A bazedoxifene acetate sustained-release preparation with excellent performance

A technology for bazedoxifene acetate and preparations, applied in the field of bazedoxifene acetate sustained-release preparations and preparation techniques thereof, can solve problems such as no research report on sustained-release preparations, achieve lasting and stable blood drug concentration, and improve medication compliance Sex, the effect of reducing side effects

Active Publication Date: 2016-03-02
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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  • A bazedoxifene acetate sustained-release preparation with excellent performance
  • A bazedoxifene acetate sustained-release preparation with excellent performance
  • A 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 ETPGS5.0g

[0031] Stearic acid 42.74g

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

[0033] Process: Grind and finely grind bazedoxifene acetate raw materials to more than 150 mesh; weigh vitamin ETPGS 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 and keep warm; transfer the above solution into a dropping device for dripping, control the temperature of the solution at 80-85°C, and drop it into the dimethylformamide at room temperature In the base silicone oil, remove and drain the silicone oil, and wipe off the silicone oil attached to the surface of the dripping pills with medicinal gauze.

Embodiment 2

[0035] Prescription: Dosage per 1000 capsules:

[0036] Bazedoxifene Acetate 4.52g

[0037] Vitamin ETPGS10.0g

[0038] Glyceryl monostearate 35.48g

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

[0040] Process: Grind the raw material of bazedoxifene acetate and finely grind it to more than 150 meshes; weigh vitamin ETPGS and monostearic acid glyceric acid according to the prescription; heat and melt the hydrophilic matrix, add bazedoxifene acetate and mix well before Add hydrophobic dripping pill base and mix well to form a suspension; keep the above eutectic solution at 80-90°C for heat preservation; transfer the above solution into a dripping device for dripping, control the solution temperature at 80-90°C, and drop it into room temperature In the simethicone oil, fish out and drain the silicone oil, and wipe off the silicone oil attached to the surface of the dripping pill with medicinal gauze.

Embodiment 3

[0042] Prescription: Dosage per 1000 capsules:

[0043] Bazedoxifene Acetate 2.26g

[0044] Vitamin ETPGS15.0g

[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 ETPGS and stearyl alcohol 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 80-90°C for heat preservation; transfer the above solution into a dripping device for dripping, control the temperature of the solution at 80-90°C, and drop it into the dimethylformamide at room temperature In the base silicone oil, remove and drain the silicone oil, and wipe off the silicone oil attached to the surface of the dripping pills with medicinal 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 Patents(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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