CN104610130A - Amlodipine-palmic acid ionic liquid as well as preparation method and application thereof - Google Patents
Amlodipine-palmic acid ionic liquid as well as preparation method and application thereof Download PDFInfo
- Publication number
- CN104610130A CN104610130A CN201510036333.4A CN201510036333A CN104610130A CN 104610130 A CN104610130 A CN 104610130A CN 201510036333 A CN201510036333 A CN 201510036333A CN 104610130 A CN104610130 A CN 104610130A
- Authority
- CN
- China
- Prior art keywords
- amlodipine
- ionic liquid
- palmitinic acid
- acid ionic
- preparation
- Prior art date
- 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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Classifications
-
- 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
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
- A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
- A61K31/4422—1,4-Dihydropyridines, e.g. nifedipine, nicardipine
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
- A61K47/50—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates
- A61K47/51—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent
- A61K47/54—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an organic compound
- A61K47/542—Carboxylic acids, e.g. a fatty acid or an amino acid
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
- C07C51/00—Preparation of carboxylic acids or their salts, halides or anhydrides
- C07C51/41—Preparation of salts of carboxylic acids
- C07C51/412—Preparation of salts of carboxylic acids by conversion of the acids, their salts, esters or anhydrides with the same carboxylic acid part
Abstract
The invention discloses amlodipine-palmic acid ionic liquid as well as a preparation method and application thereof. The DSC atlas of the amlodipine-palmic acid ionic liquid has an endothermic peak at 98+/-5 DEG C. The amlodipine-palmic acid ionic liquid has favorable medicine acceptability and proper physical chemical property, is good in stability, and more suitable for being used in medicine recipe, and can be used for preparing medicine curing hypertension.
Description
Technical field
The present invention relates to field of medicaments, be specifically related to a kind of amlodipine-palmitinic 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-palmitinic acid ionic liquid and its production and use, this amlodipine-palmitinic 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-palmitinic 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-palmitinic acid ionic liquid: at normal temperatures, by amlodipine and palmitinic acid with mol ratio mixed grinding 10 ~ 30 minutes in mortar of 1: 1, obtains amlodipine-palmitinic acid ionic liquid.
The present invention also provides the another kind of preparation method of above-mentioned amlodipine-palmitinic acid ionic liquid: at normal temperatures, by amlodipine and palmitinic 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-palmitinic acid ionic liquid.
The present invention also provides the purposes of above-mentioned amlodipine-palmitinic 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-palmitinic acid ionic liquid and its production and use, this amlodipine-palmitinic 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 palmitinic acid of 1 molar equivalent, grind under normal temperature 10 ~ 30 minutes (being preferably 30 minutes), gained powder is scraped, obtains amlodipine-palmitinic acid ionic liquid.
Embodiment 2
Take 1g amlodipine in culture dish, add the palmitinic 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-palmitinic acid ionic liquid.
The stability test of embodiment 1 and embodiment 2 gained amlodipine-palmitinic acid ionic liquid is as follows:
Respectively amlodipine-palmitinic 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-palmitinic 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-palmitinic 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-palmitinic acid ionic liquid, is characterized in that, at normal temperatures, by amlodipine and palmitinic acid with mol ratio mixed grinding 10 ~ 30 minutes in mortar of 1: 1, obtains amlodipine-palmitinic acid ionic liquid.
3. the preparation method of amlodipine according to claim 1-palmitinic acid ionic liquid, it is characterized in that, at normal temperatures, by amlodipine and palmitinic 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-palmitinic acid ionic liquid.
4. the application of the amlodipine described in claim 1,2 or 3-palmitinic acid ionic liquid in preparation treatment vascular hypertension medicine.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN201510036333.4A CN104610130A (en) | 2015-01-22 | 2015-01-22 | Amlodipine-palmic acid ionic liquid as well as preparation method and application thereof |
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN201510036333.4A CN104610130A (en) | 2015-01-22 | 2015-01-22 | Amlodipine-palmic acid ionic liquid as well as preparation method and application thereof |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| CN104610130A true CN104610130A (en) | 2015-05-13 |
Family
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Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CN201510036333.4A Withdrawn CN104610130A (en) | 2015-01-22 | 2015-01-22 | Amlodipine-palmic acid ionic liquid as well as preparation method and application thereof |
Country Status (1)
| Country | Link |
|---|---|
| CN (1) | CN104610130A (en) |
Citations (5)
| 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 |
| US20090004281A1 (en) * | 2007-06-26 | 2009-01-01 | Biovail Laboratories International S.R.L. | Multiparticulate osmotic delivery system |
| WO2010035047A1 (en) * | 2008-09-25 | 2010-04-01 | Pharmapatents Global Ltd. | Binary compositions comprising an no-donor and an a-smase inhibitor for the treatment of respiratory diseases |
| CN102292070A (en) * | 2009-01-23 | 2011-12-21 | 韩美控股株式会社 | Solid pharmaceutical composition comprising amlodipine and losartan with improved stability |
| CN103690514A (en) * | 2013-12-25 | 2014-04-02 | 润泽制药(苏州)有限公司 | Timed controlled-release amlodipine capsule and preparation method thereof |
-
2015
- 2015-01-22 CN CN201510036333.4A patent/CN104610130A/en not_active Withdrawn
Patent Citations (5)
| 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 |
| US20090004281A1 (en) * | 2007-06-26 | 2009-01-01 | Biovail Laboratories International S.R.L. | Multiparticulate osmotic delivery system |
| WO2010035047A1 (en) * | 2008-09-25 | 2010-04-01 | Pharmapatents Global Ltd. | Binary compositions comprising an no-donor and an a-smase inhibitor for the treatment of respiratory diseases |
| CN102292070A (en) * | 2009-01-23 | 2011-12-21 | 韩美控股株式会社 | Solid pharmaceutical composition comprising amlodipine and losartan with improved stability |
| CN103690514A (en) * | 2013-12-25 | 2014-04-02 | 润泽制药(苏州)有限公司 | Timed controlled-release amlodipine capsule and preparation method thereof |
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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| C06 | Publication | ||
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| WW01 | Invention patent application withdrawn after publication |
Application publication date: 20150513 |
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| WW01 | Invention patent application withdrawn after publication |