CN106822016A - A kind of quetiapine fumarate sustained release pharmaceutical composition and preparation method thereof - Google Patents
A kind of quetiapine fumarate sustained release pharmaceutical composition and preparation method thereof Download PDFInfo
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- CN106822016A CN106822016A CN201710241340.7A CN201710241340A CN106822016A CN 106822016 A CN106822016 A CN 106822016A CN 201710241340 A CN201710241340 A CN 201710241340A CN 106822016 A CN106822016 A CN 106822016A
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- medicine
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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
- A61K9/0002—Galenical forms characterised by the drug release technique; Application systems commanded by energy
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- 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
- A61K31/55—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole
- A61K31/554—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole having at least one nitrogen and one sulfur as ring hetero atoms, e.g. clothiapine, diltiazem
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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
- A61K9/284—Organic macromolecular compounds obtained by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyvinyl pyrrolidone
- A61K9/2846—Poly(meth)acrylates
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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
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Abstract
The invention discloses a kind of sustained release pharmaceutical composition of quetiapine fumarate and preparation method thereof, the sustained release pharmaceutical composition includes medicine-releasing system I and medicine-releasing system II, wherein：Medicine-releasing system I includes quetiapine fumarate, filler, disintegrant, adhesive, lubricant and antiplastering aid；Medicine-releasing system II includes quetiapine fumarate, slow-release material, pore-foaming agent, adhesive, lubricant and antiplastering aid；The pharmaceutical composition also includes a separation layer, and the separation layer is mainly made up of isolated material, and isolated material is selected from the one kind in acrylic resin copolymer, cellulose acetate.The pharmaceutical composition both can be with quick acting, continuous and effective in 24 hours is can ensure that again, maximum plasma concentration can also be reduced on the basis of effective blood drug concentration is ensured simultaneously, patient compliance is improved on the premise of not lessening the curative effect so as to solve, improve drug safety.
Description
Technical field
The invention belongs to quetiapine fumarate field of medicine preparations, and in particular to a kind of quetiapine fumarate slow releasing pharmaceutical group
Compound and preparation method thereof.
Background technology
Sustained-release preparation refers to purposefully Drug controlled release to reach a class new formulation of rational therapy effect, and it makes
Human body obtains stable therapeutic plasma concentrations, optimizes therapeutic dose.It reduces medicining times compared with common oral preparation,
The curative effect of routine dose can be reached with the dosage smaller than routine dose, the accumulated dose of medication is reduced, the compliance of patient is improved；
And with making haemoconcentration steady, it is to avoid peak valley phenomenon, the features such as advantageously reduce the adverse reaction of medicine.
Quetiapine, English name：Quetiapine, is a kind of atypical antipsychotic agents, and its structure is similar to Clozapine, category
In two Benzodiazepines derivatives, now with SEROQUEL (Seroquel) for trade name is listed, its chemical structural formula is as follows：
Prior art is more for the sustained-release preparation research of Quetiapine, but belongs to the replacement of supplementary material, and grain mostly
The restriction in footpath.Such as prior art CN1219879A discloses Quetiapine or its pharmaceutically acceptable salt, pharmaceutically acceptable
Excipient, and the Hydroxypropyl methylcellulose of 5-50% (weight) sustained release preparation.
For another example, CN101347413A discloses the quetiapine sustained release system of the sustained-release matrix material containing pH dependent solubilities
Agent, the sustained-release matrix material dissolves rapidly when pH is not less than 5.
For another example, CN101002737A discloses the sustained release preparation containing Quetiapine and sustained release framework material and additives, its
Middle medicine：Sustained-release matrix material=1:0.1~1:10.
Further, CN101912374A discloses a kind of quetiapine sustained release tablet, and it is comprised at least as the quinoline of active component
Sulphur is put down or its pharmaceutically acceptable salt, used as the ethyl cellulose of sustained-release matrix material, and low viscous water soluble adhesive
The average grain diameter of agent, wherein ethyl cellulose is no more than 80 μm.
It is still to need to solve at present in order to simplify the prescription of pharmaceutical preparation, it is ensured that the human tolerance of auxiliary material and compliance
Problem, the present invention based on this and propose.
The content of the invention
It is an object of the invention to provide a kind of multilayer medicine composition containing quick-release and sustained release composition, the drug regimen
Thing both can again can ensure that continuous and effective in 24 hours with quick acting, while can also be on the basis for ensuring effective blood drug concentration
Upper reduction maximum plasma concentration, patient compliance is improved so as to solve on the premise of not lessening the curative effect, and improves drug safety
Property.
Primary and foremost purpose of the invention is to provide a kind of sustained release pharmaceutical composition of quetiapine fumarate, and said composition includes
Medicine-releasing system I and medicine-releasing system II, wherein：
Medicine-releasing system I includes quetiapine fumarate, filler, disintegrant, adhesive, lubricant and antiplastering aid；
Medicine-releasing system II includes quetiapine fumarate, slow-release material, pore-foaming agent, adhesive, lubricant and antiplastering aid.
The pharmaceutical composition also includes a separation layer, and the separation layer is mainly made up of isolated material, and isolated material is selected from
One kind in acrylic resin copolymer, cellulose acetate.
Preferably, the quality that the quetiapine fumarate is counted with Quetiapine as 200mg~300mg, D90 is less than 50 μm；Its
Described in quetiapine fumarate is counted with Quetiapine in medicine-releasing system I quality as 40mg~90mg.
Preferably, the filler is selected from microcrystalline cellulose, lactose, mannitol, pregelatinized starch, calcium monohydrogen phosphate, sulfuric acid
One or more in calcium；
The disintegrant is selected from sodium carboxymethyl starch, sodium starch glycolate, low-substituted hydroxypropyl cellulose, the poly- second of crosslinking
One or more in alkene pyrrolidone, cross-linked carboxymethyl cellulose sodium；
Described adhesive is selected from one or more in hydroxypropyl methyl cellulose, hydroxypropyl cellulose；
The lubricant is selected from superfine silica gel powder, talcum powder, magnesium stearate, calcium stearate, fumaric acid odium stearate
Plant or various；
The antiplastering aid is selected from one or more in superfine silica gel powder, talcum powder, starch；
The slow-release material be selected from hydroxypropyl methyl cellulose, hydroxypropyl cellulose, methylcellulose, ethyl cellulose,
One or more in polyoxyethylene, hydroxyethyl cellulose；
The pore-foaming agent is selected from one or more in mannitol, sucrose, lactose.
Preferably, in medicine-releasing system I, weight content of the selected filler loading in medicine-releasing system I be 15%~
50%；Weight content of the selected disintegrant consumption in medicine-releasing system I is 1.5%~7%；Selected binder dosage is in drug release system
Weight content in system I is 1%~4%；Weight content of the selected lubricant quantity in medicine-releasing system I is 0.5%~3%；
Weight content of the selected anti-stick agent level in medicine-releasing system I is 0.5%~3%.
Preferably, in medicine-releasing system II, weight content of the selected slow-release material consumption in medicine-releasing system II is 20%
~70%；Weight content of the selected pore-foaming agent consumption in medicine-releasing system II is 2%~10%；Selected binder dosage is in drug release
Weight content in system II is 1.5%~10%；Weight content of the selected lubricant quantity in medicine-releasing system II is 0.5%
~5%；Weight content of the selected anti-stick agent level in medicine-releasing system II is 0.5%~5%.
It is still another object of the present invention to provide a kind of preparation method of the sustained release pharmaceutical composition, including following step
Suddenly：
Medicine-releasing system I and II are respectively adopted appropriate solvent and are made dry particle or powder；
The isolated material of medicine-releasing system I mass 10%~12% is taken as separation layer；
Above-mentioned substance is pressed into by multilayer tablet using multilayer tablet press machine again, and multilayer tablet to obtaining is coated.
The present invention is relative to the beneficial effect of prior art：
(1), quetiapine fumarate sustained release pharmaceutical composition of the invention, both can again be can ensure that 24 hours with quick acting
Interior continuous and effective, while maximum plasma concentration can also be reduced on the basis of effective blood drug concentration is ensured, so as to solve
Patient compliance is improved on the premise of not lessening the curative effect, drug safety is improved.
(2), quetiapine fumarate sustained release pharmaceutical composition of the invention uses this area solid pharmaceutical preparation conventional method
Prepare, preparation technology is more simple, it is easy to reappear, the quality stability of product is excellent.
(3), quetiapine fumarate sustained release pharmaceutical composition of the invention uses acrylic resin copolymer, cellulose acetate
The prominent of medicine had both effectively been intercepted as separation layer to release, and reaction in the stomach of medicine, and drug induced poor appetite had been reduced again,
Enhancing patient compliance.
Brief description of the drawings
Fig. 1 is multilayer medicine composition schematic diagram of the present invention；
Wherein, each layer only represents the composition situation of each layer in figure, and the actual size and consumption situation of each layer are not represented；
Fig. 2 is the medicament slow release curve of the scheme of the embodiment of the present invention 1.
Specific embodiment
Below in conjunction with the drawings and specific embodiments, invention is described in detail.
Embodiment 1：
According to following prescription
The specification of table 1：200mg
The preparation method includes：Medicine-releasing system I and II are respectively adopted the ethanol water solvent system of appropriate volume ratio 30/70
Into dry particle, the acrylic resin copolymer of medicine-releasing system I mass 10% is added as separation layer, then using many laminates
Machine is pressed into multilayer tablet, and the tablet is coated using Opadry, and increase weight 3%, tablet configuration reference picture 1 after coating.Dissolution
With reference to Chinese Pharmacopoeia two annex XD the first methods of drug release determination of version in 2015, using Chinese Pharmacopoeia four general rule mesh of version in 2015
The device of 0931 dissolution rate and the method for drug release determination method second under secondary item, 900mL water is dissolution medium, and rotating speed is 50r/min, temperature
It is 37 DEG C to spend, and is operated in accordance with the law, is measured by sampling respectively at 0.5,0.75,1,2,4,6,8,10,12,14,18 and 24h.
Reference picture 2, knowable to release profiles, the pharmaceutical composition both can again can ensure that and held in 24 hours with quick acting
It is continuous effective, while maximum plasma concentration can also be reduced on the basis of effective blood drug concentration is ensured, do not dropped so as to solve
Patient compliance is improved on the premise of low curative effect, drug safety is improved.
Embodiment 2：
According to following prescription
The specification of table 2：200mg
The preparation method includes：Medicine-releasing system I and II are respectively adopted the ethanol water solvent system of appropriate volume ratio 30/70
Into dry particle, the cellulose acetate of medicine-releasing system I mass 12% is added as separation layer, then using multilayer tablet press machine compacting
Into multilayer tablet, the tablet is coated using Opadry, increases weight 3% after coating, shown in tablet configuration reference picture 1.Release is bent
Line is basic consistent with embodiment 1.
Embodiment 3：
According to following prescription
The specification of table 3：200mg
The preparation method includes：Medicine-releasing system I and II are respectively adopted the ethanol water solvent system of appropriate volume ratio 30/70
Into dry particle, the cellulose acetate of medicine-releasing system I mass 10% is added as separation layer, then using multilayer tablet press machine compacting
Into multilayer tablet, the tablet is coated using Opadry, increases weight 3% after coating, shown in tablet configuration reference picture 1.Release is bent
Line is basic consistent with embodiment 1.
Test result contrasts (study on the stability)
Quetiapine fumarate sustained-release tablets in Example 1-3, aluminium-plastic bubble plate packing, 40 ± 2 DEG C, relative humidity 75 ±
Placed under the conditions of 5% constant temperature and humidity, the relevant material of detection and content were sampled with 3 months respectively at 0,1,2, testing result see the table below
4。
Table 4
Visible from the above, pharmaceutical composition quality stability of the invention is excellent, meets the requirement of medicinal application.
Above-described embodiment is the present invention preferably implementation method, but embodiments of the present invention are not by above-described embodiment
Limitation, it is other it is any without departing from Spirit Essence of the invention and the change, modification, replacement made under principle, combine, simplification,
Equivalent substitute mode is should be, is included within protection scope of the present invention.
Claims (6)
1. a kind of sustained release pharmaceutical composition of quetiapine fumarate, it is characterised in that said composition includes medicine-releasing system I and drug release
System II, wherein：
Medicine-releasing system I includes quetiapine fumarate, filler, disintegrant, adhesive, lubricant and antiplastering aid；
Medicine-releasing system II includes quetiapine fumarate, slow-release material, pore-foaming agent, adhesive, lubricant and antiplastering aid.
The pharmaceutical composition also includes a separation layer, and the separation layer is mainly made up of isolated material, and isolated material is selected from propylene
One kind in acid resin copolymer, cellulose acetate.
2. sustained release pharmaceutical composition according to claim 1, it is characterised in that the quetiapine fumarate is in terms of Quetiapine
Quality is 200mg~300mg, and D90 is less than 50 μm；Quetiapine fumarate quality in terms of Quetiapine in wherein described medicine-releasing system I
It is 40mg~90mg.
3. sustained release pharmaceutical composition according to claim 1 and 2, it is characterised in that the filler is selected from microcrystalline cellulose
One or more in element, lactose, mannitol, pregelatinized starch, calcium monohydrogen phosphate, calcium sulfate；
The disintegrant is selected from sodium carboxymethyl starch, sodium starch glycolate, low-substituted hydroxypropyl cellulose, crosslinked polyethylene pyrrole
One or more in pyrrolidone, cross-linked carboxymethyl cellulose sodium；
Described adhesive is selected from one or more in hydroxypropyl methyl cellulose, hydroxypropyl cellulose；
The lubricant be selected from superfine silica gel powder, talcum powder, magnesium stearate, calcium stearate, fumaric acid odium stearate in one kind or
It is various；
The antiplastering aid is selected from one or more in superfine silica gel powder, talcum powder, starch；
The slow-release material is selected from hydroxypropyl methyl cellulose, hydroxypropyl cellulose, methylcellulose, ethyl cellulose, polyoxy
One or more in ethene, hydroxyethyl cellulose；
The pore-foaming agent is selected from one or more in mannitol, sucrose, lactose.
4. sustained release pharmaceutical composition according to claim 3, it is characterised in that in medicine-releasing system I, selected filler is used
It is 15%~50% to measure the weight content in medicine-releasing system I；Weight content of the selected disintegrant consumption in medicine-releasing system I be
1.5%~7%；Weight content of the selected binder dosage in medicine-releasing system I is 1%~4%；Selected lubricant quantity is being released
Weight content in medicine system I is 0.5%~3%；Weight content of the selected anti-stick agent level in medicine-releasing system I is 0.5%
~3%.
5. sustained release pharmaceutical composition according to claim 3, it is characterised in that in medicine-releasing system II, selected sustained release material
Weight content of the material consumption in medicine-releasing system II is 20%~70%；Weight of the selected pore-foaming agent consumption in medicine-releasing system II
Content is 2%~10%；Weight content of the selected binder dosage in medicine-releasing system II is 1.5%~10%；Selected lubrication
Weight content of the agent consumption in medicine-releasing system II is 0.5%~5%；Weight of the selected anti-stick agent level in medicine-releasing system II
Content is 0.5%~5%.
6. according to any one of Claims 1 to 5 sustained release pharmaceutical composition preparation method, it is characterised in that including with
Lower step：
Medicine-releasing system I and II are respectively adopted appropriate solvent and are made dry particle or powder；
The isolated material of medicine-releasing system I mass 10%~12% is taken as separation layer；
Above-mentioned material is pressed into by multilayer tablet using multilayer tablet press machine again, and multilayer tablet to obtaining is coated.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN201710241340.7A CN106822016A (en) | 2017-04-13 | 2017-04-13 | A kind of quetiapine fumarate sustained release pharmaceutical composition and preparation method thereof |
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN201710241340.7A CN106822016A (en) | 2017-04-13 | 2017-04-13 | A kind of quetiapine fumarate sustained release pharmaceutical composition and preparation method thereof |
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| CN106822016A true CN106822016A (en) | 2017-06-13 |
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| CN201710241340.7A Pending CN106822016A (en) | 2017-04-13 | 2017-04-13 | A kind of quetiapine fumarate sustained release pharmaceutical composition and preparation method thereof |
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Citations (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN101347413A (en) * | 2008-07-22 | 2009-01-21 | 济南百诺医药科技开发有限公司 | Quetiapine sustained release tablets and method of preparing the same |
| CN105998026A (en) * | 2015-03-26 | 2016-10-12 | 四川海思科制药有限公司 | Ticagrelor pharmaceutical composition and preparing method thereof |
-
2017
- 2017-04-13 CN CN201710241340.7A patent/CN106822016A/en active Pending
Patent Citations (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN101347413A (en) * | 2008-07-22 | 2009-01-21 | 济南百诺医药科技开发有限公司 | Quetiapine sustained release tablets and method of preparing the same |
| CN105998026A (en) * | 2015-03-26 | 2016-10-12 | 四川海思科制药有限公司 | Ticagrelor pharmaceutical composition and preparing method thereof |
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Application publication date: 20170613 |