CN1125574A - Enteric-soluble glutamine - Google Patents
Enteric-soluble glutamine Download PDFInfo
- Publication number
- CN1125574A CN1125574A CN 95113086 CN95113086A CN1125574A CN 1125574 A CN1125574 A CN 1125574A CN 95113086 CN95113086 CN 95113086 CN 95113086 A CN95113086 A CN 95113086A CN 1125574 A CN1125574 A CN 1125574A
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- glutamine
- enteric
- soluble
- arginine
- intestinal
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Abstract
The enteric coated glutamine features that an enteric coating is applied to the medicine that uses glutamine as main raw material and arginine or soluble cellulose as auxiliary one in order to ensure that it is not disaggregated in gastric acid, but in intestinal juice to play its role and by-pass its toxic by-effect.
Description
The present invention relates to a kind of enteric-soluble glutamine that glutamine is not destroyed in sour environment.
Glutamine (Gln) is the indispensable aminoacid of body, be the vehicle that nitrogen is transported in various tissues, the necessary important source of synthetic nucleosides acid precursors stomach function regulating intestinal cell metabolism, particularly under stress situation, Gln almost becomes unique source of gastrointestinal mucosa metabolism institute energy requirement, severe trauma (is infected, burn, tumor, postoperative etc.), hungry (iatrogenic fasting etc.) and accept the TPN support for a long time or other catabolism disease patients have important clinical significance (mainly to keep the intestinal epithelial cell function, improve its barrier function and immunologic function etc.), be one of the most effective medicine of treatment intestinal tract disease.Yet the metabolic characteristic of glutamine has also become its shortcoming, promptly very unstable in aqueous solution and sour environment (as gastric juice), easily decompose and produce ammonia and pyroglutamic acid, have nerve toxicity and ammonia toxicity thereby can not make intravenous transfusion preparation and conventional oral formulations, limited the effect of glutamine.
" Chinese practical surgical magazine " nineteen ninety-five (the 15th volume) the 6th phase P323 clinical nutrition (surgery nutrition) general situation of development " (Jiang Zhuming work) described:
Glutamine: ... because the aqueous solution instability of glutamine, commodity aminoacid mixing liquid does not all contain glutamine at present.
Import simple nutrient substance from vein, develop into parenteral, very long exploration has been experienced in interior nutrition, is just to have reached preliminary maturation over nearly more than 20 years.
And for example: " Chinese Medical Journal " 1993 the 73rd volumes the 4th phase P249 " metabolism of glu famine and the application in surgery thereof " (Jiang Luo Fuwen Zhu Ming work) refers to:
The glutamine dissolubility is very low, and is unstable in aqueous solution, but cyclisation generates pyroglutamic acid and toxic product ammonia, because these shortcomings, glutamine is considered to non essential amino acid for a long time in addition, does not therefore all contain glutamine in the commodity aminoacid now.
In order to address this problem, domestic and international research all aims on the chemical compound of chemosynthesis Gln, as national chemosynthesis such as Japan, Switzerland in aqueous solution more stable " two peptide acetylglutamide ".Because this synthetics current production rate is low, cost an arm and a leg, toxic and side effects is big, therefore is not used for clinical yet.
The objective of the invention is to develop a kind of oral glutamine, can guarantee glutamine not disintegrate in gastric juice, but behind the intestinal that arrives safe and sound, disintegrate plays a role in intestinal juice.
The present invention studies successful enteric-soluble glutamine, it is chemical property according to glutamine, at glutamine is medicine appearance parcel one deck enterosoluble substance of primary raw material, look the dosage form difference, wrap up enteric coated capsule respectively, enteric coating or enteric microencapsulation, to guarantee glutamine not disintegrate in gastric acid, the ability disintegrate plays a role in intestinal juice after being directed into intestinal.
The present invention studies successful enteric-soluble glutamine, is to be primary raw material with the glutamine, is pharmaceutical presentations parcel one deck enteric integument of adjuvant with arginine or soluble fiber.This enteric integument is looked the dosage form difference, is respectively enteric coated capsule, or enteric coating, or the enteric microencapsulation, and to guarantee glutamine not disintegrate in gastric acid, after being directed into intestinal, just disintegrate plays a role in intestinal juice.
What wrapped up by the enteric integument is the medicine of primary raw material with the glutamine, and its component and percentage by weight are:
Glutamine 60～90%
Arginine or soluble cellulose 10～40%
Described enteric integument, it is enteric coated capsule, enteric coating and enteric coated capsule, respectively by being primary raw material with the hydroxy alkyl cellulose phthalate ester, add plasticizer, surfactant and pigment, or hydroxypropyl cellulose, polyvinyl ester acid esters, cellulose acetate, phthalic acid ester, plasticizer and antioxidant or make by cellulose acetate-phthalate and acetone material.
The enteric-soluble glutamine slaking test that the present invention relates to is as follows:
Disintegration result of the test
| The result of the test lot number | The investigation time | |||
| Zero month (1994.3) | January (1994.4) | February (1994.5) | March (1994.6) | |
| ????940322 ????940324 ????940326 | In hydrochloric acid solution (9 → 9000), do not see disintegrate in 2 hours, change in the simulated intestinal fluid and be whole disintegrates after 10 minutes and pass through screen cloth | With a left side | With a left side | With a left side |
(employing Chinese Pharmacopoeia) 90 years version appendix enteric coated capsulees disintegration time mensuration method is measured)
The result: three batch samples crack or disintegration phenomenon did not all occur in two hours in simulated gastric fluid, in simulated intestinal fluid in 15 clocks all disintegrate pass through screen cloth.
Presentation of results: the built-in glutamine of enteric coated capsule can not be exposed to sour environment, thereby can not cause the destruction of glutamine, and on the contrary, disintegrate disengages glutamine in intestinal, directly acts on intestinal cell.
The present invention take this not only simply but also design cleverly, both solved glutamine problem of unstable in aqueous solution and acidic gastric juice, solved the two problems that the peptide acetylglutamide costs an arm and a leg, toxic and side effects is big of chemosynthesis again, for give full play to glutamine clinically important function and the glutamine oral medicine of production stable curative effect opened up a practicable approach.
Provide embodiment below:
Example 1:
Make the enteric-soluble glutamine capsule:
To contain glutamine 75%, the medicated powder of the arginase 12 5% enteric hard capsule of packing into promptly is formed in the glutamine enteric coated capsule of disintegrate in the gastric acid environment.
Example 2:
Make the enteric-soluble glutamine tablet
To contain glutamine 80%, the medicated powder of soluble cellulose 20% breaks into all size or shaped tablets, again at its outer surface parcel one deck enteric coating, promptly is formed in the glutamine enteric coated tablet of not disintegrate in the sour environment.
Example 3:
Make the enteric-soluble glutamine microcapsule:
To contain glutamine 90%, the medicated powder granule appearance parcel enteric microencapsulation of arginine 10% promptly makes glutamine enteric microencapsulation.
Example 4:
Make enteric-soluble glutamine compound adhesive wafer:
To contain glutamine 85%, the medicated powder granule outer surface of soluble cellulose 15% is the parcel microencapsulation earlier, wraps up one deck enteric hard capsule again, promptly makes glutamine enteric compound adhesive wafer.
Claims (3)
1, enteric-soluble glutamine is characterized in that being primary raw material with the glutamine, is that the medicine appearance of auxiliary material has been wrapped up one deck enteric integument with arginine or soluble cellulose.
2, enteric-soluble glutamine according to claim 1 is characterized in that the percentage by weight of glutamine and arginine or soluble cellulose is:
Glutamine 60～90%
Arginine or soluble cellulose 10～40%
3, enteric-soluble glutamine according to claim 2 is characterized in that described enteric integument is respectively the enteric hard capsule, or enteric coating, or the enteric microencapsulation, or the enteric complex capsule.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN 95113086 CN1125574A (en) | 1995-11-10 | 1995-11-10 | Enteric-soluble glutamine |
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN 95113086 CN1125574A (en) | 1995-11-10 | 1995-11-10 | Enteric-soluble glutamine |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| CN1125574A true CN1125574A (en) | 1996-07-03 |
Family
ID=5079870
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CN 95113086 Pending CN1125574A (en) | 1995-11-10 | 1995-11-10 | Enteric-soluble glutamine |
Country Status (1)
| Country | Link |
|---|---|
| CN (1) | CN1125574A (en) |
Cited By (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN102946885A (en) * | 2010-04-20 | 2013-02-27 | 埃尔舍利克斯治疗公司 | Chemosensory receptor ligand-based therapies |
| US8828953B2 (en) | 2009-04-20 | 2014-09-09 | NaZura BioHealth, Inc. | Chemosensory receptor ligand-based therapies |
| US9486463B2 (en) | 2010-10-19 | 2016-11-08 | Ambra Bioscience Llc | Chemosensory receptor ligand-based therapies |
| CN111903855A (en) * | 2020-07-23 | 2020-11-10 | 廊坊梅花生物技术开发有限公司 | Composition for livestock feed and application thereof |
-
1995
- 1995-11-10 CN CN 95113086 patent/CN1125574A/en active Pending
Cited By (10)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US8828953B2 (en) | 2009-04-20 | 2014-09-09 | NaZura BioHealth, Inc. | Chemosensory receptor ligand-based therapies |
| US9901551B2 (en) | 2009-04-20 | 2018-02-27 | Ambra Bioscience Llc | Chemosensory receptor ligand-based therapies |
| CN102946885A (en) * | 2010-04-20 | 2013-02-27 | 埃尔舍利克斯治疗公司 | Chemosensory receptor ligand-based therapies |
| EP2560660A1 (en) * | 2010-04-20 | 2013-02-27 | Elcelyx Therapeutics, Inc | Chemosensory receptor ligand-based therapies |
| EP2560660A4 (en) * | 2010-04-20 | 2013-11-20 | Elcelyx Therapeutics Inc | Chemosensory receptor ligand-based therapies |
| CN102946885B (en) * | 2010-04-20 | 2016-06-22 | 埃尔舍利克斯治疗公司 | The treatment of chemically based sensing receptors ligand |
| CN106039313A (en) * | 2010-04-20 | 2016-10-26 | 埃尔舍利克斯治疗公司 | Chemosensory receptor ligand-based therapies |
| US9486463B2 (en) | 2010-10-19 | 2016-11-08 | Ambra Bioscience Llc | Chemosensory receptor ligand-based therapies |
| CN111903855A (en) * | 2020-07-23 | 2020-11-10 | 廊坊梅花生物技术开发有限公司 | Composition for livestock feed and application thereof |
| CN111903855B (en) * | 2020-07-23 | 2023-03-31 | 廊坊梅花生物技术开发有限公司 | Composition for livestock feed and application thereof |
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| SE01 | Entry into force of request for substantive examination | ||
| C06 | Publication | ||
| PB01 | Publication | ||
| C01 | Deemed withdrawal of patent application (patent law 1993) | ||
| WD01 | Invention patent application deemed withdrawn after publication |