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A short-acting benzodiazepine salt pharmaceutical composition for injection and its preparation method

A technology for benzodiazepine salts and compositions, which is applied in the field of short-acting benzodiazepine salt pharmaceutical compositions for injection and their preparation fields, can solve the problem that ethanesulfonate cannot exert a stable effect, the preparation period is long, and the The problem of large amount of auxiliary materials, etc., can achieve the effect of no discoloration of the appearance, short process cycle, and low impurity content.

Active Publication Date: 2019-03-29
YICHANG HUMANWELL PHARMA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0007] CN103202815B reported the preparation method of the freeze-dried preparation of the salt of formula (I), which described using mannitol or glycine as an excipient, which can exert a stable effect on the benzenesulfonate and toluenesulfonate of formula (I). effect, but the ethanesulfonate of formula (I) can not play a stable effect
However, the freeze-drying process in TW201400119A has a long preparation cycle, about 3-4 days a preparation cycle, and the amount of auxiliary materials is large, and the cost of industrial production is high

Method used

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  • A short-acting benzodiazepine salt pharmaceutical composition for injection and its preparation method
  • A short-acting benzodiazepine salt pharmaceutical composition for injection and its preparation method
  • A short-acting benzodiazepine salt pharmaceutical composition for injection and its preparation method

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Experimental program
Comparison scheme
Effect test

Embodiment 1

[0030] Embodiment 1: Preparation for injection of benzodiazepines Composition of salt medicine

[0031] prescription:

[0032] components

Dosage

Formula (I) besylate

25mg (converted into the amount of formula (I))

Poloxamer 188

5mg

pH regulator

Appropriate amount

Water for Injection

Dilute to 4ml

[0033] Preparation method: according to the feeding ratio, put poloxamer 188 into about 90% of the prescription amount of water for injection to dissolve, adjust the pH value of the above solution to 3.2 with hydrochloric acid and sodium hydroxide, and then add formula I benzenesulfonic acid while stirring Salt, stir until completely dissolved, measure the pH value of the solution to 3.0, and then adjust the volume to the full amount of the prescription. Add 0.1% (w / v, g / ml) medicinal charcoal according to the volume of the solution, and stir for 30 minutes. The medicinal solution is first filtered with a 0.45 μm micr...

Embodiment 2

[0039] Embodiment 2: except that water for injection is settled to 2ml, other is identical with embodiment 1.

Embodiment 3

[0040] Embodiment 3: except that water for injection is settled to 10ml, other is identical with embodiment 1.

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Abstract

The invention discloses a short-term effect benzodiazepines salt medicine composition for injection, which is a freeze-dried medicine composition and contains a pharmaceutically acceptable acidic salt represented as the formula (I), a freeze-dried protective agent and a pH regulator. The freeze-dried protective agent is at least one or a composition selected from poloxamer 188, gelatin and polyethylene glycol 600. The invention also discloses a preparation method for the medicine composition. The medicine composition is greatly improved in stability. The preparation method is short in process period, is less in usage quantity of auxiliary materials, is low in cost and is suitable for industrial production.

Description

technical field [0001] The invention relates to the field of medicine, in particular to a short-acting benzodiazepine for injection Salt pharmaceutical composition and preparation method thereof. Background technique [0002] Formula (Ⅰ) benzodiazepine as follows: [0003] [0004] Formula (I) is a novel 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 cases, the demand for such drugs is particularly urgent. At present, the domestic sedative-hypnotic drug market is dominated by midazolam, and research data show that, compared with similar drug midazolam, formula (I) has a faster onset of action and a shorter duration of sedative eff...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K9/19A61K31/5513A61K47/42A61K47/10A61P25/20
Inventor 李碧军吴有斌符义刚叶夏李莉娥杜文涛李仕群吕金良罗楠郑炜
Owner YICHANG HUMANWELL PHARMA
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