CN110787145A - Tofacitinib citrate sustained-release tablet and preparation method thereof - Google Patents
Tofacitinib citrate sustained-release tablet and preparation method thereof Download PDFInfo
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- CN110787145A CN110787145A CN201911300186.1A CN201911300186A CN110787145A CN 110787145 A CN110787145 A CN 110787145A CN 201911300186 A CN201911300186 A CN 201911300186A CN 110787145 A CN110787145 A CN 110787145A
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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
- A61K9/20—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]
Abstract
The invention aims to provide a tofacitinib citrate sustained-release tablet taken once a day and a preparation method thereof, and is characterized in that a drug-containing tablet core is coated with a layer of sustained-release coating. Wherein the drug-containing core comprises: tofacitinib citrate accounting for 2-20% of the weight of the tablet, framework material accounting for 20-50%, diluent accounting for 40-80% of the weight of the tablet and lubricant accounting for 0.1-3% of the weight of the tablet; the slow release coating film comprises: retarder accounting for 1-5% of the weight of the tablet, and pore-forming agent accounting for 3-15%; the weight gain of the coating accounts for 1 to 15 percent of the weight of the tablet core. The sustained-release tablet has the advantages that the sustained-release matrix tablet core and the sustained-release coating film are added, so that the drug is slowly released within a period of time, the defect of large fluctuation of blood concentration of the common tablet is avoided, the drug taking frequency is reduced, and the compliance of a patient is improved. In addition, the preparation has simple prescription and preparation process and is easy for industrial production.
Description
Technical Field
The invention relates to a pharmaceutical dosage form of tofacitinib citrate and a preparation method thereof, belonging to the field of chemical pharmaceutical preparations.
Background
Rheumatoid Arthritis (RA) is a chronic autoimmune disease with high clinical incidence and disability rate, and its main pathological feature is chronic progressive synovitis, which can occur at any age. RA clinically causes various symptoms, which are mainly manifested by polyarticular, symmetrical and invasive arthritis of hand and foot small joints, and is often accompanied by positive serum rheumatoid factor of extraarticular organs, thereby causing joint deformity and function loss.
The medicines for treating RA on the market at present mainly comprise the following medicines: nonsteroidal anti-inflammatory drugs (NSAIDs), steroid hormones, antirheumatic drugs (DMARDs), and biological agents. However, most of them only have the effects of relieving pain and inflammation, and do not fundamentally solve the progress of RA. And some biologics such as: adalimumab, infliximab, rituximab and the like are protein medicines, and are expensive, and need intravenous injection for taking medicine, so that the medicine is inconvenient to take and poor in patient compliance.
The JAK kinase family is a class of non-receptor tyrosine protein kinases with a total of four members, JAK1, JAK2, JAK3 and tyrosine kinase 2(tyrosine kinase 2, TYK 2). Among them, JAK1 and JAK3 are closely related to immune regulation, and JAK3 function loss may cause severe immunodeficiency. Tofacitinib is a selective JAK1, JAK3 inhibitor that acts by regulating JAK signaling pathways in cell membranes, preventing signal transduction and phosphorylation and activation of activator of transcription (STAT).
Tofacitinib is a novel JAK inhibitor developed by the company Perey, and two formulations of Tofacitinib citrate tablet (5 mg/tablet) and Tofacitinib citrate controlled release tablet (11 mg/tablet) are on the market at present, and the active ingredients of Tofacitinib citrate are Tofacitinib citrate. Wherein tofacitinib citrate tablet (trade name: XELJANZ) is approved by FDA in US for treating moderate-to-severe adult RA patients who are not responding or tolerant to methotrexate in 11 months of 2012 and 2016 and a tofacitinib citrate controlled release tablet (XELJANZ XR) and 2016 are approved by FDA in US for 2 months. The imported preparations on the market at present only comprise tofacitinib citrate tablets of the company Hurrill, and the domestic corporations holding the batch texts also only comprise two enterprises of the sunny pharmaceutical industry and the Qilu pharmaceutical industry. And the domestic preparations on the market are common tablets with the specification of 5mg, and patients need to take the tablets twice a day, so that the blood concentration fluctuation is large and the compliance of the patients is poor.
In order to overcome the defects of the common tablet and deeply research on the sustained and controlled release preparation, the related literature of the tofacitinib sustained release preparation is published in China at present. The Chinese patent application No. CN 108066319A has the invention name: the invention provides a tofacitinib citrate enteric-coated sustained-release pellet capsule and a preparation method thereof, and is characterized in that a drug-containing pellet core taking a compound skeleton type sustained-release material as a skeleton and a tofacitinib citrate enteric-coated sustained-release pellet with enteric coating coated outside the pellet core are adopted. Although the patent achieves the stable release of the medicine within 24h by compounding the skeleton material, the patent does not provide in-vivo pharmacokinetic data and cannot clearly show how the bioavailability of the medicine in vivo is. And the enteric-coated pellet capsule has complex prescription, complex preparation process, great difficulty in industrial production and high cost.
Disclosure of Invention
The invention aims to provide a preparation method of tofacitinib citrate sustained-release tablets, which has simple components and preparation process, can slowly release medicaments within 12 hours, can maintain stable and effective blood concentration in vivo for a long time, reduces administration times and improves the compliance of patients.
The invention aims to provide a tofacitinib citrate sustained-release tablet taken once a day, which is characterized in that a drug-containing tablet core is coated with a layer of sustained-release coating film. Wherein the drug-containing core comprises: tofacitinib citrate accounting for 2-20% of the weight of the tablet, framework material accounting for 20-50%, diluent accounting for 40-80% of the weight of the tablet and lubricant accounting for 0.1-3% of the weight of the tablet; the slow release coating film comprises: retarder accounting for 1-5% of the weight of the tablet, and pore-forming agent accounting for 3-15%; the weight gain of the coating accounts for 1 to 15 percent of the weight of the tablet core.
The preparation method of the tofacitinib citrate sustained-release tablet mainly comprises the following steps:
(1) firstly, sieving the raw and auxiliary materials by a 30-mesh sieve, respectively weighing tofacitinib citrate, a framework material and a diluent according to the prescription amount, and then mixing according to the principle of adding the same amount one by one;
(2) adding a certain amount of wetting agent into the uniformly mixed powder to prepare a soft material, sieving the soft material by a 20-mesh sieve, and granulating;
(3) after drying, sieving with a 20-mesh sieve for finishing, then adding a lubricant according to the prescription amount, and mixing;
(4) adjusting to proper hardness and weight, and tabletting;
(5) preparing the slow release coating agent with the prescription dose into coating liquid by using corresponding solvents, and placing the tablet cores into a coating pan for coating.
The tofacitinib citrate sustained-release tablet has a tablet core framework material selected from one or more of hydroxyethyl cellulose, hydroxypropyl methylcellulose, polyvinylpyrrolidone and hydroxypropyl cellulose.
The tablet core diluent of the tofacitinib citrate sustained-release tablet is selected from one or more of microcrystalline cellulose, starch, lactose and mannitol.
The tablet core lubricant of the tofacitinib citrate sustained-release tablet is selected from one or more of talcum powder, magnesium stearate and superfine silica gel powder.
The tofacitinib citrate sustained-release tablet has a sustained-release coating retarder selected from one or more of ethyl cellulose and polymethacrylate.
The citric acid tofacitinib sustained-release tablet has a sustained-release coating pore-forming agent selected from one or more of polyethylene glycol, hydroxypropyl cellulose and hydroxypropyl methylcellulose.
The tofacitinib citrate sustained-release tablet is characterized in that after a medium enters a core through a semipermeable membrane, a tablet core absorbs water to expand to break the semipermeable membrane, so that a certain release time lag is achieved.
The tofacitinib citrate sustained-release tablet is characterized in that the contact time lag between the tablet core and a medium is controlled by controlling the shape and size of the tablet core, the characteristic dosage of a sustained-release material and the thickness of a coating film.
Compared with the prior art, the preparation has the main advantages that the medicine is slowly released in a period of time by a method of adding a sustained-release coating film outside a sustained-release skeleton tablet core, the defect of large fluctuation of blood concentration of a common tablet is avoided, the medicine taking frequency is reduced, and the compliance of a patient is improved. In addition, the preparation has simple prescription and preparation process and is easy for industrial production.
Drawings
FIG. 1 is a graph of the in vitro cumulative release percentage versus time for the tofacitinib citrate sustained release tablets of example 1;
FIG. 2 is a graph of the in vitro cumulative release percentage versus time for the tofacitinib citrate sustained release tablets of example 2;
FIG. 3 is a graph of the in vitro cumulative release percentage versus time for the tofacitinib citrate sustained release tablets of example 3;
FIG. 4 is a graph of the in vitro cumulative release percentage versus time for the tofacitinib citrate sustained release tablets of example 4;
FIG. 5 is a graph of the in vitro cumulative release percentage versus time for the tofacitinib citrate sustained release tablets of example 5;
FIG. 6 is a graph of the in vitro cumulative release percentage versus time for the tofacitinib citrate sustained release tablets of example 6;
FIG. 7 is a graph of the in vitro cumulative release percentage versus time for the tofacitinib citrate sustained release tablets of example 7;
FIG. 8 is a graph of the in vitro cumulative release percentage versus time for the tofacitinib citrate sustained release tablets of example 8;
Detailed Description
Example 1
(1) Tablet core (per tablet):
preparation process (example 1):
(1) firstly, sieving raw and auxiliary materials by a 30-mesh sieve, weighing tofacitinib citrate, a framework material and a diluent according to the prescription amount, and mixing; adding a proper amount of wetting agent into the uniformly mixed powder to prepare a soft material, sieving the soft material by a 20-mesh sieve, and granulating; then drying the prepared particles for 2h at 40 ℃, and then sieving with a 20-mesh sieve for finishing; then adding the lubricant according to the prescription amount, uniformly mixing, and pressing into a tablet core of 8 mm.
Example 1-example 8. method for determining release rate of tofacitinib citrate sustained release tablet:
according to a second method of a method for measuring the dissolution rate and the release degree of 0931 according to the general rules of the four parts of the Chinese pharmacopoeia 2015 edition, a sedimentation basket device is added, a tofacitinib citrate sustained-release tablet is placed in a dissolution cup, 900mL of degassed phosphate buffer solution with pH6.8 is used as a release medium, the rotating speed is 50rpm, the temperature is (37 +/-0.5) DEG C, 10mL of fresh medium with the same amount and the same temperature is sampled at 1h, 1.5h, 2h, 2.5h, 3h, 4h, 6h, 8h and 12h respectively, a sample is filtered by a 0.45 mu m microporous filter membrane, the subsequent filtrate is measured by a high performance liquid chromatograph, and the detection wavelength is 287 nm; in addition, a proper amount of reference substance is precisely weighed, the cumulative release percentage is calculated by the same method, and the requirement is met.
Example 2
(1) Tablet core (per tablet):
(2) sustained release film coating solution (each tablet):
aqueous ethylcellulose dispersion 249mg
166mg of water
Preparation process (example 2-example 5):
(2) firstly, sieving raw and auxiliary materials by a 30-mesh sieve, weighing tofacitinib citrate, a framework material and a diluent according to the prescription amount, and mixing; adding a proper amount of wetting agent into the uniformly mixed powder to prepare a soft material, sieving the soft material by a 20-mesh sieve, and granulating; then drying the prepared particles for 2h at 40 ℃, and then sieving with a 20-mesh sieve for finishing; adding a lubricant with the prescription amount, uniformly mixing, and pressing into a tablet core with the thickness of 8 mm; then dissolving the slow release coating agent in a corresponding solvent to prepare a slow release coating agent coating solution for coating.
Example 3
(1) Tablet core (per tablet):
(2) sustained release film coating solution (each tablet):
opadry 21K68953-CN 15mg
Ethanol 155.25mg
17.25mg of water
The release rate of the tofacitinib citrate sustained-release tablet in example 1 is shown in figure 1. The release rate of the tofacitinib citrate sustained-release tablet of the example 2 is shown in a figure 2. The release rate of the tofacitinib citrate sustained-release tablet prepared in example 3 is shown in figure 3. Therefore, the problem of over-fast release of the plain tablets at the early stage can be obviously improved by coating the tablet cores with the slow release coatings, and the Opadry coating has better effect than the coating of the ethyl cellulose aqueous dispersion, so that short time lag at the early stage can be achieved, and the fast release speed at the later stage can be ensured.
Example 4
(1) Tablet core (per tablet):
(2) sustained release film coating solution (each tablet):
opadry 21K68953-CN 15mg
Ethanol 155.25mg
17.25mg of water
The release rate of the tofacitinib citrate sustained-release tablet of example 4 is shown in figure 4. In combination with example 3, it can be seen that increasing the amount of sustained release material in the formulation reduces the release rate of the tablet.
Example 5
(1) Tablet core (per tablet):
(3) sustained release film coating solution (each tablet):
opadry 21K68953-CN 15mg
Ethanol 155.25mg
17.25mg of water
The release rate of the tofacitinib citrate sustained-release tablet prepared in example 5 is shown in figure 5. In combination with example 3, it can be seen that the use of lactose and microcrystalline cellulose as diluents significantly reduces the rate of late release and improves tablet compressibility.
Example 6
(1) Tablet core (per tablet):
(2) sustained release film coating solution (each tablet):
opadry 21K68953-CN 15mg
Ethanol 155.25mg
17.25mg of water
Preparation Process (examples 6 to 8):
(1) firstly, sieving raw and auxiliary materials by a 30-mesh sieve, weighing tofacitinib citrate, a framework material and a diluent according to the prescription amount, and mixing; adding a proper amount of wetting agent into the mixed powder to prepare a soft material, sieving the soft material by a 20-mesh sieve, and granulating; then drying the prepared particles for 2h at 40 ℃, and then sieving with a 20-mesh sieve for finishing; adding a lubricant with the prescription amount, uniformly mixing, and pressing into a 7mm tablet core; then dissolving the slow release coating agent in a corresponding solvent to prepare a slow release coating agent coating solution for coating.
The release rate of the tofacitinib citrate sustained-release tablet prepared in example 6 is shown in figure 6. Combining with example 3, it can be seen that the release rate of the tablet can be obviously changed by changing the size of the tablet core, and the release rate of the 7mm tablet core is integrally slower than that of the 8mm tablet core.
Example 7
(1) Tablet core (per tablet):
(2) sustained release film coating solution (each tablet):
opadry 21K68953-CN 6mg
Ethanol 62.1mg
6.9mg of water
Example 8
(1) Tablet core (per tablet):
(2) sustained release film coating solution (each tablet):
opadry 21K68953-CN 21mg
Ethanol 217.35mg
24.15mg of water
The release rate of the tofacitinib citrate sustained-release tablet prepared in example 7 is shown in figure 7. The release rate of the tofacitinib citrate sustained-release tablet prepared in example 8 is shown in figure 8. In combination with example 3, it can be seen that the more the weight of the coating of the sustained release coating is increased, the slower the tablet is released, and the earlier release lag time can be controlled by reasonably controlling the weight increase of the coating.
Claims (7)
1. A tofacitinib citrate sustained release tablet taken once a day is characterized in that a drug-containing tablet core is coated with a layer of sustained release coating; wherein the drug-containing core comprises: tofacitinib citrate accounting for 2-20% of the weight of the tablet, framework material accounting for 20-50%, diluent accounting for 40-80% of the weight of the tablet and lubricant accounting for 0.1-3% of the weight of the tablet; the slow release coating film comprises: retarder accounting for 1-5% of the weight of the tablet, and pore-forming agent accounting for 3-15%; the weight gain of the coating accounts for 1 to 15 percent of the weight of the tablet core.
2. The tofacitinib citrate sustained-release tablet according to claim 1, wherein the core skeleton material is selected from one or more of hydroxyethyl cellulose, hydroxypropyl methylcellulose, polyvinylpyrrolidone and hydroxypropyl cellulose.
3. The tofacitinib citrate sustained-release tablet according to claim 1, wherein the tablet core diluent is selected from one or more of microcrystalline cellulose, starch, lactose and mannitol.
4. The tofacitinib citrate sustained-release tablet according to claim 1, wherein the core lubricant is one or more selected from talcum powder, magnesium stearate and aerosil.
5. The tofacitinib citrate sustained-release tablet according to claim 1, wherein the sustained-release coating retarder is one or more selected from ethyl cellulose and polymethacrylate.
6. The tofacitinib citrate sustained-release tablet of claim 1, wherein the sustained-release coating pore-forming agent is selected from one or more of polyethylene glycol, hydroxypropyl cellulose and hypromellose.
7. The preparation process of tofacitinib citrate sustained-release tablet as claimed in claim 1, characterized by comprising the following steps:
(1) firstly, sieving raw and auxiliary materials, respectively weighing tofacitinib citrate, a framework material and a diluent according to the prescription amount, and then mixing;
(2) adding a certain amount of wetting agent into the uniformly mixed powder to prepare a soft material, sieving with a 20-mesh sieve, and granulating.
(3) After drying, sieving with a 20-mesh sieve for finishing, then adding a lubricant according to the prescription amount, and mixing;
(4) adjusting to proper hardness and weight, and tabletting;
(5) preparing the slow release coating agent with the prescription dose into coating liquid by using corresponding solvents, and placing the tablet cores into a coating pan for coating.
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Cited By (11)
| Publication number | Priority date | Publication date | Assignee | Title |
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| 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 |
| CN112587492A (en) * | 2020-12-20 | 2021-04-02 | 武汉中点医药科技有限公司 | Tofacitinib citrate sustained-release tablet with membrane control and framework dual sustained release |
| WO2021169724A1 (en) * | 2020-02-26 | 2021-09-02 | 上海博志研新药物技术有限公司 | Sustained-release dosage form of tofacitinib, preparation method therefor and application thereof |
| CN113712932A (en) * | 2020-05-25 | 2021-11-30 | 南京帝昌医药科技有限公司 | Tofacitinib citrate osmotic pump tablet and preparation method thereof |
| WO2022121927A1 (en) * | 2020-12-08 | 2022-06-16 | Triastek, Inc. | Delayed sustained-release oral drug dosage forms of a janus kinase (jak) inhibitor and methods of use thereof |
| CN114652695A (en) * | 2020-12-23 | 2022-06-24 | 深圳翰宇药业股份有限公司 | Tofacitinib gastric retention floating sustained-release tablet and preparation method thereof |
| 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 |
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| US11571391B2 (en) | 2018-01-09 | 2023-02-07 | Triastek, Inc. | Oral drug dosage forms compromising a fixed-dose of an ADHD non-stimulant and an ADHD stimulant |
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| CN113712932A (en) * | 2020-05-25 | 2021-11-30 | 南京帝昌医药科技有限公司 | Tofacitinib citrate osmotic pump tablet and preparation method thereof |
| WO2022121927A1 (en) * | 2020-12-08 | 2022-06-16 | Triastek, Inc. | Delayed sustained-release oral drug dosage forms of a janus kinase (jak) inhibitor and methods of use thereof |
| CN112587492A (en) * | 2020-12-20 | 2021-04-02 | 武汉中点医药科技有限公司 | Tofacitinib citrate sustained-release tablet with membrane control and framework dual sustained release |
| CN114652695A (en) * | 2020-12-23 | 2022-06-24 | 深圳翰宇药业股份有限公司 | Tofacitinib gastric retention floating sustained-release tablet and preparation method thereof |
| CN114652695B (en) * | 2020-12-23 | 2023-12-26 | 深圳翰宇药业股份有限公司 | Tofacitinib gastric retention floating type sustained release tablet and preparation method thereof |
| WO2022262802A1 (en) * | 2021-06-18 | 2022-12-22 | 无锡叶石医药有限公司 | Sustained-release preparation of tofacitinib and preparation method therefor |
| 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 |
| CN115322051A (en) * | 2022-07-14 | 2022-11-11 | 青岛大学 | Composting method for resource utilization of waste straws |
| 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 |
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