CN108524453A - A kind of pharmaceutical composition of aspartic acid ornithine - Google Patents
A kind of pharmaceutical composition of aspartic acid ornithine Download PDFInfo
- Publication number
- CN108524453A CN108524453A CN201810741476.9A CN201810741476A CN108524453A CN 108524453 A CN108524453 A CN 108524453A CN 201810741476 A CN201810741476 A CN 201810741476A CN 108524453 A CN108524453 A CN 108524453A
- Authority
- CN
- China
- Prior art keywords
- aspartic acid
- ornithine
- acid ornithine
- pharmaceutical composition
- weight
- Prior art date
- Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
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Classifications
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/14—Particulate form, e.g. powders, Processes for size reducing of pure drugs or the resulting products, Pure drug nanoparticles
- A61K9/141—Intimate drug-carrier mixtures characterised by the carrier, e.g. ordered mixtures, adsorbates, solid solutions, eutectica, co-dried, co-solubilised, co-kneaded, co-milled, co-ground products, co-precipitates, co-evaporates, co-extrudates, co-melts; Drug nanoparticles with adsorbed surface modifiers
- A61K9/146—Intimate drug-carrier mixtures characterised by the carrier, e.g. ordered mixtures, adsorbates, solid solutions, eutectica, co-dried, co-solubilised, co-kneaded, co-milled, co-ground products, co-precipitates, co-evaporates, co-extrudates, co-melts; Drug nanoparticles with adsorbed surface modifiers with organic macromolecular compounds
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/185—Acids; Anhydrides, halides or salts thereof, e.g. sulfur acids, imidic, hydrazonic or hydroximic acids
- A61K31/205—Amine addition salts of organic acids; Inner quaternary ammonium salts, e.g. betaine, carnitine
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
- A61P1/16—Drugs for disorders of the alimentary tract or the digestive system for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
Abstract
The invention discloses a kind of pharmaceutical compositions of aspartic acid ornithine, by preparing aspartic acid ornithine and the polylactide glycolic acid copolymer (PLGA) that suitably matches, 6000 melt blending of polyethylene glycol (PEG), ideal slow release effect can be reached.The pharmaceutical preparation prepared using the pharmaceutical composition of aspartic acid ornithine disclosed in this invention, slow release can only be taken primary, patient compliance height, and can maintain more stable blood concentration daily, Small side effects, and effect is good.And supplementary product consumption is small, and preparation process is simple, is suitble to technology production.
Description
Technical field
The present invention relates to a kind of pharmaceutical compositions of aspartic acid ornithine.
Background technology
Aspartic acid ornithine can provide the substrate of urea and glutamine synthesis, and glutamine is the removing toxic substances product of ammonia,
It is also storage and the types of transportation of ammonia simultaneously；Under physiology and pathological conditions, the synthesis of urea and the synthesis of glutamine can be by
To the influence of ornithine, L-aminobutanedioic acid and other dicarboxylic compounds.Ornithine is almost related to activation and the ammonia of urea cycle
The overall process of removing toxic substances.Arginine is formed in the process, is then divided out urea and is formed ornithine.L-aminobutanedioic acid participates in liver cell
The synthesis of nucleic acid, in favor of repairing impaired liver cell.In addition, since L-aminobutanedioic acid is to tricarboxylic acid cycle generation in liver cell
The indirect facilitation for journey of apologizing for having done sth. wrong, the energy promoted in liver cell generate so that the various functions for the liver cell being damaged obtain
To restore.Aspartic acid ornithine can participate in the metabolism of liver cell, and can activate two key enzymes in liver detoxification function, because
And can assist in and remove harmful free radical, enhance the functions of expelling toxin of liver, reduce rapidly excessively high blood ammonia, promotes liver
The reparation and regeneration of cell itself restore the energy balance of body to effectively improve liver function.
Existing aspartic acid ornithine injection and granule listing at present are clinically applied to control because of acute and chronic hepatopathy
(such as various hepatitis, hepatic sclerosis, fatty liver, posthepatitic syndrome) cause blood ammonia increase and treatment hepatic encephalopathy, such as occur together or
It is damaged the potentiality or hepatic encephalopathy stage of attack of (such as hepatic sclerosis) secondary to liver detoxification function, is particularly suitable for treatment hepatic coma
Early stage or the hepatic coma phase confusional state (injection) and caused by acute and chronic hepatopathy such as hepatic sclerosis, fatty liver, hepatitis
Hyperammonemia is particularly suitable for consciousness imbalance or the neurological complication (granule) for the treatment of early stage.The L-aminobutanedioic acid listed
Ornithine preparation need to be administered repeatedly for one day, and medication is inconvenient.Patent CN103705490A discloses a kind of aspartic acid ornithine
Sustained release preparation is to solve the problems, such as, but its auxiliary material content is high, qf oral administration dosage, that is, larger (particle of aspartic acid ornithine itself
The each 3g of agent), addition auxiliary material is more to be more likely to result in medication difficulty；And blank capsule core is needed to prepare drug containing label, of high cost, work
Skill is complicated.
Invention content
The technical problem to be solved in the present invention is to provide a kind of supplementary product consumption is few, the simple L-aminobutanedioic acid bird ammonia of preparation process
Sour sustained release preparation.
In order to solve the above technical problems, the invention discloses a kind of pharmaceutical compositions of aspartic acid ornithine, by door
1 parts by weight of winter propylhomoserin ornithine, 0.3~0.6 parts by weight of Poly(D,L-lactide-co-glycolide (PLGA), polyethylene glycol (PEG)
60000.1~0.3 parts by weight are prepared by melt-blending process.
It is preferred that by 1 parts by weight of aspartic acid ornithine, 0.5 parts by weight of Poly(D,L-lactide-co-glycolide, polyethylene glycol
60000.15 parts by weight are prepared by melt-blending process.Poly(D,L-lactide-co-glycolide is preferably PLGA75:25.
The pharmaceutical composition of aspartic acid ornithine disclosed in this invention can be made by the steps：1) polylactic acid-
Co-glycolic acid is mixed with Macrogol 6000, is heated to 38~55 DEG C；2) it is evenly dispersed that aspartic acid ornithine is added；
3) 25~30 DEG C are cooled to, is crushed to obtain the final product.
It is preferred that prepared by following steps：1) Poly(D,L-lactide-co-glycolide is mixed with Macrogol 6000, is heated to 43
℃；2) aspartic acid ornithine that micronizing is added is evenly dispersed；3) 26 DEG C are cooled to, 80 mesh is crushed and sieves to obtain the final product.
The pharmaceutical composition of aspartic acid ornithine disclosed in this invention, can the independent or addition filling glue of auxiliary material appropriate
Capsule, tabletting are prepared as dry suspensoid agent.
The pharmaceutical composition of aspartic acid ornithine disclosed in this invention, by by aspartic acid ornithine with suitably match
Prepared by Poly(D,L-lactide-co-glycolide (PLGA), 6000 melt blending of polyethylene glycol (PEG) of ratio, can reach ideal slow
Release effect.The pharmaceutical preparation prepared using the pharmaceutical composition of aspartic acid ornithine disclosed in this invention, slow release can
Daily only to take once, patient compliance is high, and can maintain more stable blood concentration, Small side effects, and effect is good.And auxiliary material
Dosage is small, and preparation process is simple, is suitble to technology production.
Description of the drawings
Fig. 1 is the vitro cumulative releasing curve diagram that embodiment 1 prepares sample；
Fig. 2 is the vitro cumulative releasing curve diagram that embodiment 2 prepares sample；
Fig. 3 is the vitro cumulative releasing curve diagram that embodiment 3 prepares sample；
Fig. 4 is the vitro cumulative releasing curve diagram that embodiment 4 prepares sample；
Fig. 5 is the vitro cumulative releasing curve diagram that embodiment 5 prepares sample；
Fig. 6 is the vitro cumulative releasing curve diagram that embodiment 6 prepares sample.
Specific implementation mode
The above of the present invention is described in further detail again below by way of specific embodiment.But this should not be managed
Solution is limited only to embodiment below for the range of the above-mentioned theme of the present invention.The case where not departing from above-mentioned technological thought of the invention
Under, the various replacements or change made according to ordinary skill knowledge and customary means should all be included in the model of the present invention
In enclosing.
Embodiment 1
Prescription：
| Material forms | Prescription matches (g) |
| Aspartic acid ornithine | 100 |
| PLGA | 30 |
| PEG6000 | 10 |
Preparation method：
1) PLGA is mixed with PEG 6000, is heated to 55 DEG C；2) it is evenly dispersed that aspartic acid ornithine is added；
3) 25 DEG C are cooled to, is crushed to obtain the final product.
Embodiment 2
Prescription：
| Material forms | Prescription matches (g) |
| Aspartic acid ornithine | 100 |
| PLGA65:35 | 60 |
| PEG6000 | 30 |
Preparation method：
1) PLGA is mixed with PEG 6000, is heated to 38 DEG C；2) it is evenly dispersed that aspartic acid ornithine is added；
3) 30 DEG C are cooled to, is crushed to obtain the final product.
Embodiment 3
Prescription：
| Material forms | Prescription matches (g) |
| Aspartic acid ornithine | 100 |
| PLGA50:50 | 50 |
| PEG6000 | 15 |
Preparation method：
1) PLGA is mixed with PEG 6000, is heated to 45 DEG C；2) it is evenly dispersed that aspartic acid ornithine is added；
3) 28 DEG C are cooled to, is crushed to obtain the final product.
Embodiment 4
Prescription：
| Material forms | Prescription matches (g) |
| Aspartic acid ornithine | 100 |
| PLGA75:25 | 55 |
| PEG6000 | 20 |
Preparation method：
1) PLGA is mixed with PEG 6000, is heated to 45 DEG C；2) it is evenly dispersed that aspartic acid ornithine is added；
3) 28 DEG C are cooled to, is crushed to obtain the final product.
Embodiment 5
Prescription：
| Material forms | Prescription matches (g) |
| Aspartic acid ornithine | 100 |
| PLGA65:35 | 50 |
| PEG6000 | 15 |
Preparation method：
1) PLGA is mixed with PEG 6000, is heated to 43 DEG C；
2) it is evenly dispersed that aspartic acid ornithine is added；
3) 26 DEG C are cooled to, is crushed to obtain the final product.
Embodiment 6
Prescription：
| Material forms | Prescription matches (g) |
| Aspartic acid ornithine | 100 |
| PLGA75:25 | 50 |
| PEG6000 | 15 |
Preparation method：
1) PLGA is mixed with PEG 6000, is heated to 43 DEG C；
2) it is evenly dispersed that aspartic acid ornithine is added；
3) 26 DEG C are cooled to, is crushed to obtain the final product.
Test result is as follows for the vitro release of aspartic acid ornithine particle prepared by above example of the present invention：
Test method：Example 1~6 prepares sample (4g in terms of aspartic acid ornithine), according to drug release determination method
(second methods of 2015 editions annex 0913 of Chinese Pharmacopoeia), 0~2h is using 0.1mol/L hydrochloric acid solutions 750ml as solvent, after 2h samplings
37 DEG C of 0.2mol/L sodium radio-phosphate,P-32 solution 250ml are added, 50 revs/min of rotating speed operates, in accordance with the law respectively at 1,2,4,6,8,10,12
Hour sampling, is detected with spectrophotometric external standard method and calculates burst size.As a result it shows that the sample release prepared by embodiment is slow, releases
Medicine curve is steady, and concrete outcome is shown in Table 1 and attached drawing 1~6.
1 Examples 1 to 6 vitro cumulative release of table
Claims (6)
1. a kind of pharmaceutical composition of aspartic acid ornithine, is characterized in that：The composition is by 1 weight of aspartic acid ornithine
Part, 0.3~0.6 parts by weight of Poly(D,L-lactide-co-glycolide, 0.1~0.3 parts by weight of Macrogol 6000 are by melting altogether
It is prepared by mixed method.
2. the pharmaceutical composition of aspartic acid ornithine as described in claim 1, is characterized in that：The composition is by door winter ammonia
1 parts by weight of sour ornithine, 0.5 parts by weight of Poly(D,L-lactide-co-glycolide, 0.15 parts by weight of Macrogol 6000 pass through molten
Melt blending method preparation.
3. the pharmaceutical composition of aspartic acid ornithine as claimed in claim 2, is characterized in that, the polylactic acid-glycolic base second
Acid copolymer is PLGA 75:25.
4. the pharmaceutical composition of aspartic acid ornithine as described in claim 1, is characterized in that, it is made by the steps：
1) Poly(D,L-lactide-co-glycolide is mixed with Macrogol 6000, is heated to 38~55 DEG C；2) aspartic acid ornithine is added
It is evenly dispersed；3) 25~30 DEG C are cooled to, is crushed to obtain the final product.
5. the pharmaceutical composition of aspartic acid ornithine as claimed in claim 4, is characterized in that, it is made by the steps：
1) Poly(D,L-lactide-co-glycolide is mixed with Macrogol 6000, is heated to 43 DEG C；2) the L-aminobutanedioic acid bird of micronizing is added
Propylhomoserin is evenly dispersed；3) 26 DEG C are cooled to, 80 mesh is crushed and sieves to obtain the final product.
6. the pharmaceutical composition of aspartic acid ornithine as described in claim 1, is characterized in that：For filling capsule, tabletting
Or prepare dry suspensoid agent.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN201810741476.9A CN108524453A (en) | 2018-07-05 | 2018-07-05 | A kind of pharmaceutical composition of aspartic acid ornithine |
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN201810741476.9A CN108524453A (en) | 2018-07-05 | 2018-07-05 | A kind of pharmaceutical composition of aspartic acid ornithine |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| CN108524453A true CN108524453A (en) | 2018-09-14 |
Family
ID=63487843
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CN201810741476.9A Pending CN108524453A (en) | 2018-07-05 | 2018-07-05 | A kind of pharmaceutical composition of aspartic acid ornithine |
Country Status (1)
| Country | Link |
|---|---|
| CN (1) | CN108524453A (en) |
Cited By (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US10596136B2 (en) | 2018-06-20 | 2020-03-24 | Axcella Health Inc. | Compositions and methods for the treatment of fat infiltration in muscle |
| US10660870B2 (en) | 2017-08-14 | 2020-05-26 | Axcella Health Inc. | Compositions and methods for the treatment of liver diseases and disorders associated with one or both of hyperammonemia or muscle wasting |
| US11129804B2 (en) | 2016-12-19 | 2021-09-28 | Axcella Health Inc. | Amino acid compositions and methods for the treatment of liver diseases |
Citations (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN103705490A (en) * | 2013-10-31 | 2014-04-09 | 蚌埠丰原医药科技发展有限公司 | Slow-release preparation of ornithine aspartate and preparation process thereof |
| CN106692031A (en) * | 2015-08-21 | 2017-05-24 | 安徽中人科技有限责任公司 | Implant capable of releasing doxorubicin continuously for long term, and preparation method thereof |
-
2018
- 2018-07-05 CN CN201810741476.9A patent/CN108524453A/en active Pending
Patent Citations (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN103705490A (en) * | 2013-10-31 | 2014-04-09 | 蚌埠丰原医药科技发展有限公司 | Slow-release preparation of ornithine aspartate and preparation process thereof |
| CN106692031A (en) * | 2015-08-21 | 2017-05-24 | 安徽中人科技有限责任公司 | Implant capable of releasing doxorubicin continuously for long term, and preparation method thereof |
Cited By (8)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US11129804B2 (en) | 2016-12-19 | 2021-09-28 | Axcella Health Inc. | Amino acid compositions and methods for the treatment of liver diseases |
| US11602511B2 (en) | 2016-12-19 | 2023-03-14 | Axcella Health Inc. | Amino acid compositions and methods for the treatment of liver diseases |
| US10660870B2 (en) | 2017-08-14 | 2020-05-26 | Axcella Health Inc. | Compositions and methods for the treatment of liver diseases and disorders associated with one or both of hyperammonemia or muscle wasting |
| US10682325B2 (en) | 2017-08-14 | 2020-06-16 | Axcella Health Inc. | Compositions and methods for the treatment of liver diseases and disorders associated with one or both of hyperammonemia or muscle wasting |
| US11571404B2 (en) | 2017-08-14 | 2023-02-07 | Axcella Health Inc. | Compositions and methods for the treatment of liver diseases and disorders associated with one or both of hyperammonemia or muscle wasting |
| US10596136B2 (en) | 2018-06-20 | 2020-03-24 | Axcella Health Inc. | Compositions and methods for the treatment of fat infiltration in muscle |
| US10973793B2 (en) | 2018-06-20 | 2021-04-13 | Axcella Health Inc. | Compositions and methods for the treatment of fat infiltration in muscle |
| US11833127B2 (en) | 2018-06-20 | 2023-12-05 | Axcella Health Inc. | Compositions and methods for the treatment of fat infiltration in muscle |
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| RJ01 | Rejection of invention patent application after publication |
Application publication date: 20180914 |
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| RJ01 | Rejection of invention patent application after publication |