CN108653222A - A kind of Pa Boxini tablet compositions - Google Patents
A kind of Pa Boxini tablet compositions Download PDFInfo
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- CN108653222A CN108653222A CN201810711614.9A CN201810711614A CN108653222A CN 108653222 A CN108653222 A CN 108653222A CN 201810711614 A CN201810711614 A CN 201810711614A CN 108653222 A CN108653222 A CN 108653222A
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- Prior art keywords
- boxini
- tablet
- lactose
- crospovidone
- aerosil
- Prior art date
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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
-
- 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
- A61K9/2009—Inorganic compounds
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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
- A61K9/2013—Organic compounds, e.g. phospholipids, fats
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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
- A61K9/2013—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
- A61K9/2027—Organic macromolecular compounds obtained by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyvinyl pyrrolidone, poly(meth)acrylates
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P15/00—Drugs for genital or sexual disorders; Contraceptives
- A61P15/14—Drugs for genital or sexual disorders; Contraceptives for lactation disorders, e.g. galactorrhoea
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
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- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
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Abstract
The present invention relates to a kind of Pa Boxini (Palbociclib) tablet compositions, belong to pharmaceutical technology field.Pa Boxini tablets of the present invention, in the tablet of unit dose, 75 125mg of Pa Boxini for being 20 40 microns containing D90,38 60mg of aerosil, 16 25mg of succinic acid, 20 36mg of lactose, 0.8 1.8mg of lauryl sodium sulfate, 16 24mg of crospovidone, 1.6 2.8mg of magnesium stearate.Technical solution of the present invention obtains a kind of tablet of qualification.
Description
Technical field
The present invention relates to a kind of Pa Boxini (Palbociclib) tablet compositions, belong to pharmaceutical technology field.
Background technology
Pa Boxini (Palbociclib), entitled 6- acetyl group -8- cyclopenta -5- methyl -2- [5- (the 1- piperazines of chemistry
Base) pyridine -2- bases amino] -8H- pyridos [2-3-d] pyrimidin-7-ones are the treatment metastatic breast cancers of Pfizer's exploitation
New drug, in the approval for obtaining food and drug administration on the 3rd in 2 months in 2015.
Pa Boxini has 2 pKa values, respectively 3 .9 and 7 .4.When pH value is less than 4, solubility is high；PH value is higher than 4
When, drug solubility is remarkably decreased, about 0 .009mg/ml.The absolute bioavailability of its conventional capsule agent is about 46%, and
And absorb with whether feed it is related, under non-fed conditions, cause the drug gastric emptying time reduce, quickly arrival small intestine (physiology
For pH higher than 4), it is about 13% to lead to bioavilability.
Pa Boxini bulk pharmaceutical chemicals dissolubilities are poor, and mobility is bad, and when tabletting, sticking is serious.Therefore, former to grind with capsule
Form lists.Capsule clinic bad adaptability, some patientss are inadaptable to be taken.201711389010 .9 of Chinese patent, discloses
A kind of tablet composition contains Pa Boxini 26%- 30%, lactitol 38%-40%, microcrystalline cellulose 28%-32%, wave
Clarke woods potassium 1%-3%, methylcellulose 1%-3%, using wet granulation, then tabletting, through repetition test, the program can only
Part overcomes the problems, such as that sticking, prepared tablet weight difference are big.
Invention content
In view of the deficiencies of the prior art, the present invention provides a kind of Pa Boxini tablet compositions meeting clinical requirement and systems
Preparation Method.
Technical solution：
A kind of Pa Boxini tablet compositions, in the tablet of unit dose, the Pa Boxini 75- for being 20-40 microns containing D90
125mg, aerosil 38-60mg, succinic acid 16-25mg, lactose 20-36mg, lauryl sodium sulfate 0.8-1.8mg,
Crospovidone 16-24mg, magnesium stearate 1.6-2.8mg.
Currently preferred technical solution is：A kind of Pa Boxini tablet compositions in the tablet of unit dose, contain
Pa Boxini the 75- 125mg, aerosil 40-56mg, succinic acid 19-23mg, lactose 26- that D90 is 20-40 microns
35mg, lauryl sodium sulfate 1.0-1.6mg, crospovidone 18-22mg, magnesium stearate 1.6-2.8mg.
Currently preferred technical solution is：A kind of Pa Boxini tablet compositions in the tablet of unit dose, contain
The Pa Boxini 100mg, aerosil 55mg, succinic acid 20mg that D90 is 20-40 microns, lactose 30mg, dodecyl sulphur
Sour sodium 1.5mg, crospovidone 20mg, magnesium stearate 2.4mg.
The preparation method of Pa Boxini tablet compositions of the present invention, includes the following steps：
The first step weighs Pa Boxini, lauryl sodium sulfate, the aerosil of recipe quantity, is added to mixer-granulator
In, it mixes 30 minutes；
Obtained by the second step first step, the succinic acid, lactose, crospovidone of recipe quantity is added, adhesive is made with 50% ethyl alcohol,
Adhesive, stirring, prepares softwood；
Softwood obtained by second step is placed in fluid bed dryer by third step, dry, whole grain；
4th step third step gained, is added the magnesium stearate of recipe quantity, tabletting.
Advantageous effect：In technical solution of the present invention, the introducing of aerosil has coated Pa Boxini particles, has overcome
The problem of sticking.The compatibility of various auxiliary materials improves the dissolution of bulk pharmaceutical chemicals, and a kind of Pa Boxini of qualification is provided for clinic
Tablet composition.
Pa Boxini 75g, aerosil 38g, succinic acid 16g, the lactose 20g that 1. D90 of embodiment is 20 microns,
Lauryl sodium sulfate 0.8g, crospovidone 16g, magnesium stearate 1.6g.1000 are prepared by preparation method described in technical solution
Piece.No sticking happens.
Pa Boxini 125g, aerosil 60g, succinic acid 25g, the lactose 36g that 2. D90 of embodiment is 40 microns,
Lauryl sodium sulfate 1.8g, crospovidone 24g, magnesium stearate 2.8g.1000 are prepared by preparation method described in technical solution
Piece.No sticking happens.
The Pa Boxini 100g, aerosil 55g, succinic acid 20g that 3. D90 of embodiment is 30 microns, lactose
30g, lauryl sodium sulfate 1.5g, crospovidone 20g, magnesium stearate 2.4g.It is prepared by preparation method described in technical solution
1000.No sticking happens.
The Pa Boxini 100g, succinic acid 20g, lactose 85g that 1. D90 of reference examples is 30 microns, lauryl sodium sulfate
1.5g, crospovidone 20g, magnesium stearate 2.4g.1000 are prepared as follows.Gas phase is replaced by the lactose of same quality
Silica.
The first step weighs the Pa Boxini of recipe quantity, lauryl sodium sulfate, is added in mixer-granulator, mixing 30
Minute；
Obtained by the second step first step, the succinic acid, lactose, crospovidone of recipe quantity is added, adhesive is made with 50% ethyl alcohol,
Adhesive, stirring, prepares softwood；
Softwood obtained by second step is placed in fluid bed dryer by third step, dry, whole grain；
4th step third step gained, is added the magnesium stearate of recipe quantity, tabletting.Sticking is serious in tableting processes.
Test example 1 removes embodiment 1-3 and each 40 of 1 product of reference examples respectively, observes the appearance of piece, observation situation record
In table 1.
Table 1
| Embodiment 1 | Embodiment 2 | Embodiment 3 | Reference examples 1 | |
| Appearance, range estimation | It is smooth, no point | It is smooth, no point | It is smooth, no point | 36 have point, and sheet border is not neat. |
Table 1 illustrates that the embodiment of the present invention can obtain the good slice, thin piece of appearance, overcomes the sticking caused by bulk pharmaceutical chemicals viscosity is big
Problem.
The difference of test example 2 and Example 1-3 and each 100 of the product of reference examples 1, it is aluminum-plastic packaged respectively, it is placed in 40
DEG C, in the climatic chamber that relative humidity is 75%, dissolution rate is measured respectively at the 30th day, 40 days, 60 days, data record is in table
2.
Table 2
2 data of table illustrate that the dissolution rate of product of the embodiment of the present invention meets standards of pharmacopoeia, and stablize during storage, even
Hot and humid environment, and stablize.
Claims (4)
1. a kind of Pa Boxini tablet compositions, characterized in that in the tablet of unit dose, the pa for being 20-40 microns containing D90
Bo Xini 75- 125mg, aerosil 38-60mg, succinic acid 16-25mg, lactose 20-36mg, lauryl sodium sulfate
0.8-1.8mg, crospovidone 16-24mg, magnesium stearate 1.6-2.8mg.
2. Pa Boxini tablet compositions according to claim 1, characterized in that in the tablet of unit dose, be containing D90
20-40 microns of Pa Boxini 75- 125mg, aerosil 40-56mg, succinic acid 19-23mg, lactose 26-35mg, ten
Sodium dialkyl sulfate 1.0-1.6mg, crospovidone 18-22mg, magnesium stearate 1.6-2.8mg.
3. Pa Boxini tablet compositions according to claim 1, characterized in that in the tablet of unit dose, be containing D90
20-40 microns of Pa Boxini 100mg, aerosil 55mg, succinic acid 20mg, lactose 30mg, lauryl sodium sulfate
1.5mg, crospovidone 20mg, magnesium stearate 2.4mg.
4. the preparation method of Pa Boxini tablet compositions described in claim 1, characterized in that include the following steps：
The first step weighs Pa Boxini, lauryl sodium sulfate, the aerosil of recipe quantity, is added to mixer-granulator
In, it mixes 30 minutes；
Obtained by the second step first step, the succinic acid, lactose, crospovidone of recipe quantity is added, adhesive is made with 50% ethyl alcohol,
Adhesive, stirring, prepares softwood；
Softwood obtained by second step is placed in fluid bed dryer by third step, dry, whole grain；
4th step third step gained, is added the magnesium stearate of recipe quantity, tabletting.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN201810711614.9A CN108653222A (en) | 2018-07-03 | 2018-07-03 | A kind of Pa Boxini tablet compositions |
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN201810711614.9A CN108653222A (en) | 2018-07-03 | 2018-07-03 | A kind of Pa Boxini tablet compositions |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| CN108653222A true CN108653222A (en) | 2018-10-16 |
Family
ID=63773602
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CN201810711614.9A Withdrawn CN108653222A (en) | 2018-07-03 | 2018-07-03 | A kind of Pa Boxini tablet compositions |
Country Status (1)
| Country | Link |
|---|---|
| CN (1) | CN108653222A (en) |
Cited By (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US11464779B2 (en) | 2016-03-29 | 2022-10-11 | Shenzhen Pharmacin Co., Ltd. | Pharmaceutical formulation of palbociclib and a preparation method thereof |
| US11471418B2 (en) | 2020-09-29 | 2022-10-18 | Shenzhen Pharmacin Co., Ltd. | Pharmaceutical compositions of amorphous solid dispersions and methods of preparation thereof |
Citations (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN105213322A (en) * | 2015-10-30 | 2016-01-06 | 南京正大天晴制药有限公司 | Pharmaceutical composition prepared by a kind of dry granulation process |
| CN105816437A (en) * | 2016-03-29 | 2016-08-03 | 深圳市华力康生物医药有限公司 | Medicinal preparation of palbociclib and preparing method thereof |
| CN107666914A (en) * | 2015-06-04 | 2018-02-06 | 辉瑞公司 | Pa Boxini solid dosage forms |
-
2018
- 2018-07-03 CN CN201810711614.9A patent/CN108653222A/en not_active Withdrawn
Patent Citations (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN107666914A (en) * | 2015-06-04 | 2018-02-06 | 辉瑞公司 | Pa Boxini solid dosage forms |
| CN105213322A (en) * | 2015-10-30 | 2016-01-06 | 南京正大天晴制药有限公司 | Pharmaceutical composition prepared by a kind of dry granulation process |
| CN105816437A (en) * | 2016-03-29 | 2016-08-03 | 深圳市华力康生物医药有限公司 | Medicinal preparation of palbociclib and preparing method thereof |
Cited By (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US11464779B2 (en) | 2016-03-29 | 2022-10-11 | Shenzhen Pharmacin Co., Ltd. | Pharmaceutical formulation of palbociclib and a preparation method thereof |
| US11471418B2 (en) | 2020-09-29 | 2022-10-18 | Shenzhen Pharmacin Co., Ltd. | Pharmaceutical compositions of amorphous solid dispersions and methods of preparation thereof |
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| PB01 | Publication | ||
| PB01 | Publication | ||
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| WW01 | Invention patent application withdrawn after publication | ||
| WW01 | Invention patent application withdrawn after publication |
Application publication date: 20181016 |