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Nano lipid cubic crystal preparation and its preparation method and application

A nano-lipid and cubic technology, applied in the field of medicine, can solve the problems of mild hyperemia of palpebrae and conjunctiva, unacceptable greasy feeling, and increased oil oxidation value, so as to improve corneal penetration, increase eye comfort, and biological good compatibility

Inactive Publication Date: 2011-12-14
SECOND MILITARY MEDICAL UNIV OF THE PEOPLES LIBERATION ARMY
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0005] Because cyclosporine A is almost insoluble in water, cyclosporine A is usually dissolved in sterile olive oil, castor oil or peanut oil clinically, but the greasy feeling produced during administration makes patients unacceptable, and it has been reported that the oil solution can cause Mild conjunctiva hyperemia; rabbit eye dermatitis and hair loss occurred after instillation, which can be recovered after drug withdrawal; and it has been reported that due to the increase of oil oxidation value, the effective period of such preparations is less than 4 weeks
In recent years, there have been research reports on the use of cubic crystal carriers for intravenous administration, oral administration, oral mucosal administration, and transdermal administration, but so far there has been no research on lipid-soluble drugs such as cyclosporin A Public reports on preparations for ophthalmic administration of nanolipid cubic crystals

Method used

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  • Nano lipid cubic crystal preparation and its preparation method and application
  • Nano lipid cubic crystal preparation and its preparation method and application
  • Nano lipid cubic crystal preparation and its preparation method and application

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0038] Example 1 Preparation of cyclosporine A nano lipid cubic crystal preparation

[0039] A cyclosporine A nano lipid cubic crystal preparation is prepared, and the finished product contains 1% cyclosporine A (W / W).

[0040] Preparation method: Add 1 g of poloxamer 407 to 9 g of glycerol monooleate and melt at 40°C to form an oil phase, add 2 g of cyclosporin A to the oil phase, continue heating at 40°C and vibrate to promote drug dissolution; wait until the drug is completely After dissolving, add 188g of water preheated to 40°C, stir and mix quickly, first 10000rpm high-speed shear homogenization (FJ 200-S digital display high-speed dispersion homogenizer, Shanghai Specimen Model Factory) for 1min, and then 200bar high-pressure homogenization (EM-C3 High Pressure Homogenizer, Avestin Canada) 3 cycles. Add appropriate amount of antibacterial agent, acid-base regulator, viscosity regulator, osmotic pressure regulator and other commonly used auxiliary materials for eye drop...

Embodiment 2

[0041] Example 2 Preparation of cyclosporine A nano lipid cubic crystal preparation

[0042] A cyclosporine A nano lipid cubic crystal preparation is prepared, and the finished product contains 0.01% cyclosporine A (W / W).

[0043] Preparation method: add 0.05g polyvinyl alcohol to 0.5g glycerol monooleate and melt at 40°C to form an oil phase, add 0.1g cyclosporin A to the oil phase, continue heating at 40°C and vibrate to promote drug dissolution; wait for the drug After completely dissolving, add 200g of water preheated at 40°C, stir rapidly and mix well, first 10000rpm high-speed shear homogenization (FJ 200-S digital display high-speed dispersion homogenizer, Shanghai Specimen Model Factory) for 1min, and then 200bar high-pressure homogenization (EM-C3 high-pressure homogenizer, Avestin Canada) for 3 cycles, then add water to 1000g, and mix well. Add appropriate amount of antibacterial agent, acid-base regulator, viscosity regulator, osmotic pressure regulator and other com...

Embodiment 3

[0044] Example 3 Preparation of Cyclosporine A Nano Lipid Cubic Crystal Preparation

[0045] The cyclosporine A nano lipid cubic crystal preparation is prepared, and the finished product contains 2% cyclosporine A (W / W).

[0046] Preparation method: add 7g poloxamer 407 to 70g glycerol monooleate and melt at 40°C to form an oil phase, add 4g cyclosporine A to the oil phase, continue heating at 40°C and vibrate to promote drug dissolution; wait until the drug is completely After dissolving, add 119g of water preheated at 40°C, stir and mix quickly, and homogenize at 10000rpm high-speed shear for 5min. Add appropriate amount of antibacterial agent, acid-base regulator, viscosity regulator, osmotic pressure regulator and other commonly used auxiliary materials for eye drops to obtain the nano lipid cubic crystal preparation.

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Abstract

The invention discloses a nanometer lipid cubic crystal preparation, which comprises fat-soluble medicine, amphiphilic lipid, stabilizer and water. The invention also discloses a preparation method of the nanometer lipid cubic crystal preparation and an application of the nanometer lipid cubic crystal in preparation of an ophthalmic drug preparation for treating ophthalmic diseases. The nano lipid cubic crystal preparation of the present invention can significantly improve the corneal penetration ability of drugs, has better stability than liposomes and nanoparticles, can realize high-pressure high-temperature sterilization, has good drug release characteristics, and has broad clinical applications and market prospects.

Description

technical field [0001] The invention relates to the technical field of medicine, in particular to a nano lipid cubic crystal preparation and its preparation method and application. Background technique [0002] At present, there are still many problems in the clinical use of drugs for ophthalmic diseases. Taking cyclosporine A (cyclosporine, cyclosporine A, Cyclosporine A, CysA) as an example, the main clinical application of cyclosporine A in the eye For corneal transplant rejection, keratoconjunctiva sicca, Behcet's syndrome and hormone-dependent bullous keratoconjunctivitis. After systemic administration of cyclosporine A, it is difficult for the drug to enter the eye due to the existence of the "blood-ocular barrier": oral administration of 5 mg.Kg -1 .day -1 The average aqueous humor concentration after cyclosporine A was only 28ng.mL -1 , is 13% of the blood concentration. In addition, systemic administration is not only expensive, but also may cause complications ...

Claims

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Application Information

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IPC IPC(8): A61K9/10A61K45/08A61P27/02
Inventor 陈琰高申钟延强王庆平陈建明鲁莹邹豪
Owner SECOND MILITARY MEDICAL UNIV OF THE PEOPLES LIBERATION ARMY
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