Indissolvable drug nanosuspension and preparation method thereof

A technology of insoluble drugs and nano-suspensions, which is applied in the field of medicine and can solve problems such as adverse effects on the human body and the environment

Active Publication Date: 2021-07-06
HUBEI UNIV OF CHINESE MEDICINE
View PDF9 Cites 2 Cited by
  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0006] The purpose of the present invention is to overcome the problem of adverse effects on the human body and the environment caused by organic solvent residues in the process of preparing nano-suspensions by the existing solvent-anti-solvent method in the prior art, and to provide a nano-suspension of insoluble drugs. Suspension and preparation method thereof, the method provides a non-toxic, thermally stable, recyclable and cheap and easy-to-get green solvent to replace traditional organic solvents to prepare nano-suspensions, and is also an environmentally friendly Preparation method of friendly nanosuspension

Method used

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
View more

Image

Smart Image Click on the blue labels to locate them in the text.
Viewing Examples
Smart Image
  • Indissolvable drug nanosuspension and preparation method thereof
  • Indissolvable drug nanosuspension and preparation method thereof
  • Indissolvable drug nanosuspension and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0061] Preparation of Apigenin Nanosuspension

[0062] Get the apigenin crude drug of 1.6g in the macrogol 400 (PEG-400) of 20ml, ultrasonic bath makes it dissolve completely; Get 160mg sodium dodecyl sulfate (SDS) and 320mg polyvinylpyrrolidone K30 ( PVP-K30) as a stabilizer, dissolved in 160ml pure water to fully swell. Under the condition of continuous stirring, add the apigenin-PEG400 solution into the water containing the stabilizer through the peristaltic pump, the injection speed is 20ml / min, the stirring speed is 420r / min, after the solution is added dropwise, continue to stir and shear for 15min to obtain Apigenin nanosuspension.

Embodiment 2

[0064] Preparation of ibuprofen nanosuspension

[0065] Get the ibuprofen crude drug of 4g in the Polyethylene Glycol 600 (PEG-600) of 20ml, ultrasonic bath makes it dissolve completely; Get 200mg sodium dodecyl sulfate (SDS) and 400mg polyvinylpyrrolidone K30 ( PVP-K30) as a stabilizer, dissolved in 200ml pure water to fully swell. Under the condition of continuous stirring, add the ibuprofen-PEG600 solution into the water containing the stabilizer through the peristaltic pump, the injection speed is 20ml / min, the stirring speed is 800r / min, after the solution is added dropwise, continue to stir and shear for 10min Get ibuprofen nanosuspension.

Embodiment 3

[0067] Preparation of Perampanel Nanosuspension

[0068] Get 0.08g of perampanel crude drug in 20ml of polyethylene glycol 300 (PEG-300), and ultrasonically dissolve it completely in a boiling water bath; another 160mg of sodium dodecyl sulfate (SDS) and 320mg of polyvinylpyrrolidone K30 (PVP-K30) as a stabilizer, dissolved in 160ml of pure water to fully swell. Under the condition of continuous stirring, add the perampanel-PEG300 solution into the water containing the stabilizer through the peristaltic pump, the injection speed is 40ml / min, the stirring speed is 420r / min, after the solution is added dropwise, continue to stir and shear The perampanel nanosuspension was obtained in 20 minutes.

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
Login to View More

PUM

PropertyMeasurementUnit
particle diameteraaaaaaaaaa
particle diameteraaaaaaaaaa
refractive indexaaaaaaaaaa
Login to View More

Abstract

The invention relates to the technical field of medicines, in particular to an indissolvable drug nanosuspension and a preparation method thereof. The method includes the steps of (1) dissolving an indissolvable drug in a latent solvent to obtain a drug-latent solvent solution; (2) dissolving a stabilizer in water to obtain an aqueous solution containing the stabilizer; (3) adding the drug-latent solvent solution obtained in the step (1) into the stabilizer-containing aqueous solution obtained in the step (2) under stirring, and after the addition is completed, continuously conducting stirring and shearing to obtain the indissolvable drug nanosuspension. The volume ratio of the latent solvent to the water is 1:(2-10); and the stabilizer is a mixture of a charge stabilizer and a three-dimensional stabilizer. According to the indissolvable drug nanosuspension and the preparation method thereof, the particle size of the nanosuspension prepared according to the method is in the range of 200-350 nm, the nanosuspension has excellent stability, and the dissolution speed and the degree of the nanosuspension are obviously improved compared with the dissolution speed and the degree of bulk drugs.

Description

technical field [0001] The invention relates to the technical field of medicine, in particular to an insoluble drug nano-suspension and a preparation method thereof. Background technique [0002] In recent years, with the widespread application of combinatorial chemistry and high-throughput screening techniques in drug development, many compounds with large molecular weight and complex structures have emerged. According to statistics, 40% of the drugs on sale in the world are insoluble drugs, while 90% of the drugs are under research. Due to the extremely low solubility of these drugs in water, their dissolution in the gastrointestinal tract is poor, and their oral bioavailability is low, which limits the development and clinical use of pharmaceutical preparations. [0003] Nanosuspension is a new type of nano drug delivery system developed for insoluble drugs in recent years. It belongs to submicron colloidal dispersion system, which can be used for both insoluble drugs in...

Claims

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
Login to View More

Application Information

Patent Timeline
no application Login to View More
Patent Type & AuthorityApplications(China)
IPC IPC(8): A61K9/10A61K45/00A61K47/10A61K47/32A61K47/20A61K31/55A61K31/352A61K31/192A61K31/444A61K31/137A61K31/58A61K31/56A61K31/573
CPCA61K9/10A61K45/00A61K47/10A61K47/32A61K47/20A61K31/55A61K31/352A61K31/192A61K31/444A61K31/137A61K31/58A61K31/56A61K31/573
Inventor卢山周丽景许仁杰
OwnerHUBEI UNIV OF CHINESE MEDICINE