Nanometer preparation and preparation method thereof

A technology of nanosuspension and solid preparation, which can be applied in the directions of pill delivery, pharmaceutical formulations, and medical preparations of inactive ingredients, etc., and can solve problems such as large individual differences.

Inactive Publication Date: 2011-11-09
TIANJIN INSTITUTE OF PHARMA RESEARCH
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Probucol is poorly soluble in water, and its oral bioava

Method used

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  • Nanometer preparation and preparation method thereof
  • Nanometer preparation and preparation method thereof
  • Nanometer preparation and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0072] The nanosuspension of present embodiment 1 contains following composition by weight percentage:

[0073] Probucol 9%

[0074] Glycerin 0.9%

[0075] Poloxamer 188 0.3%

[0076] pvp K30 0.9%

[0077] Water 88.9%

[0078] Preparation method: mix and grind probucol and glycerin; mix poloxamer 188, PVP K30 Dissolve in an appropriate amount of water, add to the above mixture, add the remaining amount of water, mix evenly, and use a high-speed dispersing homogenizer at 12000r.min -1 High-speed shear pre-emulsification for 5 minutes under high-speed conditions; then the resulting suspension was circulated with a high-pressure homogenizer at a pressure of 1500 bar for 5 cycles.

[0079] The nanosuspension solid particles of the present embodiment 1 contain the following components by weight percentage:

[0080] Probucol Nanosuspension 84%

[0081] Lactose 12%

[0082] 5% PVP by weight K30 Aqueous solution 4%

[0083] Preparation method: preheat the fl...

Embodiment 2

[0099] The nanosuspension of present embodiment 2 contains following composition by weight percentage:

[0100] Probucol 30%

[0101] Propylene Glycol 9%

[0102] Lecithin 5%

[0103] Glyceryl Behenate 5%

[0104] Water 51%

[0105] Preparation method: mix and grind probucol and propylene glycol; dissolve lecithin and glyceryl behenate in water, add to the above mixture, add the remaining amount of water, mix evenly, and use a high-speed dispersing homogenizer at 12000r. min -1 High-speed shear pre-emulsification for 5 minutes under high-speed conditions; then the resulting suspension was circulated with a high-pressure homogenizer at a pressure of 1000 bar for 6 cycles.

[0106] The nanosuspension solid particle of present embodiment 2 contains following composition by weight percentage:

[0107] Probucol Nanosuspension 50%

[0108] Glucose 21%

[0109] Sucrose 10%

[0110] Starch 10%

[0111] 3% PVP by weight K30 Aqueous solution 9%

[0112] Preparation method: p...

Embodiment 3

[0128] The nanosuspension of present embodiment 3 contains following composition by weight percentage:

[0129] Silybin 3%

[0130] Glycerin 0.1%

[0131] Poloxamer 188 0.1%

[0132] pvp K30 0.3%

[0133] Water 96.5%

[0134] Preparation method: mix and grind silybin and glycerin; mix poloxamer 188, PVP K30 Dissolve in water, add to the above mixture, add the remaining amount of water, mix evenly, use a high-speed dispersing homogenizer at 12000r.min -1 High-speed shear pre-emulsification for 5 minutes under high-speed conditions; then the resulting suspension was circulated with a high-pressure homogenizer at a pressure of 1500 bar for 5 cycles.

[0135] The nanosuspension solid particle of present embodiment 3 contains following composition by weight percentage:

[0136] Silibinin Nanosuspension 90%

[0137] Mannitol 5%

[0138] 3% PVP by weight K30 Aqueous solution 5%

[0139] Preparation method: preheat the fluidized bed at 40°C for half an...

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Abstract

The invention provides a nanometer suspension of a difficult-soluble drug and a granulated preparation thereof; the preparation is prepared by the following steps: preparing a nanometer suspension by a high-speed shearing and high-pressure homogenization method, and further preparing solidified granules by the nanometer suspension through a fluidized bed or a spray-drying method, wherein the granules can be further prepared into tablets or capsules. The invention also discloses a preparation method.

Description

technical field [0001] The present invention relates to the field of pharmaceutical preparations, in particular, the present invention relates to a nanosuspension of insoluble drugs and its granulated preparation and its preparation method. The preparation adopts high-speed shearing and high-pressure homogenization to prepare nanosuspension , and then the nano-suspension is further prepared into solidified granules by fluidized bed or spray drying method, and the granules can be further prepared into tablets or capsules. The preparation process does not need organic solvents such as ethanol, which reduces production costs and avoids environmental pollution. technical background [0002] At present, more than 40% of the drugs under research have the problem of poor water solubility, which prevents potential good varieties from being marketed or cannot fully exert their curative effect. Therefore, it is very urgent to solve the problem of low bioavailability of insoluble drug...

Claims

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Application Information

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IPC IPC(8): A61K9/48A61K9/16A61K9/20A61K47/34A61K47/32A61K47/36A61K47/38A61K31/10A61K31/357A61K31/496A61K31/64A61K31/4745
Inventor 王成港靳文仙阎卉李桂龙王春龙吕守磊
Owner TIANJIN INSTITUTE OF PHARMA RESEARCH
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