CN105168131B - A kind of preparation method of TAK-438 nano-emulsions - Google Patents
A kind of preparation method of TAK-438 nano-emulsions Download PDFInfo
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- CN105168131B CN105168131B CN201510513143.7A CN201510513143A CN105168131B CN 105168131 B CN105168131 B CN 105168131B CN 201510513143 A CN201510513143 A CN 201510513143A CN 105168131 B CN105168131 B CN 105168131B
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Abstract
The present invention provides a kind of preparation method of 438 nano-emulsions of TAK, belongs to 438 pharmaceutical carrier technical fields of TAK, it can solve the problems, such as in industrial production that 438 this medicines of TAK are only capable of being piece agent dysphagia patien and be difficult to take.The preparation method of 438 nano-emulsions of TAK of the present invention includes preparing oil phase, preparing the step of water phase, emulsification, homogeneous.438 nano-emulsion stability of TAK prepared by method using the present invention is good, the preparation and storage of 438 nanoemulsion medicines of TAK are more convenient, injection is more conducive to use, the pain that medicine produces when mitigating patient's use, the preparation method technique of 438 nano-emulsions of TAK of the present invention is simple, mild condition, cost is low, suitable industrialized production.
Description
Technical field
The invention belongs to TAK-438 pharmaceutical carrier technical fields, and in particular to a kind of preparation side of TAK-438 nano-emulsions
Method.
Background technology
Gastric acid related disease (ARDs) is the pathogenesis disease of upper digestive tract closely related with hydrochloric acid in gastric juice, according to its morbidity
Species can be divided into following a few classes：Food digests bad, gastrointestinal inflammation symptom, Zollinger-Ellison to intestines and stomach reflux
The disease of digestive tract that syndrome (also known as " zes ") and non-steroid anti-inflammatory drug trigger.The incidence trend of ARDs exists
Rise from year to year, especially in China, such disease has become very serious disease, largely reduces hydrochloric acid in gastric juice phase
The quality of life of closing property Disease, and economically very big burden is caused to ARDs patient.
Having some limitations property of proton pump inhibitor-PPIs, PPIs is for some gastric acid related disease patients in evening
The upper inhibitory action that hyper acid discharges, drug effect deficiency.In order to solve this problem, new more effective medicine, Ren Menkai are found
Begin the competitive sour retarding agent-P-CAB of research K+, this new class of new acid inhibitor.
The advantage of TAK-438 be the drug effect of this class medicine gastric acid inhibitory acid not against the activity of proton pump, can be apparent
Reduce the generation that the acid of night gastric acid related disease patient is broken through.
TAK-438 is a kind of pyrrole derivatives, is a kind of acylate of fumaric acid.Its structure contains fluorophenyl, pyrrole
Piperidinyl and sulfonyl and pyrrole group, PH 6.5.Its molecular formula is C17H16FN3O2S.C4H4O4, molecular weight 461.46.White
Crystalline powder.The chemical structural formula of TAK-438 is：
Inventor has found that at least there are the following problems in the prior art：At present in industrial production, this medicines of TAK-438 are only capable of
Piece agent is done, this formulation of tablet there are some limitations, such as：There is the situation of dysphagia in gastric acid related disease patient
Under, it can not just take this medicine；In addition there are some patients due to the limitation of disease, it is impossible to use the medicine that formulation is tablet
Thing.
The content of the invention
The present invention is only capable of doing piece agent for this medicines of existing TAK-438, and this formulation of tablet has some limitations
A kind of technical problem, there is provided preparation method of TAK-438 nano-emulsions.
Technical solution is used by solving present invention problem：
A kind of preparation method of TAK-438 nano-emulsions, it is characterised in that including following preparation process：
Prepare oil phase：10-100 parts by weight of soybean oil is added in the first container, it is 15-60 to control temperature in oil phase container
℃；
Prepare water phase：1-5 parts by weight Emulsifier is added in second container, adds the deionization of 50-500 parts by weight
Water stirs evenly, and it is 15-60 DEG C to control water phase container medium temperature degree；Then 0.5-2.5 parts by weight TAK-438 is added under stirring condition；
Emulsification：Under stirring condition, oil phase is added in water phase, obtains TAK-438 colostrums；
Preferably, the deionized water is added portionwise, and the homogeneous speed is：3000r/min-10000r/min, homogeneous
Time is 5-60min.
Preferably, the emulsifying agent is Tween-80.
Preferably, in described the step of preparing oil phase, it is 25 DEG C to control temperature in oil phase container.
Preferably, in described the step of preparing water phase, it is 25 DEG C to control water phase container medium temperature degree.
TAK-438 nano-emulsions stability prepared by method using the present invention is good, the preparation of TAK-438 nanoemulsion medicines
It is more convenient with storing, it is more conducive to injection and uses, the pain that medicine produces when mitigating patient's use, TAK- of the invention
The preparation method technique of 438 nano-emulsions is simple, and mild condition, cost is low, suitable industrialized production.
Brief description of the drawings
Fig. 1 is emulsion particle diameter distribution made from embodiment 1.
Fig. 2 is emulsion average grain diameter made from embodiment 1.
Fig. 3 is emulsion particle diameter distribution made from embodiment 2.
Fig. 4 is emulsion average grain diameter made from embodiment 2.
Embodiment
To make those skilled in the art more fully understand technical scheme, below in conjunction with the accompanying drawings and specific embodiment party
Formula is described in further detail the present invention.
Embodiment 1：
The present embodiment provides a kind of preparation method of TAK-438 nano-emulsions：
Prepare oil phase：20 parts by weight of soybean oil is added in the first container, it is 25 DEG C to control temperature in oil phase container；
Prepare water phase：Emulsifying agent is added in second container, the deionized water for adding 100 parts by weight stirs evenly, control
Water phase container medium temperature degree is 25 DEG C；Then TAK-438 is added under stirring condition；
Emulsification：Under stirring condition, oil phase is added in water phase, obtains TAK-438 colostrums；
By colostrum as under homogenizer, homogeneous speed is：5000r/min, homogenizing time 5min, after homogeneous, are surpassed
Sonication can obtain TAK-438 nano-emulsions.
TAK-438 nano-emulsions average grain diameter 531.6 prepared by embodiment 1, PDI 0.153.And the result is shown in implementation
TAK-438 stable emulsions made from example 1.
Embodiment 2：
The present embodiment provides a kind of preparation method of TAK-438 nano-emulsions：
Prepare oil phase：20 parts by weight of soybean oil is added in the first container, it is 60 DEG C to control temperature in oil phase container；
Prepare water phase：Emulsifying agent is added in second container, the deionized water for adding 100 parts by weight stirs evenly, control
Water phase container medium temperature degree is 60 DEG C；Then TAK-438 is added under stirring condition；
Emulsification：Under stirring condition, oil phase is added in water phase, obtains TAK-438 colostrums；
By colostrum as under homogenizer, homogeneous speed is：5000r/min, homogenizing time 5min, after homogeneous, are surpassed
Sonication can obtain TAK-438 nano-emulsions.
TAK-438 nano-emulsion average grain diameters 2109.4nm, PDI 0.727 prepared by embodiment 2.
Emulsion obtained by embodiment 1, embodiment 2 is placed in Particle Size Analyzer sample cell and measures its particle diameter, using sharp
Light grain size analysis, as a result as shown in Figs 1-4：
Wherein, Fig. 1 is emulsion particle diameter distribution made from embodiment 1；Fig. 2 is emulsion average grain diameter made from embodiment 1；Figure
3 be emulsion particle diameter distribution made from embodiment 2；Fig. 4 is emulsion average grain diameter made from embodiment 2.
Embodiment 3：
The present embodiment provides a kind of preparation method of TAK-438 nano-emulsions：
Prepare oil phase：20 parts by weight of soybean oil is added in the first container, it is 25 DEG C to control temperature in oil phase container；
Prepare water phase：Emulsifying agent is added in second container, the deionized water for adding 100 parts by weight stirs evenly, control
Water phase container medium temperature degree is 60 DEG C；Then TAK-438 is added under stirring condition；
Emulsification：Under stirring condition, oil phase is added in water phase, obtains TAK-438 colostrums；
By colostrum as under homogenizer, homogeneous speed is：5000r/min, homogenizing time 5min, after homogeneous, are surpassed
Sonication can obtain TAK-438 nano-emulsions.
Embodiment 4：
The present embodiment provides a kind of preparation method of TAK-438 nano-emulsions：
Prepare oil phase：20 parts by weight of soybean oil is added in the first container, it is 60 DEG C to control temperature in oil phase container；
Prepare water phase：Emulsifying agent is added in second container, the deionized water for adding 100 parts by weight stirs evenly, control
Water phase container medium temperature degree is 25 DEG C；Then TAK-438 is added under stirring condition；
Emulsification：Under stirring condition, oil phase is added in water phase, obtains TAK-438 colostrums；
By colostrum as under homogenizer, homogeneous speed is：5000r/min, homogenizing time 5min, after homogeneous, are surpassed
Sonication can obtain TAK-438 nano-emulsions.
It is understood that the principle that embodiment of above is intended to be merely illustrative of the present and the exemplary implementation that uses
Mode, but the present invention is not limited thereto.For those skilled in the art, the essence of the present invention is not being departed from
In the case of refreshing and essence, various changes and modifications can be made therein, these variations and modifications are also considered as protection scope of the present invention.
Claims (1)
1. a kind of preparation method of TAK-438 nano-emulsions, it is characterised in that including following preparation process：
Prepare oil phase：10-100 parts by weight of soybean oil is added in the first container, it is 25 DEG C to control temperature in oil phase container；
Prepare water phase：The emulsifying agent of 1-5 parts by weight Tween-80s is added in second container, adds 50-500 parts by weight
Deionized water stirs evenly, and it is 25 DEG C to control water phase container medium temperature degree, and 0.5-2.5 parts by weight TAK-438 is then added under stirring condition；
Emulsification：Under stirring condition, oil phase is added in water phase, obtains TAK-438 colostrums；
Colostrum is placed under homogenizer after homogeneous, is ultrasonically treated and can obtain TAK-438 nano-emulsions, the homogeneous speed
For：3500r/min-14000r/min, homogenizing time 5min.
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| CN105663096B (en) * | 2016-01-25 | 2019-06-14 | 南京济群医药科技股份有限公司 | A kind of Wo Nuolazan oral quick-dissolving film preparation and preparation method thereof |
Citations (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN101066245A (en) * | 2007-05-25 | 2007-11-07 | 朱芳海 | Orally taken emulsion and its prepn |
| CN102470126A (en) * | 2009-07-09 | 2012-05-23 | 拉夸里亚创药株式会社 | Acid pump antagonist for treatment of diseases associated with abnormal gastrointestinal movement |
| CN103637986A (en) * | 2013-12-12 | 2014-03-19 | 挑战（天津）动物药业有限公司 | Omeprazole nano emulsion and preparation method thereof |
-
2015
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Patent Citations (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN101066245A (en) * | 2007-05-25 | 2007-11-07 | 朱芳海 | Orally taken emulsion and its prepn |
| CN102470126A (en) * | 2009-07-09 | 2012-05-23 | 拉夸里亚创药株式会社 | Acid pump antagonist for treatment of diseases associated with abnormal gastrointestinal movement |
| CN103637986A (en) * | 2013-12-12 | 2014-03-19 | 挑战（天津）动物药业有限公司 | Omeprazole nano emulsion and preparation method thereof |
Non-Patent Citations (1)
| Title |
|---|
| 1-[5-(2-Fluorophenyl)-1-(pyridin-3-ylsulfonyl)-1H-pyrrol-3-yl]-N- methylmethanamine Monofumarate (TAK-438), a Novel and Potent Potassium-Competitive Acid Blocker for the Treatment of Acid-Related Diseases;Yasunobu Hori等;《THE JOURNAL OF PHARMACOLOGY AND EXPERIMENTAL THERAPEUTICS》;20101231;第335卷(第1期);第231–238页，尤其是摘要，第232页右栏第2段 * |
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Denomination of invention: A preparation method of tak-438 nano emulsion Effective date of registration: 20220630 Granted publication date: 20180424 Pledgee: Shandong Shouguang Rural Commercial Bank Co.,Ltd. Pledgor: SHOUGUANG FUKANG PHARMACEUTICAL Co.,Ltd. Registration number: Y2022980009599 |