Bazedoxifene acetate composition with excellent property

A technology of bazedoxifene acetate and composition, applied in the field of bazedoxifene acetate composition with excellent performance, can solve problems such as affecting chemical stability, and achieve the effects of fast drug release speed and high chemical stability

Active Publication Date: 2014-06-11
JIANGSU SEMPOLL PHARMA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

thereby further affecting its chemical stability

Method used

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  • Bazedoxifene acetate composition with excellent property
  • Bazedoxifene acetate composition with excellent property
  • Bazedoxifene acetate composition with excellent property

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0032] Prescription: Dosage per 1000 capsules:

[0033] Bazedoxifene Acetate 4.52g

[0034] Vitamin E TPGS 15.0g

[0035] PEG 6000 30.48g

[0036] Specifications: main drug content 4.52mg / grain, pill weight 50mg / grain.

[0037] Process: Crush and finely grind bazedoxifene acetate raw materials to more than 150 mesh; weigh vitamin E TPGS and PEG 6000 according to the prescription; heat and melt vitamin E TPGS, add bazedoxifene acetate and mix well, then add PEG 6000 Mix well to form a suspension; heat the above eutectic solution at 80-90°C; transfer the above solution into a dripping device for dripping, control the temperature of the solution at 80-90°C, and drop it into simethicone oil at room temperature , take out and drain the silicone oil, wipe off the silicone oil attached to the surface of the dripping pill with medicinal gauze, and that's it.

Embodiment 2

[0039] Prescription: Dosage per 1000 capsules:

[0040] Bazedoxifene Acetate 2.26g

[0041] Vitamin E TPGS 2.74g

[0042] PEG 8000 45g

[0043] Specifications: main drug content 2.26mg / grain, pill weight 50mg / grain.

[0044] Process: Crush and finely grind the bazedoxifene acetate raw material to more than 150 meshes; weigh vitamin E TPGS and PEG 8000 according to the prescription; heat and melt the vitamin E TPGS, add bazedoxifene acetate and mix well, then add PEG 8000 Mix well to form a suspension; heat the above eutectic solution at 80-85°C; transfer the above solution into a dripping device for dripping, control the temperature of the solution at 80-85°C, and drop it into simethicone oil at room temperature , take out and drain the silicone oil, wipe off the silicone oil attached to the surface of the dripping pill with medicinal gauze, and that's it.

Embodiment 3

[0046] Prescription: Dosage per 1000 tablets:

[0047]

[0048]

[0049] Specifications: main drug content 22.6mg / tablet, weight 500mg / tablet.

[0050] Process: 1) Pulverize the bazedoxifene acetate raw material and grind it to a fineness of more than 150 mesh; heat and melt the vitamin E TPGS, add bazedoxifene acetate and mix well, then add PEG 6000 and mix well to form a suspension eutectic liquid; the above-mentioned eutectic liquid is cooled to room temperature and crushed to 60-80 mesh; 2), take lactose monohydrate, microcrystalline cellulose, pregelatinized starch, sodium starch glycolate and pass through 80 mesh sieve, add in process 1 The pulverized product, colloidal silicon dioxide, and magnesium stearate are mixed evenly and compressed into tablets.

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PUM

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Abstract

The invention discloses a bazedoxifene acetate composition with excellent properties. The composition comprises bazedoxifene acetate, polyethylene glycol (PEG) 6000-8000 and vitamin E tocopherol polyethylene glycol succinate (TPGS), wherein a solid solution and/or solid sol is formed by polyethylene glycol (PEG) 6000-8000 and vitamin E TPGS, and bazedoxifene acetate is dispersed into the solid solution and/or solid sol. The composition is high in chemical stability and medicine release speed.

Description

【Technical field】 [0001] The invention relates to a composition with excellent performance and a preparation process thereof. 【technical background】 [0002] Bazedoxifene, a new generation of SERM bazedoxifene, can competitively inhibit the binding of 1713-estradiol to estrogen receptors ERoc and ER13, has estrogen agonist activity on bones, and can improve spine and hip Therefore, it can significantly reduce the risk of vertebral fracture in postmenopausal women with osteoporosis. Its main indication is the prevention and treatment of postmenopausal bone. [0003] Bazedoxifene was originally researched by Wyeth and later transferred to Pfizer. It was approved by the European Food and Drug Administration on April 27, 2009 and launched in Italy and Spain under the trade name Conbriza. It was launched in Japan in July 2010 under the trade name Conbriza. Viviant. [0004] The chemical name of bazedoxifene acetate is (1-[4-(2-azepan-1-yl-ethoxy)-benzyl]-2-(4-hydroxy-phenyl)-3...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/55A61K47/34A61P19/10
Inventor 王学政周越强王晶陆晓华吕鹤涛
Owner JIANGSU SEMPOLL PHARMA
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