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Drug sustained-release gel for subconjunctival implantation and preparation method of drug sustained-release gel

A slow-release gel and drug technology, which is applied to the drug slow-release gel implanted under the conjunctiva and the field of preparation thereof, can solve the problems of tissue trauma, unfavorable antibacterial and anti-inflammatory treatment, tissue toxicity and the like

Pending Publication Date: 2021-09-07
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

Although subconjunctival drug injection after ophthalmic surgery is relatively simple and convenient, the abundant blood vessels in the conjunctiva will guide a large amount of drugs (>60%) into the systemic circulation and be rapidly eliminated by metabolism
Repeated injections under the conjunctiva will cause new tissue trauma, which is not conducive to postoperative antibacterial and anti-inflammatory treatment
Large doses of drugs continue to enter the systemic circulation and cause unnecessary tissue toxicity

Method used

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  • Drug sustained-release gel for subconjunctival implantation and preparation method of drug sustained-release gel
  • Drug sustained-release gel for subconjunctival implantation and preparation method of drug sustained-release gel
  • Drug sustained-release gel for subconjunctival implantation and preparation method of drug sustained-release gel

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0040] This example provides a drug slow-release gel for subconjunctival implantation and a preparation method thereof.

[0041] The drug sustained-release gel includes levofloxacin, prednisolone and an injectable composite gel carrier. Wherein, the injectable composite gel carrier includes polylactic acid-glycolic acid copolymer-polyethylene glycol-polylactic acid-glycolic acid triblock copolymer nanomicelle; the levofloxacin and prednisolone are uniformly dispersed in In the nanomicelle. Table 1 lists the drug sustained-release gel drug and dispersion of the present embodiment. As shown in Table 1, according to the mass percentage, the proportion of prednisolone is 0.25% (w / w), the proportion of levofloxacin is 0.15% (w / w), and the concentration of triblock copolymer is 25% (w / w). ).

[0042] The preparation method of the drug slow-release gel for subconjunctival implantation provided by this embodiment comprises the following steps:

[0043] Disperse levofloxacin (1.5 m...

Embodiment 2

[0046] This example provides a drug slow-release gel for subconjunctival implantation and a preparation method thereof.

[0047] The drug sustained-release gel includes levofloxacin, prednisolone and an injectable composite gel carrier. Wherein, the injectable composite gel carrier includes polylactic acid-glycolic acid copolymer-polyethylene glycol-polylactic acid-glycolic acid triblock copolymer nanomicelles and metal hydroxide nanoparticles, and the levofloxacin and Prednisolone is uniformly dispersed in the nanoparticles. Table 1 lists the drug sustained-release gel drug and dispersion of the present embodiment. As shown in Table 1, according to the mass percentage, the proportion of prednisolone is 0.15% (w / w), and the proportion of levofloxacin is 0.15% (w / w), which is used to load the metal hydroxide of prednisolone and levofloxacin The concentration of nanoparticle was 2.0% (w / w), the concentration of copolymer was 22% (w / w), and the proportion of composite gel as ca...

Embodiment 3

[0053] This example provides a drug slow-release gel for subconjunctival implantation and a preparation method thereof.

[0054] The drug sustained-release gel includes levofloxacin, prednisolone and an injectable composite gel carrier. This embodiment focuses on the slow delivery of anti-inflammatory and antibacterial drugs at the same time, so the anti-inflammatory drug prednisolone and the antibacterial drug levofloxacin are simultaneously loaded in porous silica nanoparticles, and then the drug-loaded nanoparticles are dispersed in polylactic acid-hydroxyl Acetic acid copolymer-polyethylene glycol-polylactic acid-glycolic acid triblock copolymer nanomicelles. Porous silica nanoparticles such as image 3 shown.

[0055] Table 1 lists the drug sustained-release gel drug and dispersion of the present embodiment. As shown in Table 1, according to the mass percentage, the proportion of levofloxacin is 0.1% (w / w), and the proportion of prednisolone is 0.15% (w / w). The concen...

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Abstract

The invention provides a drug sustained-release gel for subconjunctival implantation and a preparation method of the drug sustained-release gel, and belongs to the field of drugs and drug preparation. According to the preparation method, levofloxacin and prednisolone are taken as main drug components, drug molecules are protected and stabilized through nano particles and polymer nano-micelles, and solution injection under conjunctiva, liquid and semi-solid conversion and lasting and slow release of drugs are realized by utilizing the temperature sensitivity of a composite drug sustained-release system; and the composite drug sustained-release system is liquid at low temperature in vitro, and is gradually converted into a semi-solid state due to contact with the body temperature when being injected into the subconjunctiva, so that the sustained-release capability of the drug property is effectively prolonged, and stable and long-acting drug administration can be realized. When the drug sustained-release gel is used for administration, not only can the drug be quickly and conveniently administered, but also the flat gel can be quickly, timely, hygienically, reliably and effectively formed under the conjunctiva, so that the antibacterial and anti-inflammatory effects of the antibacterial drug and the anti-inflammatory drug can be well and stably exerted.

Description

technical field [0001] The invention belongs to the field of medicine and medicine preparation, and in particular relates to a medicine slow-release gel for subconjunctival implantation and a preparation method thereof. Background technique [0002] Ophthalmic medications to prevent postoperative eye bacterial infection or inflammation usually include eye drops, eye ointments, and eye gels. Among them, the drug residence time of ophthalmic gel is between eye drops and eye ointment, and it is usually used as an eye drop preparation. Although the ophthalmic gel of the eye drop preparation is simple and convenient to use, the residence time is relatively short and the number of administrations is high, which will still cause low patient compliance. [0003] In the prior art, another commonly used ophthalmic medication method is subconjunctival drug injection. Although subconjunctival drug injection after ophthalmic surgery is relatively simple and convenient, the abundant blo...

Claims

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Application Information

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IPC IPC(8): A61K9/06A61K45/06A61K31/573A61K47/34A61K9/107A61K47/69A61P27/02A61P31/02A61P31/04A61P29/00A61K31/5383
CPCA61K9/0051A61K9/06A61K45/06A61K47/34A61K31/5383A61K31/573A61P31/02A61P31/04A61P27/02A61P29/00A61K47/6923A61K9/1075A61K2300/00
Inventor 张少华孙建国卢奕邓勇辉竺向佳李丹方艳文
Owner EYE & ENT HOSPITAL SHANGHAI MEDICAL SCHOOL FUDAN UNIV
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