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Eye drop of pazufloxacin mesilate, its preparing method and application

A technology of pazufloxacin mesylate and eye drops, which is applied in the direction of pharmaceutical formulas, medical preparations containing active ingredients, organic active ingredients, etc., to achieve the effect of being conducive to industrial production, significant therapeutic effect, and simple preparation process

Inactive Publication Date: 2005-07-06
NANJING MEDICAL UNIV +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

But so far, the application of pazufloxacin mesylate as eye drops has not yet been listed on the market both at home and abroad.

Method used

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  • Eye drop of pazufloxacin mesilate, its preparing method and application

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 2

[0049] (1) Prescription composition:

[0050] 1. Pazufloxacin mesylate 7810.0mg

[0051] 2. Ethylparaben 600.0mg

[0052] 3. Sodium edetate 2500.0mg

[0053] 4. Methylcellulose 2500.0mg

[0054] Make up to 1000..0ml with phosphate buffer

[0055] Makes 200 bottles

[0056] (2) Preparation process:

[0057] Weigh 10g of NaH 2 PO 4 , 9gNa 2 HPO 4 Add 1000 mL of water for injection to prepare a phosphate buffer solution with a pH close to 5.0 for use.

[0058] Take by weighing ethyl paraben and edetate disodium of the prescription amount, first add ethyl paraben to the phosphate buffer 600ml of the above configuration, heat and stir to dissolve, add sodium edetate after dissolving, After stirring to dissolve, add the prescribed amount of pazufloxacin mesylate and stir until dissolved to obtain solution 1;

[0059] Weigh the prescribed amount of methylcellulose, add 200 mL of the above-mentioned phosphate buffer solution, stir to dissolve, and obtain solution 2;

[0...

Embodiment 3

[0063] (1) Prescription composition:

[0064] 1. Pazufloxacin mesylate 991.0mg

[0065] 2. Methylparaben 115.0mg

[0066] 3. Propylparaben 55.0mg

[0067] 4. Sodium bisulfite 500.0mg

[0068] 5. Polyvinylpyrrolidone (PVP-30) 5000.0mg

[0069] Add borate buffer to 500.0ml

[0070] Makes 100 bottles

[0071] (2) Preparation process:

[0072] Weigh 15g H 3 BO 3 and 7.5g Na 2 B 4 o 7 10H 2 O, add 500.0 mL of water for injection, and prepare a borate buffer solution with a pH close to 5.0 for use.

[0073] Weigh the prescribed amount of methylparaben, propylparaben, and sodium bisulfite, first add methylparaben and propylparaben to 300mL of the above-mentioned borate buffer solution, heat and stir to dissolve After dissolving, add sodium bisulfite, stir and dissolve, add the prescribed amount of pazufloxacin mesylate and stir until dissolved to obtain solution 1;

[0074] Weigh the prescribed amount of polyvinylpyrrolidone (PVP-30), add 100.0 mL of the borate buffer...

Embodiment 4

[0078] (1) Prescription composition:

[0079] 1. Pazufloxacin mesylate 3905.0mg

[0080] 2.5% benzalkonium bromide 2000.0μl (200μl contains 0.01g)

[0081] 3. Sodium citrate 1000.0mg

[0082] 4. β-cyclodextrin (β-cyclodextron) 2500.0mg

[0083] Add to 1000.0ml with 2.5% boric acid water

[0084] (2) Preparation process:

[0085] Weigh 25 g of boric acid, add 1000.0 mL of water for injection, and prepare a 2.5% borate solution for use. Take the prescribed amount of benzalkonium bromide, sodium citrate, and β-cyclodextrin, add 800.0mL of 2.5% boric acid solution, stir to dissolve, after dissolving, add the prescribed amount of pazufloxacin mesylate and stir until fully dissolved , However, use a sand funnel to filter into the filter bottle, after filtering, rinse the container and funnel with 100 mL of 2.5% boric acid solution, and filter the washing liquid into the filter bottle. After stirring evenly, add 2.5% boric acid solution to 1000.0 mL, and adjust the pH value to ...

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PUM

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Abstract

The disclosed eye drop is prepared from Pazufloxacin mesilate, preservative agent, stabilizer, viscosity increaser and solvent through the steps of, (1) preparing boric acid and cushion liquid, (2) charging preservative into buffer agent, heating, stirring, dissolving and charging into stabilizing agent, charging Pazufloxacin mesilate, heating and stirring till dissolving, obtaining solution 1, (3) charging viscosity increaser into buffer agent or boric acid water, stirring till dissolving to obtain solution 2, (4) filtering the solution to obtained filtration liquid, (5) filtering the solution 2 to obtain filtration liquid, (6) merging the filtration liquid obtained in step (4) and (5), stirring, dissolving and charging into boric acid water or cushion agent, adjusting pH with hydrochloric acid or NaOH.

Description

1. Technical field [0001] The invention relates to an eye drop, in particular to a pazufloxacin mesylate eye drop, a preparation method and an application thereof. 2. Technical background [0002] Pazufloxacin belongs to the third generation of quinolone anti-infective drugs. It was first researched and developed by Toyama Chemical Company in Japan, and it was launched on the market on April 12, 2002 abroad. Quinolones are a relatively new class of synthetic antibacterial drugs. They differ from other antibacterial drugs in that they target bacterial DNA and prevent bacterial DNA from forming supercoils by preventing DNA topoisomerase II and IV from functioning. , further causing irreversible damage to chromosomes, resulting in the inability of bacterial cells to divide and reproduce. It has a selective toxic effect on bacteria. Bacteria's resistance to many antibiotics can be widely spread due to plasmid transfer, but quinolones are not easily affected by plasmid transfer...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/5365A61P27/02
Inventor 张银娣任宝华沈建平吴建伟缪跃丰金叶冯鲁中
Owner NANJING MEDICAL UNIV
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