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Nimodipine fat emulsion concentrate and preparation method and use thereof

A technology for nimodipine fat and emulsion concentrate, which is applied in the fields of emulsion delivery, cardiovascular system diseases, nervous system diseases, etc., and can solve the problems of poor doctor-patient compliance, irritation, and poor water solubility of nimodipine.

Inactive Publication Date: 2015-06-17
天津迈迪瑞康生物医药科技有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0003] Nimodipine has poor water solubility, and its injection has added ethanol with a volume fraction of more than 20% as a cosolvent, which is prone to local irritation during injection, and crystals will precipitate during the placement of nimodipine injection, so hot water is required before use Make it dissolve, poor doctor-patient compliance

Method used

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  • Nimodipine fat emulsion concentrate and preparation method and use thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0139] Embodiment 1: the preparation of nimodipine fat emulsion concentrate sample 1

[0140] Its composition is as follows:

[0141] Nimodipine 0.25g

[0142] Medium-chain fatty acid glycerides (Crodamol, GTCC) 29 grams

[0143] soybean oil 29 grams

[0144] 1, 2-propanediol 8.7g

[0145] Soy Lecithin 10g

[0146] Polyglyceryl Oleate 3.3g

[0147] Polyethylene glycol lauryl hydroxystearate (Solutol HS 15, BASF) 10.6 g

[0148] Tween 80 8.7g

[0149] Oleic acid 0.25g

[0150] Vitamin E 0.2g

[0151] The nimodipine fat emulsion concentrate preparation method is as follows:

[0152] 1) At 20°C, add the above-mentioned weight of soybean lecithin and polyglycerol oleate into medium-chain fatty acid glycerides and soybean oil, and stir at 20,000 rpm until a transparent and clear solution is formed;

[0153] 2) Add the above weight of nimodipine to the product of step 1) at 20°C, and keep stirring at 200rpm until the whole system is transparent;

[0154] 3) Add the above-...

Embodiment 2

[0156] Embodiment 2: the preparation of nimodipine fat emulsion concentrate sample 2

[0157] Its composition is as follows:

[0158] Nimodipine 0.5g

[0159] Medium-chain fatty acid glycerides (Miglyol 812, SASOL) 67g

[0160] 1, 2-Propanediol 8.3g

[0161] Soy Lecithin 7.5g

[0162] Polyglyceryl Oleate 4.2g

[0163] Polyethylene glycol lauryl hydroxystearate (Solutol HS 15, BASF) 8.3 g

[0164] Tween 80 4g

[0165] Oleic acid 0.2g

[0166] The nimodipine fat emulsion concentrate preparation method is as follows:

[0167] 1) At 45°C, add the above-mentioned weight of soybean lecithin and polyglycerol oleate to medium-chain fatty acid glycerides, and stir at 2000rpm until a transparent and clear solution is formed;

[0168] 2) Add the above-mentioned weight of nimodipine to the product of step 1) at 35°C, and keep stirring at 1000rpm until the whole system is transparent;

[0169] 3) Add the above-mentioned weight of 1,2-propanediol, Tween 80, polyethylene glycol laur...

Embodiment 3

[0171] Embodiment 3: the preparation of nimodipine fat emulsion concentrate sample 3

[0172] Its composition is as follows:

[0173] Nimodipine 0.5g

[0174] Medium-chain fatty acid glycerides (Miglyol 812, SASOL) 67g

[0175] 1,2-propanediol 9 grams

[0176] Soy Lecithin 12g

[0177] Polyethylene glycol lauryl hydroxystearate (Solutol HS 15, BASF) 7.5 g

[0178] Tween 80 3.5g

[0179] Oleic acid 0.3g

[0180] Vitamin E 0.2g

[0181] The nimodipine fat emulsion concentrate preparation method is as follows:

[0182] 1) At 30°C, add the above-mentioned weight of soybean lecithin to medium-chain fatty acid glycerides, and stir at 10,000 rpm until a transparent and clear solution is formed;

[0183] 2) Add the above weight of nimodipine to the product of step 1) at 45°C, and keep stirring at 2000rpm until the whole system is transparent;

[0184] 3) Add the above-mentioned weight of 1,2-propanediol, polyethylene glycol lauryl hydroxystearate, Tween 80, oleic acid, and vi...

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Abstract

The invention relates to a nimodipine fat emulsion concentrate and a preparation method and use thereof, and belongs to the field of medicine and pharmacy. The nimodipine fat emulsion concentrate overcomes the defects of complex traditional fat milk preparation process and poor product stability. The nimodipine fat emulsion concentrate is simple in preparation process only needing simple physical mixing without homogenization process. The product can be sterilized through a 0.22 mum millipore filter film, and can spontaneously emulsify during clinical use by dilution with normal saline or glucose solution and other water solutions and slight oscillation, and under the optimal conditions, average particle size is about 0.2 mum, and fully shows injection fat milk properties. The nimodipine fat emulsion concentrate product has good liquidity, and may not be hung on the wall, the appearance is single-phase, transparent and clear, clarity detection is acceptable, and after repeated freezing and thawing, preparation stratification phenomenon does not occur. The nimodipine fat emulsion concentrate product is used for prevention and treatment of ischemic neurological damage caused by cerebral angiospasm after subarachnoid hemorrhage and senile brain function impairment, hemicranias, sudden deafness and other diseases.

Description

technical field [0001] The invention belongs to the field of pharmacy and pharmacy, and relates to nimodipine fat emulsion concentrate, its preparation method and application. Background technique [0002] Nimodipine is a second-generation dihydropyridine calcium antagonist, which can act on cerebrovascular and nerve cells through the blood-brain barrier. It has the functions of protecting and promoting memory and promoting mental recovery. It is clinically used to prevent Vasospasm after subarachnoid hemorrhage. The pharmacological properties of nimodipine are to selectively dilate cerebral blood vessels without stealing blood, and increase cerebral blood flow without affecting brain metabolism. It has anti-depression and improves learning and memory functions. In addition, it can reduce the fragility of red blood cells, plasma viscosity and inhibit platelet aggregation. It is clinically used for the prevention and treatment of ischemic nerve injury caused by cerebral va...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/107A61K31/4422A61P25/00A61P9/10A61P25/06A61P27/16
Inventor 杨杰其他发明人请求不公开姓名
Owner 天津迈迪瑞康生物医药科技有限公司
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