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Preparation for novel administration route of antiarrhythmic medicament

A technology of antiarrhythmia and drug delivery route, which is applied in the field of drug release, can solve the problems of no reported antiarrhythmic effect of volatile oil, unfavorable safe and convenient drug use, and slow drug effect of oral drugs, so as to achieve convenient drug administration and rapid drug delivery. Onset of effect, avoidance of prolonged effect

Inactive Publication Date: 2009-07-01
ZHEJIANG ZHENGFANG PHARMA TECH
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  • Abstract
  • Description
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AI Technical Summary

Problems solved by technology

Ma Chuangeng et al. (Ma Chuangeng, Xiang Siyuan et al. Experimental research on the antiarrhythmic effect of Gansong ethanol extract. Journal of Anhui Medical College, 1980, 15(4): 9) found that intravenous injection of ethanol extract has certain antiarrhythmic effect. Arrhythmic effects, but no antiarrhythmic effects of volatile oils have been reported so far
[0005] Further observations found that antiarrhythmic drugs have been commonly administered orally and intravenously in clinical practice for many years, but arrhythmia is often paroxysmal, and oral drugs have slow pharmacological effects, and intravenous administration often needs to be administered in time. The hospital conducts it, which is not conducive to safe and convenient medication

Method used

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  • Preparation for novel administration route of antiarrhythmic medicament
  • Preparation for novel administration route of antiarrhythmic medicament
  • Preparation for novel administration route of antiarrhythmic medicament

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0027] The preparation of embodiment 1 nard pine volatile oil

[0028] Take 1000 g of crushed Nardinus edulis, put it into a distillation device, pass through atmospheric pressure steam for distillation for 6 hours, condense the oily steam, separate the oil and water to obtain crude oil, add sodium sulfate to dry the crude oil, and filter to obtain 14.7 g of Nizhny pine volatile oil. The shape is light green transparent oily liquid with a sweet smell. Density 0.952g / ml.

[0029] Through gas chromatographic analysis, the volatile oil of nard pine includes cararene (white calorene, Calarene), △ 1(10)-Alienone-2 and Jatamansinol, Eucalyptol, α-Pinene, β-Pinene, β-Olivene ), Aristolene, 1a, 2, 3, 4, 4a, 5, 6, 7b-octylhydro-1, 1, 4, 7-tetramethyl-1H propane azulene, 4-(2 , 6,6,-Trimethyl-1-cyclohexene-1)-3-butenone, Aromadendrane (Aromadendrane), Piper orange solanadiene (Carinane), Apirapadien-3,7( Selina-3.7-diene), Spathulenol, Globulol, β-caryophyllen, 1,2,3,4,5,6,7,8- Oct...

Embodiment 2

[0030] Example 2 Effects of Nardinus volatile oil on sodium ion channels in cardiomyocytes

[0031] 1. Materials and methods

[0032] 1.1 Test solution of pine pine volatile oil: Dissolve 1.0 g of pine pine volatile oil obtained in Example 1 with dimethyl sulfoxide, add normal saline and dilute to 1000 ml to obtain pine pine volatile oil test solution (1:1k), which is equivalent to crude drug 68g / L. Dilute the pine pine volatile oil test solution (1:1k) 20 times to obtain the pine pine volatile oil test solution (1:20k), which is equivalent to 3.4g / L crude drug.

[0033] 1.2 Rat cardiomyocyte isolation method: 8 rats, weighing 200-300 grams, male or female, were intraperitoneally injected with 1000 units (1ml) of heparin, 15 minutes later intraperitoneally injected with 25-50mg (1ml) barbital sodium for anesthesia, and quickly opened The heart was taken from the chest, and perfused in a Langendorff perfusion device under the condition of constant temperature and oxygen supp...

Embodiment 3

[0041] Example 3 Effect of nard pine volatile oil on the effective refractory period of rat ventricular myocardium and its correction value

[0042] 1. Materials and methods: A total of 50 healthy male Wistar rats (250±50 g) were divided into a treatment group (n=40) and a control group (n=10). Medication groups were all given the pine pine volatile oil test solution (1:20K) in Example 2 (equivalent to crude drug 3.4g / L). The medication group was divided into epicardial local infiltration (n=20) and airway inhalation administration group (n=20), and the control group was given pine pine volatile oil solvent. The administration method of local epicardial infiltration is to drop 0.2ml of the medicinal solution to the epicardium, and the administration method of airway inhalation is to drip the medicinal solution 0.2ml (equivalent to 10ug of volatile oil, or equivalent to 0.68mg of crude drug) to the cotton As for the side tube in the three-way tube, one end of the three-way tub...

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Abstract

The invention relates to a formulation with novel administration route for the antiarrhythmic medicaments, comprising antiarrhythmic active drugs, and one or more additives of solvent, latent solvent, antioxidant or surfactant, which are packaged in the containers having a spray device. The formulation is capable of being used for the nasal, oral or sublingual administrations through the pulmonary administration or agents, which is more convenient than injection administration, faster in effect than oral administration to avoid unnecessary prolongation of effect after the onset of diseases.

Description

Technical field [0001] The invention relates to the technical field of drug release, in particular to a preparation of a new route of administration of an antiarrhythmic drug, and more particularly to a new preparation for administration of an antiarrhythmic drug to the lung, nasal cavity and oral mucosa (including sublingual). Background technique [0002] Arrhythmia is one of the main causes of death from various heart diseases, especially in heart failure, myocardial ischemia or myocardial infarction, the incidence and mortality of arrhythmia are higher. However, the total effective rate of antiarrhythmic drugs is only 30%-60% (Zhou Jiang, Zhao Fei. Observation on the clinical efficacy of Wenxin Granules in the treatment of arrhythmia. Chinese Medicine, 2006, 1(6): 342-343). So far, all the antiarrhythmic western medicines have proarrhythmic effects while being antiarrhythmic. 13%, and drug-induced arrhythmias can manifest as all arrhythmia types. This serious side effe...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/12A61K45/06A61K36/185A61K31/5415A61P9/06A61K31/165A61K31/166A61K31/4453A61K31/445A61K31/14A61K31/4402A61K31/167A61K31/198A61K31/138A61K31/404A61K31/343A61K31/277A61K31/46A61K31/133A61K31/49A61K31/137
Inventor 葛郁芝吴志婷吴炜玮
Owner ZHEJIANG ZHENGFANG PHARMA TECH
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