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Chitosan-modified methazolamide solid lipid nanoparticles and preparation method thereof

A technology of solid lipid nanometer and methazolamide, which is applied in sensory diseases, powder delivery, drug combination, etc., can solve the problems of inaccurate dosage, limitation, and technical difficulty of semi-solid preparations, and improve bioavailability degree, reduce the frequency of dosing, and enhance the effect of treatment

Inactive Publication Date: 2012-11-28
NANJING MEDICAL UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Although these several preparations have a good effect of lowering intraocular pressure, the accumulation of inorganic salts in the eyes has certain damage to the eyes; the disadvantages of liposomes are low drug loading, poor stability, and the production of sterile liposomes. Large-scale industrial production costs are high and technically difficult; and traditional gels cause irreversible damage to the gel structure due to autoclaving, so it is necessary to sterilize the raw materials and reagents used before preparing the gel and Strict aseptic operation is maintained during the production process. In addition, the inaccurate dosage of the gel as a semi-solid preparation also limits its application.

Method used

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  • Chitosan-modified methazolamide solid lipid nanoparticles and preparation method thereof
  • Chitosan-modified methazolamide solid lipid nanoparticles and preparation method thereof
  • Chitosan-modified methazolamide solid lipid nanoparticles and preparation method thereof

Examples

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Effect test

Embodiment 1

[0027]Take 5 mg of methazolamide, 100 mg of glyceryl monostearate (GMS), and 75 mg of phospholipid, add 5 mL of absolute ethanol, and heat to dissolve at 70 ° C to form an organic phase. Another 15 mL of a solution containing 150 mg Tween80 and 150 mg PEG400 was taken to form the inner aqueous phase. Aspirate the organic phase with a glass syringe through 5 # Slowly drop the organic phase into the internal water phase at the same temperature under stirring at 1200rpm, and continue stirring to completely evaporate the organic solvent to obtain colostrum (about 5mL); under stirring at 1000rpm, quickly pour the obtained colostrum into In the continuous phase (0-4°C) of 5 times the volume of colostrum, the continuous phase is a pH 4 acetic acid solution containing 5% (w / v) mannitol and 2.5 mg / mL chitosan. Stirring continued to solidify for 2 hours, returned to room temperature, and passed through a 0.45 μm microporous membrane to obtain chitosan-modified solid lipid nanoparticles...

Embodiment 2

[0029] Take 5 mg of methazolamide, 150 mg of glyceryl monostearate (GMS), and 150 mg of phospholipid, add 5 mL of absolute ethanol, and heat to dissolve at 70 ° C to form an organic phase. Another 15 mL of a solution containing 250 mg Tween80 and 250 mg PEG400 was taken to form the inner aqueous phase. Aspirate the organic phase with a glass syringe through 5 # Slowly drop the organic phase into the internal water phase at the same temperature under stirring at 1200rpm, and continue stirring to completely evaporate the organic solvent to obtain colostrum (about 5mL); under stirring at 1000rpm, quickly pour the obtained colostrum into In the continuous phase (0-4°C) of 10 times the volume of colostrum, the continuous phase is a pH 4 acetic acid solution containing 5% (w / v) mannitol and 2 mg / mL chitosan. Stirring continued to solidify for 2 hours, returned to room temperature, and passed through a 0.45 μm microporous membrane to obtain chitosan-modified solid lipid nanoparticle...

Embodiment 3

[0031] Take 5 mg of methazolamide, 25 mg of glyceryl monostearate (GMS), and 25 mg of phospholipids, add 5 mL of absolute ethanol, and heat to dissolve at 70 ° C to form an organic phase. Another 15 mL of a solution containing 50 mg Tween80 and 50 mg PEG400 was taken to form the inner aqueous phase. Aspirate the organic phase with a glass syringe through 5 # Slowly drop the organic phase into the internal water phase at the same temperature under stirring at 1200rpm, and continue stirring to completely evaporate the organic solvent to obtain colostrum (about 5mL); under stirring at 1000rpm, quickly pour the obtained colostrum into In the continuous phase (0-4°C) of 5 times the volume of colostrum, the continuous phase is a pH 6 acetic acid solution containing 5% (w / v) mannitol and 0.2 mg / mL chitosan. Stirring continued to solidify for 2 hours, returned to room temperature, and passed through a 0.45 μm microporous membrane to obtain chitosan-modified solid lipid nanoparticles....

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Abstract

The invention provides chitosan-modified methazolamide solid lipid nanoparticles and a preparation method thereof. The chitosan-modified methazolamide solid lipid nanoparticles can be used as eye drops. The preparation method is suitable for industrial production. The chitosan-modified methazolamide solid lipid nanoparticles are characterized in that based on 30ml of a nanoparticle-containing solution, the chitosan-modified methazolamide solid lipid nanoparticles comprise 5mg of methazolamide, 25 to 150mg of at least one lipid material, 25 to 150mg of phospholipid, 5 to 100mg of chitosan, 50 to 250mg of at least one non-phospholipid surfactant and 50 to 250mg of at least one assistant surfactant. The chitosan-modified methazolamide solid lipid nanoparticles have small particle sizes and high drug entrapment efficiency. Compared with solid lipid nanoparticles which are not modified by chitosan, the chitosan-modified methazolamide solid lipid nanoparticles have higher stability and better corneal permeability because of positive charges on the surfaces of the chitosan-modified methazolamide solid lipid nanoparticles so that drug bioavailability is improved. Therefore, the chitosan-modified methazolamide solid lipid nanoparticles have a large clinical application potential in glaucoma treatment.

Description

1. Technical field [0001] The invention belongs to the field of pharmaceutical preparations, and relates to a new dosage form of anti-glaucoma drugs-chitosan-modified solid lipid nanoparticles. 2. Background technology [0002] Methazolamide (MTZ) is a carbonic anhydrase inhibitor (CAI), which has a history of more than 40 years in the treatment of glaucoma and has a significant effect on lowering intraocular pressure. Carbonic anhydrase is a zinc-containing metalloenzyme that catalyzes CO in ciliary epithelial cells. 2 and H 2 O, eventually producing HCO 3 - , secreted in the aqueous humor through the cavity membrane. Since the solution is electrically neutral, Na + The secretion into the aqueous humor increases, and at the same time drives the Cl - Migrate to the aqueous humor, thereby forming high osmotic pressure in the aqueous humor, promoting H 2 O moves toward the aqueous humor to maintain the ionic balance of the aqueous humor. The principle of applying metha...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/14A61K31/433A61K47/34A61P27/06
Inventor 李瑞徐群为王凤珍张青姜孙旻辛洪亮
Owner NANJING MEDICAL UNIV
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