Amiodarone hydrochloride injection emulsion and preparation method thereof

A technology of amiodarone hydrochloride and injection milk, which is applied in the fields of pharmaceutical formula, emulsion delivery, medical preparations containing active ingredients, etc. It can solve the problems of inability to accurately predict the distribution law, increase drug solubility, and increase toxic and side effects, etc., to achieve The preparation process is simple and easy, the effect of eliminating toxic and side effects and enhancing compliance

Active Publication Date: 2013-04-24
BEIJING TIDE PHARMA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Cyclodextrin inclusion increases the solubility of the drug and decreases with the decrease in drug efficacy, and it is impossible to accurately predict its distribution in the body, etc.
At the same time, since cyclod

Method used

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  • Amiodarone hydrochloride injection emulsion and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0031] prescription:

[0032] Amiodarone Hydrochloride 0.5g

[0033] soybean oil 100g

[0034] Egg yolk phospholipids 5g

[0035] Edetate Disodium 0.01g

[0036] Oleic acid 0.1g

[0037] Glycerin 20g

[0038] Sodium hydroxide solution or hydrochloric acid solution

[0039] Makes 1000ml

[0040] Preparation Process:

[0041] (1) Amiodarone hydrochloride 0.5g, soybean oil 100g, egg yolk phospholipid 5g, oleic acid 0.1g, heated in a water bath to 65°C, stirred and dissolved to obtain an oil phase;

[0042] (2) Measure 500ml of water for injection, add 20g of glycerin and 0.01g of disodium edetate, heat to 65°C and stir to dissolve to obtain the aqueous phase;

[0043] (3) Mix the oil phase and the water phase at 65°C, and shear emulsify for 15 minutes (8000 rpm), so that the oil phase and the water phase are evenly mixed to obtain colostrum;

[0044](4) Homogenize the colostrum 5 times with a high pressure homogenizer (pressure 650bar, temperature 65°C), adjust its pH to...

Embodiment 2

[0047] prescription:

[0048] Amiodarone Hydrochloride 1g

[0049] 150g peanut oil

[0050] Phosphatidylcholine 10g

[0051] 1,2-Distearoylphosphatidylglycerol 30g

[0052] Sorbitol 40g

[0053] Sodium Oleate 0.03g

[0054] Vitamin E 0.3g

[0055] Sodium hydroxide solution or hydrochloric acid solution

[0056] Make 1000ml

[0057] Preparation Process:

[0058] (1) Take 1 g of amiodarone hydrochloride and 150 g of peanut oil, heat in a water bath to 55°C, stir and dissolve to obtain an oil phase;

[0059] (2) Measure 600ml of water for injection, add 10g of phosphatidylcholine, 30g of 1,2-distearoylphosphatidylglycerol, and 40g of sorbitol, heat to 55°C and stir to dissolve to obtain the aqueous phase;

[0060] (3) Mix the oil phase and the water phase at 55°C, shear and emulsify for 15 minutes (10,000 rpm), mix the oil phase and the water phase evenly, and adjust the pH with sodium hydroxide solution (0.1mol / L) For 11.0, colostrum was obtained;

[0061] (4) Homogen...

Embodiment 3

[0065] prescription:

[0066] Amiodarone Hydrochloride 3g

[0067] Hydrogenated corn oil 200g

[0068] Egg yolk phospholipids 25g

[0069] 1,2-Distearoylphosphatidylglycerol 25g

[0070] Disodium Calcium Edetate 0.05g

[0071] Oleic acid 0.5g

[0072] Xylitol 30g

[0073] Sodium hydroxide solution or hydrochloric acid solution

[0074] Make 1000ml

[0075] Preparation Process:

[0076] (1) Take 3g of amiodarone hydrochloride, 200g of hydrogenated corn oil, 25g of egg yolk phosphatidylglycerol, 25g of 1,2-distearoylphosphatidylglycerol, 0.5g of oleic acid, heat in a water bath to 75°C, stir and dissolve to obtain the oil phase;

[0077] (2) Measure 800ml of water for injection, add 30g of xylitol, 0.05g of disodium calcium edetate, heat to 75°C and stir to dissolve to obtain the aqueous phase;

[0078] (3) Mix the oil phase and the water phase at 75°C, shear and emulsify for 20 minutes (10,000 rpm), so that the oil phase and the water phase are evenly mixed to obtain c...

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Abstract

The invention provides an amiodarone hydrochloride injection emulsion and a preparation method thereof. The amiodarone hydrochloride injection emulsion contains 0.05-0.5% of amiodarone hydrochloride, 10-30% of oil for injection, 0.5-5% of emulsifier, 2-8% of osmotic pressure modifier, and an approximate amount of pH regulator and water for injection, and also contains 0.001-0.01% of antioxidant and 0.01-0.1% of stabilizer. The preparation method comprises the following main steps of: heating an oil phase and an aqueous phase respectively; adding medicaments into the oil phase, and then adding the oil phase into the aqueous phase (or adding the aqueous phase into the oil phase); stirring to obtain initial emulsion; regulating the pH value; homogenizing the initial emulsion through a high-pressure homogenizer; and sterilizing through high temperature steam, thereby obtaining a finished product. The emulsion for injection is uniform in granularity, stable in quality and easy for industrial production, can be used for improving the in-vivo bioavailability of the medicaments, and avoiding toxic and side effects generated by a cosolvent in a general injection, so that the controllability and safety of the clinical medication are improved greatly.

Description

technical field [0001] The invention belongs to the field of pharmaceutical preparations, in particular to an injection emulsion of a long-acting antiarrhythmic drug amiodarone hydrochloride and a preparation method thereof. Background technique [0002] Amiodarone hydrochloride is currently the most widely used antiarrhythmic drug in clinical practice. effect. Intravenous injection shows that the pharmacological effects of classes I, II, and IV are faster, and the onset of pharmacology of class III is longer, and the therapeutic effect on severe and fatal arrhythmias is very obvious. Oral tablets are commonly used at present, but amiodarone hydrochloride is slowly and incompletely absorbed in the gastrointestinal tract when taken orally, with large individual differences and unstable bioavailability. The absolute bioavailability is only 50%. The onset and clearance of oral administration are slow. It takes days to weeks to take effect when taken orally. In the case of in...

Claims

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Application Information

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IPC IPC(8): A61K9/107A61K31/343A61P9/06
Inventor 王志钢赵焰平周丽莹刘玉静肖萱张伟强
Owner BEIJING TIDE PHARMA
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