CN1060334C - Analgesic 'Kangnaipan' - Google Patents
Analgesic 'Kangnaipan' Download PDFInfo
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- CN1060334C CN1060334C CN94108418A CN94108418A CN1060334C CN 1060334 C CN1060334 C CN 1060334C CN 94108418 A CN94108418 A CN 94108418A CN 94108418 A CN94108418 A CN 94108418A CN 1060334 C CN1060334 C CN 1060334C
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- analgesic
- oxycet
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- nefopam
- edible plant
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Abstract
The present invention relates to an analgesic, namely 'kangnaipan', more specifically, the analgesic is prepared by mixing two existing analgesics according to sieving proportion. The analgesic 'kangnaipan' of the present invention is composed of naproxen and nefopam which are combined according to the weight ratio of 2 to 12:1. The effect of the analgesic 'kangnaipan' of the present invention is better than that of the existing febrifuge anti-inflammatory analgesic and the existing opium analgesic, and the dosages are fewer. Thereby, the side effect of the present invention is relieved, and the present invention has extensive applicable symptoms. Therefore, the present invention has a broad market prospect.
Description
What the present invention relates to is a kind of analgesia new drug, and concretely, it is a kind of by the ratio composite a kind of Oxycet that form of existing two kinds of analgesic in screening.
Analgesics is can make pain relief or alleviation and realize unlikely forfeiture, and other feel impregnable medicine.Existing analgesic has analgesic anti-inflammation and analgesic drugs, Opium class analgesic and other to have the medicine of analgesia or assosting effect.
1. analgesic anti-inflammatory analgesic: be applicable to mild pain, invalid to various severe trauma severe pain and visceral smooth muscle angor.Characteristics are no addiction, do not suppress to breathe.Its site of action is mainly in periphery, and the synthetic of prostaglandin worked during by inflammation-inhibiting.As aspirin, acetaminophen, the general life of the bitter edible plant, but aspirin has stimulation to gastrointestinal tract, is difficult for being accepted by the patient; Acetaminophen is little to the GI irritation effect, is easily accepted by the patient, and analgesic activity is more weak and do not have an antiinflammatory effect; The general life of the bitter edible plant is tool analgesia, antiinflammatory, refrigeration function one of the strongest medicine, and is also lighter to gastrointestinal reaction.
2. Opium class analgesic: mainly act on the central nervous system, analgesic activity is powerful, is applicable to the above pain of moderate, and characteristics are to use repeatedly to be easy to addiction, so claim addicted analgesics again, the inhibition Repiration are arranged.Dissolve as morphine, naloxone, bitter edible plant good fortune.It is novel strong analgesics that the bitter edible plant is dissolved rapidly, no addiction, does not suppress to breathe, and untoward reaction is few, and so its mechanism of action is along not clear.Tranquilizer, psychosis worker and antidepressants are often accompanied ancillary drug and are used for treatment of pain, particularly with melancholy or other mental symptoms.
At present, analgesic anti-inflammatory analgesic is subjected to more idea.WHO recommends three grades and goes up the pain therapy: the patient to mild pain uses analgesic anti-inflammatory analgesic; The moderate pain-suffered patient is used weak Opium class medicines such as codeine; To there being the patient who has an intense pain to select strong Opium class medicines such as morphine for use.In the treatment process, still according to circumstances add with adjuvant drugs such as tranquilizer.Because the Opium class analgesic of treatment moderate above pain has addiction to pay effect,, thereby partly there is the patient of severe pain to be in the circumstances that no potent analgesics treats and in pain, decocts in addition both at home and abroad to the strict control of addicted analgesics.
It is strong to press for analgesic activity clinically, easy-to-use and analgesia new drug that unfavorable factors such as addiction are few.
The object of the present invention is to provide a kind of analgesic activity strong, the analgesia new drug that side effect is little is to meet clinical needs.
The objective of the invention is and can reach by following technical measures, the novel compound analgesic is that (Nefpan, Nef) (Neproxen Nep) forms, and the general life of the nefopam and the bitter edible plant is by the combination of 1: 2～12 weight ratios with the general life of the bitter edible plant by nefopam.
The general life of the nefopam and the bitter edible plant is combined as best by 1: 3.5～6 weight ratios.
Nefopam is a kind of non-addiction strong analgesics, external commodity Nefopam by name, have another name called Acupan, Ajan, Bezoxazocine, Fenaxoxine, the Chinese another name has benzoxazocine, toluene * azoles suffering, Nefopam, chemical name is 1-phenyl-5 methyl-1,3,4, the hot hydrochlorate of 6-tetrahydrochysene-2,5 paroxazine a pair of horses going side by side oxazole.
Structural formula:
Described nefopam is a white crystalline powder, and odorless, mildly bitter flavor, are insoluble to benzene, 2.48～25.3 ℃ of fusing points at water-soluble, chloroform and methanol.Be a novel species type non-narcotic analgesics, chemical constitution belongs to the cyclisation o-methyl-diphenhydramine, and medicine mechanism is still not clear, neither opioid receptor agonist or partial agonist also are not the synthetic effects of inhibition PG that NSAID (non-steroidal anti-inflammatory drug) is arranged.To breathing, blood circulation unrestraint effect, no aspirin does not have tolerance and dependency to the gastrointestinal stimulation.Except that analgesic activity, still be central flesh pine, cholinolytic to be arranged, plan is sympathetic and slightly puts down latent bringing down a fever and anti-melancholy acting on.
The general another name of giving birth to of the bitter edible plant: congex, methoxy bitter edible plant propanoic acid.English name: Neproxon, Naprosyn, Proxen, Anaprox.
Structural formula:
Be white or micro white crystalline powder, odorless.Be soluble in the high water of PH, be dissolved in organic solvent, as ethanol, ether, chloroform.
The general life of the described bitter edible plant is the aromatic vinegar acid derivative, is a kind of non-steroidal anti-inflammatory analgesic antipyretic of high-efficiency low-toxicity.The antiinflammatory action of the general life of the experiment confirm bitter edible plant is about 11 times of Phenylbutazone, and analgesic activity is about 7 times of aspirin, and refrigeration function is about 22 times of aspirin, and action time is longer, and with aspirin machine ratio, untoward reaction is few to gastrointestinal.
The present invention dissolves bitter edible plant good fortune with the general life of the bitter edible plant to combine the novel compound analgesic according to 1: 2～12 weight ratio.
The analgesic activity of Oxycet is shown in following embodiment.
Embodiment 1-4
Contrast test adopts Ministry of Public Health to recommend analgesic experimental technique-mice hot plate method; Its result is shown in table 1,2.
Table 1. Oxycet is irritated stomach to the influence of mice hot plate method (57 ℃) (n=12, X=± SD)
* the dosage in the sequence number 1-4 in the table is nefopam before the plus sige, is that the naphthalene good fortune is given birth to after the plus sige.
Experimental result shows that sequence number 1,2 Oxycets and Nap40mg/ug irritate behind the stomach all significant prolongation incubation period.Close with it with morphine 6mg/kg, sequence number 1,2 Oxycets are significant prolongation then, and the effect of Nap40mg/kg is then not as good as morphine.Oxycet is described, what contrast model played a major role is nefopam.
The influence that table 2. Oxycet filling stomach reacts the mice acetic acid twisting (X=± SD)
* the dosage in the sequence number 1-4 in the table is nefopam before the plus sige, is that the naphthalene good fortune is given birth to after the plus sige.
The result shows that the Oxycet of sequence number 1,3 and Nef10mg/kg all significantly suppress the reaction of mice acetic acid twisting.Morphine group mouse writhing reaction incidence rate less than other 4 medication groups, but only has statistics medicine difference (P=0.037) with sequence number 4 Oxycet groups greater than sequence number 1 Oxycet group.Sequence number 1 Oxycet group mouse writhing reaction incidence rate is significantly less than Nef10mg/kg, sequence number 2 and sequence number 4 Oxycet groups.
Embodiment 5-6
The same among test method and the embodiment 1-4 only changes the wherein composition of naproxen, is meant its sodium salt at embodiment 5-6 described naproxens, and its structure is as described below:
The naproxen sodium structural formula:
Result of the test is shown in table 3,4.
Table 3. Oxycet (naproxen sodium) is irritated stomach to the influence of mice hot plate method (57 ℃) (n=12, X=± SD)
* the dosage in the sequence number 5-6 in the table is nefopam before the plus sige, is naphthalene Fu Shengna salt after the plus sige.Experimental result shows that adopting naproxen to receive the result that salt drew is consistent with the use naproxen.
The influence that table 4. Oxycet filling stomach reacts the mice acetic acid twisting (X ± SD)
* the dosage in the sequence number 5-6 in the table is nefopam before the plus sige, is naphthalene Fu Shengna salt after the plus sige.Its result is consistent with embodiment 1-4.
The result of the result of the acute toxicity test of Oxycet of the present invention (LD50) and naproxen and nefopam acute toxicity test is as follows:
(1) Oxycet: mouse stomach LD50=510MG/KG (contains Nef102mg/kg, Nap408mg/kg)
(2) Ndf: mouse stomach LD50=98mg/kg
(3) Nap: mouse stomach LD50=900mg/kg
Foregoing prompting Oxycet acute toxicity also slightly reduces than single.
Compositions of the present invention can be made into dosage forms such as tablet, micellar, slow releasing agent.
The present invention's a kind of Oxycet of new drug that eases pain is made up of general life of the bitter edible plant and nefopam, wherein the general living analgesic activity of bitter edible plant position is mainly in periphery, it is one of inhibitor of strong PG synzyme, PG's is synthetic in the time of preventing inflammation effectively, thereby analgesic activity is arranged, the site of action of nefopam is at maincenter, and it does not belong to opioid receptor agonist or partial agonist, does not also suppress the synthetic of prostaglandin.Two medicines act on the different links that pain forms, thereby use the new drug treatment pain after forming can accomplish treating both the principal and the secondary aspects of a disease at the same time, thereby play synergism, improve curative effect.It is applicable to each apoplexy due to endogenous wind severe acute and chronic pain of town.
The effect of paying of naproxen, Fenazoxine single medicinal material is few, and gastrointestinal is stimulated less than aspirin, and the present invention makes up the time spent, and survival dose reduces, thereby side effect is more alleviated, and favourablely satisfies clinical requirement.
New drug of the present invention all has stronger analgesic activity to reaching two links of maincenter on every side, has to be suitable for disease widely, thereby vast market prospect is arranged.
Claims (3)
1. an analgesic activity is strong, the analgesic that side effect is little---Oxycet, and it is made up of general the giving birth to of nefopam and the bitter edible plant, it is characterized in that described a kind of Oxycet constituent nefopam and the general life of the bitter edible plant make up by 1: 2～12 weight ratios.
2. a kind of Oxycet according to claim 1 is characterized in that the part by weight preferred 1: 3.5～6 of nefopam and the general life of the bitter edible plant.
3. a kind of Oxycet according to claim 1 is characterized in that general the surviving of the described bitter edible plant comprises the general living sodium of its derivant bitter edible plant.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN94108418A CN1060334C (en) | 1994-07-26 | 1994-07-26 | Analgesic 'Kangnaipan' |
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN94108418A CN1060334C (en) | 1994-07-26 | 1994-07-26 | Analgesic 'Kangnaipan' |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| CN1115642A CN1115642A (en) | 1996-01-31 |
| CN1060334C true CN1060334C (en) | 2001-01-10 |
Family
ID=5033463
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CN94108418A Expired - Fee Related CN1060334C (en) | 1994-07-26 | 1994-07-26 | Analgesic 'Kangnaipan' |
Country Status (1)
| Country | Link |
|---|---|
| CN (1) | CN1060334C (en) |
Families Citing this family (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN101411702B (en) * | 2008-11-29 | 2010-12-29 | 河南大学 | Nefopam hydrochloride naproxen sodium compound sustained-release preparation and preparation method thereof |
-
1994
- 1994-07-26 CN CN94108418A patent/CN1060334C/en not_active Expired - Fee Related
Non-Patent Citations (1)
| Title |
|---|
| 《当代结构药物全集》第一版 1993.1.1 王泽民主编，北京科技出版社 * |
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| Publication number | Publication date |
|---|---|
| CN1115642A (en) | 1996-01-31 |
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