CN107049981A - A kind of quick-release Amisulpride pharmaceutical composition and preparation method thereof - Google Patents
A kind of quick-release Amisulpride pharmaceutical composition and preparation method thereof Download PDFInfo
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- CN107049981A CN107049981A CN201710233402.XA CN201710233402A CN107049981A CN 107049981 A CN107049981 A CN 107049981A CN 201710233402 A CN201710233402 A CN 201710233402A CN 107049981 A CN107049981 A CN 107049981A
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- Prior art keywords
- amisulpride
- pharmaceutical composition
- quick
- release
- composition according
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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
- A61K9/20—Pills, tablets, discs, rods
- A61K9/28—Dragees; Coated pills or tablets, e.g. with film or compression coating
- A61K9/2806—Coating materials
- A61K9/2833—Organic macromolecular compounds
- A61K9/286—Polysaccharides, e.g. gums; Cyclodextrin
- A61K9/2866—Cellulose; Cellulose derivatives, e.g. hydroxypropyl methylcellulose
-
- 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
- A61K31/40—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil
-
- 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
- A61K9/20—Pills, tablets, discs, rods
- A61K9/2004—Excipients; Inactive ingredients
- A61K9/2013—Organic compounds, e.g. phospholipids, fats
- A61K9/2018—Sugars, or sugar alcohols, e.g. lactose, mannitol; Derivatives thereof, e.g. polysorbates
-
- 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
- A61K9/20—Pills, tablets, discs, rods
- A61K9/2004—Excipients; Inactive ingredients
- A61K9/2022—Organic macromolecular compounds
- A61K9/2027—Organic macromolecular compounds obtained by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyvinyl pyrrolidone, poly(meth)acrylates
-
- 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
- A61K9/20—Pills, tablets, discs, rods
- A61K9/2072—Pills, tablets, discs, rods characterised by shape, structure or size; Tablets with holes, special break lines or identification marks; Partially coated tablets; Disintegrating flat shaped forms
- A61K9/2077—Tablets comprising drug-containing microparticles in a substantial amount of supporting matrix; Multiparticulate tablets
- A61K9/2081—Tablets comprising drug-containing microparticles in a substantial amount of supporting matrix; Multiparticulate tablets with microcapsules or coated microparticles according to A61K9/50
Abstract
The invention discloses a kind of quick-release Amisulpride pharmaceutical composition and preparation method thereof, said composition is included：(a), internal layer：The inertia water-insoluble support being coated by the layer of at least one layer of Amisulpride comprising Micronised form, hydrophilic polymer, surfactant；(b), outer layer：One or several outer layers, contain a kind of sweetener.This composition result of extraction is good, and quality stability is excellent, and technique is simple, beneficial to industrialization, fully ensures that medication validity and security.
Description
Technical field
The invention belongs to Amisulpride field of medicine preparations, it is related to a kind of quick-release Amisulpride pharmaceutical composition and its preparation
Method.
Background technology
Amisulpride is a kind of selective dopamine D 2 and D3 receptor antagonists by matching Norfin, Inc's exploitation, for treating
Mental disease, especially with positive symptom (for example：Delirium, illusion, cognitive disorder) and/or negative symptoms is (for example：Reaction is slow
Slow, apathy and social ability is shunk back) acute or chronic schizophrenia, also including the mental disease based on negative symptoms
Suffer from, its chemical structural formula is as follows：
Amisulpride is a kind of atypical antipsychotics, acute for class paranoiac's process schizophrenia
The treatment of absurd Rui types mental disease, it can also be used to treat schizoid defect state, remaining spiritual disease-process and with
Blunt holddown.Amisulpride is generally administered orally by the tablet form of 100,200 and 400mg of every tablet amounts.However,
During acute psychotic episode, the oral daily dosage of Amisulpride is often improved, and can reach 1200mg/day.Therefore, make
The patient treated with Amisulpride must swallow several pieces tablets daily.
Due to the special pathological state of patient, and active component Amisulpride taste is very bitter, to correctly fixed in accordance with doctor's advice
When take a large amount of tablets and can meet difficulty, or even show significant uncommunicative, influence patient medication compliance；Therefore
The sensory issues of Amisulpride oral formulations in the urgent need to address.
Amisulpride slightly soluble in water, but clinical requirement medicine Fast Stripping, rapid-onset, during this requires that preparation is produced
Drug dissolution is improved using suitable prescription and technique.
Prior art CN1842331A discloses a kind of Amisulpride solid composite medicament, comprising by lipid-coated and poly-
The Amisulpride particle that is coated of coating that compound is coated and at least one it is suitable for the pharmaceutically acceptable of intraoral scattered administration
Excipient composition.Amisulpride pharmaceutical composition prepared by the method is that the particle containing Amisulpride is wrapped up, and rule
Lattice are very big, made intraoral dispersible tablet difficulty very big, it is difficult to reach the effect of Fast Stripping, rapid-onset.
A kind of another oral formulations containing Amisulpride of prior art CN102600132A, are by active medicine Amisulpride
Cyclodextrin inclusion compound is made, is well mixed after sieving with pharmaceutically acceptable auxiliary material, using wet method or dry granulation, by gained
Particle progress tabletting obtains tablet, filling capsule obtains capsule or direct packaging obtains granule.The Amisulpride of the present invention is orally made
Agent can strengthen the water solubility of medicine, stability, mask the bitter taste of Amisulpride, improve patient medication compliance, and very big
The bioavilability of medicine is improved in degree.But its processed complex, it is to influence the key of product utility comprising rate.
The content of the invention
The present invention in order to solve the problem of Amisulpride medicine is unable to Fast Stripping, rapid-onset in the prior art there is provided
A kind of quick-release Amisulpride pharmaceutical composition and preparation method thereof.
First, the present invention provides a kind of quick-release Amisulpride pharmaceutical composition, and said composition is included：
(a), internal layer：By the layer of at least one layer of Amisulpride, hydrophilic polymer, surfactant for including Micronised form
The inertia water-insoluble support of coating；
(b), outer layer：One or several outer layers, contain a kind of sweetener.
Preferably, the hydrophilic polymer is polyvinylpyrrolidone.
Preferably, the Amisulpride and surfactant are micronized altogether.
Preferably, the surfactant is NaLS.
Preferably, the inertia water-insoluble support is lactose, and sweetener is sweetener.
Preferably, hydrophilic polymer and inertia water-insoluble support are respectively the 80%-120% of Amisulpride quality, table
Face activating agent is the 1%-2% of Amisulpride quality.Each material mass percentage is in outer layer (coating) material：
The polyvinylpyrrolidone 92.0 of crosslinking；
Microcrystalline cellulose 145.0；
Sodium stearyl fumarate 5.5；
Cataloid 3.5；
Sweetener 1.0；
Internal layer (a) weightening 1.0%-5.0% after coating.
Preferably, the Micronised form is by fluid-bed granulation.
Secondly, present invention provides the method for preparing pharmaceutical composition of the present invention, this method comprises the following steps：
(a) particle size Micronised form Amisulpride, is prepared in the solution of hydrophilic polymer and surfactant
Suspension, any one of solution in water, ethanol or hydrous ethanol；
(b), the suspension for obtaining step (a) is administered on inertia water-insoluble support；
(c) particle being achieved in that, is coated with one or several phases or layer；
Preferably, step (b) is carried out in fluidized bed pelletizer.
The present invention includes relative to the beneficial effect of prior art：
(1) it is, simple relative to prior art processes, it is easier to industry production and application；
(2), using the composition dissolution rate of the invention prepared faster, more conducively patient uses；
(3), using the composition excellent in stability for preparing of the present invention, quality is more guaranteed, beneficial to patient use it is effective
Property and security.
Embodiment
Below in conjunction with specific embodiment, invention is described in detail.
Embodiment 1
Unit (mg)
Internal layer
The Amisulpride 100.0 of micronizing；
Polyvinylpyrrolidone 80.0；
Lactose 116.0；
NaLS 2.0.
Outer layer
The polyvinylpyrrolidone 92.0 of crosslinking；
Microcrystalline cellulose 145.0；
Sodium stearyl fumarate 5.5；
Cataloid 3.5；
Sweetener 1.0.
Preparation process：
(a) particle size, is prepared in the aqueous solution of polyvinylpyrrolidone and polyvinylpyrrolidone and is less than 60 μm
The suspension of Micronised form Amisulpride；
(b), the suspension for obtaining step (a) is administered on lactose, tabletting；
(c) tablet for being coated and being achieved in that in hydrous ethanol, is dissolved in cladding material, in right amount, weightening 2%.
Embodiment 2
Unit (mg)
Internal layer
The Amisulpride 100.0 of micronizing；
Polyvinylpyrrolidone 90.0；
Lactose 106.0；
NaLS 2.0.
Outer layer
The polyvinylpyrrolidone 92.0 of crosslinking；
Microcrystalline cellulose 145.0；
Sodium stearyl fumarate 5.5；
Cataloid 3.5；
Sweetener 1.0.
Preparation process：
(a) particle size, is prepared in the aqueous solution of polyvinylpyrrolidone and polyvinylpyrrolidone and is less than 60 μm
The suspension of Micronised form Amisulpride；
(b), the suspension for obtaining step (a) is administered on lactose, tabletting；
(c) tablet for being coated and being achieved in that in hydrous ethanol, is dissolved in cladding material, in right amount, weightening 2%.
Embodiment 3
Unit (mg)
Internal layer
The Amisulpride 100.0 of micronizing；
Polyvinylpyrrolidone 90.0；
Lactose 96.0；
NaLS 1.0.
Outer layer
The polyvinylpyrrolidone 92.0 of crosslinking；
Microcrystalline cellulose 145.0；
Sodium stearyl fumarate 5.5；
Cataloid 3.5；
Sweetener 1.0.
Preparation process：
(a) particle size, is prepared in the aqueous solution of polyvinylpyrrolidone and polyvinylpyrrolidone and is less than 60 μm
The suspension of Micronised form Amisulpride；
(b), the suspension for obtaining step (a) is administered on lactose, tabletting；
(c) tablet for being coated and being achieved in that in hydrous ethanol, is dissolved in cladding material, in right amount, weightening 2%.
Table 1. not be the same as Example and reference substance solubility results in water
Test comparison and result：
(1), the comparison of Amisulpride pharmaceutical composition solubility in aqueous；
Amisulpride pharmaceutical composition, prior art and reference substance Amisulpride raw material prepared by embodiment 1-3 is each
50mg, puts in 50ml volumetric flasks, is diluted with water to scale, shakes 1 hour, is determined respectively with ultraviolet spectrophotometry molten at room temperature
Xie Du, as a result as shown in table 1：
Result of the test can be seen that present composition Amisulpride, and relative to prior art, the solubility in water is improved about
20%.
(2), the investigation of tablet prepared by Amisulpride pharmaceutical composition about material (total impurities)；
Influence factor is tested
Amisulpride tablet in Example 1-3, puts placement under the conditions of high temperature (60 DEG C) respectively, respectively at the 10th day, 20,
The relevant material result of sampling detection in 30 days is as shown in table 2：
The embodiment 1-3 of table 2 is with contrast conventional example 1 in the relevant material changing value of high temperature influence factor testing inspection
(%)
| Time | Condition | Embodiment 1 | Embodiment 2 | Embodiment 3 | CN102600132A embodiments 1 |
| 10 days | High temperature | 0.02% | 0.01% | 0.01% | 0.01% |
| 20 days | High temperature | 0.03% | 0.02% | 0.01% | 0.04% |
| 30 days | High temperature | 0.05% | 0.03% | 0.02% | 0.09% |
Result of the test can be seen that the excellent in stability of present composition Amisulpride.
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 in the technical scope of present disclosure, 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 (9)
1. a kind of quick-release Amisulpride pharmaceutical composition, said composition is included：
(a), internal layer：It is coated by the layer of at least one layer of Amisulpride comprising Micronised form, hydrophilic polymer, surfactant
Inertia water-insoluble support；
(b), outer layer：One or several outer layers, contain a kind of sweetener.
2. quick-release Amisulpride pharmaceutical composition according to claim 1, it is characterised in that：The hydrophilic polymer is poly-
Vinylpyrrolidone.
3. quick-release Amisulpride pharmaceutical composition according to claim 2, it is characterised in that：The Amisulpride and surface
Activating agent is micronized altogether.
4. quick-release Amisulpride pharmaceutical composition according to claim 3, it is characterised in that：The surfactant is the moon
Osmanthus base sodium sulphate.
5. quick-release Amisulpride pharmaceutical composition according to claim 4, it is characterised in that：The inertia water solubility is supported
Thing is lactose, and sweetener is sweetener.
6. quick-release Amisulpride pharmaceutical composition according to claim 5, it is characterised in that：
In internal layer：Hydrophilic polymer and inertia water-insoluble support are respectively the 80%-120% of Amisulpride quality；
Surfactant is the 1%-2% of Amisulpride quality；
The raw material percentage composition of outer layer coating is：
The polyvinylpyrrolidone 92.0 of crosslinking；
Microcrystalline cellulose 145.0；
Sodium stearyl fumarate 5.5；
Cataloid 3.5；
Sweetener 1.0；
Internal layer weightening 1.0%-5.0% after coating.
7. the quick-release Amisulpride pharmaceutical composition according to claim any one of 1-6, it is characterised in that：The micronizing
Form is by fluid-bed granulation.
8. the preparation method of the quick-release Amisulpride pharmaceutical composition according to claim any one of 1-6, it is characterised in that
Comprise the following steps：
(a) suspension of particle size Micronised form Amisulpride, is prepared in the solution of hydrophilic polymer and surfactant
Liquid, any one of solution in water, ethanol or hydrous ethanol；
(b), the suspension for obtaining step (a) is administered on inertia water-insoluble support；
(c) particle being achieved in that, is coated with one or several phases or layer.
9. the preparation method of quick-release Amisulpride pharmaceutical composition according to claim 8, it is characterised in that step (b)
Carried out in fluidized bed pelletizer.
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| CN201710233402.XA CN107049981A (en) | 2017-04-11 | 2017-04-11 | A kind of quick-release Amisulpride pharmaceutical composition and preparation method thereof |
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Cited By (5)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN107126422A (en) * | 2017-03-02 | 2017-09-05 | 河北龙海药业有限公司 | A kind of Amisulpride tablet and preparation method thereof |
| US10800738B2 (en) | 2017-12-05 | 2020-10-13 | Sunovion Pharmaceuticals Inc. | Crystal forms and production methods thereof |
| CN112089698A (en) * | 2020-10-23 | 2020-12-18 | 江苏阿尔法药业有限公司 | Amisulpride tablet and preparation method thereof |
| US10874639B2 (en) | 2017-12-05 | 2020-12-29 | Sunovion Pharmaceuticals Inc. | Nonracemic mixtures and uses thereof |
| US11160758B2 (en) | 2019-06-04 | 2021-11-02 | Sunovion Pharmaceuticals Inc. | Modified release formulations and uses thereof |
Citations (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN1243438A (en) * | 1997-01-17 | 2000-02-02 | 福赫尼实验室股份有限公司 | Pharmaceutical composition of fenofibrate with high biological utilizing rate |
| CN101152154A (en) * | 2006-09-29 | 2008-04-02 | 北京德众万全药物技术开发有限公司 | Hydrochloric acid dronedarone medicinal compositions for oral use and method for preparing the same |
| EP2848246A1 (en) * | 2013-09-13 | 2015-03-18 | Bayer Pharma Aktiengesellschaft | Pharmaceutical compositions containing refametinib |
-
2017
- 2017-04-11 CN CN201710233402.XA patent/CN107049981A/en active Pending
Patent Citations (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN1243438A (en) * | 1997-01-17 | 2000-02-02 | 福赫尼实验室股份有限公司 | Pharmaceutical composition of fenofibrate with high biological utilizing rate |
| CN101152154A (en) * | 2006-09-29 | 2008-04-02 | 北京德众万全药物技术开发有限公司 | Hydrochloric acid dronedarone medicinal compositions for oral use and method for preparing the same |
| EP2848246A1 (en) * | 2013-09-13 | 2015-03-18 | Bayer Pharma Aktiengesellschaft | Pharmaceutical compositions containing refametinib |
Non-Patent Citations (2)
| Title |
|---|
| L.拉赫曼，等编，北京医学院药学系，等译: "《工业药剂学的理论与实践（第二版）》", 31 July 1984, 化学工业出版社 * |
| 陈喜生: "氨磺必利片制备工艺和质量标准研究", 《中国优秀硕士学位论文全文数据库 工程科技I辑》 * |
Cited By (10)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN107126422A (en) * | 2017-03-02 | 2017-09-05 | 河北龙海药业有限公司 | A kind of Amisulpride tablet and preparation method thereof |
| CN107126422B (en) * | 2017-03-02 | 2020-07-07 | 河北龙海药业有限公司 | Amisulpride tablet and preparation method thereof |
| US10800738B2 (en) | 2017-12-05 | 2020-10-13 | Sunovion Pharmaceuticals Inc. | Crystal forms and production methods thereof |
| US10874639B2 (en) | 2017-12-05 | 2020-12-29 | Sunovion Pharmaceuticals Inc. | Nonracemic mixtures and uses thereof |
| US11370753B2 (en) | 2017-12-05 | 2022-06-28 | Sunovion Pharmaceuticals Inc. | Crystal forms and production methods thereof |
| US11517558B2 (en) | 2017-12-05 | 2022-12-06 | Sunovion Pharmaceuticals Inc. | Nonracemic mixtures and uses thereof |
| US11767293B2 (en) | 2017-12-05 | 2023-09-26 | Sunovion Pharmaceuticals Inc. | Crystal forms and production methods thereof |
| US11160758B2 (en) | 2019-06-04 | 2021-11-02 | Sunovion Pharmaceuticals Inc. | Modified release formulations and uses thereof |
| US11654113B2 (en) | 2019-06-04 | 2023-05-23 | Sunovion Pharmaceuticals Inc. | Modified release formulations and uses thereof |
| CN112089698A (en) * | 2020-10-23 | 2020-12-18 | 江苏阿尔法药业有限公司 | Amisulpride tablet and preparation method thereof |
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