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Verapamil liposome and preparing method thereof

A technology for verapamil lipid and verapamil hydrochloride, which is applied in the field of verapamil liposome and its preparation, can solve the problems of long-term administration, long process of prevention and treatment of glaucoma and cataract, and achieves good stability , Broad industrialization prospects, the effect of improving stability

Inactive Publication Date: 2012-05-23
SHENYANG PHARMA UNIVERSITY
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

And the prevention and treatment process of glaucoma and cataract is relatively long, requiring long-term administration

Method used

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  • Verapamil liposome and preparing method thereof
  • Verapamil liposome and preparing method thereof
  • Verapamil liposome and preparing method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0071] Verapamil Hydrochloride 25mg

[0072] Phosphatidylcholine 120mg

[0073] Octadecylamine 5mg

[0074] Cholesterol 50mg

[0075] Preparation method: Dissolve the prescribed amount of phospholipids, cholesterol and octadecylamine in 4 mL of ethanol, slowly inject into 8 mL of 0.125 mol / L ammonium sulfate solution at 50 °C under magnetic stirring, keep stirring at 50 °C for 1 hour to completely volatilize the ethanol, Place the probe in an ice bath and sonicate for 5 minutes to obtain blank liposomes. The obtained blank liposomes were placed in a dialysis bag, the two ends were tied tightly, and dialyzed in 1000 mL of 0.9% NaCl solution for 24 hours to remove ammonium sulfate in the liposome external water phase. Incubate the dialyzed blank liposome at 60°C, slowly add 1mL of an aqueous solution containing 25mg of verapamil hydrochloride under stirring, continue to incubate for 20min, and adjust the final volume to 10mL with 0.9% NaCl solution to obtain verapamil hydroch...

Embodiment 2

[0077] Verapamil Hydrochloride 25mg

[0078] Phosphatidylcholine 120mg

[0079] Octadecylamine 5mg

[0080] Cholesterol 50mg

[0081] Chitosan 10mg

[0082] Preparation method: Dissolve the prescribed amount of phospholipids, cholesterol and octadecylamine in 4 mL of ethanol, slowly inject into 8 mL of 0.125 mol / L ammonium sulfate solution at 50 °C under magnetic stirring, keep stirring at 50 °C for 1 hour to completely volatilize the ethanol, Place the probe in an ice bath and sonicate for 5 minutes to obtain blank liposomes. The obtained blank liposomes were placed in a dialysis bag, the two ends were tied tightly, and dialyzed in 1000 mL of 0.9% NaCl solution for 24 hours to remove ammonium sulfate in the liposome external water phase. The dialyzed blank liposomes were incubated at 60° C., slowly added 1 mL of an aqueous solution containing 25 mg of verapamil hydrochloride under stirring, and continued to be incubated for 20 minutes to obtain verapamil hydrochloride lipos...

Embodiment 3

[0084] Verapamil Hydrochloride 50mg

[0085] Phosphatidylcholine 300mg

[0086] PEG2000-DSPE 10mg

[0087] Cholesterol 100mg

[0088] Preparation method: Dissolve the prescribed amount of verapamil hydrochloride, phospholipids, PEG2000-DSPE and cholesterol in 5 mL of ethanol, slowly inject into 10 mL of 0.9% NaCl solution at 50 °C under magnetic stirring, keep stirring at 50 °C for 30 min to dissolve the ethanol After the volatilization is complete, place the probe in an ice bath and sonicate for 5 minutes.

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Abstract

The invention discloses verapamil liposome and a preparation method of the verapamil liposome, belonging to the technical field of medicine. The verapamil liposome is composed of verapamil, phospholipid, cholesterol, chitosan, cationic lipid and antioxidant, etc., all of which are in certain weight percentage. The verapamil liposome is prepared by adopting ammonium sulphate gradients method, filmhydration method, ethanol injection method and reverse phase evaporation method. The invention adopts chitosan or derivatives of the chitosan to modify the surface of the liposome, and applies the chitosan to ophthalmic preparation, which can further increase corneal retention of the liposome and can remarkably improve the corneal penetration amount of the drug, with obvious advantages compared with ordinary liposome. With high entrapment efficiency, good stability, good biocompatibility, biological adhesiveness and biodegradability, the prepared liposome can realize sustained release and long-acting administration, particularly suitable for administration on ocular region, and can better play the ocular effects of anti-glaucoma and anti-cataract of verapamil.

Description

Technical field: [0001] The invention relates to the field of pharmaceutical preparations, in particular to verapamil liposomes and a preparation method thereof. Background technique: [0002] Verapamil is an aralkylamine calcium antagonist that exerts its pharmacological effects by regulating the influx of calcium ions on the cell membranes of cardiac conduction cells, cardiac contractile cells, and arterial vascular smooth muscle cells, but does not change serum calcium concentration. Verapamil is commonly used in the treatment of variant angina, unstable angina, and chronic stable angina; combined with digoxin to control ventricular rate in chronic atrial fibrillation and / or atrial flutter; to prevent paroxysmal supraventricular tachycardia rapid recurrent attacks; essential hypertension. [0003] With the deepening of its pharmacological research, the clinical application of verapamil is also becoming more and more extensive. Such as: treatment of bronchial asthma, liv...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K31/277A61K9/00A61K9/127A61K9/19A61K47/36A61P27/06A61P27/12
Inventor 潘卫三李宁关津李想庄春阳
Owner SHENYANG PHARMA UNIVERSITY
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