a corticosteroid and a retinoid for treating psoriasis |
| CN106539751A (en) * | 2017-01-17 | 2017-03-29 | 景德镇牧堂陶瓷科技有限公司 | A kind of Beclomethasone dipropionate emulsifiable paste and preparation method thereof |
| US11311482B2 (en) | 2017-05-12 | 2022-04-26 | Bausch Health Us, Llc | Topical compositions and methods for treating skin diseases |
-
2003
- 2003-09-29 CN CN 03158379 patent/CN1210035C/en not_active Expired - Lifetime
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| Publication number | Publication date |
|---|---|
| CN1528313A (en) | 2004-09-15 |
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Granted publication date: 20050713 |