Probucol orally administered nanometer solid preparation and preparation method for same

Abstract

The invention provides a probucol orally administered nanometer solid preparation, which comprises, by weight, 1 part of probucol, 0.01-0.1 part of additive and 0.05-0.4 part of auxiliary materials. The grain size of the probucol ranges from 10nm to 200nm. The invention further provides a preparation method for the probucol orally administered nanometer solid preparation. The preparation method includes that the probucol and water liquor with 5% of additive are prepared into nanometer suspension with the grain size ranging from 100nm to 600nm by a wet grinding method; the nanometer suspension is homogenized into nanometer grains with the grain sizes ranging from 10nm to 200nm by a high-pressure homogenizing machine; and the nanometer suspension which is homogenized is solidified and is added with the auxiliary materials to be prepared into the orally administered nanometer solid preparation. Compared with a common probucol tablet, the preparation has the advantages that dissolution in vitro of the preparation is increased by 20-30 times, and bioavailability after oral administration is improved by 10-20 times. In addition, the drug loading rate of the preparation is high, and the preparation can meet the requirements of tablet weight clinically needed by high-dose probucol administration. Besides, the preparation is stable, and the dissolution of the preparation can be kept unchanged within two years.

Description

technical field

[0001] The invention relates to the technical field of medical engineering, in particular to a probucol oral nano solid preparation and a preparation method thereof. Background technique

[0002] Probucol, also known as probucol, is the first blood lipid-lowering drug listed in the United States in 1977. Because it lowers high-density lipoprotein cholesterol (HDL) while lowering cholesterol, it fades out of the market. After twenty years of clinical research, it was found that although probucol lowered HDL, not only did atherosclerosis not aggravate, on the contrary probucol showed a strong anti-atherosclerosis effect. In addition, probucol also has powerful anti-oxidation, anti-aging, and treatment of restenosis after angioplasty. Therefore, probucol has once again been valued clinically.

[0003] The main pharmacological effects of probucol include reducing cholesterol synthesis and promoting cholesterol decomposition, changing the properties and functio...

Examples

Embodiment Construction

[0027] Sample Preparation

[0028] (1) Instrument

[0029] Particle size analyzer: Malvern nano zs90 particle size analyzer in the United States

[0030] Nano mill: PUHLER Super MicroCer TM Universal Bead Mill Germany

[0031] High pressure homogenizer: Microfluidics M-110EH USA

[0032] (2) Operation method

[0033] Prepare the probucol oral nanometer solid preparation of embodiment 1 to embodiment 6 by the prescription of table 1 and preparation process parameter:

[0034] Take a certain amount of probucol and disperse it in the aqueous solution containing 5% additive (ie 5g additive / 100ml water). The aqueous solution dispersed with probucol and additives is placed in a nanomill and ground to prepare each nanosuspension with an average particle size as shown in Table 1, wherein the grinding material is a polystyrene resin coated with a high degree of crosslinking. Ball (particle size is as shown in table 1), the rotating speed of nano mill is 5000 revolutions per min...

technical field

[0001] The invention relates to the technical field of medical engineering, in particular to a probucol oral nano solid preparation and a preparation method thereof. Background technique

[0002] Probucol, also known as probucol, is the first blood lipid-lowering drug listed in the United States in 1977. Because it lowers high-density lipoprotein cholesterol (HDL) while lowering cholesterol, it fades out of the market. After twenty years of clinical research, it was found that although probucol lowered HDL, not only did atherosclerosis not aggravate, on the contrary probucol showed a strong anti-atherosclerosis effect. In addition, probucol also has powerful anti-oxidation, anti-aging, and treatment of restenosis after angioplasty. Therefore, probucol has once again been valued clinically.

[0003] The main pharmacological effects of probucol include reducing cholesterol synthesis and promoting cholesterol decomposition, changing the properties and functio...

Examples

Embodiment Construction

[0027] Sample Preparation

[0028] (1) Instrument

[0029] Particle size analyzer: Malvern nano zs90 particle size analyzer in the United States

[0030] Nano mill: PUHLER Super MicroCer TM Universal Bead Mill Germany

[0031] High pressure homogenizer: Microfluidics M-110EH USA

[0032] (2) Operation method

[0033] Prepare the probucol oral nanometer solid preparation of embodiment 1 to embodiment 6 by the prescription of table 1 and preparation process parameter:

[0034] Take a certain amount of probucol and disperse it in the aqueous solution containing 5% additive (ie 5g additive / 100ml water). The aqueous solution dispersed with probucol and additives is placed in a nanomill and ground to prepare each nanosuspension with an average particle size as shown in Table 1, wherein the grinding material is a polystyrene resin coated with a high degree of crosslinking. Ball (particle size is as shown in table 1), the rotating speed of nano mill is 5000 revolutions per min...

Images