CN1775212A - Use of pirfenidone for treating psoriasis - Google Patents
Use of pirfenidone for treating psoriasis Download PDFInfo
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- CN1775212A CN1775212A CN 200410090851 CN200410090851A CN1775212A CN 1775212 A CN1775212 A CN 1775212A CN 200410090851 CN200410090851 CN 200410090851 CN 200410090851 A CN200410090851 A CN 200410090851A CN 1775212 A CN1775212 A CN 1775212A
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- pirfenidone
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- psoriasis
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Abstract
The present invention relates to an application of pyrifenidone in preparation of medicine for curing psoriasis. It can be oral administration or used for external application.
Description
Technical field
The present invention relates to treat psoriasic new drug; Particularly, the present invention relates to pirfenidone (Pirfenidone), the pharmaceutical usage that 5-methyl isophthalic acid-phenyl-2-(1H)-pyridone is new.More specifically, the present invention relates to the application of pirfenidone in preparation antipsoriatics thing.
Background technology
Psoriasis is a kind of dermatosis of keratinization of epidermis.When new chrotoplast forms in the low layer epidermis, and psoriasis just takes place when faster in speed from old chrotoplast to the speed of upper strata epidermis motion that come off at the skin watch than of described new skin.Because above-mentioned mechanism with other, formed the skin rashes and the speckle of the inflammation thickening that covers by dead bark layer in blocks (being scale).Therefore, psoriasic symptom comprises unusual red (being erythema) and the scleroma that produces because of inflammation, and the scale of silver color and lamination may occur.Psoriasis is shown effect usually in the surface of scalp and extremity extensor, for example positions such as elbow, lacquer, shin and vola and palm.Psoriasis is a kind of poignant chronic dermatosis, and sickness rate is higher, does not up to the present still have specific medicament and Therapeutic Method.
Except that psoriasis, other keratinization of epidermis and/or flaky skin disease are characterised in that lichenification/scleroma, scale, erythema and pruritus, and these dermatosiss include but not limited to the dermatosis of lichen chronicus simplex, lichenification atopic dermatitis, keratinization of epidermis palm dermatitis and non-specific keratinization of epidermis chronic dermatitis and so on.These dermatosiss can occur in trunk, extremity, scalp and other anatomy position.Treat many uses of these dermatosiss and the same medicine of treatment psoriasis.
The same with psoriasis, other keratinization of epidermis and/or flaky skin disease still can not be cured fully, therefore, still need the medicine and the method for more effective treatment psoriasis and other keratinization of epidermis and/or flaky skin disease.
USP 3,839, and 346 (1974.10.1 announcements) disclose the preparation method of some N-replacement 2-(1H)-pyridone.USP 3,947,281 (1976.8.10 announcements), USP 4,042,699 (1977.8.16) and USP 4,052,509 (1977.10.4) have further described wherein a kind of Compound P irfenidone, 5-methyl isophthalic acid-phenyl-2-(1H)-pyridone, Chinese translation pirfenidone, this chemical compound can reduce uric acid and concentration of glucose in the blood plasma, is used for the treatment of people and mammiferous upper respiratory tract infection and skin infection.Pirfenidone can suppress the synthetic of collagen, reduces the generation of various kinds of cell kinetins, the former new hypertrophy of barrier fibers.USP 5,310,562 and EP 0 383 591 in described Pirfenidone and be widely used aspect the fibrotic disease in prevention and treatment.This medicine is a kind of oral active small molecular medicine, is gone on the market by drugs approved by FDA, and it is clinical that the treatment of the fibrotic disease of lung, kidney regulating liver-QI has been entered the II phase.
In recent years, pirfenidone also there is extensive studies in the application of others.For example, WO00/16775 has described and pirfenidone is used for the treatment of and has prevented dermatosis, the particularly pathological changes of fibrosis character, as the fibrosis damaged tissue, and wart contagious, contact dermatitis, burn and cicatrix etc.WO99/47140 discloses application 2-(1H)-pyridine compounds, particularly pirfenidone and has prepared partly sterilised's compositions, can be used for many surfaces (comprising skin surface etc.) antibacterial, fungus and/or virus are handled.WO01/62253 discloses and can use N-replacement 2-(1H)-pyridine compounds, comprises the pirfenidone treatment epilepsy.
But up to the present, still the no-trump pirfenidone is used for the treatment of psoriasic report.
Summary of the invention
The purpose of this invention is to provide the psoriasic new drug of a kind of treatment.
Further, the purpose of this invention is to provide and a kind ofly be used for the treatment of psoriasicly, contain pirfenidone, the medicine of 5-methyl isophthalic acid-phenyl-2-(1H)-pyridone.
That is to say, the present invention relates to the application of pirfenidone in preparation antipsoriatics thing.
When pirfenidone is used for the treatment of psoriasis, can adopt oral and route of administration topical application, preferred topical application.
Pirfenidone is used for when oral, can be made into conventional peroral dosage form, for example is tablet, capsule or liquid preparation (suspensoid, syrup or solution).The daily dose of oral formulations is 300-3000mg, can once fear into or fear several times into, but preferably with 2-4 time dosed administration, every day three times for example, each 100-800mg, preferably 300-800mg.
When the pirfenidone part was tried out, the preparation that is adopted can be the external preparation of this area routine, comprises solution, cream, ointment, gel, washing liquid, suspension or emulsion etc.No matter use which kind of dosage form, the concentration of pirfenidone should be at about 0.1%-5% (wt/wt), and each amount of application is equivalent to about 1-5mg, every day 1-4 time.
Embodiment
Further specify the present invention below by specific embodiments.Described embodiment only is used for explanation or explains embodiment of the present invention, and can not limit protection scope of the present invention.Employed raw material among the embodiment, except that pirfenidone, other composition all can have been bought on market.
Embodiment 1 pirfenidone tablets
Composition consumption (mg/ sheet)
Pirfenidone 500mg
Microcrystalline Cellulose 430mg
Silica sol 20mg
Stearic acid 10mg
Mentioned component is mixed, and be pressed into tablet, every heavy 1000mg.
Embodiment 2 pirfenidone capsule
Composition consumption (mg/ capsule)
Pirfenidone 400mg
Starch 295mg
Magnesium stearate 5mg
Mentioned component is mixed, and insert gelatine capsule, the heavy 700mg of each capsule.
Similarly, according to the conventional method of this area,, can prepare the various oral formulations that contain pirfenidone, as solution, granule, powder, syrup, suspension etc. by means of carrier that is applicable to oral formulations and/or excipient.
Embodiment 3 pirfenidone lotions
Component content
Pirfenidone micropowder 20g
Water 650g
Ethoxydiglycol 230g
GLYCERYL DILAURATE 60g
Two sad propylene glycol ester 40g
Preparation method
Above-mentioned each component is fully obtained 1000g pirfenidone lotion after the dissolving in water.
Embodiment 4 pirfenidone ointment
Component content
Pirfenidone micropowder 20g
Hexanediol 120.0g
Pure water 40.0g
White beeswax 60.0g
Propylene glycol stearate 30.0g
White vaseline adds to 1000g
Preparation method
1, vaseline is positioned in the proper container, is heated to 90 ℃;
2, vaseline is cooled to 70 ℃, adds white beeswax and propylene glycol stearate, stir and melt;
3, hexanediol and pure water are mixed in another container, obtain homogeneous phase solution, be heated to 50-55 ℃;
4, the pirfenidone micropowder is added the solution of step 3, mix;
5, the liquid with step 4 adds in the fused solution of step 2, stirring and evenly mixing, and make its temperature drop to room temperature, obtain level and smooth ointment uniformly.
As required, wherein the content of pirfenidone micropowder can be regulated between 1.0-20mg/g.
Similarly, according to the conventional method of this area, by means of carrier that is applicable to topical formulations and/or excipient, can prepare the preparation of the various topical application that contain pirfenidone, as cream, gel, washing liquid, suspension or emulsion etc.
The psoriasic effect of embodiment 5 usefulness pirfenidone treatment
With pirfenidone to the psoriatic through the part or oral medication after 8 weeks, it the results are shown in following table.Wherein said percent is relative effective percentage.
Table 1 pirfenidone is to psoriatic's scale (scaling), the effect of scleroma (induration), erythema (erythema) and PASI
| Contrast ** n＝-15 | The oral 800mg/ of pirfenidone day n=15 | Pirfenidone part 3～5mg/ day n=15 | |
| Scale | 0 | 30％±4 *** | 72％±10 |
| Scleroma | 0 | 15％±5 | 45％±7 |
| Erythema | 0 | 12％±7 | 51％±11 |
| The PASI scoring * | 0 | 10％±3 | 70％±9 |
*: the serious index of PASI-psoriasis area (Psoriasis Area Severity Index) is the major parameter of reflection wholistic therapy effect;
*: matched group is used the same preparation that does not contain active component;
* *The numeral of " ± " number back is a standard deviation.
According to result of the test as can be seen, has beyond thought effect with the pirfenidone treatment psoriasis.
Be understandable that according to the general knowledge of medical domain, those of ordinary skill in the art can carry out various modifications and improvement to technical scheme of the present invention, the mutation of these related art scheme should be within the protection domain of the application's claims.
Claims (5)
1. the application of pirfenidone in preparation antipsoriatics thing.
2. according to the application of claim 1, wherein said medicine is the medicine of local application.
3. according to the application of claim 2, the medicine of wherein said local application is ointment or lotion.
4. according to the application of claim 1, wherein said medicine is the medicine that is suitable for oral administration.
5. according to the application of claim 4, wherein said medicine is tablet or capsule.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN 200410090851 CN1775212A (en) | 2004-11-16 | 2004-11-16 | Use of pirfenidone for treating psoriasis |
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN 200410090851 CN1775212A (en) | 2004-11-16 | 2004-11-16 | Use of pirfenidone for treating psoriasis |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| CN1775212A true CN1775212A (en) | 2006-05-24 |
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Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CN 200410090851 Pending CN1775212A (en) | 2004-11-16 | 2004-11-16 | Use of pirfenidone for treating psoriasis |
Country Status (1)
| Country | Link |
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| CN (1) | CN1775212A (en) |
Cited By (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN101953836A (en) * | 2010-08-13 | 2011-01-26 | 中南大学 | Application of fluoropirfenidone in preparing medicaments for treating psoriasis |
| CN101972230A (en) * | 2010-10-13 | 2011-02-16 | 北京诚创康韵医药科技有限公司 | Pirfenidone for suspension and preparation method |
| CN104780762A (en) * | 2012-08-31 | 2015-07-15 | 英特姆尼国际公司 | Methods of administering pirfenidone therapy |
-
2004
- 2004-11-16 CN CN 200410090851 patent/CN1775212A/en active Pending
Cited By (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN101953836A (en) * | 2010-08-13 | 2011-01-26 | 中南大学 | Application of fluoropirfenidone in preparing medicaments for treating psoriasis |
| CN101972230A (en) * | 2010-10-13 | 2011-02-16 | 北京诚创康韵医药科技有限公司 | Pirfenidone for suspension and preparation method |
| CN104780762A (en) * | 2012-08-31 | 2015-07-15 | 英特姆尼国际公司 | Methods of administering pirfenidone therapy |
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