Preparation method for intraocular medicine delivery system of polyacrylic resin wrapping montmorillonite loading medicine

A technology of polyacrylic acid resin and drug delivery system, applied in the field of medicine, can solve the problems of drug liquid retention, low bioavailability, short-term, etc., and achieve the effects of improving absorption and utilization, simple and convenient operation, and small particle size

Inactive Publication Date: 2019-04-19
GUANGDONG PHARMA UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, due to the special structure and physiological factors of the eye, there are many limitations in ocular anatomy and physiology (such as tear secretion and flow, nasolacrimal duct elimination, blood-aqueous barrier, blood-ocular barrier, blood-retinal barrier, etc. ), after the eye drops are instilled into the eyes, the time for the liquid to stay in the tear film is very short, so that the effective amount of the drug that can reach the intraocular tissue is only 1% to 5% of the administered dose, so the bioavailability is very low. Low (typically <5%)

Method used

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  • Preparation method for intraocular medicine delivery system of polyacrylic resin wrapping montmorillonite loading medicine
  • Preparation method for intraocular medicine delivery system of polyacrylic resin wrapping montmorillonite loading medicine
  • Preparation method for intraocular medicine delivery system of polyacrylic resin wrapping montmorillonite loading medicine

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0036] (1) Place the montmorillonite in 5v / v% sulfuric acid, acidify it in a water bath at 70°C for 0.5h, wash it with double distilled water to neutrality, treat it ultrasonically to reduce the particle size, and obtain the acidified montmorillonite after drying. Acid-activated modified montmorillonite;

[0037] Prepare an aqueous solution of betaxolol hydrochloride (BH) with a concentration of 3g / L, add acidified montmorillonite whose weight is 1 / 3 of the weight of BH, adjust the pH to 4, absorb in a water bath at 50°C for 6h, centrifuge, and dry to obtain Montmorillonite-betaxolol hydrochloride compound (i.e. drug-loaded montmorillonite);

[0038] (2) Accurately weigh 425.6mg RL PO, 22.4mg Put RS PO, 56mg BH in a test tube, add 5mL of absolute ethanol, ultrasonically dissolve at 50°C, after it is completely dissolved, add 5mg of montmorillonite-betaxolol hydrochloride complex to obtain an organic phase;

[0039] Another 1% poloxamer 188 solution was taken as the water ...

Embodiment 2

[0043] (1) Place the montmorillonite in 5v / v% sulfuric acid, acidify it in a water bath at 70°C for 0.5h, wash it with double distilled water to neutrality, treat it ultrasonically to reduce the particle size, and obtain the acidified montmorillonite after drying. Acid-activated modified montmorillonite;

[0044] Prepare an aqueous solution of betaxolol hydrochloride (BH) with a concentration of 3g / L, add acidified montmorillonite whose weight is 1 / 3 of the weight of BH, adjust the pH to 4, absorb in a water bath at 50°C for 6h, centrifuge and dry, and prepare Demontmorillonite-betaxolol hydrochloride compound (i.e. drug-loaded montmorillonite);

[0045] (2) Accurately weigh 425.6mg RL PO, 22.4mg RS PO, 56mgBH in a test tube, add 5mL of acetone, ultrasonically dissolve at 50°C, after it is completely dissolved, add 5mg of montmorillonite-betaxolol hydrochloride complex to obtain an organic phase;

[0046] (3) Take another 1% poloxamer 188 solution as the water phase;

[...

Embodiment 3

[0049] (1) Place the montmorillonite in 5v / v% sulfuric acid, acidify it in a water bath at 70°C for 0.5h, wash it with double distilled water to neutrality, treat it ultrasonically to reduce the particle size, and obtain the acidified montmorillonite after drying. Acid-activated modified montmorillonite;

[0050] Prepare an aqueous solution of betaxolol hydrochloride (BH) with a concentration of 3g / L, add acidified montmorillonite whose weight is 1 / 3 of the weight of BH, adjust the pH to 4, absorb in a water bath at 50°C for 6h, centrifuge and dry, and prepare Demontmorillonite-betaxolol hydrochloride compound (i.e. drug-loaded montmorillonite);

[0051] (2) Accurately weigh 425.6mg RL PO, 22.4mg RS PO, 56mgBH in a test tube, add 5mL of dichloromethane, ultrasonically dissolve at 50°C, after it is completely dissolved, add 5mg of montmorillonite-betaxolol hydrochloride complex to obtain an organic phase;

[0052] Another 1% poloxamer 188 solution was taken as the water phas...

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PUM

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Abstract

The invention discloses a preparation method for an intraocular medicine delivery system of polyacrylic resin wrapping montmorillonite loading medicine. The method comprises the steps that modified montmorillonite activated by acid adsorbs medicine to obtain the montmorillonite loading medicine; the polyacrylic resin and the medicine are dissolved in an organic solvent under the ultrasonic heatingcondition, the montmorillonite loading medicine is added, and an organic phase is prepared; a surface active agent is dissolved in water to prepare a water phase; the organic phase is injected into the water phase, the organic phase and water phase mixture is subjected to ultrasonic processing, after ultrasonic processing, the mixture is continuously stirred, the organic solvent volatilizes, andthe system is obtained. The particle size of the prepared nanometer medicine delivery system of the polyacrylic resin wrapping the montmorillonite loading medicine is small and is in nanoscale, the system has higher Zeta electric potentials and better adhesion to the mucosa surface, and therefore the system is beneficial for medicine absorption and utilization. A large number of toxic and organicsolvents are not used, and the operation is simple and convenient.

Description

technical field [0001] The invention relates to the field of medicine, in particular to a preparation method of a novel drug delivery system in which polyacrylic acid resin wraps drug-loaded montmorillonite. Background technique [0002] The traditional liquid dosage form for eye drops is easy to be accepted by patients because of its simple preparation, low price, convenient portability and medication, so it occupies about 90% of the market share of ophthalmic dosage forms. However, due to the special structure and physiological factors of the eye, there are many limitations in ocular anatomy and physiology (such as tear secretion and flow, nasolacrimal duct elimination, blood-aqueous barrier, blood-ocular barrier, blood-retinal barrier, etc. ), after the eye drops are instilled into the eyes, the time for the liquid to stay in the tear film is very short, so that the effective amount of the drug that can reach the intraocular tissue is only 1% to 5% of the administered dos...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/51A61K33/06A61K47/32A61P27/02
CPCA61K9/5138A61K33/06A61P27/02
Inventor 侯冬枝陈燕忠赵雅雯李娟潘育方韩鑫玥蒋阿梅
Owner GUANGDONG PHARMA UNIV
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