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P-glycoprotein monoclonal antibody modified phenytoin targeting nanopreparation and preparation method thereof

A monoclonal antibody and nano-preparation technology, applied in the direction of medical preparations with non-active ingredients, medical preparations containing active ingredients, and pharmaceutical formulas, to achieve good biocompatibility, good biocompatibility, and improved safety Effect

Inactive Publication Date: 2011-07-20
AFFILIATED HUSN HOSPITAL OF FUDAN UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Since Birrenbach first reported drug-loaded nanoparticles in 1976, nanoparticles have been widely used in the medical field as drug sustained release and targeting carriers, but the use of sustained release nanoparticles to target drug-resistant epilepsy has not yet See the report

Method used

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  • P-glycoprotein monoclonal antibody modified phenytoin targeting nanopreparation and preparation method thereof
  • P-glycoprotein monoclonal antibody modified phenytoin targeting nanopreparation and preparation method thereof
  • P-glycoprotein monoclonal antibody modified phenytoin targeting nanopreparation and preparation method thereof

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Embodiment 1

[0032] Maleimide group (Mal) capped PEG (5000) 200mg in P 2 o 5 Dry overnight in a vacuum desiccator for purification. Put it into a dried reaction bottle, add 10% stannous octoate toluene solution, seal it and vacuumize at 70°C for 2 hours to remove toluene and oxygen, then add 400 mg of caprolactone, and the temperature rises to 160°C for caprolactone The ring-opening polymerization of the monomer was carried out for 4 hours. After the reaction, cool to room temperature, add dichloromethane to dissolve, and precipitate into ether to remove unreacted caprolactone and the formed caprolactone homopolymer. The methane was dissolved and poured into a large amount of methanol to precipitate. to remove unreacted polyethylene glycol. The purified polymer was dried in a vacuum oven at 40°C for 24 hours, and then stored in a vacuum desiccator. A MAL-PEG-PCL copolymer is obtained.

[0033] Dissolve 20 mg of the polymer and 10 mg of the drug phenytoin in a mixed solution of 1.5 mL...

Embodiment 2

[0036] Maleimide group (Mal) capped PEG (5000) 200mg in P2 o 5 Dry overnight in a vacuum desiccator for purification. Put it into a dried reaction bottle, add 10% stannous octoate toluene solution, seal it and vacuumize it at 70°C for 2 hours to remove toluene and oxygen, then add 800mg of caprolactone, and the temperature rises to 160°C. Bulk ring-opening polymerization, reaction for 4 hours. After the reaction, cool to room temperature, add dichloromethane to dissolve, and precipitate into ether to remove unreacted caprolactone and the formed caprolactone homopolymer. The methane was dissolved and poured into a large amount of methanol to precipitate. to remove unreacted polyethylene glycol. The purified polymer was dried in a vacuum oven at 40°C for 24 hours, and then stored in a vacuum desiccator. A MAL-PEG-PCL copolymer is obtained.

[0037] Dissolve 20 mg of the polymer and 10 mg of the drug phenytoin in a mixed solution of 1.5 mL of dichloromethane and THF, add 10 ...

Embodiment 3

[0040] Maleimide group (Mal) capped PEG (5000) 200mg in P 2 o 5 Dry overnight in a vacuum desiccator for purification. Put it into a dried reaction bottle, add 10% stannous octoate toluene solution, seal it and vacuumize at 70°C for 2 hours to remove toluene and oxygen, then add 1.6g of caprolactone, and the temperature rises to 160°C for caprolactone The ring-opening polymerization of the monomer was carried out for 4 hours. After the reaction, cool to room temperature, add dichloromethane to dissolve, and precipitate into ether to remove unreacted caprolactone and the formed caprolactone homopolymer. The methane was dissolved and poured into a large amount of methanol to precipitate. to remove unreacted polyethylene glycol. The purified polymer was dried in a vacuum oven at 40°C for 24 hours, and then stored in a vacuum desiccator. A MAL-PEG-PCL copolymer is obtained.

[0041] Take 20 mg of the polymer and 10 mg of the drug phenytoin and dissolve them in 1.5 mL of a mi...

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Abstract

The invention belongs to medical preparations and relates to a new phenytoin targeting nanopreparation and a preparation method thereof. The nanopreparation for targeting therapy of drug-resistant epilepsy is prepared by taking phenytoin as an active ingredient, a P-glycoprotein monoclonal antibody as a targeting head group and a macromolecular polymer as a carrier. The loading rate and the releasing speed of the phenytoin are controlled by changing the proportion of polyethylene glycol to polycaprolactone in the macromolecular polymer; the problems of poor blood brain barrier permeability, low drug concentration at an epilepsy lesion area, poor treatment effect and serious adverse reaction in the conventional treatment of the drug-resistant epilepsy by the phenytoin are solved by using slow release and active targeting technologies; and the safety of the phenytoin is obviously improved. The preparation can be targeted to the lesion area of the drug-resistant epilepsy, so that the phenytoin content of the lesion area is greatly improved and the seizure of the epilepsy is suppressed.

Description

technical field [0001] The invention belongs to medical preparations, and relates to a P-glycoprotein monoclonal antibody-modified phenytoin targeting nano preparation and a preparation method thereof. Background technique [0002] Epilepsy is one of the most common neurological diseases. According to relevant statistics, there are about 9 million epilepsy patients in my country, and about 450,000 new cases are added every year, and about 30% of the patients are refractory epilepsy (refractory epilepsy, RE), also known as epilepsy. drug resistant epilepsy [1-2] . Its most prominent feature is that it has different degrees of resistance to anti-epileptic drugs (anti-epilepsy drugs, AEDs) with different chemical structures and different modes of action. The mortality rate is 4 to 7 times higher than that of general epilepsy patients, which seriously affects the quality of life of patients and consumes huge public health resources [3-5] . [0003] Phenytoin (Phenitoin, PHT) ...

Claims

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Application Information

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IPC IPC(8): A61K9/16A61K31/4166A61K47/42A61K47/34A61P25/08
Inventor 刘晓英洪震
Owner AFFILIATED HUSN HOSPITAL OF FUDAN UNIV
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