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Application of composition to the preparation of antiepileptic drug

A technology of antiepileptic drugs and compositions, which is applied in the field of medicine, can solve the problems of not being able to know the changes of drug effects, and achieve the effect of prolonging the residence time

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

AI Technical Summary

Problems solved by technology

Since the patent CN1309968A uses an animal model of acute epilepsy and only observed the antiepileptic effect of magnesium fructose diphosphate once, it is impossible to know the possible changes in the drug effect after multiple administrations

Method used

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  • Application of composition to the preparation of antiepileptic drug
  • Application of composition to the preparation of antiepileptic drug
  • Application of composition to the preparation of antiepileptic drug

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0051] Example 1: Pharmacodynamic advantages and limitations of 1,6-diphosphate fructose sodium salt in chronic epilepsy model

[0052] 1. Preparation of spontaneous chronic epilepsy model:

[0053] Temporal lobe epilepsy is the most common type of epilepsy in clinical adults, and drug resistance often occurs. The rat temporal lobe epilepsy model induced by pilocarpine can simulate the symptoms, neuropathology and histomorphological changes of human temporal lobe epilepsy, so this model is widely used at home and abroad to predict the efficacy of antiepileptic drugs and study the antiepileptic mechanism.

[0054] Adult male Sprague Dawley rats (180-200g) were injected intraperitoneally with pilocarpine (300mg / kg) to induce acute seizures, and the degree of seizures was judged according to the Racine standard: Level 1: moving whiskers and chewing; Level 2: rhythmic nodding; Level 3 : One side forelimb clonus; Grade 4: standing with double forelimb clonus; Grade 5: Grade 4...

Embodiment 2

[0068] Example 2: Establishment of a method for measuring fructose 1,6-diphosphate levels in mouse blood and brain tissue

[0069] According to the method reported in the literature [Xu K et al. Pharmacological research 2008; 57: 234-8], the determination of exogenous or endogenous FBP content can be determined by enzymatic method of nicotinamide adenine dinucleotide (NADH )to fulfill. The reaction principle is as follows:

[0070]

[0071] Briefly, FBP in aldolase (aldolase, 45units mg -1 dilute 1:27with distilled water) to decompose into dihydroxyacetone phosphate (dihydroxycetone phosphate, DAP) and 3-phosphate-D-glycerol (d-glyceraldehyde 3-phosphate, GAP), and consume NADH. DAP and GAP in triosephosphate isomerase (triosephosphate isomerase, TIM: 5290 units mg -1 diluted 1:120with distilled water) can be converted to each other under the action of phosphate dehydrogenase (Glycerol-3-phosphate dehydrogenase, GDH: 252units mg -1 dilute 1:100with distilled water)...

Embodiment 3

[0085] Example 3 : Changes of 1,6-diphosphate fructose content in blood and brain tissue after intragastric administration of 1,6-diphosphate fructose sodium salt

[0086] 2.1 one dose

[0087] The normal male mice were divided into random groups (5 groups), 7 mice in each group, administered once, including the control group and the administration group. The concentrations of the administration groups were: 200 mg / kg, 300 mg / kg, 500 mg / kg, 1000 mg / kg. The animals in the control group were given the same amount of normal saline. After intragastric administration for 2 hours, the concentration of FBP in blood and brain tissue was measured by the method established above. Research data show that the FBP content in the blood is the highest when given 200 mg / kg of FBP, which is 4 times the basal value of endogenous FBP, and when the dose is ≥ 400 mg / kg, the FBP in the blood is only about higher than the basal value ( Figure 7 ), this paradox may be because high-dose FBP ...

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Abstract

The invention provides the application of a 1,6-fructose diphosphate sodium salt, fructose and / or borneol composition to the preparation of an antiepileptic drug. The composition consists of 1,6-fructose diphosphate sodium salt and fructose, or 1,6-fructose diphosphate sodium salt and borneol combination, or 1,6-fructose diphosphate sodium salt, fructose and borneol. The composition provided by the invention can improve in vivo stability of 1, 6 1,6-fructose diphosphate, in order to maintain high level of 1,6-fructose diphosphate in the brain for a long time and make the 1,6-fructose diphosphate sodium salt exert antiepileptic effect for a long time. The composition provided by the invention particularly employs chewable tablets, orally disintegrating tablets and dispersible tablets as dosage forms for the antiepileptic drug, and the dosage forms can be directly absorbed in oral mucosa, avoid hepatic first-pass effect and further increase the level of 1,6-fructose diphosphate in the brain, thereby further improving the antiepileptic efficacy of the drug.

Description

technical field [0001] The invention belongs to the field of medicine and relates to the application of a composition containing 1,6-diphosphofructose sodium salt, fructose and borneol in the preparation of antiepileptic drugs. In this composition, 1,6-diphosphate fructose sodium salt (or called fructose diphosphate sodium) is the main agent, and its medicinal active part is 1,6-diphosphate fructose, and fructose can increase the main agent 1,6- The stability of fructose diphosphate in the body maintains a high level of blood drug concentration for a long time, which can correspondingly increase the level of fructose 1,6-diphosphate in the brain, and borneol, which can promote the opening of the blood-brain barrier, can promote blood Fructose 1,6-diphosphate enters the brain, thereby further increasing the level of fructose 1,6-diphosphate in the brain. It can be seen that fructose and borneol can increase the level of fructose 1,6-diphosphate in the brain through different m...

Claims

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Application Information

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IPC IPC(8): A61K31/7024A61P25/08A61P25/00A61K31/045A61K31/7004
Inventor 连晓媛张治针唐焕宇吴刚郭欣凌鹏朱月张宇奋
Owner ZHEJIANG UNIV
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