CN1875981A - Injection emulsion containing breviscapinum and preparation method thereof - Google Patents
Injection emulsion containing breviscapinum and preparation method thereof Download PDFInfo
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- CN1875981A CN1875981A CN 200610012641 CN200610012641A CN1875981A CN 1875981 A CN1875981 A CN 1875981A CN 200610012641 CN200610012641 CN 200610012641 CN 200610012641 A CN200610012641 A CN 200610012641A CN 1875981 A CN1875981 A CN 1875981A
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- breviscapine
- oil
- emulsion
- injection
- agent
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- 239000000839 emulsion Substances 0.000 title claims abstract description 40
- 238000002347 injection Methods 0.000 title claims abstract description 17
- 239000007924 injection Substances 0.000 title claims abstract description 17
- 238000002360 preparation method Methods 0.000 title claims abstract description 12
- DJSISFGPUUYILV-UHFFFAOYSA-N UNPD161792 Natural products O1C(C(O)=O)C(O)C(O)C(O)C1OC(C(=C1O)O)=CC2=C1C(=O)C=C(C=1C=CC(O)=CC=1)O2 DJSISFGPUUYILV-UHFFFAOYSA-N 0.000 claims abstract description 48
- DJSISFGPUUYILV-ZFORQUDYSA-N scutellarin Chemical compound O1[C@H](C(O)=O)[C@@H](O)[C@H](O)[C@@H](O)[C@@H]1OC(C(=C1O)O)=CC2=C1C(=O)C=C(C=1C=CC(O)=CC=1)O2 DJSISFGPUUYILV-ZFORQUDYSA-N 0.000 claims abstract description 48
- 239000000203 mixture Substances 0.000 claims abstract description 16
- 239000003995 emulsifying agent Substances 0.000 claims abstract description 12
- 239000007951 isotonicity adjuster Substances 0.000 claims abstract description 12
- 239000003381 stabilizer Substances 0.000 claims abstract description 12
- XLYOFNOQVPJJNP-UHFFFAOYSA-N water Chemical compound O XLYOFNOQVPJJNP-UHFFFAOYSA-N 0.000 claims abstract description 10
- 239000008215 water for injection Substances 0.000 claims abstract description 10
- 230000001804 emulsifying effect Effects 0.000 claims abstract description 4
- 230000001954 sterilising effect Effects 0.000 claims abstract description 4
- 239000003921 oil Substances 0.000 claims description 23
- 235000019198 oils Nutrition 0.000 claims description 23
- 239000000546 pharmaceutical excipient Substances 0.000 claims description 12
- 210000003022 colostrum Anatomy 0.000 claims description 9
- 235000021277 colostrum Nutrition 0.000 claims description 9
- PEDCQBHIVMGVHV-UHFFFAOYSA-N glycerol group Chemical group OCC(O)CO PEDCQBHIVMGVHV-UHFFFAOYSA-N 0.000 claims description 9
- 238000003756 stirring Methods 0.000 claims description 9
- 238000005303 weighing Methods 0.000 claims description 9
- 238000004945 emulsification Methods 0.000 claims description 8
- WRIDQFICGBMAFQ-UHFFFAOYSA-N (E)-8-Octadecenoic acid Natural products CCCCCCCCCC=CCCCCCCC(O)=O WRIDQFICGBMAFQ-UHFFFAOYSA-N 0.000 claims description 6
- LQJBNNIYVWPHFW-UHFFFAOYSA-N 20:1omega9c fatty acid Natural products CCCCCCCCCCC=CCCCCCCCC(O)=O LQJBNNIYVWPHFW-UHFFFAOYSA-N 0.000 claims description 6
- QSBYPNXLFMSGKH-UHFFFAOYSA-N 9-Heptadecensaeure Natural products CCCCCCCC=CCCCCCCCC(O)=O QSBYPNXLFMSGKH-UHFFFAOYSA-N 0.000 claims description 6
- OYHQOLUKZRVURQ-HZJYTTRNSA-N Linoleic acid Chemical compound CCCCC\C=C/C\C=C/CCCCCCCC(O)=O OYHQOLUKZRVURQ-HZJYTTRNSA-N 0.000 claims description 6
- 239000005642 Oleic acid Substances 0.000 claims description 6
- ZQPPMHVWECSIRJ-UHFFFAOYSA-N Oleic acid Natural products CCCCCCCCC=CCCCCCCCC(O)=O ZQPPMHVWECSIRJ-UHFFFAOYSA-N 0.000 claims description 6
- UIIMBOGNXHQVGW-UHFFFAOYSA-M Sodium bicarbonate Chemical group [Na+].OC([O-])=O UIIMBOGNXHQVGW-UHFFFAOYSA-M 0.000 claims description 6
- 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 claims description 6
- QXJSBBXBKPUZAA-UHFFFAOYSA-N isooleic acid Natural products CCCCCCCC=CCCCCCCCCC(O)=O QXJSBBXBKPUZAA-UHFFFAOYSA-N 0.000 claims description 6
- OYHQOLUKZRVURQ-IXWMQOLASA-N linoleic acid Natural products CCCCC\C=C/C\C=C\CCCCCCCC(O)=O OYHQOLUKZRVURQ-IXWMQOLASA-N 0.000 claims description 6
- 235000020778 linoleic acid Nutrition 0.000 claims description 6
- ZQPPMHVWECSIRJ-KTKRTIGZSA-N oleic acid Chemical compound CCCCCCCC\C=C/CCCCCCCC(O)=O ZQPPMHVWECSIRJ-KTKRTIGZSA-N 0.000 claims description 6
- -1 polyoxy Chemical class 0.000 claims description 6
- 210000000582 semen Anatomy 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 5
- 241001013934 Erigeron breviscapus Species 0.000 claims description 4
- HDTRYLNUVZCQOY-UHFFFAOYSA-N α-D-glucopyranosyl-α-D-glucopyranoside Natural products OC1C(O)C(O)C(CO)OC1OC1C(O)C(O)C(O)C(CO)O1 HDTRYLNUVZCQOY-UHFFFAOYSA-N 0.000 claims description 3
- JQWAHKMIYCERGA-UHFFFAOYSA-N (2-nonanoyloxy-3-octadeca-9,12-dienoyloxypropoxy)-[2-(trimethylazaniumyl)ethyl]phosphinate Chemical compound CCCCCCCCC(=O)OC(COP([O-])(=O)CC[N+](C)(C)C)COC(=O)CCCCCCCC=CCC=CCCCCC JQWAHKMIYCERGA-UHFFFAOYSA-N 0.000 claims description 3
- JLPULHDHAOZNQI-ZTIMHPMXSA-N 1-hexadecanoyl-2-(9Z,12Z-octadecadienoyl)-sn-glycero-3-phosphocholine Chemical compound CCCCCCCCCCCCCCCC(=O)OC[C@H](COP([O-])(=O)OCC[N+](C)(C)C)OC(=O)CCCCCCC\C=C/C\C=C/CCCCC JLPULHDHAOZNQI-ZTIMHPMXSA-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 3
- 235000003276 Apios tuberosa Nutrition 0.000 claims description 3
- 244000105624 Arachis hypogaea Species 0.000 claims description 3
- 235000010777 Arachis hypogaea Nutrition 0.000 claims description 3
- 235000010744 Arachis villosulicarpa Nutrition 0.000 claims description 3
- 235000008495 Chrysanthemum leucanthemum Nutrition 0.000 claims description 3
- 244000192528 Chrysanthemum parthenium Species 0.000 claims description 3
- 235000000604 Chrysanthemum parthenium Nutrition 0.000 claims description 3
- 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 3
- 229920002307 Dextran Polymers 0.000 claims description 3
- LFQSCWFLJHTTHZ-UHFFFAOYSA-N Ethanol Chemical compound CCO LFQSCWFLJHTTHZ-UHFFFAOYSA-N 0.000 claims description 3
- 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 3
- 229930195725 Mannitol Natural products 0.000 claims description 3
- 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 3
- 229930006000 Sucrose Natural products 0.000 claims description 3
- HDTRYLNUVZCQOY-WSWWMNSNSA-N Trehalose Natural products O[C@@H]1[C@@H](O)[C@@H](O)[C@@H](CO)O[C@@H]1O[C@@H]1[C@H](O)[C@@H](O)[C@@H](O)[C@@H](CO)O1 HDTRYLNUVZCQOY-WSWWMNSNSA-N 0.000 claims description 3
- HDTRYLNUVZCQOY-LIZSDCNHSA-N alpha,alpha-trehalose Chemical compound O[C@@H]1[C@@H](O)[C@H](O)[C@@H](CO)O[C@@H]1O[C@@H]1[C@H](O)[C@@H](O)[C@H](O)[C@@H](CO)O1 HDTRYLNUVZCQOY-LIZSDCNHSA-N 0.000 claims description 3
- 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
- 235000012000 cholesterol Nutrition 0.000 claims description 3
- 235000008384 feverfew Nutrition 0.000 claims description 3
- 235000021323 fish oil Nutrition 0.000 claims description 3
- 229930003935 flavonoid Natural products 0.000 claims description 3
- 150000002215 flavonoids Chemical class 0.000 claims description 3
- 235000017173 flavonoids Nutrition 0.000 claims description 3
- 238000004108 freeze drying Methods 0.000 claims description 3
- 239000008103 glucose Substances 0.000 claims description 3
- 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 description 3
- 239000008101 lactose Substances 0.000 claims description 3
- 239000000594 mannitol Substances 0.000 claims description 3
- 235000010355 mannitol Nutrition 0.000 claims description 3
- 235000021313 oleic acid Nutrition 0.000 claims description 3
- 150000003904 phospholipids Chemical class 0.000 claims description 3
- 229920000642 polymer Polymers 0.000 claims description 3
- 229920001451 polypropylene glycol Polymers 0.000 claims description 3
- 235000005713 safflower oil Nutrition 0.000 claims description 3
- 239000003813 safflower oil Substances 0.000 claims description 3
- 229910000030 sodium bicarbonate Inorganic materials 0.000 claims description 3
- 235000017557 sodium bicarbonate Nutrition 0.000 claims description 3
- 235000012424 soybean oil Nutrition 0.000 claims description 3
- 239000003549 soybean oil Substances 0.000 claims description 3
- 239000008347 soybean phospholipid Substances 0.000 claims description 3
- 238000004659 sterilization and disinfection Methods 0.000 claims description 3
- 239000000126 substance Substances 0.000 claims description 3
- 239000005720 sucrose Substances 0.000 claims description 3
- 238000000034 method Methods 0.000 abstract 1
- 239000008267 milk Substances 0.000 abstract 1
- 210000004080 milk Anatomy 0.000 abstract 1
- 235000013336 milk Nutrition 0.000 abstract 1
- 239000002994 raw material Substances 0.000 abstract 1
- 229940090044 injection Drugs 0.000 description 10
- FAPWRFPIFSIZLT-UHFFFAOYSA-M Sodium chloride Chemical compound [Na+].[Cl-] FAPWRFPIFSIZLT-UHFFFAOYSA-M 0.000 description 3
- 239000008280 blood Substances 0.000 description 3
- 210000004369 blood Anatomy 0.000 description 3
- 239000003146 anticoagulant agent Substances 0.000 description 2
- 208000026106 cerebrovascular disease Diseases 0.000 description 2
- 230000000694 effects Effects 0.000 description 2
- 229940093181 glucose injection Drugs 0.000 description 2
- 239000000243 solution Substances 0.000 description 2
- 208000024172 Cardiovascular disease Diseases 0.000 description 1
- 241000196324 Embryophyta Species 0.000 description 1
- 239000003708 ampul Substances 0.000 description 1
- 229940127219 anticoagulant drug Drugs 0.000 description 1
- 230000009286 beneficial effect Effects 0.000 description 1
- 230000000740 bleeding effect Effects 0.000 description 1
- 230000036770 blood supply Effects 0.000 description 1
- 230000000747 cardiac effect Effects 0.000 description 1
- NPLTVGMLNDMOQE-UHFFFAOYSA-N carthamidin Natural products C1=CC(O)=CC=C1C1OC2=CC(O)=C(O)C(O)=C2C(=O)C1 NPLTVGMLNDMOQE-UHFFFAOYSA-N 0.000 description 1
- 230000002490 cerebral effect Effects 0.000 description 1
- 239000003814 drug Substances 0.000 description 1
- 230000002526 effect on cardiovascular system Effects 0.000 description 1
- 239000000284 extract Substances 0.000 description 1
- 235000019197 fats Nutrition 0.000 description 1
- 230000006870 function Effects 0.000 description 1
- 238000001802 infusion Methods 0.000 description 1
- 230000000302 ischemic effect Effects 0.000 description 1
- 239000002075 main ingredient Substances 0.000 description 1
- 238000004519 manufacturing process Methods 0.000 description 1
- 230000004089 microcirculation Effects 0.000 description 1
- 230000010016 myocardial function Effects 0.000 description 1
- 229930190376 scutellarin Natural products 0.000 description 1
- 238000003860 storage Methods 0.000 description 1
- 230000002537 thrombolytic effect Effects 0.000 description 1
Landscapes
- Medicinal Preparation (AREA)
Abstract
The invention relates to an emulsion injection containing Breviscapine and its preparing process, which is prepared from the following raw materials (by weight portion): Breviscapine 0.01-0.04%, oil for injection 5-30%, emulsifying agent 1-5%, isotonic agent 2-10%, stabilizer 0.1-8% and balancing water for injection. The preparation process comprises the steps of proportioning, making oily phase mixture, making initial milk, emulsifying and sterilizing.
Description
Technical field
The present invention relates to a kind of medicine that is used to prevent and treat ischemic and bleeding type cerebrovascular sequelae, treatment cardiovascular and cerebrovascular disease, is the injectable emulsion that contains breviscapine specifically; The invention still further relates to the production method of the injectable emulsion that contains breviscapine.
Technical background
Breviscapine is the total flavonoids substance that extracts from feverfew Erigeron breviscapus (Vant.) Hand.-Mazz. [Erigeron breviscapus (Vant.) Hand-Mazz] plant, its 90% above content is lamp-dish flower acetic, has expansion blood capillary, microcirculation improvement, raising myocardial function and cardiac and cerebral blood-supply, reduction blood viscosity, anticoagulant, anti-bolt and functions such as thrombolytic, blood fat reducing.At present, the clinical practice of breviscapine mainly is a small-volume injection, but the breviscapine poor effect of low dosage is found in clinical practice, has only heavy dose of just produce effects of using.Pour into after clinical practice need be cut many little pins and carry out quiet in normal saline or the glucose injection, troublesome poeration not only, and cause secondary pollution easilier.In addition, the breviscapine freeze-dry preparation that has gone on the market, though aspect stable, bigger improvement is arranged, but its working condition requires high, and it is more inconvenient to use, and needs during clinical use that ampoule bottle is cut the back and injects water for injection or normal saline and shake and add normal saline again after molten or glucose injection carries out infusion.
Breviscapine Main Ingredients and Appearance scutellarin instability, apt to deteriorate in the storage, the Breviscapini injection that uses clinically all exists such problem at present, therefore is badly in need of solving the stability problem of breviscapine.
Summary of the invention
The present invention wants the technical solution problem to provide a kind of stability problem that can solve breviscapine, and can improve breviscapine bioavailability contain breviscapine injectable emulsion and preparation method thereof.
The technical solution adopted for the present invention to solve the technical problems:
One, the injectable emulsion that contains breviscapine:
The present invention is the Emulsion of being made by following weight percentages:
Breviscapine: 0.01%-0.04%
Oil for injection: 5%-30%
Emulsifying agent: 1%-5%
Transfer isotonic agent: 2%-10%
Stabilizing agent: 0.1%-8%
Water for injection: surplus
It also adds the lyophilizing excipient and makes freeze-dried emulsion, and the addition of lyophilizing excipient is 0.2-0.4 a times of Emulsion; The lyophilizing excipient is selected from any in dextran, mannitol, glucose, lactose, sucrose, the trehalose.
The total flavonoids substance of described breviscapine for from the feverfew Erigeron breviscapus (Vant.) Hand.-Mazz., extracting.
Described oil for injection is selected from any in soybean oil, Oleum Gossypii semen, Semen Maydis oil, oleic acid, fish oil, Fructus Schisandrae oil, safflower oil, hydrogenated groundnut, the linoleic acid.
Described emulsifying agent be selected from soybean phospholipid, egg yolk lecithin, hydrogenated phospholipid, polyoxy second rare-in the polyoxypropylene block polymer any.
Described accent isotonic agent is a glycerol.
Described stabilizing agent is selected from any in cholesterol, long even alcohol, oleic acid, the linoleic acid or derivatives thereof.
Two, it is as follows to contain the preparation method step of injectable emulsion of breviscapine:
(1) take by weighing following weight percentages:
Breviscapine: 0.01%-0.04%
Oil for injection: 5%-30%
Emulsifying agent: 1%-5%
Transfer isotonic agent: 2%-10%
Stabilizing agent: 0.1%-8%
Water for injection: surplus
(2) produce oil mixture: the emulsifying agent and the stabilizing agent that take by weighing are joined in the oil for injection, are heated to 60-90 ℃, be mixed into clear and bright, oil mixture;
(3) produce colostrum: with the breviscapine that takes by weighing, transfer isotonic agent to join in the water for injection, stir and make its suspendible, when the limit adds PH regulator limit and is stirred to PH7-7.5 again till, be heated to 60-90 ℃, stir and make the breviscapine dissolving and become aqueous mixture; Under stirring condition, oil mixture is added drop-wise in the aqueous mixture, make colostrum;
(4) with the further emulsifying of high pressure dispersing emulsification machine of above-mentioned colostrum, dispersing emulsification machine pressure is 100Mpa;
(5) then in 115 ℃ of sterilizations 30 minutes, promptly get the injectable emulsion that contains breviscapine.
Described PH regulator is a sodium bicarbonate.
Add the lyophilizing excipient in the above-mentioned injectable emulsion of making, its addition is 0.2-4 a times of Emulsion, removes the freeze-dried emulsion that moisture must contain breviscapine through lyophilization.
The invention has the beneficial effects as follows to have overcome in the prior art unstability that the injection with the breviscapine preparation exists, the drawback of clinical practice inconvenience also can improve the bioavailability of breviscapine, place stable, epigranular.Preparation method is easy, reasonable; Be used to prevent and treat cerebrovascular disease, have uniqueness.
The specific embodiment
One, the embodiment (seeing Table 1) that contains the injectable emulsion of breviscapine:
Table 1:
Annotate: the unit that (1) goes up proportioning in the table is weight percentage.
(2) consumption of lyophilizing excipient be Emulsion 0.2-0.4 doubly, the amount of lyophilizing excipient is respectively 0.2 times, 0.3 times, 0.4 times of Emulsion among the embodiment 4,5,6.
(3) the lyophilizing excipient is selected from any in dextran, mannitol, glucose, lactose, sucrose, the trehalose.
(4) oil for injection is selected from any in soybean oil, Oleum Gossypii semen, Semen Maydis oil, oleic acid, fish oil, Fructus Schisandrae oil, safflower oil, hydrogenated groundnut, the linoleic acid.
(5) emulsifying agent be selected from soybean phospholipid, egg yolk lecithin, hydrogenated phospholipid, polyoxy second rare-in the polyoxypropylene block polymer any.
(6) transferring isotonic agent is glycerol.
(7) stabilizing agent is selected from any in cholesterol, long even alcohol, oleic acid, the linoleic acid or derivatives thereof.
(8) embodiment 1-3 is an injectable emulsion, and embodiment 4-6 is a freeze-dried emulsion.
Two, it is as follows to contain the preparation method step of injectable emulsion of breviscapine:
(1) take by weighing following weight percentages:
Breviscapine: 0.01%-0.04%
Oil for injection: 5%-30%
Emulsifying agent: 1%-5%
Transfer isotonic agent: 2%-10%
Stabilizing agent: 0.1%-8%
Water for injection: surplus
(2) produce oil mixture: the emulsifying agent and the stabilizing agent that take by weighing are joined in the oil for injection, are heated to 60-90 ℃, be mixed into clear and bright, oil mixture;
(3) produce colostrum: with the breviscapine that takes by weighing, transfer isotonic agent to join in the water for injection, stir and make its suspendible, when the limit adds PH regulator limit and is stirred to PH7-7.5 again till, be heated to 60-90 ℃, stir and make the breviscapine dissolving and become aqueous mixture; Under stirring condition, oil mixture is added drop-wise in the aqueous mixture, make colostrum;
(4) with the further emulsifying of high pressure dispersing emulsification machine of above-mentioned colostrum, dispersing emulsification machine pressure is 100Mpa;
(5) then in 115 ℃ of sterilizations 30 minutes, promptly get the injectable emulsion that contains breviscapine.
Described PH regulator is a sodium bicarbonate.
Add the lyophilizing excipient in the above-mentioned injectable emulsion of making, its addition is 0.2-4 a times of Emulsion, removes the freeze-dried emulsion that moisture must contain breviscapine through lyophilization.
Claims (10)
1, a kind of injectable emulsion that contains breviscapine is characterized in that it is the Emulsion of being made by following weight percentages:
Breviscapine: 0.01%-0.04%
Oil for injection: 5%-30%
Emulsifying agent: 1%-5%
Transfer isotonic agent: 2%-10%
Stabilizing agent: 0.1%-8%
Water for injection: surplus.
2, the injectable emulsion that contains breviscapine according to claim 1 is characterized in that it also adds the lyophilizing excipient and makes freeze-dried emulsion, and the addition of lyophilizing excipient is 0.2-0.4 a times of Emulsion; The lyophilizing excipient is selected from any in dextran, mannitol, glucose, lactose, sucrose, the trehalose.
3, the injectable emulsion that contains breviscapine according to claim 2 is characterized in that the total flavonoids substance of described breviscapine for extracting from the feverfew Erigeron breviscapus (Vant.) Hand.-Mazz..
4, the injectable emulsion that contains breviscapine according to claim 3 is characterized in that described oil for injection is selected from any in soybean oil, Oleum Gossypii semen, Semen Maydis oil, oleic acid, fish oil, Fructus Schisandrae oil, safflower oil, hydrogenated groundnut, the linoleic acid.
5, the injectable emulsion that contains breviscapine according to claim 4, it is characterized in that described emulsifying agent be selected from soybean phospholipid, egg yolk lecithin, hydrogenated phospholipid, polyoxy second rare-in the polyoxypropylene block polymer any.
6, the injectable emulsion that contains breviscapine according to claim 5 is characterized in that described accent isotonic agent is a glycerol.
7, the injectable emulsion that contains breviscapine according to claim 6 is characterized in that described stabilizing agent is selected from any in cholesterol, long even alcohol, oleic acid, the linoleic acid or derivatives thereof.
8, a kind of claim 1,2 or 9 described preparation methoies that contain the injectable emulsion of breviscapine made is characterized in that:
(1) take by weighing following weight percentages:
Breviscapine: 0.01%-0.04%
Oil for injection: 5%-30%
Emulsifying agent: 1%-5%
Transfer isotonic agent: 2%-10%
Water for injection: surplus
Stabilizing agent: 0.1%-8%
(2) produce oil mixture: the emulsifying agent and the stabilizing agent that take by weighing are joined in the oil for injection, are heated to 60-90 ℃, be mixed into clear and bright, oil mixture;
(3) produce colostrum: with the breviscapine that takes by weighing, transfer isotonic agent to join in the water for injection, stir and make its suspendible, when the limit adds PH regulator limit and is stirred to PH7-7.5 again till, be heated to 60-90 ℃, stir and make the breviscapine dissolving and become aqueous mixture; Under stirring condition, oil mixture is added drop-wise in the aqueous mixture, make colostrum;
(4) with the further emulsifying of high pressure dispersing emulsification machine of above-mentioned colostrum, dispersing emulsification machine pressure is 100Mpa;
(5) then in 115 ℃ of sterilizations 30 minutes, promptly get the injectable emulsion that contains breviscapine.
9, preparation method according to claim 8 is characterized in that described PH regulator is a sodium bicarbonate.
10, preparation method according to claim 9 is characterized in that adding the lyophilizing excipient in the above-mentioned injectable emulsion of making, its addition is 0.2-4 a times of Emulsion, removes the freeze-dried emulsion that moisture must contain breviscapine through lyophilization.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN2006100126414A CN1875981B (en) | 2006-04-27 | 2006-04-27 | Injection emulsion containing breviscapinum and preparation method thereof |
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| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN2006100126414A CN1875981B (en) | 2006-04-27 | 2006-04-27 | Injection emulsion containing breviscapinum and preparation method thereof |
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| Publication Number | Publication Date |
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| CN1875981A true CN1875981A (en) | 2006-12-13 |
| CN1875981B CN1875981B (en) | 2010-08-11 |
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Cited By (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN102614240A (en) * | 2012-04-26 | 2012-08-01 | 王祥红 | Extract containing breviscapine and preparation method thereof |
| CN106236710A (en) * | 2016-08-29 | 2016-12-21 | 上海颂露医药科技有限公司 | Breviscapini injection and preparation method thereof |
| CN106344512A (en) * | 2016-10-10 | 2017-01-25 | 上海辰松新材料科技有限公司 | Breviscapine injection |
Family Cites Families (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN1634058A (en) * | 2004-10-20 | 2005-07-06 | 李晓祥 | Vinorelbine emulsion and its preparing method |
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2006
- 2006-04-27 CN CN2006100126414A patent/CN1875981B/en not_active Expired - Fee Related
Cited By (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN102614240A (en) * | 2012-04-26 | 2012-08-01 | 王祥红 | Extract containing breviscapine and preparation method thereof |
| CN106236710A (en) * | 2016-08-29 | 2016-12-21 | 上海颂露医药科技有限公司 | Breviscapini injection and preparation method thereof |
| CN106344512A (en) * | 2016-10-10 | 2017-01-25 | 上海辰松新材料科技有限公司 | Breviscapine injection |
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