CN101416976B - External medicine composition preparation with anti-inflammation detumescence pain-easing function - Google Patents
External medicine composition preparation with anti-inflammation detumescence pain-easing function Download PDFInfo
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Abstract
The invention relates to an externally-used medical compound preparation having the functions of being anti-inflammatory, antipyretic and analgesic. The preparation is characterized in that the preparation is prepared by the following raw materials of active ingredients with the following weight percentages: 0.01 percent to 20 percent of aescin or salts thereof acceptable in pharmacy, 0.01 percent to 10 percent of one or more of ketoprofen, tiaprofenic acid, tiaprofenic salts acceptable in the pharmacy, meloxicam, piroxicam and naproxen, and the rest amount of accessories. The externally-used medical composition can be used for preparing any externally-used preparation acceptable in the pharmacy. The preparation of the invention can be used for treating arthrodynia, hyperosteogeny, gout, neuropathic pains, traumatic injuries, chronic eparsalgia, various closed injuries and other diseases, and has strong practicability.
Description
Technical field
The present invention relates to a kind of is the external-use pharmaceutical composition formulation of raw material by natural drug and nonsteroidal antalgic anti-inflammatory agent; A kind of external-use pharmaceutical composition formulation with anti-inflammation detumescence analgesic activity particularly; The invention still further relates to the purposes of preparation.
Background technology
Arthralgia, hyperosteogeny, gout, neuropathic pain, traumatic injury and various closed injurys etc. are commonly encountered diseases, frequently-occurring disease, have a strong impact on people's work, study and daily life, treat this type of disease oral, although the injection Chinese medicine and western medicine is a lot, but the mostly side effect of various degrees, to put the above-mentioned disease of external medication on the skin be easy, the most most popular method so stick, be coated with.
At present, the external preparation kind with anti-inflammatory and analgesic effect is more, and Western medicine adopt the dosage forms such as ointment, gel, but curative effect can not be lasting take the non-steroidal antalgic anti-inflammatory agent as main more, and detumescence effect is not obvious, and has the side effect such as allergy, zest.Chinese medicine is the conventional dosage forms such as black plaster, rubber-emplastrum that adopt then more.Black plaster is because of its determined curative effect, easy to use, low price, at folks of china widely use basis is arranged, but be by experience because the preparation of plaster is mostly, technological parameter and quality standard controlled in the production lack, product quality is uneven, be not suitable for large-scale industrialized production, and easily cause oil impregnate, leakage of oil, pollution clothes.Because the large compound recipe of the many employings of Chinese medicine, the rubber-emplastrum drug loading is limited, and curative effect is a greater impact.
Aescine (or its pharmaceutically acceptable salt) is in the clinical injection purposes that mostly is, because the character of itself has obvious zest to blood vessel, causes very large misery to the patient, have in the therapeutic process shorten service time, therefore the effect of impact treatment.And the nonsteroidal antalgic anti-inflammatory agent mostly is oral, has GI irritation, can cause the distinct disadvantage of digestive tract hemorrhage, ulcer.
Summary of the invention
Technical problem to be solved by this invention provide a kind of fill a prescription simple, preparation easily, determined curative effect, the external-use pharmaceutical composition formulation with anti-inflammation detumescence analgesic activity that toxic and side effects is little.
Another technical problem to be solved by this invention has provided the as previously discussed purposes of external-use pharmaceutical composition formulation.
Technical problem to be solved by this invention is to realize by following technical scheme.The present invention is a kind of external-use pharmaceutical composition formulation with anti-inflammation detumescence analgesic activity, is characterized in, the percentage by weight of making the active ingredient raw material of medicine and accounting for whole preparation is:
(1) aescine and its acceptable salt 0.01～20% pharmaceutically;
(2) ketoprofen, thiophene are coughed up fragrant acid, thiophene and are coughed up pharmaceutically one or more in acceptable salt, meloxicam, piroxicam and the naproxen 0.01～10% of fragrant acid;
All the other are adjuvant.
Technical problem to be solved by this invention can also further be realized by following technical scheme.Above-described preparation is characterized in, the percentage by weight that the active ingredient raw material accounts for whole preparation is:
(1) aescine and its acceptable salt 0.1～5% pharmaceutically;
(2) ketoprofen, thiophene are coughed up fragrant acid, thiophene and are coughed up pharmaceutically one or more in acceptable salt, meloxicam, piroxicam and the naproxen 0.01～5% of fragrant acid.
Technical problem to be solved by this invention can also further be realized by following technical scheme.Above-described preparation is characterized in, the percentage by weight that the active ingredient raw material accounts for whole preparation is:
(1) aescine and its acceptable salt 1% pharmaceutically;
(2) ketoprofen, thiophene cough up fragrant acid, thiophene cough up fragrant acid pharmaceutically acceptable salt, meloxicam,
In piroxicam and the naproxen one or more 0.1～5%.
In above technical scheme, when the mixture that adopts two or more in active ingredient raw material (1) group, (2) group during as the active ingredient raw material, the raw material that consists of mixture can take arbitrary proportion to mix.
Technical problem to be solved by this invention can also further be realized by following technical scheme.Above-described preparation, be characterized in, described aescine refers to the total saponins that extracts from Hippocastanaceae buckeye Aesculus, Aesculus chinensis Bunge, Radix Aesculi, Aesculus hippocastanum L. or Aesculus turbinata B1 seed, perhaps refer to state at least a extract as main component in aescine A, aescine B, aescine C, aescine D, aescine E and the aescine F that extracts in the seed in the past; Described aescine pharmaceutically acceptable salt refers to the salt that aforesaid aescine and pharmaceutically acceptable inorganic base or organic base reaction generate, and comprises the aescine sodium salt, aescine potassium salt, magnesium aescine, the aescine calcium salt, arginine aescine, ornithine aescine, lysine aescine, histidine aescine, ethylenediamine aescine, diethylamine aescine, aescine monoethanolamine salt, diethanolamine aescine, triethanolamine aescine, aescine meglumine salt or aescine ammonium salt.
Technical problem to be solved by this invention can also further be realized by following technical scheme.Above-described preparation, be characterized in, described thiophene cough up fragrant acid pharmaceutically acceptable salt refer to that thiophene coughs up the salt of fragrant acid and pharmaceutically acceptable inorganic base or organic base reaction generation, comprise that thiophene coughs up fragrant acid sodium-salt, thiophene is coughed up fragrant acid potassium salt, thiophene is coughed up fragrant sour magnesium salt, thiophene is coughed up fragrant acid calcium salt, thiophene is coughed up fragrant sour arginine salt, thiophene is coughed up fragrant sour ornithine salt, thiophene is coughed up fragrant sour lysinate, thiophene is coughed up fragrant sour histidine salt, thiophene is coughed up fragrant sour ethylenediamine salt, thiophene is coughed up fragrant diethylammonium salt salt, thiophene is coughed up fragrant sour monoethanolamine salt, thiophene is coughed up fragrant sour diethanolamine salt, thiophene is coughed up fragrant triethylenetetraminehexaacetic acid alcohol amine salt, thiophene is coughed up fragrant sour meglumine salt or thiophene is coughed up fragrant acid ammonium salt.
Aescine of the present invention or its be acceptable salt pharmaceutically, can be pharmaceutically acceptable salt of commercially available aescine or its, also can be routinely extracting method from Hippocastanaceae buckeye Aesculus, Aesculus chinensis Bunge, Radix Aesculi, extract pharmaceutically acceptable salt of the escin of gained or its in Aesculus hippocastanum L. and the Aesculus turbinata B1 seed, also can be pharmaceutically acceptable salt of disclosed any extracting method extracts in the prior art aescine or its, can also be with aescine A, aescine B, aescine C, aescine D, at least a in aescine E and the aescine F is pharmaceutically acceptable salt of the extract of main component or its, preferred aescine or aescine; Described ketoprofen (comprising levo form, d-isomer and raceme), thiophene are coughed up fragrant acid or its, and pharmaceutically acceptable salt, meloxicam, piroxicam, naproxen are nonsteroidal antalgic and inflammation relieving chemical drugs commonly used at present, can be commercially available crude drug, also can be the crude drug that disclosed any method is synthesized in the prior art.
Preparation formulation of the present invention can be any medically acceptable exterior-applied formulation, comprises tincture, ointment, ointment, gel, patch, membrane, cataplasma, lotion, liniment, aerosol, spray, rubber-emplastrum or liniment; Can be applicable to the treatment of arthralgia, hyperosteogeny, gout, neuropathic pain, traumatic injury, chronic strain disease and various closed injurys.The required adjuvant of preparation can be disclosed any topical agent adjuvant applicatory in the prior art, comprise required suitable substrate or excipient, the preparation method of preparation can be taked disclosed any method applicatory in the prior art according to its dosage form.
Aescine (or its pharmaceutically acceptable salt) can be used for the inflammation that causes such as a variety of causes such as after wound, burn, scald, fracture, the operation and swelling and the treatment of the dysfunction that occurs together etc.Studies show that, onset slow (just beginning to show obvious antiinflammatory action after 6 hours) after the administration of aescine class, the appearance of antiinflammatory, anti-swelling effect has obvious time delay phenomenon, and acute inflammation and edema are produced certain adverse effect when treating.And nonsteroidal antalgic anti-inflammatory agent (ketoprofen, thiophene are coughed up fragrant acid or its pharmaceutically acceptable salt, meloxicam, piroxicam, naproxen etc.) has analgesia, antiinflammation is strong, onset is rapid, dosage is low, individual variation is little characteristics.Through studies show that, one or more of aescine (or its pharmaceutically acceptable salt) and nonsteroidal antalgic anti-inflammatory agent share and can obviously play synergism, thus the performance onset rapidly, effect is strong, duration of effect is long characteristics.The present invention orientates purposes as external, can greatly reduce untoward reaction and zest that medicine is caused by vivo medicine-feeding.
The inventor is according to following composition weight percent prescription, and all the other percetages by weight are required suitable substrate or excipient of preparation, make 5 kinds of ointments:
(1) escin sodium 1%, ketoprofen 2.5% (being called for short Qy-1 ointment);
(2) escin 1%, and thiophene is coughed up fragrant sour sodium 2% (being called for short Qy-2 ointment);
(3) aescine 1%, meloxicam 0.5% (being called for short Qy-3 ointment);
(4) aescine 1%, piroxicam 0.5% (being called for short Qy-4 ointment);
(5) aescine 1%, naproxen 1% (being called for short Qy-5 ointment);
The inventor has carried out following Pharmacodynamics screening.
1: five kind of ointment of medicine efficacy screening is on the impact of rat experiment arthritis model.
1.1 experimental technique:
Test method: get rat and be divided at random 8 groups, 10 every group.The model preparation is adopted at every intradermal injection adjuvant 0.1ml of Rat Right metapedes pad section, brings out arthritic generation.With incomplete Freunds adjuvant (IFA) and bacillus calmette-guerin vaccine (BCG) emulsifying mixing, the BCG final concentration is 10mg/ml.
The 30min preventive administration is 1 time before impact on primary affection: the Yu Zhiyan, observes to cause scorching rear 18h adjuvant injection side vola swelling, represents with miking vola thickness, takes the mean and compares with matched group, carries out statistical test.
Impact on polyarthritis: beginning administration on the 8th after the adjuvant injection, every day 1 time, successive administration to the 30 days is observed the preventive and therapeutic effect of polyarthritis.From the self administration of medication, every 1 week, with the former degree of the left back vola of miking rat (adjuvant injection offside represents with mm), as the swelling index of Multiple, take the mean and compare with matched group, carry out statistical test.
Impact on the general pathological changes: except the swelling of observing left back foot (adjuvant injection offside), outside the index as polyarthritis, also observe forelimb, ear and the general pathological changes such as afterbody pathological changes incidence rate and the order of severity, by 0 grade～4 grades point system records, 0=is normal, 1=is only red, and 2=is red to be added light swollenly, and 3=is swollen .4=joint deformity, tetanic seriously.Take the mean and carry out statistical test.
1.2 experimental result
Results suggest, five kinds of ointment can alleviate the generation of rat assist agent arthritis constitutional pathological changes, Multiple, can stop equally the generation of general pathological changes.Relatively there were significant differences (p＜0.05, p＜0.01) with the blank group.Point out five kinds of ointment to have the arthritic effect of significant anti-experimental character.See Table 1,2,3.
Five kinds of ointment of table 1 are on the impact of experimental arthritis constitutional pathological changes
Annotate: compare with the blank group,
*P＜0.01.
Five kinds of ointment of table 2 are on the impact of experimental arthritis Multiple
Annotate: compare with the blank group,
*P＜0.05,
*P＜0.01.
Five kinds of ointment of table 3 are on the impact of experimental arthritis whole body pathological changes
Annotate: compare with the blank group,
*P＜0.05,
*P＜0.01.
2: five kinds of ointment of medicine efficacy screening are on the impact of Oleum Tiglii induced mice ear swelling.
The 2-1 experimental technique:
Get normal ICR mice, body weight 25～28g, male.Be divided at random 8 groups, every group of 10 mices.The even coating in mouse ear two sides, coating is 3 continuously, twice of every day.Behind the last coating 1h on the 3rd, each administration group is cleaned with dry cotton ball with distilled water flush away plaster.Be applied to two sides before and after the left ear of mice with 2% Oleum Tiglii (containing 2% Oleum Tiglii, 5% water, 20% ethanol and 73% ether) 0.05ml, after causing scorching 4h, put to death mice, two ears about cutting along the auricle baseline, (diameter 9mm) takes off round auricle at same position respectively with card punch, scales/electronic balance weighing, as the auricular concha swelling, and calculate the swelling percentage rate with the difference of mice left and right sides auricular concha weight.
2.2 experimental result:
Five kinds of ointment all can alleviate Oleum Tiglii and cause the mice ear rate, have compared significant difference (p＜0.05, p＜0.01) with the blank group.Point out medicine to have and obviously alleviate the effect that Oleum Tiglii causes mice swelling and inflammation.The results are shown in Table 4.
Five kinds of ointment of table 4 are on the impact of Oleum Tiglii induced mice ear swelling
Annotate: compare with the blank group,
*P＜0.05,
*P＜0.01.
3: five kinds of ointment of medicine efficacy screening stimulate the impact that causes the mice pain reaction on the acetic acid abdominal cavity.
3.1 experimental technique:
Get the ICR mice, about body weight 17～21g, ♀
Half and half.Be divided at random 8 groups, the even coating of mouse peritoneal face, behind the coating 30min, each administration group is cleaned with dry cotton ball with distilled water flush away plaster.Each is organized mouse peritoneal and only injects 0.5% acetic acid 0.2ml/, respectively organizes writhing response number of animals and the writhing response number of times that mice occurs in the 15min behind the observation injection acetic acid.The result carries out x
2Check (enumeration data) and t check (measurement data).
3.2 experimental result
Experimental result shows, five kinds of ointment groups apparently higher than the blank group, more all have significant difference (p＜0.05, P＜0.01) with the blank group without the writhing response number of animals; Five kinds of ointment groups can reduce the mouse writhing reaction times, with the blank group significant difference (p＜0.01) are arranged more all.The mice pain reaction that shows five kinds of ointment groups that acetic acid is stimulated and cause has obvious inhibitory action.The results are shown in Table 5.
Five kinds of ointment of table 5 stimulate the impact that causes the mice pain reaction on acetic acid
Compare with the blank group,
*P＜0.05,
*P＜0.01.
4: five kinds of ointment of medicine efficacy screening are on the impact of thermostimulation induced pain model.
3.1 experimental technique:
Mice is placed on the thermostimulation induced pain instrument of 55 ℃ of constant temperature, drops into hot plate to the time that metapedes occurs licking with the stopwatch record from mice, as pain threshold, measure altogether 2 times, be no more than 30 seconds as qualified take meansigma methods.The qualified animal of learning from else's experience after screening is divided into 8 groups at random, and 10 every group, coating is 3 continuously, twice of every day.Every interval 0.5h measures once after the last administration, surpasses 60 seconds in 60 seconds such as pain threshold.Calculate pain threshold, relatively group difference.
3.2 experimental result
The result shows that five kinds of ointment all can suppress the pain reaction that thermostimulation causes mice.Point out five kinds of ointment that the non-specific acute pain model of animal is had definitely inhibitory action.The results are shown in Table 6.
Five kinds of ointment of table 6 cause the impact of mice pain reaction on thermostimulation
Annotate: compare with the blank group,
*P＜0.05,
*P＜0.01.
The medicine efficacy screening brief summary: in above-mentioned experiment, 5 kinds of ointment all have obvious antiinflammatory, detumescence and analgesic effect.
Compared with prior art, pharmaceutical composition of the present invention and preparation thereof have the following advantages: 1, good effect: the effective percentage that topical composition preparation of the present invention is treated various closed soft tissue injuries through clinical trial reaches 97.6%, compatibility and the addition of its basis, auxiliary composition draw through repetition test, affected part coating, every day 2-3 time; Onset time is fast, effect is strong, effect is held time length.2, prescription element is few, makes simply, and is easy to use, thereby easy to implement; 3, be widely used, all kinds of inflammation, acute and chronic pain disease all there is obvious treatment mitigation, can be used for treating the diseases such as arthralgia, hyperosteogeny, gout, neuropathic pain, traumatic injury, chronic strain disease and various closed injurys, thus practical.
The specific embodiment
Below the nonrestrictive part embodiment that the present invention relates to that enumerated.
Embodiment 1.A kind of external-use pharmaceutical composition formulation with anti-inflammation detumescence analgesic activity, the percentage by weight of making the active ingredient raw material of medicine and accounting for whole preparation is:
(1) aescine or its acceptable salt 0.01% pharmaceutically;
(2) ketoprofen, thiophene are coughed up fragrant acid, thiophene and are coughed up pharmaceutically any one in acceptable salt, meloxicam, piroxicam and the naproxen 0.01% of fragrant acid;
All the other are adjuvant.Can be used for the treatment of local muscle, joint, neural inflammation, pain.
Embodiment 2.A kind of external-use pharmaceutical composition formulation with anti-inflammation detumescence analgesic activity, the percentage by weight of making the active ingredient raw material of medicine and accounting for whole preparation is:
(1) aescine or its acceptable salt 20% pharmaceutically;
(2) ketoprofen, thiophene are coughed up fragrant acid, thiophene and are coughed up pharmaceutically any one in acceptable salt, meloxicam, piroxicam and the naproxen 10% of fragrant acid;
All the other are adjuvant.Can be used for the treatment of local muscle, joint, neural inflammation, pain.
Embodiment 3.A kind of external-use pharmaceutical composition formulation with anti-inflammation detumescence analgesic activity, the percentage by weight of making the active ingredient raw material of medicine and accounting for whole preparation is:
(1) aescine or its acceptable salt 1% pharmaceutically;
(2) ketoprofen, thiophene are coughed up fragrant acid, thiophene and are coughed up pharmaceutically any one in acceptable salt, meloxicam, piroxicam and the naproxen 1% of fragrant acid;
All the other are adjuvant.Can be used for the treatment of local muscle, joint, neural inflammation, pain.
Embodiment 4.A kind of external-use pharmaceutical composition formulation with anti-inflammation detumescence analgesic activity, the percentage by weight of making the active ingredient raw material of medicine and accounting for whole preparation is:
(1) aescine or its acceptable salt 5% pharmaceutically;
(2) ketoprofen, thiophene are coughed up fragrant acid, thiophene and are coughed up pharmaceutically any one in acceptable salt, meloxicam, piroxicam and the naproxen 5% of fragrant acid;
All the other are adjuvant.Can be used for the treatment of local muscle, joint, neural inflammation, pain.
Embodiment 5.A kind of external-use pharmaceutical composition formulation with anti-inflammation detumescence analgesic activity, the percentage by weight of making the active ingredient raw material of medicine and accounting for whole preparation is:
(1) aescine and its acceptable salt 10% pharmaceutically;
(2) ketoprofen, thiophene are coughed up fragrant acid, thiophene and are coughed up pharmaceutically any one in acceptable salt, meloxicam, piroxicam and the naproxen 3% of fragrant acid;
All the other are adjuvant.Can be used for the treatment of local muscle, joint, neural inflammation, pain.
Embodiment 6.A kind of external-use pharmaceutical composition formulation with anti-inflammation detumescence analgesic activity, the percentage by weight of making the active ingredient raw material of medicine and accounting for whole preparation is:
(1) aescine or its acceptable salt 15% pharmaceutically;
(2) ketoprofen, thiophene are coughed up fragrant acid, thiophene and are coughed up pharmaceutically any one in acceptable salt, meloxicam, piroxicam and the naproxen 8% of fragrant acid;
All the other are adjuvant.Can be used for the treatment of local muscle, joint, neural inflammation, pain.
Embodiment 7.A kind of external-use pharmaceutical composition formulation with anti-inflammation detumescence analgesic activity, the percentage by weight of making the active ingredient raw material of medicine and accounting for whole preparation is:
(1) aescine or its acceptable salt 0.05% pharmaceutically;
(2) ketoprofen, thiophene are coughed up fragrant acid, thiophene and are coughed up pharmaceutically any one in acceptable salt, meloxicam, piroxicam and the naproxen 0.05% of fragrant acid;
All the other are adjuvant.Can be used for the treatment of local muscle, joint, neural inflammation, pain.
Embodiment 8.A kind of external-use pharmaceutical composition formulation with anti-inflammation detumescence analgesic activity, the percentage by weight of making the active ingredient raw material of medicine and accounting for whole preparation is:
(1) aescine or its acceptable salt 0.01% pharmaceutically;
(2) ketoprofen, thiophene are coughed up fragrant acid, thiophene and are coughed up pharmaceutically any one in acceptable salt, meloxicam, piroxicam and the naproxen 10% of fragrant acid;
All the other are adjuvant.Can be used for the treatment of local muscle, joint, neural inflammation, pain.
Embodiment 9.A kind of external-use pharmaceutical composition formulation with anti-inflammation detumescence analgesic activity, the percentage by weight of making the active ingredient raw material of medicine and accounting for whole preparation is:
(1) aescine or its acceptable salt 20% pharmaceutically;
(2) ketoprofen, thiophene are coughed up fragrant acid, thiophene and are coughed up pharmaceutically any one in acceptable salt, meloxicam, piroxicam and the naproxen 0.01% of fragrant acid;
All the other are adjuvant.Can be used for the treatment of local muscle, joint, neural inflammation, pain.
Embodiment 10.A kind of external-use pharmaceutical composition formulation with anti-inflammation detumescence analgesic activity, the percentage by weight of making the active ingredient raw material of medicine and accounting for whole preparation is:
(1) aescine or its acceptable salt 0.01% pharmaceutically;
(2) ketoprofen, thiophene are coughed up fragrant acid, thiophene is coughed up the mixture 10% that any 2-5 kind in fragrant sour pharmaceutically acceptable salt, meloxicam, piroxicam and the naproxen is mixed with arbitrary proportion;
All the other are adjuvant.Can be used for the treatment of local muscle, joint, neural inflammation, pain.
Embodiment 11.A kind of external-use pharmaceutical composition formulation with anti-inflammation detumescence analgesic activity, the percentage by weight of making the active ingredient raw material of medicine and accounting for whole preparation is:
(1) aescine and its acceptable salt 20% pharmaceutically;
(2) ketoprofen, thiophene are coughed up fragrant acid, thiophene is coughed up the mixture 0.01% that any 2-5 kind in fragrant sour pharmaceutically acceptable salt, meloxicam, piroxicam and the naproxen is mixed with arbitrary proportion;
All the other are adjuvant.Can be used for the treatment of local muscle, joint, neural inflammation, pain.
Embodiment 12.A kind of external-use pharmaceutical composition formulation with anti-inflammation detumescence analgesic activity, the percentage by weight of making the active ingredient raw material of medicine and accounting for whole preparation is:
(1) aescine or its acceptable salt 0.01% pharmaceutically;
(2) ketoprofen, thiophene are coughed up fragrant acid, thiophene is coughed up the mixture 0.01% that any 2-5 kind in fragrant sour pharmaceutically acceptable salt, meloxicam, piroxicam and the naproxen is mixed with arbitrary proportion;
All the other are adjuvant.Can be used for the treatment of local muscle, joint, neural inflammation, pain.
Embodiment 13.A kind of external-use pharmaceutical composition formulation with anti-inflammation detumescence analgesic activity, the percentage by weight of making the active ingredient raw material of medicine and accounting for whole preparation is:
(1) aescine and its acceptable salt 20% pharmaceutically;
(2) ketoprofen, thiophene are coughed up fragrant acid, thiophene is coughed up the mixture 10% that any 2-5 kind in fragrant sour pharmaceutically acceptable salt, meloxicam, piroxicam and the naproxen is mixed with arbitrary proportion;
All the other are adjuvant.Can be used for the treatment of local muscle, joint, neural inflammation, pain.
Embodiment 14.A kind of external-use pharmaceutical composition formulation with anti-inflammation detumescence analgesic activity, the percentage by weight of making the active ingredient raw material of medicine and accounting for whole preparation is:
(1) aescine or its acceptable salt 0.05% pharmaceutically;
(2) ketoprofen, thiophene are coughed up fragrant acid, thiophene is coughed up the mixture 5% that any 2-5 kind in fragrant sour pharmaceutically acceptable salt, meloxicam, piroxicam and the naproxen is mixed with arbitrary proportion;
All the other are adjuvant.Can be used for the treatment of local muscle, joint, neural inflammation, pain.
Embodiment 15.A kind of external-use pharmaceutical composition formulation with anti-inflammation detumescence analgesic activity, the percentage by weight of making the active ingredient raw material of medicine and accounting for whole preparation is:
(1) aescine and its acceptable salt 15% pharmaceutically;
(2) ketoprofen, thiophene are coughed up fragrant acid, thiophene is coughed up the mixture 1% that any 2-5 kind in fragrant sour pharmaceutically acceptable salt, meloxicam, piroxicam and the naproxen is mixed with arbitrary proportion;
All the other are adjuvant.Can be used for the treatment of local muscle, joint, neural inflammation, pain.
Embodiment 16.A kind of external-use pharmaceutical composition formulation with anti-inflammation detumescence analgesic activity, the percentage by weight of making the active ingredient raw material of medicine and accounting for whole preparation is:
(1) aescine and its acceptable salt 12% pharmaceutically;
(2) ketoprofen, thiophene are coughed up fragrant acid, thiophene is coughed up the mixture 6% that any 2-5 kind in fragrant sour pharmaceutically acceptable salt, meloxicam, piroxicam and the naproxen is mixed with arbitrary proportion;
All the other are adjuvant.Can be used for the treatment of local muscle, joint, neural inflammation, pain.
Embodiment 17.A kind of external-use pharmaceutical composition formulation with anti-inflammation detumescence analgesic activity, the percentage by weight of making the active ingredient raw material of medicine and accounting for whole preparation is:
(1) aescine or its acceptable salt 1% pharmaceutically;
(2) ketoprofen, thiophene are coughed up fragrant acid, thiophene is coughed up the mixture 4% that any 2-5 kind in fragrant sour pharmaceutically acceptable salt, meloxicam, piroxicam and the naproxen is mixed with arbitrary proportion;
All the other are adjuvant.Can be used for the treatment of local muscle, joint, neural inflammation, pain.
Embodiment 18.A kind of external-use pharmaceutical composition formulation with anti-inflammation detumescence analgesic activity, the percentage by weight of making the active ingredient raw material of medicine and accounting for whole preparation is:
(1) aescine or its acceptable salt 3% pharmaceutically;
(2) ketoprofen, thiophene are coughed up fragrant acid, thiophene is coughed up the mixture 10% that any 2-5 kind in fragrant sour pharmaceutically acceptable salt, meloxicam, piroxicam and the naproxen is mixed with arbitrary proportion;
All the other are adjuvant.Can be used for the treatment of local muscle, joint, neural inflammation, pain.
Embodiment 19.A kind of external-use pharmaceutical composition formulation with anti-inflammation detumescence analgesic activity, the percentage by weight of making the active ingredient raw material of medicine and accounting for whole preparation is:
(1) aescine and its acceptable salt 10% pharmaceutically;
(2) ketoprofen, thiophene are coughed up fragrant acid, thiophene is coughed up the mixture 0.05% that any 2-5 kind in fragrant sour pharmaceutically acceptable salt, meloxicam, piroxicam and the naproxen is mixed with arbitrary proportion;
All the other are adjuvant.Can be used for the treatment of local muscle, joint, neural inflammation, pain.
Embodiment 20.A kind of external-use pharmaceutical composition formulation with anti-inflammation detumescence analgesic activity, the percentage by weight of making the active ingredient raw material of medicine and accounting for whole preparation is:
(1) aescine and its acceptable salt 18% pharmaceutically;
(2) ketoprofen, thiophene are coughed up fragrant acid, thiophene is coughed up the mixture 9% that any 2-5 kind in fragrant sour pharmaceutically acceptable salt, meloxicam, piroxicam and the naproxen is mixed with arbitrary proportion;
All the other are adjuvant.Can be used for the treatment of local muscle, joint, neural inflammation, pain.
Embodiment 21.A kind of external-use pharmaceutical composition formulation with anti-inflammation detumescence analgesic activity, the percentage by weight of making the active ingredient raw material of medicine and accounting for whole preparation is:
(1) aescine and its acceptable salt 0.01% pharmaceutically;
(2) ketoprofen, thiophene are coughed up fragrant acid, thiophene is coughed up the pharmaceutically mixture 0.01% of acceptable salt, meloxicam, piroxicam and naproxen of fragrant acid;
All the other are adjuvant.Can be used for the treatment of local muscle, joint, neural inflammation, pain.
Embodiment 22.A kind of external-use pharmaceutical composition formulation with anti-inflammation detumescence analgesic activity, the percentage by weight of making the active ingredient raw material of medicine and accounting for whole preparation is:
(1) aescine and its acceptable salt 20% pharmaceutically;
(2) ketoprofen, thiophene are coughed up fragrant acid, thiophene is coughed up the pharmaceutically mixture 10% of acceptable salt, meloxicam, piroxicam and naproxen of fragrant acid;
All the other are adjuvant.Can be used for the treatment of local muscle, joint, neural inflammation, pain.
Embodiment 23.A kind of external-use pharmaceutical composition formulation with anti-inflammation detumescence analgesic activity, the percentage by weight of making the active ingredient raw material of medicine and accounting for whole preparation is:
(1) aescine and its acceptable salt 0.01% pharmaceutically;
(2) ketoprofen, thiophene are coughed up fragrant acid, thiophene is coughed up the pharmaceutically mixture 10% of acceptable salt, meloxicam, piroxicam and naproxen of fragrant acid;
All the other are adjuvant.Can be used for the treatment of local muscle, joint, neural inflammation, pain.
Embodiment 24.A kind of external-use pharmaceutical composition formulation with anti-inflammation detumescence analgesic activity, the percentage by weight of making the active ingredient raw material of medicine and accounting for whole preparation is:
(1) aescine and its acceptable salt 20% pharmaceutically;
(2) ketoprofen, thiophene are coughed up fragrant acid, thiophene is coughed up the pharmaceutically mixture 0.01% of acceptable salt, meloxicam, piroxicam and naproxen of fragrant acid;
All the other are adjuvant.Can be used for the treatment of local muscle, joint, neural inflammation, pain.
Embodiment 25.A kind of external-use pharmaceutical composition formulation with anti-inflammation detumescence analgesic activity, the percentage by weight of making the active ingredient raw material of medicine and accounting for whole preparation is:
(1) aescine and its acceptable salt 0.05% pharmaceutically;
(2) ketoprofen, thiophene are coughed up fragrant acid, thiophene is coughed up the pharmaceutically mixture 8% of acceptable salt, meloxicam, piroxicam and naproxen of fragrant acid;
All the other are adjuvant.Can be used for the treatment of local muscle, joint, neural inflammation, pain.
Embodiment 26.A kind of external-use pharmaceutical composition formulation with anti-inflammation detumescence analgesic activity, the percentage by weight of making the active ingredient raw material of medicine and accounting for whole preparation is:
(1) aescine and its acceptable salt 1% pharmaceutically;
(2) ketoprofen, thiophene are coughed up fragrant acid, thiophene is coughed up the pharmaceutically mixture 0.05% of acceptable salt, meloxicam, piroxicam and naproxen of fragrant acid;
All the other are adjuvant.Can be used for the treatment of local muscle, joint, neural inflammation, pain.
Embodiment 27.A kind of external-use pharmaceutical composition formulation with anti-inflammation detumescence analgesic activity, the percentage by weight of making the active ingredient raw material of medicine and accounting for whole preparation is:
(1) aescine and its acceptable salt 15% pharmaceutically;
(2) ketoprofen, thiophene are coughed up fragrant acid, thiophene is coughed up the pharmaceutically mixture 6% of acceptable salt, meloxicam, piroxicam and naproxen of fragrant acid;
All the other are adjuvant.Can be used for the treatment of local muscle, joint, neural inflammation, pain.
Embodiment 28.A kind of external-use pharmaceutical composition formulation with anti-inflammation detumescence analgesic activity, the percentage by weight of making the active ingredient raw material of medicine and accounting for whole preparation is:
(1) aescine and its acceptable salt 18 % pharmaceutically;
(2) ketoprofen, thiophene are coughed up fragrant acid, thiophene is coughed up the pharmaceutically mixture 7% of acceptable salt, meloxicam, piroxicam and naproxen of fragrant acid;
All the other are adjuvant.Can be used for the treatment of local muscle, joint, neural inflammation, pain.
Embodiment 29.A kind of external-use pharmaceutical composition formulation with anti-inflammation detumescence analgesic activity, the percentage by weight of making the active ingredient raw material of medicine and accounting for whole preparation is:
(1) aescine or its acceptable salt 0.1% pharmaceutically;
(2) ketoprofen, thiophene are coughed up fragrant acid, thiophene is coughed up a kind of 0.01% in fragrant sour pharmaceutically acceptable salt, meloxicam, piroxicam and the naproxen.
All the other are adjuvant.Can be used for the treatment of local muscle, joint, neural inflammation, pain.
Embodiment 30.A kind of external-use pharmaceutical composition formulation with anti-inflammation detumescence analgesic activity, the percentage by weight of making the active ingredient raw material of medicine and accounting for whole preparation is:
(1) aescine or its acceptable salt 5% pharmaceutically;
(2) ketoprofen, thiophene are coughed up fragrant acid, thiophene is coughed up a kind of 5% in fragrant sour pharmaceutically acceptable salt, meloxicam, piroxicam and the naproxen.
All the other are adjuvant.Can be used for the treatment of local muscle, joint, neural inflammation, pain.
Embodiment 31.A kind of external-use pharmaceutical composition formulation with anti-inflammation detumescence analgesic activity, the percentage by weight of making the active ingredient raw material of medicine and accounting for whole preparation is:
(1) aescine or its acceptable salt 0.5% pharmaceutically;
(2) ketoprofen, thiophene are coughed up fragrant acid, thiophene is coughed up a kind of 4% in fragrant sour pharmaceutically acceptable salt, meloxicam, piroxicam and the naproxen.
All the other are adjuvant.Can be used for the treatment of local muscle, joint, neural inflammation, pain.
Embodiment 32.A kind of external-use pharmaceutical composition formulation with anti-inflammation detumescence analgesic activity, the percentage by weight of making the active ingredient raw material of medicine and accounting for whole preparation is:
(1) aescine or its acceptable salt 1% pharmaceutically;
(2) ketoprofen, thiophene are coughed up fragrant acid, thiophene is coughed up a kind of 0.05% in fragrant sour pharmaceutically acceptable salt, meloxicam, piroxicam and the naproxen.
All the other are adjuvant.Can be used for the treatment of local muscle, joint, neural inflammation, pain.
Embodiment 33.A kind of external-use pharmaceutical composition formulation with anti-inflammation detumescence analgesic activity, the percentage by weight of making the active ingredient raw material of medicine and accounting for whole preparation is:
(1) aescine or its acceptable salt 2% pharmaceutically;
(2) ketoprofen, thiophene are coughed up fragrant acid, thiophene is coughed up a kind of 0.1% in fragrant sour pharmaceutically acceptable salt, meloxicam, piroxicam and the naproxen.
All the other are adjuvant.Can be used for the treatment of local muscle, joint, neural inflammation, pain.
Embodiment 34.A kind of external-use pharmaceutical composition formulation with anti-inflammation detumescence analgesic activity, the percentage by weight of making the active ingredient raw material of medicine and accounting for whole preparation is:
(1) aescine or its acceptable salt 3% pharmaceutically;
(2) ketoprofen, thiophene are coughed up fragrant acid, thiophene is coughed up a kind of 1% in fragrant sour pharmaceutically acceptable salt, meloxicam, piroxicam and the naproxen.
All the other are adjuvant.Can be used for the treatment of local muscle, joint, neural inflammation, pain.
Embodiment 35.A kind of external-use pharmaceutical composition formulation with anti-inflammation detumescence analgesic activity, the percentage by weight of making the active ingredient raw material of medicine and accounting for whole preparation is:
(1) aescine or its acceptable salt 4% pharmaceutically;
(2) ketoprofen, thiophene are coughed up fragrant acid, thiophene is coughed up a kind of 2% in fragrant sour pharmaceutically acceptable salt, meloxicam, piroxicam and the naproxen.
All the other are adjuvant.Can be used for the treatment of local muscle, joint, neural inflammation, pain.
Embodiment 36.A kind of external-use pharmaceutical composition formulation with anti-inflammation detumescence analgesic activity, the percentage by weight of making the active ingredient raw material of medicine and accounting for whole preparation is:
(1) aescine or its acceptable salt 1.5% pharmaceutically;
(2) ketoprofen, thiophene are coughed up fragrant acid, thiophene is coughed up a kind of 3% in fragrant sour pharmaceutically acceptable salt, meloxicam, piroxicam and the naproxen.
All the other are adjuvant.Can be used for the treatment of local muscle, joint, neural inflammation, pain.
Embodiment 37.A kind of external-use pharmaceutical composition formulation with anti-inflammation detumescence analgesic activity, the percentage by weight of making the active ingredient raw material of medicine and accounting for whole preparation is:
(1) aescine and its acceptable salt 0.1～5 % pharmaceutically;
(2) ketoprofen, thiophene are coughed up fragrant acid, thiophene is coughed up the mixture 0.01～5% that the 2-5 kind in fragrant sour pharmaceutically acceptable salt, meloxicam, piroxicam and the naproxen is mixed with arbitrary proportion.
All the other are adjuvant.Can be used for the treatment of local muscle, joint, neural inflammation, pain.
Embodiment 38.A kind of external-use pharmaceutical composition formulation with anti-inflammation detumescence analgesic activity, the percentage by weight of making the active ingredient raw material of medicine and accounting for whole preparation is:
(1) aescine and its acceptable salt 0.1% pharmaceutically;
(2) ketoprofen, thiophene are coughed up fragrant acid, thiophene is coughed up the mixture 0.01% that the 2-5 kind in fragrant sour pharmaceutically acceptable salt, meloxicam, piroxicam and the naproxen is mixed with arbitrary proportion.
All the other are adjuvant.Can be used for the treatment of local muscle, joint, neural inflammation, pain.
Embodiment 39.A kind of external-use pharmaceutical composition formulation with anti-inflammation detumescence analgesic activity, the percentage by weight of making the active ingredient raw material of medicine and accounting for whole preparation is:
(1) aescine and its acceptable salt 5% pharmaceutically;
(2) ketoprofen, thiophene are coughed up fragrant acid, thiophene is coughed up the mixture 5% that the 2-5 kind in fragrant sour pharmaceutically acceptable salt, meloxicam, piroxicam and the naproxen is mixed with arbitrary proportion.
All the other are adjuvant.Can be used for the treatment of local muscle, joint, neural inflammation, pain.
Embodiment 40.A kind of external-use pharmaceutical composition formulation with anti-inflammation detumescence analgesic activity, the percentage by weight of making the active ingredient raw material of medicine and accounting for whole preparation is:
(1) aescine and its acceptable salt 2% pharmaceutically;
(2) ketoprofen, thiophene are coughed up fragrant acid, thiophene is coughed up the mixture 1% that the 2-5 kind in fragrant sour pharmaceutically acceptable salt, meloxicam, piroxicam and the naproxen is mixed with arbitrary proportion.
All the other are adjuvant.Can be used for the treatment of local muscle, joint, neural inflammation, pain.
Embodiment 41.A kind of external-use pharmaceutical composition formulation with anti-inflammation detumescence analgesic activity, the percentage by weight of making the active ingredient raw material of medicine and accounting for whole preparation is:
(1) aescine and its acceptable salt 5% pharmaceutically;
(2) ketoprofen, thiophene are coughed up fragrant acid, thiophene is coughed up the mixture 0.01% that the 2-5 kind in fragrant sour pharmaceutically acceptable salt, meloxicam, piroxicam and the naproxen is mixed with arbitrary proportion.
All the other are adjuvant.Can be used for the treatment of local muscle, joint, neural inflammation, pain.
Embodiment 43.A kind of external-use pharmaceutical composition formulation with anti-inflammation detumescence analgesic activity, the percentage by weight of making the active ingredient raw material of medicine and accounting for whole preparation is:
(1) aescine or its acceptable salt 0.1% pharmaceutically;
(2) ketoprofen, thiophene are coughed up fragrant acid, thiophene is coughed up the mixture 5% that the 2-5 kind in fragrant sour pharmaceutically acceptable salt, meloxicam, piroxicam and the naproxen is mixed with arbitrary proportion.
All the other are adjuvant.Can be used for the treatment of local muscle, joint, neural inflammation, pain.
Embodiment 44.A kind of external-use pharmaceutical composition formulation with anti-inflammation detumescence analgesic activity, the percentage by weight of making the active ingredient raw material of medicine and accounting for whole preparation is:
(1) aescine and its acceptable salt 2.5% pharmaceutically;
(2) ketoprofen, thiophene are coughed up fragrant acid, thiophene is coughed up the mixture 1.5% that the 2-5 kind in fragrant sour pharmaceutically acceptable salt, meloxicam, piroxicam and the naproxen is mixed with arbitrary proportion.
All the other are adjuvant.Can be used for the treatment of local muscle, joint, neural inflammation, pain.
Embodiment 45.A kind of external-use pharmaceutical composition formulation with anti-inflammation detumescence analgesic activity, the percentage by weight of making the active ingredient raw material of medicine and accounting for whole preparation is:
(1) aescine and its acceptable salt 5% pharmaceutically;
(2) ketoprofen, thiophene are coughed up fragrant acid, thiophene is coughed up the pharmaceutically mixture 5% of acceptable salt, meloxicam, piroxicam and naproxen of fragrant acid.
All the other are adjuvant.Can be used for the treatment of local muscle, joint, neural inflammation, pain.
Embodiment 46.A kind of external-use pharmaceutical composition formulation with anti-inflammation detumescence analgesic activity, the percentage by weight of making the active ingredient raw material of medicine and accounting for whole preparation is:
(1) aescine and its acceptable salt 2% pharmaceutically;
(2) ketoprofen, thiophene are coughed up fragrant acid, thiophene is coughed up the pharmaceutically mixture 0.01% of acceptable salt, meloxicam, piroxicam and naproxen of fragrant acid.
All the other are adjuvant.Can be used for the treatment of local muscle, joint, neural inflammation, pain.
Embodiment 47.A kind of external-use pharmaceutical composition formulation with anti-inflammation detumescence analgesic activity, the percentage by weight of making the active ingredient raw material of medicine and accounting for whole preparation is:
(1) aescine or its acceptable salt 0.1% pharmaceutically;
(2) ketoprofen, thiophene are coughed up fragrant acid, thiophene is coughed up the pharmaceutically mixture 5% of acceptable salt, meloxicam, piroxicam and naproxen of fragrant acid.
All the other are adjuvant.Can be used for the treatment of local muscle, joint, neural inflammation, pain.
Embodiment 48.A kind of external-use pharmaceutical composition formulation with anti-inflammation detumescence analgesic activity, the percentage by weight of making the active ingredient raw material of medicine and accounting for whole preparation is:
(1) aescine and its acceptable salt 1% pharmaceutically;
(2) ketoprofen, thiophene cough up fragrant acid, thiophene cough up fragrant acid pharmaceutically in acceptable salt, meloxicam, piroxicam, the naproxen any a kind or arbitrarily the 2-5 kind with the mixture 0.1% of any ratio.
All the other are adjuvant.Can be used for the treatment of local muscle, joint, neural inflammation, pain.
Embodiment 49.A kind of external-use pharmaceutical composition formulation with anti-inflammation detumescence analgesic activity, the percentage by weight of making the active ingredient raw material of medicine and accounting for whole preparation is:
(1) aescine and its acceptable salt 1% pharmaceutically;
(2) ketoprofen, thiophene cough up fragrant acid, thiophene cough up fragrant acid pharmaceutically in acceptable salt, meloxicam, piroxicam, the naproxen any a kind or arbitrarily the 2-5 kind with the mixture 5% of any ratio.
All the other are adjuvant.Can be used for the treatment of local muscle, joint, neural inflammation, pain.
Embodiment 50.A kind of external-use pharmaceutical composition formulation with anti-inflammation detumescence analgesic activity, the percentage by weight of making the active ingredient raw material of medicine and accounting for whole preparation is:
(1) aescine and its acceptable salt 1% pharmaceutically;
(2) ketoprofen, thiophene cough up fragrant acid, thiophene cough up fragrant acid pharmaceutically in acceptable salt, meloxicam, piroxicam, the naproxen any a kind or arbitrarily the 2-5 kind with the mixture 1% of any ratio.
All the other are adjuvant.Can be used for the treatment of local muscle, joint, neural inflammation, pain.
Embodiment 51.A kind of external-use pharmaceutical composition formulation with anti-inflammation detumescence analgesic activity, the percentage by weight of making the active ingredient raw material of medicine and accounting for whole preparation is:
(1) aescine or its acceptable salt 1% pharmaceutically;
(2) ketoprofen, thiophene cough up fragrant acid, thiophene cough up fragrant acid pharmaceutically in acceptable salt, meloxicam, piroxicam, the naproxen any a kind or arbitrarily the 2-5 kind with the mixture 2.5% of any ratio.
All the other are adjuvant.Can be used for the treatment of local muscle, joint, neural inflammation, pain.
Embodiment 52.A kind of external-use pharmaceutical composition formulation with anti-inflammation detumescence analgesic activity, the percentage by weight of making the active ingredient raw material of medicine and accounting for whole preparation is:
(1) aescine or its acceptable salt 1% pharmaceutically;
(2) ketoprofen, thiophene are coughed up fragrant acid, thiophene is coughed up the pharmaceutically mixture 0.1% of acceptable salt, meloxicam, piroxicam, naproxen of fragrant acid.
All the other are adjuvant.Can be used for the treatment of local muscle, joint, neural inflammation, pain.
Embodiment 53.A kind of external-use pharmaceutical composition formulation with anti-inflammation detumescence analgesic activity, the percentage by weight of making the active ingredient raw material of medicine and accounting for whole preparation is:
(1) aescine or its acceptable salt 1% pharmaceutically;
(2) ketoprofen, thiophene are coughed up fragrant acid, thiophene is coughed up the pharmaceutically mixture 5% of acceptable salt, meloxicam, piroxicam, naproxen of fragrant acid.
All the other are adjuvant.Can be used for the treatment of local muscle, joint, neural inflammation, pain.
Embodiment 54.A kind of external-use pharmaceutical composition formulation with anti-inflammation detumescence analgesic activity, the percentage by weight of making the active ingredient raw material of medicine and accounting for whole preparation is:
(1) aescine and its acceptable salt 1% pharmaceutically;
(2) ketoprofen, thiophene are coughed up fragrant acid, thiophene is coughed up the pharmaceutically mixture 1% of acceptable salt, meloxicam, piroxicam, naproxen of fragrant acid.
All the other are adjuvant.Can be used for the treatment of local muscle, joint, neural inflammation, pain.
Embodiment 55.A kind of external-use pharmaceutical composition formulation with anti-inflammation detumescence analgesic activity, the percentage by weight of making the active ingredient raw material of medicine and accounting for whole preparation is:
(1) aescine and its acceptable salt 1% pharmaceutically;
(2) ketoprofen, thiophene are coughed up fragrant acid, thiophene is coughed up the pharmaceutically mixture 2% of acceptable salt, meloxicam, piroxicam, naproxen of fragrant acid.
All the other are adjuvant.Can be used for the treatment of local muscle, joint, neural inflammation, pain.
Embodiment 56.In embodiment 1-55 in any one described preparation, described aescine refers to the total saponins that extracts from Hippocastanaceae buckeye Aesculus, Aesculus chinensis Bunge, Radix Aesculi, Aesculus hippocastanum L. or Aesculus turbinata B1 seed, perhaps refer to state at least a extract as main component in aescine A, aescine B, aescine C, aescine D, aescine E and the aescine F that extracts in the seed in the past; Described aescine pharmaceutically acceptable salt refers to the salt that aforesaid aescine and pharmaceutically acceptable inorganic base or organic base reaction generate, and comprises the aescine sodium salt, aescine potassium salt, magnesium aescine, the aescine calcium salt, arginine aescine, ornithine aescine, lysine aescine, histidine aescine, ethylenediamine aescine, diethylamine aescine, aescine monoethanolamine salt, diethanolamine aescine, triethanolamine aescine, aescine meglumine salt or aescine ammonium salt.
Embodiment 57.In embodiment 1-55 in any one described preparation, described thiophene cough up fragrant acid pharmaceutically acceptable salt refer to that thiophene coughs up the salt of fragrant acid and pharmaceutically acceptable inorganic base or organic base reaction generation, comprise that thiophene coughs up fragrant acid sodium-salt, thiophene is coughed up fragrant acid potassium salt, thiophene is coughed up fragrant sour magnesium salt, thiophene is coughed up fragrant acid calcium salt, thiophene is coughed up fragrant sour arginine salt, thiophene is coughed up fragrant sour ornithine salt, thiophene is coughed up fragrant sour lysinate, thiophene is coughed up fragrant sour histidine salt, thiophene is coughed up fragrant sour ethylenediamine salt, thiophene is coughed up fragrant diethylammonium salt salt, thiophene is coughed up fragrant sour monoethanolamine salt, thiophene is coughed up fragrant sour diethanolamine salt, thiophene is coughed up fragrant triethylenetetraminehexaacetic acid alcohol amine salt, thiophene is coughed up fragrant sour meglumine salt or thiophene is coughed up fragrant acid ammonium salt.
Any one described preparation among the above embodiment 1-57, its dosage form is any medically acceptable exterior-applied formulation, comprises tincture, ointment, ointment, gel, patch, membrane, cataplasma, lotion, liniment, aerosol, spray, rubber-emplastrum or liniment.Used adjuvant can be selected conventional adjuvant by dosage form, adds according to a conventional method the external used medicine that the active ingredient raw material is made corresponding dosage form again.
Embodiment 58.A kind of external-use pharmaceutical composition formulation with anti-inflammation detumescence analgesic activity.Present embodiment adopts aescine 1% (percentage by weight, lower same), ketoprofen 2.5%, and medium carrier adopts vaseline, liquid Paraffin, ethyl hydroxybenzoate, makes ointment.Be used for the treatment of local myalgia.
Embodiment 59.A kind of external-use pharmaceutical composition formulation with anti-inflammation detumescence analgesic activity.Present embodiment adopts aescine 1.5% (percentage by weight, lower same), thiophene to cough up fragrant sour sodium 2%, and medium carrier adopts vaseline, liquid Paraffin, ethyl hydroxybenzoate, makes ointment.Be used for the treatment of and sprain.
Embodiment 60.A kind of external-use pharmaceutical composition formulation with anti-inflammation detumescence analgesic activity.Present embodiment adopts aescine A 0.01% (percentage by weight, lower same), meloxicam 0.5%, and medium carrier adopts carbopol, and ethanol, glycerol, Polysorbate, ethyl hydroxybenzoate, sodium hydroxide, distilled water make gel.Be used for the treatment of cervical vertebra pain.
Embodiment 61.A kind of external-use pharmaceutical composition formulation with anti-inflammation detumescence analgesic activity.Present embodiment adopts aescine B 0.9% (percentage by weight, lower same), piroxicam 0.5%, adopts 60% ethanol dilution, makes tincture.Be used for the treatment of arthralgia.
Embodiment 62.A kind of external-use pharmaceutical composition formulation with anti-inflammation detumescence analgesic activity.Present embodiment adopts arginine aescine 1.5% (percentage by weight, down together), naproxen 1%, medium carrier adopts sodium polyacrylate, starch propionate, methyl hydroxybenzoate, third of nipalgin, Polysorbate, vinyl acetate, dried aluminum hydroxide gel, water make cataplasma.Be used for the treatment of hyperosteogeny.
Embodiment 63.A kind of external-use pharmaceutical composition formulation with anti-inflammation detumescence analgesic activity.Present embodiment adopts magnesium aescine 1.1% (percentage by weight, lower same), dexketoprofen 2%, naproxen 0.01%, and medium carrier adopts dibutyl phthalate, polyvinyl formal-acetal, acetone, 70% ethanol, makes liniment.Be used for the treatment of traumatic injury.
Embodiment 64.A kind of external-use pharmaceutical composition formulation with anti-inflammation detumescence analgesic activity.Present embodiment adopts lysine aescine 1.8% (percentage by weight, lower with), thiophene to cough up fragrant acid 1%, meloxicam 0.3%, and medium carrier adopts Polysorbate, glycerol, potassium sorbate, ethylparaben, makes lotion.Be used for the treatment of chronic muscular strain.
Embodiment 65.A kind of external-use pharmaceutical composition formulation with anti-inflammation detumescence analgesic activity.Present embodiment adopts histidine aescine 1% (percentage by weight, lower same), naproxen 0.5%, piroxicam 0.3%, and medium carrier adopts propylene glycol, ethanol, laurocapram, ethylparaben, makes liniment.Be used for the treatment of lumbar vertebra pain.
Embodiment 66.A kind of external-use pharmaceutical composition formulation with anti-inflammation detumescence analgesic activity.Present embodiment adopts ethylenediamine aescine 0.001% (percentage by weight, down together), naproxen 1%, left-handed ketoprofen 1.5%, medium carrier adopts rubber, Colophonium, vaseline, white oil, lanoline, dimethyl sulfoxine, laurocapram, makes rubber-emplastrum.Be used for the treatment of arthritis.
Embodiment 67.A kind of external-use pharmaceutical composition formulation with anti-inflammation detumescence analgesic activity.Present embodiment adopts diethylamine aescine 0.001% (percentage by weight, lower same), meloxicam 0.3%, naproxen 0.5%, ketoprofen 0.3%, and medium carrier adopts medical PVA, and distilled water, propylene glycol make membrane.Be used for the treatment of muscle sprain.
Embodiment 68.A kind of external-use pharmaceutical composition formulation with anti-inflammation detumescence analgesic activity.Present embodiment adopts diethanolamine aescine 0.001% (percentage by weight, down together), racemization ketoprofen 2%, piroxicam 0.3%, naproxen 0.3%, thiophene is coughed up fragrant acid 0.3%, meloxicam 0.2%, medium carrier adopts polyvinyl alcohol, polyvidone, propylene glycol, laurocapram, makes patch.Be used for the treatment of the partial gall that fracture causes.
Embodiment 69.A kind of external-use pharmaceutical composition formulation with anti-inflammation detumescence analgesic activity.Present embodiment adopts triethanolamine aescine 0.8% (percentage by weight, lower same), piroxicam 0.3%, and medium carrier adopts 95% ethanol, dichlorodifluoromethane, makes aerosol.Be used for the treatment of cancer pain.
Claims (5)
1. the external-use pharmaceutical composition formulation with anti-inflammation detumescence analgesic activity is characterized in that, the percentage by weight of making the active ingredient raw material of medicine and accounting for whole preparation is:
(1) aescine and its acceptable salt 1% pharmaceutically;
(2) ketoprofen, thiophene are coughed up fragrant acid, thiophene and are coughed up pharmaceutically one or more in acceptable salt, meloxicam, piroxicam and the naproxen 0.1～5% of fragrant acid.
2. preparation according to claim 1, it is characterized in that, described aescine refers to the total saponins that extracts from Hippocastanaceae buckeye Aesculus, Aesculus chinensis Bunge, Radix Aesculi, Aesculus hippocastanum L. or Aesculus turbinata B1 seed, perhaps refer to state at least a extract as main component in aescine A, aescine B, aescine C, aescine D, aescine E and the aescine F that extracts in the seed in the past; Described aescine pharmaceutically acceptable salt refers to the salt that aforesaid aescine and pharmaceutically acceptable inorganic base or organic base reaction generate, and comprises the aescine sodium salt, aescine potassium salt, magnesium aescine, the aescine calcium salt, arginine aescine, ornithine aescine, lysine aescine, histidine aescine, ethylenediamine aescine, diethylamine aescine, aescine monoethanolamine salt, diethanolamine aescine, triethanolamine aescine, aescine meglumine salt or aescine ammonium salt.
3. preparation according to claim 1, it is characterized in that, described thiophene cough up fragrant acid pharmaceutically acceptable salt refer to that thiophene coughs up the salt of fragrant acid and pharmaceutically acceptable inorganic base or organic base reaction generation, comprise that thiophene coughs up fragrant acid sodium-salt, thiophene is coughed up fragrant acid potassium salt, thiophene is coughed up fragrant sour magnesium salt, thiophene is coughed up fragrant acid calcium salt, thiophene is coughed up fragrant sour arginine salt, thiophene is coughed up fragrant sour ornithine salt, thiophene is coughed up fragrant sour lysinate, thiophene is coughed up fragrant sour histidine salt, thiophene is coughed up fragrant sour ethylenediamine salt, thiophene is coughed up fragrant diethylammonium salt salt, thiophene is coughed up fragrant sour monoethanolamine salt, thiophene is coughed up fragrant sour diethanolamine salt, thiophene is coughed up fragrant triethylenetetraminehexaacetic acid alcohol amine salt, thiophene is coughed up fragrant sour meglumine salt or thiophene is coughed up fragrant acid ammonium salt.
4. preparation according to claim 1, it is characterized in that, its dosage form is any medically acceptable exterior-applied formulation, comprises tincture, ointment, ointment, gel, patch, membrane, cataplasma, lotion, liniment, aerosol, spray, rubber-emplastrum or liniment.
5. preparation as claimed in claim 1 is preparing the purposes for the treatment of in arthralgia and the arthritic medicine.
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| CN1771981A (en) | 2005-10-18 | 2006-05-17 | 夏运岳 | Pile ointment |
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