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Ibolite fumarate nasal cavity administration preparation

A technology for ibutilide fumarate and intranasal administration, which is applied in the directions of drug delivery, drug combination, and pharmaceutical formulations, can solve problems such as low bioavailability, and achieve the effects of controllable quality and stable performance

Active Publication Date: 2005-08-10
广东同德药业有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0008] Oral administration of ibutilide, such as the preparation of ibutilide fumarate, has a strong first-pass metabolic effect and low bioavailability, so it is administered intravenously, and intravenous administration must be performed by professional medical personnel operate

Method used

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  • Ibolite fumarate nasal cavity administration preparation

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0038] Embodiment 1: the preparation of ibutilide fumarate spray

[0039] Ingredient Amount

[0040] Ibutilide Fumarate 50mg

[0041] Polyvinylpyrrolidone 0.3g

[0042] Laurazone 0.5ml

[0043] Propylene glycol 1.0g

[0044] Ethylparaben 0.1g

[0045] Distilled water to 100ml

[0046] Preparation method: Fully stir the above-mentioned amount of polyvinylpyrrolidone, ibutilide fumarate, propylene glycol, and lauryl nitrogen statistical ethylparaben to dissolve them all, and finally add distilled water to 100ml. Hydrochloric acid to adjust pH. The obtained solution is distributed in a spray pump or a quantitative drop pump.

Embodiment 2

[0047] Embodiment 2: the preparation of ibutilide fumarate spray

[0048] Ingredient Amount

[0049] Ibutilide Fumarate 50mg

[0050]Hydroxypropyl-β-cyclodextrin 2.5g

[0051] Ethylparaben 0.1g

[0052] Mannitol 0.5g

[0053] Macrogol 400 1.0ml

[0054] Distilled water to 100ml

[0055] Preparation method: After shaking the above-mentioned amount of ibutilide fumarate, hydroxypropyl-β-cyclodextrin, ethylparaben, mannitol and distilled water to dissolve, add the above-mentioned polyethylene glycol 400, and finally add Add distilled water to 100ml. Hydrochloric acid to adjust pH.

Embodiment 3

[0056] Embodiment 3: the preparation of ibutilide fumarate spray

[0057] Ingredient Amount

[0058] Ibutilide Fumarate 150mg

[0059] Methyl-beta-cyclodextrin 5g

[0060] Ethylparaben 0.1g

[0061] Polyvinyl alcohol 0.5g

[0062] Mannitol 2-4g

[0063] Distilled water to 100ml

[0064] Preparation method: add distilled water to the above amount of ibutilide fumarate, methyl-β-cyclodextrin, ethylparaben, polyvinyl alcohol, shake to dissolve all, and finally add distilled water to 100ml. Hydrochloric acid to adjust pH.

[0065] Pharmacological experiment

[0066] Carry out the pharmacokinetic test in beagle dogs after the administration of 1 fumaric acid ililide nasal spray and fumarate ililide injection, the results are shown in Table 1

[0067] Table 1 After administration of Iilide Fumarate Nasal Spray and Iilide Fumarate Injection

[0068] Comparison of Plasma Protein Binding and Plasma Clearance in Beagle Dogs

[0069] Drug Dose Plasma Clearance Plasma Protei...

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Abstract

An ibutilide fumarate applied via nasal cavity for treating arrhythmia contanis ibutilide fumarate, the free alkali of ibutilide or pharmacologically acceptable medical salts of ibutilide, the stereoisomer with pharmacologic activity, and absorption promoter.

Description

field of invention [0001] The invention relates to a preparation for nasal cavity administration, in particular to a preparation for nasal cavity administration of ibutilide fumarate. Background technique [0002] Arrhythmias are very common and can be caused or induced by many diseases and drugs. According to relevant data, a comparison of the incidence rates of various arrhythmias shows that sinus arrhythmia has the highest incidence rate of 25% to 27%, followed by sinus tachycardia at 20% to 22%. Brady is 13% to 15%, ventricular premature beat is 14% to 16%, atrial premature beat is 5% to 7%, atrial fibrillation is 11% to 15%, atrioventricular block is 5% to 7%, other various arrhythmias about 5% to 8%. Therefore, people have been devoting themselves to prescribing an antiarrhythmic drug that can be administered to patients at the first time, is convenient to use, and has good therapeutic effect. [0003] Ibutilide fumarate (Ibutilide fumarate) is a new type of antiarr...

Claims

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Application Information

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IPC IPC(8): A61K9/72A61K31/165A61P9/06
Inventor 夏敏张同祥
Owner 广东同德药业有限公司