CN104523695A - Pharmaceutical composition for treating excessive proliferation diseases - Google Patents
Pharmaceutical composition for treating excessive proliferation diseases Download PDFInfo
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- CN104523695A CN104523695A CN201410635523.3A CN201410635523A CN104523695A CN 104523695 A CN104523695 A CN 104523695A CN 201410635523 A CN201410635523 A CN 201410635523A CN 104523695 A CN104523695 A CN 104523695A
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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
- A61K31/495—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
- A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
- A61K31/519—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
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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
- A61K9/14—Particulate form, e.g. powders, Processes for size reducing of pure drugs or the resulting products, Pure drug nanoparticles
- A61K9/16—Agglomerates; Granulates; Microbeadlets ; Microspheres; Pellets; Solid products obtained by spray drying, spray freeze drying, spray congealing,(multiple) emulsion solvent evaporation or extraction
- A61K9/1605—Excipients; Inactive ingredients
- A61K9/1629—Organic macromolecular compounds
- A61K9/1652—Polysaccharides, e.g. alginate, cellulose derivatives; Cyclodextrin
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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
- A61K9/2004—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
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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
- A61K9/2004—Excipients; Inactive ingredients
- A61K9/2022—Organic macromolecular compounds
- A61K9/205—Polysaccharides, e.g. alginate, gums; Cyclodextrin
- A61K9/2059—Starch, including chemically or physically modified derivatives; Amylose; Amylopectin; Dextrin
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Abstract
The invention relates to a pharmaceutical composition for treating excessive proliferation diseases, and belongs to the field of pharmaceutical preparations. The pharmaceutical composition comprises active ingredients which include 1-[(3R)-3-[4-amino-3-(4-phenoxy phenyl)-1H-pyrazol[3,4-D]pyrimidine-1-group]-1-piperidyl]-2-propylene-1-ketone, a solvate of 1-[(3R)-3-[4-amino-3-(4-phenoxy phenyl)-1H-pyrazol[3,4-D]pyrimidine-1-group]-1-piperidyl]-2-propylene-1-ketone, a hydrate and salt acceptable in pharmacy or a composition of the salt and at least one excipient acceptable in pharmacy; and the active ingredients at least occupies 30% of the composition. The pharmaceutical composition is easy to swallow; the number of times of drug feeding is decreased; the compliance of a patient can be obviously improved; in addition, the pharmaceutical composition has the good dissolution characteristic, the excellent bioavailability, the high stability and the sufficient hardness; and the pharmaceutical composition is suitable for clinic treatment of cancers. The preparation method of the pharmaceutical composition is simple and practical, and the pharmaceutical composition is suitable for industrial production.
Description
Technical field
The present invention relates to a kind of pharmaceutical composition of overmedication proliferative disease, specifically, relate to a kind of pharmaceutical composition comprising Ibrutinib and preparation method thereof, belong to field of pharmaceutical preparations.
Background technology
Ibrutinib is a kind of micromolecular tyrosine kinase (BTK) inhibitor, its chemistry 1-[(3R)-3-[4-amino-3-(4-Phenoxyphenyl)-1H-pyrazolo [3 by name, 4-D] pyrimidine-1-base]-piperidino]-2-propylene-1-ketone, concrete structure is as follows:
Ibrutinib optionally suppresses tyrosine kinase (BTK), and this enzyme is an important albumen in cellular physiological events, participates in the intracellular signaling pathways of mediation regulation and control B cell maturation and existence.In malignant B cell, B-cell receptor signal path overacfivity, Ibrutinib is by forming strong covalent bond with the cysteine residues in tyrosine kinase (BTK) active center, thus the transmission of the survival signaling of overacfivity in suppression malignant B cell, reach the effect of Tumor suppression growth and transfer.
At present, Ibrutinib preparation pertinent literature is had no.Combination of oral medication must provide the plasma activities agent level being enough to produce effectively treatment.This depends on dissolubility and the release behavior of active component, with regard to solid composite medicament, and importantly stripping property and stability.The size of solid preparation should consequently cannot well not swallowed too greatly in addition, and its size depends on the consumption of activating agent needed for effectively treating and the consumption of excipient.Develop a kind of taking convenience, the oral antineoplastic pharmaceutical compositions increasing the solid of patient compliance is necessary very much.
Summary of the invention
Summary of the invention
The present invention aims to provide a kind of pharmaceutical composition comprising high concentration Ibrutinib, this pharmaceutical composition is easily swallowed, is reduced administration number of times, patient's compliance can be significantly improved, and demonstrate good dissolution characteristic, excellent bioavailability, height stability and enough hardness, be applicable to the clinical treatment of cancer.
First aspect present invention provides a kind of pharmaceutical composition comprising high concentration Ibrutinib.
Second aspect present invention provides the preparation method of described pharmaceutical composition.
Term definition
Term " comprises " or " comprising " is open language, namely comprises the content specified by the present invention, but does not get rid of otherwise content.
Above of the present invention, no matter whether use the wording such as " approximately " or " about ", all numerals disclosed at this are approximation.The numerical value of each numeral likely there will be difference or the rational difference thought of those skilled in the art of less than 10%, as the difference of 1%, 2%, 3%, 4% or 5%.
Detailed Description Of The Invention
First aspect, the present invention relates to the pharmaceutical composition of the Ibrutinib comprising high concentration, and this pharmaceutical composition comprises Ibrutinib and the pharmaceutically acceptable excipient of at least one.
The invention provides a kind of pharmaceutical composition, it comprises 1-[(3R)-3-[4-amino-3-(4-Phenoxyphenyl)-1H-pyrazolo [3,4-D] pyrimidine-1-base]-piperidino]-2-propylene-1-ketone, its solvate, hydrate, pharmaceutically acceptable salt or their combination be as active component, and the pharmaceutically acceptable excipient of at least one, described active component at least accounts for 30% of composition weight.
Pharmaceutically acceptable excipient of the present invention includes but not limited to one or more pharmaceutically acceptable filleies, one or more pharmaceutically acceptable disintegrating agents, one or more pharmaceutically acceptable binding agents, one or more pharmaceutically acceptable lubricants, one or more pharmaceutically acceptable surfactants, one or more pharmaceutically acceptable film coating materials, one or more pharmaceutically acceptable fluidizer, one or more pharmaceutically acceptable plasticizers, one or more pharmaceutically acceptable pigments.
Filler includes but not limited to mannitol, lactose, maltose alcohol, Sorbitol, xylitol, dextrose, maltose, sucrose, glucose, fructose, maltodextrin, starch, pregelatinized Starch, microcrystalline Cellulose, silicified microcrystalline cellulose, calcium hydrogen phosphate, calcium carbonate, sodium carbonate, sodium phosphate or its combination.With the total weight of compositions, in pharmaceutical composition, the content of filler is 0%-55%.
Disintegrating agent includes but not limited to crospolyvinylpyrrolidone, cross-linking sodium carboxymethyl cellulose, alginic acid, sodium alginate, carboxymethylcellulose calcium, sodium carboxymethyl cellulose, low-substituted hydroxypropyl cellulose, microcrystalline Cellulose, polacrilin potassium, starch, sodium starch glycollate, boiling starch, carboxymethyl starch sodium or its combination.With the total weight of compositions, in pharmaceutical composition, the content of disintegrating agent is 0%-15%.
Binding agent includes but not limited to polyvinylpyrrolidone, pregelatinized Starch, methylcellulose, ethyl cellulose, hydroxypropyl cellulose, hydroxypropyl emthylcellulose, carboxymethyl cellulose, sodium carboxymethyl cellulose, carboxymethylcellulose calcium, hydroxyethyl-cellulose, ethylhydroxyethylcellulose, liquid glucose, alginic acid, polyvinyl alcohol, polyacrylate, gelatin or its combination.With the total weight of compositions, in pharmaceutical composition, the content of binding agent is 0%-15%.
Lubricant includes but not limited to magnesium stearate, calcium stearate, zinc stearate, stearic acid, fumaric acid, sodium stearyl fumarate, Polyethylene Glycol, Glyceryl Behenate or its combination.With the total weight of compositions, in pharmaceutical composition, the content of lubricant is 0%-5%.
Surfactant includes but not limited to lecithin, benzalkonium chloride, sorbitol monooleate, poly yamanashi esters, sorbitan monopalmitate, sodium lauryl sulphate, dioctyl sodium sulphosuccinate, sorbitan mono-laurate, glyceryl monostearate, the ester of fatty acid and polyvinyl alcohol, Polyethylene Glycol sorbitan mono-laurate, Polyethylene Glycol sorbitan monostearate, Polyethylene Glycol sorbitan monooleate, the ether of fatty alcohol and polyvinyl alcohol, the copolymer of ethylene oxide and propylene oxide and ethoxylated triglycerides, polyoxyethylene 80 sorbitan monooleate, Myrj 45, polyoxyethylene 20 sorbitan monolaurate.With the total weight of compositions, in pharmaceutical composition, the content of surfactant is 0%-8%.
Pharmaceutical composition of the present invention is finally prepared into the appropriate dosage forms of rapid release of active ingredients, as capsule, tablet, coated tablet, chewable tablet, dispersible tablet, granule, pill.
When pharmaceutical composition of the present invention is tablet, coating can also be carried out through thin film further.Wherein film coating agent comprises coating material, fluidizer, plasticizer, pigment.Wherein coating material includes but not limited to hydroxypropyl emthylcellulose, hydroxypropyl cellulose, ethyl cellulose; Fluidizer includes but not limited to Pulvis Talci, micropowder silica gel; Plasticizer includes but not limited to propylene glycol, Polyethylene Glycol, triethyl citrate, Polysorbate, Oleum Ricini; Pigment includes but not limited to red No. 3 of pigment, inorganic pigment, FD & C, red No. 20 of FD & C, yellow No. 6 of FD & C, blue No. 2 of FD & C, green No. 5 of D & C, red No. 8 of orange No. 5 of D & C, D & C, caramel, iron oxide red, iron oxide yellow, titanium dioxide.
In some embodiments, with the weighing scale of compositions, described pharmaceutical composition comprises at least 45% active component.
In some embodiments, with the weighing scale of compositions, described pharmaceutical composition comprises at least 60% active component.
In some embodiments, with the weighing scale of compositions, described pharmaceutical composition comprise at least 30% active component, 0%-55% filler, 0%-15% binding agent, 0%-15% disintegrating agent, 0%-8% surface active ingredient and 0%-5% lubricant.
In some embodiments, with the weighing scale of compositions, it comprise 1-[(3R)-3-[4-amino-3-(4-Phenoxyphenyl)-1H-pyrazolo [3,4-D] pyrimidine-1-base]-the piperidino]-2-propylene-1-ketone of at least 30%, the mannitol of 0%-55% as filler, 0%-15% microcrystalline Cellulose as binding agent, 0%-15% cross-linking sodium carboxymethyl cellulose as disintegrating agent, 0%-8% sodium lauryl sulphate as surfactant and 0%-5% magnesium stearate as lubricant.
Second aspect, the present invention relates to the preparation method preparing described pharmaceutical composition.
Wet granulation is the method preparing capsule or compressed tablets be widely used.Be divided into as follows by the method step prepared needed for capsule or tablet: (1) weighs and hybrid medicine composition; (2) wet granular is prepared; (3) wet granular is sieved into bead or granule, dry wet particle; (4) dry pellet through sieves; (5) lubricate and mix; (6) be filled to capsule or be compressed into tablet.Weighing active component and in being mixed with disintegrating agent by active component, always the whole amount of disintegrating agent all not joined in medicine and other excipient mixture, but a part is remained, joining together with lubricant in the drug particles prepared.By adding granulation solution in powder mixture, make the screen cloth in order footpath of moistening material by wanting, dried particles, then by less second screen cloth in order footpath to subtract short grained size further, complete described granulation.Usually, moistening granule is pressed through mesh.After total material is all converted to granule, by particle drying.After drying, usually lubricant is added in granule, to make each granule be covered with lubricant, be finally filled to capsule or be pressed into tablet.
In wet granulation method, granulation solvent can be purified water, ethanol, methanol, isopropyl alcohol, acetone, and solvent is volatile components, and it does not remain in end product.By active component, disintegrating agent and other excipient premixings except lubricant, shearing force granulator is usually used to granulate.
Dry granulation method is by being compressed by a large amount of mixture, is pulverized subsequently again and these fragments is made less granule to form granule, and then being filled to capsule or being compressed into large plain film or pill.
Powder direct pressure closing directly medicine and adjuvant is sieved without pelletization, and mix homogeneously, carries out filled capsules or tabletting.
In some embodiments, the method for pharmaceutical compositions comprises:
(1) in high shear granulator, mix all the components except lubricant and disintegrating agent;
(2) pure water is used to carry out pelletize as Granulation fluid;
(3) dried particles in fluidized bed pelletizer;
(4) with the granule of vibrosieve mill dry, suitable particle size is reached;
(5) with appropriate size by the granule that sieves and mix lubricant even;
(6) be filled to capsule or be pressed into tablet.
In some embodiments, the method for pharmaceutical compositions comprises:
(1) in high shear granulator, mix all the components except lubricant and Extra Section disintegrating agent;
(2) pure water is used to carry out pelletize as Granulation fluid;
(3) dried particles in fluidized bed pelletizer;
(4) with the granule of vibrosieve mill dry, suitable particle size is reached;
(5) with appropriate size, the granule sieved is mixed with the disintegrating agent of Extra Section;
(6) lubricant is added and mix homogeneously;
(7) be filled to capsule or be pressed into tablet.
Detailed description of the invention
In order to make those skilled in the art understand technical scheme of the present invention better, below disclose further some non-limiting embodiments the present invention is described in further detail.
Reagent used in the present invention all can be buied from the market or can be obtained by method described in the invention preparation.
In the present invention, min represents minute, and mg represents milligram, and mL represents milliliter.
Embodiment 1
Prescription
| Component | Prescription ratio (%) | Recipe quantity (mg) |
| Ibrutinib | 75.0 | 140.0 |
| Mannitol | 10.7 | 20.0 |
| Microcrystalline Cellulose | 5.8 | 10.8 |
| Cross-linking sodium carboxymethyl cellulose | 6.6 | 12.3 |
| Sodium lauryl sulphate | 1.1 | 2.1 |
| Magnesium stearate | 0.8 | 1.5 |
Preparation method:
(1) in high shear granulator, mix 140.0mg Ibrutinib, 20.0mg mannitol, 10.8mg microcrystalline Cellulose, 12.3mg cross-linking sodium carboxymethyl cellulose and 2.1mg sodium lauryl sulphate;
(2) pure water is used to carry out pelletize as Granulation fluid;
(3) dried particles in fluidized bed pelletizer;
(4) with the granule of vibrosieve mill dry, suitable particle size is reached;
(5) with appropriate size, the granule sieved is mixed homogeneously with 1.5mg magnesium stearate;
(6) be filled to capsule, be prepared into capsule.
Embodiment 2
Prescription
| Component | Prescription ratio (%) | Recipe quantity (mg) |
| Ibrutinib | 60.0 | 280.0 |
| Microcrystalline Cellulose | 20.8 | 97.1 |
| Polyvinylpyrrolidone | 9.0 | 42.0 |
| Low-substituted hydroxypropyl cellulose | 8.3 | 38.7 |
| Sodium lauryl sulphate | 0.9 | 4.2 |
| Sodium stearyl fumarate | 1.0 | 4.7 |
Preparation method:
(1) in high shear granulator, mix 280.0mg Ibrutinib, 97.1mg microcrystalline Cellulose, 42.0mg polyvinylpyrrolidone, 4.2mg sodium lauryl sulphate and 20.7mg low-substituted hydroxypropyl cellulose;
(2) pure water is used to carry out pelletize as Granulation fluid;
(3) dried particles in fluidized bed pelletizer;
(4) with the granule of vibrosieve mill dry, suitable particle size is reached;
(5) with appropriate size, the granule sieved is mixed with 18.0mg disintegrating agent;
(6) 4.7mg sodium stearyl fumarate is added and mix homogeneously;
(7) be filled to capsule, be prepared into capsule.
Embodiment 3
Prescription
| Component | Prescription ratio (%) | Recipe quantity (mg) |
| Ibrutinib | 60.0 | 140.0 |
| Pregelatinized Starch | 15.8 | 36.9 |
| Hydroxypropyl cellulose | 12.6 | 29.4 |
| Crospolyvinylpyrrolidone | 10.1 | 23.6 |
| Sodium lauryl sulphate | 1.0 | 2.3 |
| Magnesium stearate | 0.5 | 1.2 |
Preparation method:
(1) in high shear granulator, mix 140.0mg Ibrutinib, 36.9mg pregelatinized Starch, 29.4mg hydroxypropyl cellulose, 10.2mg crospolyvinylpyrrolidone and 2.3mg sodium lauryl sulphate;
(2) pure water is used to carry out pelletize as Granulation fluid;
(3) dried particles in fluidized bed pelletizer;
(4) with the granule of vibrosieve mill dry, suitable particle size is reached;
(5) with appropriate size, the granule sieved is mixed with 13.4mg crospolyvinylpyrrolidone;
(6) 1.2mg magnesium stearate is added and mix homogeneously;
(7) tablet is pressed into.
Embodiment 4
Prescription
| Component | Prescription ratio (%) | Recipe quantity (mg) |
| Ibrutinib | 80.0 | 280.0 |
| Lactose | 9.3 | 32.6 |
| Polyvinylpyrrolidone | 4.0 | 14.0 |
| Sodium carboxymethyl cellulose | 5.1 | 17.9 |
| Sodium lauryl sulphate | 0.9 | 3.2 |
| Glyceryl Behenate | 0.7 | 2.5 |
Preparation method:
(1) in high shear granulator, mix 280.0mg Ibrutinib, 32.6mg lactose, 14.0mg polyvinylpyrrolidone, 8.9mg sodium carboxymethyl cellulose and 3.2mg sodium lauryl sulphate;
(2) pure water is used to carry out pelletize as Granulation fluid;
(3) dried particles in fluidized bed pelletizer;
(4) with the granule of vibrosieve mill dry, suitable particle size is reached;
(5) with appropriate size, the granule sieved is mixed with 9.0mg sodium carboxymethyl cellulose;
(6) 2.5mg Glyceryl Behenate is added and mix homogeneously;
(7) tablet is pressed into.
Embodiment 5 stability test
With reference to the long term test method in the pharmaceutical preparation stability test of " Chinese Pharmacopoeia " version in 2010 two annex XIXC, stability test is carried out to the preparation prepared by embodiment 1 ~ 4.By tablet in temperature 25 DEG C ± 2 DEG C, place 24 months under the condition of relative humidity 60% ± 10%, respectively at sampling in 0 month, 3 months, 6 months, 9 months, 12 months, 24 months, measure active component content by high performance liquid chromatography (HPLC), test result was in table 1.
Table 1. embodiment 1 ~ 4 preparation long-term stable experiment result
Stability result shows, pharmaceutical composition provided by the invention is in temperature 25 DEG C ± 2 DEG C, and place 24 months under the condition of relative humidity 60% ± 10%, active component content still remains on more than 98%, shows excellent stability.
Method of the present invention is described by preferred embodiment, and related personnel obviously can change methods and applications as herein described or suitably change and combination in content of the present invention, spirit and scope, realizes and applies the technology of the present invention.Those skilled in the art can use for reference present disclosure, and suitable improving technique parameter realizes.Special needs to be pointed out is, all similar replacements and change apparent to those skilled in the art, they are all deemed to be included in the present invention.
Claims (10)
1. a pharmaceutical composition, it comprises 1-[(3R)-3-[4-amino-3-(4-Phenoxyphenyl)-1H-pyrazolo [3,4-D] pyrimidine-1-base]-piperidino]-2-propylene-1-ketone, its solvate, hydrate, pharmaceutically acceptable salt or their combination be as active component, and the pharmaceutically acceptable excipient of at least one, described active component at least accounts for 30% of composition weight.
2. pharmaceutical composition according to claim 1, with the weighing scale of compositions, it comprises at least 45% active component.
3. pharmaceutical composition according to claim 1, with the weighing scale of compositions, it comprises at least 60% active component.
4. pharmaceutical composition according to claim 1, with the weighing scale of compositions, it comprise at least 30% active component, 0%-55% filler, 0%-15% binding agent, 0%-15% disintegrating agent, 0%-8% surface active ingredient and 0%-5% lubricant.
5. according to the pharmaceutical composition of claim 1-4 described in any one, with the weighing scale of compositions, it comprise 1-[(3R)-3-[4-amino-3-(4-Phenoxyphenyl)-1H-pyrazolo [3,4-D] pyrimidine-1-base]-the piperidino]-2-propylene-1-ketone of at least 30%, the mannitol of 0%-55% as filler, 0%-15% microcrystalline Cellulose as binding agent, 0%-15% cross-linking sodium carboxymethyl cellulose as disintegrating agent, 0%-8% sodium lauryl sulphate as surface activity and 0%-5% magnesium stearate as lubricant.
6. pharmaceutical composition according to claim 1, its dosage form is oral solid formulation.
7. pharmaceutical composition according to claim 1, its dosage form is capsule.
8. prepare a method for the pharmaceutical composition of claim 1-7 described in any one, comprise the following steps:
1) active component and the pharmaceutically acceptable excipient of at least one are carried out wet granulation;
2) by granule and lubricant or other pharmaceutically acceptable mixed with excipients even;
3) be filled to capsule or be pressed into tablet.
9. method according to claim 8, can mix described active component and the pharmaceutically acceptable excipient of at least one without granulation, and directly be filled to capsule or tabletted.
10. method according to claim 8, active component and the pharmaceutically acceptable excipient of at least one can directly be filled to capsule or tabletted after dry granulation method process.
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Cited By (10)
| Publication number | Priority date | Publication date | Assignee | Title |
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| CN105399756A (en) * | 2014-09-05 | 2016-03-16 | 广东东阳光药业有限公司 | BTK inhibitor and uses thereof |
| WO2016164404A1 (en) * | 2015-04-06 | 2016-10-13 | Janssen Pharmaceutica Nv | Compositions containing ibrutinib |
| US9655857B2 (en) | 2015-03-03 | 2017-05-23 | Pharmacyclics Llc | Pharmaceutical formulations of a Bruton's tyrosine kinase inhibitor |
| US9713617B2 (en) | 2012-06-04 | 2017-07-25 | Pharmacyclics Llc | Crystalline forms of a Bruton's tyrosine kinase inhibitor |
| WO2017125423A1 (en) * | 2016-01-19 | 2017-07-27 | Janssen Pharmaceutica Nv | Formulations/compositions comprising a btk inhibitor |
| US20180028537A1 (en) | 2014-08-07 | 2018-02-01 | Pharmacyclics Llc | Novel Formulations of a Bruton's Tyrosine Kinase Inhibitor |
| CN108472258A (en) * | 2016-01-19 | 2018-08-31 | 詹森药业有限公司 | Include preparation/composition of BTK inhibitor |
| CN108653231A (en) * | 2017-04-01 | 2018-10-16 | 北京赛林泰医药技术有限公司 | Composition and preparation method thereof containing bruton's tyrosine kinase inhibitor |
| CN116211865A (en) * | 2023-01-04 | 2023-06-06 | 中国农业大学 | Application of compound Ibrutinib in preparation of antiviral drugs and pharmaceutical composition |
| CN108472258B (en) * | 2016-01-19 | 2024-05-24 | 詹森药业有限公司 | Formulations/compositions comprising BTK inhibitors |
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| US9713617B2 (en) | 2012-06-04 | 2017-07-25 | Pharmacyclics Llc | Crystalline forms of a Bruton's tyrosine kinase inhibitor |
| US20180028537A1 (en) | 2014-08-07 | 2018-02-01 | Pharmacyclics Llc | Novel Formulations of a Bruton's Tyrosine Kinase Inhibitor |
| CN105399756B (en) * | 2014-09-05 | 2019-06-25 | 广东东阳光药业有限公司 | BTK inhibitor and application thereof |
| CN105399756A (en) * | 2014-09-05 | 2016-03-16 | 广东东阳光药业有限公司 | BTK inhibitor and uses thereof |
| US9655857B2 (en) | 2015-03-03 | 2017-05-23 | Pharmacyclics Llc | Pharmaceutical formulations of a Bruton's tyrosine kinase inhibitor |
| US10010507B1 (en) | 2015-03-03 | 2018-07-03 | Pharmacyclics Llc | Pharmaceutical formulations of a bruton's tyrosine kinase inhibitor |
| US10828259B2 (en) | 2015-03-03 | 2020-11-10 | Pharmacyclics Llc | Pharmaceutical formulations of a Bruton's tyrosine kinase inhibitor |
| US10213386B2 (en) | 2015-03-03 | 2019-02-26 | Pharmacyclics Llc | Pharmaceutical formulations of a Bruton's tyrosine kinase inhibitor |
| WO2016164404A1 (en) * | 2015-04-06 | 2016-10-13 | Janssen Pharmaceutica Nv | Compositions containing ibrutinib |
| EA033992B1 (en) * | 2015-04-06 | 2019-12-17 | Янссен Фармацевтика Нв | Compositions containing ibrutinib |
| CN108472258B (en) * | 2016-01-19 | 2024-05-24 | 詹森药业有限公司 | Formulations/compositions comprising BTK inhibitors |
| CN108472258A (en) * | 2016-01-19 | 2018-08-31 | 詹森药业有限公司 | Include preparation/composition of BTK inhibitor |
| WO2017125423A1 (en) * | 2016-01-19 | 2017-07-27 | Janssen Pharmaceutica Nv | Formulations/compositions comprising a btk inhibitor |
| CN108653231A (en) * | 2017-04-01 | 2018-10-16 | 北京赛林泰医药技术有限公司 | Composition and preparation method thereof containing bruton's tyrosine kinase inhibitor |
| CN116211865A (en) * | 2023-01-04 | 2023-06-06 | 中国农业大学 | Application of compound Ibrutinib in preparation of antiviral drugs and pharmaceutical composition |
| CN116211865B (en) * | 2023-01-04 | 2024-03-29 | 中国农业大学 | Application of compound Ibrutinib in preparation of antiviral drugs and pharmaceutical composition |
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