CN1679580A - Ganciclovir injection and preparation thereof - Google Patents
Ganciclovir injection and preparation thereof Download PDFInfo
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- CN1679580A CN1679580A CN 200510005177 CN200510005177A CN1679580A CN 1679580 A CN1679580 A CN 1679580A CN 200510005177 CN200510005177 CN 200510005177 CN 200510005177 A CN200510005177 A CN 200510005177A CN 1679580 A CN1679580 A CN 1679580A
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- ganciclovir
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Abstract
An injection of ganciclovir and its preparing process are disclosed.
Description
Technical field
The invention belongs to medical technical field, the present invention relates generally to the ganciclovir injection its preparation method.
Background technology
Ganciclovir is the deoxyguanosine analog.Chinese Pharmacopoeia Commission compiles, become a full member the 24 of standard of new drug, and standard No. is WS
1-(X-015)-and 2001H, write down it
Chemistry is by name: 9-(1,3-dihydroxy-2-third oxygen methyl)-guanine
English name: Ganciclovir Injection
Structural formula is as follows:
Ganciclovir is the effective antiviral thing that first treatment human body cytomegalovirus (CMV) infects.That multiple dosage forms such as at present existing intravenous injection, capsule, intraocular implant and 0.15% eye ointment are applied to is clinical (Li Chun metacomplie. the Clinical advances of ganciclovir. the external medicine-biochemical medicine preparation of synthetic drug fascicle 1998,19 (3): 172-175).Because the dissolubility of ganciclovir is a slightly soluble in water, dissolubility is very low, therefore, the intravenous injection of ganciclovir is the injection freeze-dried powder at present, said preparation is the preparation method complexity not only, and in use will be with a large amount of water for injection through using after the dissolving for a long time, clinical practice is got up extremely inconvenient.
Summary of the invention
The present invention seeks to overcome the low prior art deficiency of ganciclovir dissolubility in water, the agent of a kind of ganciclovir liquid infusion is provided, be ganciclovir injection.
The present invention also provides the preparation method of ganciclovir injection.
Ganciclovir injection of the present invention can be made by following method.
Get an amount of water and ganciclovir by following proportioning:
1000～2000 parts in 50～100 parts of water of ganciclovir
Above-mentioned umber is a weight portion.
Get suitable quantity of water and ganciclovir by said ratio, ganciclovir is added to the water, and dropping sodium solution to solution pH value is 9～12 under stirring, and continuing to be stirred to ganciclovir dissolves fully, the needle-use activated carbon that adds overall solution volume 0.02% (g/ml), stirred 30 minutes, and filtered, supplementing water to liquor capacity equals originally to add the volume of entry in filtrate, filtering with microporous membrane with 0.45 μ m, in the embedding ampoule, sterilized 10～30 minutes for 100 ℃, promptly.
The optimum ratio scope of ganciclovir and water is in the above-mentioned preparation method:
1300～1600 parts in 70～80 parts of water of ganciclovir
The best proportioning of ganciclovir and water is in the above-mentioned preparation method:
1500 parts in 75 parts of water of ganciclovir
In the above-mentioned preparation method after the dropping sodium pH value preferable range of solution be 10.8～11.2.
In the above-mentioned preparation method after the dropping sodium pH value optimum of solution be 11.
The sodium hydroxide solution that is used to regulate pH value in the above-mentioned preparation method also can substitute with other alkaline reagents such as potassium hydroxide.
Advantage of the present invention is that in the ganciclovir injection with preparation method preparation of the present invention, ganciclovir dissolves in the entry well, and long-time the placement stablized.
Get an amount of ganciclovir and water by 75 parts of ganciclovirs, 1500 parts of weight proportions of water.Ganciclovir is added to the water, stirring down, dropping sodium solution to solution pH value is 11, continue to be stirred to ganciclovir and dissolve fully, add the needle-use activated carbon of overall solution volume 0.02% (g/ml), stirred 30 minutes, filter, supplementing water to liquor capacity is equal to the volume that originally adds entry in filtrate, with the filtering with microporous membrane of 0.45 μ m, in the embedding ampoule, sterilized 10～30 minutes, and promptly got ganciclovir injection of the present invention for 100 ℃.Be called ganciclovir injection 1..
The ganciclovir injection of getting the preparation of above-mentioned preparation method 1., room temperature was placed 9 months, respectively at placing 0 day, press regulation detection clarity among Chinese Pharmacopoeia version appendix in 2000 the I B, observation solution appearance, result such as following table 1 when placing 3 months, 6 months and 9 months
Table 1, ganciclovir injection room temperature keep sample and investigate result 1
| Time | Placed 0 day | Placed 3 months | Placed 6 months | Placed 9 months |
| Solution appearance | Colourless clear liquid | Colourless clear liquid | Colourless clear liquid | Colourless clear liquid |
| Clarity | Up to specification | Up to specification | Up to specification | Up to specification |
Table 1 shows through the ganciclovir injection of the present invention's preparation good through long-time room temperature placement rear stability, and ganciclovir can dissolve in the entry well.
The ganciclovir injection of following pathology evidence preparation method preparation of the present invention is safe.
Get body weight 18 of the Cavia porcelluss of 250～290g, anti-medical Group Co.,Ltd provides credit number by the Shandong, Shandong: SCCK Shandong 20030006.Cavia porcellus is divided into negative control group, is tried thing group and positive controls, 6 every group.Negative control group lumbar injection every day 0.9% normal saline 0.5ml/ only, tried 1. 0.5ml/ of thing group lumbar injection every day ganciclovir injection, positive controls lumbar injection every day 5% ovalbumin normal saline 0.5ml/ only, 5% ovalbumin normal saline is self-control, get fresh albumen, face the time spent under aseptic condition, to be made into 5% concentration with normal saline.Every group of Cavia porcellus injected three days continuously.Only get relative medicine 1ml/ that 3 Cavia porcellus intravenous injections inject for the first time for the first time injecting every group of back 14 days and 21 day respectively, observe the reaction of Cavia porcellus in injection 15 minutes.The result is as follows: the 14th day and the 21st day intravenous injection 0.9% normal saline 1ml/ be only behind first time abdominal cavity 0.9% normal saline for the negative control group Cavia porcellus, symptoms such as hello sound, tic, collapse or death do not appear in symptom such as perpendicular hair, dyspnea, sneeze, dry cough all occur or cough 3 yet.Tried thing group Cavia porcellus in the first time lumbar injection ganciclovir injection 1. back the 14th day and the 21st day intravenous injection ganciclovir injection 1. 1ml/ is only, symptom such as perpendicular hair, dyspnea, sneeze, dry cough all occur or cough 3, symptoms such as hello sound, tic, collapse or death do not appear yet, with the negative control group zero difference.Intravenous injection 5% ovalbumin normal saline 1ml/ is only respectively the 14th day and the 21st day after the administration first time for the positive control treated animal, symptoms such as 6 Cavia porcelluss astasia all occurs, twitch, fall down to the ground in 5 minutes after administration, dyspnea, dead in 1 minute 15 seconds～2 minutes and 00 second respectively, with negative control group very big-difference is arranged.
According to Wang Beiying, one of the Mount Liang heroes in Water Margin's instrument chief editor " new Chinese medicine development technology and method " 2001,851～852, Shanghai science tech publishing house, the ganciclovir injection hypersensitive test result of preparation method preparation of the present invention is negative, illustrates that medicine of the present invention is safe.
Specific embodiment
In order to understand better and to implement the present invention, the specific embodiment of the invention is explained
Embodiment 1
Take by weighing ganciclovir 75g, water 1500g, ganciclovir is added to the water, and dropping sodium solution to solution pH value is 11 under stirring, and continuing to be stirred to ganciclovir dissolves fully, the needle-use activated carbon that adds overall solution volume 0.02% (g/ml), stirred 30 minutes, and filtered, supplementing water to liquor capacity equals originally to add the volume of entry in filtrate, filtering with microporous membrane with 0.45 μ m, in the embedding ampoule, sterilized 20 minutes, and promptly got ganciclovir injection of the present invention for 100 ℃.
Embodiment 2
Take by weighing ganciclovir 50g, water 2000g, ganciclovir is added to the water, and dropping sodium solution to solution pH value is 9 under stirring, and continuing to be stirred to ganciclovir dissolves fully, the needle-use activated carbon that adds overall solution volume 0.02% (g/ml), stirred 30 minutes, and filtered, supplementing water to liquor capacity equals originally to add the volume of entry in filtrate, filtering with microporous membrane with 0.45 μ m, in the embedding ampoule, sterilized 10 minutes, and promptly got ganciclovir injection of the present invention for 100 ℃.
Embodiment 3
Take by weighing ganciclovir 100g, water 1000g, ganciclovir is added to the water, dropping sodium solution to solution pH value is 12 under stirring, and continuing to be stirred to ganciclovir dissolves fully, adds the needle-use activated carbon of overall solution volume 0.02% (g/ml); Stirred 30 minutes, and filtered, supplementing water to liquor capacity equals originally to add the volume of entry in filtrate, with the filtering with microporous membrane of 0.45 μ m, in the embedding ampoule, sterilizes 30 minutes, and promptly gets ganciclovir injection of the present invention for 100 ℃.
Embodiment 4
Take by weighing ganciclovir 70g, water 1600g, ganciclovir is added to the water, and stirring and dripping potassium hydroxide solution to solution pH value down is 11.2, and continuing to be stirred to ganciclovir dissolves fully, the needle-use activated carbon that adds overall solution volume 0.02% (g/ml), stirred 30 minutes, and filtered, supplementing water to liquor capacity equals originally to add the volume of entry in filtrate, filtering with microporous membrane with 0.45 μ m, in the embedding ampoule, sterilized 30 minutes, and promptly got ganciclovir injection of the present invention for 100 ℃.
Embodiment 5
Take by weighing ganciclovir 70g, water 1300g, ganciclovir is added to the water, and stirring and dripping potassium hydroxide solution to solution pH value down is 10.8, and continuing to be stirred to ganciclovir dissolves fully, the needle-use activated carbon that adds overall solution volume 0.02% (g/ml), stirred 30 minutes, and filtered, supplementing water to liquor capacity equals originally to add the volume of entry in filtrate, filtering with microporous membrane with 0.45 μ m, in the embedding ampoule, sterilized 30 minutes, and promptly got ganciclovir injection of the present invention for 100 ℃.
Embodiment 6
Take by weighing ganciclovir 80g, water 1300g, ganciclovir is added to the water, and stirring and dripping potassium hydroxide solution to solution pH value down is 11, and continuing to be stirred to ganciclovir dissolves fully, the needle-use activated carbon that adds overall solution volume 0.02% (g/ml), stirred 30 minutes, and filtered, supplementing water to liquor capacity equals originally to add the volume of entry in filtrate, filtering with microporous membrane with 0.45 μ m, in the embedding ampoule, sterilized 30 minutes, and promptly got ganciclovir injection of the present invention for 100 ℃.
Claims (8)
1. ganciclovir injection is characterized in that its liquid infusion preparation by 9-(1,3-dihydroxy-2-third oxygen methyl)-guanine preparation.
2. according to the described ganciclovir injection of claim 1, wherein said liquid infusion preparation is an aqueous solution injection.
3. the preparation method of a ganciclovir injection is characterized in that preparing as follows:
Get an amount of ganciclovir and water by following proportioning:
1000～2000 parts in 50～100 parts of water of ganciclovir
Above-mentioned umber is a weight portion.
Get suitable quantity of water and ganciclovir by said ratio, ganciclovir is added to the water, and dropping sodium solution to solution pH value is 9～12 under stirring, and continuing to be stirred to ganciclovir dissolves fully, the needle-use activated carbon that adds overall solution volume 0.02% (g/ml), stirred 30 minutes, and filtered, supplementing water to liquor capacity equals originally to add the volume of entry in filtrate, filtering with microporous membrane with 0.45 μ m, in the embedding ampoule, sterilized 10～30 minutes for 100 ℃, promptly.
4. according to the preparation method of the described ganciclovir injection of claim 3., it is characterized in that the ratio range of ganciclovir and water is: 1300～1600 parts in 70～80 parts of water of ganciclovir
5. according to the preparation method of the described ganciclovir injection of claim 3., it is characterized in that the proportioning of ganciclovir and water is: 1500 parts in 75 parts of water of ganciclovir
6. according to the preparation method of the described ganciclovir injection of claim 3., it is characterized in that sodium hydroxide solution is other basic formulations such as potassium hydroxide.
7. according to the preparation method of the described ganciclovir injection of claim 3., it is characterized in that it is 10.8～11.2 that sodium hydroxide is regulated the pH value scope of back solution.
8. the preparation method of ganciclovir injection according to claim 3 is characterized in that it is 11 that sodium hydroxide is regulated the pH value of back solution.
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| CN 200510005177 CN1679580A (en) | 2005-02-01 | 2005-02-01 | Ganciclovir injection and preparation thereof |
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| CN 200510005177 CN1679580A (en) | 2005-02-01 | 2005-02-01 | Ganciclovir injection and preparation thereof |
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Cited By (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN102274197A (en) * | 2011-07-19 | 2011-12-14 | 江苏奥赛康药业股份有限公司 | Ganciclovir composition for injection and preparation method thereof |
| CN104414967A (en) * | 2013-09-06 | 2015-03-18 | 康普药业股份有限公司 | Ganciclovir injection solution and preparation method thereof |
| CN106176595A (en) * | 2016-08-31 | 2016-12-07 | 辰欣药业股份有限公司 | A kind of ganciclovir injection and preparation technology thereof |
| US11723978B2 (en) * | 2013-08-30 | 2023-08-15 | Exela Pharma Sciences, LLC | Ganciclovir compositions and related methods |
-
2005
- 2005-02-01 CN CN 200510005177 patent/CN1679580A/en active Pending
Cited By (6)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN102274197A (en) * | 2011-07-19 | 2011-12-14 | 江苏奥赛康药业股份有限公司 | Ganciclovir composition for injection and preparation method thereof |
| CN102274197B (en) * | 2011-07-19 | 2013-01-16 | 江苏奥赛康药业股份有限公司 | Ganciclovir composition for injection and preparation method thereof |
| US11723978B2 (en) * | 2013-08-30 | 2023-08-15 | Exela Pharma Sciences, LLC | Ganciclovir compositions and related methods |
| CN104414967A (en) * | 2013-09-06 | 2015-03-18 | 康普药业股份有限公司 | Ganciclovir injection solution and preparation method thereof |
| CN106176595A (en) * | 2016-08-31 | 2016-12-07 | 辰欣药业股份有限公司 | A kind of ganciclovir injection and preparation technology thereof |
| CN106176595B (en) * | 2016-08-31 | 2019-10-22 | 辰欣药业股份有限公司 | A kind of ganciclovir injection and its preparation process |
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