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Cation-modified pilocarpine hydrochloride flexible nano-liposome eye-drops preparation and preparation method thereof

A nano-lipid and cation technology, applied in the field of medicine, can solve the problems of short eye retention time and poor corneal permeability, and achieve the effects of changing the physical and chemical properties of drugs, increasing the permeability, and reducing the elimination rate.

Active Publication Date: 2018-05-04
TIANJIN UNIV OF TRADITIONAL CHINESE MEDICINE
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0003] The common dosage form of pilocarpine hydrochloride is eye drops, which has the disadvantages of short residence time in the eye and poor corneal permeability.

Method used

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  • Cation-modified pilocarpine hydrochloride flexible nano-liposome eye-drops preparation and preparation method thereof
  • Cation-modified pilocarpine hydrochloride flexible nano-liposome eye-drops preparation and preparation method thereof
  • Cation-modified pilocarpine hydrochloride flexible nano-liposome eye-drops preparation and preparation method thereof

Examples

Experimental program
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Effect test

Embodiment 1

[0033] The preparation method of the cation-modified pilocarpine hydrochloride flexible nano-liposome ophthalmic preparation comprises the following steps:

[0034] (1) Put 400mg of lecithin and 20mg of cholesterol in 20mL of chloroform, and sonicate for 4min to obtain a suspension; Solution 1 was obtained in methanol;

[0035] (2) Mix the suspension and the solution evenly, and remove the organic solvent by rotary evaporation at 40° C. until a uniform lipid film is formed at the bottom of the container;

[0036] (3) 25 mg sodium deoxycholate was dissolved in pure water to obtain solution 2, and the lipid film was dissolved in solution 2 to obtain a mixed primary emulsion;

[0037] (4) Under the condition of a power of 150W, the mixed primary emulsion was ultrasonicated for 60 minutes, and warmed at 60° C. for 0.5 hours to obtain a flexible nanoliposome preparation of pilocarpine hydrochloride;

[0038] (5) 20mgN-trimethyl chitosan (degree of quaternization≥60%) is dissolved...

Embodiment 2

[0041] The preparation method of the cation-modified pilocarpine hydrochloride flexible nano-liposome ophthalmic preparation comprises the following steps:

[0042] (1) Put 400mg of lecithin and 20mg of cholesterol in 20mL of chloroform, and sonicate for 3 minutes to obtain a suspension; dissolve 10mg of pilocarpine hydrochloride and 0.3mg of Labrasol (caprylic capric acid macrogolglyceride PEG-8) in 10mL of methanol get solution one;

[0043] (2) Mix the suspension and the solution evenly, and remove the organic solvent by rotary evaporation at 45° C. until a uniform lipid film is formed at the bottom of the container;

[0044] (3) 25mg sodium cholate was dissolved in pure water to obtain solution two, and the lipid film was dissolved in solution two to obtain a mixed primary emulsion;

[0045] (4) Under the condition of a power of 200W, the mixed primary emulsion was sonicated for 10 minutes, and warmed at 25° C. for 2 hours to obtain a flexible nanoliposome preparation of ...

Embodiment 3

[0049] The preparation method of the cation-modified pilocarpine hydrochloride flexible nano-liposome ophthalmic preparation comprises the following steps:

[0050] (1) Put 400mg of lecithin and 20mg of cholesterol in 10mL of chloroform, and sonicate for 4 minutes to obtain a suspension; dissolve 5mg of pilocarpine hydrochloride and 0.1mg of Transcutol HP (diethylene glycol monoethyl ether) in 10mL of methanol to obtain solution 1 ;

[0051] (2) Mix the suspension and the solution evenly, and remove the organic solvent by rotary evaporation at 35° C. until a uniform lipid film is formed at the bottom of the container;

[0052] (3) 12mg of 1,2 propylene glycol was dissolved in pure water to obtain solution two, and the lipid film was dissolved in solution two to obtain a mixed primary emulsion;

[0053] (4) Under the condition of a power of 100W, the mixed primary emulsion was ultrasonicated for 50 minutes, and warmed at 30° C. for 1 hour to obtain a flexible nanoliposome prep...

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Abstract

The invention discloses a cation-modified pilocarpine hydrochloride flexible nano-liposome eye-drops preparation and a preparation method thereof. The preparation method comprises the following steps:(1) adding lecithin and cholesterol into chloroform, and performing ultrasonic treatment to obtain suspension; and dissolving pilocarpine hydrochloride and a penetration enhancer in methanol to obtain a solution I; (2) uniformly mixing the suspension and the solution I, and removing an organic solvent to obtain a uniform lipid membrane; (3) dissolving a softener into purified water to obtain a solution II, and dissolving the lipid membrane into the solution II so as to obtain primary mixed emulsion; (4) performing ultrasonic treatment on the primary mixed emulsion, and adding into a warm bathso as to obtain a pilocarpine hydrochloride flexible nano-liposome preparation; and (5) dissolving a cationic material into the purified water to obtain a solution III, stirring the pilocarpine hydrochloride flexible nano-liposome preparation, dropping the solution III, and stirring, thereby obtaining the eye-drops preparation in the invention. The preparation disclosed by the invention has hugemembrane surface area and high adhesion, and the drug penetration is increased. The eye-drops preparation has excellent biocompatibility and low eye irritation.

Description

technical field [0001] The invention relates to the field of medicine, in particular to a cation-modified pilocarpine hydrochloride flexible nano-liposome ophthalmic preparation and a preparation method. Background technique [0002] Glaucoma is a slowly progressive degeneration of retinal ganglion cells and optic nerve axons that can lead to irreversible blindness if undiagnosed or untreated. Glaucoma is the second leading cause of blindness worldwide, accounting for 12.3% of all blindness. Modern studies have shown that pilocarpine hydrochloride has obvious effects of lowering intraocular pressure and controlling inflammation, and can treat primary glaucoma, including open-angle and angle-closure glaucoma, and is the first-line drug for clinical treatment of glaucoma. [0003] The commonly used dosage form of pilocarpine hydrochloride is eye drops, which has the disadvantages of short ocular residence time and poor corneal permeability. [0004] Advances in drug delivery...

Claims

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Application Information

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IPC IPC(8): A61K9/127A61K31/4178A61K47/36A61P27/06
CPCA61K9/0048A61K9/127A61K31/4178A61K47/36
Inventor 刘睿赵芳金鑫王佳露王泽
Owner TIANJIN UNIV OF TRADITIONAL CHINESE MEDICINE
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