CN1210035C - Complex external medicine for treating psoriasis - Google Patents
Complex external medicine for treating psoriasis Download PDFInfo
- Publication number
- 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
- Authority
- CN
- China
- Prior art keywords
- tazarotene
- effective active
- medicine
- skin
- present
- Prior art date
- Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
- Expired - Lifetime
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- 239000003814 drug Substances 0.000 title claims abstract description 23
- 201000004681 Psoriasis Diseases 0.000 title abstract description 8
- OGQICQVSFDPSEI-UHFFFAOYSA-N Zorac Chemical compound N1=CC(C(=O)OCC)=CC=C1C#CC1=CC=C(SCCC2(C)C)C2=C1 OGQICQVSFDPSEI-UHFFFAOYSA-N 0.000 claims abstract description 17
- 229960000565 tazarotene Drugs 0.000 claims abstract description 17
- 150000001875 compounds Chemical class 0.000 claims abstract description 15
- 239000000203 mixture Substances 0.000 claims description 19
- 238000011282 treatment Methods 0.000 claims description 13
- 230000001185 psoriatic effect Effects 0.000 claims description 11
- MFYSYFVPBJMHGN-ZPOLXVRWSA-N Cortisone Chemical compound O=C1CC[C@]2(C)[C@H]3C(=O)C[C@](C)([C@@](CC4)(O)C(=O)CO)[C@@H]4[C@@H]3CCC2=C1 MFYSYFVPBJMHGN-ZPOLXVRWSA-N 0.000 claims description 9
- 239000002674 ointment Substances 0.000 claims description 6
- 229940092705 beclomethasone Drugs 0.000 claims description 5
- 229960004311 betamethasone valerate Drugs 0.000 claims description 5
- 229960004703 clobetasol propionate Drugs 0.000 claims description 5
- 229960005465 clobetasone butyrate Drugs 0.000 claims description 5
- 229960004154 diflorasone Drugs 0.000 claims description 5
- GFNANZIMVAIWHM-OBYCQNJPSA-N triamcinolone Chemical compound O=C1C=C[C@]2(C)[C@@]3(F)[C@@H](O)C[C@](C)([C@@]([C@H](O)C4)(O)C(=O)CO)[C@@H]4[C@@H]3CCC2=C1 GFNANZIMVAIWHM-OBYCQNJPSA-N 0.000 claims description 5
- 230000000694 effects Effects 0.000 abstract description 7
- 230000001054 cortical effect Effects 0.000 abstract description 3
- 229940088597 hormone Drugs 0.000 abstract description 3
- 239000005556 hormone Substances 0.000 abstract description 3
- 230000009471 action Effects 0.000 abstract description 2
- 230000004060 metabolic process Effects 0.000 abstract description 2
- 206010067484 Adverse reaction Diseases 0.000 abstract 2
- 230000006838 adverse reaction Effects 0.000 abstract 2
- 230000000295 complement effect Effects 0.000 abstract 1
- 230000007794 irritation Effects 0.000 abstract 1
- 239000011159 matrix material Substances 0.000 abstract 1
- 230000002195 synergetic effect Effects 0.000 abstract 1
- DNIAPMSPPWPWGF-UHFFFAOYSA-N Propylene glycol Chemical compound CC(O)CO DNIAPMSPPWPWGF-UHFFFAOYSA-N 0.000 description 12
- 229940099259 vaseline Drugs 0.000 description 11
- VBICKXHEKHSIBG-UHFFFAOYSA-N 1-monostearoylglycerol Chemical compound CCCCCCCCCCCCCCCCCC(=O)OCC(O)CO VBICKXHEKHSIBG-UHFFFAOYSA-N 0.000 description 10
- LFQSCWFLJHTTHZ-UHFFFAOYSA-N Ethanol Chemical compound CCO LFQSCWFLJHTTHZ-UHFFFAOYSA-N 0.000 description 10
- 239000003995 emulsifying agent Substances 0.000 description 10
- 229940057995 liquid paraffin Drugs 0.000 description 10
- 239000003963 antioxidant agent Substances 0.000 description 5
- 230000003078 antioxidant effect Effects 0.000 description 5
- 229960001617 ethyl hydroxybenzoate Drugs 0.000 description 5
- NUVBSKCKDOMJSU-UHFFFAOYSA-N ethylparaben Chemical compound CCOC(=O)C1=CC=C(O)C=C1 NUVBSKCKDOMJSU-UHFFFAOYSA-N 0.000 description 5
- 229940075507 glyceryl monostearate Drugs 0.000 description 5
- BXWNKGSJHAJOGX-UHFFFAOYSA-N hexadecan-1-ol Chemical compound CCCCCCCCCCCCCCCCO BXWNKGSJHAJOGX-UHFFFAOYSA-N 0.000 description 5
- 235000019388 lanolin Nutrition 0.000 description 5
- 239000001788 mono and diglycerides of fatty acids Substances 0.000 description 5
- GYCKQBWUSACYIF-UHFFFAOYSA-N o-hydroxybenzoic acid ethyl ester Natural products CCOC(=O)C1=CC=CC=C1O GYCKQBWUSACYIF-UHFFFAOYSA-N 0.000 description 5
- 210000003491 skin Anatomy 0.000 description 5
- 239000002904 solvent Substances 0.000 description 5
- 230000000699 topical effect Effects 0.000 description 5
- SHGAZHPCJJPHSC-YCNIQYBTSA-N all-trans-retinoic acid Chemical compound OC(=O)\C=C(/C)\C=C\C=C(/C)\C=C\C1=C(C)CCCC1(C)C SHGAZHPCJJPHSC-YCNIQYBTSA-N 0.000 description 4
- 239000012153 distilled water Substances 0.000 description 4
- 229960001727 tretinoin Drugs 0.000 description 4
- XLYOFNOQVPJJNP-UHFFFAOYSA-N water Chemical compound O XLYOFNOQVPJJNP-UHFFFAOYSA-N 0.000 description 4
- PEDCQBHIVMGVHV-UHFFFAOYSA-N Glycerine Chemical compound OCC(O)CO PEDCQBHIVMGVHV-UHFFFAOYSA-N 0.000 description 3
- 229940079593 drug Drugs 0.000 description 3
- 239000002547 new drug Substances 0.000 description 3
- 238000003756 stirring Methods 0.000 description 3
- 206010061218 Inflammation Diseases 0.000 description 2
- 206010040799 Skin atrophy Diseases 0.000 description 2
- 230000003110 anti-inflammatory effect Effects 0.000 description 2
- 210000004027 cell Anatomy 0.000 description 2
- 239000003795 chemical substances by application Substances 0.000 description 2
- 238000002651 drug therapy Methods 0.000 description 2
- 230000001804 emulsifying effect Effects 0.000 description 2
- 210000004969 inflammatory cell Anatomy 0.000 description 2
- 230000004054 inflammatory process Effects 0.000 description 2
- 210000002510 keratinocyte Anatomy 0.000 description 2
- 230000008506 pathogenesis Effects 0.000 description 2
- 238000002360 preparation method Methods 0.000 description 2
- 230000001225 therapeutic effect Effects 0.000 description 2
- 238000002560 therapeutic procedure Methods 0.000 description 2
- 206010067482 No adverse event Diseases 0.000 description 1
- 206010040880 Skin irritation Diseases 0.000 description 1
- 230000024932 T cell mediated immunity Effects 0.000 description 1
- 210000001744 T-lymphocyte Anatomy 0.000 description 1
- 230000002159 abnormal effect Effects 0.000 description 1
- 230000001028 anti-proliverative effect Effects 0.000 description 1
- 230000015572 biosynthetic process Effects 0.000 description 1
- 239000005482 chemotactic factor Substances 0.000 description 1
- 238000011262 co‐therapy Methods 0.000 description 1
- 230000004069 differentiation Effects 0.000 description 1
- 201000010099 disease Diseases 0.000 description 1
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 description 1
- 230000000857 drug effect Effects 0.000 description 1
- 230000009977 dual effect Effects 0.000 description 1
- 230000008556 epithelial cell proliferation Effects 0.000 description 1
- 210000002950 fibroblast Anatomy 0.000 description 1
- 238000009472 formulation Methods 0.000 description 1
- 230000002068 genetic effect Effects 0.000 description 1
- 125000005456 glyceride group Chemical group 0.000 description 1
- 230000008595 infiltration Effects 0.000 description 1
- 238000001764 infiltration Methods 0.000 description 1
- 208000027866 inflammatory disease Diseases 0.000 description 1
- 230000002757 inflammatory effect Effects 0.000 description 1
- 230000002401 inhibitory effect Effects 0.000 description 1
- 230000005764 inhibitory process Effects 0.000 description 1
- 230000007774 longterm Effects 0.000 description 1
- 210000002540 macrophage Anatomy 0.000 description 1
- 230000007246 mechanism Effects 0.000 description 1
- 230000007170 pathology Effects 0.000 description 1
- 208000028280 polygenic inheritance Diseases 0.000 description 1
- 230000003389 potentiating effect Effects 0.000 description 1
- 108090000623 proteins and genes Proteins 0.000 description 1
- 238000011450 sequencing therapy Methods 0.000 description 1
- 230000036556 skin irritation Effects 0.000 description 1
- 231100000475 skin irritation Toxicity 0.000 description 1
- 230000008685 targeting Effects 0.000 description 1
- 210000001519 tissue Anatomy 0.000 description 1
- 230000001988 toxicity Effects 0.000 description 1
- 231100000419 toxicity Toxicity 0.000 description 1
- 210000003556 vascular endothelial cell Anatomy 0.000 description 1
Landscapes
- Medicinal Preparation (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
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 |
|---|---|---|---|---|
| EA201400806A1 (en) | 2012-01-09 | 2015-02-27 | Альмираль, С.А. | PHARMACEUTICAL COMPOSITIONS FOR LOCAL APPLICATION CONTAINING BEXAROTEN AND CORTICOSTEROIDS |
| EP2612665A1 (en) | 2012-01-09 | 2013-07-10 | 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
Also Published As
| Publication number | Publication date |
|---|---|
| CN1528313A (en) | 2004-09-15 |
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| Date | Code | Title | Description |
|---|---|---|---|
| C06 | Publication | ||
| PB01 | Publication | ||
| C10 | Entry into substantive examination | ||
| SE01 | Entry into force of request for substantive examination | ||
| C14 | Grant of patent or utility model | ||
| GR01 | Patent grant | ||
| CX01 | Expiry of patent term | ||
| CX01 | Expiry of patent term |
Granted publication date: 20050713 |