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Pharmaceutical composition of tapentadol or pharmaceutically acceptable salt thereof for nasal mucosa administration and preparation method and application of pharmaceutical composition

A technology for the administration of tapentadol and mucosal administration, which is applied in drug combination, drug delivery, and pharmaceutical formulation, and can solve the problems of complicated preparation process of sustained-release pellets, inconvenient medication for patients, and poor compliance

Active Publication Date: 2020-06-30
YICHANG HUMANWELL PHARMA
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  • 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 sustained-release pellets is relatively complicated
However, it needs to be used under the guidance of professional doctors in clinical practice, and it is often accompanied by injection pain during injection, which is inconvenient for patients to use and has poor compliance.

Method used

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  • Pharmaceutical composition of tapentadol or pharmaceutically acceptable salt thereof for nasal mucosa administration and preparation method and application of pharmaceutical composition
  • Pharmaceutical composition of tapentadol or pharmaceutically acceptable salt thereof for nasal mucosa administration and preparation method and application of pharmaceutical composition
  • Pharmaceutical composition of tapentadol or pharmaceutically acceptable salt thereof for nasal mucosa administration and preparation method and application of pharmaceutical composition

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0069] Example 1 Preparation of pharmaceutical composition for nasal mucosal administration of tapentadol hydrochloride

[0070] The liposome prescription is as shown in the table,

[0071]

[0072] Preparation Process:

[0073] 1. Microparticle preparation:

[0074] (1) Micronize tapentadol hydrochloride, Soluplus, and magnesium stearate, mix well, and after making a physical mixture, add polyethylene glycol P6000.

[0075] (2) Set the extrusion temperature of the twin-screw extruder to 150±10°C, start the screw after rising to the set temperature, add the physical mixture in the step (1) to the extruder, heat-melt, extrude Press and extrude in the form of spherical particles to obtain amorphous particles, which are then micronized to obtain particles with a diameter of less than 150nm.

[0076] 2. Liposome preparation:

[0077] (1) Weigh the microparticles, lecithin, cholesterol, buffer, BHT, and 80% water of the prescribed amount.

[0078] (2) Dissolve lecithin, cho...

Embodiment 2

[0083] Example 2 Preparation of the pharmaceutical composition for nasal mucosal administration of tapentadol

[0084] The liposome prescription is as shown in the table,

[0085]

[0086] Preparation Process:

[0087] 1. Microparticle preparation:

[0088] (1) Micronize tapentadol, K30, and magnesium stearate, and mix them evenly to obtain a physical mixture, then add polyethylene glycol P4000.

[0089] (2) Set the extrusion temperature of the twin-screw extruder to 160±10°C, start the screw after rising to the set temperature, add the physical mixture in the step (1) to the extruder, heat-melt, extrude Press and extrude in the form of spherical particles to obtain amorphous particles, which are then micronized to obtain particles with a diameter of less than 150nm.

[0090] 2. Liposome preparation:

[0091] (1) Weigh the prescribed amount of microparticles, lecithin, cholesterol, buffer solution, antioxidant 1010, and 80% of the prescribed amount of water.

[0092] (...

Embodiment 3

[0097] Example 3 Preparation of Tapentadol Hydrochloride Nasal Administration Pharmaceutical Composition

[0098] The liposome prescription is as shown in the table,

[0099]

[0100] Preparation Process:

[0101] 1. Microparticle preparation:

[0102] (1) Micronize tapentadol hydrochloride, K90, and talcum powder, and mix them uniformly to obtain a physical mixture, then add polyethylene glycol P2000.

[0103] (2) Set the extrusion temperature of the twin-screw extruder to 150°C, start the screw after rising to the set temperature, add the physical mixture in step (1) to the extruder, heat-melt and extrude, It is extruded in the form of spherical particles to obtain amorphous particles, and then micronized to obtain particles with a diameter of less than 150nm.

[0104] 2. Liposome preparation:

[0105] (1) Weigh the prescribed amount of microparticles, phosphatidylcholine, cholesterol, buffer, p-phenylenediamine, and 80% of the prescribed amount of water.

[0106] (2...

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Abstract

The invention discloses a pharmaceutical composition for nasal mucosa administration. The composition comprises 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 for nasal mucosa administration comprises the following steps: micronizing thetapentadol or the pharmaceutically acceptable salt thereof, the polymer dispersion carrier material and the hot melt protective agent, mixing micronized materials with the optional solubilizer, and carrying out hot-melt extrusion and micronization to obtain particles of the tapentadol or the pharmaceutically acceptable salt thereof. The pharmaceutical composition for nasal mucosa administration isused for treating diseases such as depression and related diseases thereof.

Description

technical field [0001] The invention relates to pharmaceutical preparation technology, more specifically to a pharmaceutical composition for nasal mucosal administration of tapentadol or a pharmaceutically acceptable salt thereof, 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. Oral analgesia administered twice a day can provide continuous, opioid-like analgesic effects that can last for a period of time. [0003] In the prior art, delayed formulations are available for many different active ingredients. Common forms of delay include coating delay and matrix delay. Coating delay refers to providing the core of the pha...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/137A61K9/12A61K9/127A61K47/28A61K47/10A61P25/24
CPCA61K31/137A61K9/0043A61K9/127A61K47/28A61K47/10A61P25/24
Inventor 张丽娜汪淼刘敏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
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