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Slow-release eye drops and preparation method thereof

A technology for sustained-release eye drops and sustained-release drugs, which is applied in the directions of pharmaceutical formulations, medical preparations containing inactive ingredients, and medical preparations containing active ingredients, and achieves the effects of simple preparation method, convenient use and low cost

Inactive Publication Date: 2020-12-04
EYE & ENT HOSPITAL SHANGHAI MEDICAL SCHOOL FUDAN UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

So far, no suitable sustained-release eye drops have been used clinically

Method used

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  • Slow-release eye drops and preparation method thereof
  • Slow-release eye drops and preparation method thereof
  • Slow-release eye drops and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0053] A sustained-release eye drop comprising sustained-release drug 1 and dispersion liquid 2. Such as Figure 3a As shown, the sustained-release drug 1 comprises an ophthalmic drug 10 and a sustained-release carrier. The slow-release carrier includes: nanoparticles 21 and a surface function modification layer 22 . Wherein, the nanoparticle 21 is selected metal hydroxide nanoparticle, and its SEM picture is as follows Figure 3b Shown; the biological material constituting the surface function modification layer 22 is sodium hyaluronate. The ophthalmic drug 10 loaded on the sustained-release carrier is a small-molecule integrin antagonist, and its loading amount in the sustained-release carrier accounts for 2% of the total mass of the sustained-release drug 1 .

[0054] The preparation method of sustained-release eye drops of the present invention comprises:

[0055] Step 1, using a hydrothermal method to synthesize metal hydroxide nanoparticles, specifically including: p...

Embodiment 2

[0060] A kind of sustained-release eye drops, wherein, described nanoparticle 21 selects montmorillonite nanoparticle, and its SEM figure is as follows Figure 4a As shown; due to the serious agglomeration of montmorillonite, the outline of nanoparticles in the SEM image is not very clear. The biological material constituting the surface functional modification layer 22 is cationic gelatin; the structural representation of montmorillonite nanoparticles, surface functional modification layer and drug loading is as follows: Figure 4b shown. The ophthalmic drug 10 loaded on the sustained-release carrier is an anti-inflammatory drug dexamethasone;

[0061] In the preparation process, first synthesize montmorillonite nanoparticles, then use cationic gelatin to modify montmorillonite nanoparticles by physical adsorption, and then load dexamethasone (dexamethasone) in the surface-modified montmorillonite nanoparticles, The drug-loaded solid powder is obtained by freeze-drying; fin...

Embodiment 3

[0066] A sustained-release eye drop, the nanoparticles 21 are metal hydroxide nanoparticles; the biological material forming the surface function modification layer is sodium alginate; the ophthalmic drug loaded by the sustained-release carrier is levofloxacin (levofloxacin) ; The loading amount of the ophthalmic drug in the sustained-release carrier accounts for 1.5% of the total mass of the sustained-release drug.

[0067] In the preparation process, metal hydroxide nanoparticles were first prepared by hydrothermal synthesis, and then sodium alginate was used to modify metal hydroxide nanoparticles by physical adsorption, and then levofloxacin was loaded on the surface-modified metal Hydroxide nanoparticles are freeze-dried to obtain drug-loaded solid powder; finally, the solid sustained-release drug powder is sterilized, and together with the dispersion, are packaged in dry-wet separation eye drop bottles.

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Abstract

The invention discloses slow-release eye drops and a preparation method thereof. The slow-release eye drops comprise a slow-release drug and a dispersion liquid for dispersing the slow-release drug, wherein the slow-release drug is composed of an eye drug and a slow-release carrier; the slow-release carrier is a composite nano material and comprises nano particles and a surface function modification layer connected to the outer parts of the nano particles; a plurality of communicated gaps are formed among the nano particles and are used for loading or conveying the eye drug; and the surface function modification layer is connected or disconnected with the nano particles to control the release and diffusion speeds of the loaded eye drug. The stable release of the loaded drug is realized ina gradual degradation process of a carrier material by the communicated gaps with a layered structure of the composite nano material and the surface function modification layer. The slow-release eye drops have the advantages of simple preparation method and low cost, can efficiently and stably release the drug and are convenient to stably store for a long period; a patient can simply and conveniently use the slow-release eye drops according to self illness conditions; and the slow-release eye drops technology can be used for dosing eye surfaces, lacrimal passages and eyes.

Description

technical field [0001] The invention belongs to the technical field of biomedicine, and relates to a slow-release eye drop and a preparation method thereof. Background technique [0002] The local treatment of eye diseases is mainly based on eye drops. However, the bioavailability of conventional eye drops is very limited, and more than 95% of the drugs cannot enter the eyes, and the drugs entering the systemic circulation will also cause certain adverse reactions. The bioavailability of eye drops is very important. [0003] On the other hand, long-term and frequent ocular surface administration will also lead to poor patient compliance, and only 31%-67% of patients can persist in using it for 12 months, which seriously affects the therapeutic effect. However, the treatment of eye diseases, especially the treatment of chronic eye diseases, often ends up in a state of protracted treatment and relapse. [0004] Therefore, the bioavailability and patient compliance of eye dro...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/08A61K45/00A61K47/59A61K47/60A61K47/61A61K47/62A61K47/69A61P27/02
CPCA61K47/6949A61K47/61A61K47/60A61K47/593A61K47/62A61K45/00A61K9/0048A61K9/08A61P27/02
Inventor 孙兴怀孙建国吴继红张圣海赵玉瑾杨金玲
Owner EYE & ENT HOSPITAL SHANGHAI MEDICAL SCHOOL FUDAN UNIV