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A drug nanoparticle delivery system

A nanoparticle and delivery system technology, applied in the field of drug nanoparticle delivery system, can solve the problems of drug instability, high melting point of active ingredients, incompatibility, etc., and achieve improved bioavailability, particle size reduction, and dissolution rate increased effect

Inactive Publication Date: 2017-10-20
新加坡纳诺泰克药物科技有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

A disadvantage of this method is that if the active ingredient has a high melting point, high temperatures are required in the extrusion barrel to achieve sufficient dispersion of the active ingredient, and therefore higher energy consumption
[0007] The solid dispersion technology of active ingredients also includes the following disadvantages: it is not easy to scale up the laboratory formula to industrial batch production; it is difficult to control the physical and chemical properties of the drug; it is difficult to make the solid dispersion into tablets or capsules; The drug produced is not resistant to high temperatures, so special handling and storage are required; this form of the drug is very unstable
The disadvantage of this method is that a large amount of emulsifier is required to form a stable emulsion due to the inherent incompatibility of the materials
Since the droplet size is determined by the system, this method cannot accurately control the particle size of the prepared drug
Moreover, the large use of emulsifiers can cause side effects, especially on the production process and formulation of the active ingredient
[0010] The common shortcoming of the existence of the above methods is exactly the problem of scaling up to industrialized production in the pharmaceutical industry

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0311] Embodiment 1---Preparation of Fenofibrate Nanoparticles

[0312] In this example, fenofibrate nanoparticles are produced by the process of the present invention and such as figure 2Prepared by the post-precipitation treatment process shown in 8a, including the process of precipitating fenofibrate nanoparticles from the precipitant solution and spray-drying the fenofibrate nanoparticles.

[0313] During the drug precipitation process, the solution containing fenofibrate and the anti-solvent form a suspension of fenofibrate nanoparticles and excipients in a micro-mixed environment.

[0314] The solution to be precipitated was prepared by dissolving 20 g of fenofibrate and 0.5 g of sodium lauryl sulfate (SLS) in 200 ml of ethanol at 40° C. The solution temperature was maintained at 35°C.

[0315] The anti-solvent solution was prepared by dissolving 76g of lactose and 2g of hydroxypropylmethylcellulose (HPMC)-E3, 1.5g of SLS in 2000ml of water at 25°C. The temperature o...

Embodiment 2

[0344] Embodiment 2: Preparation of Lopinavir Nanoparticles

[0345] In this example, the lopinavir nano-particle is made of process described in the present invention and figure 2 Prepared by the post-precipitation treatment process shown in 8a, which also includes the process of precipitating lopinavir nanoparticles and spray-drying lopinavir nanoparticles from the solution to be precipitated.

[0346] In the precipitation step, the lopinavir-containing solution and the anti-solvent are mixed under conditions of high shear and high gravity to form a suspension of lopinavir and excipients.

[0347] The solution to be precipitated is prepared by dissolving 20 g of lopinavir and 0.5 SLS in 200 ml of ethanol at 40° C. The solution was then cooled and maintained at 20°C.

[0348] The anti-solvent solution was prepared by dissolving 76g of lactose, 2g of hydroxypropylmethylcellulose (HPMC)-E3 and 1.5g of SLS in 2000ml of water at 25°C. The solution temperature was then maintai...

Embodiment 3

[0383] The preparation of embodiment 3-cefuroxim axetil (CFA)

[0384] In this example, CFA nanoparticles are produced by process of the present invention and such as figure 2 It is prepared by the post-precipitation treatment process shown in 8a, which also includes precipitating CFA nanoparticles from the solution to be precipitated, and then preparing the obtained CFA nanoparticles by spray drying.

[0385] In the precipitation step, under high shear force and high gravity conditions, the CFA solution is mixed with the antisolvent solution to obtain a cefuroxime axetil suspension containing excipients.

[0386] Take by weighing 20g of CFA raw material drug, 0.5g sodium lauryl sulfate (SLS) and dissolve in 100ml ethanol / acetone (proportioning is 1: 3) at 40 ℃, make cefuroxime axetil solution, wherein temperature is cooled gradually And keep it at about 20°C.

[0387] Weigh 76g of lactose, 4g of hydroxypropylmethylcellulose (HPMC)-E3 and 1.5g of SLS and dissolve them in 10...

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Abstract

The invention relates to a drug nanoparticle delivery system comprising skeleton particles formed from solidified auxiliary materials, and drug nanoparticles wrapped in the auxiliary materials and scattered in the skeleton particles independently. The particle size of the skeleton particles is 1-10 micrometers and the average particle size of the drug nanoparticles is 50-1000 nanometers. Compared with conventional preparations, the preparations provided by the invention have a higher dissolution rate and dissolution degree. The preparations have high bioavailability when being absorbed by human bodies and are suitable for oral administration of mammals.

Description

technical field [0001] The invention relates to a drug nanoparticle delivery system, which belongs to the field of drug preparation. This system is suitable for industrial mass production. Background technique [0002] Synthetic or natural medicines treat and prevent disease and can be given by injection or orally. Compared with other drug delivery methods, oral drug delivery is more popular, causing less pain to patients, and thus has higher patient compliance. Oral administration is also a more convenient and simpler way of administration than injection administration. [0003] Many important drugs in the treatment of diseases are usually poorly water soluble drugs. Because of the low bioavailability of poorly water-soluble drugs, scientists are constantly striving to develop new formulations of such drugs to improve their solubility in the human body. An ideal drug should have the highest possible bioavailability in the human body. However, due to incomplete absorpti...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/16A61K9/14A61K9/20B01J2/06B01J19/00
CPCA61K9/14A61K9/1623A61K9/1652A61K9/1694A61K9/2077B01J2/06B01J19/0093B01J2219/00788B01J2219/00889A61P1/00A61P3/10A61P7/02A61P7/04A61P9/08A61P9/12A61P11/14A61P17/00A61P23/00A61P23/02A61P25/06A61P25/08A61P25/16A61P25/18A61P25/20A61P25/24A61P29/00A61P31/04A61P31/10A61P31/12A61P33/00A61P33/02A61P35/00
Inventor 沈志刚甄崇礼胡俊尼塔尔·阿文德·朱嘉德张纪尧陈文浩王哲高凌燕威廉·格洛夫陈建峰
Owner 新加坡纳诺泰克药物科技有限公司
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