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Gelatin for Balofloxacin eye and method of preparing the same

An ophthalmic gel, balofloxacin technology, applied in pharmaceutical formulations, drug delivery, sensory diseases, etc., can solve the problems that patients are reluctant to use, low bioavailability, poor compliance, etc., to maintain effective drug concentration , long residence time, and the effect of improving bioavailability

Inactive Publication Date: 2008-08-27
WENZHOU MEDICAL UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

As the most commonly used dosage form in ophthalmology, eye drops are diluted to 0.1% of the original concentration by tears within a few minutes after administration or are lost from the nasolacrimal duct, resulting in low bioavailability of only 1% to 10%. Increase the frequency of eye drops, the patient is inconvenient to use, the compliance is poor, and it may cause systemic toxicity
Although the release of eye ointment is slow, patients are not willing to use it because of its strong greasy feeling and easy to cause "blurred vision" due to the base of Vaseline

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0029] Prescription 1:

[0030] Baloxacin 3.0g, sodium hyaluronate (sodium hyaluronate) 2.0g, medicinal lactic acid 0.63g, chlorobutanol 5.0g, glycerin for injection 20.0g, water for injection to a total weight of 1000g.

[0031] Preparation process 1:

[0032] Agent A: Take sodium hyaluronate and sprinkle it into about 400ml of water for injection. After it is fully swollen, use ultrasonic degassing, seal it, and refrigerate it for later use.

[0033] Agent B: add lactic acid to about 400ml of water for injection, stir well, add baloxacin, stir well, after it dissolves, add glycerin containing chlorobutanol, stir to dissolve, set aside.

[0034] Slowly add Agent B into Agent A, stir while adding, and then ultrasonically degas the air after mixing. After primary filtration, filter through a 0.22 μm microporous filter membrane, add water for injection through the filter membrane to a total weight of 1000g, and aseptically dispense. Instantly.

Embodiment 2

[0036] Prescription 2:

[0037] Baloxacin 2.0g, sodium hyaluronate (sodium hyaluronate) 3.0g, medicinal lactic acid 0.42g, chlorobutanol 3.0g, glycerin for injection 21.0g, and water for injection to a total weight of 1000g.

[0038] Preparation process 2:

[0039] Agent A: Take sodium hyaluronate and sprinkle it into about 400ml of water for injection. After it is fully swollen, use ultrasonic degassing, seal it, and refrigerate it for later use.

[0040] Agent B: add lactic acid to about 400ml of water for injection, stir well, add baloxacin, stir well, after it dissolves, add glycerin containing chlorobutanol, stir to dissolve, set aside.

[0041] Slowly add Agent B into Agent A, stir while adding, and then ultrasonically degas the air after mixing. After primary filtration, filter through a 0.22 μm microporous filter membrane, add water for injection through the filter membrane to a total weight of 1000g, and aseptically dispense. Instantly.

Embodiment 3

[0043] Prescription 3:

[0044] Baloxacin 3.0g, hydroxypropyl methylcellulose 15g, medicinal lactic acid 0.63g, benzalkonium bromide 0.1g, and water for injection were added to a total weight of 1000g.

[0045] Preparation process 3:

[0046] Agent A: Sprinkle hydroxypropyl methylcellulose into about 400ml of water for injection. After fully swelling, ultrasonically degas the air, seal it, and refrigerate it for later use.

[0047] Agent B: Add lactic acid to about 400ml of water for injection, stir well, add baloxacin, stir well, after it dissolves, add benzalkonium bromide, stir to dissolve, set aside.

[0048] Slowly add Agent B into Agent A, stir while adding, and then ultrasonically degas the air after mixing. After primary filtration, filter through a 0.22 μm microporous filter membrane, add water for injection through the filter membrane to a total weight of 1000g, and aseptically dispense. Instantly.

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PUM

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Abstract

The invention relates to a reasonable formulation of balofloxacin gel for eyes and a preparation method thereof. The preparation contains balofloxacin as an active component and adjuvant including thickeners, acidic auxiliary solvents, antiseptics, isoosmotic adjusting agent and water for injection. The preparation is a flowable clarified semi-solid with slightly yellow or extremely slightly yellow color and has pH value of 5.1-6.0. The invention radically solves the problem of low solubility of balofloxacin, has no crystal formation under low temperature, has less irritation to eyes, and retains local drug concentration during a long period of time. the preparation method comprises the following steps: adding thickeners into water, debubbling under ultrasonic action after swelling to obtain solution A, dissolving acidic auxiliary solvents in water, adding balofloxacin and then isoosmotic adjusting agent and antiseptics, stirring for dissolution to obtain solution B, slowly adding the solution B into the solution A, filtering with a microporous filter film, adding water to a desired volume, and packaging under aseptic conditions. The preparation is used to treat bacterial infections of eye surface.

Description

【Technical field】 [0001] The invention belongs to the technical field of pharmacy, and specifically relates to a formula of an ophthalmic preparation and a preparation method thereof. 【Background technique】 [0002] According to statistics, more than 80% of the patients who visit the ophthalmology department are eye infections, including conjunctivitis, keratitis and global inflammation caused by various pathogenic bacteria. Baloxacin chemical name: 1-cyclopropyl-7-(3-methylamino-1-piperidinyl)-8-methoxy-6-fluoro-1,4-dihydro-4-oxo -3-quinolinecarboxylic acid dihydrate is a quinolone antibacterial drug. The 7-position of its mother nucleus has a 3-methylaminopiperidine ring, which expands the antibacterial spectrum and enhances the antibacterial activity. Its in vitro antibacterial activity is ciproza Star and ofloxacin 2 to 24 times. Gram-positive bacteria, such as Streptococcus pneumoniae and Staphylococcus aureus; Gram-negative bacteria, such as Neisseria gonorrhoeae, Mo...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/00A61K31/4709A61P27/02A61P31/00
Inventor 姜义娜李校堃郁引飞徐龙高慧升周志彩
Owner WENZHOU MEDICAL UNIV