A pharmaceutical composition for administering benzodiazepines through nasal mucosa, its preparation method and application

A benzodiazepine and composition technology, applied in the field of pharmaceutical preparations, can solve the problems of high industrialized production cost, inconvenient medication for patients, large amount of auxiliary materials, etc., and achieve the effects of prolonging action time, enhancing self-immunity, and ensuring drug efficacy.

Active Publication Date: 2022-05-17
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 freeze-drying process has a long preparation cycle, about 5 days a production cycle, the amount of auxiliary materials is large, the industrial production cost is high, and the preparations all need professional medical personnel to inject them, which is very unsafe. convenient
[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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  • A pharmaceutical composition for administering benzodiazepines through nasal mucosa, its preparation method and application
  • A pharmaceutical composition for administering benzodiazepines through nasal mucosa, its preparation method and application
  • A pharmaceutical composition for administering benzodiazepines through nasal mucosa, its preparation method and application

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0069] Compound (R) shown in embodiment 1 formula (I) 1 is methyl, R 2 Prepared for nasal mucosal administration of methyl) benzenesulfonate

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

[0071]

[0072] Preparation Process:

[0073] 1. Microparticle preparation:

[0074] (1) Compound (R) shown in formula (I) 1 is methyl, R 2 Be methyl) besylate as API and Soluplus, magnesium stearate micronization, mix homogeneously, after making 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, buffe...

Embodiment 2

[0083] Compound (R) shown in embodiment 2 formula (I) 1 is methyl, R 2 Preparation of pharmaceutical composition for ethyl) administration through nasal mucosa

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

[0085]

[0086] Preparation Process:

[0087] 1. Microparticle preparation:

[0088] (1) Compound (R) shown in formula (I) 1 is methyl, R 2 Be ethyl) as API and K30, magnesium stearate micronization, mix uniformly, after making physical mixture, add polyethylene glycol P6000.

[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, lecithi...

Embodiment 3

[0097] Compound (R) shown in embodiment 3 formula (I) 1 for hydrogen, R 2 Preparation of pharmaceutical composition for nasal mucosa administration

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

[0099]

[0100] Preparation Process:

[0101] 1. Microparticle preparation:

[0102] (1) Compound (R) shown in formula (I) 1 for hydrogen, R 2 For methyl) as API and K90, talcum powder micronization, mix well, after making physical mixture, 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 microparticles, phosphatidylcholine, cholesterol, buffer, p-phenylenediamine,...

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Abstract

The invention discloses a pharmaceutical composition for administering benzodiazepines through nasal mucosa, which comprises a compound represented by formula (I) or a pharmaceutically acceptable salt thereof, a polymer dispersion carrier material, a thermal melt protector and Optional fluxing agent, R in formula (I) 1 and R 2 For the definition of , refer to the instructions for details; the preparation method of the pharmaceutical composition includes micronizing the benzodiazepine compound or its pharmaceutically acceptable salt, the polymer dispersion carrier material and the hot-melt protective agent, and optionally adding The solvent is uniformly mixed to obtain a physical mixture, and then subjected to hot-melt extrusion and micronization to obtain particles of the benzodiazepine compound or a pharmaceutically acceptable salt thereof. In addition, the preparation method and application of the above pharmaceutical composition are also provided. The pharmaceutical composition can be used for the treatment of depression, delirium and other diseases.

Description

technical field [0001] The present invention relates to pharmaceutical preparation technology, more specifically to a kind of benzodiazepine A pharmaceutical composition for administering a class of compounds (that is, a compound represented by formula (I)) through the nasal mucosa, and a preparation method and use thereof. The pharmaceutical composition can be used for the treatment of depression, delirium and other diseases. Background technique [0002] Compound shown in formula (I) (wherein, R 1 selected from hydrogen, methyl, ethyl, isopropyl; R 2 methyl, ethyl) is a new type of benzodiazepine Compounds that 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 the patient to regain consciousness quickly and be discharged from the hospital as soon as possible. In the face of the gradual increase in short-term hospitalization case...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K9/14A61K31/5517A61K9/127A61P25/24A61P25/00
CPCA61K31/5517A61K9/0043A61K9/146A61K9/127A61P25/24A61P25/00
Inventor 曲龙妹田峦鸢吕金良廖娇金芬郭建锋汪淼李莉娥李仕群符义刚杜文涛李杰杨玉萍张丽娜陈轶苗
Owner YICHANG HUMANWELL PHARMA
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