Fasudil hydrochloride lipo-microballoons carrier preparation and preparation method thereof

A technology of fasudil hydrochloride and lipid microspheres, applied in the field of medicine, can solve problems such as poor stability, and achieve the effects of improving stability, reducing drug toxicity, and reducing drug side effects

Inactive Publication Date: 2009-08-19
HAINAN LINGKANG PHARMA CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0006] Aiming at the defect of poor stability of the current Fasudil Hydrochloride Injection, the object of the present invention is to provide a Fasudil Hydrochloride Injection with significantly improved stability

Method used

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  • Fasudil hydrochloride lipo-microballoons carrier preparation and preparation method thereof
  • Fasudil hydrochloride lipo-microballoons carrier preparation and preparation method thereof
  • Fasudil hydrochloride lipo-microballoons carrier preparation and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0029] Embodiment 1 The preparation of Fasudil hydrochloride lipid microsphere preparation

[0030] Prescription (1000 bottles): Fasudil Hydrochloride 30g

[0031] Soy Lecithin 50g

[0032] Glycerin 40g

[0033] Oleic acid 5g

[0034] Sodium bisulfite 12g

[0035] Corn oil for injection 120g

[0036] Water for injection 1000g

[0037] Preparation Process

[0038] (1) 30g fasudil hydrochloride is added in 120g corn oil for injection to obtain an oil phase;

[0039] (2) 50g of soybean lecithin, 40g of glycerin, 5g of oleic acid, and 12g of sodium bisulfite were dissolved in water to obtain an aqueous phase;

[0040] (3) Mix the oil phase and the water phase, transfer to a tissue masher, rotate at 8000r / min, stir at high speed for 10 minutes, filter through a microporous membrane, fill with nitrogen, potting, and autoclave at 115°C to obtain the product.

Embodiment 2

[0041] Embodiment 2 Preparation of Fasudil Hydrochloride Lipid Microsphere Preparation

[0042] Prescription (1000 bottles): Fasudil Hydrochloride 30g

[0043] Soy Lecithin 80g

[0044] Myristic acid 20g

[0045] Sodium thiosulfate 25g

[0046] Corn oil for injection 90g

[0047] Water for injection 800g

[0048] Preparation Process

[0049](1) 30g of fasudil hydrochloride is added in 90g of corn oil to obtain an oil phase;

[0050] (2) 80g soybean lecithin, 20g myristic acid, and 25g sodium thiosulfate are dissolved in water to obtain an aqueous phase;

[0051] (3) Mix the oil phase and the water phase, transfer to a tissue grinder, rotate at 12000r / min, stir at high speed for 30 minutes, filter through a microporous membrane, fill with nitrogen, potting, and autoclave at 115°C to obtain the product.

Embodiment 3

[0052] Example 3 Preparation of Fasudil Hydrochloride Lipid Microsphere Preparation

[0053] Prescription (1000 bottles): Fasudil Hydrochloride 15g

[0054] Soy Lecithin 130g

[0055] Linoleic Acid 20g

[0056] Sodium chloride 14g

[0057] Sodium formaldehyde bisulfite 15g

[0058] Corn oil for injection 200g

[0059] Water for injection 1000g

[0060] Preparation Process

[0061] (1) 15g of fasudil hydrochloride is added in 200g of corn oil to obtain the oil phase;

[0062] (2) 130g of soybean lecithin, 20g of linoleic acid, 14g of sodium chloride, and 15g of sodium formaldehyde bisulfite were dissolved in water to obtain an aqueous phase;

[0063] (3) Mix the oil phase and the water phase, transfer to a tissue grinder, rotate at 10,000r / min, stir at high speed for 20 minutes, filter through a microporous membrane, fill with nitrogen, potting, and autoclave at 115°C to...

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Abstract

The invention relates to a hydrochloric acid Fasudil fat microsphere preparation and a method for preparing the same. By taking soyabean lecithin as an emulsifying agent and corn oil for injection as an oil phase solvent and comprising an antioxidant commonly used in pharmaceutical products, the preparation is prepared. The preparation has the advantages of simple process, low cost and easy industrialized production; and compared with the prior hydrochloric acid Fasudil injection, the injection prepared by the method has obviously improved stability.

Description

technical field [0001] The invention relates to a lipid microsphere preparation, in particular to a fasudil hydrochloride lipid microsphere preparation and a preparation method thereof, belonging to the technical field of medicine. Background technique [0002] Fasudil hydrochloride, chemical name is hexahydro-1-(5-isoquinolinesulfonyl)-1H-1,4-diazepine hydrochloride, molecular formula C 14 h 17 N 3 o 2 S HCl, molecular weight 327.83, structural formula: [0003] [0004] Is a protein kinase inhibitor that is intracellular calcium antagonists. The contraction of vascular smooth muscle is due to intracellular Ca 2+ The significant increase in concentration activates key enzymes, when Ca 2+ When reaching a certain concentration, with Ca 2+ The binding protein calmodulin binds, activates myosin light chain phosphorylase, phosphorylates the myosin light chain, and causes muscle contraction. During subarachnoid hemorrhage, various vasoconstrictor substances released fr...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/10A61K31/551A61K47/44A61P9/10A61K47/24
Inventor 邓菊娟
Owner HAINAN LINGKANG PHARMA CO LTD
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