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Block polymer for eyes

A technology of block polymers and di-block polymers, applied in drug combinations, medical preparations of non-active ingredients, sensory diseases, etc., can solve the problems of low corneal permeability and low bioavailability, and reduce side effects , improve curative effect, improve the effect of utilization

Inactive Publication Date: 2007-12-05
涂家生 +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

In general, the low corneal permeability of the drug, the rapid washing of tears, and the absorption into the conjunctiva are the reasons for the low intraocular bioavailability of common eye drops

Method used

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  • Block polymer for eyes

Examples

Experimental program
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Effect test

Embodiment 1

[0044] Embodiment 1 This embodiment is the preparation of ophthalmic pirenzepine polymer micelle gel

[0045] Materials and Methods

[0046] D, L-lactide: purchased from Sigma, recrystallized three times with anhydrous ethyl acetate at 60°C before use, and at room temperature in P 2 o 5 Dry under medium vacuum for 24 hours. Both stannous octoate and methyl polyethylene glycol (molecular weight 2000) were purchased from Sigma Company.

[0047] 1. Synthesis of methyl polyethylene glycol-polylactic acid (mPEG-PLA) diblock polymer:

[0048] The ring-opening polymerization method was used to prepare methyl polyethylene glycol-polylactic acid block polymers with a mass ratio of 75 / 25. That is: Weigh 7.5g of methyl polyethylene glycol and 2.5g of lactide, place them in a closed reactor, raise the temperature to 120-140°C under nitrogen flow to melt the solid, add 50mg of stannous octoate, and raise the temperature Reaction at 150-180°C for 3-6 hours. After cooling, a white soli...

Embodiment 2

[0057] Embodiment 2 This embodiment is the isolated corneal penetration experiment of ophthalmic pirenzepine polymer micelle gel

[0058] Rabbits were taken and anesthetized to death. The eyeballs were enucleated and placed in the center. Make a transverse cut along the sclera 2 mm from the corneal edge to separate the cornea. The lens, vitreous body and other tissues at the back of the eyeball were removed, and the iris was peeled off to obtain a cornea with a 2mm scleral ring. Corneal permeation experiments were started within 20 min after the animals were sacrificed. Adopt osmotic diffusion device, including supply pool and accept pool, maintain the shape of the isolated cornea and fix it between the two pools, so that the epithelial layer faces the supply pool. Add pirenzepine hydrochloride to be dissolved in the gel 2mL that diluent obtains in embodiment 1 in the supply pool or ophthalmic pirenzepine polymer micelle gel, accept the pool to be Ringer's solution, and who...

Embodiment 3

[0063] Example 3 Pharmacokinetics of pirenzepine polymer micellar gel, eye drops in rabbit aqueous humor

[0064] The 40 rabbits were randomly divided into 8 groups according to the sampling time, with 5 rabbits in each group. The prescription was changed every two weeks for a total of 2 times (pirenzepine hydrochloride ophthalmic gel and pirenzepine polymer micelles ophthalmic gel, respectively). During the administration, 2 drops (100 μL) of the prepared pirenzepine eye drops were dripped in the conjunctival sac of one eye respectively, and no medicine was used in the left eye. At 0.5, 1, 2, 4, 8, 12, 24, and 48 hours after eye drops, 0.2ml of aqueous humor was drawn from the right eye at 8 time points in total. Take 0.1 mL of aqueous humor, add 0.1 mL of methanol, and vortex to mix to precipitate proteins and impurities. Centrifuge at a speed of 16000r / min for 10min, take the supernatant, inject it into a high-performance liquid chromatograph, record the peak area, and ca...

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Abstract

A block copolymer used as the carrier of ocular medicine is composed of hydrophilic polyethylene glycol methyleter (mPEG) and hydrophobic polylactic acid (PLA) or polyglycollin acid (PGA) or glycollide-lactide polymer (PLGA).

Description

Technical field: [0001] The present invention relates to the ophthalmic use of a block polymer composed of two polymers (A, B) fragments, wherein the A and B fragments in the polymer are respectively hydrophilic polymer-polyethylene glycol methyl ether (mPEG) and hydrophobic polymers - polylactic acid (PLA) or polyglycolic acid (PGA) or glycolide-lactide polymer (PLGA), block polymers can be AB type diblock polymers or multi-block polymers things. This is suitable for intraocular administration. Background technique: [0002] Intraocular administration is an important administration method for the treatment of eye diseases, and intraocular preparations include eye drops, ophthalmic gels, etc. At present, ophthalmic preparations can be divided into: 1) preparations that should enter the eye through the cornea, such as pirenzepine hydrochloride as an M1 receptor blocker, which can prevent the further development of myopia. In the eye, it is necessary for pirenzepine to ente...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K47/34A61P27/02
Inventor 涂家生吴建梅
Owner 涂家生
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