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Apixaban co-micronized product

A technology of co-micronization and apixaban, which is applied in the field of medicine, can solve the problems of poor reproducibility, poor compressibility of excipients, and difficult particle control, so as to improve bioavailability, increase dissolution rate, and good stability Effect

Active Publication Date: 2020-06-02
ZHANGZHOU PIEN TZE HUANG PHARM
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, the repeated compression and crushing of dry granulation makes the compressibility of excipients worse, which is not conducive to subsequent tablet compression, and the process is more cumbersome
[0011] The publication number is CN102770126, which discloses the technology of dry granulation and wet granulation. The disadvantage of its wet granulation is that the production process is complicated, the production cycle is relatively long, and wet granulation machines, fluidized beds or dryers are required. Granulator, etc., the production cost is relatively high; dry granulation requires dry granulator and granulator, and the control of granules produced by different equipment is difficult and the reproducibility is poor

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0047] Example 1: Screening of excipients for co-micronization of apixaban

[0048] 1. Materials and methods

[0049] Apixaban was mixed with the co-micronized excipients to be tested in the desired weight ratios in a hopper mixer until a homogeneous mixture was obtained. Subsequently, the obtained mixture was micronized in a jet mill.

[0050] In Vitro Dissolution of Comicronized Apixaban

[0051] For each co-micronized product obtained, a tablet containing an amount corresponding to 2.5 mg of apixaban was prepared.

[0052] The dissolution determination method adopts the second method in the dissolution determination method of the Chinese Pharmacopoeia 2015 edition, selects 0.05mol / L sodium phosphate solution (adjusting the pH value to 6.8 with phosphoric acid) as the dissolution medium with distinguishing power, paddle method 75 rpm, The temperature is 37±0.5°C, and it is determined by a Lugen dissolution apparatus.

[0053] The sampling time is 5, 10, 15, 20, 30, 45,...

Embodiment 2

[0061] Example 2 Effect of Apixaban / Sodium Lauryl Sulfate Weight Ratio on the In Vitro Dissolution of Apixaban

[0062] 1. Materials and methods

[0063] Various apixaban / sodium lauryl sulfate co-micronized products were prepared according to the co-micronization method described above in order to study the effect of apixaban / sodium lauryl sulfate weight ratio on the in vitro effect of apixaban effect on the dissolution rate.

[0064] 2. Results

[0065] Table 2 below and figure 2 The dissolution results obtained for each co-micronized material prepared are represented.

[0066] Table 2: Percentage of Apixaban Released Relative to the Initial Amount of Apixaban Contained in Tablets

[0067]

[0068] The above results indicated that the dissolution rate of apixaban increased with the decrease of the weight ratio of apixaban / sodium lauryl sulfate.

Embodiment 3

[0069] Embodiment 3: Apixaban / sodium lauryl sulfate co-micronized product mixed with apixaban / sodium lauryl sulfate Comparison of dissolution properties between compounds

[0070] 1. Materials and methods

[0071] Apixaban and sodium lauryl sulfate can be mixed in a mortar and mortar in a weight ratio of 3 / 1 and ground until a homogeneous mixture is obtained.

[0072] The remaining mixture was co-micronized using an airflow milling micronizer, and the obtained micronized product (ie, each tablet containing 2.5 mg of apixaban) was compressed into tablets.

[0073] The dissolution of apixaban from these two types of tablets was studied under the same conditions as described in Example 1 and in the same dissolution medium.

[0074] 2. Results

[0075] The dissolution results obtained for the apixaban / SLS co-micronized and non-micronized apixaban / SLS mixtures (physical mixtures) are presented in Table 3 below and image 3 shown in .

[0076] Table 3: Percentage of Apixaban...

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Abstract

The invention discloses an apixaban co-micronized product and a preparation method thereof and also discloses pharmaceutical composition containing the co-micronized product and a preparation method of the pharmaceutical composition. The pharmaceutical composition containing the apixaban co-micronized product is good in stability, can realize industrialization, is better applied to clinic, has more obvious advantages and can effectively improve the dissolution rate and the bioavailability.

Description

[0001] 1. Technical field [0002] The invention belongs to the technical field of medicine, and in particular relates to a co-micronized product of apixaban, a pharmaceutical composition containing the above-mentioned co-micronized product and a preparation method thereof. [0003] 2. Background technology [0004] Apixaban (Apixaban, trade name Eliquis) is an oral selective activated factor Xa inhibitor. In 2007, BMS teamed up with Pfizer to announce the joint development of apixaban, a new oral anticoagulant owned by BMS, as an upgraded alternative to warfarin. [0005] In 2011, Apixaban was approved for marketing in the European Union; in 2012, it was approved by the FDA; in 2013, it entered China, and in 2017, it entered the new version of the medical insurance catalog, which is used for adult patients undergoing elective hip or knee replacement to prevent venous thrombosis Embolic event. [0006] Apixaban is the third new-generation oral anticoagulant to be marketed aft...

Claims

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Application Information

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IPC IPC(8): A61K9/14A61K47/20A61K9/28A61K31/4545A61P7/02
CPCA61K9/145A61K9/2095A61K9/2013A61K9/28A61K31/4545A61P7/02
Inventor 黄进明洪绯于娟陈志亮罗志毅高龙辉纪学慧曹亮
Owner ZHANGZHOU PIEN TZE HUANG PHARM
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