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Micro-emulsion/submicro-emulsion in-situ gel preparation for eyes and its making method

An in-situ gel and sub-microemulsion technology, which is used in pharmaceutical formulations, drug delivery, active ingredients of hydroxyl compounds, etc.

Inactive Publication Date: 2010-06-09
SHANGHAI INST OF MATERIA MEDICA CHINESE ACAD OF SCI
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Compared with the microemulsion in-situ gel, common gels have the following defects: ①Although common gels can increase the residence time of drugs in the eyes to exert their drug effects, there is also the phenomenon of evaporation of the drug aqueous solution, which requires frequent Drug administration can easily induce or aggravate lipid layer abnormalities; ②The viscosity is high in vitro, the fluidity is not good, and clinical medication is inconvenient; ③The viscosity is high, it is easy to produce a large number of bubbles, and industrial production and filling are inconvenient; , and does not have pseudoplastic deformation, the drug is not easy to spread evenly on the surface of the cornea and conjunctiva by blinking
[0012] air bubbles, inconvenient for industrial production and filling; ④Due to high viscosity and no pseudoplastic deformation, it is difficult for the drug to spread on the surface of the cornea and conjunctiva by blinking uniform

Method used

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  • Micro-emulsion/submicro-emulsion in-situ gel preparation for eyes and its making method
  • Micro-emulsion/submicro-emulsion in-situ gel preparation for eyes and its making method
  • Micro-emulsion/submicro-emulsion in-situ gel preparation for eyes and its making method

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0053] First, according to the composition of Example 1 given in Table 1 below, 1g VA palmitate, 1g vitamin E, 20g MCT, 10g soybean lecithin and 26g glycerin were mixed uniformly at 60°C, and then 500ml deionized water was added, Shear emulsification to obtain colostrum, and then use a high-pressure homogenizer to homogenize, and filter the prepared emulsion with a 0.45 μm microporous membrane; then dissolve 0.5 g of gellan gum in 400 ml of deionized water, stir and dissolve at 40 ° C, and Add it into the emulsion; then adjust the pH to 6.2 with a 0.3M triethanolamine solution; add 0.05g of the bacteriostatic agent benzalkonium chloride, make up to 1000ml with deionized water, and fill it.

Embodiment 2～4

[0055] Using the same preparation method as in Example 1, the microemulsion / submicroemulsion in-situ gel preparations of Examples 2-4 were prepared from the composition and process parameters given in Table 1.

[0056] Table 1 Example 1-4 Ion-sensitive microemulsion / submicroemulsion in-situ gel preparation composition and preparation process

[0057]

[0058]

Embodiment 5～7

[0060] Using the same preparation method as in Example 1, the microemulsion / submicroemulsion in-situ gel preparations of Examples 5-7 were prepared from the composition and process parameters given in Table 2.

[0061] Table 2 Example 5-7 Ion-sensitive microemulsion / submicroemulsion in-situ gel preparation composition and preparation process

[0062]

[0063]

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Abstract

An in-situ microemulsion / sub-microemulsion gel for treating eye disease is prepared from VA or its derivative, VE or its derivative, oil phase, emulsifier, thickening agent, isotonic regulator, antibacterial agent, pH regulator and purified water through shearing-high-pressure homogenizing process. It has high flowability. If it is dropped in eye, it can become hydrogel.

Description

technical field [0001] The present invention relates to an ophthalmic microemulsion / submicroemulsion in-situ gel preparation and a preparation method thereof, more specifically, to an ophthalmic microemulsion containing vitamin A or its derivatives and vitamin E or its derivatives / Submicroemulsion in situ gel preparation and preparation method thereof. Background technique [0002] Dry eye is one of the common diseases in ophthalmology clinic. The main symptoms are foreign body sensation, burning sensation and general eye discomfort. These discomforts are typically described as scratching, dry eyes, pain, grittiness, stinging or burning. [0003] The treatment of dry eye is usually to use artificial tears as an alternative treatment, that is, to use imitation artificial tears to form a new tear film with normal structure on the surface of the eyeball, so as to relieve the above-mentioned various discomfort symptoms. [0004] At present, artificial tears or drugs similar...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K9/00A61K31/07A61K31/355A61P27/02
Inventor 甘勇甘莉马守伟朱春柳
Owner SHANGHAI INST OF MATERIA MEDICA CHINESE ACAD OF SCI
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