CN1076195C - Composition containing zinc compound and p-acetaminophenyl acetic acid - Google Patents
Composition containing zinc compound and p-acetaminophenyl acetic acid Download PDFInfo
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- CN1076195C CN1076195C CN97109038A CN97109038A CN1076195C CN 1076195 C CN1076195 C CN 1076195C CN 97109038 A CN97109038 A CN 97109038A CN 97109038 A CN97109038 A CN 97109038A CN 1076195 C CN1076195 C CN 1076195C
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Abstract
The present invention relates to a composition which is composed of a zinc compound and p-acetaminophenyl acetic acid. The composition has the functions of regulating immunization, protecting a digestive system and replenishing zinc for organisms. The composition is used as an effective component of medicine for preventing or controlling or treating rheumatoid arthritis, medicine for preventing or controlling or treating peptic ulcer, medicine for preventing or controlling or treating peptic ulcer caused by non-steroidal anti-inflammatory medicine and medicine for preventing or controlling or treating relevant diseases caused by zinc deficiency of organisms. The zinc compound and the p-acetaminophenyl acetic acid are used as effective components for preparing a series of compositions in the medicinally acceptable form of medication.
Description
The present invention relates to contain the compositions of zinc compound and acetparaminosalol phenylacetic acid.Compositions mainly is made up of acceptable zinc compound of pharmacy and acetylaminobenzene acetic acid.This compositions has immunoregulation effect, digestive system cytoprotection and replenishes the zinc effect to body.This compositions is as the active ingredient of prevention, control or treatment medicine for treating rheumatoid arthritis; Active ingredient as prevention, control or treatment digestive ulcer medicament; Bring out the active ingredient of digestive ulcer medicament and the active ingredient that causes the diseases related medicine as prevention, control or treatment body zinc deficiency as prevention, control or treatment NSAID (non-steroidal anti-inflammatory drug).Zinc compound and acetparaminosalol phenylacetic acid and pharmaceutic adjuvant, or other medicines are made a series of pharmacy acceptable composition.
Though NSAID (non-steroidal anti-inflammatory drug) does not have breakaway action to the development of rheumatoid arthritis feelings, but can improve the symptom of the state of an illness, therefore the patient of patient with rheumatoid arthritis or other diseases related needs the clothes NSAID (non-steroidal anti-inflammatory drug) to remove many worries of pain band, improves the quality of living.
NSAID (non-steroidal anti-inflammatory drug) is to bring into play antiinflammatory action by suppressing the prostaglandin synthesis mechanism, the side effect of NSAID (non-steroidal anti-inflammatory drug) simultaneously also comes from the mechanism identical with their therapeutical effect, the most common and the serious adverse of NSAID (non-steroidal anti-inflammatory drug) is when number gastrointestinal mucosa pathological changes, this pathological changes shows as insidiousness and silent, until occurring hemorrhage or perforation just is found, as handle untimely easy threat to life.The patient of NSAID (non-steroidal anti-inflammatory drug) was taken in the data introduction, and the gastric ulcer prevalence that confirms by endoscope is 20～25%; Among the patient who is in hospital because of the gastrointestinal pathological changes, the routine number of taking NSAID (non-steroidal anti-inflammatory drug) person is 6 times of user not; NSAID (non-steroidal anti-inflammatory drug) is systemic administration not only, and local application causes the gastrointestinal mucosa pathology damage equally, therefore there is the people to propose, will suppose all that to all patients that take NSAID (non-steroidal anti-inflammatory drug) the probability that ulcer and concurrent hemorrhage or perforation take place is arranged, it is more important than treatment therefore to prevent NSAID (non-steroidal anti-inflammatory drug) to bring out ulcer.Except that the indication and dosage that uses NSAID (non-steroidal anti-inflammatory drug) grasped in strictness, in order to prevent gastric ulcer due to the NSAID (non-steroidal anti-inflammatory drug), abroad be to take misoprostol or omeprazole simultaneously, the prevention NSAID (non-steroidal anti-inflammatory drug) is to gastric mucosa injury, but medicine is extremely expensive, is difficult in the near future be extensive use of.
The acetparaminosalol phenylacetic acid is used for the treatment of rheumatoid arthritis as immunomodulator at present, determined curative effect, and safety is good, and no serious side effects is to be fit to the medicine that patient with rheumatoid arthritis is taken for a long time, and curative effect is better than golden preparation.Because disease feature and acetparaminosalol phenylacetic acid promptly do not have analgesic activity, there is not antiulcer action yet, need together to take, and the non-steroidal anti-inflammatory medical instrument has the shortcoming that causes ulcer, so there is certain defective in the acetparaminosalol phenylacetic acid in clinical use with NSAID (non-steroidal anti-inflammatory drug).
Purpose of the present invention, be at right in the treatment diseases related, there is certain defective in the acetparaminosalol phenylacetic acid in clinical use, but a kind of compositions of hyoscine is proposed, compositions mainly is made up of zinc compound and acetylaminobenzene acetic acid, promptly mainly is made up of the acceptable zinc compound of pharmacy and acetparaminosalol phenylacetic acid or alkali metal, alkali salt or zinc compound.
Zinc is biological element, belong to essential trace element, content is only second to ferrum and occupies second in human body, have very important Nutrition, known zinc is present in 200 plurality of enzymes, and zinc and nucleic acid and protein metabolism are closely related, promote growth promoter, keep vision and taste function, improve the immunocompetence of body, promote wound healing; Zinc deficiency can cause the immune organ dysplasia, and influence humoral immunization, cellular immunization, complement system, the natural defending system of body, by replenishing an amount of zinc, body's immunological function is recovered, oral zinc compound can suppress that alkaline phosphatase activities that rat assist agent arthritis brings out reduces and the minimizing of the key calcium content of femur, zinc promotes the formation of sclerotin, make the change of the blood parameters of adjuvant arthritis rats be able to remarkable recovery, during the zinc compound transdermal administration, and zinc is not owing to form metal sulfydryl albumen, it is more to enter intravital zinc, the rat of two kinds of different adjuvant-induced arthritis all there is the immunization of prevention and treatment, the effect of certain resisting rheumatoid arthritis is arranged, can compare with the golden preparation effect of injection, so zinc compound has immunization.Four kinds of organic zinc class medicine [zinc glycyrrhetates have been arranged; Zinc Acexamate; glycerin zinc and carnosine zinc] be used for the treatment of peptic ulcer; the dominant mechanism of zinc treatment peptic ulcer is the biological cell membrane stabilizing action; can stablize mastocyte; suppress the release of histamine; prevention or treatment NSAID (non-steroidal anti-inflammatory drug) are as aspirin; indomethacins etc. cause the destruction of gastric mucosal barrier and the protective effect of PGE2 and mucus minimizing; increase the PGE2 concentration and the mucus amount of gastrointestinal mucosa; protection gastrointestinal mucosa barrier; keep the integrity of mucosa form and structure; has cytoprotection; zinc has moderate gastric acid inhibitory and the excretory effect of pepsin; zinc has the effect of removing free radical by promoting synthesizing glutathion.
One of active ingredient zinc compound is meant in the compositions: inorganic zinc compounds or organic zinc compounds such as zinc acetate, zinc chloride, zinc sulfate, zinc phosphate, [alkali formula] zinc carbonate, zinc oxide, zinc hydroxide, Zinc acelylsalicylate, indomethacin zinc, zinc gluconate, structure lemon acid zinc, zinc lysine, Aspartic acid zinc, zinc glycyrrhetate, glycerin zinc, alanylhistidine zinc, acetylamino caproic acid zinc, acetylglutamide zinc, zinc stearate or zinc propionate.
One of active ingredient is meant in the compositions: acetparaminosalol phenylacetic acid or alkali metal, alkali salt or zinc compound.
Zinc compound and acetylaminobenzene acetic acid group compound have certain physiologically active, the effect that this compositions has immunoregulation effect, digestive system cytoprotection simultaneously and replenishes zinc to body.
Experimental result shows: bring out gastric mucosal damage by alleviating dehydrated alcohol, illustrate that compositions has cytoprotection to digestive system; Bring out gastric mucosal damage by alleviating the NSAID (non-steroidal anti-inflammatory drug) indomethacin, illustrate that compositions has the damage that prevention or treatment NSAID (non-steroidal anti-inflammatory drug) cause gastric mucosa and the effect of the peptic ulcer that produces.Compare with single active ingredient; replenish aspect the zinc effect at immunoregulation effect, digestive system cytoprotection with to body; the compositions pharmacological action is more perfect, more comprehensively, more reasonable, compositions has outstanding substantive distinguishing features and significant technological progress.
The purposes that contains the compositions of zinc compound and acetparaminosalol phenylacetic acid is: as the active ingredient of prevention, control or treatment medicine for treating rheumatoid arthritis; Active ingredient as prevention, control or treatment digestive ulcer medicament; Bring out the active ingredient of digestive ulcer medicament and the active ingredient that causes the diseases related medicine as prevention, control or treatment body zinc deficiency as prevention, control or treatment NSAID (non-steroidal anti-inflammatory drug).
In order to realize purpose of the present invention, with zinc compound and acetparaminosalol phenylacetic acid, handle according to the acceptable method of pharmaceutics, be prepared into a series of pharmaceutically acceptable preparations.
The type of service of zinc compound and acetylaminobenzene acetic acid group compound is: zinc compound and acetparaminosalol phenylacetic acid do not add or add pharmaceutic adjuvant as excipient, binding agent, disintegrating agent, fluidizer, lubricant, coloring agent, correctives, sweeting agent, stabilizing agent, controlled release agent, coating materials, pharmaceutic adjuvants such as isotonic agent, make per os or non-per os as: oral, intramuscular injection, subcutaneous injection, intravenous injection, rectum, the solid that vagina and skin etc. use, the compositions of form of medication such as semi-solid and liquid is as tablet, coated tablet, coated tablet, chewable tablet, buccal tablet, hard capsule, soft capsule, transfer release formulation, pill, granule, pulvis subtilis, powder, solution, oral liquid, suspension, Emulsion, injection [liquid], aseptic [lyophilizing] powder pin, oil [water] dissolubility substrate suppository, oil [water] dissolubility substrate vaginal suppository, membrane, oil [water] dissolubility ointment, the various pharmaceutically acceptable dosage forms of plaster or the like.
The main compositions of forming by zinc compound and acetylaminobenzene acetic acid, also can contain L-glutaminate as active ingredient, the N-acetyl-L-glutamine, the N-alanyl-L-glutamine, glutathion etc. or their alkali metal, alkali salt or zinc compound, histidine or N-alanyl-L-histidine or their alkali metal, alkali salt or zinc compound, leucine, isoleucine, lysine, methionine, acetylmethionine, phenylalanine, threonine, tryptophan, valine, citrulline, ornithine, glycine, alanine, proline, hydroxyproline, the acetyl hydroxyproline, glucose, fructose, galactose, misoprostol, vitamin E, vitamin D, the calcic medicine, the isopropoxy isoflavone, antipyretic analgesic, NSAID (non-steroidal anti-inflammatory drug), medicine such as gold preparation or other resisting rheumatoid arthritis medicine and pharmaceutic adjuvant etc., make per os or non-per os as: oral, intramuscular injection, subcutaneous injection, quiet injection arteries and veins, rectum, the solid that vagina and skin etc. use, pharmacy such as semisolid and liquid can be accepted the compositions of form of medication, has immunoregulation effect, digestive system cytoprotection and replenish the zinc effect to body, and as prevention, the active ingredient of control or treatment medicine for treating rheumatoid arthritis; Active ingredient as prevention, control or treatment digestive ulcer medicament; Bring out the active ingredient of digestive ulcer medicament and the active ingredient that causes the diseases related medicine as prevention, control or treatment body zinc deficiency as prevention, control or treatment NSAID (non-steroidal anti-inflammatory drug).
The use amount of this compositions effective ingredient every day is respectively: the oral administration zinc compound is that 1mg～1000mg[is with the zinc cubage] and the acetparaminosalol phenylacetic acid to be 1mg～3000mg[calculate with the acetylaminobenzene acetic acid content]; Non-per os use zinc compound as 1mg～3000mg[with the zinc cubage] and the acetparaminosalol phenylacetic acid calculate with the acetylaminobenzene acetic acid content as 1mg～1000mg[], according to concrete conditions such as the symptom of age, body weight, disease type, disease and degree, divide for several times every day and use.
This compositions does not have significant side effects to health, meets social need, and is free from environmental pollution, can be applied to commercial production.
Below in conjunction with embodiment the pharmacological action of inventive compositions is described further:
Embodiment 1: to the pharmacological action of indomethacin and alcohol-induced gastric mucosa injury:
(Gastroenterology 1979 to press the method for Robert etc.; 77:433), dosage with acetylglutamide zinc 300mg/kg/d and acetparaminosalol phenylacetic acid 100mg/kg/d is given rat oral gavage three days, administration is preceding 30 minutes the last time, indomethacin with 30mg/kg dosage is irritated stomach, irritate the dehydrated alcohol of stomach 1ml after 3 hours, locate rat after 1 hour, measure the ulcer length that is caused.
(Gastroenterology 1979 to press the method for Robert etc.; 77:433), dosage with acetylglutamide zinc 300mg/kg/d and acetparaminosalol phenylacetic acid 100mg/kg/d is given rat oral gavage three days, and administration was irritated the dehydrated alcohol of stomach 1ml after 3 hours the last time, locate rat after 1 hour, measure the ulcer length that is caused.
Table acetparaminosalol phenylacetic acid and acetylglutamide zinc are to indomethacin
The blank group of the blank group of influence [ulcer length (mm)] dehydrated alcohol dehydrated alcohol+indomethacin medication group medication group 76.3 ± 17.5 0.8 ± 1.2 120.9 ± 18.2 4.4 ± 2.1 with the alcohol-induced gastric mucosa injury
Claims (1)
1. the pharmacy acceptable composition with anti-digestive system and ulcer effect is characterized in that containing zinc compound and acetparaminosalol phenylacetic acid.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN97109038A CN1076195C (en) | 1997-03-17 | 1997-03-17 | Composition containing zinc compound and p-acetaminophenyl acetic acid |
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN97109038A CN1076195C (en) | 1997-03-17 | 1997-03-17 | Composition containing zinc compound and p-acetaminophenyl acetic acid |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| CN1166963A CN1166963A (en) | 1997-12-10 |
| CN1076195C true CN1076195C (en) | 2001-12-19 |
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| Application Number | Title | Priority Date | Filing Date |
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| CN97109038A Expired - Fee Related CN1076195C (en) | 1997-03-17 | 1997-03-17 | Composition containing zinc compound and p-acetaminophenyl acetic acid |
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| CN106461803B (en) | 2014-03-20 | 2019-01-18 | 施蓝姆伯格技术公司 | Air-gun array data reconstruction Pulse Source seismic data is ignited from Annual distribution formula |
| CN105434465B (en) * | 2015-12-14 | 2019-07-16 | 米军 | It is a kind of to prevent and treat arthritic pharmaceutical composition and preparation method thereof |
Citations (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN1139667A (en) * | 1995-07-03 | 1997-01-08 | 储亮侪 | Zinc P-acetlaminoacetate with anti ulcer and immunoregulation action |
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- 1997-03-17 CN CN97109038A patent/CN1076195C/en not_active Expired - Fee Related
Patent Citations (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN1139667A (en) * | 1995-07-03 | 1997-01-08 | 储亮侪 | Zinc P-acetlaminoacetate with anti ulcer and immunoregulation action |
Non-Patent Citations (3)
| Title |
|---|
| 中国医院药学杂志第13卷第11期 1993.1.1 杨先德，戴华成和舒平，有机酸锌化合物抗溃疡作用研究 * |
| 山东医药工业第10卷第4期 1991.1.1 庞华，张君仁，邵瑞琪和韩纪超，一种新型抗类风湿免疫调节剂对乙酰氨基苯乙酸的合成 * |
| 山东医药工业第10卷第4期 1991.1.1 庞华，张君仁，邵瑞琪和韩纪超，一种新型抗类风湿免疫调节剂对乙酰氨基苯乙酸的合成;中国医院药学杂志第13卷第11期 1993.1.1 杨先德，戴华成和舒平，有机酸锌化合物抗溃疡作用研究 * |
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| CN1166963A (en) | 1997-12-10 |
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