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Medicament application of 1, 6-fructose bisphosphate sodium salt containing borneol

A technology of sodium fructose diphosphate and borneol, applied in the application field of preparing antiepileptic drugs, can solve the problem of increasing the drug concentration of carbamazepine and sodium valproate in cerebrospinal fluid, no research report on the efficacy of epilepsy, and no research on borneol karma Effects of Xiping and Sodium Valproate on Antiepileptic Therapy and Other Issues

Inactive Publication Date: 2014-02-26
ZHEJIANG UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

The above two studies only studied that borneol can increase the drug concentration of carbamazepine and sodium valproate in cerebrospinal fluid, and did not investigate whether borneol can really improve the antiepileptic therapeutic effect of carbamazepine and sodium valproate
Moreover, there has been no research report on the effect of borneol on the penetration of sodium fructose 1,6-diphosphate through the blood-brain barrier and the combined use of borneol and sodium fructose 1,6-diphosphate in the treatment of epilepsy.

Method used

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  • Medicament application of 1, 6-fructose bisphosphate sodium salt containing borneol
  • Medicament application of 1, 6-fructose bisphosphate sodium salt containing borneol
  • Medicament application of 1, 6-fructose bisphosphate sodium salt containing borneol

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0012] Embodiment 1. Borneol enhances the effect of sodium fructose 1,6-diphosphate against penicillin-induced epileptic seizures in mice

[0013] The acute epilepsy model in mice induced by intraperitoneal injection of penicillin is a commonly used epilepsy model for studying the antiepileptic effect of drugs. By observing the latency of seizures (convulsions) and the percentage of epilepsy, it is judged whether the tested drug has antiepileptic effect.

[0014] Take 160 male ICR mice weighing 18-22g, and randomly group them into groups (see Table 1), 20 in each group. The test used 1,6-diphosphate fructose sodium salt (the raw material purchased from Zhangjiagang Huatian Pharmaceutical Co., Ltd., the same below) and borneol (commercially available traditional Chinese medicine, the same below), each group was administered by gavage, and the model The animals in the group without drug were fed with the same volume of distilled water, and the animals in each group were intra...

Embodiment 2

[0018] Embodiment 2. Borneol enhances the effect of sodium fructose 1,6-diphosphate on pentetrazol convulsions in rats

[0019] Pentylenetetrazol is a gamma-aminobutyric acid (GABA) receptor blocker, which can enhance the depolarization process of excitatory synapses and induce acute epilepsy models. The acute epilepsy model induced by a one-time injection of a large dose of pentylenetetrazol is one of the most commonly used methods for studying the activity of antiepileptic drugs. The acute epilepsy model was induced by intraperitoneal injection of large doses of pentylenetetrazol in rats to observe the effects of drugs on the behavior, latency, duration and incidence of epileptic seizures in rats. 180-220g male SD rats were randomly divided into groups (Table 2). Pre-administration was administered continuously for 3 days, once a day. The model group was given normal saline. 120 minutes after the last administration, the animals in each group were intraperitoneally inj...

Embodiment 3

[0023] Example 3: Borneol significantly enhances the antiepileptic efficacy of 1,6-diphosphate fructose sodium salt

[0024] The pilocarpine-induced chronic spontaneous epilepsy model in rats is an internationally recognized model of temporal lobe epilepsy, which is widely used in the study of the efficacy and mechanism of antiepileptic drugs. The pilocarpine-induced chronic spontaneous epilepsy model of adult male SD rats was prepared by conventional methods. According to the Racine standard, the degree of epileptic seizures was judged: grade 1: vibrating whiskers and chewing; grade 2: rhythmic nodding; grade 3: clonus of one forelimb; grade 4: standing with clonus of both forelimbs; grade 5: grade 4 + falling Accompanied by convulsions all over the body. The epileptic seizures of the animals with chronic epilepsy were continuously observed, and the specific observation time was from week 1 to week 6, from 9:00 am to 7:00 pm every day (continuous 10 hours). According to t...

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Abstract

The invention provides application of 1, 6-fructose bisphosphate sodium salt containing borneol to preparation of antiepileptic drug, wherein the 1,6-fructose bisphosphate sodium salt and borneol are in the proportion of 100:0.01-100:20. Research shows that borneol can enhance the antiepileptic effect of 1, 6-fructose bisphosphate sodium salt; the synergistic effect of borneol is related to increase of fructose bisphosphate sodium salt level in the brain; and combination borneol can significantly improve the antiepileptic therapeutic effect. The medicament is an oral solid preparation selected from a chewing tablet, a dispersible tablet, an orally disintegrating tablet or a common tablet, and is an efficient antiepileptic candidate medicament.

Description

technical field [0001] The invention belongs to the use of medicines, and relates to the application of a sodium fructose 1,6-diphosphate composition containing borneol in the preparation of antiepileptic drugs. In the composition, sodium fructose 1,6-diphosphate is the main drug (abbreviated as sodium fructose diphosphate), and the borneol can strengthen the antiepileptic effect of the main drug and act as an antiepileptic synergistic application. Background technique [0002] Epilepsy is a common and recurrent worldwide intractable disease that requires new antiepileptic drugs. Magnesium fructose 1,6-diphosphate has the effect of fighting acute epileptic seizures [Chinese patent, CN1309968A]. The onset of epilepsy is in the brain, and therapeutic drugs need to reach the brain to exert their antiepileptic effect. However, the entry of drugs into the brain is usually hindered by the blood-brain barrier, which limits the antiepileptic effect of drugs. Therefore, promoting t...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/7024A61P25/08A61K31/045
Inventor 连晓媛张治针唐焕宇
Owner ZHEJIANG UNIV
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