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Transdermal delivery based pharmaceutical composition and preparation method and application thereof

A technology for transdermal drug delivery and composition, applied in the field of transdermal drug delivery pharmaceutical composition and preparation thereof, can solve the problems of inconvenient medication for patients, adverse psychological effects of patients, poor compliance and the like

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

[0006] However, at present, ketamine or its isomer dexketamine is mainly used in the injection form on the market, which needs to be used under the guidance of professional doctors in clinical practice, and is often accompanied by injection pain during injection, which is inconvenient for patients and poor compliance , often bring adverse psychological effects to patients, especially when used for young children, this situation is more likely to occur

Method used

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  • Transdermal delivery based pharmaceutical composition and preparation method and application thereof
  • Transdermal delivery based pharmaceutical composition and preparation method and application thereof
  • Transdermal delivery based pharmaceutical composition and preparation method and application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0069] The transdermal patch preparation of compound (dexketamine) hydrochloride shown in embodiment 1 formula (I)

[0070] (1) 5 g of compound (dexketamine) hydrochloride shown in formula (I), 2 g of povidone (PVP-S630), 0.12 g of magnesium stearate are micronized, and polyethylene glycol (molecular weight 2000) 2.88 g is added , mixed evenly to obtain a physical mixture;

[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, heat-melt and extrude, Extrude in the form of spherical particles to obtain amorphous particles, and then micronize them to obtain micronized amorphous particles, 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 leci...

Embodiment 2

[0077] Example 2 Preparation of transdermal patch of compound (ketamine) represented by formula (I)

[0078] (1) Micronize compound (ketamine) 6g and povidone (PVP-S630) 1g, magnesium stearate 0.18g shown in formula (I), add polyethylene glycol (molecular weight 3000) 2.82g, mix well, produce a physical mixture;

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

[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 the compoun...

Embodiment 3

[0085] Example 3 Preparation of the transdermal patch of the compound represented by formula (I) (levoketamine)

[0086] (1) Micronize 7 g of the compound represented by formula (I) (levoketamine), 1.5 g of povidone (PVP-VA64) and 0.2 of talc, add 1.3 g of polyethylene glycol (molecular weight 4000), mix well, and prepare a physical mixture;

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

[0088] (3) Weigh 7g of micronized amorphous particles prepared in step (2), 2g of dipalmitoyl phosphatidylcholine, 0.3g of cholesterol, 30g of dehydrated alcohol, and 60.7g of water;

[0089] (4) dissolving dipalmitoyl ph...

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Abstract

The present invention discloses a transdermal delivery based pharmaceutical composition. The composition comprises a compound as shown in a formula (I) or pharmaceutically acceptable salt thereof, a macromolecular dispersing carrier material, a hot melting protecting agent and an optional fluxing agent. A preparation method of the transdermal delivery based pharmaceutical composition comprises thesteps of micronizing the compound as shown in the formula (I) or the pharmaceutically acceptable salt thereof, the macromolecular dispersing carrier material and the hot melting protecting agent, optionally adding the fluxing agent, mixing the components uniformly, and performing hot melting extrusion and micronizing to obtain microparticles of the compound as shown in the formula (I) or the pharmaceutically acceptable salt thereof. In addition, the invention provides an application of the pharmaceutical composition. The transdermal delivery based pharmaceutical composition can enable the compound as shown in the formula (I) to be quickly absorbed, so that the purpose of calming before anesthesia is achieved, breathing is not affected, and the adverse psychological effects on children dueto intramuscular injection or intravenous injection are avoided. Meanwhile, the pharmaceutical composition also can be used for preventing and / or treating hyperactivity.

Description

technical field [0001] The present invention relates to pharmaceutical preparation technology, and more particularly to a pharmaceutical composition for transdermal administration of a compound represented by formula (I) and a preparation method and application thereof. Background technique [0002] Ketamine (the corresponding racemic mixture of the dextro- and levo-enantiomers) is an N-methyl-D-aspartate (NMDA) receptor antagonist that produces a wide range of effects in humans, including sedation Pain, anesthesia, hallucinations, dissociative effects, elevated blood pressure and bronchiectasis. Ketamine is primarily used to induce and maintain general anesthesia. Other uses include sedation in intensive care, analgesia (particularly in emergency medicine), and treatment of bronchospasm. D-ketamine enantiomer (or S-(+) ketamine or esketamine) is a non-competitive and subtype non-selective activity-dependent NMDA receptor antagonist with a new and unique mechanism of actio...

Claims

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Application Information

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IPC IPC(8): A61K9/70A61K31/135A61P23/00A61P29/00A61K9/127
CPCA61K31/135A61K9/7053A61K9/7061A61P23/00A61P29/00A61K9/1271
Inventor 李莉娥曲龙妹田峦鸢吕金良吴有斌汪淼金芬陈雷郭建锋张丽娜符义刚李仕群李杰杜文涛
Owner YICHANG HUMANWELL PHARMA
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