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Febrile convulsion resisting benzodiazepine pharmaceutical composition and intelligent transdermal delivery system thereof

A technology for transdermal delivery of benzodiazepines, applied in the field of biomedicine, can solve the problems of inappropriate iontophoresis transdermal drug delivery, poor water solubility, etc., and achieve the effect of facilitating remote control of drug delivery

Active Publication Date: 2020-05-01
NANTONG UNIVERSITY
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, BDZ drugs are generally poor in water solubility, and according to drug pKa analysis, such drugs cannot be fully dissociated to form charged ionized structures under skin-acceptable neutral or near-neutral conditions. Physical and chemical properties make it unsuitable for transdermal drug delivery using iontophoresis, and other methods need to be invented to solve this problem and prove their effectiveness

Method used

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  • Febrile convulsion resisting benzodiazepine pharmaceutical composition and intelligent transdermal delivery system thereof
  • Febrile convulsion resisting benzodiazepine pharmaceutical composition and intelligent transdermal delivery system thereof
  • Febrile convulsion resisting benzodiazepine pharmaceutical composition and intelligent transdermal delivery system thereof

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Experimental program
Comparison scheme
Effect test

Embodiment 1

[0047] Synthesis of LZP-Gly: Weigh lorazepam (LZP, 0.50g, 1.56mmol), 1-ethyl-(3-dimethylaminopropyl) carbodiimide hydrochloride (EDCI, 0.48g, 3.10mmol), 4-dimethylaminopyridine (DMAP, 0.10g, 0.78mmol), Boc-glycine (Boc-Gly, 0.33g, 1.89mmol), dissolved in 30ml of dichloromethane (DCM), magnetically stirred at room temperature Stir overnight. The reaction was monitored by thin layer chromatography. After the reaction was completed, the precipitate was removed by filtration, and the solution was spin-dried. The residue was redissolved with ethyl acetate and washed with water (2×30ml), saturated NaHCO 3 The solution (2 x 30ml) was washed successively with saturated NaCl solution (1 x 30ml). Anhydrous MgSO for organic layer 4 Dry, filter, and spin dry the solvent. The product was purified by silica gel column chromatography (petroleum ether: ethyl acetate = 4:1). Collect the eluate containing the product and spin dry. Take the purified substance in a flask, add 5ml DCM and 5...

Embodiment 2

[0050] Synthesis of LZP-Phe: Weigh LZP (0.77g, 2.40mmol), EDCI (0.75g, 4.84mmol), DMAP (0.15g, 1.23mmol) and Boc-phenylalanine (Boc-Phe, 0.77g, 2.91mmol ), dissolved in 30ml of DCM, and stirred overnight with magnetic stirring at room temperature. The reaction was monitored by thin layer chromatography. After the reaction was completed, the precipitate was removed by filtration, and the solution was spin-dried. The residue was redissolved with ethyl acetate and washed with water (2×30ml), saturated NaHCO 3 The solution (2 x 30ml) was washed successively with saturated NaCl solution (1 x 30ml). Anhydrous MgSO for organic layer 4 Dry, filter, and spin dry the solvent. The product was purified by silica gel column chromatography (petroleum ether: ethyl acetate = 3:1). Collect the eluate containing the product and spin dry. Take the purified substance in a flask, add 5ml DCM and 5ml TFA in sequence, and stir magnetically for 2h under ice bath conditions. After the solvent w...

Embodiment 3

[0053] Synthesis of LZP-Ile: Weigh LZP (0.90g, 2.80mmol), EDCI (0.90g, 5.61mmol), DMAP (0.17g, 1.39mmol) and Boc-isoleucine (Boc-Ile, 0.79g, 3.40mmol ), dissolved in 30ml of dichloromethane (DCM), and stirred overnight with magnetic stirring at room temperature. The reaction was monitored by thin layer chromatography. After the reaction was completed, the precipitate was removed by filtration, and the solution was spin-dried. The residue was redissolved with ethyl acetate and washed with water (2×30ml), saturated NaHCO 3The solution (2 x 30ml) was washed successively with saturated NaCl solution (1 x 30ml). Anhydrous MgSO for organic layer 4 Dry, filter, and spin dry the solvent. The product was purified by silica gel column chromatography (petroleum ether: ethyl acetate = 3:1). Collect the eluate containing the product and spin dry. Take the purified substance in a flask, add 5ml DCM and 5ml TFA in sequence, and stir magnetically for 2h under ice bath conditions. After...

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Abstract

The invention provides a febrile convulsion resisting pharmaceutical composition and an exclusive transdermal ion introduction technology based delivery system thereof. The febrile convulsion resisting pharmaceutical composition comprises a benzodiazepine prodrug and a pharmaceutical adjuvant, wherein the benzodiazepine prodrug is a water-soluble ionized precursor derivative, which is prepared through chemically modifying a benzodiazepine compound which has 3-hydroxyl, does not dissociate at a physiological pH value and is insoluble in water. According to the intelligent transdermal delivery system of the febrile convulsion resisting pharmaceutical composition, an artificial ionized 3-hydroxyl benzodiazepine compound derivative is subjected to rapid and dosage-controllable transdermal administration by using direct current, an effective blood-drug treatment concentration can be achieved in a short time, and febrile convulsion is effectively intervened.

Description

technical field [0001] The invention belongs to the technical field of biomedicine, and relates to the application of benzodiazepine prodrugs in the preparation of anti-convulsant drugs for transdermal iontophoresis, in particular to a benzodiazepine drug composition for anti-febrile convulsions and its intelligent transdermal delivery system. Background technique [0002] Febrile seizures (Febrile seizures, FS) is a common disease in infants and young children, the incidence rate is about 4%, mostly in infants and young children aged 2 months to 5 years old. FS is a common emergency in pediatrics, and it is also the most common neurological symptom in children, which mostly occurs within 24 hours after fever. The onset of FS symptoms is relatively clear, and most of them are symptoms based on fever: such as temporary coma, neck stiffness, convulsions, eyes looking up, jaws closed, and even screaming, foaming at the mouth, incontinence, etc. . Convulsive seizures may cont...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/00A61K31/551A61K31/5513A61P25/08A61N1/30
CPCA61K9/0014A61K31/551A61K31/5513A61P25/08A61N1/303
Inventor 陈勇凌勇朱丽刘季
Owner NANTONG UNIVERSITY
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