CN101066244A - Small volume vincamine injection and its prepn process - Google Patents
Small volume vincamine injection and its prepn process Download PDFInfo
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- CN101066244A CN101066244A CN 200610152514 CN200610152514A CN101066244A CN 101066244 A CN101066244 A CN 101066244A CN 200610152514 CN200610152514 CN 200610152514 CN 200610152514 A CN200610152514 A CN 200610152514A CN 101066244 A CN101066244 A CN 101066244A
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- Prior art keywords
- vinpocetine
- antioxidant
- cosolvent
- physically stable
- stable agent
- Prior art date
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- Granted
Links
- 238000002347 injection Methods 0.000 title claims abstract description 22
- 239000007924 injection Substances 0.000 title claims abstract description 22
- RXPRRQLKFXBCSJ-GIVPXCGWSA-N vincamine Chemical compound C1=CC=C2C(CCN3CCC4)=C5[C@@H]3[C@]4(CC)C[C@](O)(C(=O)OC)N5C2=C1 RXPRRQLKFXBCSJ-GIVPXCGWSA-N 0.000 title abstract description 26
- RXPRRQLKFXBCSJ-UHFFFAOYSA-N dl-Vincamin Natural products C1=CC=C2C(CCN3CCC4)=C5C3C4(CC)CC(O)(C(=O)OC)N5C2=C1 RXPRRQLKFXBCSJ-UHFFFAOYSA-N 0.000 title abstract description 13
- 229960002726 vincamine Drugs 0.000 title abstract description 13
- 238000000034 method Methods 0.000 title description 4
- 239000006184 cosolvent Substances 0.000 claims abstract description 16
- 239000003963 antioxidant agent Substances 0.000 claims abstract description 14
- 230000003078 antioxidant effect Effects 0.000 claims abstract description 14
- 239000003814 drug Substances 0.000 claims abstract description 12
- 238000002360 preparation method Methods 0.000 claims abstract description 11
- 230000000638 stimulation Effects 0.000 claims abstract description 10
- DDNCQMVWWZOMLN-IRLDBZIGSA-N Vinpocetine Chemical compound C1=CC=C2C(CCN3CCC4)=C5[C@@H]3[C@]4(CC)C=C(C(=O)OCC)N5C2=C1 DDNCQMVWWZOMLN-IRLDBZIGSA-N 0.000 claims description 28
- 229960000744 vinpocetine Drugs 0.000 claims description 28
- 239000003795 chemical substances by application Substances 0.000 claims description 18
- GEHJYWRUCIMESM-UHFFFAOYSA-L sodium sulfite Chemical compound [Na+].[Na+].[O-]S([O-])=O GEHJYWRUCIMESM-UHFFFAOYSA-L 0.000 claims description 16
- CIWBSHSKHKDKBQ-JLAZNSOCSA-N Ascorbic acid Chemical compound OC[C@H](O)[C@H]1OC(=O)C(O)=C1O CIWBSHSKHKDKBQ-JLAZNSOCSA-N 0.000 claims description 14
- 235000006708 antioxidants Nutrition 0.000 claims description 13
- 230000002792 vascular Effects 0.000 claims description 10
- XLYOFNOQVPJJNP-UHFFFAOYSA-N water Chemical compound O XLYOFNOQVPJJNP-UHFFFAOYSA-N 0.000 claims description 10
- QTBSBXVTEAMEQO-UHFFFAOYSA-N Acetic acid Chemical compound CC(O)=O QTBSBXVTEAMEQO-UHFFFAOYSA-N 0.000 claims description 9
- 229940079593 drug Drugs 0.000 claims description 9
- 235000010265 sodium sulphite Nutrition 0.000 claims description 8
- OKTJSMMVPCPJKN-UHFFFAOYSA-N Carbon Chemical compound [C] OKTJSMMVPCPJKN-UHFFFAOYSA-N 0.000 claims description 7
- 239000003610 charcoal Substances 0.000 claims description 7
- 229940105082 medicinal charcoal Drugs 0.000 claims description 7
- 239000000203 mixture Substances 0.000 claims description 7
- 239000008215 water for injection Substances 0.000 claims description 6
- 235000010323 ascorbic acid Nutrition 0.000 claims description 5
- 239000011668 ascorbic acid Substances 0.000 claims description 5
- 229960005070 ascorbic acid Drugs 0.000 claims description 5
- 239000000047 product Substances 0.000 claims description 5
- HRZFUMHJMZEROT-UHFFFAOYSA-L sodium disulfite Chemical compound [Na+].[Na+].[O-]S(=O)S([O-])(=O)=O HRZFUMHJMZEROT-UHFFFAOYSA-L 0.000 claims description 5
- 235000010262 sodium metabisulphite Nutrition 0.000 claims description 5
- FBPFZTCFMRRESA-FSIIMWSLSA-N D-Glucitol Natural products OC[C@H](O)[C@H](O)[C@@H](O)[C@H](O)CO FBPFZTCFMRRESA-FSIIMWSLSA-N 0.000 claims description 4
- 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 4
- 229930195725 Mannitol Natural products 0.000 claims description 4
- 239000002671 adjuvant Substances 0.000 claims description 4
- 210000004204 blood vessel Anatomy 0.000 claims description 4
- JVTAAEKCZFNVCJ-UHFFFAOYSA-N lactic acid Chemical compound CC(O)C(O)=O JVTAAEKCZFNVCJ-UHFFFAOYSA-N 0.000 claims description 4
- 239000000594 mannitol Substances 0.000 claims description 4
- 235000010355 mannitol Nutrition 0.000 claims description 4
- 239000000600 sorbitol Substances 0.000 claims description 4
- UMGDCJDMYOKAJW-UHFFFAOYSA-N thiourea Chemical compound NC(N)=S UMGDCJDMYOKAJW-UHFFFAOYSA-N 0.000 claims description 4
- 238000010521 absorption reaction Methods 0.000 claims description 3
- 238000001816 cooling Methods 0.000 claims description 3
- 238000009472 formulation Methods 0.000 claims description 3
- AKHNMLFCWUSKQB-UHFFFAOYSA-L sodium thiosulfate Chemical compound [Na+].[Na+].[O-]S([O-])(=O)=S AKHNMLFCWUSKQB-UHFFFAOYSA-L 0.000 claims description 3
- 235000019345 sodium thiosulphate Nutrition 0.000 claims description 3
- KGRVJHAUYBGFFP-UHFFFAOYSA-N 2,2'-Methylenebis(4-methyl-6-tert-butylphenol) Chemical compound CC(C)(C)C1=CC(C)=CC(CC=2C(=C(C=C(C)C=2)C(C)(C)C)O)=C1O KGRVJHAUYBGFFP-UHFFFAOYSA-N 0.000 claims description 2
- ZZZCUOFIHGPKAK-UHFFFAOYSA-N D-erythro-ascorbic acid Natural products OCC1OC(=O)C(O)=C1O ZZZCUOFIHGPKAK-UHFFFAOYSA-N 0.000 claims description 2
- 229920002307 Dextran Polymers 0.000 claims description 2
- 108010010803 Gelatin Proteins 0.000 claims description 2
- XUJNEKJLAYXESH-REOHCLBHSA-N L-Cysteine Chemical compound SC[C@H](N)C(O)=O XUJNEKJLAYXESH-REOHCLBHSA-N 0.000 claims description 2
- FFEARJCKVFRZRR-BYPYZUCNSA-N L-methionine Chemical compound CSCC[C@H](N)C(O)=O FFEARJCKVFRZRR-BYPYZUCNSA-N 0.000 claims description 2
- XSQUKJJJFZCRTK-UHFFFAOYSA-N Urea Natural products NC(N)=O XSQUKJJJFZCRTK-UHFFFAOYSA-N 0.000 claims description 2
- 229930003268 Vitamin C Natural products 0.000 claims description 2
- XUJNEKJLAYXESH-UHFFFAOYSA-N cysteine Natural products SCC(N)C(O)=O XUJNEKJLAYXESH-UHFFFAOYSA-N 0.000 claims description 2
- 235000018417 cysteine Nutrition 0.000 claims description 2
- 229920000159 gelatin Polymers 0.000 claims description 2
- 239000008273 gelatin Substances 0.000 claims description 2
- 235000019322 gelatine Nutrition 0.000 claims description 2
- 235000011852 gelatine desserts Nutrition 0.000 claims description 2
- 239000004310 lactic acid Substances 0.000 claims description 2
- 235000014655 lactic acid Nutrition 0.000 claims description 2
- 229930182817 methionine Natural products 0.000 claims description 2
- 235000019154 vitamin C Nutrition 0.000 claims description 2
- 239000011718 vitamin C Substances 0.000 claims description 2
- 238000005303 weighing Methods 0.000 claims description 2
- FBPFZTCFMRRESA-JGWLITMVSA-N D-glucitol Chemical compound OC[C@H](O)[C@@H](O)[C@H](O)[C@H](O)CO FBPFZTCFMRRESA-JGWLITMVSA-N 0.000 claims 1
- 108010009736 Protein Hydrolysates Proteins 0.000 claims 1
- FZWBNHMXJMCXLU-BLAUPYHCSA-N isomaltotriose Chemical compound O[C@@H]1[C@@H](O)[C@H](O)[C@@H](CO)O[C@@H]1OC[C@@H]1[C@@H](O)[C@H](O)[C@@H](O)[C@@H](OC[C@@H](O)[C@@H](O)[C@H](O)[C@@H](O)C=O)O1 FZWBNHMXJMCXLU-BLAUPYHCSA-N 0.000 claims 1
- 238000003756 stirring Methods 0.000 claims 1
- 239000008280 blood Substances 0.000 abstract 1
- 210000004369 blood Anatomy 0.000 abstract 1
- 239000003381 stabilizer Substances 0.000 abstract 1
- WVDDGKGOMKODPV-UHFFFAOYSA-N Benzyl alcohol Chemical compound OCC1=CC=CC=C1 WVDDGKGOMKODPV-UHFFFAOYSA-N 0.000 description 6
- KRKNYBCHXYNGOX-UHFFFAOYSA-N citric acid Chemical compound OC(=O)CC(O)(C(O)=O)CC(O)=O KRKNYBCHXYNGOX-UHFFFAOYSA-N 0.000 description 6
- VMHLLURERBWHNL-UHFFFAOYSA-M Sodium acetate Chemical compound [Na+].CC([O-])=O VMHLLURERBWHNL-UHFFFAOYSA-M 0.000 description 5
- 239000001632 sodium acetate Substances 0.000 description 5
- 235000017281 sodium acetate Nutrition 0.000 description 5
- 206010008190 Cerebrovascular accident Diseases 0.000 description 3
- 235000014489 Cinnamomum aromaticum Nutrition 0.000 description 3
- 206010012289 Dementia Diseases 0.000 description 3
- LFQSCWFLJHTTHZ-UHFFFAOYSA-N Ethanol Chemical compound CCO LFQSCWFLJHTTHZ-UHFFFAOYSA-N 0.000 description 3
- 208000006011 Stroke Diseases 0.000 description 3
- FEWJPZIEWOKRBE-UHFFFAOYSA-N Tartaric acid Natural products [H+].[H+].[O-]C(=O)C(O)C(O)C([O-])=O FEWJPZIEWOKRBE-UHFFFAOYSA-N 0.000 description 3
- 235000001014 amino acid Nutrition 0.000 description 3
- 150000001413 amino acids Chemical class 0.000 description 3
- 230000002490 cerebral effect Effects 0.000 description 3
- 239000011975 tartaric acid Substances 0.000 description 3
- 235000002906 tartaric acid Nutrition 0.000 description 3
- 241000522254 Cassia Species 0.000 description 2
- FEWJPZIEWOKRBE-JCYAYHJZSA-N Dextrotartaric acid Chemical compound OC(=O)[C@H](O)[C@@H](O)C(O)=O FEWJPZIEWOKRBE-JCYAYHJZSA-N 0.000 description 2
- 229940099471 Phosphodiesterase inhibitor Drugs 0.000 description 2
- 230000002378 acidificating effect Effects 0.000 description 2
- 235000019445 benzyl alcohol Nutrition 0.000 description 2
- 201000010099 disease Diseases 0.000 description 2
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 description 2
- 230000000694 effects Effects 0.000 description 2
- 239000012535 impurity Substances 0.000 description 2
- 230000000302 ischemic effect Effects 0.000 description 2
- 239000002571 phosphodiesterase inhibitor Substances 0.000 description 2
- 239000002994 raw material Substances 0.000 description 2
- 244000037364 Cinnamomum aromaticum Species 0.000 description 1
- 241000196324 Embryophyta Species 0.000 description 1
- PIICEJLVQHRZGT-UHFFFAOYSA-N Ethylenediamine Chemical compound NCCN PIICEJLVQHRZGT-UHFFFAOYSA-N 0.000 description 1
- 208000031226 Hyperlipidaemia Diseases 0.000 description 1
- 206010020772 Hypertension Diseases 0.000 description 1
- DGAQECJNVWCQMB-PUAWFVPOSA-M Ilexoside XXIX Chemical compound C[C@@H]1CC[C@@]2(CC[C@@]3(C(=CC[C@H]4[C@]3(CC[C@@H]5[C@@]4(CC[C@@H](C5(C)C)OS(=O)(=O)[O-])C)C)[C@@H]2[C@]1(C)O)C)C(=O)O[C@H]6[C@@H]([C@H]([C@@H]([C@H](O6)CO)O)O)O.[Na+] DGAQECJNVWCQMB-PUAWFVPOSA-M 0.000 description 1
- 241000283973 Oryctolagus cuniculus Species 0.000 description 1
- HCBIBCJNVBAKAB-UHFFFAOYSA-N Procaine hydrochloride Chemical compound Cl.CCN(CC)CCOC(=O)C1=CC=C(N)C=C1 HCBIBCJNVBAKAB-UHFFFAOYSA-N 0.000 description 1
- UIIMBOGNXHQVGW-DEQYMQKBSA-M Sodium bicarbonate-14C Chemical compound [Na+].O[14C]([O-])=O UIIMBOGNXHQVGW-DEQYMQKBSA-M 0.000 description 1
- 201000006559 Vertebrobasilar insufficiency Diseases 0.000 description 1
- 239000002253 acid Substances 0.000 description 1
- 230000001154 acute effect Effects 0.000 description 1
- 239000003708 ampul Substances 0.000 description 1
- 238000003556 assay Methods 0.000 description 1
- 201000010861 basilar artery insufficiency Diseases 0.000 description 1
- 230000037396 body weight Effects 0.000 description 1
- 210000004556 brain Anatomy 0.000 description 1
- 239000003153 chemical reaction reagent Substances 0.000 description 1
- 238000005660 chlorination reaction Methods 0.000 description 1
- 230000001684 chronic effect Effects 0.000 description 1
- 235000015165 citric acid Nutrition 0.000 description 1
- 239000000470 constituent Substances 0.000 description 1
- 208000029078 coronary artery disease Diseases 0.000 description 1
- 230000007812 deficiency Effects 0.000 description 1
- 238000001514 detection method Methods 0.000 description 1
- 206010012601 diabetes mellitus Diseases 0.000 description 1
- 239000002552 dosage form Substances 0.000 description 1
- 230000004153 glucose metabolism Effects 0.000 description 1
- 230000002008 hemorrhagic effect Effects 0.000 description 1
- 239000000413 hydrolysate Substances 0.000 description 1
- 208000014674 injury Diseases 0.000 description 1
- 239000007788 liquid Substances 0.000 description 1
- 238000004811 liquid chromatography Methods 0.000 description 1
- 239000008176 lyophilized powder Substances 0.000 description 1
- 238000004519 manufacturing process Methods 0.000 description 1
- 235000006109 methionine Nutrition 0.000 description 1
- 230000000324 neuroprotective effect Effects 0.000 description 1
- 230000002093 peripheral effect Effects 0.000 description 1
- 230000003285 pharmacodynamic effect Effects 0.000 description 1
- 230000000144 pharmacologic effect Effects 0.000 description 1
- WVDDGKGOMKODPV-ZQBYOMGUSA-N phenyl(114C)methanol Chemical compound O[14CH2]C1=CC=CC=C1 WVDDGKGOMKODPV-ZQBYOMGUSA-N 0.000 description 1
- 239000000843 powder Substances 0.000 description 1
- 229960001309 procaine hydrochloride Drugs 0.000 description 1
- 239000002510 pyrogen Substances 0.000 description 1
- 150000003839 salts Chemical class 0.000 description 1
- 238000012216 screening Methods 0.000 description 1
- 239000011734 sodium Substances 0.000 description 1
- 229910052708 sodium Inorganic materials 0.000 description 1
- 239000000243 solution Substances 0.000 description 1
- 239000000126 substance Substances 0.000 description 1
- 238000001356 surgical procedure Methods 0.000 description 1
- 230000001225 therapeutic effect Effects 0.000 description 1
- 230000008733 trauma Effects 0.000 description 1
- 239000000052 vinegar Substances 0.000 description 1
- 235000021419 vinegar Nutrition 0.000 description 1
Landscapes
- Medicinal Preparation (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
Abstract
The present invention discloses one kind of small volume vincamine injection and its preparation process. The small volume vincamine injection consists of vincamine as main medicine component 3-20 weight portions and supplementary material including co-solvent 0.1-1 weight portions, antioxidant 0.5-10 weight portions, physical stabilizer 50-100 weight portions, and blood stimulation regulator 0.5-10 weight portions. It has high stability, long validity period, high bioavailability, capacity of being used directly and other advantages.
Description
Technical field
The present invention relates to injection that contains vinpocetine and preparation method thereof, particularly the prescription of low capacity vinpocetine injection and preparation technology.
Background technology
Vinpocetine is to extract from the natural plants Herba Catharanthi Rosei, then through chemosynthesis and medicine, it is representative phosphodiesterase inhibitor, fat-soluble strong, be insoluble in water, have selectivity expansion cerebral vessels, initiatively improve pharmacological actions such as glucose metabolism, neuroprotective unit, be used for the treatment of ischemic cerebrovascular, apoplexy sequela, dementia etc., circulatory disturbance ophthalmic and otology disease are also had good therapeutical effect; Vinpocetine also is a kind of good reagent of studying the phosphodiesterase inhibitor effect.
Vinpocetine is succeeded in developing by Hungary Gedeon Richter company at first, and the chemosynthesis process is open, by former expect be prepared into medicine, the oral formulations bioavailability is poor, lyophilized powder needs the secondary dissolving, influences drug level and ease of use, and the probability of secondary pollution is arranged.Need clinically a kind of easy to use, can preserve the dosage form of long period again.
Summary of the invention
With regard to above technological deficiency, the invention provides a kind of small volume vincamine injection (ampoule) and preparation technology thereof.
Small volume vincamine injection of the present invention is by as the vinpocetine of pharmacodynamic raw materials with form as cosolvent, antioxidant, physically stable agent and the vascular stimulation regulator of adjuvant.
Wherein, vinpocetine is the vinpocetine that meets the national drug standards;
Cosolvent adopts conventional medicinal cosolvent, one or more in preferred acetic acid, lactic acid, the ascorbic acid;
In the antioxidant, conventional medicinal antioxidant such as sodium sulfite, sodium pyrosulfite, sodium sulfite, sodium thiosulfate, thiourea, cysteine, methionine, vitamin C all can use, and preferably adopt sodium sulfite, in the sodium pyrosulfite, sodium sulfite, sodium thiosulfate one or more;
In the preferred mannitol of physically stable agent, dextran, sorbitol, the gelatin hydrolysate one or more;
One or more of the preferred procaine hydrochloride of vascular stimulation regulator, benzyl alcohol, cassia oil alcohol.
The inventor adopts conventional screening technique that the use amount of principal agent and adjuvant is studied, determine the compositions of small volume vincamine injection of the present invention, it forms by weight, and ratio is, vinpocetine 3～20, cosolvent 0.1～1, antioxidant 0.5～10, physically stable agent 50～100, vascular stimulation regulator 0.5～10.
Further optimize composition weight portion ratio and be vinpocetine 5～10, cosolvent 0.3～0.8, antioxidant 1～5, physically stable agent 40～85, vascular stimulation regulator 1～5.
Small volume vincamine injection of the present invention can prepare with conventional production technology, but the preferred following preparation technology of the present invention.
Press accurate weighing vinpocetine of formulation ratio and cosolvent, antioxidant, physically stable agent, vascular stimulation regulator, and be equipped with pH value regulator, medicinal charcoal and water for injection.The water for injection that in preparing tank, adds 2/3 amount of preparation, getting load weighted cosolvent and vinpocetine adds in the preparing tank successively, vinpocetine is dissolved fully, add load weighted antioxidant, physically stable agent and regulation of blood vessels stimulant more successively, and make it to dissolve fully, the nearly full dose of water is penetrated in after-teeming, regulate pH value to 2.8～3.6, stirred about 30 minutes the cooling back, adds medicinal charcoal absorption 15～20 minutes, the amount of used medicinal charcoal is about 0.03%, filters canned the getting product in back.
Wherein, be used to regulate the acid of pH value pH value regulator acceptable salts vinegar, citric acid, tartaric acid, acidic amino acid, sodium bicarbonate, sodium acetate, ethylenediamine, basic amino acid etc., and in the preferably citric acid, tartaric acid, acidic amino acid, sodium acetate one or more.
According to clinical needs, small volume vincamine injection of the present invention can be made the product of different size, as 5mg/ prop up, 10mg/ props up, 20mg/ props up, 30mg/ props up etc., preferred specification is that 10mg/ props up.
Small volume vincamine injection of the present invention is when producing in batches, and finished product can reach following technical standard:
Contain vinpocetine (C
22H
26N
2O
2) be the 98%-107% of labelled amount, be colourless clear liquid;
PH value is 2.8～3.6;
Its related substances: main constituent chromatograph peak height is 60%～80% of a full scale, and single impurity peak area is not more than 0.8% of total peak area, each impurity peaks peak area and be not more than 1.5% of total peak area;
Assay: according to high effective liquid chromatography for measuring, the detection wavelength is 273nm, and number of theoretical plate calculates by the vinpocetine peak and is not less than 2500;
Aseptic: as after the membrane-filter procedure processing, to meet " Chinese pharmacopoeia (two appendix XIH of version in 2000) regulation;
Pyrogen: add the solution that the chlorination sodium injection contains 0.5mg in making every milliliter, dosage is slowly injected 10ml by rabbit body weight per kilogram, meets " Chinese pharmacopoeia (two appendix XID of version in 2000) regulation.
Small volume vincamine injection of the present invention can be used for treating acute and chronic ischemic cerebrovascular, apoplexy sequela, hemorrhagic apoplexy convalescent period, cerebral trauma sequela, cerebral surgery operation sequela, vertebro-basilar artery insufficiency, vascular brain dementia, dementia polysclerotica, coronary heart disease, diabetes, hypertension, hyperlipidemia clinically, and disease such as the ophthalmology that is caused by circulatory disturbance, otology, peripheral vessels obstacle.
Small volume vincamine injection good stability of the present invention, effect duration is long, preserves after 4 years according to the above-mentioned technical standard still conformance with standard of testing.Compare advantage such as have the bioavailability height, can directly use with tablet, lyophilized injectable powder.
The specific embodiment
The present invention is further elaborated by following examples, but the present invention is not limited to this.
Embodiment 1～4 selects raw material variety and quantity for use
| Embodiment 1 | Embodiment 2 | Embodiment 3 | Embodiment 4 | |
| Principal agent | Vinpocetine 10g | Vinpocetine 10g | Vinpocetine 10g | Vinpocetine 10g |
| Cosolvent | Acetic acid 1g | Ascorbic acid 1g | Ascorbic acid 1g | Ascorbic acid 1g |
| Antioxidant | Sodium sulfite 2g | Sodium sulfite 2g | Sodium pyrosulfite 2g | Sodium pyrosulfite 2g |
| The physically stable agent | Mannitol 100g | Sorbitol 100g | Mannitol 100g | Sorbitol 100g |
| The regulation of blood vessels stimulant | Benzyl alcohol 20g | Cassia oil alcohol 20g | Cassia oil alcohol 20g | Benzyl alcohol 20g |
| The pH value regulator | Sodium acetate is an amount of | Sodium acetate is an amount of | Sodium acetate is an amount of | Tartaric acid is an amount of |
| Medicinal charcoal | In right amount | In right amount | In right amount | In right amount |
| Water for injection | 2000ml | 2000ml | 2000ml | 2000ml |
The water for injection that in preparing tank, adds 2/3 amount of preparation, getting load weighted cosolvent and vinpocetine adds in the preparing tank successively, vinpocetine is dissolved fully, add load weighted antioxidant, physically stable agent and regulation of blood vessels stimulant more successively and make it to dissolve fully, the nearly full dose of water is penetrated in after-teeming, regulates pH value to 2.8～3.6 with the pH value regulator, and stirred 30 minutes the cooling back, canned the getting product in back filtered in the medicinal charcoal absorption of adding 0.03% 15～20 minutes.
Claims (7)
1. drug injection that contains vinpocetine, it is characterized in that, it is made up of vinpocetine and cosolvent, antioxidant, physically stable agent, vascular stimulation regulator, the composition of principal agent and each adjuvant ratio by weight is vinpocetine 3～20, cosolvent 0.1～1, antioxidant 0.5～10, physically stable agent 50～100, vascular stimulation regulator 0.5～10.
2. drug injection according to claim 1, it is characterized in that, the composition of principal agent and each adjuvant ratio by weight is vinpocetine 5～10 weight portions, cosolvent 0.3～0.8, antioxidant 1～5, physically stable agent 40～85, vascular stimulation regulator 1～5.
3. drug injection according to claim 1 and 2 is characterized in that, described cosolvent is any in acetic acid, lactic acid, the ascorbic acid, or any combination is used simultaneously.
4. drug injection according to claim 1 and 2, it is characterized in that, described antioxidant is any in sodium sulfite, sodium pyrosulfite, sodium sulfite, sodium thiosulfate, thiourea, cysteine, methionine, the vitamin C, or any combination is used simultaneously.
5. drug injection according to claim 1 and 2 is characterized in that, described physically stable agent is any in mannitol, dextran, sorbitol, the gelatin hydrolysate, or any combination is used simultaneously.
6. drug injection according to claim 1 and 2 is characterized in that, the preparation specification is that 5mg/ props up, 10mg/ props up, 20mg/ props up, 30mg/ any in propping up.
7. the preparation method of claim 1 or 2 described drug injections is characterized in that, takes by weighing vinpocetine and cosolvent, antioxidant, physically stable agent, vascular stimulation regulator by formulation ratio, and is equipped with pH value regulator, medicinal charcoal and water for injection; The water for injection that in preparing tank, adds 2/3 amount of preparation, add cosolvent and vinpocetine in the preparing tank successively, vinpocetine is dissolved fully, add antioxidant, physically stable agent and regulation of blood vessels stimulant more successively, and make it to dissolve fully, the nearly full dose of water is penetrated in after-teeming, regulate pH value to 2.8～3.6, stir the cooling back, adds medicinal charcoal absorption 15～20 minutes, filters canned the getting product in back.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CNB2006101525144A CN100522163C (en) | 2006-09-28 | 2006-09-28 | Small volume vincamine injection and its preparation process |
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CNB2006101525144A CN100522163C (en) | 2006-09-28 | 2006-09-28 | Small volume vincamine injection and its preparation process |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| CN101066244A true CN101066244A (en) | 2007-11-07 |
| CN100522163C CN100522163C (en) | 2009-08-05 |
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| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CNB2006101525144A Active CN100522163C (en) | 2006-09-28 | 2006-09-28 | Small volume vincamine injection and its preparation process |
Country Status (1)
| Country | Link |
|---|---|
| CN (1) | CN100522163C (en) |
Cited By (14)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN101889978A (en) * | 2010-04-29 | 2010-11-24 | 袁璐 | Pharmaceutical composition containing vinpocetine, preparation method and application thereof |
| CN101264064B (en) * | 2008-04-17 | 2011-04-20 | 孙向阳 | Vinpocetine freeze-dried powder for injection and preparation thereof |
| CN102160853A (en) * | 2011-02-11 | 2011-08-24 | 方宝林 | Vinpocetine injection and preparation method thereof |
| CN102228428A (en) * | 2011-06-30 | 2011-11-02 | 武汉同源药业有限公司 | Large volume injection composition containing vinpocetine and preparation method thereof |
| CN102327210A (en) * | 2011-07-14 | 2012-01-25 | 海南灵康制药有限公司 | Vinpocetine suspension injection |
| CN102423295A (en) * | 2011-06-30 | 2012-04-25 | 武汉同源药业有限公司 | Small volume injection composition containing vinpocetine and preparation method thereof |
| CN101874776B (en) * | 2009-04-28 | 2012-06-13 | 中国人民解放军军事医学科学院毒物药物研究所 | Dry emulsion of vinpocetine and preparation method thereof |
| CN102716066A (en) * | 2011-11-14 | 2012-10-10 | 河南润弘制药股份有限公司 | Vinpocetine injection and preparation method thereof |
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| CN102716066A (en) * | 2011-11-14 | 2012-10-10 | 河南润弘制药股份有限公司 | Vinpocetine injection and preparation method thereof |
| CN105878178A (en) * | 2014-10-16 | 2016-08-24 | 山西国润制药有限公司 | Vinpocetine injection and preparation method thereof |
| CN110179745A (en) * | 2018-07-16 | 2019-08-30 | 北京海浈医药科技有限公司 | A kind of Vinpocetine injection and preparation method thereof |
| CN110179745B (en) * | 2018-07-16 | 2021-09-10 | 北京海浈医药科技有限公司 | Vinpocetine injection and preparation method thereof |
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