CN105943510A - Idelalisib preparation and application thereof - Google Patents
Idelalisib preparation and application thereof Download PDFInfo
- Publication number
- CN105943510A CN105943510A CN201610408599.1A CN201610408599A CN105943510A CN 105943510 A CN105943510 A CN 105943510A CN 201610408599 A CN201610408599 A CN 201610408599A CN 105943510 A CN105943510 A CN 105943510A
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- CN
- China
- Prior art keywords
- dailalisi
- purposes
- idelalisib
- preparation
- content
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- Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
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Classifications
-
- 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
- A61K31/52—Purines, e.g. adenine
-
- 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
-
- 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
- A61K9/48—Preparations in capsules, e.g. of gelatin, of chocolate
- A61K9/4841—Filling excipients; Inactive ingredients
- A61K9/4866—Organic macromolecular compounds
Abstract
The invention discloses an idelalisib preparation and application thereof. The idelalisib preparation is prepared from idelalisib, lactose, microcrystalline cellulose and a carrier acceptable to pharmacy. The idelalisib preparation which is good in mobility, stability and dissolution rate can be obtained, and thus the idelalisib preparation is suitable for industrialized mass production. The idelalisib preparation is a pharmaceutical composition for treating recurrent follicular B cell non-hodgkin lymphoma (FL) and recurrent small lymphocytic lymphoma (SLL), is reasonable in matching, capable of rapidly releasing medicine and capable of generating a quite good curative effect on symptoms of diseases.
Description
Technical field
The present invention relates to Ai Dailalisi for preparing the purposes of medicine, in particular for preparation be suitable to the tablet that is administered orally and
Capsule.
Ai Dailalisi (Idelalisib), be for treat recurrent follicular B cells non-Hodgkin lymphoma (FL) and
Three kind new medicines of recurrent small lymphocyte lymphoma (SLL), currently carry out preclinical study.
Background technology
Ai Dailalisi Idelalisib is oral, the selective phosphoinositide 3-kinase delta of first listing
(PI3K-delta, P110-delta) inhibitor.P110-delta participates in changing the immune environment of bone-marrow-derived lymphocyte, to this kind of swollen
The activation of oncocyte, breed, survive and migrate (trafficking) and play pivotal role.Ai Dailalisi Idelalisib's
Accelerating approval is based on a single armed, multicenter, the actively second phase clinical effectiveness of open label.This clinical experiment has recruited 123
The 'inertia' non-Hodgkin lymphoma (iNHL) of position recurrent and small lymphocyte lymphoma (SLL) patient.Patient accepts every day
Twice, each 150 milligrams of Chinese mugworts are for this treatment of Larry, and one-level experimental endpoints is total response rate (ORR), and two grades of experimental endpoints are responses
Time and Progression free survival phase.Wherein total response rate of FL and SLL patient is respectively 54% and 58%.The middle position of the latter's response time
Number is 11.9 months.This result is compared quite with the usual curative effect of standard treatment or more preferably.Ai Dailalisi
(Idelalisib) granted listing, the treatment for chronic lymphocytic leukemia (CLL) brings again one after ibrutinib
Individual new selection.In the U.S., chronic lymphocytic leukemia (CLL) number in Patients With Adult Leukemia ranked second, it is contemplated that
Within 2014, can increase more than 15000 new patients.CLL new drug development including Idelalisib and ibrutinib, is expected to
CLL is developed into a kind of controllable chronic disease from death sentence.Certainly, correspondingly CLL market the most gradually expands, Bloomberg News
Analyst thinks will rise 9,000,000,000 dollars soon in CLL market.
Summary of the invention
The present invention relates to the pharmaceutical composition containing Ai Dailalisi and this based composition and treat recurrence for safely and effectively
Property follicular B cells non-Hodgkin lymphoma (FL) and recurrent small lymphocyte lymphoma (SLL).
The invention still further relates to the pharmaceutical composition containing Ai Dailalisi Yu the oral administration of other drug active substance.Should
Compositions is to be obtained by the surface making the granule of pharmaceutically active substance adhere to carrier matrix.Make pharmaceutically active substance calm
Method on carrier matrix is minimum in order to make the gathering of active substance/carrier substrate particles be reduced to.
The present invention relates to the pharmaceutical composition containing about 10mg--350 mg Ai Dailalisi, said composition is given daily three
Secondary for chronic heart failure；The preferred pharmaceutical composition of hypertension contains the Ai Dailalisi of about 50mg--250 mg,
Most preferably pharmaceutical composition contains the Ai Dailalisi of about 50mg--200 mg.Further, this kind of preferred and most preferred medicine
Compositions be given daily 2 times thin for treating recurrent follicular B cells non-Hodgkin lymphoma (FL) and recurrent primary lymphedema
Born of the same parents' lymphoma (SLL).
Above-mentioned Ai Dailali pharmacist's compositions for being given daily also can be the most regular some patient is administered.
This maintaining treatment scheme include every day not enough once take Ai Dailali pharmacist's compositions.Such as, within every three or four days, give
Once just it is enough for medicine.
Ai Dailali pharmacist's compositions of the present invention can be configured to the form through any suitable administration, the most preferably
Oral administration combination can be tablet, capsule, granule or powder type.According to method well known in the art, Ai Dailalisi
Pharmaceutical composition can be to be configured to the form that parenteral, rectum or via intranasal application are administered.This kind of preparation can include pharmaceutically acceptable figuration
Agent, described excipient includes in this based composition conventional filler, fluidizer, lubricant, disintegrating agent, binding agent etc..This
Bright also include slow releasing preparation.
Tablet and capsule preparations containing about 50mg 200mg Ai Dailalisi can be prepared by the following method, with
Guarantee the efficient of product and good uniformity.First Ai Dailalisi calmness is prepared group on the surface of carrier matrix
Compound.This step is completed by following operation: form Ai Dailalisi and the solution of adhesive material, then at carrier matrix
Grain applies this solution while keeping motion in the way of spraying.Control condition is so that the gathering of granule is preferably minimized.
Any other composition that will comprise in granule and compositions after drying, such as disintegrating agent/fluidizer/lubricant mix
Close.Then the powder obtained it is pressed into sheet or is filled into capsule.
Preferred solvent in said method is the ethanol of water or variable concentrations.
Adhesive material preferably has the polymer of high-consistency.The material being suitable for includes polyvidone, methylcellulose, hydroxyl
Methylcellulose, hydroxypropyl methylcellulose, hydroxypropyl cellulose, hydroxyethyl cellulose, polyvidone, hydroxymethyl cellulose are preferred
's.In whole compositions, the content of adhesive material is preferably the about 1%--about 10%(weight of compositions gross weight).
The disintegrant content that whole compositions includes is preferably the about 1%--7% of compositions gross weight.The disintegrating agent being suitable for includes
Polyvinylpolypyrrolidone, cross-linked carboxymethyl cellulose, low-substituted hydroxypropyl methylcellulose, Explotab, pregelatinized Starch and Semen Maydis
Starch, polyvinylpolypyrrolidone is preferred.
The lubricant content that whole compositions includes is preferably the about 1%--5% of compositions gross weight.The lubricant being suitable for includes
Micropowder silica gel, magnesium stearate, stearic acid, stearyl fumarate and sodium lauryl sulfate, micropowder silica gel, magnesium stearate are preferred
's.
Detailed description of the invention
The Ai Dailalisi compositions of the following example explanation present invention
Embodiment 1
Said method is used to prepare 50 milligrams of Ai Dailalisi capsules
| Composition | Amount %(w/w) | Amount/grain |
| Ai Dailalisi | 20.00 | 50mg |
| Microcrystalline Cellulose | 37.60 | 94 mg |
| Lactose | 28.00 | 70 mg |
| Polyvidone | 4.00 | 10 mg |
| Low-substituted hydroxypropyl methylcellulose | 8.00 | 20.0mg |
| Magnesium stearate | 0.80 | 2.0mg |
| Silicon dioxide | 1.6 | 4.0 mg |
| Purified water | In right amount | In right amount |
| Amount to | 100.00 | 250.00 mg |
Embodiment 2
Said method is used to prepare 100 milligrams of Ai Dailalisi capsules
| Composition | Amount %(w/w) | Amount/grain |
| Ai Dailalisi | 27.60 | 100 mg |
| Microcrystalline Cellulose | 27.60 | 100 mg |
| Lactose | 41.44 | 150 mg |
| Polyvidone | 8.29 | 30mg |
| Polyvinylpolypyrrolidone | 8.29 | 30mg |
| Silicon dioxide | 0.55 | 2.00mg |
| Purified water | In right amount | In right amount |
| Amount to | 100.00 | 362.00 mg |
Embodiment 3
Said method is used to prepare 150 milligrams of Ai Dailalisi capsules
| Composition | Amount %(w/w) | Amount/piece |
| Ai Dailalisi | 38.31 | 150 mg |
| Microcrystalline Cellulose | 12.77 | 50 mg |
| Lactose | 38.31 | 150 mg |
| Polyvidone | 2.55 | 10 mg |
| Polyvinylpolypyrrolidone | 5.10 | 20 mg |
| Low-substituted hydroxypropyl methylcellulose | 2.55 | 10 mg |
| Magnesium stearate | 0.38 | 1.5 mg |
| Purified water | In right amount | In right amount |
| Amount to | 100.00 | 391.50 mg |
Embodiment 4
Said method is used to prepare 100 milligrams of Ai Dailalisi sheets
| Composition | Amount %(w/w) | Amount/piece |
| Ai Dailalisi | 25.00 | 100 mg |
| Microcrystalline Cellulose | 25.00 | 100 mg |
| Lactose | 37.50 | 150 mg |
| Polyvidone | 2.50 | 10 mg |
| Low-substituted hydroxypropyl methylcellulose | 5.00 | 20 mg |
| Magnesium stearate | 2.5 | 10 mg |
| Silicon dioxide | 2.5 | 10 mg |
| Purified water | In right amount | In right amount |
| Amount to | 100.00 | 401.50 mg |
Embodiment 5
Said method is used to prepare 150 milligrams of Ai Dailalisi sheets
| Composition | Amount %(w/w) | Amount/piece |
| Ai Dailalisi | 38.31 | 150 mg |
| Microcrystalline Cellulose | 12.77 | 50 mg |
| Lactose | 38.31 | 150 mg |
| Polyvidone | 2.55 | 10 mg |
| Polyvinylpolypyrrolidone | 5.10 | 20 mg |
| Low-substituted hydroxypropyl methylcellulose | 2.55 | 10 mg |
| Magnesium stearate | 0.38 | 1.5 mg |
| Purified water | In right amount | In right amount |
| Amount to | 100.00 | 391.50 mg |
Embodiment 6
Said method is used to prepare 200 milligrams of Ai Dailalisi sheets
| Composition | Amount %(w/w) | Amount/grain |
| Ai Dailalisi | 51.02 | 200 mg |
| Microcrystalline Cellulose | 12.76 | 50 mg |
| Lactose | 38.27 | 150 mg |
| Polyvidone | 5.10 | 20mg |
| Polyvinylpolypyrrolidone | 5.10 | 20mg |
| Magnesium stearate | 0.5 | 2.00mg |
| Purified water | In right amount | In right amount |
| Amount to | 100.00 | 392.00 mg |
Embodiment 7
Said method is used to prepare 50 milligrams of Ai Dailalisi sheets
| Composition | Amount %(w/w) | Amount/grain |
| Ai Dailalisi | 20.00 | 50mg |
| Microcrystalline Cellulose | 37.60 | 94 mg |
| Lactose | 28.00 | 70 mg |
| Polyvidone | 4.00 | 10 mg |
| Low-substituted hydroxypropyl methylcellulose | 8.00 | 20.0mg |
| Magnesium stearate | 0.80 | 2.0mg |
| Silicon dioxide | 1.6 | 4.0 mg |
| Purified water | In right amount | In right amount |
| Amount to | 100.00 | 250.00 mg |
Claims (9)
1. Ai Dailalisi is used for preparing oral administration every day 1 time for treating recurrent follicular B cells non-Hodgkin lymphoma
And recurrent small lymphocyte lymphoma (SLL) (FL), the purposes of pharmaceutical composition in the form of tablets or capsules, wherein said
Pharmaceutical composition contains the Ai Dailalisi of 10mg 350mg.
2. the purposes of claim 1, the content of wherein said Ai Dailalisi is 20mg 250mg.
3. the purposes of claim 1, the content of wherein said Ai Dailalisi is 50mg 200mg.
4. the purposes of claim 3, the content of wherein said Ai Dailalisi is 50mg.
5. the purposes of claim 3, the content of wherein said Ai Dailalisi is 100mg.
6. the purposes of claim 3, the content of wherein said Ai Dailalisi is 150mg.
7. the purposes of claim 3, the content of wherein said Ai Dailalisi is 200mg.
8. the purposes of claim 1, described compositions therein contains one or more other drug active substances.
9. the purposes of claims 1, wherein said filler is selected from lactose, xylitol, microcrystalline Cellulose, dextrin, manna
Alcohol, sorbitol, sucrose, starch, pregelatinized Starch, glucose, calcium phosphate, calcium hydrogen phosphate, calcium carbonate, and mixture, and
Described Ai Dailalisi be by have enough stickiness polymerization emplastic stick together on described filler.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN201610408599.1A CN105943510A (en) | 2016-06-13 | 2016-06-13 | Idelalisib preparation and application thereof |
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN201610408599.1A CN105943510A (en) | 2016-06-13 | 2016-06-13 | Idelalisib preparation and application thereof |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| CN105943510A true CN105943510A (en) | 2016-09-21 |
Family
ID=56908828
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CN201610408599.1A Pending CN105943510A (en) | 2016-06-13 | 2016-06-13 | Idelalisib preparation and application thereof |
Country Status (1)
| Country | Link |
|---|---|
| CN (1) | CN105943510A (en) |
Citations (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN104262344A (en) * | 2014-08-22 | 2015-01-07 | 苏州明锐医药科技有限公司 | A preparing method of Idelalisib |
| CN105073128A (en) * | 2013-04-03 | 2015-11-18 | Ibc药品公司 | Combination therapy for inducing immune response to disease |
| CN105380956A (en) * | 2015-11-04 | 2016-03-09 | 张陆军 | Medicine composition which is used for treating leukemia and contains idelalisi and application |
-
2016
- 2016-06-13 CN CN201610408599.1A patent/CN105943510A/en active Pending
Patent Citations (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN105073128A (en) * | 2013-04-03 | 2015-11-18 | Ibc药品公司 | Combination therapy for inducing immune response to disease |
| CN104262344A (en) * | 2014-08-22 | 2015-01-07 | 苏州明锐医药科技有限公司 | A preparing method of Idelalisib |
| CN105380956A (en) * | 2015-11-04 | 2016-03-09 | 张陆军 | Medicine composition which is used for treating leukemia and contains idelalisi and application |
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| Date | Code | Title | Description |
|---|---|---|---|
| C06 | Publication | ||
| PB01 | Publication | ||
| C10 | Entry into substantive examination | ||
| SE01 | Entry into force of request for substantive examination | ||
| WD01 | Invention patent application deemed withdrawn after publication |
Application publication date: 20160921 |
|
| WD01 | Invention patent application deemed withdrawn after publication |