CN113712932A - Tofacitinib citrate osmotic pump tablet and preparation method thereof - Google Patents
Tofacitinib citrate osmotic pump tablet and preparation method thereof Download PDFInfo
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- CN113712932A CN113712932A CN202010448495.XA CN202010448495A CN113712932A CN 113712932 A CN113712932 A CN 113712932A CN 202010448495 A CN202010448495 A CN 202010448495A CN 113712932 A CN113712932 A CN 113712932A
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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
- A61K9/28—Dragees; Coated pills or tablets, e.g. with film or compression coating
- A61K9/2806—Coating materials
- A61K9/2833—Organic macromolecular compounds
- A61K9/286—Polysaccharides, e.g. gums; Cyclodextrin
- A61K9/2866—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
- 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
- A61K9/0002—Galenical forms characterised by the drug release technique; Application systems commanded by energy
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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
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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
- A61K9/2027—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
- 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
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P19/00—Drugs for skeletal disorders
- A61P19/02—Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
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Abstract
The invention relates to tofacitinib citrate and a pharmaceutically acceptable salt osmotic pump tablet and a preparation method thereof, and the osmotic pump tablet comprises a single-layer drug-containing tablet core and a controlled-release film coating, wherein the tablet core contains 5-60 wt% of tofacitinib citrate or pharmaceutically acceptable salt thereof, 10-50 wt% of a filling agent, 0-10 wt% of an osmotic pressure promoter, 5-40 wt% of a pH regulator and 2-10 wt% of an adhesive, the controlled-release film coating material contains 2-10 wt% of the osmotic pump tablet based on the weight of the drug-containing tablet core, and the controlled-release film coating material contains 10-90 wt% of a pore-forming agent and 0-10 wt% of a plasticizer based on the weight of the controlled-release film coating material. The tofacitinib citrate osmotic pump tablet has zero-order release rate, can improve the treatment compliance of patients, avoid or reduce the great fluctuation of blood concentration, and reduce toxic and side effects.
Description
Technical Field
The invention belongs to the field of pharmaceutical preparations, and particularly relates to a tofacitinib citrate osmotic pump tablet which is a preparation for treating rheumatoid arthritis and is suitable for being orally taken once a day.
Background
On day 11/6 of 2012, jointly announced by the united states Food and Drug Administration (FDA) and the company feverre, Xeljanz (tofacitinib citrate) was approved for adult patients with moderate to severe active Rheumatoid Arthritis (RA) who responded poorly or intolerant to methotrexate treatment. Xeljanz is a Janus kinase inhibitor. The inhibition strength of tofacitinib on JAK3 is 5-100 times that of JAK1 and JAK 2. Tofacitinib is the first-in-class drug (first-in-drug) developed for the treatment of rheumatoid arthritis (rhematoid arthritis). Since the birth of tofacitinib in the fevered own laboratory, it was held the hope of weighing a pound of drug.
Tofacitinib (CP-690550) is a novel oral JAK pathway inhibitor developed by Perey. Unlike most other RA therapeutics currently acting primarily on extracellular targets, tofacitinib targets intracellular signal transduction pathways, acting on the core of the cytokine network.
Indications are as follows: rheumatoid arthritis where methotrexate is poorly responsive or intolerant. Can be used as monotherapy or in combination with methotrexate or other non-biological disease modifying antirheumatic drugs
JAK (Janus Kinase) is a non-receptor tyrosine protein kinase (PTK), and the members of the protein family have 7 homologous regions (JH 1-7), wherein a JH1 region is a kinase region, and a JH2 region is a pseudo-kinase region. Unlike other PTKs, JAKs lack the Src homology 2 (SH2) structure, which can be activated by either catalyzing tyrosine phosphorylation of cytokine receptors linked to them, or by phosphorylating a variety of signaling molecules containing a specific SH2 domain.
The signal pathway is a signal transduction pathway stimulated by cytokines and is involved in many important biological processes such as proliferation, differentiation, apoptosis and immunoregulation of cells.
Relevant researches show that JAK1, JAK2 and TYK2 are widely present in various tissues and cells, JAK1 is closely related to the activation of inflammatory factors such as IL-6 and IFN, and JAK2 can independently mediate cytokines such as EPO; JAK3 is present only in the bone marrow and lymphatic systems and mediates signaling of IL-2, IL-4, IL-7, IL-9, IL-15, and IL-21.
Relevant research shows that the STAT family has 7 members, 6 regions are totally arranged from the N end to the C end, and the N-terminal region of the STAT can be combined with other transcription factors to form a dimer; the DNA binding region can be combined with the DNA of the target gene regulatory region; the SH2 region can recognize a specific receptor tyrosine kinase region and promote the formation of STAT dimer together with active JAK; the C end is a transcription active region, and phosphoserine in the C end determines nuclear translocation of STAT and regulates and controls transcription reaction.
The dosage is as follows: twice a day, 5mg each time.
On 23/02/23 years, the united states Food and Drug Administration (FDA) approved Xeljanz XR (sustained release formulation) for marketing with an approved specification of 11mg in the form of a tablet, which is the first once-a-day approved oral therapeutic RA drug to be marketed; the indications are Xeljanz and are used for treating adult patients with moderate to severe active rheumatoid arthritis which do not respond or tolerate the treatment of methotrexate.
Disclosure of Invention
The tofacitinib citrate osmotic pump preparation prepared by the method has the zero-order release kinetics characteristic, can release the drug at a constant speed within 12 hours, is beneficial to maintaining long-term and efficient blood concentration in vivo and improving the treatment effect of the drug. The invention provides an osmotic pump controlled release preparation of tofacitinib citrate and pharmaceutically acceptable salts thereof, which comprises a single-layer tablet core and a controlled release film coating. After the osmotic pump tablet is orally taken, pore-forming agent is dissolved by water in gastrointestinal tract and is formed in situ, water enters the tablet core through the coating film and the film, the medicine is dissolved into saturated solution, the solution in the tablet core becomes high osmotic pressure solution by the osmotic active substance, the water continues to enter the tablet core by the osmotic pressure existing inside and outside the coating film, static pressure is formed in the tablet core, and the medicine is driven to release from the film at a constant speed by the static pressure.
The tofacitinib citrate osmotic pump tablet comprises a drug-containing tablet core and a controlled-release film coating, wherein the controlled-release film coating contains a pore-forming agent capable of forming a drug release, the tablet core contains 5-60 wt% of tofacitinib citrate or pharmaceutically acceptable salt thereof, 10-50 wt% of a filling agent, 0-10 wt% of an osmotic pressure promoter, 5-40 wt% of a pH regulator and 2-10 wt% of an adhesive, the controlled-release film coating material contains 2-10 wt% of the drug-containing tablet core, and the controlled-release film coating material contains 10-90 wt% of the pore-forming agent and 0-10 wt% of a plasticizer.
The tofacitinib citrate osmotic pump tablet is characterized in that the filler is one or a mixture of more than two of starch, lactose, microcrystalline cellulose, pregelatinized starch, dextrin, sucrose and mannitol.
The osmotic pressure promoter of the tofacitinib citrate osmotic pump tablet is one or a mixture of more than two of mannitol, sodium chloride, potassium chloride, calcium chloride, sulfate and phosphate.
The tofacitinib citrate osmotic pump tablet provided by the invention has the advantages that the pH regulator is one or a mixture of more than two of tartaric acid, succinic acid, maleic acid, lactic acid, citric acid and sodium citrate.
The tofacitinib citrate osmotic pump tablet is characterized in that the adhesive is one or a mixture of more than two of polyvinylpyrrolidone, hydroxypropyl methylcellulose, hydroxypropyl cellulose, methylcellulose and ethanol.
The tofacitinib citrate osmotic pump tablet is characterized in that the pore-forming agent is one or a mixture of more than two of hydroxypropyl methylcellulose, polyethylene glycol, glycerol, propylene glycol, water-soluble inorganic salt, saccharides and polyvinylpyrrolidone.
The tofacitinib citrate osmotic pump tablet is characterized in that the controlled-release film coating material is one or a mixture of more than two of cellulose acetate, ethyl cellulose and hydroxypropyl methylcellulose.
The tofacitinib citrate osmotic pump tablet provided by the invention is characterized in that the plasticizer is one or a mixture of more than two of phthalate, polyethylene glycol, triacetin, triethyl citrate and dibutyl sebacate.
The tofacitinib citrate osmotic pump tablet is characterized by comprising the following preparation processes:
(1) mixing tofacitinib citrate with a filling agent, an osmotic pressure promoter and a pH regulator, adding an adhesive to prepare a soft material, sieving with a 20-mesh sieve for granulation, drying in an oven at 40-60 ℃ for 5-60 min, sieving with a 18-mesh sieve for granulation, adding a lubricant, uniformly mixing, and tabletting;
(2) dissolving the semipermeable film coating material, the pore-forming agent and the plasticizer by using acetone to prepare semipermeable film coating liquid;
(3) coating the tablet cores and volatilizing the coating solvent.
The tofacitinib citrate osmotic pump tablet disclosed by the invention is proved to have a reduced Cmax and a prolonged Tmax in a Beagle canine satiety test, and has an obvious sustained-release effect, wherein the relative bioavailability is 98.37% compared with a lericarb capsule.
It is an object of the present invention to provide a method for substantially improving rheumatoid arthritis.
Another object of the present invention is to provide an osmotic pump formulation, wherein the pore-forming agent is dissolved by the water in the gastrointestinal tract after administration, and formed in situ, the water continues to enter the core by the osmotic pressure existing inside and outside the coating film, and a static pressure is formed in the core, which drives the drug to release from the film at a constant rate, and exhibits a significant zero-order release profile within 12 hours. The invention also aims to reduce the daily medicine taking times of a patient, improve the treatment compliance of the patient, avoid or reduce the large fluctuation of the blood concentration and reduce the toxic and side effect.
The above and other objects are achieved by the present invention which relates to a solid controlled release oral dosage form comprising 5-60 wt% tofacitinib citrate, wherein the in vitro release rate of the dosage form (measured at 37 ℃ in 900mL water medium at 50rpm using the second release apparatus of 0931 dissolution and release rate test of the four general rules of pharmacopoeia 2015 edition of china).
Detailed Description
Example 1
Tablet core prescription:
tofacitinib citrate 68 g
Lactose 500g
Mannitol 300g
Sorbitol 200g
PVPK30 10g
Magnesium stearate 5g
The prescription of the coating liquid is as follows:
HPMC 200g
2000ml of ethanol
Acetone 1000ml
2000ml of water
The preparation process comprises the following steps: mixing tofacitinib citrate with filler, osmotic pressure promoter, and pH regulator, mixing in fluidized bed, granulating, drying, adding magnesium stearate, mixing, and tabletting. Dissolving the coating material and other auxiliary materials in the coating layer by using acetone, coating by using a coating pot, and curing for 12 hours at 40 ℃ after coating.
Example 2
Tablet core prescription:
tofacitinib citrate 68 g
Lactose 500g
Mannitol 300g
Sorbitol 200g
PVPK30 10g
Magnesium stearate 5g
The prescription of the coating liquid is as follows:
ethyl cellulose 200g
2000ml of ethanol
Acetone 1000ml
2000ml of water
The preparation process comprises the following steps: mixing tofacitinib citrate with filler, osmotic pressure promoter, and pH regulator, mixing in fluidized bed, granulating, drying, adding magnesium stearate, mixing, and tabletting. Dissolving the coating material and other auxiliary materials in the coating layer by using acetone, coating by using a coating pot, and curing for 12 hours at 40 ℃ after coating.
Example 3
Tablet core prescription:
tofacitinib citrate 68 g
Lactose 500g
Mannitol 300g
Sorbitol 200g
HPMC 10g
Magnesium stearate 5g
The prescription of the coating liquid is as follows:
HPMC 200g
acetone 1000ml
2000ml of water
The preparation process comprises the following steps: mixing tofacitinib citrate with filler, osmotic pressure promoter, and pH regulator, adding appropriate amount of 5% hydroxypropyl methylcellulose E5 water solution to prepare soft material, sieving with 20 mesh sieve, granulating, oven drying at 40 deg.C for 15min, sieving with 18 mesh sieve, grading, adding magnesium stearate, mixing, and tabletting. Dissolving the coating material and other auxiliary materials in the coating layer by using acetone, coating by using a coating pot, and curing for 12 hours at 40 ℃ after coating.
Example 4
Tablet core prescription:
tofacitinib citrate 68 g
Lactose 500g
Mannitol 300g
Sorbitol 200g
CMC-NA 10g
Magnesium stearate 5g
The prescription of the coating liquid is as follows:
HPMC 200g
acetone 1000ml
2000ml of water
The preparation process comprises the following steps: mixing tofacitinib citrate with filler, osmotic pressure promoter, and pH regulator, mixing in fluidized bed, granulating, drying, adding magnesium stearate, mixing, and tabletting. Dissolving the coating material and other auxiliary materials in the coating layer by using acetone, coating by using a coating pot, and curing for 12 hours at 40 ℃ after coating.
Evaluation of pharmacokinetic parameters in tofacitinib citrate osmotic pump tablets by Beagle dogs: a double-cycle double-cross administration scheme is adopted, the original preparation is taken as a reference preparation, the tofacitinib citrate osmotic pump tablet in example 3 is taken as a tested preparation, and pharmacokinetic parameters and relative bioavailability are examined. Compared with the original preparation, the citric acid tofacitinib osmotic pump tablet has the advantages of reduced Cmax, prolonged Tmax and relative bioavailability of 99.28%.
Claims (10)
1. The tofacitinib citrate osmotic pump tablet comprises a drug-containing tablet core and a controlled-release film coating, wherein the tablet core contains 5-60 wt% of tofacitinib citrate or other pharmaceutically acceptable salts thereof, 10-50 wt% of a filling agent, 0-10 wt% of an osmotic pressure promoter, 5-40 wt% of a pH regulator and 2-10 wt% of an adhesive, the controlled-release film coating comprises 2-10 wt% of a controlled-release film coating material based on the weight of the drug-containing tablet core, and the controlled-release film coating comprises 10-90 wt% of a pore-forming agent and 0-10 wt% of a plasticizer based on the weight of the controlled-release film coating material.
2. The tofacitinib citrate osmotic pump tablet according to claim 1, wherein the filler is selected from one or a mixture of more than two of starch, lactose, microcrystalline cellulose, pregelatinized starch, dextrin, sucrose and mannitol.
3. The tofacitinib citrate osmotic pump tablet according to claim 1, wherein the osmotic pressure promoter is one or a mixture of more than two of mannitol, sodium chloride, potassium chloride, calcium chloride, sulfate and phosphate.
4. The tofacitinib citrate osmotic pump tablet according to claim 1, wherein the pH regulator is one or a mixture of more than two of tartaric acid, succinic acid, maleic acid, lactic acid, citric acid and sodium citrate.
5. The tofacitinib citrate osmotic pump tablet according to claim 1, wherein the binder is one or a mixture of more than two of polyvinylpyrrolidone, hydroxypropyl methylcellulose, hydroxypropyl cellulose, methylcellulose and ethanol.
6. The tofacitinib citrate osmotic pump tablet as claimed in claim 1, wherein the pore-forming agent is selected from hydroxypropyl methylcellulose, polyethylene glycol, glycerol, propylene glycol, water-soluble inorganic salt, saccharide, and polyvinylpyrrolidone.
7. The tofacitinib citrate osmotic pump tablet according to claim 1, wherein the controlled release film coating material is one or a mixture of more than two of cellulose acetate, ethyl cellulose and hypromellose.
8. The tofacitinib citrate osmotic pump tablet according to claim 1, wherein the plasticizer is one or a mixture of two or more selected from phthalate, polyethylene glycol, triacetin, triethyl citrate and dibutyl sebacate.
9. The tofacitinib citrate osmotic pump tablet according to any one of claims 1 to 8, which is prepared by the following steps:
(1) mixing tofacitinib citrate or its pharmaceutically acceptable salt with filler, osmotic pressure promoter, and pH regulator, mixing in fluidized bed, granulating, drying, mixing, and tabletting;
(2) dissolving the semipermeable film coating material, the pore-forming agent and the plasticizer by using acetone to prepare semipermeable film coating liquid;
(3) coating the tablet cores and volatilizing the coating solvent.
10. The tofacitinib citrate osmotic pump tablet according to claim 1, which provides an effective treatment mode with stable blood concentration once a day for patients in the treatment of rheumatoid arthritis, psoriatic arthritis and the like.
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| CN202010448495.XA CN113712932A (en) | 2020-05-25 | 2020-05-25 | Tofacitinib citrate osmotic pump tablet and preparation method thereof |
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| CN202010448495.XA CN113712932A (en) | 2020-05-25 | 2020-05-25 | Tofacitinib citrate osmotic pump tablet and preparation method thereof |
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Cited By (4)
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| CN115006361A (en) * | 2022-06-10 | 2022-09-06 | 北京诺康达医药科技股份有限公司 | Tofacitinib slow-release core-spun tablet and preparation method thereof |
| CN115068432A (en) * | 2022-08-02 | 2022-09-20 | 沈阳信康药物研究有限公司 | Tofacitinib citrate pressed coating sustained release tablet and preparation method thereof |
| CN115381788A (en) * | 2022-09-19 | 2022-11-25 | 苏州弘森药业股份有限公司 | Tofacitinib citrate preparation and preparation method thereof |
| CN115671070A (en) * | 2022-09-13 | 2023-02-03 | 广西纯正堂制药有限公司 | Desloratadine citrate osmotic pump controlled release tablet and preparation method thereof |
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| CN111150711A (en) * | 2018-11-07 | 2020-05-15 | 上海博志研新药物技术有限公司 | Tofacitinib controlled-release tablet, preparation method and application thereof |
| CN111184696A (en) * | 2020-02-26 | 2020-05-22 | 江苏艾立康药业股份有限公司 | Tofacitinib citrate sustained-release tablet and preparation method thereof |
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Cited By (5)
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|---|---|---|---|---|
| CN115006361A (en) * | 2022-06-10 | 2022-09-06 | 北京诺康达医药科技股份有限公司 | Tofacitinib slow-release core-spun tablet and preparation method thereof |
| CN115068432A (en) * | 2022-08-02 | 2022-09-20 | 沈阳信康药物研究有限公司 | Tofacitinib citrate pressed coating sustained release tablet and preparation method thereof |
| CN115068432B (en) * | 2022-08-02 | 2024-08-16 | 沈阳信康药物研究有限公司 | Tofacitinib citrate compression-coated sustained-release tablet and preparation method thereof |
| CN115671070A (en) * | 2022-09-13 | 2023-02-03 | 广西纯正堂制药有限公司 | Desloratadine citrate osmotic pump controlled release tablet and preparation method thereof |
| CN115381788A (en) * | 2022-09-19 | 2022-11-25 | 苏州弘森药业股份有限公司 | Tofacitinib citrate preparation and preparation method thereof |
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