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Lomefloxacin hydrochloride lyophilized powder for injection and preparation method therefor

A technology of lomefloxacin hydrochloride and freeze-dried powder injection, which is applied in the field of lomefloxacin hydrochloride freeze-dried powder injection for injection and its preparation, can solve the difference of product formability and resolubility, affect product quality and curative effect, and pH value fluctuation It can achieve the effect of good tolerance, low incidence of adverse reactions, and low toxicity and side effects

Active Publication Date: 2009-06-03
SHANXI PUDE PHARMA CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Among them, when the injection is exposed to light and the temperature is too high, the stability is poor, it is easy to decompose, easy to precipitate, and the effect is unstable, which seriously affects the product quality and curative effect.
In addition, the prescription of lomefloxacin hydrochloride injection also needs to add DMF (N, N-dimethylformamide) as a co-solvent, but DMF has certain toxicity, and the Chinese Pharmacopoeia classifies it as the second most common residual solvent in drugs. Class II, use should be limited to prevent potential adverse effects on patients
[0008] In the production process of currently commercially available lomefloxacin hydrochloride powder injections, water for injection is generally used directly for dosing, and the pH value fluctuates greatly, resulting in unstable quality and poor tolerance of patients; different freeze-drying processes will also cause The formability and resolubility of the produced products have great differences

Method used

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  • Lomefloxacin hydrochloride lyophilized powder for injection and preparation method therefor
  • Lomefloxacin hydrochloride lyophilized powder for injection and preparation method therefor
  • Lomefloxacin hydrochloride lyophilized powder for injection and preparation method therefor

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0048] Example 1 Preparation of 0.1g Lomefloxacin Hydrochloride Injection Freeze-dried Powder Injection

[0049] Prescription composition: (1000 bottles of prescription volume)

[0050] Lomefloxacin hydrochloride (pure product is calculated as lomefloxacin) 100g

[0051] Mannitol 41.4g

[0052] Glacial acetic acid-sodium acetate buffer (pH 4.5) 2600ml

[0053] Filled in 7ml vials

[0054] Preparation of glacial acetic acid-sodium acetate buffer (pH 4.5): Take 9.8ml of glacial acetic acid, add 18g of sodium acetate, and dilute to 1000ml with water for injection.

[0055] Add the prescribed amount of buffer into the concentrated tank and heat to about 70°C.

[0056] Add the prescribed amount of mannitol into the concentrated tank and stir to dissolve.

[0057] Slowly and evenly add the prescribed amount of lomefloxacin hydrochloride into the concentrated tank and stir to dissolve, then cool to about 60°C.

[0058] Measure the pH value of the liquid, and adjust the pH value...

Embodiment 2

[0068] Example 2 Preparation of 0.2g Lomefloxacin Hydrochloride Injection Freeze-dried Powder Injection

[0069] Prescription composition: (1000 bottles of prescription volume)

[0070] Lomefloxacin hydrochloride (pure product is calculated as lomefloxacin) 200g

[0071] Mannitol 82.8g

[0072] Glacial acetic acid-sodium acetate buffer (pH 4.5) 5400ml

[0073] Potting in 12ml vials

[0074] Preparation of glacial acetic acid-sodium acetate buffer (pH 4.5): Take 9.8ml of glacial acetic acid, add 18g of sodium acetate, and dilute to 1000ml with water for injection.

[0075] Add the prescribed amount of buffer into the concentrated tank and heat to about 70°C.

[0076] Add the prescribed amount of mannitol into the concentrated tank and stir to dissolve.

[0077] Slowly and evenly add the prescribed amount of lomefloxacin hydrochloride into the concentrated tank and stir to dissolve, then cool to about 60°C.

[0078] Measure the pH value of the liquid, and adjust the pH val...

Embodiment 3

[0088] Example 3 Preparation of 0.4g lomefloxacin hydrochloride freeze-dried powder for injection

[0089] Prescription composition: (1000 bottles of prescription volume)

[0090]Lomefloxacin hydrochloride (pure product is calculated as lomefloxacin) 400g

[0091] Mannitol 165.6g

[0092] Glacial acetic acid-sodium acetate buffer (pH 4.5) 10400ml

[0093] Filled in 30ml vials

[0094] Preparation of glacial acetic acid-sodium acetate buffer (pH 4.5): Take 9.8ml of glacial acetic acid, add 18g of sodium acetate, and dilute to 1000ml with water for injection.

[0095] Add the prescribed amount of buffer into the concentrated tank and heat to about 70°C.

[0096] Add the prescribed amount of mannitol into the concentrated tank and stir to dissolve.

[0097] Slowly and evenly add the prescribed amount of lomefloxacin hydrochloride into the concentrated tank and stir to dissolve, then cool to about 60°C.

[0098] Measure the pH value of the medicinal solution, adjust the pH v...

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Abstract

The invention relates to a lomefloxacin hydrochloride lyophilized powder for injection and a preparation method therefor. The lomefloxacin hydrochloride lyophilized powder for injection is prepared by an active ingredient of lomefloxacin hydrochloride, an acceptable lyophilized powder for injection excipient on pharmacy and a buffer solution with the pH value being 3.0-6.5, and the proportion of the three components is (50-150): (20-60): (1500-3500) (g:g:ml). The lomefloxacin hydrochloride lyophilized powder for injection has the advantages that the efficacy of the lyophilized powder for injection is stable, the lyophilized powder for injection is not easily decomposed and separated, the application is convenient, the tolerance is good, the physiological stimulation is slight, and the lyophilized powder for injection can be stably deposited for a long term.

Description

technical field [0001] The invention belongs to the field of pharmaceutical preparations, and in particular relates to a lomefloxacin hydrochloride freeze-dried powder injection for injection with stable drug effect and difficult to decompose and separate out and a preparation method thereof. Background technique [0002] Lomefloxacin hydrochloride is a third-generation quinolone antibacterial agent with a quinoline ring as the mother nucleus, and its chemical name is (±)-1-ethyl-6,8-difluoro-1,4-dihydro-7- (3-Methyl-1-piperazinyl)-4-oxo-3-quinolinecarboxylate hydrochloride. The chemical structure is as shown in the figure below. There are fluorine atoms at the 6 and 8 positions of the quinoline ring, and 3-methyl-piperazinyl at the 7 position. Lomefloxacin introduces a fluorine atom at the 6-position of the quinoline ring, which expands the antibacterial spectrum against Gram-positive bacteria and enhances the antibacterial activity. The fluorine atom was introduced into ...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/19A61K31/496A61P31/04
Inventor 胡成伟解晓荣李立忠李润宝韩忠王勇
Owner SHANXI PUDE PHARMA CO LTD
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