Eureka AIR delivers breakthrough ideas for toughest innovation challenges, trusted by R&D personnel around the world.

Huperzine-A framework particles, orally disintegrating tablets and preparation methods thereof

A technology for huperzine A and orally disintegrating tablets, which is applied to pharmaceutical formulas, medical preparations containing no active ingredients, medical preparations containing active ingredients, etc., and can solve problems such as difficulty swallowing, poor patient compliance, and uneven content , to achieve the effect of stable process, good reproducibility and simple operation

Active Publication Date: 2017-03-22
SUN YAT SEN UNIV
View PDF12 Cites 6 Cited by
  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0006] Huperzine A is a low-dose, high-efficiency drug. The commercially available oral preparations are only ordinary tablets and capsules (50 μg / tablet / grain). Both of these two preparations have to be taken multiple times a day, have difficulty swallowing and poor patient compliance.
In addition, due to the extremely low dosage of the drug, single unit preparations produced by traditional methods, such as Chinese patent applications CN200710093156.9, CN200910174864.4, CN201410657374.0, 201110454189.8, are prone to the problem of uneven content

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
  • Huperzine-A framework particles, orally disintegrating tablets and preparation methods thereof
  • Huperzine-A framework particles, orally disintegrating tablets and preparation methods thereof
  • Huperzine-A framework particles, orally disintegrating tablets and preparation methods thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0052] The theoretical drug loading capacity of the fixed huperzine A matrix particles is 0.2% (w / v). Take by weighing an appropriate amount of huperzine A, be dissolved in 200ml 80% v / v ethanol solution, obtain drug solution, slowly add a certain amount of skeleton material (ethyl cellulose EC (EC7 / EC10 / EC20 / EC45), acrylic resin Eudragit RSPO or vinyl acetate-povidone blend Kollidon SR), to form a drug-containing polymer solution with a concentration of 5% to 20% (w / v) of the skeleton material . The drug-containing polymer solution is fed into the UPPS at an average speed of 7.8ml / min through a peristaltic pump, and is sheared and atomized under the action of a high-speed rotating disc (9000rpm) to form droplets. The solvent in the droplets is in the airflow field The huperzine A skeleton microparticles are obtained by evaporating in medium, solidifying the microdroplets, and finally collecting the huperzine A skeleton microparticles. The yield and formability of huperzine...

Embodiment 2

[0057] Weigh 20mg of huperzine A, dissolve in 200ml 80% v / v ethanol solution to obtain a drug solution, slowly add 10g of skeleton materials EC10, EC20 and EC45 to the drug solution under the action of magnetic stirring, until the swelling of EC is completely formed Uniform drug-containing polymer solution. The drug-containing polymer solution is fed into the UPPS at an average speed of 7.8ml / min through a peristaltic pump, and micro-droplets are formed under the action of a 9000rpm high-speed rotating disc. Huperzine A skeleton microparticles were obtained. The prepared huperzine A matrix particles were stored in a desiccator for subsequent research.

[0058] The assay method of drug content in the huperzine A skeleton particle (being the assay method of drug encapsulation efficiency) is: accurately weigh 10~10.5mg huperzine A skeleton particle and place in 5ml volumetric flask, add 80% methanol ultrasonic to After the particle skeleton is completely dissolved, adjust to vo...

Embodiment 3

[0065] Take by weighing 21 mg of Huperzine A, dissolve in 200ml 80% v / v ethanol solution to obtain a drug solution, slowly add 10 g of framework material EC45 and additives of the type and dosage shown in Table 3 to the drug solution under the action of magnetic stirring until the skeleton material swells completely to form a uniform drug-containing polymer solution. The drug-containing polymer solution is fed into the UPPS high-speed rotating disc (9000rpm) through a peristaltic pump at an average speed of 7.8ml / min to form microdroplets, and then the solvent in the microdroplets is evaporated in the air field to further solidify into huperzine A skeleton particle. The encapsulation efficiency and release curve of the huperzine A matrix microparticles are carried out according to Example 2. The effects of various additives and their dosage on the encapsulation efficiency and drug release of huperzine A matrix particles are as follows: image 3 and Figure 4 shown. The res...

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

No PUM Login to View More

Abstract

The invention relates to huperzine-A framework particles, orally disintegrating tablets and preparation methods thereof. The huperzine-A framework particles are prepared by an ultrafine particle preparation system (UPPS) and through taking huperzine-A, a framework material and an ethanol aqueous solution as raw materials, wherein the mass ratio of the huperzine-A to the framework material is (0.01 to 2): 100; the framework material is ethyecellulose or a mixture of ethyecellulose and an additive with a mass ratio of (2 to 40): 1; and the additive is selected from at least one of triethyl citrate, polyethylene glycol, hydroxypropyl methyl cellulose and povidone. The huperzine-A framework particles disclosed by the invention are high in medicine entrapment efficiency, high in formability and compact in structure, have obvious rough surfaces, and are high in mixing uniformity thereamong, high in compressibility and good in sustained-release effect. The orally disintegrating tablets disclosed by the invention are high in medicine uniformity, and keep the medicine release behaviour of the huperzine-A framework particles before tabletting.

Description

technical field [0001] The invention relates to the technical field of pharmaceutical preparations, in particular to a huperzine A skeleton particle, an orally disintegrating tablet and a preparation method thereof. Background technique [0002] Multi-unit preparations, also known as dose-dispersed preparations, refer to a complete dosage composed of a group of subunits with similar or identical structures. Compared with single-unit preparations, multi-unit preparations have the advantages of reducing gastrointestinal tract irritation, improving bioavailability and clinical drug safety, but their disadvantages are that the dosage cannot be divided and the dosage cannot be flexibly adjusted to meet clinical needs. In order to combine the advantages of multi-unit and single-unit preparations, the currently reported method is to make the drug and drug-loaded matrix into microparticles, such as pellets, microspheres, and matrix particles, and then compress the microparticles and...

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
IPC IPC(8): A61K31/4748A61K47/38A61K9/22A61P25/28
CPCA61K47/38A61K9/0002A61K9/0056A61K9/2059A61K31/4748
Inventor 潘昕彭婷婷杨佩佩朱春娥吴传斌
Owner SUN YAT SEN UNIV
Who we serve
  • R&D Engineer
  • R&D Manager
  • IP Professional
Why Eureka
  • Industry Leading Data Capabilities
  • Powerful AI technology
  • Patent DNA Extraction
Social media
Eureka Blog
Learn More
PatSnap group products

Browse by: Latest US Patents, China's latest patents, Technical Efficacy Thesaurus, Application Domain, Technology Topic, Popular Technical Reports.

© 2024 PatSnap. All rights reserved.Legal|Privacy policy|Modern Slavery Act Transparency Statement|Sitemap|About US| Contact US: help@patsnap.com