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Antiepileptic external medicine and application thereof

An external drug and anti-epileptic technology, applied in the field of medicine, can solve the problems of central system adverse reactions, unfavorable combined use of antihistamine drugs and anti-epileptic drugs, and limited broad application prospects

Pending Publication Date: 2019-01-15
王海玲
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, Amlexanox cannot pass through the blood-brain barrier, which limits its possible broad application prospects in central nervous system diseases.
In recent years, a long-forgotten antihistamine, clemizole, was found to inhibit seizures in zebrafish. Amlexanox’s inability to pass through the blood-brain barrier limits its possible antiepileptic effect. Of course, this also It has led to the improvement of the safety of amlexanox, and the occurrence of adverse reactions in the central system is rare
However, other antihistamines tend to cause central depression and have a sedative effect, which is not conducive to the combined use of antihistamines and antiepileptic drugs

Method used

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  • Antiepileptic external medicine and application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0025] Example 1 Carbamazepine / Amlexanox Compound Gel 1

[0026] Party:

[0027] Carbamazepine 20g

[0028] Amlexanol 5g

[0029] Carbomer 941 8g

[0030] Glycerin 250g

[0031] Triethanolamine 20g

[0032] Purified water 650g

[0033] preparation:

[0034] (1) Take the prescription amount of Carbomer 941 and add purified water to make a 4% solution, fully swell; add 40g glycerin, grind

[0035] Grind until completely wet, add the prescribed amount of triethanolamine and stir evenly to make a transparent gel matrix;

[0036] (2) Add the prescribed amount of carbamazepine and amlexanox to the remaining amount of glycerin, add the resulting mixture to the transparent gel matrix, stir while adding, then add the remaining amount of purified water, continue to stir evenly, and make a gel for external use preparation.

Embodiment 2

[0037] Embodiment 2 carbamazepine / amlexanox compound gel 2

[0038] Party:

[0039] Carbamazepine 40g

[0040] Amlexanol 5g

[0041] Carbomer 941 8g

[0042] Glycerin 250g

[0043] Triethanolamine 20g

[0044] Purified water 650g

[0045] preparation:

[0046] (2) Take the prescribed amount of Carbomer 941 and add purified water to make a 4% solution, fully swell; add 40g glycerin, grind

[0047] Grind until completely wet, add the prescribed amount of triethanolamine and stir evenly to make a transparent gel matrix;

[0048](2) Add the prescribed amount of carbamazepine and amlexanox to the remaining amount of glycerin, add the resulting mixture to the transparent gel matrix, stir while adding, then add the remaining amount of purified water, continue to stir evenly, and make a gel for external use preparation.

Embodiment 3

[0049] Example 3 Carbamazepine / Amlexanox Compound Gel 3

[0050] Party:

[0051] Carbamazepine 50g

[0052] Amlexanol 5g

[0053] Carbomer 941 8g

[0054] Glycerin 250g

[0055] Triethanolamine 20g

[0056] Purified water 650g

[0057] preparation:

[0058] (3) Take the prescribed amount of Carbomer 941 and add purified water to make a 4% solution, fully swell; add 40g glycerin, grind

[0059] Grind until completely wet, add the prescribed amount of triethanolamine and stir evenly to make a transparent gel matrix;

[0060] (2) Add the prescribed amount of carbamazepine and amlexanox to the remaining amount of glycerin, add the resulting mixture to the transparent gel matrix, stir while adding, then add the remaining amount of purified water, continue to stir evenly, and make a gel for external use preparation.

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Abstract

The invention belongs to the field of medicines, and particularly relates to an anti-epileptic external medicine and application thereof. The active ingredients of the anti-epileptic external medicineare carbamazepine and ammonia. The anti-epileptic externally-applied medicine comprises the following components in parts by weight: 4 -10 parts of carbamazepine and 4 -10 parts of ammonia, 1 part byweight of ammonia and 1 part by weight of xanthenone. The dosage form of the antiepileptic external medicine is preferably an external gel preparation. The external pharmaceutical adjuvants of the external gel preparation are carbomer 941, glycerol, triethanolamine and purified water. When the anti-epileptic external medicine is subjected to transdermal drug delivery, the anti-epileptic effect ofthe epilepsy animal is superior to that of carbamazepine alone.

Description

technical field [0001] The invention belongs to the field of medicine, and in particular relates to an antiepileptic drug for external use and its application. Background technique [0002] Epilepsy, commonly known as "epilepsy", is a type of disease caused by the sudden and excessive repeated discharge of excitatory neurons in the brain, resulting in sudden and temporary disorders of brain function. Patients often present with transient sensory disturbances, limb twitching, Loss of consciousness, called a seizure. It is estimated that there are about 9 million epilepsy patients in my country. [0003] Carbamazepine is a sodium channel modulator, which can block the rapid release of sodium ion-dependent action potentials to exert an antiepileptic effect. It is the first-line drug for the treatment of epilepsy and generalized tonic-clonic seizures. Its clinical main dosage form is oral tablet, and the required dose is relatively large. The initial dose is 100 mg, and the an...

Claims

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Application Information

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IPC IPC(8): A61K31/55A61K31/436A61K9/06A61K47/32A61P25/08
CPCA61K9/0014A61K9/06A61K31/436A61K31/55A61K47/32A61P25/08A61K2300/00
Inventor 王海玲张爱云郑学明卜文
Owner 王海玲
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