CN103211751A - Medical composition containing vilazodone and preparation method thereof - Google Patents
Medical composition containing vilazodone and preparation method thereof Download PDFInfo
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- CN103211751A CN103211751A CN2013101076605A CN201310107660A CN103211751A CN 103211751 A CN103211751 A CN 103211751A CN 2013101076605 A CN2013101076605 A CN 2013101076605A CN 201310107660 A CN201310107660 A CN 201310107660A CN 103211751 A CN103211751 A CN 103211751A
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- officinal salt
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- wella oxazolone
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Abstract
The invention belongs to the technical field of medicines, and in particular relates to a medical composition which is high in stability, digestion and absorption and a preparation method thereof. The medical composition contains vilazodone or officinal salt of vilazodone and a solid matrix.
Description
Technical field
The invention belongs to medical technical field, be specially solid dispersion and preparation field thereof, particularly relate to and contain the medicine Wella oxazolone that is insoluble in water or pharmaceutical composition of its officinal salt and solid matrix and preparation method thereof.
Background technology
The Wella oxazolone is a kind of novel antidepressant, the treatment of the major depressive disorder that is used to be grown up.The Wella oxazolone is because its relatively poor dissolubility easily causes the absorption of oral administration incomplete, and bioavailability is poor.Therefore the solid preparations such as tablet, capsule, granule, powder that prepare the Wella oxazolone should at first solve the low problem of preparation stripping.
In the pharmaceutical manufacturing practice at present, be conceived to improve the dissolubility and the dissolution rate of medicine at the measure of insoluble drug more, widely the means of Ying Yonging are drug micronizations, promptly medicine is machined to micron order with means such as gas pulverizing, colloid mill, ball millings, particle diameter is generally less than 25 μ m, has only only a few drug particle particle diameter less than 1 μ m.In this range scale,, can increase the dissolution rate of medicine owing to the long-pending increase of particle surface.Except that micronization, to drug modified PEGization, saccharifying, synthesizing water-solubility prodrug, by cyclodextrin inclusion compound, adopt technology such as solid dispersion also can improve the solubility property of medicine, improve bioavailability of medicament and promote curative effect, reduce toxicity.
In above-mentioned the whole bag of tricks, the solid dispersion body method is considered to one of the most resultful method.After medicine made solid dispersion, medicine was scattered in the water-solubility carrier with molecule, colloidal state, crystallite or amorphous state.Mainly contain two class solid dispersion preparations at present, one is a fusion method, and it two is a solvent method.Because removing fully, the higher and a large amount of organic solvents of Wella oxazolone fusing point are difficult for realizing that therefore commonly used at present these two kinds are separated independent solid dispersion preparation and are not suitable for the Wella oxazolone in suitability for industrialized production.
Summary of the invention
Purpose of the present invention aims to provide a kind of Wella oxazolone compositions with good stripping property and oral absorption.Adopt fusion-solvent method solid dispersions technique, the Wella oxazolone is dispersed in the Polyethylene Glycol solid matrix with molecularity.
Present composition stable preparation process favorable reproducibility, the tissue that helps producing, and minimizing capable of reducing energy consumption is polluted.Solid dispersion compositions of the present invention through suitably pulverizing, exists with particulate form, adds suitable vehicle, can make the different dosage form that can Gong take, as oral solid formulations such as tablet, capsule, granule, dry suspension.
Solid dispersion of the present invention, its component comprises: Wella oxazolone or its officinal salt and one or more pharmaceutically useful solid matrixs.
Described solid matrix is a polyethylene glycols, preferred Macrogol 4000,6000.
The preparation method of a kind of Wella oxazolone of the present invention or its officinal salt solid dispersion comprises:
(1) solid matrix is put 70 ℃ of water-baths, heating and melting.
(2) will add in the fused solid dielectric with Wella oxazolone or its officinal salt of dissolve with ethanol,
Abundant mix homogeneously.
(3) said mixture is cooled to solid rapidly with liquid nitrogen, transfers to then that lyophilization promptly gets Wella oxazolone or its officinal salt solid dispersion in the vacuum freeze dryer.
Wella oxazolone or its officinal salt and alcoholic acid mass ratio are 1:1-50 in the described step (2).
Solid matrix in the described step (2) is a polyethylene glycols, preferred Macrogol 4000,6000.
The mass ratio of Wella oxazolone or its officinal salt and solid matrix is 1:1-50 in the described preparation method, preferred 1:1-15.
Solid dispersion pharmaceutical composition of the present invention adds suitable vehicle, can be made into for oral solid preparation, as tablet, capsule, granule etc.Solid composite medicament of the present invention is compared with the physical mixture (embodiment 1) of principal agent and adjuvant gained, has high dissolution in vitro and absorbability.
The specific embodiment
Following examples only are of the present invention further specifying, and should not be construed as limitation of the present invention.Wherein " % " is meant " weight % ".
Embodiment 1
| Hydrochloric acid Wella oxazolone | 10% |
| Lactose | 50% |
| Microcrystalline Cellulose | 39% |
| Silica sol | 0.5% |
| Magnesium stearate | 0.5% |
Preparation technology:
With hydrochloric acid Wella oxazolone, lactose, the microcrystalline Cellulose mix homogeneously behind mistake 80 mesh sieves, add then and make tablet, the heavily about 200mg of sheet after silica sol and magnesium stearate are mixed.
Embodiment 2
| Hydrochloric acid Wella oxazolone | 10% |
| PEG6000 | 10% |
| Lactose | 40% |
| Microcrystalline Cellulose | 39% |
| Silica sol | 0.5% |
| Magnesium stearate | 0.5% |
Preparation technology:
PEG6000 is put 70 ℃ of water-baths, heating and melting.To join with the hydrochloric acid Wella azoles of dissolve with ethanol among the fused PEG6000, fully mix homogeneously.Then this mixture is cooled to solid rapidly with liquid nitrogen, transfers to then in the vacuum freeze dryer, take out solid dispersion behind the 24h.The gained solid dispersion is through suitably pulverizing tabletting behind adding lactose, MCC, silica sol and the magnesium stearate mix homogeneously, the heavily about 200mg of sheet.
Embodiment 3
| Hydrochloric acid Wella oxazolone | 10% |
| PEG6000 | 50% |
| Lactose | 15% |
| Microcrystalline Cellulose | 24% |
| Silica sol | 0.5% |
| Magnesium stearate | 0.5% |
Preparation technology:
PEG6000 is put 70 ℃ of water-baths, heating and melting.To join with the hydrochloric acid Wella azoles of dissolve with ethanol among the fused PEG6000, fully mix homogeneously.Then this mixture is cooled to solid rapidly with liquid nitrogen, transfers to then in the vacuum freeze dryer, take out solid dispersion behind the 24h.The gained solid dispersion is through suitably pulverizing tabletting behind adding lactose, MCC, silica sol and the magnesium stearate mix homogeneously, the heavily about 200mg of sheet.
The dissolution test
Press dissolution method (two appendix of Chinese Pharmacopoeia version in 2000
C second method), be dissolution medium with aqueous solution 1000ml, rotating speed is 50 rev/mins.
| Time (min) | Embodiment 1 | Embodiment 2 | Embodiment 3 |
| 5 | 10.22±6.01 | 20.56±5.32 | 25.35±4.10 |
| 10 | 30.29±3.17 | 53.21±2.87 | 60.77±3.27 |
| 15 | 49.89±1.88 | 86.39±1.58 | 90.53±1.92 |
| 30 | 55.25±1.44 | 99.52±1.98 | 99.51±1.66 |
| 45 | 65.08±1.90 | 99.05±1.35 | 100.20±1.15 |
| 60 | 69.23±1.57 | 100.01±0.88 | 99.82±1.46 |
As can be seen from the above table, do not take the preparation of solid dispersion prepared, the stripping of medicine is low.And according to the hydrochloric acid Wella oxazolone solid preparation of prescription of the present invention and prepared, the dissolution height of Wella oxazolone.
Compositions of the present invention and preparation method have good dissolubility and dissolution rate.
Claims (9)
1. solid dispersion pharmaceutical composition, its component comprises: Wella oxazolone or its officinal salt and one or more pharmaceutically useful solid matrixs.
2. pharmaceutical composition as claimed in claim 1 is characterized in that: described solid matrix is a polyethylene glycols.
3. pharmaceutical composition as claimed in claim 2 is characterized in that: polyethylene glycols is Macrogol 4000 and/or polyethylene glycol 6000.
4. pharmaceutical composition as claimed in claim 1 is characterized in that: the mass ratio of Wella oxazolone or its officinal salt and solid matrix is 1:1-50.
5. pharmaceutical composition as claimed in claim 4 is characterized in that: the mass ratio of Wella oxazolone or its officinal salt and solid matrix is 1:1-15.
6. the preparation method of a Wella oxazolone or its officinal salt solid dispersion comprises:
(1) solid matrix is put 70 ℃ of water-baths, heating and melting;
(2) will add in the fused solid dielectric with Wella oxazolone or its officinal salt of dissolve with ethanol, fully mix homogeneously;
(3) said mixture is cooled to solid rapidly with liquid nitrogen, transfers to then that lyophilization promptly gets Wella oxazolone or its officinal salt solid dispersion in the vacuum freeze dryer.
7. the preparation method of a kind of Wella oxazolone as claimed in claim 6 or its officinal salt solid dispersion is characterized in that: Wella oxazolone or its officinal salt and alcoholic acid mass ratio are 1:1-50 in the described step (2).
8. the preparation method of a kind of Wella oxazolone as claimed in claim 6 or its officinal salt solid dispersion, it is characterized in that: the solid matrix in the described step (2) is a polyethylene glycols, and the mass ratio of Wella oxazolone or its officinal salt and solid matrix is 1:1-50.
9. the preparation method of a kind of Wella oxazolone as claimed in claim 8 or its officinal salt solid dispersion, it is characterized in that: polyethylene glycols is Macrogol 4000 and/or polyethylene glycol 6000, and the mass ratio of Wella oxazolone or its officinal salt and solid matrix is 1:1-15.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN2013101076605A CN103211751A (en) | 2013-03-30 | 2013-03-30 | Medical composition containing vilazodone and preparation method thereof |
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN2013101076605A CN103211751A (en) | 2013-03-30 | 2013-03-30 | Medical composition containing vilazodone and preparation method thereof |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| CN103211751A true CN103211751A (en) | 2013-07-24 |
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Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CN2013101076605A Pending CN103211751A (en) | 2013-03-30 | 2013-03-30 | Medical composition containing vilazodone and preparation method thereof |
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Cited By (6)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN104983711A (en) * | 2015-06-27 | 2015-10-21 | 万特制药(海南)有限公司 | Vilazodone hydrochloride capsule composition |
| CN105832737A (en) * | 2016-06-10 | 2016-08-10 | 青岛科瑞元生物科技有限公司 | Vilazodone-containing pharmaceutical composition and application thereof |
| CN106580895A (en) * | 2016-12-07 | 2017-04-26 | 万全万特制药（厦门）有限公司 | Orally disintegrating tablet containing vilazodone hydrochloride solid dispersions and preparation method thereof |
| CN106667939A (en) * | 2017-02-14 | 2017-05-17 | 万全万特制药（厦门）有限公司 | Orally disintegrating tablet containing vilazodone hydrochloride and preparation method thereof |
| WO2018082557A1 (en) * | 2016-11-02 | 2018-05-11 | Sunshine Lake Pharma Co., Ltd. | Vilazodone inclusion complexes, compositions and preparation thereof |
| WO2020119701A1 (en) * | 2018-12-13 | 2020-06-18 | 广东东阳光药业有限公司 | Vilazodone solid dispersion and preparation method therefor |
Citations (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN102219783A (en) * | 2011-05-05 | 2011-10-19 | 天津市汉康医药生物技术有限公司 | Vilazodone hydrochloride and composition thereof |
| WO2012131706A1 (en) * | 2011-03-20 | 2012-10-04 | Cadila Healthcare Limited | Amorphous form of vilazodone hydrochloride and process for its preparation |
| CN102860993A (en) * | 2012-10-16 | 2013-01-09 | 北京诚创思达医药科技有限公司 | Hydrochloric acid vilazodone quick-release tablet and preparation method thereof |
| CN102949364A (en) * | 2011-08-30 | 2013-03-06 | 天津药物研究院 | Sustained release tablet containing effective component hydrochloric acid vilazodone |
-
2013
- 2013-03-30 CN CN2013101076605A patent/CN103211751A/en active Pending
Patent Citations (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2012131706A1 (en) * | 2011-03-20 | 2012-10-04 | Cadila Healthcare Limited | Amorphous form of vilazodone hydrochloride and process for its preparation |
| CN102219783A (en) * | 2011-05-05 | 2011-10-19 | 天津市汉康医药生物技术有限公司 | Vilazodone hydrochloride and composition thereof |
| CN102949364A (en) * | 2011-08-30 | 2013-03-06 | 天津药物研究院 | Sustained release tablet containing effective component hydrochloric acid vilazodone |
| CN102860993A (en) * | 2012-10-16 | 2013-01-09 | 北京诚创思达医药科技有限公司 | Hydrochloric acid vilazodone quick-release tablet and preparation method thereof |
Cited By (13)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN104983711A (en) * | 2015-06-27 | 2015-10-21 | 万特制药(海南)有限公司 | Vilazodone hydrochloride capsule composition |
| CN105832737A (en) * | 2016-06-10 | 2016-08-10 | 青岛科瑞元生物科技有限公司 | Vilazodone-containing pharmaceutical composition and application thereof |
| CN105832737B (en) * | 2016-06-10 | 2019-04-16 | 青岛海盈智高新技术有限公司 | A kind of pharmaceutical composition and its application comprising vilazodone |
| US10688090B2 (en) | 2016-11-02 | 2020-06-23 | Sunshine Lake Pharma Co., Ltd. | Vilazodone inclusion complexes, compositions and preparation thereof |
| WO2018082557A1 (en) * | 2016-11-02 | 2018-05-11 | Sunshine Lake Pharma Co., Ltd. | Vilazodone inclusion complexes, compositions and preparation thereof |
| CN109922807A (en) * | 2016-11-02 | 2019-06-21 | 广东东阳光药业有限公司 | Vilazodone inclusion compound and combinations thereof and preparation method |
| US11517569B2 (en) | 2016-11-02 | 2022-12-06 | Sunshine Lake Pharma Co., Ltd. | Vilazodone inclusion complexes, compositions and preparation thereof |
| CN106580895A (en) * | 2016-12-07 | 2017-04-26 | 万全万特制药（厦门）有限公司 | Orally disintegrating tablet containing vilazodone hydrochloride solid dispersions and preparation method thereof |
| CN106667939A (en) * | 2017-02-14 | 2017-05-17 | 万全万特制药（厦门）有限公司 | Orally disintegrating tablet containing vilazodone hydrochloride and preparation method thereof |
| CN113164394A (en) * | 2018-12-13 | 2021-07-23 | 广东东阳光药业有限公司 | Vilazodone solid dispersion and preparation method thereof |
| CN113164473A (en) * | 2018-12-13 | 2021-07-23 | 广东东阳光药业有限公司 | Vilazodone solid dispersion and preparation method thereof |
| WO2020119701A1 (en) * | 2018-12-13 | 2020-06-18 | 广东东阳光药业有限公司 | Vilazodone solid dispersion and preparation method therefor |
| CN113164394B (en) * | 2018-12-13 | 2023-06-23 | 广东东阳光药业有限公司 | Vilazodone solid dispersion and preparation method thereof |
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Application publication date: 20130724 |
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