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Gatifloxacin liposome ophthalmic gel and preparation method thereof

A technology of gatifloxacin and cationic liposome, which is applied in the field of gatifloxacin liposome ophthalmic gel and its preparation, can solve the problem of large fluctuations in drug concentration, difficult control of dosage, and reduced frequency of use, etc. problems, to achieve the effects of quality control, broad industrialization prospects, and increased contact time

Inactive Publication Date: 2016-01-06
SHENYANG XINMA PHARMA +2
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

The above inventions all use hydrophilic polymer materials as carriers. Compared with traditional eye drops, ophthalmic gels can be combined with the eyes for a relatively long time, reducing the frequency of use, but the dosage is not easy to control, and the concentration of drugs in the eyes High volatility

Method used

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  • Gatifloxacin liposome ophthalmic gel and preparation method thereof
  • Gatifloxacin liposome ophthalmic gel and preparation method thereof
  • Gatifloxacin liposome ophthalmic gel and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0024] Formulations were prepared according to the ingredients contained in the unit dosage forms shown in Table 1.

[0025] 1. Preparation process of samples 1 to 7:

[0026] (1) Place the phospholipids, cholesterol, and octadecylamine of the prescribed amount in a glass bottle, add an appropriate amount of ether to dissolve, then rotate the ether solution in the glass bottle to form a film on the inner wall of the glass bottle;

[0027] (2) the gatifloxacin of recipe quantity is dissolved in the phosphate buffer solution that pH is 6, adds in the glass bottle and constantly stirs, obtains gatifloxacin liposomal colostrum, colostrum is passed through high-pressure homogenizer in 1.4×10 6 Under the pressure of kPa, squeeze the emulsion through a 50nm membrane 5 times to obtain the gatifloxacin liposome solution. Add a preservative and an osmotic pressure regulator, adjust the pH value to 6.5, stir to make it uniform, and obtain liposome solution I;

[0028] (3) Add the pres...

Embodiment 2

[0043] prescription:

[0044]

[0045] Preparation:

[0046] (1) Place the phospholipids, cholesterol, and octadecylamine of the prescribed amount in a glass bottle, add an appropriate amount of ether to dissolve, then rotate the ether solution in the glass bottle to form a film on the inner wall of the glass bottle;

[0047] (2) the gatifloxacin of recipe quantity is dissolved in the phosphate buffer solution that pH is 6, adds in the glass bottle and constantly stirs, obtains gatifloxacin liposomal colostrum, colostrum is passed through high-pressure homogenizer in 1.4×10 6 Under the pressure of kPa, squeeze the emulsion through a 50nm membrane 5 times to obtain the gatifloxacin liposome solution. Add a preservative and an osmotic pressure regulator, adjust the pH value to 6.5, stir to make it uniform, and obtain liposome solution I;

[0048] (3) Add the prescribed amount of water-soluble gel matrix into 80% boiled water for injection, disperse evenly, sterilize by aut...

Embodiment 3

[0051] prescription:

[0052]

[0053] Preparation:

[0054] (1) Place the phospholipids, cholesterol, and octadecylamine of the prescribed amount in a glass bottle, add an appropriate amount of ether to dissolve, then rotate the ether solution in the glass bottle to form a film on the inner wall of the glass bottle;

[0055] (2) the gatifloxacin of recipe quantity is dissolved in the phosphate buffer solution that pH is 7, adds in the glass bottle and constantly stirs, obtains gatifloxacin liposomal colostrum, colostrum is passed through high-pressure homogenizer in 1.4×10 6 Under the pressure of kPa, squeeze the milk through a 50nm membrane for 3 times to obtain the gatifloxacin liposome solution. Add a preservative and an osmotic pressure regulator, adjust the pH to 6, stir to make it uniform, and obtain liposome solution I;

[0056] (3) Add the prescribed amount of water-soluble gel matrix into 80% boiled water for injection, disperse evenly, sterilize by autoclaving...

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Abstract

The invention provides gatifloxacin liposome gel for eyes and a preparation method thereof. The gatifloxacin liposome gel for eyes is composed of gatifloxacin, phospholipids, cholesterol, and the cationic liposome and hydrogel base material prepared through octadecylamine. The gel is uniform in particle diameter distribution, excellent in stability, and easy to be combined with a cornea with negative electricity to improve the permeability of the cornea, and can be continuously positioned at eyes for drug release, so that the toxic and side effects of a drug are reduced, and the biological availability of the drug is improved. The preparation method is practicable in process, and controllable in quality, and has a very broad industrial prospect.

Description

technical field [0001] The invention relates to a pharmaceutical preparation, in particular to a gatifloxacin liposome ophthalmic gel and a preparation method thereof. Background technique [0002] According to statistics, more than 80% of patients who visit the ophthalmology department have eye infections, which include conjunctivitis, keratitis, and global inflammation. Among them, bacterial conjunctivitis is an infectious conjunctivitis that occurs mainly in summer and autumn, and is a common and frequently-occurring disease in ophthalmology clinics. At present, eye drops for the treatment of bacterial conjunctivitis mainly include ciprofloxacin and ofloxacin eye drops. However, its eye drops have little effect on Gram-positive bacteria, anaerobic bacteria, mycoplasma, chlamydia and mycobacteria. Gatifloxacin has a broad antibacterial spectrum. In addition to the antibacterial properties of ciprofloxacin and ofloxacin, it also has good antibacterial effects on these pat...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K9/06A61K9/127A61K31/496A61K47/18A61P27/02A61P31/04A61P31/00
Inventor 闫志刚王淑君陈斌刘莹关玉晶刘婷
Owner SHENYANG XINMA PHARMA