Solid preparation of bisoprolol / hydrochlorothiazide medicine composition liposome

A technology of hydrochlorothiazide and bisoprolol is applied in the field of medicine to achieve the effects of high encapsulation rate, good sustained release effect and high stability

Inactive Publication Date: 2013-12-11
HAINAN MEILAN SMITH KLINE PHARMA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0015] However, the challenge in preparing liposomes lies in selecting the appropriate liposome composition and formulation

Method used

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  • Solid preparation of bisoprolol / hydrochlorothiazide medicine composition liposome
  • Solid preparation of bisoprolol / hydrochlorothiazide medicine composition liposome
  • Solid preparation of bisoprolol / hydrochlorothiazide medicine composition liposome

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0089] Example 1 Bisoprolol / Hydrochlorothiazide Liposomal Tablets

[0090]

[0091] Adopt the following production process to prepare bisoprolol / hydrochlorothiazide liposome tablet:

[0092] (1) Accurately weigh 2.5g bisoprolol fumarate, 6.25g hydrochlorothiazide, 80g hydrogenated soybean lecithin, 20g dilauroylphosphatidylcholine, 50g cholesterol, 60g Tween 60, dissolve in 1200ml with a volume ratio of 2:1 In the mixed solvent of dichloromethane and isopropanol, stir to dissolve it;

[0093] (2) Put the above solution in an eggplant-shaped bottle, remove dichloromethane and isopropanol under reduced pressure in a 45°C water bath, and form a uniform transparent film on the wall of the bottle;

[0094] (3) Add 1200ml of phosphate buffer solution with a pH value of 7.0 to the eggplant-shaped bottle, and continue to rotate in a water bath at 45°C under normal pressure to swell and hydrate the film;

[0095] (4) Filter the above solution with a 0.45 μm microporous membrane,...

Embodiment 2

[0099] Example 2 Bisoprolol / Hydrochlorothiazide Liposomal Tablets

[0100]

[0101]

[0102] Adopt the following production process to prepare bisoprolol / hydrochlorothiazide liposome tablet:

[0103] (1) Accurately weigh 5g of bisoprolol fumarate, 6.25g of hydrochlorothiazide, 80g of hydrogenated soybean lecithin, 20g of dilauroylphosphatidylcholine, 50g of cholesterol, 120g of Tween 60, and dissolve them in 1500ml of In the mixed solvent of dichloromethane and isopropanol, stir to dissolve it;

[0104] (2) Put the above solution in an eggplant-shaped bottle, remove dichloromethane and isopropanol under reduced pressure in a 45°C water bath, and form a uniform transparent film on the wall of the bottle;

[0105] (3) Add 1500ml of phosphate buffer solution with a pH value of 7.0 to the eggplant-shaped bottle, and continue to rotate in a water bath at 45°C under normal pressure to swell and hydrate the film;

[0106] (4) Filter the above solution with a 0.45 μm micropo...

Embodiment 3

[0110] Example 3 Bisoprolol / Hydrochlorothiazide Liposomal Tablets

[0111] The raw and auxiliary materials used are as follows:

[0112]

[0113]

[0114] Adopt the following production process to prepare bisoprolol / hydrochlorothiazide liposome tablet:

[0115] (1) Accurately weigh 5g of bisoprolol fumarate, 6.25g of hydrochlorothiazide, 320g of hydrogenated soybean lecithin, 80g of dilauroylphosphatidylcholine, 200g of cholesterol, 120g of Tween 60 and dissolve them in 2000ml of bismuth with a volume ratio of 2:1. In the mixed solvent of methyl chloride and isopropanol, stir to dissolve it;

[0116] (2) Put the above solution in an eggplant-shaped bottle, remove dichloromethane and isopropanol under reduced pressure in a 45°C water bath, and form a uniform transparent film on the wall of the bottle;

[0117] (3) Add 2000ml of phosphate buffer solution with a pH value of 7.0 to the eggplant-shaped bottle, and continue to rotate in a water bath at 45°C under normal pr...

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PUM

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Abstract

The invention discloses a solid preparation of a bisoprolol / hydrochlorothiazide medicine composition liposome and a preparation method thereof. Active components of bisoprolol fumarat, hydrochlorothiazide and specified compositions of hydrogenated granulesten, dilauroyl phosphatidylcholine, cholesterol and tween 60 are prepared into the liposome. Stability, dissolution rate and biological utilization rate of a medicine are greatly improved, functions are stable and durable, and curative effects are remarkable. The solid preparation of the bisoprolol / hydrochlorothiazide medicine composition liposome improves product quality and reduces toxic and side effects.

Description

technical field [0001] The invention relates to a new solid preparation of a bisoprolol / hydrochlorothiazide pharmaceutical composition, in particular to a bisoprolol / hydrochlorothiazide liposome solid preparation and a preparation method thereof, belonging to the technical field of medicine. Background technique [0002] Bisoprolo, chemical name: 1-[4-[[2-(1-methylethoxy)-ethoxy]-methyl]-phenoxy]-3-[(1-methyl Ethyl) amino] -2-propanol, molecular formula C 18 h 31 NO 4 , molecular weight: 323.25, the structural formula is as follows: [0003] [0004] Bisoprolol is a new long-acting and highly selective β-adrenergic receptor blocker. It is an antihypertensive drug with better efficacy and is often administered in the form of fumarate. As the third-generation long-acting and highly selective β-adrenergic receptor blocker, bisoprolol has no intrinsic sympathomimetic activity and membrane stabilizing effect, and its affinity for β1 receptors is 100 times stronger than tha...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K31/549A61K31/138A61K47/28A61K9/127A61P9/12
Inventor 杨明贵
Owner HAINAN MEILAN SMITH KLINE PHARMA
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