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Moxifloxacin eye drop having both bionic function and targeting function and preparation method thereof

A technology of moxifloxacin and moxifloxacin hydrochloride, which is applied in the field of moxifloxacin eye drops and its preparation, can solve problems such as increased difficulty, achieve targeted absorption, increase cell uptake, and improve bioavailability Effect

Inactive Publication Date: 2016-12-21
SHANGHAI HAOHAI BIOLOGICAL TECH
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

At the same time, due to the renewal effect of tears, the medicine can only stay in the eye for 1 to 2 minutes after mixing with tears, which further increases the difficulty for the medicine to reach the ocular surface.

Method used

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  • Moxifloxacin eye drop having both bionic function and targeting function and preparation method thereof
  • Moxifloxacin eye drop having both bionic function and targeting function and preparation method thereof
  • Moxifloxacin eye drop having both bionic function and targeting function and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0029] Example 1: Preparation of moxifloxacin eye drops with both tear bionic and corneal targeting functions.

[0030] formula:

[0031]

[0032]

[0033] Preparation:

[0034] (1) Weigh 5.0 g of moxifloxacin hydrochloride, add it to 400 ml of distilled water, heat to 50-80 ° C, stir to dissolve it, and obtain solution A;

[0035] (2) Add 4.0 g of sodium hyaluronate to solution A prepared in step (1), heat to 50-80°C, stir to dissolve it, and obtain solution B;

[0036] (3) Weigh 3.0 g of xanthan gum and 6.0 g of sodium chloride, add them to 400 ml of distilled water, stir to make them fully swell, and pass through 5 μm and 1 μm secondary filter membranes to obtain solution C;

[0037] (4) Slowly add the solution B prepared in the step (2) to the solution C prepared in the step (3), adjust the pH to 7.0 with a borate buffer solution, replenish water to 1000ml, and obtain the solution D;

[0038] (5) The solution D prepared in the step (4) was sterilized by high-press...

Embodiment 2

[0039] Example 2: Preparation of moxifloxacin eye drops with both tear bionic and corneal targeting functions.

[0040] formula:

[0041]

[0042] Preparation:

[0043] (1) Weigh 6.0 g of moxifloxacin hydrochloride, add it to 400 ml of distilled water, heat to 50-80 ° C, stir to dissolve it, and obtain solution A;

[0044] (2) Add 1.0 g of sodium hyaluronate to solution A prepared in step (1), heat to 50-80° C., stir to dissolve it, and obtain solution B;

[0045] (3) Weigh 5.0 g of xanthan gum and 8.0 g of sodium chloride, add them to 400 ml of distilled water, stir to make them fully swell, and pass through 5 μm and 1 μm secondary filter membranes to obtain solution C;

[0046] (4) Slowly add the solution B prepared in the step (2) to the solution C prepared in the step (3), adjust the pH to 6.0 with a borate buffer solution, replenish water to 1000ml, and obtain the solution D;

[0047] (5) The solution D prepared in the step (4) was sterilized by high-pressure steam at...

Embodiment 3

[0048] Example 3: Preparation of moxifloxacin eye drops with both tear bionic and corneal targeting functions.

[0049] formula:

[0050]

[0051] Preparation:

[0052] (1) Weigh 5.45g of moxifloxacin hydrochloride, add it to 400ml of distilled water, heat to 50-80°C, stir to dissolve it, and obtain solution A;

[0053] (2) Add 2.0 g of sodium hyaluronate to solution A prepared in step (1), heat to 50-80°C, stir to dissolve, and obtain solution B;

[0054] (3) Weigh 4.0 g of xanthan gum and 7.0 g of sodium chloride, add them to 400 ml of distilled water, stir to make them fully swell, and pass through 5 μm and 1 μm secondary filter membranes to obtain solution C;

[0055] (4) Slowly add the solution B prepared in the step (2) to the solution C prepared in the step (3), adjust the pH to 8.0 with a borate buffer solution, replenish water to 1000ml, and obtain the solution D;

[0056] (5) The solution D prepared in the step (4) was sterilized by high-pressure steam at 121°C...

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Abstract

The invention discloses a moxifloxacin eye drop having both a bionic function and a targeting function and a preparation method of the moxifloxacin eye drop. Specifically, the moxifloxacin eye drop comprises the following components according to mass concentration: 5-6g / L of moxifloxacin hydrochloride, 3-5g / L of xanthan gum, 1-4g / L of sodium hyaluronate, 6-8g / L of an isoosmotic adjusting agent, and the balance of distilled water; the pH value is regulated through a pH regulator to 6.0-8.0. A xanthan gum / sodium hyaluronate gel system is creatively applied compositely to achieve both the bionic function of tears and the targeting function of a cornea; the xanthan gum has the bionic rheological property similar to that of the tear, so that higher viscosity is achieved when the shearing force is low, and the xanthan gum is evenly coated on the surface of an eyeball when the shearing force is high; the sodium hyaluronate acts on a receptor CD44 of a corneal cell, so that the cell intake is increased, and the targeting absorption is achieved. Compared with a common moxifloxacin eye drop, the moxifloxacin eye drop having both the bionic function and the targeting function has the characteristics of compatibility with the tear, no foreign-matter irritation, long residence time, higher bioavailability and the like.

Description

technical field [0001] The invention belongs to the technical field of medicine, and relates to a moxifloxacin eye drop with tear bionic and corneal targeting functions and a preparation method thereof. Background technique [0002] The ocular drug delivery system is a drug delivery system with local therapeutic characteristics. It is mainly used clinically for antibacterial, anti-inflammatory, mydriasis, anesthesia, treatment of glaucoma, and reduction of intraocular pressure. At present, ophthalmic drugs are mainly divided into eye drops, eye oils, eye ointment, subconjunctival injection and intravitreal injection. Topical instillation of drugs is the preferred way of ocular administration, but due to the innate protection of the eye against foreign substances, the bioavailability of the drug is low, and only 5% of the drug can be absorbed through the cornea . [0003] The main barriers for ocular instillation come from the three major barriers in the anterior segment: t...

Claims

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Application Information

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IPC IPC(8): A61K9/08A61K47/36A61K31/4709A61P31/04A61P27/02
CPCA61K9/08A61K9/0048A61K31/4709A61K47/36
Inventor 张真真廉云飞张军东吴剑英
Owner SHANGHAI HAOHAI BIOLOGICAL TECH
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