CN1331476C - Method for preparing coenzyme-A sublingual lozenge - Google Patents
Method for preparing coenzyme-A sublingual lozenge Download PDFInfo
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- CN1331476C CN1331476C CNB200510043972XA CN200510043972A CN1331476C CN 1331476 C CN1331476 C CN 1331476C CN B200510043972X A CNB200510043972X A CN B200510043972XA CN 200510043972 A CN200510043972 A CN 200510043972A CN 1331476 C CN1331476 C CN 1331476C
- Authority
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- China
- Prior art keywords
- coenzyme
- antioxidant
- diluent
- sublingual
- povidone
- 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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- RGJOEKWQDUBAIZ-IBOSZNHHSA-N CoASH Chemical compound O[C@@H]1[C@H](OP(O)(O)=O)[C@@H](COP(O)(=O)OP(O)(=O)OCC(C)(C)[C@@H](O)C(=O)NCCC(=O)NCCS)O[C@H]1N1C2=NC=NC(N)=C2N=C1 RGJOEKWQDUBAIZ-IBOSZNHHSA-N 0.000 title claims abstract description 52
- RGJOEKWQDUBAIZ-UHFFFAOYSA-N coenzime A Natural products OC1C(OP(O)(O)=O)C(COP(O)(=O)OP(O)(=O)OCC(C)(C)C(O)C(=O)NCCC(=O)NCCS)OC1N1C2=NC=NC(N)=C2N=C1 RGJOEKWQDUBAIZ-UHFFFAOYSA-N 0.000 title claims abstract description 52
- 239000005516 coenzyme A Substances 0.000 title claims abstract description 52
- 229940093530 coenzyme a Drugs 0.000 title claims abstract description 52
- KDTSHFARGAKYJN-UHFFFAOYSA-N dephosphocoenzyme A Natural products OC1C(O)C(COP(O)(=O)OP(O)(=O)OCC(C)(C)C(O)C(=O)NCCC(=O)NCCS)OC1N1C2=NC=NC(N)=C2N=C1 KDTSHFARGAKYJN-UHFFFAOYSA-N 0.000 title claims abstract description 52
- 239000007937 lozenge Substances 0.000 title claims description 16
- 238000000034 method Methods 0.000 title description 7
- 239000003963 antioxidant agent Substances 0.000 claims abstract description 14
- 230000003078 antioxidant effect Effects 0.000 claims abstract description 14
- 239000008187 granular material Substances 0.000 claims abstract description 9
- 238000002360 preparation method Methods 0.000 claims abstract description 6
- 229920003081 Povidone K 30 Polymers 0.000 claims description 13
- 235000006708 antioxidants Nutrition 0.000 claims description 13
- VYPSYNLAJGMNEJ-UHFFFAOYSA-N Silicium dioxide Chemical compound O=[Si]=O VYPSYNLAJGMNEJ-UHFFFAOYSA-N 0.000 claims description 12
- 239000000741 silica gel Substances 0.000 claims description 12
- 229910002027 silica gel Inorganic materials 0.000 claims description 12
- 229940093429 polyethylene glycol 6000 Drugs 0.000 claims description 11
- 239000003085 diluting agent Substances 0.000 claims description 10
- GUBGYTABKSRVRQ-QKKXKWKRSA-N Lactose Natural products OC[C@H]1O[C@@H](O[C@H]2[C@H](O)[C@@H](O)C(O)O[C@@H]2CO)[C@H](O)[C@@H](O)[C@H]1O GUBGYTABKSRVRQ-QKKXKWKRSA-N 0.000 claims description 9
- 239000008101 lactose Substances 0.000 claims description 9
- CZMRCDWAGMRECN-UGDNZRGBSA-N Sucrose Chemical compound O[C@H]1[C@H](O)[C@@H](CO)O[C@@]1(CO)O[C@@H]1[C@H](O)[C@@H](O)[C@H](O)[C@@H](CO)O1 CZMRCDWAGMRECN-UGDNZRGBSA-N 0.000 claims description 7
- 229930006000 Sucrose Natural products 0.000 claims description 7
- 239000005720 sucrose Substances 0.000 claims description 7
- LFQSCWFLJHTTHZ-UHFFFAOYSA-N Ethanol Chemical compound CCO LFQSCWFLJHTTHZ-UHFFFAOYSA-N 0.000 claims description 6
- WQZGKKKJIJFFOK-GASJEMHNSA-N Glucose Natural products OC[C@H]1OC(O)[C@H](O)[C@@H](O)[C@@H]1O WQZGKKKJIJFFOK-GASJEMHNSA-N 0.000 claims description 6
- 239000008103 glucose Substances 0.000 claims description 6
- RWSXRVCMGQZWBV-WDSKDSINSA-N glutathione Chemical compound OC(=O)[C@@H](N)CCC(=O)N[C@@H](CS)C(=O)NCC(O)=O RWSXRVCMGQZWBV-WDSKDSINSA-N 0.000 claims description 6
- 235000003969 glutathione Nutrition 0.000 claims description 6
- 229960003180 glutathione Drugs 0.000 claims description 6
- 239000002671 adjuvant Substances 0.000 claims description 5
- XUJNEKJLAYXESH-UHFFFAOYSA-N cysteine Natural products SCC(N)C(O)=O XUJNEKJLAYXESH-UHFFFAOYSA-N 0.000 claims description 4
- 235000018417 cysteine Nutrition 0.000 claims description 4
- 239000000203 mixture Substances 0.000 claims description 4
- 239000007779 soft material Substances 0.000 claims description 4
- 238000003756 stirring Methods 0.000 claims description 4
- WQZGKKKJIJFFOK-VFUOTHLCSA-N beta-D-glucose Chemical compound OC[C@H]1O[C@@H](O)[C@H](O)[C@@H](O)[C@@H]1O WQZGKKKJIJFFOK-VFUOTHLCSA-N 0.000 claims description 3
- GUBGYTABKSRVRQ-XLOQQCSPSA-N Alpha-Lactose Chemical compound O[C@@H]1[C@@H](O)[C@@H](O)[C@@H](CO)O[C@H]1O[C@@H]1[C@@H](CO)O[C@H](O)[C@H](O)[C@H]1O GUBGYTABKSRVRQ-XLOQQCSPSA-N 0.000 claims description 2
- FBPFZTCFMRRESA-KVTDHHQDSA-N D-Mannitol Chemical compound OC[C@@H](O)[C@@H](O)[C@H](O)[C@H](O)CO FBPFZTCFMRRESA-KVTDHHQDSA-N 0.000 claims description 2
- 229930195725 Mannitol Natural products 0.000 claims description 2
- 239000000594 mannitol Substances 0.000 claims description 2
- 235000010355 mannitol Nutrition 0.000 claims description 2
- 238000012856 packing Methods 0.000 claims description 2
- 239000002245 particle Substances 0.000 claims description 2
- 239000002904 solvent Substances 0.000 claims description 2
- 239000006190 sub-lingual tablet Substances 0.000 claims 2
- 229940098466 sublingual tablet Drugs 0.000 claims 2
- 208000004930 Fatty Liver Diseases 0.000 abstract description 6
- 206010019708 Hepatic steatosis Diseases 0.000 abstract description 6
- 208000010706 fatty liver disease Diseases 0.000 abstract description 6
- 231100000240 steatosis hepatitis Toxicity 0.000 abstract description 6
- 238000002347 injection Methods 0.000 abstract description 4
- 239000007924 injection Substances 0.000 abstract description 4
- 229940046011 buccal tablet Drugs 0.000 abstract description 3
- 239000006189 buccal tablet Substances 0.000 abstract description 3
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 abstract description 3
- 208000007848 Alcoholism Diseases 0.000 abstract description 2
- 208000008589 Obesity Diseases 0.000 abstract description 2
- 201000007930 alcohol dependence Diseases 0.000 abstract description 2
- 230000000694 effects Effects 0.000 abstract description 2
- 201000005577 familial hyperlipidemia Diseases 0.000 abstract description 2
- 208000030159 metabolic disease Diseases 0.000 abstract description 2
- 208000024172 Cardiovascular disease Diseases 0.000 abstract 1
- 210000001035 gastrointestinal tract Anatomy 0.000 abstract 1
- 239000000463 material Substances 0.000 abstract 1
- 239000003826 tablet Substances 0.000 abstract 1
- CIWBSHSKHKDKBQ-JLAZNSOCSA-N Ascorbic acid Chemical compound OC[C@H](O)[C@H]1OC(=O)C(O)=C1O CIWBSHSKHKDKBQ-JLAZNSOCSA-N 0.000 description 16
- HVYWMOMLDIMFJA-DPAQBDIFSA-N cholesterol Chemical compound C1C=C2C[C@@H](O)CC[C@]2(C)[C@@H]2[C@@H]1[C@@H]1CC[C@H]([C@H](C)CCCC(C)C)[C@@]1(C)CC2 HVYWMOMLDIMFJA-DPAQBDIFSA-N 0.000 description 8
- ZZZCUOFIHGPKAK-UHFFFAOYSA-N D-erythro-ascorbic acid Natural products OCC1OC(=O)C(O)=C1O ZZZCUOFIHGPKAK-UHFFFAOYSA-N 0.000 description 7
- 229930003268 Vitamin C Natural products 0.000 description 7
- 235000019154 vitamin C Nutrition 0.000 description 7
- 239000011718 vitamin C Substances 0.000 description 7
- UFTFJSFQGQCHQW-UHFFFAOYSA-N triformin Chemical compound O=COCC(OC=O)COC=O UFTFJSFQGQCHQW-UHFFFAOYSA-N 0.000 description 5
- 239000003814 drug Substances 0.000 description 4
- 239000000126 substance Substances 0.000 description 4
- 210000004369 blood Anatomy 0.000 description 3
- 239000008280 blood Substances 0.000 description 3
- 150000002632 lipids Chemical class 0.000 description 3
- 239000000314 lubricant Substances 0.000 description 3
- GHOKWGTUZJEAQD-ZETCQYMHSA-N (D)-(+)-Pantothenic acid Chemical compound OCC(C)(C)[C@@H](O)C(=O)NCCC(O)=O GHOKWGTUZJEAQD-ZETCQYMHSA-N 0.000 description 2
- CSCPPACGZOOCGX-UHFFFAOYSA-N Acetone Chemical compound CC(C)=O CSCPPACGZOOCGX-UHFFFAOYSA-N 0.000 description 2
- 208000031226 Hyperlipidaemia Diseases 0.000 description 2
- XUJNEKJLAYXESH-REOHCLBHSA-N L-Cysteine Chemical compound SC[C@H](N)C(O)=O XUJNEKJLAYXESH-REOHCLBHSA-N 0.000 description 2
- 241001465754 Metazoa Species 0.000 description 2
- 239000000853 adhesive Substances 0.000 description 2
- 230000001070 adhesive effect Effects 0.000 description 2
- 235000012000 cholesterol Nutrition 0.000 description 2
- 150000001875 compounds Chemical class 0.000 description 2
- UFULAYFCSOUIOV-UHFFFAOYSA-N cysteamine Chemical compound NCCS UFULAYFCSOUIOV-UHFFFAOYSA-N 0.000 description 2
- 201000010099 disease Diseases 0.000 description 2
- 238000001647 drug administration Methods 0.000 description 2
- JYGXADMDTFJGBT-VWUMJDOOSA-N hydrocortisone Chemical compound O=C1CC[C@]2(C)[C@H]3[C@@H](O)C[C@](C)([C@@](CC4)(O)C(=O)CO)[C@@H]4[C@@H]3CCC2=C1 JYGXADMDTFJGBT-VWUMJDOOSA-N 0.000 description 2
- 230000003516 hyperlipidaemic effect Effects 0.000 description 2
- 230000002779 inactivation Effects 0.000 description 2
- 229960003151 mercaptamine Drugs 0.000 description 2
- 230000004060 metabolic process Effects 0.000 description 2
- 235000015097 nutrients Nutrition 0.000 description 2
- XTWYTFMLZFPYCI-KQYNXXCUSA-N 5'-adenylphosphoric acid Chemical group C1=NC=2C(N)=NC=NC=2N1[C@@H]1O[C@H](COP(O)(=O)OP(O)(O)=O)[C@@H](O)[C@H]1O XTWYTFMLZFPYCI-KQYNXXCUSA-N 0.000 description 1
- 208000010444 Acidosis Diseases 0.000 description 1
- 208000002874 Acne Vulgaris Diseases 0.000 description 1
- PQSUYGKTWSAVDQ-ZVIOFETBSA-N Aldosterone Chemical compound C([C@@]1([C@@H](C(=O)CO)CC[C@H]1[C@@H]1CC2)C=O)[C@H](O)[C@@H]1[C@]1(C)C2=CC(=O)CC1 PQSUYGKTWSAVDQ-ZVIOFETBSA-N 0.000 description 1
- PQSUYGKTWSAVDQ-UHFFFAOYSA-N Aldosterone Natural products C1CC2C3CCC(C(=O)CO)C3(C=O)CC(O)C2C2(C)C1=CC(=O)CC2 PQSUYGKTWSAVDQ-UHFFFAOYSA-N 0.000 description 1
- 206010003210 Arteriosclerosis Diseases 0.000 description 1
- GHOKWGTUZJEAQD-UHFFFAOYSA-N Chick antidermatitis factor Natural products OCC(C)(C)C(O)C(=O)NCCC(O)=O GHOKWGTUZJEAQD-UHFFFAOYSA-N 0.000 description 1
- 208000012239 Developmental disease Diseases 0.000 description 1
- 241000196324 Embryophyta Species 0.000 description 1
- 229920002527 Glycogen Polymers 0.000 description 1
- 206010029164 Nephrotic syndrome Diseases 0.000 description 1
- 239000002202 Polyethylene glycol Substances 0.000 description 1
- 206010043561 Thrombocytopenic purpura Diseases 0.000 description 1
- 230000003187 abdominal effect Effects 0.000 description 1
- OIPILFWXSMYKGL-UHFFFAOYSA-N acetylcholine Chemical compound CC(=O)OCC[N+](C)(C)C OIPILFWXSMYKGL-UHFFFAOYSA-N 0.000 description 1
- 229960004373 acetylcholine Drugs 0.000 description 1
- 230000007950 acidosis Effects 0.000 description 1
- 208000026545 acidosis disease Diseases 0.000 description 1
- 206010000496 acne Diseases 0.000 description 1
- 230000003213 activating effect Effects 0.000 description 1
- 229960002478 aldosterone Drugs 0.000 description 1
- 235000001014 amino acid Nutrition 0.000 description 1
- 150000001413 amino acids Chemical class 0.000 description 1
- 208000011775 arteriosclerosis disease Diseases 0.000 description 1
- 229960005070 ascorbic acid Drugs 0.000 description 1
- 235000010323 ascorbic acid Nutrition 0.000 description 1
- 239000011668 ascorbic acid Substances 0.000 description 1
- 230000015572 biosynthetic process Effects 0.000 description 1
- 230000036772 blood pressure Effects 0.000 description 1
- 210000004027 cell Anatomy 0.000 description 1
- 238000006243 chemical reaction Methods 0.000 description 1
- 239000005515 coenzyme Substances 0.000 description 1
- 238000000748 compression moulding Methods 0.000 description 1
- 235000009508 confectionery Nutrition 0.000 description 1
- 210000002808 connective tissue Anatomy 0.000 description 1
- 206010012601 diabetes mellitus Diseases 0.000 description 1
- 229940079593 drug Drugs 0.000 description 1
- 238000001035 drying Methods 0.000 description 1
- 238000005516 engineering process Methods 0.000 description 1
- 239000000284 extract Substances 0.000 description 1
- 238000000855 fermentation Methods 0.000 description 1
- 230000004151 fermentation Effects 0.000 description 1
- 235000013305 food Nutrition 0.000 description 1
- 229940096919 glycogen Drugs 0.000 description 1
- 239000000745 gonadal hormone Substances 0.000 description 1
- 235000013402 health food Nutrition 0.000 description 1
- 230000002440 hepatic effect Effects 0.000 description 1
- 229960000890 hydrocortisone Drugs 0.000 description 1
- 210000000987 immune system Anatomy 0.000 description 1
- 238000007689 inspection Methods 0.000 description 1
- 230000000968 intestinal effect Effects 0.000 description 1
- 201000002364 leukopenia Diseases 0.000 description 1
- 231100001022 leukopenia Toxicity 0.000 description 1
- 210000004185 liver Anatomy 0.000 description 1
- 230000003908 liver function Effects 0.000 description 1
- 230000007774 longterm Effects 0.000 description 1
- 238000004519 manufacturing process Methods 0.000 description 1
- 230000002503 metabolic effect Effects 0.000 description 1
- 230000000813 microbial effect Effects 0.000 description 1
- 244000005700 microbiome Species 0.000 description 1
- 210000004400 mucous membrane Anatomy 0.000 description 1
- 208000010125 myocardial infarction Diseases 0.000 description 1
- 231100000957 no side effect Toxicity 0.000 description 1
- 235000020824 obesity Nutrition 0.000 description 1
- 239000003960 organic solvent Substances 0.000 description 1
- 239000007800 oxidant agent Substances 0.000 description 1
- 230000003647 oxidation Effects 0.000 description 1
- 238000007254 oxidation reaction Methods 0.000 description 1
- 230000001590 oxidative effect Effects 0.000 description 1
- 229940055726 pantothenic acid Drugs 0.000 description 1
- 235000019161 pantothenic acid Nutrition 0.000 description 1
- 239000011713 pantothenic acid Substances 0.000 description 1
- 238000005453 pelletization Methods 0.000 description 1
- 210000002381 plasma Anatomy 0.000 description 1
- 229920001223 polyethylene glycol Polymers 0.000 description 1
- 229920000036 polyvinylpyrrolidone Polymers 0.000 description 1
- 235000013855 polyvinylpyrrolidone Nutrition 0.000 description 1
- FYPMFJGVHOHGLL-UHFFFAOYSA-N probucol Chemical compound C=1C(C(C)(C)C)=C(O)C(C(C)(C)C)=CC=1SC(C)(C)SC1=CC(C(C)(C)C)=C(O)C(C(C)(C)C)=C1 FYPMFJGVHOHGLL-UHFFFAOYSA-N 0.000 description 1
- 238000000926 separation method Methods 0.000 description 1
- 210000002966 serum Anatomy 0.000 description 1
- 239000000243 solution Substances 0.000 description 1
- 239000003270 steroid hormone Substances 0.000 description 1
- 210000002784 stomach Anatomy 0.000 description 1
- 230000004102 tricarboxylic acid cycle Effects 0.000 description 1
- XLYOFNOQVPJJNP-UHFFFAOYSA-N water Substances O XLYOFNOQVPJJNP-UHFFFAOYSA-N 0.000 description 1
- 239000012138 yeast extract Substances 0.000 description 1
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- Medicinal Preparation (AREA)
Abstract
The present invention discloses a preparation method for a sublingual buccal tablet containing coenzyme A, which is prepared from coenzyme A, an antioxidant and medicinal auxiliary materials. Blank granules and the coenzyme A are uniformly mixed and compressed into tablets. The preparation method solves the problems that coenzyme A for injection is not convenient for use for a long period of time and the activity of oral coenzyme A is easy to damage when the oral coenzyme A passes through gastrointestinal tracts; thus, the coenzyme A can be conveniently used for preventing and treating various metabolic disorder diseases, (such as hyperlipemia, adiposis, fatty liver, and the like.), cardiovascular disease and alcoholism which are caused by the shortage of the coenzyme A. The sublingual buccal tablet containing coenzyme A has very good development and application prospects.
Description
Technical field
The invention belongs to medicine, health product, new resource food technical field, be specially a kind of manufacture method and application of coenzyme-A sublingual lozenge.
Technical background
Coenzyme A is a kind of natural biochemical substances that extensively is present in animal, plant, microorganism cultures and cell, has no side effect.Its molecule by pantothenic acid, Mercamine Cysteamine and 3 ', 5 '-adenosine diphosphate (ADP) forms, and is soluble in water, is insoluble to ethanol, acetone and other organic solvent, more stable, but in the presence of alkalescence, high temperature, oxidant easy inactivation.Coenzyme A is the coenzyme of acetylization reaction in the organism; sugar, lipid and proteinic metabolism in the body are played an important role; as synthetic, the reduction of cholesterol of the accumulating of tricarboxylic acid cycle, hepatic glycogen, acetylcholine and the adjusting of blood plasma lipide content, synthetic (aldosterone, hydrocortisone and the gonadal hormone) of steroid hormone etc.; also but activating immune system does not have internal metabolism to detoxifcation, the formation of promotion connective tissue and the reparation etc. of harmful substance without coenzyme A.Coenzyme A lacks in the body, all kinds of diseases that will cause Developmental and Metabolic Disorder to cause.Clinical hyperlipemia, fatty liver, obesity, arteriosclerosis, myocardial infarction, thrombocytopenic purpura, leukopenia, the nephrotic syndrome, diabetes acidosis, the alcoholism of being used for, also can treat acne, the speckle etc. that discolors is a kind of important biochemical drug, health product.Because the easy oxidation inactivation of coenzyme A and in intestinal destructible, coenzyme A can only be by injection administration so far, and when preventing, treating metabolic imbalance class disease, the course of treatment is long, drug administration by injection is very inconvenient, has limited the extensive use of coenzyme A.
Summary of the invention
The present invention enriches medicine according to hypoglossis mucous membrane and absorbs easily and the little characteristics of coenzyme A dosage, adopt suitable antioxidant, correctives and adjuvant that coenzyme A is made and be easy to the sublingual lozenge that absorbs and utilize, overcome the difficult problem of coenzyme A drug administration by injection inconvenience and oral destructible, but make coenzyme A long-term prescription, extensive use, have a extensive future.
The invention provides a kind of coenzyme-A sublingual lozenge preparation method.
Coenzyme-A sublingual lozenge of the present invention is made up of active component coenzyme A and adjuvant antioxidant, diluent, adhesive, lubricant, fluidizer.
The used coenzyme A of coenzyme-A sublingual lozenge of the present invention can be derive from that animal livers, heart extract, yeast extracts or microbial fermentation.Antioxidant can be a kind of of vitamin C, cysteine, glutathion or it is several compound, diluent can be a kind of of sucrose, glucose, lactose, mannitol or it is several compound, adhesive is a 30 POVIDONE K 30 BP/USP 30, and lubricant is a polyethylene glycol 6000, and fluidizer is micropowder silica gel.
The antioxidant vitamin C has another name called ascorbic acid in the above-mentioned adjuvant, is that human life institute is essential, can make medicine and can make health food again, mainly makes antioxidant in this coenzyme-A sublingual lozenge, can make acidulant, correctives again.Cysteine, glutathion are the amino acids nutrient substance, all contain sulfydryl, can make antioxidant and nutrient substance.Diluent sucrose, glucose, the easy compression molding of lactose easily dissolve in the Sublingual, and pleasantly sweet, mouthfeel is good, also can make correctives.Polyvidone not only is easy to granulate, and also is easy to buccal tablet and is bonding on the Sublingual.Polyethylene Glycol, micropowder silica gel are easy to tabletting as lubricant and fluidizer, and mouthfeel is good.
Every of above-mentioned coenzyme-A sublingual lozenge contains coenzyme A 10-10000U, and the adjuvant ratio of components is: antioxidant 10%-50%, diluent 50%-80%, 30 POVIDONE K 30 BP/USP 30 0.1%-1.5%, polyethylene glycol 6000 1%-5%, micropowder silica gel 0.1%-15%.
Above-mentioned coenzyme-A sublingual lozenge adopts blank pelletizing press sheet technology, contains following operation successively:
1) coenzyme A is passed with antioxidant doubly diluted 10-20 doubly, standby;
2) diluent was pulverized 100 mesh sieves, standby;
3) it is an amount of that inventory 30 POVIDONE K 30 BP/USP 30 adds 70% ethanol, and stirring and dissolving is standby;
4) diluent, antioxidant were mixed in mixer 20 minutes by the prescription proportioning according to inventory, stir slow down solvent 30 POVIDONE K 30 BP/USP 30 solution that add, mix the system soft material;
5) soft material is granulated with 18 mesh sieves, and particle requirement is evenly loose, sabot;
6) wet grain is put drying in the 50-60 ℃ of baking oven, notes turning over, and makes oven dry evenly, and moisture Control is at 5 5%-7%;
7) dry granular takes out the back and crosses 20 mesh sieve granulate, makes blank granule;
8) will dilute good coenzyme A and polyethylene glycol 6000, micropowder silica gel adds in the blank granule mix homogeneously, sample examination, tabletting by proportioning according to inventory;
9) pick test, qualified back packing.
Use a kind of coenzyme-A sublingual lozenge of the present invention's preparation, every contains coenzyme A 200 units, as follows to treatment hyperlipidemia (triglyceride TG, cholesterol TC) and fatty liver result of the test.
1. treatment hyperlipidemia
Object: select hyperlipemic patients for use, i.e. triglyceride TG 〉=2.1mmol/l or serum cholesterol TC 〉=5.2mmol/l person's 46 examples, male's 28 examples wherein, women's 18 examples, age 30-73 year.
Method: 1 of everyone each sublingual administration, sooner or later respectively once, 12 weeks of the course of treatment.
Lipid determination: before using coenzyme-A sublingual lozenge, reached for the 4th, 8,12 weekends, 12-14 hour on an empty stomach, venous blood samples, in time separation of serum is measured serum cholesterol and content of triglyceride, and measuring blood pressure, liver function and blood glucose.
The result: use coenzyme-A sublingual lozenge after the 4th, 8,12 weeks, triglyceride TG has on average descended 9.1%, 12.2%, 13.9% than with preceding difference, and serum cholesterol TC has on average descended 7.5%, 17.1%, 21.3% than with preceding difference, the effect highly significant.After 46 examples used for 12 weeks, triglyceride TG descended and surpasses 1.0mmol/l person's 35 examples, and effective percentage reaches 76%, and serum cholesterol descends and surpasses 2.0mmol/l person's 30 examples, and effective percentage reaches 65%.Data see Table 1.
Table 1: coenzyme-A sublingual lozenge is to the influence of hyperlipemic patients
| Blood lipids index | Case | Meansigma methods before the treatment | The 4th weekend meansigma methods | Reduce % | The 8th weekend meansigma methods | Reduce % | The 8th weekend meansigma methods | Reduce % |
| TG (mmol/l) | 46 | 3.020 | 2.745 | 9.1 | 2.651 | 12.2 | 2.598 | 13.9 |
| TC (mmol/l) | 46 | 7.705 | 7.127 | 7.5 | 6.39 | 17.1 | 6.108 | 21.3 |
2. treatment fatty liver
Patients with Fatty Liver 16 examples, 1 of everyone each sublingual administration, each once adopts the abdominal CT inspection 6 months courses of treatment sooner or later, and 9 routine fatty livers disappear, and other case all significantly improves.
The specific embodiment
Example 1: coenzyme A 1,000,000 U
Vitamin C 200g
Sucrose 500g
Lactose 300g
Polyethylene glycol 6000 10g
Micropowder silica gel 5g
30 POVIDONE K 30 BP/USP 30 4.5g
Make 10000
Example 2: coenzyme A 2,000,000 U
Vitamin C 200g
Sucrose 500g
Lactose 200g
Polyethylene glycol 6000 10g
Micropowder silica gel 5g
30 POVIDONE K 30 BP/USP 30 4.5g
Make 10000
Example 3: coenzyme A 2,000,000 U
Glutathion 100g
Sucrose 600g
Lactose 200g
Polyethylene glycol 6000 20g
Micropowder silica gel 6g
30 POVIDONE K 30 BP/USP 30 5g
Make 10000
Example 4: coenzyme A 2,500,000 U
Glutathion 100g
Vitamin C 200g
Sucrose 500g
Lactose 200g
Polyethylene glycol 6000 20g
Micropowder silica gel 6g
30 POVIDONE K 30 BP/USP 30 6g
Make 10000
Example 5: coenzyme A 3,000,000 U
Glutathion 100g
Vitamin C 200g
Lactose 400g
Glucose 300g
Polyethylene glycol 6000 20g
Micropowder silica gel 6g
30 POVIDONE K 30 BP/USP 30 6g
Make 10000
Example 6: coenzyme A 3,000,000 U
Cysteine 100g
Vitamin C 200g
Lactose 800g
Glucose 300g
Polyethylene glycol 6000 20g
Micropowder silica gel 8g
30 POVIDONE K 30 BP/USP 30 8g
Make 10000
Claims (3)
1. a coenzyme-A sublingual lozenge is characterized by described coenzyme-A sublingual lozenge, and every contains coenzyme A 10-10000U, the adjuvant ratio of components is: antioxidant 10%-50%, diluent 50%-80%, 30 POVIDONE K 30 BP/USP 30 0.1%-1.5%, polyethylene glycol 6000 1%-5%, micropowder silica gel 0.1%-1.5%.
2. coenzyme A Sublingual tablet according to claim 1 is characterized by: antioxidant is one or more in the plain C of dimension dirt, cysteine, the glutathion; Diluent is one or more in sucrose, glucose, lactose, the mannitol.
3. the preparation method of the coenzyme A Sublingual tablet of a claim 1 comprises the steps:
1) coenzyme A is passed with antioxidant doubly diluted 10-20 doubly, standby;
2) prepare blank granule
A, diluent was pulverized 100 mesh sieves, standby;
It is an amount of that B, 30 POVIDONE K 30 BP/USP 30 adds 70% ethanol, and stirring and dissolving is standby;
C, diluent, antioxidant were mixed in mixer 20 minutes, stir and slowly add solvent 30 POVIDONE K 30 BP/USP 30 solution down, mix the system soft material;
D, soft material are granulated with 18 mesh sieves, and particle requirement is evenly loose, sabot;
E, wet grain are put in the 50-60 ℃ of baking oven dry, note turning over, and make oven dry evenly, and moisture Control is at 5%-7%;
F, dry granular take out the back and cross 20 mesh sieve granulate, make blank granule;
3) will dilute good coenzyme A and polyethylene glycol 6000, micropowder silica gel adds in the blank granule mix homogeneously, sample examination, tabletting by proportioning according to inventory;
4) pick test, qualified back packing.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CNB200510043972XA CN1331476C (en) | 2005-07-05 | 2005-07-05 | Method for preparing coenzyme-A sublingual lozenge |
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CNB200510043972XA CN1331476C (en) | 2005-07-05 | 2005-07-05 | Method for preparing coenzyme-A sublingual lozenge |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| CN1723913A CN1723913A (en) | 2006-01-25 |
| CN1331476C true CN1331476C (en) | 2007-08-15 |
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| Application Number | Title | Priority Date | Filing Date |
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| CNB200510043972XA Expired - Fee Related CN1331476C (en) | 2005-07-05 | 2005-07-05 | Method for preparing coenzyme-A sublingual lozenge |
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| Country | Link |
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| CN (1) | CN1331476C (en) |
Families Citing this family (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN101693014B (en) * | 2009-11-04 | 2011-09-07 | 马鞍山丰原制药有限公司 | Process for preparing coenzyme A medicament freeze drying preparation |
| CN109568280A (en) * | 2018-12-29 | 2019-04-05 | 正大青春宝药业有限公司 | A kind of salviandic acid A sublingual tablet formulation and preparation method thereof |
| JP6864301B2 (en) | 2019-03-26 | 2021-04-28 | 宮崎 徹 | Composition for increasing blood-free AIM |
Citations (5)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN1253781A (en) * | 1999-08-16 | 2000-05-24 | 上海本草生物医学工程研究所 | CoA oral preparation for reducing blood fat and its preparation method |
| JP2001270825A (en) * | 2000-03-24 | 2001-10-02 | Sankyo Co Ltd | Pharmaceutical preparation containing pravastatin sodium |
| WO2004108161A1 (en) * | 2003-06-06 | 2004-12-16 | Takeda Pharmaceutical Company Limited | Solid pharmaceutical preparation |
| WO2005011634A1 (en) * | 2003-08-04 | 2005-02-10 | Pfizer Products Inc. | Dosage forms providing controlled release of cholesteryl ester transfer protein inhibitors and immediate release of hmg-coa reductase inhibitors |
| CN1628681A (en) * | 2004-08-30 | 2005-06-22 | 王永发 | Notoginsen triterpenes Notoginsen triterpenes lozenge |
-
2005
- 2005-07-05 CN CNB200510043972XA patent/CN1331476C/en not_active Expired - Fee Related
Patent Citations (5)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN1253781A (en) * | 1999-08-16 | 2000-05-24 | 上海本草生物医学工程研究所 | CoA oral preparation for reducing blood fat and its preparation method |
| JP2001270825A (en) * | 2000-03-24 | 2001-10-02 | Sankyo Co Ltd | Pharmaceutical preparation containing pravastatin sodium |
| WO2004108161A1 (en) * | 2003-06-06 | 2004-12-16 | Takeda Pharmaceutical Company Limited | Solid pharmaceutical preparation |
| WO2005011634A1 (en) * | 2003-08-04 | 2005-02-10 | Pfizer Products Inc. | Dosage forms providing controlled release of cholesteryl ester transfer protein inhibitors and immediate release of hmg-coa reductase inhibitors |
| CN1628681A (en) * | 2004-08-30 | 2005-06-22 | 王永发 | Notoginsen triterpenes Notoginsen triterpenes lozenge |
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| Publication number | Publication date |
|---|---|
| CN1723913A (en) | 2006-01-25 |
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