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Method for preparing pH sensitive in-situ gel nano slow-release eye drop

An in-situ gel and slow-release eye technology, applied in the field of pharmaceuticals, can solve problems such as short duration, low bioavailability of drugs, frequent administration, etc., to increase permeability, prolong drug action time, and reduce adverse reactions Effect

Inactive Publication Date: 2013-04-17
广州悦新生物科技有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, with the development of biopharmaceuticals and the deepening of ocular pharmacokinetic research, it is found that solution-type eye drops have problems such as short duration, low drug bioavailability and the need for frequent administration; and due to the inconvenience of nighttime administration , which makes the pharmacological peak and valley phenomenon prominent

Method used

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  • Method for preparing pH sensitive in-situ gel nano slow-release eye drop

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Experimental program
Comparison scheme
Effect test

Embodiment 1

[0026] (1) Take by weighing 100mg poly(lactic acid-glycolic acid) copolymer (average molecular weight is 30000, and LA:GA copolymerization ratio is 50:50 in the molecular chain segment) is dissolved in 5ml dichloromethane and makes organic phase; With 30mg levofloxacin Dissolve in 0.3ml of distilled water to make the water phase; add the water phase to the organic phase, and obtain an emulsion after ultrasonication for 1 minute; add the emulsion dropwise to 100ml of polyethylene glycol 1000 vitamin E succinate with a mass fraction of 0.025% In the aqueous solution, stir at 800rpm for 6 hours; centrifuge at 2000rpm to remove large particles of impurities and aggregates, filter with an ultrafiltration tube at 5000rpm, and wash with water for 3 times to remove the emulsifier to obtain nanoparticles loaded with levofloxacin.

[0027] (2) Weigh 0.15g of hydroxypropyl methylcellulose and dissolve it in 40ml of distilled water, and let it stand overnight at 4°C to obtain a clear solut...

Embodiment 2

[0031] (1) Weigh 100mg of poly(lactic acid-glycolic acid) copolymer (the average molecular weight is 30000, and the LA:GA copolymerization ratio in the molecular segment is 50:50) and dissolve it in 5ml of methylene chloride to make an organic phase; Dissolve ciclovir in 0.2ml of distilled water to make water phase; add the water phase to the organic phase, and obtain an emulsion after ultrasonication for 1 minute; add dropwise the emulsion to 100ml of 0.025% polyethylene glycol 1000 vitamin E In the succinate aqueous solution, stir at 800rpm for 6 hours; centrifuge at 2000rpm to remove large particles of impurities and agglomerates, filter with an ultrafiltration tube at 5000rpm, and wash with water for 3 times to remove the emulsifier to obtain nanoparticles loaded with levofloxacin.

[0032] (2) Weigh 0.01g of hydroxypropyl methylcellulose and dissolve it in 40ml of distilled water, and let it stand overnight at 4°C to obtain a clear solution; weigh 0.5g of polyacrylic acid ...

Embodiment 3

[0036](1) Weigh 100mg poly(lactic acid-glycolic acid) copolymer (average molecular weight is 30000, LA:GA copolymerization ratio in molecular segment is 50:50) and dissolve in 5ml N'N'-dimethylformamide to prepare into an organic phase; dissolve 20mg of dexamethasone in 0.2ml of absolute ethanol to make an aqueous phase; add the aqueous phase to the organic phase, and obtain an emulsion after ultrasonication for 1 minute; add the emulsion dropwise to 100ml with a mass fraction of 0.025% In polyethylene glycol 1000 vitamin E succinate aqueous solution, stir at 800rpm for 6 hours; centrifuge at 2000rpm to remove large particles of impurities and agglomerates, filter with an ultrafiltration tube at 5000rpm, wash with water for 3 times to remove emulsifiers and obtain nanoparticles loaded with levofloxacin medicine.

[0037] (2) Weigh 0.25g of hydroxypropyl methylcellulose and dissolve it in 40ml of distilled water, and let it stand overnight at 4°C to obtain a clear solution; weig...

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Abstract

The invention discloses a method for preparing pH sensitive in-situ gel nano slow-release eye drop, which comprises the following steps of: wrapping ophthalmic medicaments in nano particles by using an emulsifying method to prepare medicament slow-release carriers, dispersing the medicament slow-release carriers in a pH sensitive liquid medium, and regulating the pH value, the osmotic pressure value and the like to obtain the pH sensitive in-situ gel nano slow-release eye drop. The eye drop prepared by the method has good pH sensitivity, biological adhesiveness and medicament long-acting slowrelease; the in vitro pH value is 4.0 to 4.5; the eye drop is liquid with good mobility and low viscosity; after the eye drop is dropped into the eye, the pH value is raised to about 7.4, the liquid preparation is quickly gelled in situ, the nano particle medicament carriers are immobilized therein and medicaments are slowly released, so the detention time of the medicaments in the eye can be increased, the bioavailability of the medicaments is improved, the frequency of eye medicament administration is reduced, and the eye drop has low stimulus at the same time.

Description

technical field [0001] The invention belongs to the technical field of medicines. It relates to a preparation method of pH-sensitive in-situ gel nano-sustained-release eye drops, in particular to a method of encapsulating ophthalmic drugs in polymer-based nanoparticles and dispersing them in a pH-sensitive in-situ gel liquid medium to obtain pH Preparation method of sensitive in-situ gel nano sustained-release eye drops. Background technique [0002] With the development of society and the acceleration of industrialization, the air quality in which human beings live is polluted, coupled with the popularization of modern technological video terminals, the incidence of ophthalmic diseases is increasing year by year. Among them, glaucoma, cataract, ocular infectious inflammation and dry eye are common ophthalmic diseases. The dosage form adopted for traditional ophthalmic administration is solution type eye drops. Because of its simple preparation process, low price and easy...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K9/00A61K47/32A61K47/34A61K47/38A61P27/02A61P27/06A61P27/12A61K47/14
Inventor 魏坤凌友
Owner 广州悦新生物科技有限公司
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