CN106580895A - Orally disintegrating tablet containing vilazodone hydrochloride solid dispersions and preparation method thereof - Google Patents
Orally disintegrating tablet containing vilazodone hydrochloride solid dispersions and preparation method thereof Download PDFInfo
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- CN106580895A CN106580895A CN201611113819.4A CN201611113819A CN106580895A CN 106580895 A CN106580895 A CN 106580895A CN 201611113819 A CN201611113819 A CN 201611113819A CN 106580895 A CN106580895 A CN 106580895A
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- Prior art keywords
- solid dispersion
- vilazodone hydrochloride
- hydrochloride solid
- oral cavity
- solvent
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- 239000007962 solid dispersion Substances 0.000 title claims abstract description 54
- 229960003381 vilazodone hydrochloride Drugs 0.000 title claims abstract description 52
- RPZBRGFNBNQSOP-UHFFFAOYSA-N vilazodone hydrochloride Chemical compound Cl.C1=C(C#N)C=C2C(CCCCN3CCN(CC3)C=3C=C4C=C(OC4=CC=3)C(=O)N)=CNC2=C1 RPZBRGFNBNQSOP-UHFFFAOYSA-N 0.000 title claims abstract description 52
- 238000002360 preparation method Methods 0.000 title claims abstract description 18
- 239000006191 orally-disintegrating tablet Substances 0.000 title abstract 4
- 210000000214 mouth Anatomy 0.000 claims description 23
- 239000003795 chemical substances by application Substances 0.000 claims description 20
- 239000002904 solvent Substances 0.000 claims description 18
- LFQSCWFLJHTTHZ-UHFFFAOYSA-N Ethanol Chemical compound CCO LFQSCWFLJHTTHZ-UHFFFAOYSA-N 0.000 claims description 15
- HQKMJHAJHXVSDF-UHFFFAOYSA-L magnesium stearate Chemical compound [Mg+2].CCCCCCCCCCCCCCCCCC([O-])=O.CCCCCCCCCCCCCCCCCC([O-])=O HQKMJHAJHXVSDF-UHFFFAOYSA-L 0.000 claims description 14
- 238000000034 method Methods 0.000 claims description 13
- 238000002156 mixing Methods 0.000 claims description 12
- 238000007908 dry granulation Methods 0.000 claims description 8
- 229920000168 Microcrystalline cellulose Polymers 0.000 claims description 7
- 229940031703 low substituted hydroxypropyl cellulose Drugs 0.000 claims description 7
- 235000019359 magnesium stearate Nutrition 0.000 claims description 7
- 235000019813 microcrystalline cellulose Nutrition 0.000 claims description 7
- 239000008108 microcrystalline cellulose Substances 0.000 claims description 7
- 229940016286 microcrystalline cellulose Drugs 0.000 claims description 7
- 229960003740 vilazodone Drugs 0.000 claims description 7
- SGEGOXDYSFKCPT-UHFFFAOYSA-N vilazodone Chemical compound C1=C(C#N)C=C2C(CCCCN3CCN(CC3)C=3C=C4C=C(OC4=CC=3)C(=O)N)=CNC2=C1 SGEGOXDYSFKCPT-UHFFFAOYSA-N 0.000 claims description 7
- XEKOWRVHYACXOJ-UHFFFAOYSA-N Ethyl acetate Chemical compound CCOC(C)=O XEKOWRVHYACXOJ-UHFFFAOYSA-N 0.000 claims description 6
- 239000000945 filler Substances 0.000 claims description 6
- 239000000314 lubricant Substances 0.000 claims description 6
- 238000001694 spray drying Methods 0.000 claims description 6
- DGAQECJNVWCQMB-PUAWFVPOSA-M Ilexoside XXIX Chemical compound C[C@@H]1CC[C@@]2(CC[C@@]3(C(=CC[C@H]4[C@]3(CC[C@@H]5[C@@]4(CC[C@@H](C5(C)C)OS(=O)(=O)[O-])C)C)[C@@H]2[C@]1(C)O)C)C(=O)O[C@H]6[C@@H]([C@H]([C@@H]([C@H](O6)CO)O)O)O.[Na+] DGAQECJNVWCQMB-PUAWFVPOSA-M 0.000 claims description 5
- 239000000203 mixture Substances 0.000 claims description 5
- 239000011734 sodium Substances 0.000 claims description 5
- 229910052708 sodium Inorganic materials 0.000 claims description 5
- 238000000935 solvent evaporation Methods 0.000 claims description 5
- FBPFZTCFMRRESA-KVTDHHQDSA-N D-Mannitol Chemical group OC[C@@H](O)[C@@H](O)[C@H](O)[C@H](O)CO FBPFZTCFMRRESA-KVTDHHQDSA-N 0.000 claims description 4
- 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 4
- 229930195725 Mannitol Natural products 0.000 claims description 4
- 229920002472 Starch Polymers 0.000 claims description 4
- 239000008101 lactose Substances 0.000 claims description 4
- 239000000594 mannitol Substances 0.000 claims description 4
- 235000010355 mannitol Nutrition 0.000 claims description 4
- 239000001253 polyvinylpolypyrrolidone Substances 0.000 claims description 4
- 235000013809 polyvinylpolypyrrolidone Nutrition 0.000 claims description 4
- 229920000523 polyvinylpolypyrrolidone Polymers 0.000 claims description 4
- 229920000036 polyvinylpyrrolidone Polymers 0.000 claims description 4
- 235000013855 polyvinylpyrrolidone Nutrition 0.000 claims description 4
- 239000008107 starch Substances 0.000 claims description 4
- 235000019698 starch Nutrition 0.000 claims description 4
- 229920002261 Corn starch Polymers 0.000 claims description 3
- 229920000881 Modified starch Polymers 0.000 claims description 3
- DPXJVFZANSGRMM-UHFFFAOYSA-N acetic acid;2,3,4,5,6-pentahydroxyhexanal;sodium Chemical compound [Na].CC(O)=O.OCC(O)C(O)C(O)C(O)C=O DPXJVFZANSGRMM-UHFFFAOYSA-N 0.000 claims description 3
- 125000002057 carboxymethyl group Chemical group [H]OC(=O)C([H])([H])[*] 0.000 claims description 3
- 239000008120 corn starch Substances 0.000 claims description 3
- MVPICKVDHDWCJQ-UHFFFAOYSA-N ethyl 3-pyrrolidin-1-ylpropanoate Chemical compound CCOC(=O)CCN1CCCC1 MVPICKVDHDWCJQ-UHFFFAOYSA-N 0.000 claims description 3
- 229940045902 sodium stearyl fumarate Drugs 0.000 claims description 3
- 229920002785 Croscarmellose sodium Polymers 0.000 claims description 2
- 241000196324 Embryophyta Species 0.000 claims description 2
- 239000012876 carrier material Substances 0.000 claims description 2
- 229960001681 croscarmellose sodium Drugs 0.000 claims description 2
- 235000010947 crosslinked sodium carboxy methyl cellulose Nutrition 0.000 claims description 2
- 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 2
- 229920006316 polyvinylpyrrolidine Polymers 0.000 claims description 2
- 238000002390 rotary evaporation Methods 0.000 claims description 2
- GUBGYTABKSRVRQ-XLOQQCSPSA-N Alpha-Lactose Chemical compound O[C@@H]1[C@@H](O)[C@@H](O)[C@@H](CO)O[C@H]1O[C@@H]1[C@@H](CO)O[C@H](O)[C@H](O)[C@H]1O GUBGYTABKSRVRQ-XLOQQCSPSA-N 0.000 claims 1
- 235000011194 food seasoning agent Nutrition 0.000 claims 1
- 229940057838 polyethylene glycol 4000 Drugs 0.000 claims 1
- 229940093429 polyethylene glycol 6000 Drugs 0.000 claims 1
- 239000001267 polyvinylpyrrolidone Substances 0.000 claims 1
- 238000005507 spraying Methods 0.000 claims 1
- 239000003814 drug Substances 0.000 abstract description 7
- 239000000969 carrier Substances 0.000 abstract 1
- XLYOFNOQVPJJNP-UHFFFAOYSA-N water Substances O XLYOFNOQVPJJNP-UHFFFAOYSA-N 0.000 abstract 1
- VEXZGXHMUGYJMC-UHFFFAOYSA-N Hydrochloric acid Chemical compound Cl VEXZGXHMUGYJMC-UHFFFAOYSA-N 0.000 description 14
- 208000024714 major depressive disease Diseases 0.000 description 8
- 238000003756 stirring Methods 0.000 description 6
- 238000004090 dissolution Methods 0.000 description 4
- 239000004376 Sucralose Substances 0.000 description 3
- MTHSVFCYNBDYFN-UHFFFAOYSA-N diethylene glycol Chemical compound OCCOCCO MTHSVFCYNBDYFN-UHFFFAOYSA-N 0.000 description 3
- 229940079593 drug Drugs 0.000 description 3
- 235000019408 sucralose Nutrition 0.000 description 3
- BAQAVOSOZGMPRM-QBMZZYIRSA-N sucralose Chemical compound O[C@@H]1[C@@H](O)[C@@H](Cl)[C@@H](CO)O[C@@H]1O[C@@]1(CCl)[C@@H](O)[C@H](O)[C@@H](CCl)O1 BAQAVOSOZGMPRM-QBMZZYIRSA-N 0.000 description 3
- 229920001030 Polyethylene Glycol 4000 Polymers 0.000 description 2
- 240000000111 Saccharum officinarum Species 0.000 description 2
- 235000007201 Saccharum officinarum Nutrition 0.000 description 2
- 230000015572 biosynthetic process Effects 0.000 description 2
- 230000008859 change Effects 0.000 description 2
- 239000013078 crystal Substances 0.000 description 2
- 230000000694 effects Effects 0.000 description 2
- 150000002576 ketones Chemical class 0.000 description 2
- 229920000136 polysorbate Polymers 0.000 description 2
- 239000004094 surface-active agent Substances 0.000 description 2
- RTHCYVBBDHJXIQ-MRXNPFEDSA-N (R)-fluoxetine Chemical compound O([C@H](CCNC)C=1C=CC=CC=1)C1=CC=C(C(F)(F)F)C=C1 RTHCYVBBDHJXIQ-MRXNPFEDSA-N 0.000 description 1
- 102100022738 5-hydroxytryptamine receptor 1A Human genes 0.000 description 1
- 101710138638 5-hydroxytryptamine receptor 1A Proteins 0.000 description 1
- WBZFUFAFFUEMEI-UHFFFAOYSA-M Acesulfame k Chemical compound [K+].CC1=CC(=O)[N-]S(=O)(=O)O1 WBZFUFAFFUEMEI-UHFFFAOYSA-M 0.000 description 1
- 108010011485 Aspartame Proteins 0.000 description 1
- 206010010144 Completed suicide Diseases 0.000 description 1
- 208000020401 Depressive disease Diseases 0.000 description 1
- 229920002153 Hydroxypropyl cellulose Polymers 0.000 description 1
- 208000019022 Mood disease Diseases 0.000 description 1
- 102000008092 Norepinephrine Plasma Membrane Transport Proteins Human genes 0.000 description 1
- 108010049586 Norepinephrine Plasma Membrane Transport Proteins Proteins 0.000 description 1
- 239000008118 PEG 6000 Substances 0.000 description 1
- 229920002584 Polyethylene Glycol 6000 Polymers 0.000 description 1
- 239000002202 Polyethylene glycol Substances 0.000 description 1
- 102000019208 Serotonin Plasma Membrane Transport Proteins Human genes 0.000 description 1
- 108010012996 Serotonin Plasma Membrane Transport Proteins Proteins 0.000 description 1
- 238000009825 accumulation Methods 0.000 description 1
- 235000010358 acesulfame potassium Nutrition 0.000 description 1
- 229960004998 acesulfame potassium Drugs 0.000 description 1
- 239000000619 acesulfame-K Substances 0.000 description 1
- 230000009471 action Effects 0.000 description 1
- 239000000556 agonist Substances 0.000 description 1
- 239000000605 aspartame Substances 0.000 description 1
- 235000010357 aspartame Nutrition 0.000 description 1
- IAOZJIPTCAWIRG-QWRGUYRKSA-N aspartame Chemical compound OC(=O)C[C@H](N)C(=O)N[C@H](C(=O)OC)CC1=CC=CC=C1 IAOZJIPTCAWIRG-QWRGUYRKSA-N 0.000 description 1
- 229960003438 aspartame Drugs 0.000 description 1
- 238000003556 assay Methods 0.000 description 1
- 230000004888 barrier function Effects 0.000 description 1
- 230000009286 beneficial effect Effects 0.000 description 1
- 230000008901 benefit Effects 0.000 description 1
- 210000004556 brain Anatomy 0.000 description 1
- 210000000481 breast Anatomy 0.000 description 1
- 239000001768 carboxy methyl cellulose Substances 0.000 description 1
- 235000009508 confectionery Nutrition 0.000 description 1
- 238000004132 cross linking Methods 0.000 description 1
- 235000005911 diet Nutrition 0.000 description 1
- 230000037213 diet Effects 0.000 description 1
- 239000012738 dissolution medium Substances 0.000 description 1
- 201000003104 endogenous depression Diseases 0.000 description 1
- 229960002464 fluoxetine Drugs 0.000 description 1
- 239000001863 hydroxypropyl cellulose Substances 0.000 description 1
- 235000010977 hydroxypropyl cellulose Nutrition 0.000 description 1
- 238000000338 in vitro Methods 0.000 description 1
- -1 indolyl amine Chemical class 0.000 description 1
- 239000003112 inhibitor Substances 0.000 description 1
- 208000011736 mal de Debarquement Diseases 0.000 description 1
- 206010025482 malaise Diseases 0.000 description 1
- 230000003340 mental effect Effects 0.000 description 1
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 description 1
- TZBAVQKIEKDGFH-UHFFFAOYSA-N n-[2-(diethylamino)ethyl]-1-benzothiophene-2-carboxamide;hydrochloride Chemical compound [Cl-].C1=CC=C2SC(C(=O)NCC[NH+](CC)CC)=CC2=C1 TZBAVQKIEKDGFH-UHFFFAOYSA-N 0.000 description 1
- 229920001223 polyethylene glycol Polymers 0.000 description 1
- 230000003389 potentiating effect Effects 0.000 description 1
- 239000002994 raw material Substances 0.000 description 1
- 235000019812 sodium carboxymethyl cellulose Nutrition 0.000 description 1
- 229920001027 sodium carboxymethylcellulose Polymers 0.000 description 1
- 239000007787 solid Substances 0.000 description 1
- 231100000331 toxic Toxicity 0.000 description 1
- 230000002588 toxic effect Effects 0.000 description 1
Classifications
-
- 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
- A61K9/0012—Galenical forms characterised by the site of application
- A61K9/0053—Mouth and digestive tract, i.e. intraoral and peroral administration
- A61K9/0056—Mouth soluble or dispersible forms; Suckable, eatable, chewable coherent forms; Forms rapidly disintegrating in the mouth; Lozenges; Lollipops; Bite capsules; Baked products; Baits or other oral forms for animals
-
- 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
- A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
- A61K31/496—Non-condensed piperazines containing further heterocyclic rings, e.g. rifampin, thiothixene or sparfloxacin
-
- 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
- A61K9/2031—Organic macromolecular compounds obtained otherwise than by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyethylene glycol, polyethylene oxide, poloxamers
-
- 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
- A61K9/205—Polysaccharides, e.g. alginate, gums; Cyclodextrin
- A61K9/2054—Cellulose; Cellulose derivatives, e.g. hydroxypropyl methylcellulose
Landscapes
- Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- Epidemiology (AREA)
- Pharmacology & Pharmacy (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Medicinal Chemistry (AREA)
- Chemical & Material Sciences (AREA)
- Biophysics (AREA)
- Molecular Biology (AREA)
- Zoology (AREA)
- Nutrition Science (AREA)
- Physiology (AREA)
- Medicinal Preparation (AREA)
Abstract
The invention belongs to the field of a medicine preparation, and particularly relates to an orally disintegrating tablet containing vilazodone hydrochloride solid dispersions and a preparation method thereof. By aiming at the problems of poor water solubility and low preparation dissolubility of the vilazodone hydrochloride, the vilazodone hydrochloride and carriers are prepared into the solid dispersions for improving the solubility. The solid dispersions are used for preparing the orally disintegrating tablet; the orally disintegrating tablet can fast disintegrate in 30s; and the main medicine dissolubility is obviously improved.
Description
Technical field
The application belongs to technical field of medicine.
Background technology
Vilazodone Hydrochloride is the anti-suppression of indolyl amine first of new generation of Trovis Pharmaceutical Co exploitation
Strongly fragrant medicine, is listed by FDA approvals on January 21st, 2011, for treating major depressive disorder（Major depressive
disorder, MDD）.Major depressive disorder, also referred to as clinical depression, major depression, unipolar depression or single-phase barrier
Hinder, be a kind of mental sickness, its typical performance is：Patient is immersed in the affective state of depression, and sense of personal worth is reduced, to feeling in the past
Interesting activity loses interest.Major depressive disorder is a kind of family to patient, work, study, diet and sleep, with
And the disability situation that other body functions have a negative impact.In the U.S., about 3.4% Suicide of Depression Patients.It is all from
In senilicide, the people that may have 60% suffers from major depressive disorder or other mood disorders.
Hydrochloric acid vilazodone is a potent selectivity 5-HT reuptake inhibitor, while it is also a 5-HT1A receiving
Body portion agonist.The affinity in hydrochloric acid vilazodone and 5-HT transporters site is high, and with norepinephrine transporter position
The affinity in point or DAT site is all weaker, therefore toxic and side effects are relatively low.Hydrochloric acid vilazodone suppresses rat brain to dash forward
The 5-HT reuptakes of contact are 30 times of fluoxetine.Although Vilazodone Hydrochloride strong drug action, which dissolves under physiological ph conditions
Degree is extremely low, and agent in vitro dissolution is poor.
The content of the invention
This application provides a kind of oral cavity disintegration tablet of hydrochloric vilazodone solid dispersion, grinds consistent using with original
Crystal formation IV raw materials, are added without any surfactant, improve its dissolubility by preparing Vilazodone Hydrochloride solid dispersion, enter
And improve preparation dissolution.
Specific embodiment is as follows：
A kind of oral cavity disintegration tablet of hydrochloric vilazodone solid dispersion, described Vilazodone Hydrochloride solid dispersion is by leading
Medicine, carrier and solvent are prepared from using spray drying method or solvent evaporation method, and the oral cavity disintegration tablet is by with percentage by weight
The following component composition of meter：Vilazodone Hydrochloride solid dispersion 20-40%, filler 50-73%, disintegrating agent 5-12%, lubricant
0.5-3%, sweeting agent 0.1-1%.
Wherein, described Vilazodone Hydrochloride solid dispersion is made up of the following component in terms of weight fraction：Hydrochloric acid is tieed up
Draw 1 part of ketone of assistant, carrier 1-3 parts, solvent 10-50 parts, it is preferable that 2 parts of carrier, solvent 15-35 parts.
Wherein, described Vilazodone Hydrochloride solid dispersion, its carrier material are Macrogol 4000, Polyethylene Glycol
6000th, one or more in polyvinylpyrrolidone K-15, PVP K-30, PVP K-90.
Wherein, described Vilazodone Hydrochloride solid dispersion, in its solvent selected from ethanol, acetoneand ethyl acetate
Plant or several.
Wherein, described Vilazodone Hydrochloride solid dispersion, its preparation method are solvent evaporation method or spray drying method,
Which comprises the steps of：（1）Principal agent and carrier are codissolved in solvent, are sufficiently stirred for；（2）Common solution of the principal agent with carrier is adopted
Solvent is removed with rotary evaporation or spray drying method, solid dispersion is obtained.
Wherein, described Vilazodone Hydrochloride solid dispersion, helps for hydrochloric acid Wella after crossing 60-200 mesh sieve pretreatment
The preparation of ketone oral cavity disintegration tablet.
Wherein, the described oral cavity disintegration tablet prepared by Vilazodone Hydrochloride solid dispersion, filler are Mannitol, breast
Sugar, corn starch, pregelatinized Starch, one or more in Microcrystalline Cellulose.
Wherein, the described oral cavity disintegration tablet prepared by Vilazodone Hydrochloride solid dispersion, disintegrating agent are crosslinking carboxylic first
One or more in base sodium cellulosate, carboxymethyl starch sodium, low-substituted hydroxypropyl cellulose and polyvinylpolypyrrolidone.
Wherein, the described oral cavity disintegration tablet prepared by Vilazodone Hydrochloride solid dispersion, lubricant be magnesium stearate,
One or more in sodium stearyl fumarate and Pulvis Talci.
Wherein, the described oral cavity disintegration tablet prepared by Vilazodone Hydrochloride solid dispersion, sweeting agent be sucralose,
One or more in aspartame and acesulfame potassium.
Wherein, the described oral cavity disintegration tablet prepared by Vilazodone Hydrochloride solid dispersion, its preparation method are as follows：Will
Vilazodone Hydrochloride solid dispersion, filler, disintegrating agent mixing after dry granulation, additional disintegrating agent, lubricant and sweeting agent
Tabletting after mix homogeneously.
The beneficial effect reached by the application：Compared with prior art, the present invention grinds consistent crystal formation with original in employing, no
On the premise of adding any surfactant, principal agent is prepared into into solid point using solvent evaporation method or spray drying method with carrier
A prose style free from parallelism, greatly improves drug solubility, and then improves dissolution.
Specific embodiment
In order to be illustrated more clearly that the advantage and feature of the application, with reference to specific embodiment party of the embodiment to the application
Formula is further described, it will be appreciated by those skilled in the art that specifically described content is illustrative rather than limiting below
Property, the protection domain of the application should not be limited with this.
The assay method of stripping curve in embodiment：Jing is screened, and 0.1M hydrochloric acid adds 0.5% tween more to distinguish power, therefore
Adopt 0.1M hydrochloric acid to add 0.5% tween for dissolution medium, paddle method measure, rotating speed is 60rpm/min, respectively with 5,10,15,30,
45th, the accumulation dissolution of each time points of 60min and former triturate contrast f2The factor.
Embodiment 1
Vilazodone Hydrochloride oral cavity disintegration tablet is prepared from the following components, and measures by 1000
Its preparation method is comprised the following steps：
（1）The PEG6000 that recipe quantity is added in the ethanol solution of Vilazodone Hydrochloride, dissolving and 10 times of weight is taken, stirring is allowed to
Clear transparent solutions are dissolved as, revolving removes solvent, obtains solid dispersion.
（2）Gained solid dispersion crosses 60 mesh sieve pretreatment.
（3）By pretreated Vilazodone Hydrochloride solid dispersion and the Lactose of recipe quantity, Microcrystalline Cellulose, interior plus friendship
Dry granulation after the uniform mixing of connection sodium carboxymethyl cellulose, adds additional Croscarmellose Sodium, magnesium stearate and An Sai
Tabletting after sweet uniform mixing.
Result of the test：
Disintegration time 25s, is contrasted with former triturate stripping curve：f2For 58.
Embodiment 2
Vilazodone Hydrochloride oral cavity disintegration tablet is prepared from the following components, and measures by 1000
Its preparation method is comprised the following steps：
（1）The PVPK-30 that recipe quantity is added in the ethanol solution of Vilazodone Hydrochloride, dissolving and 50 times of weight is taken, stirring is allowed to
Clear transparent solutions are dissolved as, revolving removes solvent, obtains solid dispersion.
（2）Gained solid dispersion crosses 120 mesh sieve pretreatment.
（3）By the Mannitol of pretreated Vilazodone Hydrochloride solid dispersion and recipe quantity, Microcrystalline Cellulose, it is interior plus
Low-substituted hydroxypropyl cellulose uniformly mix after dry granulation, add additional low-substituted hydroxypropyl cellulose, magnesium stearate and Ah
Tabletting after the uniform mixing of this Ba Tian.
Result of the test：
Disintegration time 20s, is contrasted with former triturate stripping curve：f2For 65.
Embodiment 3
Vilazodone Hydrochloride oral cavity disintegration tablet is prepared from the following components, and measures by 1000
Its preparation method is comprised the following steps：
（1）The PVPK-90 that recipe quantity is added in the ethanol solution of Vilazodone Hydrochloride, dissolving and 25 times of weight is taken, stirring is allowed to
Clear transparent solutions are dissolved as, revolving removes solvent, obtains solid dispersion.
（2）Gained solid dispersion crosses 120 mesh sieve pretreatment.
（3）By the Mannitol of pretreated Vilazodone Hydrochloride solid dispersion and recipe quantity, pregelatinized Starch, it is interior plus
Dry granulation after the uniform mixing of polyvinylpolypyrrolidone, adds additional low-substituted hydroxypropyl cellulose, sodium stearyl fumarate and trichlorine sugarcane
Tabletting after sugared uniform mixing.
Result of the test：
Disintegration time 23s, is contrasted with former triturate stripping curve：f2For 60.
Embodiment 4
Vilazodone Hydrochloride oral cavity disintegration tablet is prepared from the following components, and measures by 1000
Its preparation method is comprised the following steps：
（1）The PVPK-15 that recipe quantity is added in the ethanol solution of Vilazodone Hydrochloride, dissolving and 20 times of weight is taken, stirring is allowed to
Clear transparent solutions are dissolved as, revolving removes solvent, obtains solid dispersion.
（2）Gained solid dispersion crosses 120 mesh sieve pretreatment.
（3）By pretreated Vilazodone Hydrochloride solid dispersion and the corn starch of recipe quantity, Microcrystalline Cellulose, interior
Plus dry granulation after the uniform mixing of carboxymethyl starch sodium, add additional low-substituted hydroxypropyl cellulose, magnesium stearate and trichlorine sugarcane
Tabletting after sugared uniform mixing.
Result of the test：
Disintegration time 27s, is contrasted with former triturate stripping curve：f2For 52.
Embodiment 5
Vilazodone Hydrochloride oral cavity disintegration tablet is prepared from the following components, and measures by 1000
Its preparation method is comprised the following steps：
（1）The PEG4000 that recipe quantity is added in the ethanol solution of Vilazodone Hydrochloride, dissolving and 20 times of weight is taken, stirring is allowed to
Clear transparent solutions are dissolved as, revolving removes solvent, obtains solid dispersion.
（2）Gained solid dispersion crosses 120 mesh sieve pretreatment.
（3）By pretreated Vilazodone Hydrochloride solid dispersion and the Lactose of recipe quantity, Microcrystalline Cellulose, interior plus carboxylic
Dry granulation after the uniform mixing of methyl starch sodium, adds additional low-substituted hydroxypropyl cellulose, magnesium stearate and sucralose equal
Tabletting after even mixing.
Result of the test：
Disintegration time 27s, is contrasted with former triturate stripping curve：f2For 52.
Embodiment 6
Vilazodone Hydrochloride oral cavity disintegration tablet is prepared from the following components, and measures by 1000
Its preparation method is comprised the following steps：
（1）The PEG4000 that recipe quantity is added in the ethanol solution of Vilazodone Hydrochloride, dissolving and 20 times of weight is taken, stirring is allowed to
Clear transparent solutions are dissolved as, revolving removes solvent, obtains solid dispersion.
（2）Gained solid dispersion crosses 200 mesh sieve pretreatment.
（3）By pretreated Vilazodone Hydrochloride solid dispersion and the Lactose of recipe quantity, Microcrystalline Cellulose, interior plus low
Dry granulation after replacing hydroxypropyl cellulose uniformly to mix, adds additional polyvinylpolypyrrolidone, magnesium stearate and sucralose uniform
Tabletting after mixing.
Result of the test：
Disintegration time 29s, is contrasted with former triturate stripping curve：f2For 50.
Obviously, the above embodiment of the present invention is only intended to clearly illustrate example of the present invention, and is not right
The restriction of embodiments of the present invention, for those of ordinary skill in the field, may be used also on the basis of the above description
To make other changes in different forms, all of embodiment cannot be exhaustive here, it is every to belong to this
Bright technical scheme it is extended obvious change or change still in protection scope of the present invention row.
Claims (10)
1. the oral cavity disintegration tablet of hydrochloric vilazodone solid dispersion, it is characterised in that：Described Vilazodone Hydrochloride solid
Dispersion is prepared from using spray drying method or solvent evaporation method by principal agent, carrier and solvent, and oral cavity disintegration tablet is by with weight
The following component composition of percentages：Vilazodone Hydrochloride solid dispersion 20-40%, filler 50-73%, disintegrating agent 5-12%,
Lubricant 0.5-3%, sweeting agent 0.1-1%.
2., according to the Vilazodone Hydrochloride solid dispersion described in claim 1, it is made up of the following component in terms of weight fraction：
1 part of Vilazodone Hydrochloride, carrier 1-3 parts, solvent 10-50 parts, it is preferable that 2 parts of carrier, solvent 15-35 parts.
3. according to the Vilazodone Hydrochloride solid dispersion described in claim 1, it is characterised in that：Described carrier material is poly-
Ethylene glycol 4000, polyethylene glycol 6000, polyvinylpyrrolidone K-15, PVP K-30, polyvinylpyrrolidone
One or more in K-90.
4. according to the Vilazodone Hydrochloride solid dispersion described in claim 1, it is characterised in that：Described solvent is selected from second
One or more in alcohol, acetoneand ethyl acetate.
5., according to the Vilazodone Hydrochloride solid dispersion described in claim 1, its preparation method is solvent evaporation method or spraying
Seasoning, which comprises the steps of：（1）Principal agent and carrier are codissolved in solvent, are sufficiently stirred for；（2）By principal agent and carrier
Solution adopts rotary evaporation or spray drying method to remove solvent altogether, obtains solid dispersion.
6. Vilazodone Hydrochloride solid dispersion according to claim 1, it is characterised in that：Needed 60-200 mesh sieves pre-
It is used for the preparation of Vilazodone Hydrochloride oral cavity disintegration tablet after process.
7. according to the oral cavity disintegration tablet prepared by Vilazodone Hydrochloride solid dispersion described in claim 1, it is characterised in that：
Filler is Mannitol, Lactose, corn starch, pregelatinized Starch, one or more in Microcrystalline Cellulose.
8. according to the oral cavity disintegration tablet prepared by Vilazodone Hydrochloride solid dispersion described in claim 1, it is characterised in that：
Disintegrating agent is in Croscarmellose Sodium, carboxymethyl starch sodium, low-substituted hydroxypropyl cellulose and polyvinylpolypyrrolidone
Plant or several.
9. according to the oral cavity disintegration tablet prepared by Vilazodone Hydrochloride solid dispersion described in claim 1, it is characterised in that：
Lubricant is one or more in magnesium stearate, sodium stearyl fumarate and Pulvis Talci.
10. according to the oral cavity disintegration tablet prepared by Vilazodone Hydrochloride solid dispersion described in claim 1, its preparation method
It is as follows：By Vilazodone Hydrochloride solid dispersion, filler, disintegrating agent mixing after dry granulation, additional disintegrating agent, lubricant and
Tabletting after sweeting agent mix homogeneously.
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| Application Number | Priority Date | Filing Date | Title |
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| CN201611113819.4A CN106580895A (en) | 2016-12-07 | 2016-12-07 | Orally disintegrating tablet containing vilazodone hydrochloride solid dispersions and preparation method thereof |
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| Application Number | Priority Date | Filing Date | Title |
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| CN201611113819.4A CN106580895A (en) | 2016-12-07 | 2016-12-07 | Orally disintegrating tablet containing vilazodone hydrochloride solid dispersions and preparation method thereof |
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| WO2019172420A1 (en) * | 2018-03-09 | 2019-09-12 | 協和発酵キリン株式会社 | Pharmaceutical composition |
| WO2020119698A1 (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 |
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