CN105327351A - Anti-inflammatory analgesic preparation for external application - Google Patents
Anti-inflammatory analgesic preparation for external application Download PDFInfo
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- CN105327351A CN105327351A CN201410396347.2A CN201410396347A CN105327351A CN 105327351 A CN105327351 A CN 105327351A CN 201410396347 A CN201410396347 A CN 201410396347A CN 105327351 A CN105327351 A CN 105327351A
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Abstract
The invention relates to an anti-inflammatory analgesic preparation for external application. The anti-inflammatory analgesic preparation comprises non-steroid anti-inflammatory analgesic drug and levobupivacaine or pharmaceutically acceptable salt which serve as active ingredients, content of the non-steroid anti-inflammatory analgesic drug is equivalent to 0.1-10% of total weight of the preparation, and content of the levobupivacaine or pharmaceutically acceptable salt is equivalent to 0.01-60% of the total weight of the preparation. The anti-inflammatory analgesic preparation can bring anti-inflammatory analgesic effect of the non-steroid anti-inflammatory analgesic drug into effective play to relieve skin irritation at a position where the preparation is applied, and has excellent effect on rheumatoid arthritis or arthronosos deformans and pain with inflammation such as lumbago.
Description
Technical field
The present invention relates to anti-inflammatory analgesic, specifically, relate to containing Non-steroidanalgetic drug with as the levobupivacaine of local anesthetic or pharmaceutically acceptable salt class is made as active ingredient, anti-inflammatory analgesic effect significantly improves external preparation.
Background technology
Up to now, be developed multiple Non-steroidanalgetic drug with the steroid anti-inflammatory analgesic replacing side effect many, and be applied to clinical gradually.
Although these Non-steroidanalgetic drugs play excellent antiinflammatory, analgesic effect, but pass through oral administration, the side effect of its gastrointestinal dysfunction is strong, therefore people are studying the transdermal formulation as the route of administration alleviating side effect, as the external preparation containing Non-steroidanalgetic drug, people, carrying out the exploitation of liquid preparation, the aerosol agent etc. such as such as ointment, plaster (alite paste), cataplasma, patch, suspending agent, Emulsion, lotion, have several preparation to be applied to clinical.
But the Percutaneously absorbable of usual Non-steroidanalgetic drug is not ideal enough, when carrying out administration with the form of external preparation, compared with oral administration, its effect has the trend of reduction.
So in order to improve its Percutaneously absorbable, people have carried out various research, such as, make an effort as on the Non-steroidanalgetic drug content in the formulation of effective ingredient or mixing transdermal absorption accelerator improving.
Recently, as one of its research contents, someone proposes and add local anesthetic to seek to improve the motion of Percutaneously absorbable etc. in Non-steroidanalgetic drug.Such as, in No. WO01/47559, International Publication, someone motion is mixed with the external use plaster of such as indomethacin, the ketoprofen etc. as Non-steroidanalgetic drug and the lignocaine as local anesthetic or benzocaine etc. simultaneously, particularly pointing out this is to the external use plaster with the analgesic effect excellence of the pain of inflammation such as rheumatoid arthritis (rheumatoidarthritis) or arthronosos deformans (also claiming osteoarthritis, osteoarthritis), lumbago diseases.In Japanese Unexamined Patent Publication 2003-335663 publication, people's motion is had to be mixed with the external preparation of diclofenac sodium and lignocaine or benzocaine etc. as local anesthetic; In Japanese Unexamined Patent Publication 2004-123632 publication, there is people's motion to be mixed with the external preparation of piroxicam and lignocaine simultaneously; In Japanese Unexamined Patent Publication 2004-323502 publication, Japanese Unexamined Patent Publication 2005-068035 publication and Japanese Unexamined Patent Publication 2005-145932 publication, have people also motion be mixed with the external use plaster of such as indomethacin, the diclofenac etc. as Non-steroidanalgetic drug and the lignocaine as local anesthetic or tetracaine etc. simultaneously.
The external preparation of above institute motion, its object is to such as to alleviate the skin irritation of Non-steroidanalgetic drug or improve medicine permeability in the tissue or diffusibility, is the external preparation effectively playing antiinflammatory that Non-steroidanalgetic drug has, analgesic effect.
But when considering actual dermal application, the realistic situation of these external preparations is: the antiinflammatory that Non-steroidanalgetic drug has, analgesic effect are not ideal enough, need further to improve.
Summary of the invention
The present inventor in view of described present situation, with provide effectively play Non-steroidanalgetic drug and have anti-inflammatory analgesic effect, relax skin irritation to sticking portion, there is the external preparation of excellent effect for problem to rheumatoid arthritis or arthronosos deformans and lumbago diseases etc. with the pain of inflammation simultaneously.
In order to solve above-mentioned problem, the present inventor etc. conduct in-depth research, have studied the mixed effect being mixed with particularly local anesthetic in the external preparation of Non-steroidanalgetic drug and local anesthetic in motion up to now, found that: when the levobupivacaine in local anesthetic and Non-steroidanalgetic drug are combined, have effectively improve Non-steroidanalgetic drug and have analgesia, anti-inflammatory effects effect.
Namely, preparation is simultaneously containing as the levobupivacaine of local anesthetic and the analgesia of Non-steroidanalgetic drug, antipruritic external preparation, when afterwards said preparation being applied to the skin affected part with pain or the skin affected part with inflammation and pain, find that skin irritation is relaxed, complement each other with the analgesic activity of the levobupivacaine as local anaesthetics simultaneously, confirm high analgesia, anti-inflammatory effects, thus complete the present invention.
Therefore, as basic scheme of the present invention, relate to external preparation, make as active ingredient containing Non-steroidanalgetic drug and levobupivacaine or pharmaceutically acceptable salt class.
Specifically, the present invention relates to external preparation, wherein, the content of Non-steroidanalgetic drug is 0.1 ~ 10% (weight) relative to pastille total formulation weight amount, and the content of levobupivacaine or pharmaceutically acceptable salt class is 0.01 ~ 60% (weight) relative to pastille total formulation weight amount.
More specifically, the present invention relates to external preparation, relative to the Non-steroidanalgetic drug of 1 weight portion, the levobupivacaine containing 0.1 ~ 10 weight portion or pharmaceutically acceptable salt class.
Specifically, the present invention relates to external preparation, the Non-steroidanalgetic drug wherein mixed is selected from indomethacin, ketoprofen, piroxicam, felbinac, bufexamac, suprofen, flurbiprofen, diclofenac, ibuprofen and their pharmacologically acceptable salt.
The invention still further relates to above-mentioned external preparation, wherein, the dosage form as external preparation is the dosage form of ointment, solution, suspending agent, Emulsion, lotion, cataplasma, patch, aerosol agent or external pulvis.
Wherein, as one of most preferred scheme of the present invention, be simultaneously containing as the felbinac of Non-steroidanalgetic drug and levobupivacaine or the pharmaceutically acceptable salt class external preparation as the cataplasma of effective ingredient or the form of patch.
Beneficial effect of the present invention is: according to the present invention, provides the anti-inflammatory analgesic effect effectively playing Non-steroidanalgetic drug and have, the skin irritation relaxing sticking portion, the pain with inflammation is had to the external preparation of excellent effect simultaneously.External preparation provided by the present invention, its Percutaneously absorbable is excellent, simultaneously in vivo after distribution effective ingredient permeability in the tissue and diffusibility excellent.Therefore, according to the present invention, provide and complement each other with the effect of levobupivacaine, the various pain of skin and scratching where it itches had to the considerably less external preparation with various dosage form of sufficient curative effect, side effect, it is very large in value medically.
Analgesic anti-inflammatory preparation for external application of the present invention, not only to such as rheumatoid arthritis, arthronosos deformans, the chronic pains such as lumbago diseases, the diseases associated with inflammation such as scapulohumeral periarthritis or tenosynovitis, the pain that operation or wound etc. cause etc. are effective with the disease of pain, to atopic dermatitis, eczema, contact dermatitis, seborrheic dermatitis, urticaria, children's's papular urticaria, worm stings wound, skin pruritus, uremia, the metabolic diseases such as chronic renal insufficiency, the endocrinopathyes such as diabetes etc. with pruritus and incised wound, post-surgical trauma, the skin traumas such as hot wound with pruritus etc. with the disease of scratching where it itches, or neuropathic pain is also very effective.
Detailed description of the invention
Below in conjunction with embodiment, embodiment of the present invention are described in detail.It will be understood to those of skill in the art that following examples are only the preferred embodiments of the present invention, so that understand the present invention better, thus should not be considered as limiting scope of the present invention.For a person skilled in the art, the present invention can have various modifications and variations, within the spirit and principles in the present invention all, and any amendment done, equivalent replacement or improvement etc., all should be included within protection scope of the present invention.Experimental technique in following embodiment, if no special instructions, is conventional method; Experiment material used, if no special instructions, is and is purchased available from routine biochemistry chemical reagent work.
As mentioned above, substance of the present invention relates to external preparation, and the feature of this external preparation is: make as active ingredient containing Non-steroidanalgetic drug and levobupivacaine.
The Non-steroidanalgetic drug contained as effective ingredient such as has: the compound being selected from indomethacin, ketoprofen, piroxicam, felbinac, bufexamac, suprofen, flurbiprofen, diclofenac, ibuprofen and their pharmacologically acceptable salt, but is not limited to these.
These Non-steroidanalgetic drugs only can use a kind, also two or more can be combined.The typical case be combined but the example of indefiniteness comprise: indomethacin and ketoprofen are combined, indomethacin and piroxicam are combined, indomethacin and felbinac are combined, indomethacin and bufexamac are combined, indomethacin and suprofen are combined, indomethacin and flurbiprofen are combined, indomethacin and diclofenac are combined, indomethacin and ibuprofen are combined, ketoprofen and piroxicam are combined, ketoprofen and felbinac are combined, ketoprofen and bufexamac are combined, ketoprofen and suprofen are combined, ketoprofen and flurbiprofen are combined, ketoprofen and diclofenac are combined, ketoprofen and ibuprofen are combined, piroxicam and felbinac are combined, piroxicam and bufexamac are combined, piroxicam and suprofen are combined, piroxicam and flurbiprofen are combined, piroxicam and diclofenac are combined, piroxicam and ibuprofen are combined, felbinac and bufexamac are combined, felbinac and suprofen are combined, felbinac and flurbiprofen are combined, felbinac and diclofenac are combined, felbinac and ibuprofen are combined, bufexamac and suprofen are combined, bufexamac and flurbiprofen are combined, bufexamac and diclofenac are combined, bufexamac and ibuprofen are combined, suprofen and flurbiprofen are combined, suprofen and diclofenac are combined, suprofen and ibuprofen are combined, flurbiprofen and diclofenac are combined, flurbiprofen and ibuprofen are combined, diclofenac and ibuprofen are combined, indomethacin, ketoprofen and piroxicam are combined, ketoprofen, piroxicam and felbinac are combined, piroxicam, felbinac and bufexamac are combined, felbinac, bufexamac and suprofen are combined, bufexamac, suprofen and flurbiprofen are combined, suprofen, flurbiprofen and diclofenac are combined, flurbiprofen, diclofenac and ibuprofen are combined, etc..
Wherein distinguish: by selecting felbinac as Non-steroidanalgetic drug, very effective external preparation can be provided.
The content of above-mentioned Non-steroidanalgetic drug is different from the dosage form of Non-steroidanalgetic drug used and target external preparation, relative to pastille total formulation weight amount, preferably 0.1 ~ 10% (weight), such as 0.1% (weight), 0.2% (weight), 0.5% (weight), 0.8% (weight), 1.0% (weight), 1.5% (weight), 2% (weight), 2.5% (weight), 3% (weight), 4% (weight), 5% (weight), 6% (weight), 7% (weight), 8% (weight), 9% (weight) or 9.9% (weight), be more preferably 0.2 ~ 5% (weight).
If containing the above-mentioned scope of quantity not sufficient, then effect is insufficient, therefore not preferred; In addition, even if content exceeds above-mentioned scope, the effect of more than this effect can not be expected, likely occur side effect on the contrary, therefore not preferred.
On the other hand, develop as local anesthetic with the blended together levobupivacaine of these Non-steroidanalgetic drugs, it has surface and infiltrates, transmits anesthetic action, is mainly used for the medicine of the topical anesthesia in field of ophthalmology etc.
Distinguish in the present invention: by this levobupivacaine and Non-steroidanalgetic drug are together mixed, due to the local anaesthesia effect that levobupivacaine has, Non-steroidanalgetic drug is worked in coordination with raising in the analgesic effect of application site, and mitigation skin irritation, the Percutaneously absorbable simultaneously from external preparation preparation is also improved.
The content of levobupivacaine or pharmaceutically acceptable salt class is different according to the kind of blended together Non-steroidanalgetic drug, can not limit without exception, such as, but preferred is 0.01 ~ 60% (weight) relative to pastille total formulation weight amount, 0.02% (weight), 0.05% (weight), 0.08% (weight), 0.1% (weight), 0.2% (weight), 0.5% (weight), 0.8% (weight), 1% (weight), 1.2% (weight), 1.5% (weight), 2% (weight), 3% (weight), 4% (weight), 5% (weight), 8% (weight), 10% (weight), 12% (weight), 15% (weight), 18% (weight), 20% (weight), 25% (weight), 30% (weight), 35% (weight), 40% (weight), 45% (weight), 50% (weight), 52% (weight), 55% (weight), 58% (weight) or 59% (weight), be more preferably 0.1 ~ 30% (weight).
If levobupivacaine or pharmaceutically acceptable salt class containing the above-mentioned scope of quantity not sufficient, then the effect be combined is insufficient, therefore not preferred; If exceed above-mentioned scope, then the physicochemical property of preparation is had an impact, also likely occur side effect, therefore not preferred.
Distinguish in the present invention: in above-mentioned content range, contain 0.1 ~ 10 weight portion relative to the Non-steroidanalgetic drug of 1 weight portion, the such as levobupivacaine of 0.1 weight portion, 0.2 weight portion, 0.5 weight portion, 0.8 weight portion, 1.0 weight portions, 1.2 weight portions, 1.5 weight portions, 2 weight portions, 3 weight portions, 4 weight portions, 5 weight portions, 6 weight portions, 7 weight portions, 8 weight portions, 9 weight portions or 9.9 weight portions or the preparation of pharmaceutically acceptable salt class are more effective.
As external preparation provided by the present invention, as long as directly can give the dosage form of effective ingredient to the illness portion faces of skin, be not particularly limited, such as, use after can making the preparations such as ointment, liquid preparation (suspending agent, Emulsion, lotion etc.), cataplasma, patch, aerosol agent and external pulvis.
When preparing these preparations, except the Non-steroidanalgetic drug contained as effective ingredient and levobupivacaine, suitably can be generally used for the various blending constituents preparing external preparation by choice for use.
As such composition, when for ointment, cream, gel, lotion, can enumerate: the substrate such as White petrolatum, yellow petrolatum, lanoline, white beeswax, spermol, stearyl alcohol, stearic acid, fixed oil, Ultralube W 389, Polyethylene Glycol, liquid paraffin, squalane; Oleic acid, isopropyl myristate, three isooctyl acid glyceride, crotamiton, ethyl sebacate, diisopropyl adipate, lauric acid hexyl ester, fatty acid, fatty acid ester, aliphatic alcohol, vegetable oil equal solvent and cosolvent; The antioxidant such as Tocopheryl derivatives, L-AA, dibenzylatiooluene, Butylated hydroxyanisole; The antiseptic such as p-Hydroxybenzoate; The wetting agents such as glycerol, propylene glycol, hyaluronate sodium; The surfactants such as polyoxyethylene deriv, fatty acid glyceride, sucrose fatty acid ester, sorbitan fatty acid esters, methyl glycol fatty acid ester, lecithin; The thickening agents etc. such as CVP Carbopol ETD2050, xanthan gum, carboxymethyl cellulose, sanlose class, hydroxypropyl cellulose, hydroxypropyl emthylcellulose.
As required, can mixed stabilizer, preservative agent, absorption enhancer, pH adjusting agent, other suitable additives further.
When for cataplasma, can enumerate: the adhesion such as polyacrylic acid, acrylic copolymer imparting agent; The cross-linking agent such as aluminum sulfate, aluminium potassium sulfate, aluminum chloride, aluminosilicate magnesium, dihydroxy acetic acid aluminum; The thickening agents such as sodium polyacrylate, polyvinyl alcohol, polyvinylpyrrolidone, gelatin, sodium alginate, carboxymethyl cellulose, sanlose class, hydroxypropyl cellulose, hydroxypropyl emthylcellulose; The polyalcohols such as glycerol, Polyethylene Glycol (Macrogol), propylene glycol, 1,3 butylene glycol; The surfactants such as polyoxyethylene deriv; The spice such as Menthol; The antiseptic such as p-Hydroxybenzoate; Purified water etc.
As required, can mixed stabilizer, preservative agent, absorption enhancer, pH adjusting agent, other suitable additives further.
When for patch, can mix: the binding agents such as styrene isoprene styrene block copolymer (SIS) (SIS block copolymer) or acrylic resin; Resin is paid in the bonding such as alicyclic saturated hydrocarbon system resin, rosin series resin, terpenic series resin; The softening agents such as aqueous natural gum, liquid paraffin; The antioxidant such as dibenzylatiooluene; The polyhydric alcohol such as propylene glycol; The absorption enhancers such as oleic acid; The surfactants such as polyoxyethylene deriv, other suitable additives.
Can also add sodium polyacrylate or polyvinyl alcohol such can be moisture macromolecule and a small amount of purified water, make moisture patch.
Even if in this case, as required, can mixed stabilizer, preservative agent, absorption enhancer, pH adjusting agent, other suitable additives further.
When for aerosol agent, can mix: for the preparation of the substrate such as White petrolatum, yellow petrolatum, lanoline, white beeswax, spermol, stearyl alcohol, stearic acid, fixed oil, Ultralube W 389, Polyethylene Glycol, liquid paraffin, squalane of ointment, cream, gel, suspending agent, Emulsion, solution and lotion etc.; Oleic acid, isopropyl myristate, diisopropyl adipate, decanedioic acid isopropyl ester, three isooctyl acid glyceride, crotamiton, ethyl sebacate, lauric acid hexyl ester, fatty acid, fatty acid ester, aliphatic alcohol, vegetable oil equal solvent and cosolvent; The antioxidant such as Tocopheryl derivatives, L-AA, dibenzylatiooluene, Butylated hydroxyanisole; The antiseptic such as p-Hydroxybenzoate; The wetting agents such as glycerol, propylene glycol, hyaluronate sodium; The surfactants such as polyoxyethylene deriv, fatty acid glyceride, sucrose fatty acid ester, sorbitan fatty acid esters, methyl glycol fatty acid ester, lecithin; The thickening agents such as CVP Carbopol ETD2050, xanthan gum, carboxymethyl cellulose, sanlose class, hydroxypropyl cellulose, hydroxypropyl emthylcellulose; And various stabilizing agent, buffer agent, correctives, suspending agent, emulsifying agent, aromatic, preservative agent, cosolvent, other suitable additives.
When for external pulvis, can mix: excipient or other suitable additives such as potato starch, wheaten starch, corn starch, Pulvis Talci, zinc oxide.
Even if in this case, as required, various stabilizing agent, preservative agent, absorption enhancer, other suitable additives can be mixed further.
The preparation method of external preparation provided by the present invention is not particularly limited, according to desired dosage form, adopts the method for the common external preparation of preparation of abundant mixing each composition and required matrix components etc. to be prepared.
When preparing cataplasma and patch, the mixture sprawled on peeling paper, drying is mixing can be passed through, then fit with the supporter of softness, be cut into desired size, be prepared.
External preparation provided by the present invention, such as when for ointment, liquid preparation (suspending agent, Emulsion, lotion etc.), aerosol agent and external pulvis time, use according to following common using method: use by smearing etc. to directly apply to skin affected part or smear or impregnated in after on the supporters such as cloth.
When for cataplasma or patch, use according to the method these preparations being directly attached at skin affected part.
Embodiment
Below, by embodiment and test example, external preparation provided by the present invention is described, but the present invention is not by any restriction of these embodiments.
Embodiment 1
Prepare the pastille substrate of formula shown in following table 1.Specifically, felbinac is dissolved in crotamiton, by levobupivacaine and is dissolved in propylene glycol, then both are mixed, then other compositions shown in these solute and tables 1 are mixed until evenly, obtain pastille substrate.By the pastille substrate so prepared with 1000g/m
2spread on non-woven fabrics, add the lining of polypropylene, be cut into 10 × 14cm afterwards
2, obtain external use plaster.
Table 1
| Composition | Combined amount |
| Felbinac | 0.5 |
| Levobupivacaine | 8 |
| Propylene glycol | 4 |
| Glycerol | 12 |
| The sorbitol solution of 70% | 12 |
| Sodium polyacrylate | 6 |
| Carboxymethyl cellulose sodium | 6 |
| Dihydroxy acetic acid aluminum | 0.5 |
| Diethanolamine | 0.5 |
| Crotamiton | 2 |
| Tartaric acid | 1 |
| Purified water | Surplus |
| Amount to | 100 |
Unit: weight portion
Embodiment 2
Prepare the pastille substrate of formula shown in following table 2.Specifically, indomethacin is dissolved in crotamiton, levobupivacaine is dissolved in propylene glycol.
Then, these solutees are mixed with other compositions shown in table 2 until evenly, obtain pastille substrate.By the pastille substrate so prepared with 1000g/m
2spread on non-woven fabrics, add the lining of polypropylene, be cut into 10 × 14cm afterwards
2, obtain external use plaster.
Table 2
| Composition | Combined amount |
| Indomethacin | 0.5 |
| Levobupivacaine | 4 |
| Propylene glycol | 10 |
| Crotamiton | 2 |
| Oleum Ricini | 0.5 |
| Glycerol | 12 |
| Polyacrylic acid | 4 |
| Polyacrylic acid part corrective | 5 |
| Carboxymethyl cellulose sodium | 5 |
| Aluminium hydroxide | 0.5 |
| Aluminosilicate magnesium | 0.05 |
| Tartaric acid | 0.05 |
| Edetate sodium | 0.05 |
| Purified water | Surplus |
| Amount to | 100 |
Unit: weight portion
Embodiment 3
Prepare the pastille substrate of formula shown in following table 3.Specifically, diclofenac sodium is dissolved in METHYLPYRROLIDONE, levobupivacaine is dissolved in propylene glycol.
Then, these solutees are mixed with other compositions shown in table 3 until evenly, obtain pastille substrate.By the pastille substrate so prepared with 1000g/m
2spread on non-woven fabrics, add the lining of polypropylene, be cut into 10 × 14cm
2, obtain external use plaster.
Table 3
| Composition | Combined amount |
| Diclofenac sodium | 1 |
| Levobupivacaine | 5 |
| Propylene glycol | 10 |
| METHYLPYRROLIDONE | 4 |
| 70% sorbitol solution | 25 |
| Sodium polyacrylate | 5 |
| Carboxymethyl cellulose sodium | 4 |
| Dry gel aluminum hydroxide | 0.5 |
| Tartaric acid | 3 |
| Kaolin | 5 |
| Purified water | Surplus |
| Amount to | 100 |
Unit: weight portion
Embodiment 4
Formula according to following table 4, add styrene isoprene styrene block copolymer (SIS) (SIS block copolymer), hydrogenated rosin glyceride, liquid paraffin, polybutene, antioxidant etc., melt with toluene mixing, mixing felbinac and levobupivacaine is dropped in this mixture, fully mixing, the mixture obtained is spread on peeling paper, dry toluene afterwards, fit with the supporter of softness, and be cut into desired size, obtain patch.
Table 4
| Composition | Combined amount |
| Felbinac | 6 |
| Levobupivacaine | 12 |
| Crotamiton | 5 |
| SIS block copolymer | 30 |
| Hydrogenated rosin glyceride | 30 |
| Polybutene | 5 |
| Liquid paraffin | 14 |
| Dibenzylatiooluene | 1 |
| Purified water | Surplus |
| Amount to | 100 |
Unit: weight portion
Comparative example 1
In embodiment 1, the purified water of equivalent volumes is to replace levobupivacaine, and profit uses the same method and obtains external use plaster.
Comparative example 2
In embodiment 1, the purified water of equivalent volumes is to replace felbinac, and profit uses the same method and obtains external use plaster.
Comparative example 3
In embodiment 1, the purified water of equivalent volumes is to replace felbinac and levobupivacaine, and profit uses the same method and obtains external use plaster.
Test example
The external use plaster obtained in embodiment 1 and comparative example 1 ~ 3 is attached to the affected part that 10 are suffered from the male volunteers of lumbago respectively, carries out function test.
Administration time is 1 day 12 hours, and test carries out 7 days.
After off-test, effect volunteer produced by " Be very effective ", " effectively ", " constant ", " deterioration " 4 grade evaluations.
Drug withdrawal after 1 week, then repeats same test, until the evaluation of all patches terminates.
It the results are shown in following table 5.
Table 5
| Embodiment 1 | Comparative example 1 | Comparative example 2 | Comparative example 3 | |
| Be very effective | 9 | 4 | 0 | 0 |
| Effectively | 1 | 4 | 4 | 0 |
| Constant | 0 | 2 | 6 | 8 |
| Worsen | 0 | 0 | 0 | 2 |
As above shown in table, containing as the felbinac of Non-steroidanalgetic drug and these two kinds of compositions of levobupivacaine patch as the external use plaster of the present invention of effective ingredient, i.e. embodiment 1, its improvement rate (effectively) is 100% (10/10), significantly improve than the improvement rate 80% (8/10) of patch of the comparative example 1 not being combined levobupivacaine, confirm significant difference, effectiveness of the present invention can be realized.
As mentioned above, according to the present invention, the anti-inflammatory analgesic effect effectively playing Non-steroidanalgetic drug and have, the skin irritation relaxing sticking portion are provided, rheumatoid arthritis or arthronosos deformans and lumbago diseases etc. are had to the external preparation of the various dosage forms of excellent effect simultaneously with the pain of inflammation.
External preparation provided by the present invention, its Percutaneously absorbable is excellent, simultaneously in vivo after distribution effective ingredient permeability in the tissue and diffusibility excellent, side effect is considerably less, so it is very large in value medically.
Applicant states, the present invention illustrates detailed features of the present invention and method detailed by above-described embodiment, but the present invention is not limited to above-mentioned detailed features and method detailed, namely do not mean that the present invention must rely on above-mentioned detailed features and method detailed could be implemented.Person of ordinary skill in the field should understand, any improvement in the present invention, to equivalence replacement and the interpolation of auxiliary element, concrete way choice etc. that the present invention selects component, all drops within protection scope of the present invention and open scope.
Claims (10)
1. an analgesic anti-inflammatory preparation for external application, containing Non-steroidanalgetic drug and levobupivacaine or pharmaceutically acceptable salt class as active ingredient, wherein, the content of Non-steroidanalgetic drug is 0.1 ~ 10% (weight) relative to pastille total formulation weight amount, and the content of levobupivacaine or pharmaceutically acceptable salt class is 0.01 ~ 60% (weight) relative to pastille total formulation weight amount.
2. analgesic anti-inflammatory preparation for external application according to claim 1, is characterized in that, relative to the Non-steroidanalgetic drug of 1 weight portion, and the levobupivacaine containing 0.1 ~ 10 weight portion.
3. analgesic anti-inflammatory preparation for external application according to claim 1 and 2, is characterized in that, the content of described Non-steroidanalgetic drug is 0.2 ~ 5% (weight) relative to pastille total formulation weight amount.
4. the analgesic anti-inflammatory preparation for external application according to any one of claim 1-3, is characterized in that, the content of described levobupivacaine or pharmaceutically acceptable salt class is 0.1 ~ 30% (weight) relative to pastille total formulation weight amount.
5. the analgesic anti-inflammatory preparation for external application according to any one of claim 1-4, it is characterized in that, described Non-steroidanalgetic drug is selected from indomethacin, ketoprofen, piroxicam, felbinac, bufexamac, suprofen, flurbiprofen, diclofenac, ibuprofen and their pharmacologically acceptable salt.
6. the analgesic anti-inflammatory preparation for external application according to any one of claim 1-5, is characterized in that, described Non-steroidanalgetic drug is felbinac.
7. the analgesic anti-inflammatory preparation for external application according to any one of claim 1-6, is characterized in that, described external preparation is the dosage form of ointment, solution, suspending agent, Emulsion, lotion, cataplasma, patch, aerosol agent or external pulvis.
8. the analgesic anti-inflammatory preparation for external application according to any one of claim 1-7, is characterized in that, containing felbinac and levobupivacaine or pharmaceutically acceptable salt class as active ingredient.
9. the analgesic anti-inflammatory preparation for external application according to any one of claim 1-8, it is characterized in that, the levobupivacaine of the felbinac and 0.1 ~ 30% (weight) containing 0.2 ~ 5% (weight) or pharmaceutically acceptable salt class are as active ingredient.
10. the analgesic anti-inflammatory preparation for external application according to any one of claim 1-9, it is characterized in that, described analgesic anti-inflammatory preparation for external application is used for the treatment of or improves rheumatoid arthritis, arthronosos deformans, lumbago diseases, scapulohumeral periarthritis, tenosynovitis, the pain that operation or wound cause, atopic dermatitis, eczema, contact dermatitis, seborrheic dermatitis, urticaria, children's's papular urticaria, worm stings wound, skin pruritus, uremia, chronic renal insufficiency metabolic disease, diabetes with pruritus and incised wound, post-surgical trauma, hot trauma with pruritus or neuropathic pain.
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| CN201410396347.2A CN105327351A (en) | 2014-08-12 | 2014-08-12 | Anti-inflammatory analgesic preparation for external application |
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| CN201410396347.2A CN105327351A (en) | 2014-08-12 | 2014-08-12 | Anti-inflammatory analgesic preparation for external application |
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| CN201410396347.2A Pending CN105327351A (en) | 2014-08-12 | 2014-08-12 | Anti-inflammatory analgesic preparation for external application |
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| CN (1) | CN105327351A (en) |
Cited By (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN113194938A (en) * | 2018-12-19 | 2021-07-30 | 美德阿利克斯株式会社 | External-use anti-inflammatory analgesic |
| CN113262216A (en) * | 2020-02-14 | 2021-08-17 | 北京泰德制药股份有限公司 | External preparation for eliminating skin surface red swelling and easing pain |
-
2014
- 2014-08-12 CN CN201410396347.2A patent/CN105327351A/en active Pending
Cited By (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN113194938A (en) * | 2018-12-19 | 2021-07-30 | 美德阿利克斯株式会社 | External-use anti-inflammatory analgesic |
| CN113262216A (en) * | 2020-02-14 | 2021-08-17 | 北京泰德制药股份有限公司 | External preparation for eliminating skin surface red swelling and easing pain |
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