Pharmaceutical composition of bazedoxifene acetate tablets and preparation method thereof

A technology of bazedoxifene acetate and its composition, which is applied in the field of pharmaceutical preparations, can solve the problems of clinical treatment effect and potential safety hazards, large inter-batch differences, and poor reproducibility, so as to improve inter-batch quality differences and ensure uniform content degree of effect

Active Publication Date: 2020-12-15
SICHUAN KELUN PHARMA RES INST CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0006] Through the in-depth comparative study on the in vitro dissolution of multiple batches of samples of existing commercially available products, it is found that commercially available products have large batch-to-batch differences and poor reproducibility, which leads to certain hidden dangers in clinical treatment effect and safety

Method used

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  • Pharmaceutical composition of bazedoxifene acetate tablets and preparation method thereof
  • Pharmaceutical composition of bazedoxifene acetate tablets and preparation method thereof
  • Pharmaceutical composition of bazedoxifene acetate tablets and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0074] Embodiment 1 Bazedoxifene acetate particle size investigation test

[0075] Get the bazedoxifene acetate bulk drug of different particle diameters, prepare bazedoxifene acetate tablet according to following prescription and preparation process, carry out dissolution rate measurement to gained tablet under the condition of pH4.5 and 0.25%SDS, to investigate The effect of the particle size of the bulk drug on the dissolution of the tablet, the results are shown in Table 1.

[0076] prescription:

[0077] Material name Prescription amount (mg) bazedoxifene acetate 22.60 lactose 127.94 Vitamin C 6.00 precrossified starch 15.50 Low-substituted hydroxypropyl cellulose 54.25 Colloidal silica 4.65 microcrystalline cellulose 62.00 Sodium dodecyl sulfate 4.65 Glyceryl behenate 6.20

[0078] Preparation Process:

[0079] Mix bazedoxifene acetate, vitamin C, colloidal silicon dioxide and 1 / 2 prescription amount...

Embodiment 2

[0083] Embodiment 2 wet granulation time research

[0084] According to the prescription of embodiment 1, adopt different wet granulation time to prepare bazedoxifene acetate tablet respectively, all the other preparation processes are identical with embodiment 1. The prepared tablets were tested for dissolution under the conditions of pH 4.5 and 0.25% SDS to investigate the influence of different granulation times on the dissolution of the tablets. The results are shown in Table 2.

[0085] Table 2 Wet granulation time investigation trial sample dissolution curve detection results

[0086]

[0087]

[0088] It can be seen from the above table that when the granulation time is in the range of 2min to 6min, the dissolution rate of the samples in Examples 2-1 to 2-7 is above 80% in 60 minutes, especially when the granulation time is in the range of 2min to 6min. At 3 minutes, the dissolution rate can reach more than 90%, indicating that the granulation time can meet the p...

Embodiment 3

[0089] Example 3 Wetting agent solution addition time investigation

[0090] According to the prescription of Example 1, Bazedoxifene Acetate Tablets were prepared at different adding times of the wetting agent solution, and the rest of the preparation process was the same as in Example 1. The prepared tablets were tested for dissolution under the conditions of pH 4.5 and 0.25% SDS to investigate the effect of adding time of different wetting agent solutions on the dissolution of the tablets. The results are shown in Table 3.

[0091] Table 3 Wetting agent solution addition time investigation test results of dissolution curve of trial samples

[0092]

[0093] It can be seen from the above table that when the adding time of the wetting agent is in the range of 90s to 120s, the dissolution rates of the samples in Examples 3-1 to 3-4 are all above 75% within 60 minutes, especially when the wetting agent solution is added When the time is in the range of 100s to 120s, the dis...

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Abstract

The invention relates to a pharmaceutical composition containing bazedoxifene acetate as an effective component and a preparation method thereof. The composition comprises bazedoxifene acetate; lactose; microcrystalline cellulose; pregelatinized starch; low-substituted hydroxypropyl cellulose; colloidal silica; sodium dodecyl sulfate; vitamin C; and glyceryl behenate. The invention also relates toa preparation method of the composition. The pharmaceutical composition of the present invention has the effects of improving the inter-batch difference on drugs, and ensuring the content uniformityof drugs and consistent dissolution of different batches of drugs, and has medicinal safety and effectiveness.

Description

technical field [0001] The invention belongs to the field of pharmaceutical preparations, in particular to a pharmaceutical composition of bazedoxifene acetate tablets and a preparation method thereof. Background technique [0002] Bazedoxifene acetate, English name: Bazedoxifene Acetate, also known as bazedoxifene acetate, chemical name is 1-{4-2-(cyclohexaneimino-1-)ethoxy]benzyl}-2-( 4-hydroxyphenyl)-3-methyl-1H-indole-5-phenol acetate has the following structural formula: [0003] [0004] Bazedoxifene acetate is a selective estrogen receptor modulator (SERM) developed by European Ligand company partner Wyeth in 1997. In April 2009, it was approved for marketing by Pfizer in the European Union (EMA). ファイザー Co., Ltd. was approved for listing in Japan on July 23, 2010, under the trade name Viviant. Bazedoxifene acetate can competitively inhibit the binding of 17β-estradiol to ERα and ERβ, and has no agonist activity on human breast cancer cell lines when used alone, ...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/20A61K47/38A61K47/36A61K47/22A61K47/26A61K47/20A61K31/55A61P19/10
CPCA61K9/2059A61K9/2054A61K9/2018A61K9/2013A61K31/55A61P19/10
Inventor 陈俊蓉刘小均李锐秦亚陈龙江沈利赵栋王晶翼
Owner SICHUAN KELUN PHARMA RES INST CO LTD
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