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Tofacitinib citrate sustained release tablet

A technology of tofacitinib and citric acid, which is applied in the field of tofacitinib citrate sustained-release tablets and their preparation, can solve related substances, active ingredient content, changes in dissolution, easily affected by external environment, materials Problems such as decreased liquidity

Pending Publication Date: 2021-05-07
CSPC OUYI PHARM CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Due to its strong hygroscopicity, sorbitol is easy to bond with other materials into agglomerates in the premixing step, which reduces the fluidity of the material and reduces the content uniformity and dissolution uniformity of the preparation.
And the obtained sustained-release preparation is easily affected by the external environment during storage, resulting in changes in related substances, active ingredient content, dissolution rate, etc.

Method used

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  • Tofacitinib citrate sustained release tablet
  • Tofacitinib citrate sustained release tablet
  • Tofacitinib citrate sustained release tablet

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0142] The consumption of embodiment 1 osmotic pressure forming agent (sorbitol SI150, sodium chloride) is investigated

[0143] The dosage of osmotic pressure forming agent (sorbitol SI150 and sodium chloride) is screened, and the specific preparation prescription is as follows:

[0144]

[0145] Remarks: *17.77g of tofacitinib citrate is equivalent to 11g of tofacitinib.

[0146] **The perforated tablet is obtained by laser perforation of the sustained-release layer-coated tablet. The perforation diameter is 0.65mm, which has little effect on the tablet weight.

[0147] The preparation method is as follows:

[0148] 1. Pretreatment of raw and auxiliary materials

[0149] Weigh in turn the components of the tablet core: tofacitinib citrate, sorbitol SI150, sodium chloride, hydroxyethylcellulose 250L, hydroxyethylcellulose 250G, copovidone VA64, magnesium stearate, ②Sustained-release layer coating material: cellulose acetate 398-10, hydroxypropyl cellulose EF, ③film coat...

Embodiment 2

[0172] Example 2 Investigation on the dosage ratio of sustained-release materials (hydroxyethyl cellulose 250L, hydroxyethyl cellulose 250G)

[0173] Referring to the prescription 1-1 and its preparation method in Example 1, only the dosage ratio of the sustained-release materials hydroxyethyl cellulose 250L and hydroxyethyl cellulose 250G was adjusted. The specific dosage values ​​and the measured dissolution curve results are shown in Table 2.

[0174] The results show that with the increase of the dosage of hydroxyethyl cellulose 250L and the decrease of the dosage of 250G of hydroxyethyl cellulose, the dissolution rate tends to accelerate.

[0175] Table 2 Influence of composition of sustained-release material on dissolution profile

[0176]

Embodiment 3

[0177] Example 3 Investigation on the dosage ratio of osmotic pressure forming agent and sustained-release material

[0178]With reference to the prescription 1-1 and preparation method of Example 1, adjust the consumption ratio of osmotic pressure forming agent (sorbitol, sodium chloride) and slow-release material (hydroxyethyl cellulose 250L, hydroxyethyl cellulose 250G). The values ​​and dissolution profile results determined are shown in Table 3.

[0179] The results showed that the dosage of osmotic pressure-forming agent was increased and the dosage of slow-release material was decreased in prescription 3-2 compared with prescription 3-1, the dissolution rate of the obtained preparation was accelerated, and the release was basically complete within 6 hours (94% dissolution), resulting in weak release in the later stage. , 6h-10h release only 4%, which is not conducive to maintaining a uniform and stable blood concentration.

[0180] Compared with prescription 3-1, the d...

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Abstract

The invention provides a tofacitinib citrate sustained release tablet. The tofacitinib citrate sustained release tablet is composed of a tablet core, a sustained release layer coating and a color layer coating, wherein drug release pores are formed in the sustained release layer coating. According to the tofacitinib citrate sustained release tablet, the composition of an osmotic pressure forming agent and the dosage ratio of the osmotic pressure forming agent to a sustained release agent are adjusted, and the composition of the sustained release layer coating and the weight increment of the coating are further optimized, so that the defect that the dissolution speed is reduced after long-term storage when sorbitol is singly used as the osmotic pressure forming agent is avoided, the initial release speed of the tofacitinib citrate sustained release tablet is increased, the tofacitinib citrate sustained release tablet can be slowly and continuously released after being kept for 6 hours, the drug release is relatively complete, the blood concentration is kept at a uniform and stable level for a long time, the fluctuation of the blood concentration during the administration interval is reduced, the bioavailability is further improved, the adverse reaction is reduced, and the clinical curative effect and safety are guaranteed.

Description

technical field [0001] The invention belongs to the field of pharmaceutical preparations, and particularly relates to a tofacitinib citrate sustained-release tablet and a preparation method thereof. Background technique [0002] Tofacitinib citrate is a prescription drug of a class of oral Janus kinase (JAK) inhibitors originally developed by Pfizer, which can selectively inhibit JAK kinase and block the JAK / STAT pathway, thereby inhibiting cell signal transduction and related gene expression and activation , for the treatment of rheumatoid arthritis, psoriatic arthritis, ulcerative colitis and other immune diseases. The products currently on the market are Pfizer's Xeljanz and Xeljanz XR. Among them, Xeljanz is an immediate-release tablet of tofacitinib citrate, which needs to be taken twice a day, lacking convenience and poor compliance. Xeljanz XR, the first oral once-daily JAK inhibitor for the treatment of rheumatoid arthritis. The use of this sustained-release dosag...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/36A61K9/22A61K31/519A61K47/38A61K47/32A61K47/26A61K47/02A61P1/04A61P19/02A61P29/00A61P37/02
CPCA61K31/519A61K9/2054A61K9/2018A61K9/2027A61K9/2009A61K9/2886A61K9/2866A61P19/02A61P29/00A61P1/04A61P37/02
Inventor 贾广辉魏俊卿王亚平白艳玲王建明
Owner CSPC OUYI PHARM CO LTD
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