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

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...

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