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Improved release dosage of febuxostat and preparation method of release dosage

A technology of febuxostat and slow-release clothing, which is applied to medical preparations with non-active ingredients, medical preparations containing active ingredients, and pharmaceutical formulas, and can solve the problem of high side effects

Inactive Publication Date: 2017-10-03
JIANGSU HENGRUI MEDICINE CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

If the drug dissolves too quickly from the drug formulation, the blood concentration of the drug will increase rapidly, with a high risk of side effects

Method used

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  • Improved release dosage of febuxostat and preparation method of release dosage
  • Improved release dosage of febuxostat and preparation method of release dosage
  • Improved release dosage of febuxostat and preparation method of release dosage

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0087] Example 1 Formulation of febuxostat consisting of an immediate release portion of febuxostat and febuxostat sustained release pellets that release the drug slowly over a period of about 24 hours

[0088] The following composition is a single pulse and slow release drug delivery system in which a single capsule contains two types of febuxostat granules / pellets. One pulse consisted of immediate-release febuxostat granules containing a total of 20 mg of febuxostat, wherein the febuxostat was released immediately after ingestion by the patient. The remainder of the capsule contained controlled-release febuxostat pellets containing a total of 20 mg of febuxostat, which were released over an extended period of about 24 hours (immediately after ingestion by the patient). The immediate release febuxostat granules are prepared by dry granulation process, and its formulation composition is listed in Table 1 below. The composition of the controlled-release 24-hour pellets is list...

Embodiment 2

[0100] Example 2 The febuxostat preparation consisting of the febuxostat part for immediate release and the febuxostat sustained-release pellets for slow release of the drug over a period of about 12 hours under pH 6.8 conditions

[0101] The following composition is a single pulse and slow release drug delivery system under specific pH conditions, where a single capsule contains two types of febuxostat pellets. One pulse consisted of immediate-release febuxostat pellets containing a total of 12 mg of febuxostat, which was released immediately after ingestion by the patient. The remainder of the capsule contains a total of 28 mg of febuxostat under specific pH conditions (pH 6.8) slow-release febuxostat pellets, the febuxostat under pH 6.8 conditions for an extended period of about 12 hours Release (starts immediately after ingestion by the patient). The immediate-release febuxostat pellets were prepared by extrusion-spheronization process, and their formulation compositions ...

Embodiment 3

[0114] Embodiment 3 human body pharmacokinetic research

[0115] Taking the commercially available 40mg specification febuxostat tablet as the reference preparation, the human pharmacokinetic research was carried out together with the preparations obtained in Example 1 and Example 2, and the research results are shown in the following table:

[0116] Table 7. Pharmacokinetic parameters of different preparations

[0117] preparation

C max (ng / mL)

T max (h)

AUC 0→∞( ng / mL*h)

T C≥100μg / mL (h)

Fr(％)

Example 1

591±212.231

3.286±0.756

3522.18±981.16

10

44.54

Example 2

1067±788.339

3.188±2.267

6278.621±3186.562

12

79.38

Reference preparation

1963.75±787.12

1.438±0.98

7908.342±3311.135

10

—

[0118] C max : maximum peak plasma concentration

[0119] T max : Maximum blood concentration time

[0120] AUC 0→∞ : drug-time curve area

[0121] T C≥100μg / mL : effective blood conc...

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Abstract

The invention relates to an improved release dosage form of febuxostat and a preparation method thereof. Specifically, the febuxostat preparation of the present invention consists of febuxostat granules or pellets with different release properties. The preparation can effectively reduce the peak value of drug concentration in blood plasma, prolong drug action time, reduce side effects and improve patient compliance.

Description

technical field [0001] The present invention relates to solid formulations which exhibit improved drug dissolution properties from the formulation. In addition, the present invention also relates to methods for treating certain diseases using the solid preparation of the present invention. Background technique [0002] The chemical name of Febuxostat is 2-[(3-cyano-4-isobutoxy)phenyl]-4-methyl-5-thiazolecarboxylic acid, and its molecular formula is C 16 h 16 N 2 o 3 S, molecular weight is 316.374, its structural formula is as follows: [0003] [0004] Teijin Corporation of Japan applied for listing in Japan in 2004, and it applied for listing in the United States at the end of the year. IPSEN Company applied for listing in Europe. At present, febuxostat tablets have been listed in China. Febuxostat is an effective non-purine selective inhibitor of a new generation of xanthine oxidase, which can selectively inhibit xanthine oxidase (XO), reduce the level of uric acid...

Claims

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Application Information

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IPC IPC(8): A61K9/58A61K9/56A61K47/32A61K47/14A61K9/16A61K31/426A61P19/06
CPCA61K9/5026A61K9/1652A61K9/5015A61K9/5073A61K9/5089A61K31/426
Inventor 张强徐林强曹笑立张辉刘凯
Owner JIANGSU HENGRUI MEDICINE CO LTD
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