Bazedoxifene acetate sustained release preparation with excellent performance

The technology of bazedoxifene acetate and preparation is applied in the field of bazedoxifene acetate sustained-release preparation and its preparation technology, which can solve the problems such as no research report on sustained-release preparation, achieve lasting and stable blood concentration and simple preparation process , the effect of improving medication adherence

Active Publication Date: 2014-06-25
JIANGSU SEMPOLL PHARMA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

There is no report on the development of sustained-release preparations

Method used

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  • Bazedoxifene acetate sustained release preparation with excellent performance
  • Bazedoxifene acetate sustained release preparation with excellent performance
  • Bazedoxifene acetate sustained release preparation with excellent performance

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0028] Prescription: Dosage per 1000 capsules:

[0029] Bazedoxifene Acetate 2.26g

[0030] Vitamin E TPGS 5.0g

[0031] Stearic acid 42.74g

[0032] Specifications: main drug content 2.26mg / grain, pill weight 50mg / grain.

[0033] Process: Grind the raw material of bazedoxifene acetate and finely grind it to more than 150 meshes; weigh vitamin E TPGS and stearic acid according to the prescription; heat and melt the hydrophilic matrix, add bazedoxifene acetate and mix well, then add hydrophobic Mix the base of the dropping pills to form a suspension; keep the above eutectic solution at 80-85°C; In the methyl silicone oil, remove and drain the silicone oil, and wipe off the silicone oil attached to the surface of the dripping pill with medical gauze.

Embodiment 2

[0035] Prescription: Dosage per 1000 capsules:

[0036] Bazedoxifene Acetate 4.52g

[0037] Vitamin E TPGS 10.0g

[0038] Glyceryl monostearate 35.48g

[0039] Specifications: main drug content 4.52mg / grain, pill weight 50mg / grain.

[0040] Process: Grind and finely grind bazedoxifene acetate raw materials to more than 150 meshes; weigh vitamin E TPGS and monostearic acid glyceric acid according to the prescription; heat and melt the hydrophilic matrix, add bazedoxifene acetate and mix well Then add the hydrophobic dropping pill matrix and mix well to form a suspension; keep the above eutectic solution at 80-90°C; In the simethicone oil at room temperature, remove the silicone oil and wipe off the silicone oil attached to the surface of the dropping pills with medicinal gauze.

Embodiment 3

[0042] Prescription: Dosage per 1000 capsules:

[0043] Bazedoxifene Acetate 2.26g

[0044] Vitamin E TPGS 15.0g

[0045] Octadecanol 32.74g

[0046] Specifications: main drug content 2.26mg / grain, pill weight 50mg / grain.

[0047] Process: Grind and finely grind bazedoxifene acetate raw materials to more than 150 meshes; weigh vitamin E TPGS and stearyl alcohol according to the prescription; heat and melt the hydrophilic matrix, add bazedoxifene acetate and mix well, and then add hydrophobic Mix the base of the dropping pills to form a suspension; keep the above eutectic solution at 80-90°C; In the methyl silicone oil, remove and drain the silicone oil, and wipe off the silicone oil attached to the surface of the dripping pill with medical gauze.

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PUM

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Abstract

The invention discloses a bazedoxifene acetate sustained release preparation with excellent performance and a preparation process thereof. The preparation is a sustained release dropping pill, which comprises the following components in percentage by weight: 1-25 percent of bazedoxifene acetate, 40-70 percent of hydrophobic dropping pill matrix, and 5-40 percent of hydrophilic matrix. The sustained release dropping pill has a higher chemical stability, physical stability (low-crystal form conversion rate) and in-vivo drug-release behavior (higher bioavailability and smooth and durable plasma concentration).

Description

【Technical field】 [0001] The present invention relates to a particularly stable bazedoxifene preparation with excellent properties. More specifically, the present invention relates to a bazedoxifene acetate sustained-release preparation with excellent performance, especially stable one, and its preparation process. 【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] The chemical name of bazedoxifene acetate is (1-[4-(2-azepan-1-yl-ethoxy)-benzyl]-2-(4-hydroxy-phenyl)-3-methyl base-1H-indole-5-ol acetic acid), has the chemical structure shown below: [0004] [0005] Polymorph A of ...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K47/34A61K31/55A61K9/22A61K9/48
Inventor 王学政汪亚萍王晶陈玉兰陈镭
Owner JIANGSU SEMPOLL PHARMA
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