Benzodiazepine compound topical pharmaceutical composition as well as preparation method and application thereof

A composition and compound technology, which is applied in the directions of drug combinations, pharmaceutical formulations, and non-active ingredients medical preparations, etc., can solve the problems of poor compliance, inconvenient use of preparations for injection, and high production costs.

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

Compound (R) shown in formula (I) has been reported in Chinese patent CN103202815B 1 and R 2 Both are freeze-dried preparations of salts of methyl), the preparation cycle of the freeze-drying process is long, about 5 days a production cycle, the amount of excipients is large, the cost of industrial production is high, and the preparation requires professional medical personnel to inject it, which is very inconvenient
[0004] Most of the current literature reports are that the compound shown in formula (I) is prepared as a freeze-dried powder preparation and then used clinically. The preparation process of this dosage form has a long production cycle and high production costs; clinically, it needs to be temporarily formulated into a solution before it can be used clinically. It is used under the guidance of a professional doctor, and it is often accompanied by injection pain during injection, which makes it inconvenient for patients to take medication and has poor compliance

Method used

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  • Benzodiazepine compound topical pharmaceutical composition as well as preparation method and application thereof
  • Benzodiazepine compound topical pharmaceutical composition as well as preparation method and application thereof
  • Benzodiazepine compound topical pharmaceutical composition as well as preparation method and application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0075] Example 1 Compound (R) represented by formula (I) 1 is methyl, R 2 Preparation of transdermal patch for methyl)benzenesulfonate

[0076] (1) Compound (R) represented by formula (I) 1 is methyl, R 2 Be methyl) benzene sulfonate 8g and Soluplus7.4g, magnesium stearate 0.5g micronization, add polyethylene glycol (molecular weight 2000) 14g, mix well, make physical mixture;

[0077] (2) Set the extrusion temperature of the twin-screw extruder to be 120°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 100-150 nm.

[0078] (3) Weigh 3 g of micronized amorphous particles prepared in step (2), 2 g of soybean lecithin, 0.3 g of cholesterol, 30 g of dehydrated alcohol, and 64.7 g of water;

[0079] ...

Embodiment 2

[0086] Embodiment 2 Compound (R) represented by formula (I) 1 is methyl, R 2 Preparation of transdermal patch for ethyl)

[0087] (1) Compound (R) represented by formula (I) 1 is methyl, R 2 For ethyl) 0.9g and povidone (PVP-S630) 3.1g, talc 0.2g micronized, add polyethylene glycol (molecular weight 4000) 5.8g, mix uniformly to obtain a physical mixture;

[0088] (2) Set the extrusion temperature of the twin-screw extruder to be 120°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 150-175 nm.

[0089] (3) Weighing the compound (R) represented by the formula (I) prepared in step (2) 1 is methyl, R 2 ethyl) micronized amorphous particles 0.3g, phosphatidylcholine 2g, cholesterol 0.3g, propylene gl...

Embodiment 3

[0097] Embodiment 3 Compound (R) represented by formula (I) 1 for hydrogen, R 2 Preparation of transdermal patch for methyl)

[0098] (1) Compound (R) represented by formula (I) 1 for hydrogen, R 2 Be methyl) 0.8g and povidone (PVP-K30) 3g, magnesium stearate 0.2g micronize, add polyethylene glycol (molecular weight 6000) 6.0g, mix well, make physical mixture;

[0099] (2) The extrusion temperature of the twin-screw extruder is set to 120°C, the screw is started after rising to the set temperature, the physical mixture in step (1) is added to the extruder, and after hot melting and extrusion, 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 180-230 nm.

[0100] (3) Weighing the compound (R) represented by the formula (I) prepared in step (2) 1 for hydrogen, R 2 For methyl) micronized amorphous particles 7g, phosphatidylethanolamine 2g, ch...

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Abstract

The invention discloses a benzodiazepine compound topical pharmaceutical composition. The composition comprises a benzodiazepine compound represented by a formula (I) shown in the specification or a pharmaceutically acceptable salt thereof, a polymer dispersion carrier material, a hot-melt protective agent and an optional solubilizer, the definitions of R1 and R2 in the formula (I) are detailed inthe specification, and the topical pharmaceutical composition is administered transdermally and externally; and a preparation method of the topical pharmaceutical composition includes the steps of micronizing the benzodiazepine compound, the polymer dispersion carrier material and the hot-melt protective agent, optionally adding the solubilizer, performing uniform mixing to obtain a physical mixture, performing hot-melt extrusion, and performing micronization to obtain the benzodiazepine compound particles. The invention also provides an application of the above pharmaceutical composition. The pharmaceutical composition can be used for calming the heart and tranquilizing and allaying excitement, and realizing hypnosis, and improves sleep quality, people is clear-headed after using the pharmaceutical composition, the compound represented by the formula (I) has no residues or accumulation in vivo, does not affect work in a next day, and makes the user full of spirit and energy.

Description

technical field [0001] The present invention relates to pharmaceutical preparation technology, more particularly to a kind of benzodiazepine The topical pharmaceutical composition of the compound (namely the compound represented by formula (I)) and the preparation method and use thereof. The pharmaceutical composition can be used for calming the heart, soothing the mind, sedation, hypnosis, and improving sleep quality. Background technique [0002] The compound represented by formula (I) (wherein, R 1 Selected from hydrogen, methyl, ethyl, isopropyl; R 2 For methyl, ethyl) is a new type of benzodiazepine class of compounds, are short-acting sedatives. Clinically, it can be used for procedural sedation, induction and maintenance of general anesthesia, sedation of ICU patients, etc. Short-acting sedatives allow patients to regain consciousness quickly and be discharged from the hospital as soon as possible. In the face of the gradual increase in short-term hospitalizat...

Claims

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Application Information

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IPC IPC(8): A61K31/5517A61K9/70A61K9/127A61K47/28A61K47/10A61P25/20A61P17/02
CPCA61K31/5517A61K9/7023A61K9/127A61K47/28A61K47/10A61P25/20A61P17/02
Inventor 田峦鸢刘朋金芬曲龙妹郭建锋吴有斌汪淼吕金良李莉娥符义刚李仕群李杰杜文涛
Owner YICHANG HUMANWELL PHARMA
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