CN110946834B - Tofacitinib citrate tablet and preparation process thereof - Google Patents
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Abstract
The invention belongs to the field of pharmaceutical preparations, and provides tofacitinib citrate tablet which is prepared from a filling agent, a disintegrating agent, a lubricating agent, a coating material and other pharmaceutically acceptable auxiliary materials. The tablet has low impurity content, good stability after long-term storage, simple process operation, high production efficiency and good reproducibility, and is beneficial to industrial mass production.
Description
Technical Field
The invention belongs to the technical field of pharmaceutical preparations, and particularly relates to a solid oral preparation, in particular to a tofacitinib citrate-containing tablet and a preparation process thereof.
Background
Tofacitinib, chemical name: 3- [ (3R, 4R) -4-methyl-3- [ methyl- (7H-pyrrolo [2,3-d ] pyrimidin-4-yl) amino ] piperidin-1-yl ] -3-oxopropanenitrile citrate. The structural formula is as follows:
tofacitinib is a JAK kinase inhibitor. It is used for adult patients with moderate to severe rheumatoid arthritis with unsatisfactory methotrexate therapeutic effect or allergy to methotrexate.
As is well known, the gastrointestinal tract is the most ideal administration way for the medicine to enter the body to play a therapeutic role, and the administration way is the safest, the most convenient and the most effective on the whole, so the gastrointestinal tract is always the most widely used administration way in clinical application. The tablet has the characteristics of safety, effectiveness, convenient taking, accurate dosage, simple process, good stability and the like, and is always the most popular and advocated dosage form in clinic, so that the focus of medicine manufacturing industry is on how to design and produce the tablet with the optimal curative effect.
The most applied current tablet manufacturing technology is a wet granulation process, which is relatively complex in manufacturing process and mainly shows more process steps. The wet granulation, drying, granule finishing, tabletting and coating are carried out, so that the hidden danger of stability exists for the moisture and heat sensitive medicines.
The process of directly tabletting powder directly without granulating (wet granulation or dry granulation) is a process of directly tabletting. The method has the advantages of good product stability, high production efficiency, good reproducibility, energy and time conservation and cost conservation, the biggest obstacle restricting the industrial mass production of the direct powder tabletting process is the technology, the method mainly comprises the powder control (such as compressibility, fluidity, dilution potential, content uniformity, lubrication sensitivity and the like) of raw and auxiliary materials, and the existing process for producing the tofacitinib citrate tablets mainly adopts the steps of crushing the raw material medicines to control the particle size and/or sieving the filling agent before use. The step of crushing the raw material medicines is added in the production process program, so that the waste of the raw material medicines is caused, and the production process program is added; the filler is sieved before use, the production process procedure and the cost are increased, the inventor finds that the citric acid tofacitinib tablet with high purity, good stability and quick dissolution can be produced by selecting proper filler components and the mass ratio of the filler through simple process steps without additional process steps such as particle size control of raw material medicines and/or sieving of the filler before use through a large amount of experimental screening, and the preparation process has the advantages of simple operation, high production efficiency and good reproducibility, and is favorable for industrial mass production.
Disclosure of Invention
The invention aims to provide tofacitinib citrate tablets.
The tofacitinib citrate tablet provided by the invention consists of tofacitinib citrate, a filler, a disintegrant, a lubricant, a coating material and other pharmaceutically acceptable auxiliary materials, wherein the filler consists of spray-dried lactose and microcrystalline cellulose, and the mass ratio of the filler to the microcrystalline cellulose is 3;
the filling agent of the tofacitinib citrate tablet provided by the invention is preferably the mass ratio of spray-dried lactose to microcrystalline cellulose of (2-1).
The tofacitinib citrate tablet provided by the invention is characterized in that spray-dried lactose is selected from one or more of lactose F100, lactose F80 and lactose F60, preferably lactose F100; and/or the microcrystalline cellulose is selected from one or more of microcrystalline cellulose PH101, PH102, PH103, PH105, PH301 and PH302, and is preferably microcrystalline cellulose PH102.
The tofacitinib citrate tablet provided by the invention comprises a filler consisting of lactose F100 and microcrystalline cellulose PH102, wherein the mass ratio of the lactose F100 to the microcrystalline cellulose PH102 is (2-1).
The citric acid tofacitinib tablet provided by the invention has the advantages that the disintegrant is selected from one or two of croscarmellose sodium and crospovidone.
The lubricant of the tofacitinib citrate tablet provided by the invention is selected from one or more of magnesium stearate, stearic acid, talcum powder, sodium stearyl fumarate and glyceryl behenate, and is preferably magnesium stearate.
The coating material is made of Opadry coating powder, preferably one or more of Opadry 03F180012, opadry 03K18416 and Opadry 03G58632 without talcum powder, and more preferably Opadry 03G58632.
The tofacitinib citrate tablet provided by the invention comprises the following components in parts by weight: 9-10 parts of tofacitinib citrate: 170-190 parts of a filler: 5-12 parts of disintegrating agent: 0.5-2 parts of a lubricant: 5-9 parts of a coating material;
the tofacitinib citrate tablet provided by the invention comprises the following components in parts by weight: 8-8.5 parts of tofacitinib citrate: 180 parts of a filler: 6-10 parts of a disintegrating agent: 1-1.5 parts of a lubricant: 6-8 parts of a coating material.
The invention also provides a tofacitinib citrate tablet prepared by the following preparation method:
1) Weighing and proportioning: weighing and mixing the raw materials and the auxiliary materials according to the mass ratio;
2) Mixing: adding a part of prescription dose of spray-dried lactose into tofacitinib citrate, adding a disintegrant and mixing; pouring the obtained mixture and the rest prescription amount of spray-dried lactose and microcrystalline cellulose into a shaking screen;
3) Total mixing: after the sieved materials are placed in a multi-directional motion mixer to be mixed, the lubricant with the prescribed amount is added to be mixed again;
4) Tabletting: and (4) putting the mixed powder into a tablet machine for tabletting.
The invention also aims to provide a preparation process of tofacitinib citrate tablets, which comprises the following steps
1) Weighing and proportioning: weighing and mixing the raw materials and the auxiliary materials according to the mass ratio;
2) Mixing: adding a part of prescription dose of spray-dried lactose into tofacitinib citrate, adding a disintegrant and mixing; pouring the obtained mixture and the rest prescription amount of spray-dried lactose and microcrystalline cellulose into a shaking screen;
3) Total mixing: mixing the sieved materials in a multidirectional motion mixer, adding a lubricant with a prescribed amount, and mixing again;
4) Tabletting: putting the mixed powder into a tablet press to be pressed into tablets
5) Coating: weighing the coating powder according to the prescription amount, and preparing the coating liquid by using purified water; coating the tablets by using a coating pan, and drying the coated tablets to obtain the tofacitinib citrate tablets.
The preparation process does not comprise the step of crushing the raw materials and/or the step of sieving and pre-treating the filler.
The step 2) in the preparation process is as follows: adding 1/2 of prescription amount of spray-dried lactose into tofacitinib citrate, adding a disintegrant and mixing; the resulting mixture was poured onto a shaker screen with the remaining 1/2 of the prescribed amount of spray dried lactose and microcrystalline cellulose.
In the preparation process, the oscillating screen in the step 2) is a 40-mesh screen, and the screening is repeated twice.
The step 3) in the preparation process is as follows: placing the sieved materials into a multidirectional motion mixer to be mixed for 20 minutes; the lubricant was added in the prescribed amount and mixed for 5 minutes.
The theoretical tablet weight of the plain tablets in the step 4) in the preparation process is as follows: 5 mg/mixed powder (calculated according to tofacitinib), a phi-tofacitinib circular shallow concave die is adopted for tabletting, the difference of tablet weight is controlled within +/-die pressing tablets, and the hardness is controlled to be 50-70N.
In step 5) of the above preparation process: the concentration of the coating solution is 12% (w/w) of solid content; and/or controlling the weight increase of the coating to be 2.0-4.0%; and/or drying for at least 5 minutes after coating is complete. Wherein the rotating speed of the coating pan is 1.8-6 rpm, the air inlet temperature is 45-60 ℃, the air outlet temperature is 35-45 ℃, and the rotating speed of the peristaltic pump is 3.0-8.0rpm.
The tofacitinib citrate tablet and the preparation process thereof provided by the invention have the following advantages:
1. the particle size of API is not required to be controlled by a crushing process, and the filler is not required to be sieved before use, so that the production process is simplified, the production efficiency is improved, the raw materials are saved, and the cost is reduced;
2. the compatibility of the main component and the coating material is good, which is beneficial to improving the stability of the product;
3. the prepared tablet has the advantages of low impurity content and good long-term storage stability.
Detailed Description
The raw materials and equipment used in the embodiment of the invention are known products, and are obtained by purchasing commercially available products
Example 1
Tofacitinib citrate tablet, the tablet core comprises: tofacitinib citrate (8.078 g), lactose (F100) (120 g), microcrystalline cellulose (PH 102) (60 g), croscarmellose sodium (10 g), magnesium stearate (1 g); the coating layer comprises: film coated premix (8 g), purified water (58.67 g).
Example 2
Tofacitinib citrate tablet, the tablet core comprises: tofacitinib citrate (8.078 g), lactose F100 (90 g), microcrystalline cellulose PH102 (90 g), crospovidone (10 g), magnesium stearate (1 g); the coating layer comprises: film coating premix (7 g), purified water (56.64 g).
Example 3
Tofacitinib citrate tablet, the tablet core comprises: tofacitinib citrate (8.078 g), lactose F100 (120 g), microcrystalline cellulose PH102 (60 g), croscarmellose sodium (6 g), magnesium stearate (1 g); the coating layer comprises: film coating premix (6 g), purified water (54 g).
Example 4
Tofacitinib citrate tablet, the tablet core comprises: tofacitinib citrate (8.078 g), lactose F100 (90 g), microcrystalline cellulose PH102 (90 g), croscarmellose sodium (6 g), magnesium stearate (1 g), the coating comprising: film coating premix (8 g), purified water (58.67 g).
The preparation of examples 1 to 4 is carried out in the following process steps:
step 1) weighing and batching: weighing raw and auxiliary materials according to the prescription amount for later use;
step 2) mixing: weighing 1/2 of prescription amount of lactose F100, adding the lactose F100 into tofacitinib citrate, adding a disintegrating agent, pouring the mixture and the rest prescription amount of lactose F100 and microcrystalline cellulose PH102 into a shaking sieve at the same time, sieving the mixture by a 40-mesh sieve, collecting mixed powder, and repeatedly sieving the mixed powder twice. The sieved material was collected and placed in a multi-directional motion mixer to mix for 20 minutes.
Step 3) total mixing: adding magnesium stearate in a prescription amount, mixing for 5 minutes, and sampling to detect the content of mixed powder;
step 4), tabletting: calculating the theoretical tablet weight according to the detection result of the mixed powder content, wherein the theoretical tablet weight of the plain tablet is as follows: 5 mg/mixed powder content. Putting the mixed powder into a tablet press, adopting a phi tablet machine, adopting a round shallow concave punching die for tabletting, controlling the difference of tablet weight within +/-die pressing tablets, and controlling the hardness within 50-70N;
step 5), coating: weighing the coating powder according to the prescription amount, and preparing coating liquid with the solid content of 12 percent by using purified water (the coating liquid is prepared immediately after use); controlling the rotating speed of a coating pan at 1.8-6 rpm, the air inlet temperature at 45-60 ℃, the air outlet temperature at 35-45 ℃, the rotating speed of a peristaltic pump at 3.0-8.0rpm, adjusting the position of a spray gun, the atomization degree and the spraying sector, controlling the weight of the coating to be increased by 2.0-4.0%, and drying the coating at the air inlet temperature for at least 5min before tablet collection.
Step 6), packaging: packaging with HDPE bottle, adding 1 bag of desiccant per bottle, and heat sealing. After external packaging, full inspection and warehousing.
Experimental example 1 dissolution examination
Examples 1-4 dissolution profile measurements were carried out as follows:
according to the first method of 0931 in the four-part general rules of the national pharmacopoeia 2015 edition: basket method, HPLC method determination, dissolution medium:
volume of medium: 500mL; temperature of the medium: 37 ℃; rotating speed: 50 revolutions per minute; sampling time: 5. 10, 15, 20 and 30min;
respectively taking the solution as a test solution at a set time point; preparing a tofacitinib citrate reference substance solution with the concentration of 0.16mg/10ml; the sample is measured by an HPLC method, and the chromatographic conditions are as follows: a chromatographic column: a shishengtang MGII C18,4.6mm multiplied by 250mm,5 μm or a chromatographic column with equivalent efficiency; detection wavelength: 220nm; flow rate: 1.0ml/min; column temperature: 30 ℃; mobile phase (a: B = 80): a mobile phase A:0.01mol/L dipotassium hydrogen phosphate solution (pH adjusted to 6.3 with phosphoric acid) -acetonitrile (90; and (3) mobile phase B: acetonitrile-water (90. The amount of elution was calculated as peak area by external standard method. The results are shown in Table 1
TABLE 1 measurement results of dissolution curves
As can be seen from Table 1, the tofacitinib citrate tablet provided by the invention has good dissolution effects in a meta-acid dissolution medium, a meta-alkali dissolution medium and a neutral dissolution medium, the dissolution rate is high, the dissolution rate is over 94% in 15 minutes, the dissolution is sufficient, and the dissolution rate is over 97% in 30 minutes.
EXAMPLE 2 test for investigating the quality and stability of tofacitinib citrate tablets
The related substance investigation results of the tofacitinib citrate tablet are shown in the following table 2:
TABLE 2 substance assay results of Tofacitinib citrate tablet
| Investigation time | Day 0 (%) | Long term test * 12 month (%) | Accelerated test ** 6 month (%) |
| Impurity A | *** N.D. | *** N.D. | *** N.D. |
| Impurity B | *** N.D. | *** N.D. | 0.04 |
| Impurity D | *** N.D. | *** N.D. | *** N.D. |
| Impurity P | *** N.D. | *** ND | *** N.D. |
| Impurity H | *** N.D. | *** N.D. | *** N.D. |
| Simple impurity | *** N.D. | 0.06 | 0.04 |
| Total miscellaneous | *** N.D. | 0.06 | 0.08 |
* Long-term test conditions: the temperature is 30 +/-2 ℃, and the relative humidity is highDegree 65% RH. + -.5% RH;
** accelerated test conditions: the temperature is 40 ℃. + -. 2 ℃, the relative humidity is 75 percent RH. + -. 5 percent RH;
*** n.d. indicates no detection.
TABLE 3 impurity names and structures
As can be seen from table 2, neither known nor unknown impurities were detected, neither known nor unknown impurities increased after being left for 12 months under the long-term experimental conditions, the total impurity growth amount was small, and the sample quality was stable.
Experimental example 3 compatibility test of API and film coating premix
API and film coating premix were mixed as 1:1 (w/w), placing in a stability box, standing at 60 + -2 deg.C for 10 days, and measuring the contents of the related substances in the samples at 0 day and 10 days, respectively, as shown in Table 4.
TABLE 4 compatibility of API with coating Agents
* The talcum powder-free coating agent comprises the following components: hydroxypropyl methylcellulose, titanium dioxide, polyethylene glycol and glyceryl triacetate
** The coating agent containing talcum powder comprises the following components: hydroxypropyl methylcellulose, titanium dioxide, polyethylene glycol, pulvis Talci, and glyceryl triacetate
As can be seen from Table 4, the coating powder containing the talcum powder and the API have obvious impurity growth trend during stability investigation, and the growth rate is 70%; the coating powder without talcum powder is relatively stable, and the impurity growth rate is 9%.
The coating powder without talcum powder is further used for coating the tablet, and the compatibility is checked again, and the result is shown in table 5.
TABLE 5 compatibility test results of tofacitinib citrate tablets with coating agent without talc
* The coating agent comprises the following components: hydroxypropyl methylcellulose, titanium dioxide, polyethylene glycol and glyceryl triacetate
** N.D. indicates no detection
As can be seen from Table 5, the coating powder without talcum powder is further used for coating the tablets, and the raw materials and the auxiliary materials have good compatibility, low impurity growth rate and high product purity, so that the coating material without talcum powder is used for coating the tofacitinib citrate, the quality of the tablets is improved, and the medication safety of people can be better guaranteed.
Claims (8)
1. Tofacitinib citrate tablet, which consists of tofacitinib citrate, a filling agent, a disintegrating agent, a lubricant, a coating material and other pharmaceutically acceptable auxiliary materials, and is characterized in that the filling agent consists of spray-dried lactose and microcrystalline cellulose;
the weight parts of the components are as follows: 9-10 parts of tofacitinib citrate: 170-190 parts of a filler: 5-12 parts of a disintegrating agent: 0.5-2 parts of a lubricant: 5-9 parts of a coating material;
the spray-dried lactose is lactose F100, the microcrystalline cellulose is microcrystalline cellulose PH102, and the mass ratio of the lactose F100 to the microcrystalline cellulose PH102 is (2);
the coating material is opadry coating powder without talcum powder, and comprises the following components: hypromellose, titanium dioxide, polyethylene glycol, and glyceryl triacetate.
2. The tofacitinib citrate tablet according to claim 1, wherein the disintegrant is selected from one or both of croscarmellose sodium and crospovidone; and/or, the lubricant is selected from any one or more of magnesium stearate, stearic acid, sodium stearyl fumarate and glyceryl behenate.
3. The tofacitinib citrate tablet according to claim 1, wherein said lubricant is magnesium stearate.
4. The tofacitinib citrate tablet as claimed in claim 1, wherein the tofacitinib citrate tablet comprises the following components in parts by weight: 8-8.5 parts of tofacitinib citrate: 180 parts of a filler: 6-10 parts of a disintegrating agent: 1-1.5 parts of a lubricant: 6-8 parts of a coating material.
5. The method for preparing tofacitinib citrate tablets according to any one of claims 1 to 4, wherein the method comprises the following steps:
1) Weighing and proportioning: weighing and mixing the raw materials and the auxiliary materials according to the mass ratio;
2) Mixing: adding a part of prescription dose of spray-dried lactose into tofacitinib citrate, adding a disintegrant and mixing; pouring the obtained mixture and the rest prescription amount of spray-dried lactose and microcrystalline cellulose into a shaking screen;
3) Total mixing: placing the sieved materials into a multidirectional motion mixer to be mixed; adding the lubricant with the prescription amount and mixing again;
4) Tabletting: and (4) putting the mixed powder into a tablet machine for tabletting.
6. The process for preparing tofacitinib citrate tablet according to claim 5, further comprising the steps of:
5) Coating: weighing the coating powder according to the prescription amount, and preparing coating liquid by using purified water; coating the tablets by using a coating pan, and drying the coated tablets to obtain the tofacitinib citrate tablets.
7. The process for preparing tofacitinib citrate tablet according to claim 5 or 6, wherein the process does not comprise the step of crushing the raw materials; and/or the step of sieving the filler.
8. The method for preparing tofacitinib citrate tablet as claimed in claim 5 or 6, wherein the step 2) is: adding 1/2 of prescription amount of spray-dried lactose into tofacitinib citrate, adding a disintegrant and mixing;
pouring the resulting mixture with the remaining 1/2 of the prescribed amount of spray-dried lactose and microcrystalline cellulose into a shaker screen; and/or the oscillating screen is a 40-mesh oscillating screen, and the screening is repeated twice.
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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 |
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| CN103585126A (en) * | 2013-11-18 | 2014-02-19 | 南京艾德凯腾生物医药有限责任公司 | Tofacitinib composition and preparation method thereof |
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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 |
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