CN107260705A - A kind of preparation method of Aprepitant Nano capsule - Google Patents
A kind of preparation method of Aprepitant Nano capsule Download PDFInfo
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- CN107260705A CN107260705A CN201710429116.0A CN201710429116A CN107260705A CN 107260705 A CN107260705 A CN 107260705A CN 201710429116 A CN201710429116 A CN 201710429116A CN 107260705 A CN107260705 A CN 107260705A
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- China
- Prior art keywords
- aprepitant
- gelatin
- parts
- acetic acid
- capsule
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Classifications
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/48—Preparations in capsules, e.g. of gelatin, of chocolate
- A61K9/50—Microcapsules having a gas, liquid or semi-solid filling; Solid microparticles or pellets surrounded by a distinct coating layer, e.g. coated microspheres, coated drug crystals
- A61K9/51—Nanocapsules; Nanoparticles
- A61K9/5107—Excipients; Inactive ingredients
- A61K9/513—Organic macromolecular compounds; Dendrimers
- A61K9/5169—Proteins, e.g. albumin, gelatin
-
- 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
- A61K31/535—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
- A61K31/5375—1,4-Oxazines, e.g. morpholine
- A61K31/5377—1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
Abstract
The present invention relates to pharmaceutical technology field, especially a kind of preparation method of Aprepitant Nano capsule, including getting the raw materials ready, the dissolving of gelatin, the dissolving of powder Aprepitant, the configuration of acetic acid solution, the mixing of raw material and detecting step, auspicious prepared smooth Nano capsule improves auspicious smooth water solubility and bioavilability, reduce toxic side effect, improve medicine stability, during disease is treated, both it is orally available and can injection injection, because there is gelatin coatings when oral, just start to play drug effect after stomach is entered, alleviate to gastral toxic side effect, its Nano capsule diameter reaches Nano grade when injection is injected, thrombus is not resulted in the blood vessel, the place of illness can be smoothly reached with blood circulation, directly focus is acted on, it can be good at playing drug effect, having reached improves the therapeutic effect of Aprepitant medicine.
Description
Technical field
The present invention relates to pharmaceutical technology field, more particularly to a kind of preparation method of Aprepitant Nano capsule.
Background technology
Aprepitant is clinically mainly used in during the first and repetitive therapy of prevention height cause telling property anti-tumor chemotherapeutic
The acute and Delayed onset nausea and vomiting occurred.Aprepitant is not dissolved in water, is metabolized soon, and bioavilability is low, therefore controls
Dosage is larger when treating disease.Oral Aprepitant medicine is not allowed in water, absorbs slow, efficiency is low, have impact on treatment
Effect.
The content of the invention
The invention aims to solve to have oral Aprepitant medicine in the prior art not allowing in water, absorb
Slowly, efficiency is low, have impact on the shortcoming of therapeutic effect, and a kind of preparation method of the Aprepitant Nano capsule proposed.
To achieve these goals, present invention employs following technical scheme：
A kind of preparation method of Aprepitant Nano capsule is designed, is comprised the following steps：
S1, get the raw materials ready, take gelatin, distilled water, vacuumfilter, powder Aprepitant, acetic acid standby；
S2, gelatin dissolving, take 2-5 parts of gelatin in S1 to be dissolved in 70-100 parts of distilled water, in 20-24 DEG C stir at room temperature
Mix to gelatin and be swelled to form colloid, suction filtration then is carried out to colloid using vacuumfilter, the impurity in colloid is removed；
S3, powder Aprepitant dissolving, take 2-5 parts of powder Aprepitant in S1 to be dissolved in 70-100 parts of ethanol,
20-24 DEG C of stirring at room temperature is completely dissolved powder Aprepitant；
S4, acetic acid solution configuration, glacial acetic acid are dissolved in distilled water, configure 7-10% acetic acid solution；
S5, raw material mixing, take 8-14 parts of gelatin in S2 after removal of impurities to be placed in beaker, are subsequently placed in 37-40 DEG C of perseverance
Tepidarium is heated and stirred, and then takes 2-5 parts to be slowly added dropwise into gelatin solution the Aprepitant ethanol solution dissolved in S3,
The acetic acid solution of 7-10% in S4 is added, regulation pH value is then cold how to room temperature between 4.8-5.1, and then makes Aprepitant
Capsule solidifies, and obtains Nano capsule；
S6, detection, obtained nanocapsules mixture in S5 is irradiated using e-Pointer, Tyndall scattering inspection is carried out
Survey.
It is preferred that, the gelatin, in cooling, puts the condition of mixture and ice bath with Aprepitant ethanol solution mixture
Under, controller temperature is 1-4 degrees Celsius, and formaldehyde is slowly added dropwise stirs to Aprepitant capsule and be fully cured.
It is preferred that, the Aprepitant capsule after hardening, filtration sterilization processing is carried out using the filter membrane in 200nm apertures.
A kind of preparation method of Aprepitant Nano capsule proposed by the present invention, beneficial effect is：By preparing A Rui
Smooth Nano capsule improves the water solubility and bioavilability of Aprepitant, reduces toxic side effect, improves medicine stability,
During treating disease, it is both orally available and also can injection injection, because there is gelatin coatings when oral, just start hair after stomach is entered
Drug effect is waved, is alleviated to gastral toxic side effect, its Nano capsule diameter reaches Nano grade when injection is injected, in the blood vessel
Thrombus is not resulted in, the place of illness can be smoothly reached with blood circulation, directly focus is acted on, can be good at playing medicine
Effect, having reached improves the therapeutic effect of Aprepitant medicine.
Embodiment
In order to make the purpose , technical scheme and advantage of the present invention be clearer, below in conjunction with specific embodiment, to this
Invention is further elaborated.It should be appreciated that the specific embodiments described herein are merely illustrative of the present invention, not
For limiting the present invention.
Embodiment one
A kind of preparation method of Aprepitant Nano capsule, comprises the following steps：
S1, get the raw materials ready, take gelatin, distilled water, vacuumfilter, powder Aprepitant, acetic acid standby；
S2, gelatin dissolving, take 2 parts of gelatin in S1 to be dissolved in 70 parts of distilled water, in 21 DEG C of stirrings at room temperature to gelatin
It is swelled to form colloid, suction filtration then is carried out to colloid using vacuumfilter, the impurity in colloid is removed；
S3, powder Aprepitant dissolving, take 2 parts of powder Aprepitant in S1 to be dissolved in 70 parts of ethanol, at 21 DEG C
Stirring is completely dissolved powder Aprepitant at room temperature；
S4, acetic acid solution configuration, glacial acetic acid are dissolved in distilled water, the acetic acid solution of configuration 7%；
S5, raw material mixing, take 8 parts of gelatin in S2 after removal of impurities to be placed in beaker, are subsequently placed in 37 DEG C of waters bath with thermostatic control
Heat and stir, then take 2 parts to be slowly added dropwise into gelatin solution the Aprepitant ethanol solution dissolved in S3, add in S4
7% acetic acid solution, regulation pH value is then cold how to room temperature between 4.8, and then solidifies Aprepitant capsule, is received
Rice glue capsule, gelatin and Aprepitant ethanol solution mixture in cooling, put mixture with conditions of ice bath, controller temperature
For 1 degree Celsius, and formaldehyde is slowly added dropwise stirs to Aprepitant capsule and be fully cured, Aprepitant capsule after hardening, is used
The filter membrane in 200nm apertures carries out filtration sterilization processing；
S6, detection, obtained nanocapsules mixture in S5 is irradiated using e-Pointer, Tyndall scattering inspection is carried out
Survey.
Embodiment two
A kind of preparation method of Aprepitant Nano capsule, comprises the following steps：
S1, get the raw materials ready, take gelatin, distilled water, vacuumfilter, powder Aprepitant, acetic acid standby；
S2, gelatin dissolving, take 3 parts of gelatin in S1 to be dissolved in 80 parts of distilled water, in 22 DEG C of stirrings at room temperature to gelatin
It is swelled to form colloid, suction filtration then is carried out to colloid using vacuumfilter, the impurity in colloid is removed；
S3, powder Aprepitant dissolving, take 3 parts of powder Aprepitant in S1 to be dissolved in 80 parts of ethanol, at 22 DEG C
Stirring is completely dissolved powder Aprepitant at room temperature；
S4, acetic acid solution configuration, glacial acetic acid are dissolved in distilled water, the acetic acid solution of configuration 8%；
S5, raw material mixing, take 10 parts of gelatin in S2 after removal of impurities to be placed in beaker, are subsequently placed in 38 DEG C of waters bath with thermostatic control
Heat and stir, then take 3 parts to be slowly added dropwise into gelatin solution the Aprepitant ethanol solution dissolved in S3, add in S4
8% acetic acid solution, regulation pH value is then cold how to room temperature between 4.9, and then solidifies Aprepitant capsule, is received
Rice glue capsule, gelatin and Aprepitant ethanol solution mixture in cooling, put mixture with conditions of ice bath, controller temperature
For 2 degrees Celsius, and formaldehyde is slowly added dropwise stirs to Aprepitant capsule and be fully cured, Aprepitant capsule after hardening, is used
The filter membrane in 200nm apertures carries out filtration sterilization processing；
S6, detection, obtained nanocapsules mixture in S5 is irradiated using e-Pointer, Tyndall scattering inspection is carried out
Survey.
Embodiment three
A kind of preparation method of Aprepitant Nano capsule, comprises the following steps：
S1, get the raw materials ready, take gelatin, distilled water, vacuumfilter, powder Aprepitant, acetic acid standby；
S2, gelatin dissolving, take 4 parts of gelatin in S1 to be dissolved in 90 parts of distilled water, in 23 DEG C of stirrings at room temperature to gelatin
It is swelled to form colloid, suction filtration then is carried out to colloid using vacuumfilter, the impurity in colloid is removed；
S3, powder Aprepitant dissolving, take 4 parts of powder Aprepitant in S1 to be dissolved in 90 parts of ethanol, at 23 DEG C
Stirring is completely dissolved powder Aprepitant at room temperature；
S4, acetic acid solution configuration, glacial acetic acid are dissolved in distilled water, the acetic acid solution of configuration 9%；
S5, raw material mixing, take 12 parts of gelatin in S2 after removal of impurities to be placed in beaker, are subsequently placed in 39 DEG C of waters bath with thermostatic control
Heat and stir, then take 4 parts to be slowly added dropwise into gelatin solution the Aprepitant ethanol solution dissolved in S3, add in S4
9% acetic acid solution, regulation pH value is then cold how to room temperature between 5.0, and then solidifies Aprepitant capsule, is received
Rice glue capsule, gelatin and Aprepitant ethanol solution mixture in cooling, put mixture with conditions of ice bath, controller temperature
For 3 degrees Celsius, and formaldehyde is slowly added dropwise stirs to Aprepitant capsule and be fully cured, Aprepitant capsule after hardening, is used
The filter membrane in 200nm apertures carries out filtration sterilization processing；
S6, detection, obtained nanocapsules mixture in S5 is irradiated using e-Pointer, Tyndall scattering inspection is carried out
Survey.
Example IV
A kind of preparation method of Aprepitant Nano capsule, comprises the following steps：
S1, get the raw materials ready, take gelatin, distilled water, vacuumfilter, powder Aprepitant, acetic acid standby；
S2, gelatin dissolving, take 5 parts of gelatin in S1 to be dissolved in 100 parts of distilled water, in 24 DEG C of stirrings at room temperature to gelatin
It is swelled to form colloid, suction filtration then is carried out to colloid using vacuumfilter, the impurity in colloid is removed；
S3, powder Aprepitant dissolving, take 5 parts of powder Aprepitant in S1 to be dissolved in 100 parts of ethanol, at 24 DEG C
Stirring is completely dissolved powder Aprepitant at room temperature；
S4, acetic acid solution configuration, glacial acetic acid are dissolved in distilled water, the acetic acid solution of configuration 10%；
S5, raw material mixing, take 14 parts of gelatin in S2 after removal of impurities to be placed in beaker, are subsequently placed in 40 DEG C of waters bath with thermostatic control
Heat and stir, then take 5 parts to be slowly added dropwise into gelatin solution the Aprepitant ethanol solution dissolved in S3, add in S4
10% acetic acid solution, regulation pH value is then cold how to room temperature between 5.1, and then solidifies Aprepitant capsule, is received
Rice glue capsule, gelatin and Aprepitant ethanol solution mixture in cooling, put mixture with conditions of ice bath, controller temperature
For 4 degrees Celsius, and formaldehyde is slowly added dropwise stirs to Aprepitant capsule and be fully cured, Aprepitant capsule after hardening, is used
The filter membrane in 200nm apertures carries out filtration sterilization processing；
S6, detection, obtained nanocapsules mixture in S5 is irradiated using e-Pointer, Tyndall scattering inspection is carried out
Survey.
The foregoing is only a preferred embodiment of the present invention, but protection scope of the present invention be not limited thereto,
Any one skilled in the art the invention discloses technical scope in, technique according to the invention scheme and its
Inventive concept is subject to equivalent substitution or change, should all be included within the scope of the present invention.
Claims (3)
1. a kind of preparation method of Aprepitant Nano capsule, it is characterised in that comprise the following steps：
S1, get the raw materials ready, take gelatin, distilled water, vacuumfilter, powder Aprepitant, acetic acid standby；
S2, gelatin dissolving, take 2-5 parts of gelatin in S1 to be dissolved in 70-100 parts of distilled water, in 20-24 DEG C of stirring at room temperature extremely
Gelatin is swelled to form colloid, then carries out suction filtration to colloid using vacuumfilter, removes the impurity in colloid；
S3, powder Aprepitant dissolving, take 2-5 parts of powder Aprepitant in S1 to be dissolved in 70-100 parts of ethanol, in 20-24
DEG C stirring at room temperature be completely dissolved powder Aprepitant；
S4, acetic acid solution configuration, glacial acetic acid are dissolved in distilled water, configure 7-10% acetic acid solution；
S5, raw material mixing, take 8-14 parts of gelatin in S2 after removal of impurities to be placed in beaker, are subsequently placed in 37-40 DEG C of thermostatted water
Bath is heated and stirred, and then takes 2-5 parts to be slowly added dropwise into gelatin solution the Aprepitant ethanol solution dissolved in S3, is added
7-10% acetic acid solution in S4, regulation pH value is then cold how to room temperature between 4.8-5.1, and then makes Aprepitant capsule
Solidification, obtains Nano capsule；
S6, detection, obtained nanocapsules mixture in S5 is irradiated using e-Pointer, Tyndall scattering detection is carried out.
2. a kind of preparation method of Aprepitant Nano capsule according to claim 1, it is characterised in that the gelatin with
Aprepitant ethanol solution mixture puts mixture and under conditions of ice bath, controller temperature is 1-4 degrees Celsius in cooling,
And formaldehyde is slowly added dropwise stirs to Aprepitant capsule and be fully cured.
3. the preparation method of a kind of Aprepitant Nano capsule according to claim 1, it is characterised in that described A Rui
Smooth capsule after hardening, filtration sterilization processing is carried out using the filter membrane in 200nm apertures.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN201710429116.0A CN107260705A (en) | 2017-06-08 | 2017-06-08 | A kind of preparation method of Aprepitant Nano capsule |
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN201710429116.0A CN107260705A (en) | 2017-06-08 | 2017-06-08 | A kind of preparation method of Aprepitant Nano capsule |
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| Publication Number | Publication Date |
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| CN107260705A true CN107260705A (en) | 2017-10-20 |
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| Application Number | Title | Priority Date | Filing Date |
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| CN201710429116.0A Pending CN107260705A (en) | 2017-06-08 | 2017-06-08 | A kind of preparation method of Aprepitant Nano capsule |
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Citations (5)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN1617712A (en) * | 2001-12-10 | 2005-05-18 | 麦克公司 | Pharmaceutical nanoparticulate composition of a tachykinin receptor antagonist |
| CN101642448A (en) * | 2009-06-29 | 2010-02-10 | 中南民族大学 | Nano-Artesunate capsule and preparation process thereof |
| US20110009362A1 (en) * | 2008-02-27 | 2011-01-13 | Dr. Reddy's Laboratories Ltd. | Solubility-enhanced forms of aprepitant and pharmaceutical compositions thereof |
| CN104586814A (en) * | 2015-02-04 | 2015-05-06 | 山东新时代药业有限公司 | Aprepitant capsules |
| CN105878250A (en) * | 2014-10-29 | 2016-08-24 | 北京乐嘉宝医药科技有限责任公司 | Aprepitant nano composition |
-
2017
- 2017-06-08 CN CN201710429116.0A patent/CN107260705A/en active Pending
Patent Citations (5)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN1617712A (en) * | 2001-12-10 | 2005-05-18 | 麦克公司 | Pharmaceutical nanoparticulate composition of a tachykinin receptor antagonist |
| US20110009362A1 (en) * | 2008-02-27 | 2011-01-13 | Dr. Reddy's Laboratories Ltd. | Solubility-enhanced forms of aprepitant and pharmaceutical compositions thereof |
| CN101642448A (en) * | 2009-06-29 | 2010-02-10 | 中南民族大学 | Nano-Artesunate capsule and preparation process thereof |
| CN105878250A (en) * | 2014-10-29 | 2016-08-24 | 北京乐嘉宝医药科技有限责任公司 | Aprepitant nano composition |
| CN104586814A (en) * | 2015-02-04 | 2015-05-06 | 山东新时代药业有限公司 | Aprepitant capsules |
Non-Patent Citations (1)
| Title |
|---|
| 王淑华等: "阿瑞匹坦纳米胶囊的制备", 《药学研究》 * |
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Application publication date: 20171020 |
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