Slow release microsphere preparation of derivative of 3,3 ¿C diphenyl propylamine as receptor antagon of toadstool alkali in use for injection

A technology of diphenylpropylamine derivative and sustained-release microsphere preparation, applied in 3 as a muscarinic receptor antagonist, can solve problems such as increased treatment cost, inability to long-act sustained release, and low bioavailability

Inactive Publication Date: 2006-07-05
长春健欣生物医药科技开发有限公司
View PDF4 Cites 1 Cited by
  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

US6517864 has reported the 24-hour transdermal formulation of tolterodine and (R)-N, N-diisopropyl-3-(2-hydroxyl-5-hydroxymethylphenyl)-3-phenylpropylamine, although This dosage form can release drug at a relatively stable speed, but because the bioavailability is very low (<20%), it causes the improvement of its treatment cost, and it cannot be sustained-release for a long time, so it still needs to be developed as a muscarinic receptor antagonist New Injectable Long-acting Sustained-release Dosage Form of 3,3-Diphenylpropylamine Derivatives

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
  • Slow release microsphere preparation of derivative of 3,3 ¿C diphenyl propylamine as receptor antagon of toadstool alkali in use for injection
  • Slow release microsphere preparation of derivative of 3,3 ¿C diphenyl propylamine as receptor antagon of toadstool alkali in use for injection
  • Slow release microsphere preparation of derivative of 3,3 ¿C diphenyl propylamine as receptor antagon of toadstool alkali in use for injection

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0061] 0.6g (R)-N, N-diisopropyl-3-(2-hydroxyl-5-hydroxymethylphenyl)-3-phenylpropylamine (compound Ia), 9.4g polylactide-glycolide Ester (lactide: glycolide = 50:50, molecular weight 25,000) was dissolved in 50ml of dichloromethane, under vigorous stirring (1200-1600rpm), it was dripped into 2500ml of 0.5% PVA aqueous solution, and continued to vigorously Stir for 3-10 minutes, then reduce the stirring speed to 300 rpm, evaporate the solvent for 4-6 hours, filter, wash the microspheres with distilled water three times, and freeze-dry. The particle size is 1-200 μm, the drug content is 3.8%, and the embedding rate is 63%.

[0062] The slow-release microspheres were tested for in vivo release in rabbits. The dose is 10 mg / kg, the microspheres are suspended in normal saline for injection, and intramuscularly administered. Within 1 to 20 days, blood is collected for HPLC-MS detection, and the blood drug concentration is 1-20 ng / ml. It is proved that the sustained-release micros...

Embodiment 2

[0064] Weigh (R)-N, N-diisopropyl-3-(2-hydroxyl-5-hydroxymethylphenyl)-3-phenylpropylamine (compound Ia) 0.5g, polylactide-glycolide (lactide:glycolide=50:50, molecular weight 13000) 9.5g, prepared by the method of Example 1, containing 4.7% of the drug microspheres with a particle size of 1-200 μm, the embedding rate was 94%.

Embodiment 3

[0066] Weigh (R)-N, N-diisopropyl-3-(2-hydroxyl-5-hydroxymethylphenyl)-3-phenylpropylamine (compound Ia) 1.0g, polylactide-glycolide (Lactide:glycolide=50:50, molecular weight 35000) 9.0g, prepared by the method of Example 1 containing 6.5% drug, microspheres with a particle size of 1-200 μm, the embedding rate was 65%.

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
molecular weightaaaaaaaaaa
molecular weightaaaaaaaaaa
particle diameteraaaaaaaaaa
Login to view more

Abstract

A slowly-releasing microspherical medicine used for the injection to treat the diseases associated with the antagon of muscarinic receptor, the impulsive inoontinence and urination urgency or frequency is prepared from 3,3-diphenyl propylamine derivative, its optical enantiomer or cacemer, and the biodegradable medical high-molecular auxiliary. Its preparing process is also disclosed.

Description

technical field [0001] The present invention relates to a sustained-release microsphere preparation for injection of 3,3-diphenylpropylamine derivatives and a preparation method thereof. The present invention also relates to the preparation of said preparation for the treatment or auxiliary treatment of diseases related to muscarinic receptors and Use of medications for unstable or overactive bladder including urge incontinence, urinary urgency, or frequency. Background technique [0002] [0003] It is reported that (R)-N,N-diisopropyl-3-(2-hydroxy-5-hydroxymethylphenyl)-3-phenylpropylamine (Ia) and (R)-N,N-di Isopropyl-3-(2-hydroxy-5-methylphenyl)-3-phenylpropylamine (tolterodine) (II) is a muscarinic receptor antagonist (EP0325571; WO94 / 11337), which It can be used to treat unstable or overactive bladder including impulse incontinence, urgency or frequency. By modifying their structures, it is found that some of their derivatives or prodrugs have similar effects (EP0...

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 & Authority Applications(China)
IPC IPC(8): A61K31/137A61K9/16A61P13/00A61P13/10
CPCA61K9/0019A61K31/135A61K9/16A61P11/04A61P13/00A61P13/10
Inventor 李又欣
Owner 长春健欣生物医药科技开发有限公司
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