Tapentadol pharmaceutical composition for transdermal administration as well as preparation method and application of pharmaceutical composition

A transdermal drug delivery technology for tapentadol, which is applied in the field of pharmaceutical preparations and can solve problems such as poor compliance, complicated preparation process of sustained-release pellets, and inconvenient medication for patients

Active Publication Date: 2020-06-30
YICHANG HUMANWELL PHARMA
View PDF5 Cites 2 Cited by
  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0005] Chinese patent CN104434881A discloses tapentadol hydrochloride sustained-release pellets comprising an enteric-coated layer and an isolation layer, wherein the enteric-coated layer is wrapped on the outside of the isolation layer, but the preparation process of the s

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
  • Tapentadol pharmaceutical composition for transdermal administration as well as preparation method and application of pharmaceutical composition
  • Tapentadol pharmaceutical composition for transdermal administration as well as preparation method and application of pharmaceutical composition
  • Tapentadol pharmaceutical composition for transdermal administration as well as preparation method and application of pharmaceutical composition

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0069] Embodiment 1 Preparation of transdermal patch of tapentadol hydrochloride

[0070] (1) 5 g of tapentadol hydrochloride, 1.95 g of Soluplus, and 0.1 g of magnesium stearate were micronized, mixed uniformly to obtain a physical mixture, and 2.95 g of polyethylene glycol (molecular weight 2000) was added;

[0071] (2) Set the extrusion temperature of the twin-screw extruder to 120°C, start the screw after rising to the set temperature, add the physical mixture in step (1) to the extruder, melt and extrude, and Spherical pellets are extruded to produce amorphous particles, which are then micronized, and the particle size is controlled at about 100-150nm.

[0072] (3) Weigh 5 g of micronized amorphous particles prepared in step (2), 0.2 g of soybean lecithin, 0.03 g of cholesterol, 3 g of absolute ethanol, and 1.77 g of water;

[0073] (4) Dissolving soybean lecithin, cholesterol, and tapentad hydrochloride multiparticles in absolute ethanol, and heating to 30-45°C to disso...

Embodiment 2

[0077] Embodiment 2 Preparation of transdermal patch of tapentadol hydrochloride

[0078] (1) Micronize 6 g of tapentadol hydrochloride, 1 g of povidone (PVP-S630) and 0.13 g of magnesium stearate, and mix uniformly to obtain a physical mixture, adding 2.87 g of polyethylene glycol (molecular weight 3000);

[0079] (2) Set the extrusion temperature of the twin-screw extruder to 100°C, start the screw after rising to the set temperature, add the physical mixture in step (1) to the extruder, melt and extrude, and Spherical pellets are extruded to produce amorphous particles, which are then micronized, and the particle size is controlled at about 150-200nm.

[0080] (3) Weigh 5 g of micronized amorphous particles prepared in step (2), 0.2 g of phosphatidylcholine, 0.08 g of cholesterol, 3 g of propylene glycol, and 1.72 g of water;

[0081] (4) Dissolving phosphatidylcholine, cholesterol, and tapentad hydrochloride multiparticulates in propylene glycol, and heating to 30-45°C to...

Embodiment 3

[0085] Embodiment 3 Preparation of transdermal patch of tapentadol hydrochloride

[0086] (1) Micronize 7 g of tapentadol hydrochloride, 1.5 g of povidone (PVP-VA64), and 0.1 g of talcum powder, mix uniformly to obtain a physical mixture, and add 1.4 g of polyethylene glycol (molecular weight 4000);

[0087] (2) Set the extrusion temperature of the twin-screw extruder to 140°C, start the screw after rising to the set temperature, add the physical mixture in the step (1) to the extruder, melt and extrude, and Spherical pellets are extruded to produce amorphous particles, which are then micronized, and the particle size is controlled at about 250-300nm.

[0088] (3) Weighing 7 g of micronized amorphous particles prepared in step (2), 2 g of dipalmitoylphosphatidylcholine, 0.3 g of cholesterol, 30 g of absolute ethanol, and 60.7 g of water;

[0089] (4) Dissolving dipalmitoylphosphatidylcholine, cholesterol, and tapentad hydrochloride multiparticles in absolute ethanol, and heat...

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
Diameteraaaaaaaaaa
Login to view more

Abstract

The invention discloses a pharmaceutical composition for transdermal administration. The pharmaceutical composition contains tapentadol or a pharmaceutically acceptable salt thereof, a polymer dispersion carrier material, a hot-melt protective agent and an optional solubilizer. A preparation method of the pharmaceutical composition includes the following steps: mixing the tapentadol or the pharmaceutically acceptable salt thereof, the polymer dispersion carrier material, the hot-melt protective agent and the optional solubilizer, performing hot-melt extrusion, and performing micronization to obtain the microparticles of the tapentadol or the pharmaceutically acceptable salt thereof. The pharmaceutical composition for the transdermal administration can make the tapentadol or the pharmaceutically acceptable salt thereof rapidly absorbed, and achieve the purpose of sedation before anesthesia without affecting breathing, thereby avoiding the adverse psychological effects of intramuscular injection or intravenous injection acupuncture on children; and at the same time, the pharmaceutical composition can also be used to prevent and/or treat and delay the development of Parkinson disease.

Description

technical field [0001] The invention relates to pharmaceutical preparation technology, more specifically to a pharmaceutical composition for transdermal administration of tapentadol, a preparation method and application thereof. Background technique [0002] Tapentadol hydrochloride is a new type of oral analgesic drug jointly developed by Johnson & Johnson Pharmaceuticals of the United States and Gruenenthal GmbH of Germany. Its sustained-release tablet was approved by the FDA in August 2012 for the treatment of adult diabetic peripheral neuropathy (DPN). associated neuropathic pain. Through oral analgesia twice a day, continuous opioid analgesia can be achieved and maintained for a period of time. [0003] Delayed formulations are generally known in the prior art for many different active ingredients. Common forms of delay include coating delay and matrix delay. Coating delay means that the core of the pharmaceutical composition comprising the active ingredient provides...

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): A61K31/137A61K9/70A61K9/127A61K47/28A61K47/10A61P25/16
CPCA61K31/137A61K9/7023A61K9/127A61K47/28A61K47/10A61P25/16
Inventor 汪淼刘敏张丽娜杨玉萍袁靖郭建锋田峦鸢曲龙妹吕金良朱圣姬李莉娥李仕群杜文涛金芬熊俊
Owner YICHANG HUMANWELL PHARMA
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