CN104529877A - Amlodipine-decylic acid ion liquid as well as preparation method and application thereof - Google Patents
Amlodipine-decylic acid ion liquid as well as preparation method and application thereof Download PDFInfo
- Publication number
- CN104529877A CN104529877A CN201510036331.5A CN201510036331A CN104529877A CN 104529877 A CN104529877 A CN 104529877A CN 201510036331 A CN201510036331 A CN 201510036331A CN 104529877 A CN104529877 A CN 104529877A
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- China
- Prior art keywords
- amlodipine
- capric acid
- ionic liquid
- preparation
- acid ionic
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- 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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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D211/00—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings
- C07D211/04—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
- C07D211/80—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having two double bonds between ring members or between ring members and non-ring members
- C07D211/84—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having two double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms, with at the most one bond to halogen directly attached to ring carbon atoms
- C07D211/90—Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen
Abstract
The invention discloses amlodipine-decylic acid ion liquid as well as a preparation method and application thereof. The DSC spectrum of the amlodipine-decylic acid ion liquid has an endothermic peak at 98+/-5 DEG C. The amlodipine-decylic acid ion liquid has the advantages of good pharmaceutical acceptability, proper physicochemical property and good stability, is more suitable for a physicochemical formula and can be used for preparing a medicament for treating vascular hypertension.
Description
Technical field
The present invention relates to field of medicaments, be specifically related to a kind of amlodipine-capric acid ionic liquid and its production and use.
Background technology
Amlodipine is a kind of as flow blocker in antihypertensive drug 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 cytolemma, by relaxing at the unstriated muscle of arterial wall, reduces total peripheral resistance, thus removes coronary vasospasm angina.Pfizer company of the U.S. discloses the preparation method of amlodipine and oxalate, maleate, hydrochloride, hydrobromate, vitriol, phosphoric acid salt, Citrate trianion and gluconate in European patent EP 89167 and US Patent No. 4572909, and thinks that amlodipine maleate is ideal.Amlodipine besylate 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 thermostability 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 novel 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-capric acid ionic liquid and its production and use, this amlodipine-capric acid ionic liquid has good pharmaceutical acceptability, suitable physico-chemical property, good stability, be more suitable for for formula of medicine, can be used for preparation treatment vascular hypertension medicine.
For achieving the above object, the invention provides a kind of amlodipine-capric acid ionic liquid, its DSC collection of illustrative plates has endotherm(ic)peak at 98 ± 5 DEG C.
The present invention also provides the preparation method of above-mentioned amlodipine-capric acid ionic liquid: at normal temperatures, by amlodipine and capric acid with mol ratio mixed grinding 10 ~ 30 minutes in mortar of 1: 1, obtains amlodipine-capric acid ionic liquid.
The present invention also provides the another kind of preparation method of above-mentioned amlodipine-capric acid ionic liquid: at normal temperatures, by amlodipine and capric 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 normal temperature, obtain amlodipine-capric acid ionic liquid.
The present invention also provides the purposes of above-mentioned amlodipine-capric acid ionic 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-capric acid ionic liquid and its production and use, this amlodipine-capric acid ionic liquid has good pharmaceutical acceptability, suitable physico-chemical property, good stability, be more suitable for for formula of medicine, can be used for preparation treatment vascular hypertension medicine.
Embodiment
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 capric acid of 1 molar equivalent, grind under normal temperature 10 ~ 30 minutes (being preferably 30 minutes), gained powder is scraped, obtains amlodipine-capric acid ionic liquid.
Embodiment 2
Take 1g amlodipine in culture dish, add the capric acid of 1 molar equivalent, mix under normal 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 normal temperature, obtain amlodipine-capric acid ionic liquid.
The stability test of embodiment 1 and embodiment 2 gained amlodipine-capric acid ionic liquid is as follows:
Respectively amlodipine-capric acid ionic liquid 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-capric acid ionic liquid, its DSC collection of illustrative plates has endotherm(ic)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-capric acid ionic liquid, is characterized in that, its DSC collection of illustrative plates has endotherm(ic)peak at 98 ± 5 DEG C.
2. the preparation method of amlodipine according to claim 1-capric acid ionic liquid, is characterized in that, at normal temperatures, by amlodipine and capric acid with mol ratio mixed grinding 10 ~ 30 minutes in mortar of 1: 1, obtains amlodipine-capric acid ionic liquid.
3. the preparation method of amlodipine according to claim 1-capric acid ionic liquid, is characterized in that, at normal temperatures, by amlodipine and capric 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 normal temperature, obtain amlodipine-capric acid ionic liquid.
4. the application of the amlodipine described in claim 1,2 or 3-capric acid ionic liquid in preparation treatment vascular hypertension medicine.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN201510036331.5A CN104529877A (en) | 2015-01-22 | 2015-01-22 | Amlodipine-decylic acid ion liquid as well as preparation method and application thereof |
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN201510036331.5A CN104529877A (en) | 2015-01-22 | 2015-01-22 | Amlodipine-decylic acid ion liquid as well as preparation method and application thereof |
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| Publication Number | Publication Date |
|---|---|
| CN104529877A true CN104529877A (en) | 2015-04-22 |
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| CN201510036331.5A Withdrawn CN104529877A (en) | 2015-01-22 | 2015-01-22 | Amlodipine-decylic acid ion liquid as well as preparation method and application thereof |
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Citations (8)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US4572909A (en) * | 1982-03-11 | 1986-02-25 | Pfizer Inc. | 2-(Secondary aminoalkoxymethyl) dihydropyridine derivatives as anti-ischaemic and antihypertensive agents |
| CN87102493A (en) * | 1986-04-04 | 1987-10-14 | 菲泽有限公司 | Improvements in or relating to pharmaceutically acceptable salts |
| WO2002053538A1 (en) * | 2000-12-29 | 2002-07-11 | Pfizer Limited | Amlodipine fumarate |
| US20030199559A1 (en) * | 2000-12-29 | 2003-10-23 | Benneker Franciscus B. G. | Process for making amlodipine maleate |
| CN1495166A (en) * | 2002-08-21 | 2004-05-12 | ��һ������ʽ���� | Organic acid salt of amlodipine |
| KR20050030393A (en) * | 2003-09-26 | 2005-03-30 | 케이비 테크놀러지 (주) | Credit-card transaction method of taxi terminal |
| CN101307020A (en) * | 2008-06-06 | 2008-11-19 | 苏州东南药物研发有限责任公司 | Amlodipine-zinc sulfate salts, preparing process thereof and application thereof |
| KR20100063915A (en) * | 2008-12-04 | 2010-06-14 | 화일약품주식회사 | Method of preparing s-(-)-amlodipine with high optical purity and intermediate compound produced during the same |
-
2015
- 2015-01-22 CN CN201510036331.5A patent/CN104529877A/en not_active Withdrawn
Patent Citations (8)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US4572909A (en) * | 1982-03-11 | 1986-02-25 | Pfizer Inc. | 2-(Secondary aminoalkoxymethyl) dihydropyridine derivatives as anti-ischaemic and antihypertensive agents |
| CN87102493A (en) * | 1986-04-04 | 1987-10-14 | 菲泽有限公司 | Improvements in or relating to pharmaceutically acceptable salts |
| WO2002053538A1 (en) * | 2000-12-29 | 2002-07-11 | Pfizer Limited | Amlodipine fumarate |
| US20030199559A1 (en) * | 2000-12-29 | 2003-10-23 | Benneker Franciscus B. G. | Process for making amlodipine maleate |
| CN1495166A (en) * | 2002-08-21 | 2004-05-12 | ��һ������ʽ���� | Organic acid salt of amlodipine |
| KR20050030393A (en) * | 2003-09-26 | 2005-03-30 | 케이비 테크놀러지 (주) | Credit-card transaction method of taxi terminal |
| CN101307020A (en) * | 2008-06-06 | 2008-11-19 | 苏州东南药物研发有限责任公司 | Amlodipine-zinc sulfate salts, preparing process thereof and application thereof |
| KR20100063915A (en) * | 2008-12-04 | 2010-06-14 | 화일약품주식회사 | Method of preparing s-(-)-amlodipine with high optical purity and intermediate compound produced during the same |
Non-Patent Citations (3)
| 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》 * |
| 杨凤霞: "不同成盐方式的左旋氨氯地平片的稳定性考察", 《中国医院药学杂志》 * |
| 王晓科，等: "氨氯地平苯磺酸盐的合成", 《精细化工》 * |
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| WW01 | Invention patent application withdrawn after publication |
Application publication date: 20150422 |
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| WW01 | Invention patent application withdrawn after publication |