Crocetin solid dispersion and preparation method thereof

A technology of solid dispersion and crocetin, applied in medical preparations with non-active ingredients, medical preparations containing active ingredients, and pharmaceutical formulas, etc., can solve problems such as toxic side effects, aging, and affecting drug solubilization effects , to achieve the effects of increased solubility, improved stability, and increased bioavailability

Active Publication Date: 2021-06-22
HANGZHOU JIURUTANG BIOTECH
View PDF4 Cites 1 Cited by
  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Since the drug exists in a high-energy unstable form such as molecules or crystallites in the solid dispersion, the solid dispersion often faces the problem of "aging", that is, the degradation or precipitation of the drug in the solid dispersion not only affects the Solubilization effect, the degradation products of the drug may also cause toxic side effects

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
  • Crocetin solid dispersion and preparation method thereof
  • Crocetin solid dispersion and preparation method thereof
  • Crocetin solid dispersion and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1-6

[0048] table 5

[0049]

[0050] According to Table 5, the meglumine and the hydrophilic polymer carrier material in Examples 1-6 are dissolved in water and ultrasonicated for 1 h, so that the hydrophilic polymer material and meglumine are dissolved and cross-linked to form a carrier polymer I: Add crocetin to the system containing the carrier polymer I, and dissolve the crocetin by ultrasonication or stirring. The solvent is removed by rotary evaporation or spray drying to obtain a solid dispersion of crocetin, which is passed through a 100-mesh sieve. With pH 6.8 phosphate buffer as the dissolution medium, the volume of the dissolution medium is 900mL, and the rotation speed is 75rpm. The dissolution test is carried out by the paddle method, the dissolution results are determined by high performance liquid chromatography, and the cumulative dissolution rate is calculated.

[0051] Table 6

[0052]

[0053]

[0054] According to the dissolution rate obtained in Tab...

Embodiment 7

[0056] Crocetin solid dispersion, comprises the composition of following weight ratio:

[0057] Crocetin 10g

[0058] Soluplus 10g

[0059] Meglumine 40g

[0060] The preparation process is as follows:

[0061] (1) Soluplus and meglumine were dissolved in 500 mL of 95% ethanol solution and ultrasonicated for 1 h to obtain carrier polymer I.

[0062] (2) Adding crocetin to the solution system containing the carrier polymer I obtained in step (1), and ultrasonically dissolving the crocetin.

[0063] (3) Use a rotary evaporator to evaporate the solvent from the solution obtained in step (2), dry it under reduced pressure at 60° C. for 12 hours, collect the solid, pulverize it and pass it through a 100-mesh sieve to obtain the crocetin solid dispersion.

Embodiment 8

[0065] Crocetin solid dispersion, comprises the composition of following weight ratio:

[0066] Crocetin 10g

[0067] Soluplus 20g

[0068] Meglumine 40g

[0069] The preparation process is as follows:

[0070] Step 1) Soluplus and meglumine were dissolved in 500 mL of purified water, and stirred at 300 rpm for 1 h to obtain carrier polymer I.

[0071] Step 2) adding crocetin to the solution system containing carrier polymer I obtained in step 1), and stirring to dissolve the crocetin.

[0072] Step 3) Use the spray drying method to remove moisture from the solution obtained in step 2), the inlet air temperature is 135°C, the outlet air temperature is 60°C, and the air volume is 0.8m 3 / min, the atomization pressure is 8kPa, and the flow rate is 1.5mL / min. During the spray drying process, the temperature of the mixed solution containing the drug is kept at 70°C.

[0073] Step 4) The spray-dried product was dried under reduced pressure at 60° C. for 12 hours, the solid was...

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 provides a crocetin solid dispersion and a preparation method thereof. The formula of the crocetin solid dispersion is as follows: 1 part of an insoluble drug crocetin, 1-15 parts of a hydrophilic polymer carrier material and 1-12 parts of a solubilizer meglumine. The preparation method of the solid dispersion comprises the following steps: dissolving the hydrophilic polymer carrier material and the meglumine in an organic reagent or water, carrying out ultrasonic treatment or stirring to enable the hydrophilic polymer material and the meglumine to be crosslinked to form a carrier polymer I, adding the crocetin into a solution containing the carrier polymer I, carrying out ultrasonic treatment or stirring to to dissolve the crocetin, and adopting a solvent evaporation method or a spray drying method to obtain the solid dispersion. The crocetin solid dispersion prepared by the method has good solubility and stability, can be quickly absorbed in vivo, has high bioavailability, is simple in preparation process, and is suitable for industrial production.

Description

technical field [0001] The invention belongs to the field of pharmacy and relates to a solid dispersion and a preparation method thereof, in particular to a crocetin solid dispersion and a preparation method thereof. Background technique [0002] Saffron is the dry stigma of Crocus sativus L., a plant of the family Iridaceae, which is recorded in the 2020 edition of the Chinese Pharmacopoeia. Saffron is sweet in taste and flat in nature, with heart-guiding and liver meridians, has the effects of promoting blood circulation and removing blood stasis, cooling blood and detoxification, relieving stagnation and calming the nerves. "Compendium of Materia Medica" is recorded in the Ministry of Cao, named saffron, also known as Xiaofulan, and withdrawing method, it is mainly used to treat depression and depression, lingering breath, promoting blood circulation, and also controlling palpitations. Historically, my country has been importing from Western countries, so it is called sa...

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): A61K9/14A61K47/34A61K47/18A61K31/202A61P35/00A61P25/00A61P9/00A61P1/16A61P25/24A61P17/02A61P3/06A61P11/06A61P25/28A61P3/10A61P1/00A61P9/10A61P27/02A61P39/06A61P29/00
CPCA61K9/146A61K31/202A61P35/00A61P25/00A61P9/00A61P1/16A61P25/24A61P17/02A61P3/06A61P11/06A61P25/28A61P3/10A61P1/00A61P9/10A61P27/02A61P39/06A61P29/00Y02A50/30
Inventor 王平徐子金林素素李桥桥江山山尤雅姜玉丽朱琳钟情柔
Owner HANGZHOU JIURUTANG BIOTECH
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
Try Eureka
PatSnap group products

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

© 2024 PatSnap. All rights reserved.Legal|Privacy policy|Modern Slavery Act Transparency Statement|Sitemap