CN104546800A - Quetiapine fumarate sustained-release capsule and preparation method thereof - Google Patents
Quetiapine fumarate sustained-release capsule and preparation method thereof Download PDFInfo
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- CN104546800A CN104546800A CN201510005598.8A CN201510005598A CN104546800A CN 104546800 A CN104546800 A CN 104546800A CN 201510005598 A CN201510005598 A CN 201510005598A CN 104546800 A CN104546800 A CN 104546800A
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- quetiapine fumarate
- slow releasing
- releasing capsule
- hydroxypropyl methylcellulose
- binding agent
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- ABFPKTQEQNICFT-UHFFFAOYSA-M 2-chloro-1-methylpyridin-1-ium;iodide Chemical compound [I-].C[N+]1=CC=CC=C1Cl ABFPKTQEQNICFT-UHFFFAOYSA-M 0.000 title claims abstract description 50
- 229960005197 quetiapine fumarate Drugs 0.000 title claims abstract description 50
- 239000002775 capsule Substances 0.000 title claims abstract description 44
- 238000002360 preparation method Methods 0.000 title claims abstract description 23
- 238000013268 sustained release Methods 0.000 title claims abstract description 11
- 239000012730 sustained-release form Substances 0.000 title claims abstract description 11
- 239000011159 matrix material Substances 0.000 claims abstract description 10
- 201000000980 schizophrenia Diseases 0.000 claims abstract description 4
- 239000001866 hydroxypropyl methyl cellulose Substances 0.000 claims description 20
- 229920003088 hydroxypropyl methyl cellulose Polymers 0.000 claims description 20
- 235000010979 hydroxypropyl methyl cellulose Nutrition 0.000 claims description 20
- UFVKGYZPFZQRLF-UHFFFAOYSA-N hydroxypropyl methyl cellulose Chemical compound OC1C(O)C(OC)OC(CO)C1OC1C(O)C(O)C(OC2C(C(O)C(OC3C(C(O)C(O)C(CO)O3)O)C(CO)O2)O)C(CO)O1 UFVKGYZPFZQRLF-UHFFFAOYSA-N 0.000 claims description 20
- 239000001856 Ethyl cellulose Substances 0.000 claims description 16
- ZZSNKZQZMQGXPY-UHFFFAOYSA-N Ethyl cellulose Chemical compound CCOCC1OC(OC)C(OCC)C(OCC)C1OC1C(O)C(O)C(OC)C(CO)O1 ZZSNKZQZMQGXPY-UHFFFAOYSA-N 0.000 claims description 16
- 229920001249 ethyl cellulose Polymers 0.000 claims description 16
- 235000019325 ethyl cellulose Nutrition 0.000 claims description 16
- NINIDFKCEFEMDL-UHFFFAOYSA-N Sulfur Chemical compound [S] NINIDFKCEFEMDL-UHFFFAOYSA-N 0.000 claims description 15
- 239000011230 binding agent Substances 0.000 claims description 15
- 239000011593 sulfur Substances 0.000 claims description 15
- 229910052717 sulfur Inorganic materials 0.000 claims description 15
- 239000007779 soft material Substances 0.000 claims description 12
- 239000000945 filler Substances 0.000 claims description 11
- 239000000314 lubricant Substances 0.000 claims description 11
- 239000000203 mixture Substances 0.000 claims description 11
- 229920000168 Microcrystalline cellulose Polymers 0.000 claims description 10
- FPAFDBFIGPHWGO-UHFFFAOYSA-N dioxosilane;oxomagnesium;hydrate Chemical compound O.[Mg]=O.[Mg]=O.[Mg]=O.O=[Si]=O.O=[Si]=O.O=[Si]=O.O=[Si]=O FPAFDBFIGPHWGO-UHFFFAOYSA-N 0.000 claims description 10
- 239000008108 microcrystalline cellulose Substances 0.000 claims description 10
- 235000019813 microcrystalline cellulose Nutrition 0.000 claims description 10
- 229940016286 microcrystalline cellulose Drugs 0.000 claims description 10
- 239000006187 pill Substances 0.000 claims description 9
- WHNWPMSKXPGLAX-UHFFFAOYSA-N N-Vinyl-2-pyrrolidone Chemical group C=CN1CCCC1=O WHNWPMSKXPGLAX-UHFFFAOYSA-N 0.000 claims description 8
- 229920003081 Povidone K 30 Polymers 0.000 claims description 8
- 238000001035 drying Methods 0.000 claims description 7
- 238000001125 extrusion Methods 0.000 claims description 7
- 239000000463 material Substances 0.000 claims description 7
- 238000005563 spheronization Methods 0.000 claims description 7
- VYPSYNLAJGMNEJ-UHFFFAOYSA-N Silicium dioxide Chemical compound O=[Si]=O VYPSYNLAJGMNEJ-UHFFFAOYSA-N 0.000 claims description 6
- 239000012530 fluid Substances 0.000 claims description 6
- 230000002209 hydrophobic effect Effects 0.000 claims description 6
- 238000002156 mixing Methods 0.000 claims description 6
- 239000003795 chemical substances by application Substances 0.000 claims description 5
- 238000012216 screening Methods 0.000 claims description 5
- XLYOFNOQVPJJNP-UHFFFAOYSA-N water Substances O XLYOFNOQVPJJNP-UHFFFAOYSA-N 0.000 claims description 5
- HQKMJHAJHXVSDF-UHFFFAOYSA-L magnesium stearate Chemical compound [Mg+2].CCCCCCCCCCCCCCCCCC([O-])=O.CCCCCCCCCCCCCCCCCC([O-])=O HQKMJHAJHXVSDF-UHFFFAOYSA-L 0.000 claims description 4
- 239000000825 pharmaceutical preparation Substances 0.000 claims description 3
- 239000000377 silicon dioxide Substances 0.000 claims description 3
- 235000012239 silicon dioxide Nutrition 0.000 claims description 3
- 102220487426 Actin-related protein 2/3 complex subunit 3_K15M_mutation Human genes 0.000 claims description 2
- LFQSCWFLJHTTHZ-UHFFFAOYSA-N Ethanol Chemical compound CCO LFQSCWFLJHTTHZ-UHFFFAOYSA-N 0.000 claims description 2
- GUBGYTABKSRVRQ-QKKXKWKRSA-N Lactose Natural products OC[C@H]1O[C@@H](O[C@H]2[C@H](O)[C@@H](O)C(O)O[C@@H]2CO)[C@H](O)[C@@H](O)[C@H]1O GUBGYTABKSRVRQ-QKKXKWKRSA-N 0.000 claims description 2
- NKWPZUCBCARRDP-UHFFFAOYSA-L calcium bicarbonate Chemical compound [Ca+2].OC([O-])=O.OC([O-])=O NKWPZUCBCARRDP-UHFFFAOYSA-L 0.000 claims description 2
- 229910000020 calcium bicarbonate Inorganic materials 0.000 claims description 2
- 239000008101 lactose Substances 0.000 claims description 2
- 235000019359 magnesium stearate Nutrition 0.000 claims description 2
- 239000002994 raw material Substances 0.000 claims description 2
- 239000001509 sodium citrate Substances 0.000 claims description 2
- NLJMYIDDQXHKNR-UHFFFAOYSA-K sodium citrate Chemical compound O.O.[Na+].[Na+].[Na+].[O-]C(=O)CC(O)(CC([O-])=O)C([O-])=O NLJMYIDDQXHKNR-UHFFFAOYSA-K 0.000 claims description 2
- 239000002904 solvent Substances 0.000 claims description 2
- 230000000694 effects Effects 0.000 abstract description 4
- 239000008188 pellet Substances 0.000 abstract description 3
- 231100000331 toxic Toxicity 0.000 abstract description 2
- 230000002588 toxic effect Effects 0.000 abstract description 2
- 239000003814 drug Substances 0.000 description 13
- 229940079593 drug Drugs 0.000 description 11
- VZCYOOQTPOCHFL-OWOJBTEDSA-N Fumaric acid Chemical compound OC(=O)\C=C\C(O)=O VZCYOOQTPOCHFL-OWOJBTEDSA-N 0.000 description 10
- 238000005516 engineering process Methods 0.000 description 6
- 239000001530 fumaric acid Substances 0.000 description 5
- 238000000034 method Methods 0.000 description 5
- VZCYOOQTPOCHFL-UHFFFAOYSA-N trans-butenedioic acid Natural products OC(=O)C=CC(O)=O VZCYOOQTPOCHFL-UHFFFAOYSA-N 0.000 description 5
- 239000003826 tablet Substances 0.000 description 4
- 238000012360 testing method Methods 0.000 description 4
- 239000007864 aqueous solution Substances 0.000 description 3
- 230000000561 anti-psychotic effect Effects 0.000 description 2
- 210000004556 brain Anatomy 0.000 description 2
- VYFYYTLLBUKUHU-UHFFFAOYSA-N dopamine Chemical compound NCCC1=CC=C(O)C(O)=C1 VYFYYTLLBUKUHU-UHFFFAOYSA-N 0.000 description 2
- 229960004667 ethyl cellulose Drugs 0.000 description 2
- 210000001035 gastrointestinal tract Anatomy 0.000 description 2
- 239000000243 solution Substances 0.000 description 2
- 239000000126 substance Substances 0.000 description 2
- OTEKOJQFKOIXMU-UHFFFAOYSA-N 1,4-bis(trichloromethyl)benzene Chemical group ClC(Cl)(Cl)C1=CC=C(C(Cl)(Cl)Cl)C=C1 OTEKOJQFKOIXMU-UHFFFAOYSA-N 0.000 description 1
- 102000040125 5-hydroxytryptamine receptor family Human genes 0.000 description 1
- 108091032151 5-hydroxytryptamine receptor family Proteins 0.000 description 1
- 101150049660 DRD2 gene Proteins 0.000 description 1
- 229920003157 Eudragit® RL 30 D Polymers 0.000 description 1
- 229920000881 Modified starch Polymers 0.000 description 1
- DOOTYTYQINUNNV-UHFFFAOYSA-N Triethyl citrate Chemical compound CCOC(=O)CC(O)(C(=O)OCC)CC(=O)OCC DOOTYTYQINUNNV-UHFFFAOYSA-N 0.000 description 1
- 238000010521 absorption reaction Methods 0.000 description 1
- 230000001133 acceleration Effects 0.000 description 1
- 230000002411 adverse Effects 0.000 description 1
- QVGXLLKOCUKJST-UHFFFAOYSA-N atomic oxygen Chemical compound [O] QVGXLLKOCUKJST-UHFFFAOYSA-N 0.000 description 1
- 230000033228 biological regulation Effects 0.000 description 1
- 239000008280 blood Substances 0.000 description 1
- 210000004369 blood Anatomy 0.000 description 1
- 238000000576 coating method Methods 0.000 description 1
- 230000000052 comparative effect Effects 0.000 description 1
- 150000001875 compounds Chemical class 0.000 description 1
- 230000002354 daily effect Effects 0.000 description 1
- 230000007423 decrease Effects 0.000 description 1
- 238000001514 detection method Methods 0.000 description 1
- 239000012738 dissolution medium Substances 0.000 description 1
- 238000011978 dissolution method Methods 0.000 description 1
- 229960003638 dopamine Drugs 0.000 description 1
- 239000002552 dosage form Substances 0.000 description 1
- 230000000857 drug effect Effects 0.000 description 1
- 230000008030 elimination Effects 0.000 description 1
- 238000003379 elimination reaction Methods 0.000 description 1
- 230000003203 everyday effect Effects 0.000 description 1
- 238000013265 extended release Methods 0.000 description 1
- 235000013305 food Nutrition 0.000 description 1
- 230000030136 gastric emptying Effects 0.000 description 1
- 239000008187 granular material Substances 0.000 description 1
- 238000007689 inspection Methods 0.000 description 1
- 230000007794 irritation Effects 0.000 description 1
- 238000011068 loading method Methods 0.000 description 1
- 230000007774 longterm Effects 0.000 description 1
- 238000004519 manufacturing process Methods 0.000 description 1
- 230000007246 mechanism Effects 0.000 description 1
- 238000012986 modification Methods 0.000 description 1
- 230000004048 modification Effects 0.000 description 1
- 238000007500 overflow downdraw method Methods 0.000 description 1
- 229910052760 oxygen Inorganic materials 0.000 description 1
- 239000001301 oxygen Substances 0.000 description 1
- 238000012856 packing Methods 0.000 description 1
- 235000010603 pastilles Nutrition 0.000 description 1
- 230000036470 plasma concentration Effects 0.000 description 1
- 229920003023 plastic Polymers 0.000 description 1
- 239000004033 plastic Substances 0.000 description 1
- 239000004014 plasticizer Substances 0.000 description 1
- 238000011160 research Methods 0.000 description 1
- 230000033764 rhythmic process Effects 0.000 description 1
- 238000005070 sampling Methods 0.000 description 1
- 230000000698 schizophrenic effect Effects 0.000 description 1
- 239000007962 solid dispersion Substances 0.000 description 1
- 239000007939 sustained release tablet Substances 0.000 description 1
- 239000002700 tablet coating Substances 0.000 description 1
- 238000009492 tablet coating Methods 0.000 description 1
- 239000001069 triethyl citrate Substances 0.000 description 1
- VMYFZRTXGLUXMZ-UHFFFAOYSA-N triethyl citrate Natural products CCOC(=O)C(O)(C(=O)OCC)C(=O)OCC VMYFZRTXGLUXMZ-UHFFFAOYSA-N 0.000 description 1
- 235000013769 triethyl citrate Nutrition 0.000 description 1
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- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Medicinal Preparation (AREA)
Abstract
The invention discloses a matrix type sustained-release pellet capsule rich in quetiapine fumarate. The matrix type sustained-release pellet capsule has the characteristics of sustained release, long administration interval, low toxic and side effects and the like, and is used for treating schizophrenia. The invention also provides a preparation method and belongs to the technical field of medical science and pharmacy.
Description
Technical field
The present invention relates to the flat slow releasing capsule of a kind of fumaric acid Kui sulfur, in particular to a kind of quetiapine fumarate matrix type sustained-release micro-pill capsules agent and preparation method thereof, belong to field of pharmaceutical preparations.Described quetiapine fumarate slow releasing capsule can be used for treating schizophrenia.
Background technology
Quetiapine fumarate is a kind of atypia antipsychotic drug, and it is hexichol oxygen azatropylidene class medicine, belongs to polyceptor and does medication, have high affinity, and have stronger affinity to dopamine D 1 in brain and D2 receptor in brain to Serotonin receptor.
The flat conventional tablet specification of current fumaric acid Kui sulfur has 25mg, 100mg, 200mg and 300mg, and domestic oral routine dose is each 25mg, every day twice, increases 25mg every 1-3 day, increases to treatment accumulated dose 300-600mg gradually.The flat oral absorption of Kui sulfur is fast, and about 1 ~ 1.5h reaches peak plasma concentrations, and the elimination half-life is shorter.On the whole, patient medication is comparatively frequent, again because schizophrenic patients needs long-term prescription, brings constant and painful greatly to patient and family members.Therefore need to research and develop a kind of Kui sulfur release preparation, the release time of prolong drug, drug release is stablized, improves drug effect, reduce administration frequency.
Patent CN102614147A discloses the flat slow releasing tablet of fumaric acid Kui sulfur, and it is made up of quetiapine fumarate, modification pregelatinized Starch, filler, binding agent and lubricant, and the matrix sustained release tablet of preparation has good external sustained release performance.Patent CN102198113A discloses the flat slow releasing tablet preparation technology of fumaric acid Kui sulfur, and technique adopts erodible slow-release auxiliary material as blocker, adopts fusion method solid dispersion technology to prepare slow-releasing granules, and compress tablet coating.Compared with slow releasing tablet, slow-release micro-pill belongs to multiple agent type, has many advantages, and slow-release micro-pill is made up of the multiple piller of different release Mechanisms usually, and rate of releasing drug can reach zero level, and without time delay; Seldom by the impact of the digestive tract conveying food rhythm and pace of moving things, therefore gastric emptying rate is very little on its impact; Medicine increases at the area of gastrointestinal tract surface distributed, improves bioavailability, decreases local irritation; Slow-release micro-pill pastille percent ranges is large, can from more than 1% ~ 95%, and the maximal dose loading the slow-release micro-pill in single capsule can reach 600mg, and many other drug dosage forms are difficult to reach; Good fluidity, size is even, is easy to process; Improve medicine stability, cover adverse drug taste; Compound preparation compatibility can be applicable to.
Less about the patent of invention of the flat slow releasing capsule of fumaric acid Kui sulfur at present, CN103211794A discloses quetiapine fumarate film-controlled slow-release pellet capsule, its extended release coatings film comprises Eudragit RL 30D, plasticizer triethyl citrate and antiplastering aid Pulvis Talci composition, but its preparation process is more, complex process.The present invention relates to the agent of a kind of matrix type sustained-release micro-pill capsules, have had good sustained release effect, technique is simple, is easy to realize suitability for industrialized production.
Summary of the invention
The object of the present invention is to provide a kind of antipsychotic drug quetiapine fumarate matrix type sustained-release micro-pill capsules agent and preparation method thereof.Quetiapine fumarate slow releasing capsule prepared by the present invention daily once can ensure effective blood drug concentration in 24 hours, and reduces toxic and side effects, significantly reduces preparation differences between batches, improves the stability of sample.
The technical scheme of the present invention realizing above-mentioned purpose is as follows:
Described quetiapine fumarate matrix type sustained-release micro-pill capsules forms primarily of quetiapine fumarate, hydroxypropyl methylcellulose, filler, binding agent and lubricant, wherein according to mass ratio, quetiapine fumarate (putting down in Kui sulfur): hydroxypropyl methylcellulose: filler: binding agent: lubricant=1:(0.25 ~ 3): (0 ~ 2): (0.02 ~ 0.1): (0.01 ~ 1).
Described quetiapine fumarate slow releasing capsule content matrix type micropill comprises hydrophobic framework material, and quetiapine fumarate (putting down in Kui sulfur) in mass ratio: hydrophobic framework material=1:(0.25 ~ 2), described hydrophobic framework material is ethyl cellulose.
Described hydroxypropyl methylcellulose model is K15M.
Described filler is one or more mixture in lactose, microcrystalline Cellulose, calcium bicarbonate or sodium citrate.
Described binding agent is PVP K30, ethyl cellulose, hydroxypropyl methylcellulose, and solvent is the alcohol-water solution of water or alcohol or both arbitrary proportions.
Described lubricant is one or both in magnesium stearate, Pulvis Talci, silicon dioxide.
The preparation method of described quetiapine fumarate slow releasing capsule, comprise the following steps: (1) prepares raw material according to the proportioning of quetiapine fumarate, ethyl cellulose, hydroxypropyl methylcellulose, filler, binding agent, lubricant, quetiapine fumarate, ethyl cellulose, hydroxypropyl methylcellulose, filler and lubricant to be sieved mixing, add binding agent soft material; (2) add in extrusion spheronization machine by above-mentioned soft material, extrude with bar shaped state, extruding order number is 20 orders; (3) strip will be extruded and be placed in centrifugal spheronizator, and regulate and be applicable to rotating speed 200rpm ~ 600rpm, round as a ball; (4) fluid bed drying is 1% ~ 4% to moisture, is cooled to room temperature, screening 18-24 order micropill; (5) micropill content is measured, fill capsule.
Described quetiapine fumarate slow releasing capsule can be used for treating schizophrenia, belongs to field of pharmaceutical preparations.
Detailed description of the invention
Further illustrate the present invention by embodiment below, understand a kind of quetiapine fumarate slow releasing capsule further, but the present invention is not limited.
Slow releasing capsule prepared by following embodiment and comparative example, according to 1000 capsules amount preparations.Unless otherwise noted, all carry out with the extrusion spheronization machine of same model.
The preparation of embodiment 1 quetiapine fumarate slow releasing capsule (putting down in Kui sulfur, 50mg)
| Micropill composition | Consumption g |
| Quetiapine fumarate | 58 |
| Ethyl cellulose | 20 |
| Hydroxypropyl methylcellulose | 20 |
| Microcrystalline Cellulose | 110 |
| PVP K30 | 37 |
| Pulvis Talci | 5 |
| Add up to | 250 |
Preparation technology:
(1) get recipe quantity quetiapine fumarate, ethyl cellulose, microcrystalline Cellulose, PVP K30, Pulvis Talci mix homogeneously, cross 80 mesh sieve mixings;
(2) the hydroxypropyl methylcellulose aqueous solution preparing 3% does binding agent;
(3) appropriate (2) are added in (1), prepare soft material;
(4) add in extrusion spheronization machine by above-mentioned soft material, extrude with bar shaped state, extruding order number is 20 orders, will extrude strip in centrifugal spheronizator, regulates and is applicable to rotating speed 200rpm ~ 600rpm, round as a ball;
(5) fluid bed drying is 1% ~ 4% to moisture, is cooled to room temperature, sieves out 18 ~ 24 object micropills;
(6) micropill content is measured, fill capsule.
The preparation of embodiment 2 quetiapine fumarate slow releasing capsule (putting down in Kui sulfur, 200mg)
| Micropill composition | Consumption g |
| Quetiapine fumarate | 230 |
| Ethyl cellulose | 50 |
| Hydroxypropyl methylcellulose | 16.5 |
| Microcrystalline Cellulose | 53.5 |
| PVP K30 | 6 |
| Pulvis Talci | 24 |
| Add up to | 380 |
Preparation technology:
(1) get recipe quantity quetiapine fumarate, ethyl cellulose, hydroxypropyl methylcellulose, microcrystalline Cellulose, Pulvis Talci mix homogeneously, cross 80 mesh sieve mixings;
(2) the PVP K30 aqueous solution preparing 3% does binding agent;
(3) appropriate (2) are added in (1), prepare soft material;
(4) add in extrusion spheronization machine by above-mentioned soft material, extrude with bar shaped state, extruding order number is 20 orders, will extrude strip in centrifugal spheronizator, regulates and is applicable to rotating speed 200rpm ~ 600rpm, round as a ball;
(5) fluid bed drying is 1% ~ 4% to moisture, is cooled to room temperature, screening 18-24 object micropill;
(6) micropill content is measured, fill capsule.
The preparation of embodiment 3 quetiapine fumarate slow releasing capsule (putting down in Kui sulfur, 300mg)
| Micropill composition | Consumption g |
| Quetiapine fumarate | 345 |
| Ethyl cellulose | 86.25 |
| Hydroxypropyl methylcellulose | 86.25 |
| Microcrystalline Cellulose | 103.5 |
| PVP K30 | 2.1 |
| Silicon dioxide | 6.9 |
| Add up to | 630 |
(1) get recipe quantity quetiapine fumarate, ethyl cellulose, microcrystalline Cellulose, PVP K30, Pulvis Talci mix homogeneously, cross 80 mesh sieve mixings;
(2) the hydroxypropyl methylcellulose aqueous solution preparing 3% does binding agent;
(3) appropriate (2) are added in (1), prepare soft material;
(4) add in extrusion spheronization machine by above-mentioned soft material, extrude with bar shaped state, extruding order number is 20 orders, will extrude strip in centrifugal spheronizator, regulates and is applicable to rotating speed 200rpm ~ 600rpm, round as a ball;
(5) fluid bed drying is 1% ~ 4% to moisture, is cooled to room temperature, screening 18 ~ 24 object micropills;
(6) micropill content is measured, fill capsule.
The preparation of embodiment 4 quetiapine fumarate slow releasing capsule (putting down in Kui sulfur, 400mg)
| Micropill composition | Consumption g |
| Quetiapine fumarate | 461 |
| Ethyl cellulose | 179 |
| Hydroxypropyl methylcellulose | 135 |
| Microcrystalline Cellulose | 220 |
| Pulvis Talci | 5 |
| Add up to | 1000 |
Preparation technology:
(1) get recipe quantity quetiapine fumarate, ethyl cellulose, hydroxypropyl methylcellulose, microcrystalline Cellulose, Pulvis Talci mix homogeneously, cross 80 mesh sieve mixings;
(2) binding agent is done with 30% alcohol-water solution;
(3) appropriate (2) are added in (1), prepare soft material;
(4) add in extrusion spheronization machine by above-mentioned soft material, extrude with bar shaped state, extruding order number is 20 orders, will extrude strip in centrifugal spheronizator, regulates and is applicable to rotating speed 200rpm ~ 600rpm, round as a ball;
(5) fluid bed drying is 1% ~ 4% to moisture, is cooled to room temperature, screening 18 ~ 24 object micropills;
(6) micropill content is measured, fill capsule.
Test example 1: stripping is investigated
According to dissolution method (Chinese Pharmacopoeia version in 2000 two annex X C first methods), respectively with 900ml, pH4.8 and pH6.6 for dissolution medium, rotating speed is 100 turns per minute.Operate, the slow releasing capsule prepared by embodiment of the present invention 1-4 carries out stripping curve detection in accordance with the law.
From above result of the test, quetiapine fumarate slow releasing capsule content is all qualified, all has obvious slow release effect.
Test example 2: study on the stability
Quetiapine fumarate slow releasing capsule in Example 1, aluminium-plastic bubble plate packing, 40 ± 2 DEG C, place under relative humidity 75 ± 5% constant temperature and humidity condition, detect related substance and content respectively at sampling in 0,1,2,3 and 6 month, testing result sees the following form.
From the above results, the quetiapine fumarate slow releasing capsule of this formula preparation places 1,2,3 and 6 month under acceleration conditions, and related substance slightly increases, and character and content inspection all conform with the regulations.Preparation should be stored under hermetically drying condition.
Claims (8)
1. quetiapine fumarate matrix type sustained-release micro-pill capsules agent, it is characterized in that: described quetiapine fumarate slow releasing capsule forms primarily of quetiapine fumarate, hydroxypropyl methylcellulose, filler, binding agent and lubricant, wherein according to mass ratio, quetiapine fumarate (putting down in Kui sulfur): hydroxypropyl methylcellulose: filler: binding agent: lubricant=1:(0.25 ~ 3): (0 ~ 2): (0.02 ~ 0.1): (0.01 ~ 1).
2. quetiapine fumarate slow releasing capsule according to claim 1, it is characterized in that: described quetiapine fumarate slow releasing capsule content matrix type micropill comprises hydrophobic framework material, and quetiapine fumarate (putting down in Kui sulfur) in mass ratio: hydrophobic framework material=1:(0.25 ~ 2), described hydrophobic framework material is ethyl cellulose.
3. quetiapine fumarate slow releasing capsule according to claim 1, it is characterized in that, described hydroxypropyl methylcellulose model is K15M.
4. quetiapine fumarate slow releasing capsule according to claim 1, is characterized in that described filler is one or more mixture in lactose, microcrystalline Cellulose, calcium bicarbonate or sodium citrate.
5. quetiapine fumarate slow releasing capsule according to claim 1, is characterized in that: described binding agent is PVP K30, ethyl cellulose, hydroxypropyl methylcellulose, and solvent is the alcohol-water solution of a kind of in water, alcohol or both arbitrary proportions.
6. quetiapine fumarate slow releasing capsule according to claim 1, is characterized in that described lubricant is one or both in magnesium stearate, Pulvis Talci, silicon dioxide.
7. the preparation method of quetiapine fumarate slow releasing capsule according to claim 1, comprise the following steps: (1) prepares raw material according to the proportioning of quetiapine fumarate, ethyl cellulose, hydroxypropyl methylcellulose, filler, binding agent, lubricant in claim 1 or 2, quetiapine fumarate, ethyl cellulose, hydroxypropyl methylcellulose, filler and lubricant to be sieved mixing, add binding agent soft material; (2) add in extrusion spheronization machine by above-mentioned soft material, extrude with bar shaped state, extruding order number is 20 orders; (3) strip will be extruded and be placed in centrifugal spheronizator, and regulate and be applicable to rotating speed 200rpm ~ 600rpm, round as a ball; (4) fluid bed drying is 1% ~ 4% to moisture, is cooled to room temperature, screening 18-24 order micropill; (5) micropill content is measured, fill capsule.
8. quetiapine fumarate slow releasing capsule according to claim 1 can be used for treating schizophrenia, belongs to field of pharmaceutical preparations.
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| CN201510005598.8A CN104546800A (en) | 2015-01-07 | 2015-01-07 | Quetiapine fumarate sustained-release capsule and preparation method thereof |
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| CN201510005598.8A CN104546800A (en) | 2015-01-07 | 2015-01-07 | Quetiapine fumarate sustained-release capsule and preparation method thereof |
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Cited By (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN105362252A (en) * | 2015-10-09 | 2016-03-02 | 北京万全德众医药生物技术有限公司 | Sustained-release capsule containing levodopa and carbidopa and preparation method of sustained-release capsule |
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- 2015-01-07 CN CN201510005598.8A patent/CN104546800A/en active Pending
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| CN101005829A (en) * | 2003-10-21 | 2007-07-25 | 艾克塔维斯集团公司 | Quetiapine formulations |
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| CN101912374A (en) * | 2010-08-08 | 2010-12-15 | 浙江华海药业股份有限公司 | Quetiapine sustained release tablet and preparation method thereof |
| CN102406606A (en) * | 2011-11-29 | 2012-04-11 | 海南美大制药有限公司 | Quetiapine fumarate liposome solid preparation |
Cited By (1)
| Publication number | Priority date | Publication date | Assignee | Title |
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| CN105362252A (en) * | 2015-10-09 | 2016-03-02 | 北京万全德众医药生物技术有限公司 | Sustained-release capsule containing levodopa and carbidopa and preparation method of sustained-release capsule |
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Application publication date: 20150429 |