Triopisetron Hydrochloride microcapsule and method for preparing injection

A technology for tropisetron hydrochloride and injection, which is applied in capsule delivery, pharmaceutical formulations, medical preparations of non-active ingredients, etc. It can solve the problems of poor clarity, hydrolysis and separation of tropisetron hydrochloride, etc., and achieve slow release , Improve bioavailability, improve the effect of stability

Inactive Publication Date: 2008-10-08
HAINAN LINGKANG PHARMA CO LTD
View PDF0 Cites 7 Cited by
  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

When the freeze-dried preparation is used, water should be used as the solvent, which will also cause tr

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
  • Triopisetron Hydrochloride microcapsule and method for preparing injection
  • Triopisetron Hydrochloride microcapsule and method for preparing injection

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0061] Tropisetron Hydrochloride 2g

[0062] Gelatin 6g

[0063] Dextran 5g

[0064] Soy Lecithin 1.1g

[0065] Tween 80 1.5g

[0066] Mannitol 50g

[0067] Preparation Process

[0068] (1) 2g tropisetron hydrochloride is added in the water for injection, dissolves completely;

[0069] (2) Add 6g gelatin and 1.1g soybean lecithin to the solution obtained in step (1), prepare water-in-oil emulsion with mechanical stirring;

[0070] (3) Add 200ml of 2.5% dextran solution and 1.5g Tween 80 to the emulsion obtained in step (2), and prepare a water-in-oil-in-water multiple emulsion by mechanical stirring;

[0071] (4) The multiple emulsion obtained in step (3) is dripped into the 2mol / L sodium hydroxide solidified liquid in the high-voltage electrostatic field by an orifice injection, the electric field voltage is 2.2kv, and the injection speed is 15ml / min, after solidifying for 20min Filter out the microcapsules, inject the double emulsion, and then stir the strong alkali c...

Embodiment 2

[0074] Tropisetron Hydrochloride 5g

[0075] Gelatin 20g

[0076] Dextran 8g

[0077] Egg yolk lecithin 6.1g

[0078] Poloxamer 188 7.0g

[0079] Glucose 300g

[0080] The preparation process is the same as in Example 1, and tropisetron hydrochloride freeze-dried powder injection is obtained.

Embodiment 3

[0082] Tropisetron Hydrochloride 3g

[0083] Gelatin 10g

[0084] Dextran 5g

[0085] Cholesterol 2.7g

[0086] Poloxamer 188 3.6g

[0087] Glucose 120g

[0088] The preparation process is the same as in Example 1, and tropisetron hydrochloride freeze-dried powder injection is obtained.

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 sizeaaaaaaaaaa
Login to view more

Abstract

The invention provides a tropisetron hydrochloride freeze-dry preparation for treating emesis, containing tropisetron hydrochloride, gelatin, dextran, oleophilic emulsifier, hydrophilic emulsifier and freeze-dry supporting agent. The invention also relates to a preparation method of the tropisetron hydrochloride freeze-dry preparation, containing the following steps: (1) the tropisetron hydrochloride is added into injection water and completely dissolved; (2) the gelatin and the oleophilic emulsifier are added in solution prepared in step (1) to prepare water-in-oil emulsion; (3) dextran solution and the hydrophilic emulsifier are added in the solution prepared in step (2) to prepare water-in-oil-in-water double emulsion; (4) the prepared double emulsion is dropped by bolus injection into strong base solidified liquor in a high-voltage electrostatic field by an orifice; after solidifying, a microcapsule is filtered and washed by water or PH regulator to lead PH to be 5-7; (5) the freeze-dry supporting agent is dissolved in the injection water and mixed with the microcapsule evenly; after subpackage and freeze drying, the tropisetron hydrochloride freeze-dry preparation is obtained.

Description

technical field [0001] The invention provides a tropisetron hydrochloride microcapsule for injection, and also provides a tropisetron hydrochloride freeze-dried powder injection and a preparation method thereof. It belongs to the field of medicine. Background technique [0002] Tropisetron hydrochloride is a potent and highly selective competitive antagonist of peripheral neurons and central nervous system 5-hydroxytryptamine 3 (5-HT3) receptors. Stimulation by surgery or certain substances, including some chemotherapy drugs, can stimulate the chromaffin-like cells of the visceral mucosa to release 5-HT, thereby inducing the vomiting reflex with nausea. This product mainly inhibits the vomiting reflex by selectively blocking the presynaptic 5-HT3 receptors of peripheral neurons. In addition, its antiemetic effect may also inhibit the area postrema by directly blocking the central 5-HT3 receptors. Stimulation of the vagus nerve. [0003] Tropisetron hydrochloride is unstab...

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): A61K9/48A61K9/19A61K31/46A61K47/36A61P1/08
Inventor 邱民
Owner HAINAN LINGKANG PHARMA CO LTD
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