CN1265799C - Composite of zinc containing compound and glutamines - Google Patents
Composite of zinc containing compound and glutamines Download PDFInfo
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- CN1265799C CN1265799C CN 97109039 CN97109039A CN1265799C CN 1265799 C CN1265799 C CN 1265799C CN 97109039 CN97109039 CN 97109039 CN 97109039 A CN97109039 A CN 97109039A CN 1265799 C CN1265799 C CN 1265799C
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- zinc
- glutamines
- glutamine
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Abstract
The present invention relates to a composition comprising zinc compounds, and glutamines disclosed in formula (I) in a specification, which has the functions of immunological regulation, digestive system cytoprotection, and replenishment of zinc and/or glutamines to an organism. The composition is used as an effective component of a drug for preventing, controlling or treating peptic ulcer, peptic ulcer induced by a non-steroidal anti-inflammatory drug, harm of ethanol to a digestive system, relevant diseases caused by difficiency of zinc and/or glutamines, etc. Zinc compounds and glutamines are used as effective components which are made into a series of pharmacologically acceptable compositions.
Description
The present invention relates to contain the compositions of zinc compound and glutamy amine.Compositions is mainly formed by the acceptable zinc compound of pharmacy with suc as formula the glutamy amine shown in (I) or alkali metal, alkali salt or zinc compound.This compositions has immunoregulation effect, digestive system cytoprotection, cheats the effect of the additional zinc of body and/or the effect of additional glutamine.This compositions is as the active ingredient of prevention, control or treatment digestive ulcer medicament; Bring out the active ingredient of digestive ulcer medicament as prevention, control or treatment NSAID (non-steroidal anti-inflammatory drug); Prevention, control or treatment ethanol are to the active ingredient of digestion system damage medicine; Cause the active ingredient of diseases related medicine as prevention, control or treatment body zinc deficiency; Cause the active ingredient of diseases related medicine as prevention, control or treatment body glutamine shortage.Zinc compound and glutamy amine and pharmaceutic adjuvant, perhaps other medicines are made a series of pharmacy acceptable composition.
The glutamine compounds is characterized in that in the formula (I):
Formula (I)
R
1Be H, R
2It when being H L-glutaminate;
R
1Be-COCH
3, R
2When being H acetylglutamide [N-acetyl-L-glutamine];
R
1Be-COCH
2CH
2NH
2, R
2When being H alanyl glutamine [N-alanyl-L-glutamine];
R
1Be H, R
2Be
The time be to be glutathion [γ-L-glutamy-L-cysteinyl-glycine] or their pharmaceutically acceptable 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, has very important Nutrition, just confirm that in 1934 zinc is human indispensable biological element, known zinc is present in 200 plurality of enzymes, zinc and nucleic acid and protein metabolism are closely related, in the retina location, keep vision and taste function, aspects such as the normal growth of skeleton all are essential, particularly the g and D to the child has important function, improves the immunocompetence of body, promotes wound healing, and can prevent or treat peptic ulcer, the prevention carbon tetrachloride, ethanol, hepatic injury due to alkylating agent and the cadmium.Zinc deficiency can cause the immune organ dysplasia, and influences the natural defending system of humoral immunization, cellular immunization, complement system and body, by replenishing an amount of zinc, body's immunological function is recovered.Zinc compound has been used for sicklemia, rheumatoid arthritis, at wound healing, zinc deficiency, viral influenza, infantile diarrhea, hepatic disease and the gastric ulcer of operations such as acute tissue injury, burn, surgery, promote body's immunological function to recover, certain therapeutical effect is arranged.
Just found that zinc compound had certain therapeutical effect to peptic ulcer in 72 years clinically, found that zinc compound had prevention and therapeutical effect to experimental peptic ulcer model in 1976, zinc compound has human body immunity improving ability and digestive system cytoprotection; Has the biological cell membrane stabilizing action, prevent mast cell degranulation, suppress to discharge the effect of histamine, zinc is by the activity of metal sulfydryl albumen and glutathion, has the effect of removing free radical, keep gastrointestinal tract mucous epithelial cell integrity, prevent NSAID (non-steroidal anti-inflammatory drug) as: aspirin, indomethacin etc. causes the destruction and the PGE of gastric mucosal barrier
2With the protective effect that mucus reduces, quicken the division and the propagation of cell, the reparation of damage location there is the healing of promotion effect.Zinc compound has the stomach of inhibition H
+, K
+The effect of-ATP enzyme, zinc compound not only suppress urease, suppress the growth of campylobacter pyloridis, and clinical treatment has also been proved conclusively zinc compound campylobacter pyloridis is had good killing action.There have been four kinds of organic zinc compound class medicines [zinc glycyrrhetate, Zinc Acexamate, glycerin zinc and alanylhistidine zinc] to be used for the treatment of peptic ulcer.
In a word, zinc compound is when the treatment peptic ulcer, though have cytoprotection, zinc ion all is to work indirectly, can not participate in histiocytic reparation and formation directly, can not provide to repair required energy and nutrient substance.Therefore certain defective that the existing zinc compound class medicine that is used for the treatment of peptic ulcer exists on treatment mechanism.
Purpose of the present invention is to improve at above-mentioned the deficiencies in the prior art, but proposes a kind of compositions of hyoscine, and compositions mainly is made up of zinc compound and glutamy amine, i.e. acceptable zinc compound of pharmacy and the acceptable salt of glutamy amine pharmacy.
Reported that glutamine had the effect of the irritability gastric mucosa injury of prevention rat in 68 years, nearest result of study has changed the view of for a long time paddy ammonia amine acyl physiological action importance being underestimated, paddy ammonia amine acyl is main nutrition of digestive system and energy source, glutamine provides energy for gastrointestinal tract mucous epithelial cell, help to keep gastrointestinal organ's metabolism, to protecting and safeguarding that the structure and the function of the organ of digestive system have important effect, paddy ammonia amine acyl is aminoacid, proteinic synthetic provide nitrogenous source and energy; Participate in DNA, RNA precursor--synthesizing of purine and pyrimidine, improve DNA and the protein content and the mucosal thickness of gastrointestinal mucosa, promote the reparation of damage location; For immunocyte division and immunoglobulin,exocrine provide nitrogenous source and energy, raising gastrointestinal tract immunologic function, and be considered to immunomodulator; Can promote cell to upgrade and regeneration, protect the gastrointestinal mucosa barrier, keep the integrity of mucosa form and structure; Participate in the synthetic of the sweet smooth peptide of paddy, resist the biomembranous infringement of radical pair indirectly.Promote brain development in addition, improve intelligence, prevention and treatment carbon tetrachloride, ethanol or cadmium the effect of hepatic injury, the certain effect of performance in acute tissue injury, burn, surgical operation.The glutamy amine be used for separately peptic ulcer and or the NSAID (non-steroidal anti-inflammatory drug) treatment of peptic ulcer effect of bringing out undesirable.
In order to realize purpose of the present invention, one of active ingredient zinc compound is meant in this compositions: the acceptable zinc compounds of pharmacy 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 rafter acid zinc, zinc lysine, Aspartic acid zinc, zinc glycyrrhetate, glycerin zinc, alanylhistidine zinc, acetylamino caproic acid zinc, zinc P-acetlaminoacetate, zinc stearate or zinc propionate.
In order to realize purpose of the present invention, one of active ingredient glutamy amine is meant in this compositions: L-glutaminate, acetylglutamide [N-acetyl-L-glutamine], alanyl glutamine [N-alanyl-L-glutamine], glutathion [γ-L-glutamy-L-cysteinyl-glycine] or alkali metal, alkali salt or zinc compound.
Zinc compound and glutamine based composition have immunoregulation effect, digestive system cytoprotection, replenish a series of physiologically actives such as effect of zinc and/or additional glutamine to body.
The dehydrated alcohol experiment shows: compositions has the digestive system cytoprotection, has prevention or the treatment ethanol detrimental effect to digestive system, the effect of prevention and treatment peptic ulcer, and prevention and treatment ethanol are to the immanoprotection action of the infringement of mucosa.Indomethacin be in the non-steroidal anti-inflammatory medicine to the strongest medicine of mucosal injury effect, indomethacin experiment shows: compositions has the effect that prevention or treatment NSAID (non-steroidal anti-inflammatory drug) are brought out peptic ulcer, and the active ingredient of compositions has collaborative pharmacological action.
The purposes of zinc compound and glutamine based composition is: as the active ingredient of prevention, control or treatment digestive ulcer medicament; Bring out the active ingredient of digestive ulcer medicament as prevention, control or treatment NSAID (non-steroidal anti-inflammatory drug); As the active ingredient of prevention, control or treatment ethanol to digestion system damage medicine; Cause the active ingredient of diseases related medicine as prevention, control or treatment body zinc deficiency and/or lack and cause the active ingredient of diseases related medicine as prevention, control or treatment body glutamine.
Compare with zinc compound or independent use of glutamy amine; at immunoregulation effect; the digestive system cytoprotection; replenish aspects such as zinc and/or additional glutamine effect to body; the pharmacological action of zinc compound and glutamine based composition is more perfect; more comprehensive; more reasonable; the indirect cytoprotection that promptly has zinc ion; the effect that nutrient substance such as ammonia source and energy are provided for gastrointestinal tract of glutamine is also arranged; and participate in biosynthetic direct cytoprotection; compare with single active ingredient; the active ingredient of compositions has collaborative pharmacological action, and compositions has outstanding substantive distinguishing features and significant technological progress.
In order to realize purpose of the present invention, with zinc compound and glutamy amine, 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 glutamine based composition is, zinc compound and glutamy amine do not add or add 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: for 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 rectal suppository, oil [water] dissolubility substrate vaginal suppository, membrane, oil [water] dissolubility ointment, various pharmacy acceptable forms such as plaster.
The main compositions of being made up of zinc compound and glutamy amine also can contain glucose, fructose, galactose, leucine, isoleucine, lysine, methionine, acetylmethionine, phenylalanine, threonine, tryptophan, valine, citrulline, ornithine, acetyl hydroxyproline, proline, glycine, alanine, histidine or N-alanyl-L-histidine or alkali metal, alkali salt or zinc compound, vitamin E, misoprostol, H as active ingredient
2Medicines such as receptor antagonist, proton pump inhibitor, antacid, antipyretic analgesic, NSAID (non-steroidal anti-inflammatory drug) or golden preparation and pharmaceutic adjuvant etc., make per os or non-per os as the compositions that can accept form of medication for the pharmacy such as solid, semisolid and liquid of uses such as oral, intramuscular injection, subcutaneous injection, quiet injection arteries and veins, rectum, vagina and skin, have immunoregulation effect, digestive system cytoprotection, replenish the zinc effect and replenish the glutamine effect, as the active ingredient of prevention, control or treatment digestive ulcer medicament to body to body; Bring out the active ingredient of digestive ulcer medicament as prevention, control or treatment NSAID (non-steroidal anti-inflammatory drug); Prevention, control or treatment ethanol are to the active ingredient of digestion system damage medicine; Cause the active ingredient of diseases related medicine and/or prevention, control or treatment body glutamine to lack as prevention, control or treatment body zinc deficiency and cause the active ingredient of diseases related medicine.
The use amount of this compositions effective ingredient every day is respectively: oral zinc compound is that 1mg～1000mg[is with the zinc cubage] and the glutamy amine be 1mg～90g[with corresponding glutamy amine content: glutamine, acetylglutamide, alanyl glutamine or glutathion are effective dose or total]; Non-per os use zinc compound as 1mg～3000mg[with the zinc cubage] and glutamine as 1mg～90g[with corresponding glutamy amine content: glutamine, acetylglutamide, alanyl glutamine or glutathion are effective dose or total], according to the concrete conditions such as symptom degree of age, body weight, disease type, disease, divide for several times every day and use.
This compositions does not have significant side effects to health, meets social need, can be applied to commercial production.
Below in conjunction with embodiment the pharmacological effect of inventive compositions is further described:
Embodiment 1:
Influence to indomethacin and alcohol-induced gastric mucosa injury:
(Gastroenterology 1979 to press the method for Robert etc.; 77:433), compositions with acetylglutamide (300mg/kg/d) and zinc P-acetlaminoacetate (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, after 1 hour, locate rat, measure the ulcer length that is caused.
(Gastroenterology 1979 to press the method for Robert etc.; 77:433), compositions with acetylglutamide (300mg/kg/d), zinc P-acetlaminoacetate (100mg/kg/d), acetylglutamide (300mgmg/kg/d) and zinc P-acetlaminoacetate (100mg/kg/d) is given rat oral gavage three days, the dehydrated alcohol of stomach 1ml is irritated in administration after 3 hours the last time, after 1 hour, locate rat, measure the ulcer length that is caused.
Table zinc P-acetlaminoacetate and acetylglutamide are to indomethacin and alcohol-induced gastric mucosa
The influence [ulcer length (mm)] of damage
| Dehydrated alcohol | Dehydrated alcohol+indomethacin | ||||
| Blank group | Compositions | Blank group | Zinc P-acetlaminoacetate | Acetylglutamide | Compositions |
| 73.1±17.5 | 16.3±4.4 | 120.9±18.2 | 51.3±14.9 | 39.4±7.9 | 26.7±5.7 |
Claims (1)
1. the pharmacy acceptable composition with anti-digestive system and ulcer effect is characterized in that containing zinc compound and glutamine compounds.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN 97109039 CN1265799C (en) | 1997-03-17 | 1997-03-17 | Composite of zinc containing compound and glutamines |
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN 97109039 CN1265799C (en) | 1997-03-17 | 1997-03-17 | Composite of zinc containing compound and glutamines |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| CN1166320A CN1166320A (en) | 1997-12-03 |
| CN1265799C true CN1265799C (en) | 2006-07-26 |
Family
ID=5170863
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CN 97109039 Expired - Fee Related CN1265799C (en) | 1997-03-17 | 1997-03-17 | Composite of zinc containing compound and glutamines |
Country Status (1)
| Country | Link |
|---|---|
| CN (1) | CN1265799C (en) |
Families Citing this family (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2011051742A1 (en) | 2009-10-28 | 2011-05-05 | Modutech S.A. | Preparation comprising amino acids and plants and its activity in the alcohol detoxification |
| CN102973541A (en) * | 2011-09-02 | 2013-03-20 | 徐州医学院 | Use of L-citrulline in preparation of anti-gastric ulcer drugs |
| CN103750344B (en) * | 2014-01-25 | 2015-11-04 | 北京凯因科技股份有限公司 | A kind of yeast glutathione nutrition preparation |
| KR102094182B1 (en) * | 2018-06-28 | 2020-03-30 | 주식회사 알랙스탠드 | water-soluble polyglutamic acid complex composition containing zinc |
-
1997
- 1997-03-17 CN CN 97109039 patent/CN1265799C/en not_active Expired - Fee Related
Also Published As
| Publication number | Publication date |
|---|---|
| CN1166320A (en) | 1997-12-03 |
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