CN1399549A - 超细l-肉碱、其制备方法、含有它的组合物及其使用方法 - Google Patents
超细l-肉碱、其制备方法、含有它的组合物及其使用方法 Download PDFInfo
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- CN1399549A CN1399549A CN00812109A CN00812109A CN1399549A CN 1399549 A CN1399549 A CN 1399549A CN 00812109 A CN00812109 A CN 00812109A CN 00812109 A CN00812109 A CN 00812109A CN 1399549 A CN1399549 A CN 1399549A
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- Prior art keywords
- carnitine
- alkanoyl
- acid
- tartrate
- fumarate
- 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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Links
- 238000000034 method Methods 0.000 title claims description 24
- 239000000203 mixture Substances 0.000 title claims description 21
- 229960004203 carnitine Drugs 0.000 title description 3
- PHIQHXFUZVPYII-ZCFIWIBFSA-N (R)-carnitine Chemical compound C[N+](C)(C)C[C@H](O)CC([O-])=O PHIQHXFUZVPYII-ZCFIWIBFSA-N 0.000 claims abstract description 192
- 239000002253 acid Substances 0.000 claims description 68
- HNSUOMBUJRUZHJ-REVJHSINSA-N [(2r)-3-carboxy-2-hydroxypropyl]-trimethylazanium;(z)-4-hydroxy-4-oxobut-2-enoate Chemical compound OC(=O)\C=C/C(O)=O.C[N+](C)(C)C[C@H](O)CC([O-])=O HNSUOMBUJRUZHJ-REVJHSINSA-N 0.000 claims description 25
- -1 alkanoyl L-carnitine Chemical compound 0.000 claims description 25
- VOTPLFCPIRIALF-UHFFFAOYSA-N 3-(2,4-dioxo-1h-pyrimidine-6-carbonyl)oxy-4-(trimethylazaniumyl)butanoate Chemical compound C[N+](C)(C)CC(CC([O-])=O)OC(=O)C1=CC(=O)NC(=O)N1 VOTPLFCPIRIALF-UHFFFAOYSA-N 0.000 claims description 20
- CKLJMWTZIZZHCS-REOHCLBHSA-N L-aspartic acid Chemical compound OC(=O)[C@@H](N)CC(O)=O CKLJMWTZIZZHCS-REOHCLBHSA-N 0.000 claims description 20
- HTLKVLPYYQCQCA-ZCFIWIBFSA-N S(=O)(=O)(O)O[C@@H](C[N+](C)(C)C)CC([O-])=O Chemical compound S(=O)(=O)(O)O[C@@H](C[N+](C)(C)C)CC([O-])=O HTLKVLPYYQCQCA-ZCFIWIBFSA-N 0.000 claims description 20
- 229940009098 aspartate Drugs 0.000 claims description 20
- 229950005627 embonate Drugs 0.000 claims description 20
- 150000003839 salts Chemical class 0.000 claims description 19
- VZCYOOQTPOCHFL-UHFFFAOYSA-N trans-butenedioic acid Natural products OC(=O)C=CC(O)=O VZCYOOQTPOCHFL-UHFFFAOYSA-N 0.000 claims description 17
- RZALONVQKUWRRY-FYZOBXCZSA-N 2,3-dihydroxybutanedioic acid;(3r)-3-hydroxy-4-(trimethylazaniumyl)butanoate Chemical compound OC(=O)C(O)C(O)C(O)=O.C[N+](C)(C)C[C@H](O)CC([O-])=O RZALONVQKUWRRY-FYZOBXCZSA-N 0.000 claims description 11
- RZALONVQKUWRRY-XOJLQXRJSA-N (2r,3r)-2,3-dihydroxybutanedioate;hydron;(3r)-3-hydroxy-4-(trimethylazaniumyl)butanoate Chemical compound OC(=O)[C@H](O)[C@@H](O)C(O)=O.C[N+](C)(C)C[C@H](O)CC([O-])=O RZALONVQKUWRRY-XOJLQXRJSA-N 0.000 claims description 10
- JXXCENBLGFBQJM-UHFFFAOYSA-N (3-carboxy-2-hydroxypropyl)-trimethylazanium;chloride Chemical compound [Cl-].C[N+](C)(C)CC(O)CC(O)=O JXXCENBLGFBQJM-UHFFFAOYSA-N 0.000 claims description 10
- MUXKDGQFSLPPKJ-ZCFIWIBFSA-N (3r)-3-(2,2,2-trichloroacetyl)oxy-4-(trimethylazaniumyl)butanoate Chemical compound C[N+](C)(C)C[C@@H](CC([O-])=O)OC(=O)C(Cl)(Cl)Cl MUXKDGQFSLPPKJ-ZCFIWIBFSA-N 0.000 claims description 10
- ZXMGVWQWKVBCCN-BRFYHDHCSA-N (3r)-3-(2-hydroxypropanoyloxy)-4-(trimethylazaniumyl)butanoate Chemical compound CC(O)C(=O)O[C@H](CC([O-])=O)C[N+](C)(C)C ZXMGVWQWKVBCCN-BRFYHDHCSA-N 0.000 claims description 10
- NYEBOVKDJRAMOF-FYZOBXCZSA-N (3r)-3-hydroxy-4-(trimethylazaniumyl)butanoate;2,2,2-trifluoroacetic acid Chemical compound OC(=O)C(F)(F)F.C[N+](C)(C)C[C@H](O)CC([O-])=O NYEBOVKDJRAMOF-FYZOBXCZSA-N 0.000 claims description 10
- SVVSJSVMXCEDDA-FYZOBXCZSA-N (3r)-3-hydroxy-4-(trimethylazaniumyl)butanoate;oxalic acid Chemical class OC(=O)C(O)=O.C[N+](C)(C)C[C@H](O)CC([O-])=O SVVSJSVMXCEDDA-FYZOBXCZSA-N 0.000 claims description 10
- OXLHQQYLBMZDMF-ZCFIWIBFSA-N (3r)-3-iodyloxy-4-(trimethylazaniumyl)butanoate Chemical compound C[N+](C)(C)C[C@@H](CC([O-])=O)OI(=O)=O OXLHQQYLBMZDMF-ZCFIWIBFSA-N 0.000 claims description 10
- LYVAHVJXBSPAKI-SSDOTTSWSA-N (3r)-3-methylsulfonyloxy-4-(trimethylazaniumyl)butanoate Chemical compound C[N+](C)(C)C[C@@H](CC([O-])=O)OS(C)(=O)=O LYVAHVJXBSPAKI-SSDOTTSWSA-N 0.000 claims description 10
- DEVLFMFUNRCKGE-FYZOBXCZSA-N 2-hydroxypropane-1,2,3-tricarboxylic acid;(3r)-3-hydroxy-4-(trimethylazaniumyl)butanoate Chemical compound C[N+](C)(C)C[C@H](O)CC([O-])=O.OC(=O)CC(O)(C(O)=O)CC(O)=O DEVLFMFUNRCKGE-FYZOBXCZSA-N 0.000 claims description 10
- KRKNYBCHXYNGOX-UHFFFAOYSA-K Citrate Chemical compound [O-]C(=O)CC(O)(CC([O-])=O)C([O-])=O KRKNYBCHXYNGOX-UHFFFAOYSA-K 0.000 claims description 10
- MUBZPKHOEPUJKR-UHFFFAOYSA-N Oxalic acid Chemical compound OC(=O)C(O)=O MUBZPKHOEPUJKR-UHFFFAOYSA-N 0.000 claims description 10
- 229910019142 PO4 Inorganic materials 0.000 claims description 10
- AWUCVROLDVIAJX-UHFFFAOYSA-N alpha-glycerophosphate Natural products OCC(O)COP(O)(O)=O AWUCVROLDVIAJX-UHFFFAOYSA-N 0.000 claims description 10
- 239000008187 granular material Substances 0.000 claims description 10
- VZCYOOQTPOCHFL-UPHRSURJSA-N maleic acid Chemical compound OC(=O)\C=C/C(O)=O VZCYOOQTPOCHFL-UPHRSURJSA-N 0.000 claims description 10
- NBIIXXVUZAFLBC-UHFFFAOYSA-K phosphate Chemical compound [O-]P([O-])([O-])=O NBIIXXVUZAFLBC-UHFFFAOYSA-K 0.000 claims description 10
- 239000010452 phosphate Substances 0.000 claims description 10
- AWUCVROLDVIAJX-GSVOUGTGSA-N sn-glycerol 3-phosphate Chemical compound OC[C@@H](O)COP(O)(O)=O AWUCVROLDVIAJX-GSVOUGTGSA-N 0.000 claims description 10
- VZCYOOQTPOCHFL-OWOJBTEDSA-N Fumaric acid Chemical compound OC(=O)\C=C\C(O)=O VZCYOOQTPOCHFL-OWOJBTEDSA-N 0.000 claims description 8
- ACTIUHUUMQJHFO-UHFFFAOYSA-N Coenzym Q10 Natural products COC1=C(OC)C(=O)C(CC=C(C)CCC=C(C)CCC=C(C)CCC=C(C)CCC=C(C)CCC=C(C)CCC=C(C)CCC=C(C)CCC=C(C)CCC=C(C)C)=C(C)C1=O ACTIUHUUMQJHFO-UHFFFAOYSA-N 0.000 claims description 4
- 235000017471 coenzyme Q10 Nutrition 0.000 claims description 4
- ACTIUHUUMQJHFO-UPTCCGCDSA-N coenzyme Q10 Chemical compound COC1=C(OC)C(=O)C(C\C=C(/C)CC\C=C(/C)CC\C=C(/C)CC\C=C(/C)CC\C=C(/C)CC\C=C(/C)CC\C=C(/C)CC\C=C(/C)CC\C=C(/C)CCC=C(C)C)=C(C)C1=O ACTIUHUUMQJHFO-UPTCCGCDSA-N 0.000 claims description 4
- 229940110767 coenzyme Q10 Drugs 0.000 claims description 4
- 239000000546 pharmaceutical excipient Substances 0.000 claims description 4
- 238000012216 screening Methods 0.000 claims description 4
- 229940046374 chromium picolinate Drugs 0.000 claims description 3
- GJYSUGXFENSLOO-UHFFFAOYSA-N chromium;pyridine-2-carboxylic acid Chemical compound [Cr].OC(=O)C1=CC=CC=N1.OC(=O)C1=CC=CC=N1.OC(=O)C1=CC=CC=N1 GJYSUGXFENSLOO-UHFFFAOYSA-N 0.000 claims description 3
- 229940088594 vitamin Drugs 0.000 claims description 3
- 229930003231 vitamin Natural products 0.000 claims description 3
- 235000013343 vitamin Nutrition 0.000 claims description 3
- 239000011782 vitamin Substances 0.000 claims description 3
- 150000003722 vitamin derivatives Chemical class 0.000 claims description 3
- ZMJBYMUCKBYSCP-UHFFFAOYSA-N Hydroxycitric acid Chemical compound OC(=O)C(O)C(O)(C(O)=O)CC(O)=O ZMJBYMUCKBYSCP-UHFFFAOYSA-N 0.000 claims description 2
- QNVSXXGDAPORNA-UHFFFAOYSA-N Resveratrol Natural products OC1=CC=CC(C=CC=2C=C(O)C(O)=CC=2)=C1 QNVSXXGDAPORNA-UHFFFAOYSA-N 0.000 claims description 2
- LUKBXSAWLPMMSZ-OWOJBTEDSA-N Trans-resveratrol Chemical compound C1=CC(O)=CC=C1\C=C\C1=CC(O)=CC(O)=C1 LUKBXSAWLPMMSZ-OWOJBTEDSA-N 0.000 claims description 2
- 239000003963 antioxidant agent Substances 0.000 claims description 2
- 230000003078 antioxidant effect Effects 0.000 claims description 2
- 235000006708 antioxidants Nutrition 0.000 claims description 2
- VZCCETWTMQHEPK-UHFFFAOYSA-N gamma-Linolensaeure Natural products CCCCCC=CCC=CCC=CCCCCC(O)=O VZCCETWTMQHEPK-UHFFFAOYSA-N 0.000 claims description 2
- VZCCETWTMQHEPK-QNEBEIHSSA-N gamma-linolenic acid Chemical compound CCCCC\C=C/C\C=C/C\C=C/CCCCC(O)=O VZCCETWTMQHEPK-QNEBEIHSSA-N 0.000 claims description 2
- 235000020664 gamma-linolenic acid Nutrition 0.000 claims description 2
- 229960002733 gamolenic acid Drugs 0.000 claims description 2
- 229940089491 hydroxycitric acid Drugs 0.000 claims description 2
- 235000021283 resveratrol Nutrition 0.000 claims description 2
- 229940016667 resveratrol Drugs 0.000 claims description 2
- 239000000463 material Substances 0.000 abstract description 6
- 230000003247 decreasing effect Effects 0.000 abstract 1
- 239000002245 particle Substances 0.000 abstract 1
- 229960001518 levocarnitine Drugs 0.000 description 22
- 150000002148 esters Chemical class 0.000 description 21
- 238000002360 preparation method Methods 0.000 description 13
- 239000003921 oil Substances 0.000 description 12
- 235000019198 oils Nutrition 0.000 description 12
- VYPSYNLAJGMNEJ-UHFFFAOYSA-N Silicium dioxide Chemical compound O=[Si]=O VYPSYNLAJGMNEJ-UHFFFAOYSA-N 0.000 description 10
- 239000002994 raw material Substances 0.000 description 8
- 230000000694 effects Effects 0.000 description 5
- 239000000047 product Substances 0.000 description 5
- 239000000377 silicon dioxide Substances 0.000 description 5
- FEWJPZIEWOKRBE-JCYAYHJZSA-N Dextrotartaric acid Chemical compound OC(=O)[C@H](O)[C@@H](O)C(O)=O FEWJPZIEWOKRBE-JCYAYHJZSA-N 0.000 description 4
- 239000002131 composite material Substances 0.000 description 4
- 238000005516 engineering process Methods 0.000 description 4
- 238000002156 mixing Methods 0.000 description 4
- 235000012239 silicon dioxide Nutrition 0.000 description 4
- 239000000126 substance Substances 0.000 description 4
- 229940095064 tartrate Drugs 0.000 description 4
- 150000001875 compounds Chemical class 0.000 description 3
- 235000015872 dietary supplement Nutrition 0.000 description 3
- 239000003937 drug carrier Substances 0.000 description 3
- 239000010419 fine particle Substances 0.000 description 3
- 235000013305 food Nutrition 0.000 description 3
- 235000016709 nutrition Nutrition 0.000 description 3
- 230000035764 nutrition Effects 0.000 description 3
- 230000009467 reduction Effects 0.000 description 3
- GVJHHUAWPYXKBD-UHFFFAOYSA-N (±)-α-Tocopherol Chemical compound OC1=C(C)C(C)=C2OC(CCCC(C)CCCC(C)CCCC(C)C)(C)CCC2=C1C GVJHHUAWPYXKBD-UHFFFAOYSA-N 0.000 description 2
- 241000196324 Embryophyta Species 0.000 description 2
- 239000001828 Gelatine Substances 0.000 description 2
- 239000007864 aqueous solution Substances 0.000 description 2
- 239000002775 capsule Substances 0.000 description 2
- 239000003795 chemical substances by application Substances 0.000 description 2
- 239000002270 dispersing agent Substances 0.000 description 2
- 229910021485 fumed silica Inorganic materials 0.000 description 2
- 229920000159 gelatin Polymers 0.000 description 2
- 235000019322 gelatine Nutrition 0.000 description 2
- 230000002209 hydrophobic effect Effects 0.000 description 2
- 239000004615 ingredient Substances 0.000 description 2
- 235000015097 nutrients Nutrition 0.000 description 2
- 239000012925 reference material Substances 0.000 description 2
- 239000007787 solid Substances 0.000 description 2
- 239000000243 solution Substances 0.000 description 2
- 235000011496 sports drink Nutrition 0.000 description 2
- 238000003860 storage Methods 0.000 description 2
- XLYOFNOQVPJJNP-UHFFFAOYSA-N water Substances O XLYOFNOQVPJJNP-UHFFFAOYSA-N 0.000 description 2
- OKTJSMMVPCPJKN-UHFFFAOYSA-N Carbon Chemical compound [C] OKTJSMMVPCPJKN-UHFFFAOYSA-N 0.000 description 1
- 208000024172 Cardiovascular disease Diseases 0.000 description 1
- FEWJPZIEWOKRBE-UHFFFAOYSA-N Tartaric Acid Chemical class [H+].[H+].[O-]C(=O)C(O)C(O)C([O-])=O FEWJPZIEWOKRBE-UHFFFAOYSA-N 0.000 description 1
- 229930003427 Vitamin E Natural products 0.000 description 1
- 238000010521 absorption reaction Methods 0.000 description 1
- 125000002777 acetyl group Chemical group [H]C([H])([H])C(*)=O 0.000 description 1
- 230000002730 additional effect Effects 0.000 description 1
- 235000019728 animal nutrition Nutrition 0.000 description 1
- 235000004251 balanced diet Nutrition 0.000 description 1
- 230000008901 benefit Effects 0.000 description 1
- 230000037396 body weight Effects 0.000 description 1
- 230000008859 change Effects 0.000 description 1
- 239000011248 coating agent Substances 0.000 description 1
- 238000000576 coating method Methods 0.000 description 1
- 239000013078 crystal Substances 0.000 description 1
- 230000007423 decrease Effects 0.000 description 1
- 229940079593 drug Drugs 0.000 description 1
- 239000003814 drug Substances 0.000 description 1
- 235000019197 fats Nutrition 0.000 description 1
- 239000001530 fumaric acid Substances 0.000 description 1
- WIGCFUFOHFEKBI-UHFFFAOYSA-N gamma-tocopherol Natural products CC(C)CCCC(C)CCCC(C)CCCC1CCC2C(C)C(O)C(C)C(C)C2O1 WIGCFUFOHFEKBI-UHFFFAOYSA-N 0.000 description 1
- 238000000227 grinding Methods 0.000 description 1
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- 210000003470 mitochondria Anatomy 0.000 description 1
- 230000004048 modification Effects 0.000 description 1
- 238000012986 modification Methods 0.000 description 1
- 239000004006 olive oil Substances 0.000 description 1
- 235000008390 olive oil Nutrition 0.000 description 1
- 230000008520 organization Effects 0.000 description 1
- 239000006187 pill Substances 0.000 description 1
- 239000000843 powder Substances 0.000 description 1
- 230000002265 prevention Effects 0.000 description 1
- 230000008569 process Effects 0.000 description 1
- 230000001737 promoting effect Effects 0.000 description 1
- 238000010298 pulverizing process Methods 0.000 description 1
- 238000012958 reprocessing Methods 0.000 description 1
- 210000000582 semen Anatomy 0.000 description 1
- 239000003549 soybean oil Substances 0.000 description 1
- 235000012424 soybean oil Nutrition 0.000 description 1
- 239000003826 tablet Substances 0.000 description 1
- 230000001988 toxicity Effects 0.000 description 1
- 231100000419 toxicity Toxicity 0.000 description 1
- 125000003774 valeryl group Chemical group O=C([*])C([H])([H])C([H])([H])C([H])([H])C([H])([H])[H] 0.000 description 1
- 235000013311 vegetables Nutrition 0.000 description 1
- 235000003563 vegetarian diet Nutrition 0.000 description 1
- 235000019165 vitamin E Nutrition 0.000 description 1
- 229940046009 vitamin E Drugs 0.000 description 1
- 239000011709 vitamin E Substances 0.000 description 1
Classifications
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- 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
- A23—FOODS OR FOODSTUFFS; TREATMENT THEREOF, NOT COVERED BY OTHER CLASSES
- A23L—FOODS, FOODSTUFFS, OR NON-ALCOHOLIC BEVERAGES, NOT COVERED BY SUBCLASSES A21D OR A23B-A23J; THEIR PREPARATION OR TREATMENT, e.g. COOKING, MODIFICATION OF NUTRITIVE QUALITIES, PHYSICAL TREATMENT; PRESERVATION OF FOODS OR FOODSTUFFS, IN GENERAL
- A23L33/00—Modifying nutritive qualities of foods; Dietetic products; Preparation or treatment thereof
- A23L33/10—Modifying nutritive qualities of foods; Dietetic products; Preparation or treatment thereof using additives
- A23L33/17—Amino acids, peptides or proteins
- A23L33/175—Amino acids
-
- 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
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P3/00—Drugs for disorders of the metabolism
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P3/00—Drugs for disorders of the metabolism
- A61P3/04—Anorexiants; Antiobesity agents
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P3/00—Drugs for disorders of the metabolism
- A61P3/06—Antihyperlipidemics
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P9/00—Drugs for disorders of the cardiovascular system
-
- A—HUMAN NECESSITIES
- A23—FOODS OR FOODSTUFFS; TREATMENT THEREOF, NOT COVERED BY OTHER CLASSES
- A23V—INDEXING SCHEME RELATING TO FOODS, FOODSTUFFS OR NON-ALCOHOLIC BEVERAGES AND LACTIC OR PROPIONIC ACID BACTERIA USED IN FOODSTUFFS OR FOOD PREPARATION
- A23V2002/00—Food compositions, function of food ingredients or processes for food or foodstuffs
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- Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- General Health & Medical Sciences (AREA)
- Medicinal Chemistry (AREA)
- Animal Behavior & Ethology (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Epidemiology (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Organic Chemistry (AREA)
- Obesity (AREA)
- Hematology (AREA)
- Diabetes (AREA)
- Food Science & Technology (AREA)
- Polymers & Plastics (AREA)
- Proteomics, Peptides & Aminoacids (AREA)
- Mycology (AREA)
- Nutrition Science (AREA)
- Cardiology (AREA)
- Child & Adolescent Psychology (AREA)
- Heart & Thoracic Surgery (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
- Medicinal Preparation (AREA)
- Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Coloring Foods And Improving Nutritive Qualities (AREA)
- Cosmetics (AREA)
Abstract
一种L-肉碱。其具有的颗粒大小使其基本上能通过100 USBS目筛,其有提高的生物利用度、降低的吸湿性、也可以方便地与油性基材料制成制剂。
Description
本申请要求1999年9月3日提交的美国临时申请60/152,240及1999年10月8日提交的美国临时申请60/158,245的优先权。
发明背景
发明领域
本发明涉及一种超细的L-肉碱及其盐类。具体的,本发明涉及以超细颗粒形式存在的L-肉碱及其盐类。该超细L-肉碱能够与其他原料的细微颗粒均匀混合而保持其本身离散的形态。该超细L-肉碱的整体细度使它可与油基原料理想地混合,而油基原料原本是不易与常规尺寸的肉碱完全混合的。由于其细微原料总表面积的增加,本发明超细L-肉碱的整体细度也促进其在肠内的快速吸收。本发明还涉及制备这种超细L-肉碱及其盐类的方法。本发明进一步涉及含此种超细L-肉碱及其盐类的组合物。此外,本发明还涉及此种超细L-肉碱及其盐类的使用方法。
背景说明
众所周知,L-肉碱有很多用途。具体地说,L-肉碱的口服给药显示出对治疗心血管疾病的积极的疗效。L-肉碱及其盐还作为食物增补剂使用,尤其用于促进脂肪的代谢。
但是,人们希望提高L-肉碱及其公知的盐的生物利用度。同样人们希望制备含有L-肉碱及一种或多种不与大尺寸L-肉碱混合的其他组分诸如油基原料的组合物。进一步的,人们还希望降低L-肉碱的吸湿性。
因此,人们仍然需要口服给药时生物利用度提高的L-肉碱及其盐的形式。同样人们仍需要这样形式的L-肉碱及其盐类:它们可与不与大尺寸L-肉碱混合的其他组分如油基原料轻易制成制剂。同样人们还需要显示降低的吸湿性的L-肉碱及其盐类的形式。
发明概述
因此,本发明的一个目的是提供新形式的L-肉碱及其盐类,其口服给药时生物利用度得到了提高。
本发明的另一个目的是提供新形式的L-肉碱及其盐类,它可以和不与大尺寸L-肉碱混合的其他组分如油基原料轻易地制成制剂。
本发明的另一个目的是提供新形式的L-肉碱及其盐类,其具有降低的吸湿性。
本发明的另一个目的是提供新的制备所述L-肉碱的方法。
本发明的另一个目的是提供含有所述L-肉碱的新的组合物。
本发明的另一个目的是提供所述L-肉碱的新的使用方法。
在以下的详细说明中,上述发明目的及其他发明目的将变得显而易见。这些发明目的通过发明人的发现而得以实现,即,以超细颗粒形式存在的L-肉碱及其盐类在口服给药时显示出高的生物利用度。发明人还发现所述L-肉碱可以很方便地与油基原料制成制剂。同时发明人还发现所述L-肉碱具有降低的吸湿性。
优选实施方案的详细描述
在第一个实施方案中,本发明提供了超细L-肉碱及其盐类。纵观本文,术语L-肉碱及其盐类不仅包括L-肉碱本身,还包括L-肉碱的盐类、烷酰基L-肉碱、以及烷酰基L-肉碱的盐类。适宜的L-肉碱的盐包括L-肉碱盐酸盐、L-肉碱氢溴酸盐、L-肉碱乳清酸盐、L-肉碱酸式天冬氨酸盐、L-肉碱酸式磷酸盐、L-肉碱富马酸盐、L-肉碱乳酸盐、L-肉碱马来酸盐、L-肉碱酸式马来酸盐、L-肉碱酸式草酸盐、L-肉碱酸式硫酸盐、L-肉碱葡萄糖磷酸盐、L-肉碱酒石酸盐、L-肉碱酸式酒石酸盐、L-肉碱碘酸盐、L-肉碱天冬氨酸盐、L-肉碱柠檬酸盐、L-肉碱酸式柠檬酸盐、L-肉碱酸式富马酸盐、L-肉碱甘油磷酸盐、L-肉碱粘酸盐、L-肉碱乳清酸盐、L-肉碱草酸盐、L-肉碱硫酸盐、L-肉碱三氯乙酸盐、L-肉碱三氟乙酸盐、L-肉碱甲磺酸盐、L-肉碱双羟萘酸盐以及L-肉碱酸式双羟萘酸盐。
适宜的烷酰基L-肉碱包括C2-8烷酰基L-肉碱、尤其是乙酰基、丁酰基、异丁酰基、戊酰基、异戊酰基以及更优选的丙酰基L-肉碱。
适宜的烷酰基L-肉碱的盐包括C2-8烷酰基L-肉碱盐酸盐、C2-8烷酰基L-肉碱氢溴酸盐、C2-8烷酰基L-肉碱乳清酸盐、C2-8烷酰基L-肉碱酸式天冬氨酸盐、C2-8烷酰基L-肉碱酸式磷酸盐、C2-8烷酰基L-肉碱富马酸盐、C2-8烷酰基L-肉碱乳酸盐、C2-8烷酰基L-肉碱马来酸盐、C2-8烷酰基L-肉碱酸式马来酸盐、C2-8烷酰基L-肉碱酸式草酸盐、C2-8烷酰基L-肉碱酸式硫酸盐、C2-8烷酰基L-肉碱葡萄糖磷酸盐、C2-8烷酰基L-肉碱酒石酸盐、C2-8烷酰基L-肉碱酸式酒石酸盐、C2-8烷酰基L-肉碱碘酸盐、C2-8烷酰基L-肉碱天冬氨酸盐、C2-8烷酰基L-肉碱柠檬酸盐、C2-8烷酰基L-肉碱酸式柠檬酸盐、C2-8烷酰基L-肉碱酸式富马酸盐、C2-8烷酰基L-肉碱甘油磷酸盐、C2-8烷酰基L-肉碱粘酸盐、C2-8烷酰基L-肉碱乳清酸盐、C2-8烷酰基L-肉碱草酸盐、C2-8烷酰基L-肉碱硫酸盐、C2-8烷酰基L-肉碱三氯乙酸盐、C2-8烷酰基L-肉碱三氟乙酸盐、C2-8烷酰基L-肉碱甲磺酸盐、C2-8烷酰基L-肉碱双羟萘酸盐以及C2-8烷酰基L-肉碱酸式双羟萘酸盐。
因此,本发明不仅提供了L-肉碱的超细颗粒还提供了L-肉碱的盐的超细颗粒。本发明同时提供由L-肉碱的超细颗粒和一种或多种L-肉碱的盐的超细颗粒组成的混合物,同样还提供由两种或两种以上L-肉碱的盐的超细颗粒组成的混合物。
本发明的超细L-肉碱及其盐类的颗粒足够的细微,以致基本上全部通过一个100美国标准化局(USBS)目筛。在一个优选的实施方案中,本发明的超细L-肉碱及其盐类的颗粒足够细微,可以基本全部通过一个150USBS目筛。在一个最优选的实施方案中,本发明的超细L-肉碱及其盐类具有足够细微的颗粒其基本上全部通过一个200USBS目筛。
本发明的超细L-肉碱及其盐类可以通过减小常规L-肉碱及其盐类的大小然后经筛分筛选大小合适的颗粒而得到。目前,L-肉碱及其盐类可以依据美国专利4,254,053、4,602,039和5,412,113以及欧洲专利申请EP-A-0150688中描述的方法方便的制得,这些文献在这里并入作为本发明的参考资料。这些方法通常得到的L-肉碱的尺寸使10%以上重量的L-肉碱被截留在50目的筛网上;40%以上重量的L-肉碱被截留在100目的筛网上。本发明的超细L-肉碱可通过减小这样的L-肉碱的尺寸而制得。可以通过任一种合适的工艺来达到使尺寸变小的目的,比如粉碎、研磨等等。减小尺寸的方法众所周知而且也记载在Kirk-Othmer所著的《
Encyclopedia of Chemical Technology》第四版,Wiley,New York,第22卷,第279-296页中,将此书作为本发明的参考资料之一并入本文。
当将由普通方法制得的L-肉碱经过减小尺寸的操作后,可以通过对尺寸减小后的L-肉碱进行筛分而选择本发明的超细L-肉碱。筛分是一种公知的用于选择具有某一特定尺寸的物料的工艺,这种方法在Kirk-0thmer所著的《
Encyclopedia of Chemical Technology》第四版,Wiley,New York,第22卷,第256-278页中有详细的描述,此书在此并入本文作参考。选择能通过100USBS目筛,优选150USBS目筛,更优选200USBS目筛的物料而获得本发明的超细L-肉碱。
在另一个实施方案中,本发明提供了含有超细L-肉碱与药学上可接受的赋形剂或载体的组合物。适宜的药学上可接受的赋形剂或载体在Remington’sPharmaceutical Sciences Handbook,Mack Publishing中有详细的记载。此书在此并入本文作参考。
在一个优选的实施方案中,药学上可接受的赋形剂或载体是一种油基物质,比如包括但不限于维生素E的合成或天然的油基维生素;例如但不限于大豆油、橄榄油、棕榈油或玉米油的从任一种子或者蔬菜中提炼的油料;以及可以预先溶解、悬浮或者混合在上述一种或多种油料中的任一营养物质。
基于该组合物的总重量,此组合物中超细L-肉碱适宜的含量为重量计10-99%,优选25-95%更优选的是50-90%。此组合物可制成软明胶胶囊、粉剂、丸剂、片剂等形式的制剂。在一优选的实施方案中,此组合物制成明胶胶囊、预混剂、囊剂、可复配的运动饮料混合剂。
此组合物可进一步包含任一种所知的能与L-肉碱或其盐类相组合的附加活性成分如羟基柠檬酸、辅酶Q10、吡啶甲酸铬、γ-亚麻酸、白藜芦醇、ω3酸、抗氧化剂、维生素等等。
在另一个实施方案中,本发明提供了处置、治疗或预防的方法,该方法包括给需要此处置、治疗、或预防的对象口服有效量的本发明的超细L-肉碱或其盐。本发明的超细L-肉碱可在其中使用的处置、治疗和/或预防方法在美国专利Nos.4,474,812和5,861,434中有详细描述,此文献亦并入本文作参考。
本发明的组合物的最低活性物质含量是57%;且在含于软明胶胶囊、预混物、囊剂和可复配的运动饮料混合物中的组合制剂中,能够延长保存期。加工者(将本发明超细L-肉碱转化为成品的人或实体)能在地理位置遥远的销售市场上获得成功,就是因为干燥产品运输到销售地的费用和仓储的费用低廉,然后在当地复配,即为加工者削减了成本、制造了商机。
还有其他方面的益处。因为本发明的超细L-肉碱及其盐类或许是制备组合物制剂(比如L-肉碱和辅酶Q10)的最佳L-肉碱来源,由于颗粒大小相似。
超细L-肉碱富马酸盐和本发明的化合物被发现具有通过线粒体途径的较高生物利用度。经比较其与常规尺寸的L-肉碱酒石酸盐在达到相同的人体血浆浓度时各自需要的相同预给药量而证实了这个结果。加工者因此能够使用减少的活性药团来达到目标剂量,即功效节省了成本。总的来说,消费者基于纯的重量/体积(W/V)基准购买了营养物质。而商家添加的活性物重量越多,其产品质量也被认为越高。
本发明的化合物可经“BSE”安全认证,因为它不含动物产品,而且是以化学合成为基础的。由于酒石酸盐是生物发酵物质(bioferm),因此避免了潜在的健康威胁和不必要的未知生物体的消耗。“国际食品销售组织”、绿色和平组织和其他的组织都发布了关于BSE的将来危险的文章。消费者对这种危险增加了警惕性。
本发明的化合物不象酒石酸盐那样,需要再加工(再制粒、再调整)。这样降低了生产成本、人力、环境接触。如果加工者不对酒石酸盐进行再加工,用酒石酸盐制得的片剂不能在明胶胶囊内或货架上较好的保质。
细微颗粒(200目)和亲水性和或疏水性二氧化硅包衣提供优异的混合和含量均匀性,尤其适于使用其他细微颗粒成分比如吡啶甲酸铬和辅酶Q10的制剂,而且由于其固有的低吸湿性使得其保质期延长。器具(冲头)和压制在理论上比使用酒石酸盐时在更低温下操作,因为其中的二氧化硅增加了润滑性,这将节省昂贵的停工费用,从而节省了成本。
本发明的超细L-肉碱特别适用于保证健康和均衡饮食的食物补充剂。它同样也可作为辅因子用于体重的控制及作为食物补充剂用于运动营养、素食营养、动物营养。同样它也可用于兽医学营养。
本发明的其他特点将在以下的公开的示范性的实施方式中得到清楚的说明。这些实施方式用于详细说明本发明,但是不能理解为本发明仅限于这些实施方式。
实施例
在以下的实施例中,贯穿说明书的始终,所有份数和百分比都以重量计、所有的温度是指摄氏温度,除非另外有明确的说明。当报道分散剂或者溶液的固体含量时,它表示基于分散剂或者溶液各自的总重量的固体重量。当说明分子量时,它是指由供货商提供的已鉴定的产品的分子量范围。通常认为它是重均分子量。
实施例1
将L-肉碱富马酸盐研磨成一种总体颗粒大小,使之能最低程度地通过100号USBS目筛。迄今为止,用于评价本发明效果的颗粒实际上已研磨得能通过150-200目,而且有非常优异的效果。然后将颗粒同食品级的亲水性和/或疏水性的热解法二氧化硅或沉淀的二氧化硅混合,这些类型的二氧化硅可以从Degussa公司购得,这些二氧化硅的总表面积为每克190-475平方米,摇实密度为每升80-275克。
如此制备的超细L-肉碱富马酸盐具有如下的分析性质:
描述:白色结晶状粉末
分析:58.0%±2%肉碱
41.5%±1%富马酸
含水量:≤1%(Karl Fischer)
比旋光:[α]D 20=17.5°±1°(1%水溶液)
pH:3.0到4.0(1%水溶液)
溶解度:水中5g/100m1
网目大小:通过150目,用食品级热解法二氧化硅调整。
毒性:LD50(口服)>8,000mg/kg(大鼠)
显然,根据上述内容的教导,大量的针对本发明的修改和改变是可能的。因此应当这样理解:在所附权利要求书的范围内,本发明可采用在说明书中详细描述的方法之外的方法来实施。
上文提及的所有专利和相关文献全文在此并入作参考,就象全文在此阐述过一样。
此申请基于在1999年9月3日提交的美国临时申请60/152,240和1999年10月8日提交的美国临时申请60/158,245,这两件美国临时申请全文并入本文作参考。
Claims (14)
1.一种L-肉碱,具有的颗粒大小使它能基本上通过100USBS目筛。
2.权利要求1的L-肉碱,选自下组:
L-肉碱、L-肉碱的盐类、烷酰基L-肉碱和烷酰基L-肉碱的盐类。
3.权利要求1的L-肉碱,选自下组:
L-肉碱盐酸盐、L-肉碱氢溴酸盐、L-肉碱乳清酸盐、L-肉碱酸式天冬氨酸盐、L-肉碱酸式磷酸盐、L-肉碱富马酸盐、L-肉碱乳酸盐、L-肉碱马来酸盐、L-肉碱酸式马来酸盐、L-肉碱酸式草酸盐、L-肉碱酸式硫酸盐、L-肉碱葡萄糖磷酸盐、L-肉碱酒石酸盐、L-肉碱酸式酒石酸盐、L-肉碱碘酸盐、L-肉碱天冬氨酸盐、L-肉碱柠檬酸盐、L-肉碱酸式柠檬酸盐、L-肉碱酸式富马酸盐、L-肉碱甘油磷酸盐、L-肉碱粘酸盐、L-肉碱乳清酸盐、L-肉碱草酸盐、L-肉碱硫酸盐、L-肉碱三氯乙酸盐、L-肉碱三氟乙酸盐、L-肉碱甲磺酸盐、L-肉碱双羟萘酸盐、L-肉碱酸式双羟萘酸盐、C2-8烷酰基L-肉碱、C2-8烷酰基L-肉碱盐酸盐、C2-8烷酰基L-肉碱氢溴酸盐、C2-8烷酰基L-肉碱乳清酸盐、C2-8烷酰基L-肉碱酸式天冬氨酸盐、C2-8烷酰基L-肉碱酸式磷酸盐、C2-8烷酰基L-肉碱富马酸盐、C2-8烷酰基L-肉碱乳酸盐、C2-8烷酰基L-肉碱马来酸盐、C2-8烷酰基L-肉碱酸式马来酸盐、C2-8烷酰基L-肉碱酸式草酸盐、C2-8烷酰基L-肉碱酸式硫酸盐、C2-8烷酰基L-肉碱葡萄糖磷酸盐、C2-8烷酰基L-肉碱酒石酸盐、C2-8烷酰基L-肉碱酸式酒石酸盐、C2-8烷酰基L-肉碱碘酸盐、C2-8烷酰基L-肉碱天冬氨酸盐、C2-8烷酰基L-肉碱柠檬酸盐、C2-8烷酰基L-肉碱酸式柠檬酸盐、C2-8烷酰基L-肉碱富马酸盐、C2-8烷酰基L-肉碱甘油磷酸盐、C2-8烷酰基L-肉碱粘酸盐、C2-8烷酰基L-肉碱乳清酸盐、C2-8烷酰基L-肉碱草酸盐、C2-8烷酰基L-肉碱硫酸盐、C2-8烷酰基L-肉碱三氯乙酸盐、C2-8烷酰基L-肉碱三氟乙酸盐、C2-8烷酰基L-肉碱甲磺酸盐、C2-8烷酰基L-肉碱双羟萘酸盐和C2-8烷酰基L-肉碱酸式双羟萘酸盐。
4.一种制备具有一定颗粒大小而使其能基本通过100USBS目筛的L-肉碱的方法,包括:
(1)将所具有的颗粒大小使其不能通过100USBS目筛的L-肉碱进行减小颗粒大小的操作,以得到颗粒大小减小的L-肉碱;和
(2)将上述颗粒大小减小的L-肉碱用100USBS目筛筛分,选出能通过此100USBS目筛的部分。
5.权利要求4的方法,其中所述L-肉碱选自下组:
L-肉碱、L-肉碱的盐类、烷酰基L-肉碱、烷酰基L-肉碱的盐类。
6.权利要求4的方法,其中所述L-肉碱选自下组:
L-肉碱盐酸盐、L-肉碱氢溴酸盐、L-肉碱乳清酸盐、L-肉碱酸式天冬氨酸盐、L-肉碱酸式磷酸盐、L-肉碱富马酸盐、L-肉碱乳酸盐、L-肉碱马来酸盐、L-肉碱酸式马来酸盐、L-肉碱酸式草酸盐、L-肉碱酸式硫酸盐、L-肉碱葡萄糖磷酸盐、L-肉碱酒石酸盐、L-肉碱酸式酒石酸盐、L-肉碱碘酸盐、L-肉碱天冬氨酸盐、L-肉碱柠檬酸盐、L-肉碱酸式柠檬酸盐、L-肉碱酸式富马酸盐、L-肉碱甘油磷酸盐、L-肉碱粘酸盐、L-肉碱乳清酸盐、L-肉碱草酸盐、L-肉碱硫酸盐、L-肉碱三氯乙酸盐、L-肉碱三氟乙酸盐、L-肉碱甲磺酸盐、L-肉碱双羟萘酸盐、L-肉碱酸式双羟萘酸盐、C2-8烷酰基L-肉碱、C2-8烷酰基L-肉碱盐酸盐、C2-8烷酰基L-肉碱氢溴酸盐、C2-8烷酰基L-肉碱乳清酸盐、C2-8烷酰基L-肉碱酸式天冬氨酸盐、C2-8烷酰基L-肉碱酸式磷酸盐、C2-8烷酰基L-肉碱富马酸盐、C2-8烷酰基L-肉碱乳酸盐、C2-8烷酰基L-肉碱马来酸盐、C2-8烷酰基L-肉碱酸式马来酸盐、C2-8烷酰基L-肉碱酸式草酸盐、C2-8烷酰基L-肉碱酸式硫酸盐、C2-8烷酰基L-肉碱葡萄糖磷酸盐、C2-8烷酰基L-肉碱酒石酸盐、C2-8烷酰基L-肉碱酸式酒石酸盐、C2-8烷酰基L-肉碱碘酸盐、C2-8烷酰基L-肉碱天冬氨酸盐、C2-8烷酰基L-肉碱柠檬酸盐、C2-8烷酰基L-肉碱酸式柠檬酸盐、C2-8烷酰基L-肉碱富马酸盐、C2-8烷酰基L-肉碱甘油磷酸盐、C2-8烷酰基L-肉碱粘酸盐、C2-8烷酰基L-肉碱乳清酸盐、C2-8烷酰基L-肉碱草酸盐、C2-8烷酰基L-肉碱硫酸盐、C2-8烷酰基L-肉碱三氯乙酸盐、C2-8烷酰基L-肉碱三氟乙酸盐、C2-8烷酰基L-肉碱甲磺酸盐、C2-8烷酰基L-肉碱双羟萘酸盐和C2-8烷酰基L-肉碱酸式双羟萘酸盐。
7.一种组合物,包括:
(A)一种具有一定颗粒大小使得其基本能通过100USBS目筛的L-肉碱;和
(B)一种药学可接受的赋形剂或载体。
8.权利要求7的组合物,其中所述L-肉碱选自下组:
L-肉碱、L-肉碱的盐类,烷酰基L-肉碱、和烷酰基L-肉碱的盐类。
9.权利要求7的组合物,其中所述L-肉碱选自下组:
L-肉碱盐酸盐、L-肉碱氢溴酸盐、L-肉碱乳清酸盐、L-肉碱酸式天冬氨酸盐、L-肉碱酸式磷酸盐、L-肉碱富马酸盐、L-肉碱乳酸盐、L-肉碱马来酸盐、L-肉碱酸式马来酸盐、L-肉碱酸式草酸盐、L-肉碱酸式硫酸盐、L-肉碱葡萄糖磷酸盐、L-肉碱酒石酸盐、L-肉碱酸式酒石酸盐、L-肉碱碘酸盐、L-肉碱天冬氨酸盐、L-肉碱柠檬酸盐、L-肉碱酸式柠檬酸盐、L-肉碱酸式富马酸盐、L-肉碱甘油磷酸盐、L-肉碱粘酸盐、L-肉碱乳清酸盐、L-肉碱草酸盐、L-肉碱硫酸盐、L-肉碱三氯乙酸盐、L-肉碱三氟乙酸盐、L-肉碱甲磺酸盐、L-肉碱双羟萘酸盐、L-肉碱酸式双羟萘酸盐、C2-8烷酰基L-肉碱、C2-8烷酰基L-肉碱盐酸盐、C2-8烷酰基L-肉碱氢溴酸盐、C2-8烷酰基L-肉碱乳清酸盐、C2-8烷酰基L-肉碱酸式天冬氨酸盐、C2-8烷酰基L-肉碱酸式磷酸盐、C2-8烷酰基L-肉碱富马酸盐、C2-8烷酰基L-肉碱乳酸盐、C2-8烷酰基L-肉碱马来酸盐、C2-8烷酰基L-肉碱酸式马来酸盐、C2-8烷酰基L-肉碱酸式草酸盐、C2-8烷酰基L-肉碱酸式硫酸盐、C2-8烷酰基L-肉碱葡萄糖磷酸盐、C2-8烷酰基L-肉碱酒石酸盐、C2-8烷酰基L-肉碱酸式酒石酸盐、C2-8烷酰基L-肉碱碘酸盐、C2-8烷酰基L-肉碱天冬氨酸盐、C2-8烷酰基L-肉碱柠檬酸盐、C2-8烷酰基L-肉碱酸式柠檬酸盐、C2-8烷酰基L-肉碱富马酸盐、C2-8烷酰基L-肉碱甘油磷酸盐、C2-8烷酰基L-肉碱粘酸盐、C2-8烷酰基L-肉碱乳清酸盐、C2-8烷酰基L-肉碱草酸盐、C2-8烷酰基L-肉碱硫酸盐、C2-8烷酰基L-肉碱三氯乙酸盐、C2-8烷酰基L-肉碱三氟乙酸盐、C2-8烷酰基L-肉碱甲磺酸盐、C2-8烷酰基L-肉碱双羟萘酸盐和C2-8烷酰基L-肉碱酸式双羟萘酸盐。
10.权利要求7的组合物,其适用于经口摄入。
11.权利要求7的组合物,其进一步包含羟基柠檬酸、辅酶Q10、吡啶甲酸铬、γ-亚麻酸、白藜芦醇、ω3酸、抗氧化剂或维生素。
12.在处置、治疗或者预防的方法中,包括给需要的对象口服施以有效剂量的L-肉碱。其中改进之处在于所述L-肉碱具有一定颗粒大小使其能基本通过100USBS目筛。
13.权利要求12的方法,其中所述的L-肉碱选自下组:
L-肉碱、L-肉碱的盐类、烷酰基L-肉碱、以及烷酰基L-肉碱的盐类。
14.权利要求12的方法,其中所述的L-肉碱选自下组:
L-肉碱盐酸盐、L-肉碱氢溴酸盐、L-肉碱乳清酸盐、L-肉碱酸式天冬氨酸盐、L-肉碱酸式磷酸盐、L-肉碱富马酸盐、L-肉碱乳酸盐、L-肉碱马来酸盐、L-肉碱酸式马来酸盐、L-肉碱酸式草酸盐、L-肉碱酸式硫酸盐、L-肉碱葡萄糖磷酸盐、L-肉碱酒石酸盐、L-肉碱酸式酒石酸盐、L-肉碱碘酸盐、L-肉碱天冬氨酸盐、L-肉碱柠檬酸盐、L-肉碱酸式柠檬酸盐、L-肉碱酸式富马酸盐、L-肉碱甘油磷酸盐、L-肉碱粘酸盐、L-肉碱乳清酸盐、L-肉碱草酸盐、L-肉碱硫酸盐、L-肉碱三氯乙酸盐、L-肉碱三氟乙酸盐、L-肉碱甲磺酸盐、L-肉碱双羟萘酸盐、L-肉碱酸式双羟萘酸盐、C2-8烷酰基L-肉碱、C2-8烷酰基L-肉碱盐酸盐、C2-8烷酰基L-肉碱氢溴酸盐、C2-8烷酰基L-肉碱乳清酸盐、C2-8烷酰基L-肉碱酸式天冬氨酸盐、C2-8烷酰基L-肉碱酸式磷酸盐、C2-8烷酰基L-肉碱富马酸盐、C2-8烷酰基L-肉碱乳酸盐、C2-8烷酰基L-肉碱马来酸盐、C2-8烷酰基L-肉碱酸式马来酸盐、C2-8烷酰基L-肉碱酸式草酸盐、C2-8烷酰基L-肉碱酸式硫酸盐、C2-8烷酰基L-肉碱葡萄糖磷酸盐、C2-8烷酰基L-肉碱酒石酸盐、C2-8烷酰基L-肉碱酸式酒石酸盐、C2-8烷酰基L-肉碱碘酸盐、C2-8烷酰基L-肉碱天冬氨酸盐、C2-8烷酰基L-肉碱柠檬酸盐、C2-8烷酰基L-肉碱酸式柠檬酸盐、C2-8烷酰基L-肉碱富马酸盐、C2-8烷酰基L-肉碱甘油磷酸盐、C2-8烷酰基L-肉碱粘酸盐、C2-8烷酰基L-肉碱乳清酸盐、C2-8烷酰基L-肉碱草酸盐、C2-8烷酰基L-肉碱硫酸盐、C2-8烷酰基L-肉碱三氯乙酸盐、C2-8烷酰基L-肉碱三氟乙酸盐、C2-8烷酰基L-肉碱甲磺酸盐、C2-8烷酰基L-肉碱双羟萘酸盐和C2-8烷酰基L-肉碱酸式双羟萘酸盐。
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Cited By (2)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
WO2009082883A1 (fr) * | 2007-12-26 | 2009-07-09 | Guangzhou Konzern Pharmaceutical Co., Ltd. | Composition anti-obésité |
CN112250588A (zh) * | 2020-11-06 | 2021-01-22 | 哈尔滨工业大学(深圳) | 一种左旋肉碱离子液体及其制备方法、应用 |
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