CN104523588A - Amlodipine-stearic acid ionic liquid as well as preparation method and application thereof - Google Patents
Amlodipine-stearic acid ionic liquid as well as preparation method and application thereof Download PDFInfo
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- CN104523588A CN104523588A CN201510036332.XA CN201510036332A CN104523588A CN 104523588 A CN104523588 A CN 104523588A CN 201510036332 A CN201510036332 A CN 201510036332A CN 104523588 A CN104523588 A CN 104523588A
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- amlodipine
- ion liquid
- stearic acid
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- ionic liquid
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Abstract
The invention discloses an amlodipine-stearic acid ionic liquid as well as a preparation method and application thereof. The DSC thermogram of the amlodipine-stearic acid ionic liquid has an endothermic peak at 98+/-5 DEG C; the amlodipine-stearic acid ionic liquid has the advantages of good medicine acceptability, appropriate physical and chemical properties and good stability, is suitable for a pharmaceutical formulation, and can be used for preparing medicines for treating vascular hypertension.
Description
Technical field
The present invention relates to field of medicaments, be specifically related to a kind of amlodipine-stearate ion liquid and its production and use.
Background technology
Amlodipine is a kind of as flow blocker in antihypertensive and the anginal dihydropyridines long-term calcium-channel for the treatment of.The effect of amlodipine is that retardance cardiac muscle and the outer calcium ion of vascular smooth muscle cell enter cell through the calcium channel of cell membrane, by relaxing at the smooth muscle of arterial wall, reduces total peripheral resistance, thus removes coronary vasospasm angor.Pfizer company of the U.S. discloses the preparation method of amlodipine and oxalates, maleate, hydrochlorate, hydrobromate, sulfate, phosphate, citrate and gluconate in European patent EP 89167 and US Patent No. 4572909, and thinks that amlodipine maleate is ideal.Amlodipine Besylate Tablet is recommended again in US Patent No. 4879303.
The physico-chemical properties of ionic liquid, biological property received much concern in recent years.Ionic liquid is almost without vapour pressure, high heat stability and chemical stability, excellent solubility property, excellent electrochemical properties and easily reclaims, the advantage such as can to design, and the overwhelming majority studies and concentrates on solvent, the application of catalysis and new material aspect.Because the activity of ionic liquid can be regulated by the designability of ionic liquid, and the structure of much common ion liquid or component similar with the presoma of active pharmaceutical ingredient or active pharmaceutical ingredient, people start to recognize that it may have potential biological activity.Many scholars were devoted to the research that ionic liquid is applied to medicine one after another in recent years.
Summary of the invention
The object of the present invention is to provide a kind of amlodipine-stearate ion liquid and its production and use, this amlodipine-stearate ion liquid has good pharmaceutical acceptability, suitable physicochemical property, good stability, be more suitable for for pharmaceutical formulation, can be used for preparation treatment vascular hypertension medicine.
For achieving the above object, the invention provides a kind of amlodipine-stearate ion liquid, its DSC collection of illustrative plates has endothermic peak at 98 ± 5 DEG C.
The present invention also provides the preparation method of above-mentioned amlodipine-stearate ion liquid: at normal temperatures, by amlodipine and stearic acid with mol ratio mixed grinding 10 ~ 30 minutes in mortar of 1: 1, obtains amlodipine-stearate ion liquid.
The present invention also provides the another kind of preparation method of above-mentioned amlodipine-stearate ion liquid: at normal temperatures, by amlodipine and stearic acid with 1: 1 mixed in molar ratio, put into 80 ~ 120 DEG C of baking ovens again, take out after 12 hours and be cooled to room temperature, obtain amlodipine-stearate ion liquid.
The present invention also provides the purposes of above-mentioned amlodipine-stearate ion liquid: for the preparation for the treatment of vascular hypertension medicine.
Advantage of the present invention and beneficial effect are: provide a kind of amlodipine-stearate ion liquid and its production and use, this amlodipine-stearate ion liquid has good pharmaceutical acceptability, suitable physicochemical property, good stability, be more suitable for for pharmaceutical formulation, can be used for preparation treatment vascular hypertension medicine.
Detailed description of the invention
Below in conjunction with embodiment, the specific embodiment of the present invention is further described.Following examples only for technical scheme of the present invention is clearly described, and can not limit the scope of the invention with this.
The technical scheme that the present invention specifically implements is:
Embodiment 1
Take 1g amlodipine in agate mortar, add the stearic acid of 1 molar equivalent, grind under room temperature 10 ~ 30 minutes (being preferably 30 minutes), gained powder is scraped, obtains amlodipine-stearate ion liquid.
Embodiment 2
Take 1g amlodipine in culture dish, add the stearic acid of 1 molar equivalent, mix homogeneously under room temperature, this mixture is placed in 80 ~ 120 DEG C of (being preferably 100 DEG C) baking ovens, take out after 12 hours and be cooled to room temperature, obtain amlodipine-stearate ion liquid.
The stability test of embodiment 1 and embodiment 2 gained amlodipine-stearate ion liquid is as follows:
Respectively amlodipine-stearate ion fluid sample being placed in 60 DEG C of baking ovens, the environment of humidity 92.5% and the light of illumination 45001ux stablizes in case, after 5 days, 10 days, sample taking-up is carried out PXRD test, to investigate the physical stability of sample to temperature.Result shows, sample PXRD collection of illustrative plates does not under these conditions change, and illustrates that its physical stability under high temperature, high humidity, illumination condition is good.
Embodiment 1 and embodiment 2 gained amlodipine-stearate ion liquid, its DSC collection of illustrative plates has endothermic peak at 98 ± 5 DEG C, can be used for preparation treatment vascular hypertension medicine.
The above is only the preferred embodiment of the present invention; it should be pointed out that for those skilled in the art, under the prerequisite not departing from the technology of the present invention principle; can also make some improvements and modifications, these improvements and modifications also should be considered as protection scope of the present invention.
Claims (4)
1. amlodipine-stearate ion liquid, is characterized in that, its DSC collection of illustrative plates has endothermic peak at 98 ± 5 DEG C.
2. the preparation method of amlodipine according to claim 1-stearate ion liquid, is characterized in that, at normal temperatures, by amlodipine and stearic acid with mol ratio mixed grinding 10 ~ 30 minutes in mortar of 1: 1, obtains amlodipine-stearate ion liquid.
3. the preparation method of amlodipine according to claim 1-stearate ion liquid, it is characterized in that, at normal temperatures, by amlodipine and stearic acid with 1: 1 mixed in molar ratio, put into 80 ~ 120 DEG C of baking ovens again, take out after 12 hours and be cooled to room temperature, obtain amlodipine-stearate ion liquid.
4. the application of the amlodipine described in claim 1,2 or 3-stearate ion liquid in preparation treatment vascular hypertension medicine.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN201510036332.XA CN104523588A (en) | 2015-01-22 | 2015-01-22 | Amlodipine-stearic acid ionic liquid as well as preparation method and application thereof |
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
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| CN201510036332.XA CN104523588A (en) | 2015-01-22 | 2015-01-22 | Amlodipine-stearic acid ionic liquid as well as preparation method and application thereof |
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| CN104523588A true CN104523588A (en) | 2015-04-22 |
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| CN201510036332.XA Pending CN104523588A (en) | 2015-01-22 | 2015-01-22 | Amlodipine-stearic acid ionic liquid as well as preparation method and application thereof |
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Citations (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN87102493A (en) * | 1986-04-04 | 1987-10-14 | 菲泽有限公司 | Improvements in or relating to pharmaceutically acceptable salts |
| KR20040080039A (en) * | 2003-03-10 | 2004-09-18 | 한림제약(주) | Improved method for the preparation of intermediate of amlodipine |
| CN101326275A (en) * | 2005-10-07 | 2008-12-17 | 阿拉巴马大学 | Multi-functional ionic liquid compositions |
-
2015
- 2015-01-22 CN CN201510036332.XA patent/CN104523588A/en active Pending
Patent Citations (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN87102493A (en) * | 1986-04-04 | 1987-10-14 | 菲泽有限公司 | Improvements in or relating to pharmaceutically acceptable salts |
| KR20040080039A (en) * | 2003-03-10 | 2004-09-18 | 한림제약(주) | Improved method for the preparation of intermediate of amlodipine |
| CN101326275A (en) * | 2005-10-07 | 2008-12-17 | 阿拉巴马大学 | Multi-functional ionic liquid compositions |
Non-Patent Citations (1)
| Title |
|---|
| 孟坤燕 等: "氨氯地平离子液体盐的制备与研究", 《第三届中国晶型药物研发技术学术研讨会》 * |
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Application publication date: 20150422 |
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| RJ01 | Rejection of invention patent application after publication |