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Nimodipine sub micro-emulsion injection and preparation method thereof

A technology of nimodipine and nimodipine, which is applied in the field of medicine, can solve the problems of patient inconvenience and reinforcement, and achieve the effects of reducing workload, improving compliance, and avoiding drug precipitation

Inactive Publication Date: 2009-04-29
李淑斌
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, on June 10, 2005, the State Food and Drug Administration issued a notice that due to the monitoring of adverse reactions, it was required to strengthen the management of the use of benzyl alcohol injection and strictly prohibit it from being used for intramuscular injection in children, which brought inconvenience to patients.

Method used

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  • Nimodipine sub micro-emulsion injection and preparation method thereof
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  • Nimodipine sub micro-emulsion injection and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0039] (1) Under the protection of nitrogen, weigh 1.0 g of nimodipine, 80 g of soybean oil, 25 g of soybean lecithin, 1.0 g of oleic acid, and 0.5 g of α-tocopherol, and stir and dissolve in a water bath at 65° C. as the oil phase; ( 2) Weigh 15 g of glycerin and add it to an appropriate amount of water for injection, and dissolve it in a water bath at 65° C. as the water phase. (3) Drop the water phase into the oil phase under stirring, cut it into colostrum by high-speed shearing machine, adjust the pH to 5.5 with 0.2% citric acid, add water for injection to 1000mL; Circulate the emulsion 6 times to reach the specified particle size, filter and sterilize through a 0.22 μm filter membrane, fill with nitrogen and repackage, and sterilize to obtain nimodipine submicroemulsion injection with a particle size of 197.6 nm and a zeta potential value of -36 mv.

Embodiment 2

[0041] (1) Under nitrogen protection, weigh 1.5 g of nimodipine, 60 g of medium-chain triglycerides, 30 g of egg yolk phospholipids, 3.0 g of linoleic acid, and 1 g of tocopherol, and place them in a water bath at 70° C. for stirring and dissolving as an oil phase; (2) Weigh 5.0 g of poloxamer, add 20 g of sorbitol into an appropriate amount of water for injection, dissolve in a water bath at 70° C., and serve as the water phase. (3) Drop the water phase into the oil phase under stirring, and cut it into colostrum by high-speed shearing machine, adjust the pH to 5.0 with 0.5mol / L phosphoric acid, add water for injection to 1000mL; The machine circulates the emulsion 7 times until it reaches the specified particle size, and then it is sterilized by filtration through a 0.22 μm filter membrane, filled with nitrogen, and then sterilized to obtain nimodipine submicroemulsion injection with a particle size of 200.4nm and a zeta potential value of -25mv .

Embodiment 3

[0043] (1) Under the protection of nitrogen, weigh 3.0 g of nimodipine, 100 g of olive oil, and 45 g of egg yolk phospholipids, place them in a water bath at 75°C and stir to dissolve them as the oil phase; (2) weigh 2.0 g of sodium oleate and 2.0 g of sodium sulfite g, adding 60 g of glycerin into water for injection, and dissolving in a water bath at 75° C. as the water phase. (3) Drop the water phase into the oil phase under stirring, cut it into colostrum by high-speed shearing machine, adjust the pH to 7.0 with 0.1mol / L NaOH solution, add water for injection to 1000mL; The machine circulates the emulsion 8 times until the specified particle size is reached, and is sterilized by filtration through a 0.22 μm filter membrane, filled with nitrogen, subpackaged, and sterilized to obtain nimodipine submicroemulsion injection with a particle size of 199.4nm and a zeta potential value of -32mv .

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Abstract

The invention provides a nimodipine submicron emulsion injection and a preparation method thereof. The invention adopts nimodipine of effective dose as a drug and contains pharmaceutic adjuvant such as oil phase, an emulsifier, an auxiliary emulsifying agent, a pH regulator, and an iso-osmotic regulator; the nimodipine, the emulsifier; the auxiliary emulsifying agent and oil used for injection are weighed according to the formula amount, stirred and dissolved in a water bath, added with water used for injection and the iso-osmotic regulator and the like, and fully mixed and emulsified; the pH value of the solution is regulated and the solution is added with the water used for injection until the specified cubage; a high-pressure homogenizer is used for carrying out homogenization for a plurality of times until specified granularity is realized; a filtering membrane of 0.22 Mum is used for filtering and sterilizing; and nitrogenization, subpackaging and sterilization are carried out, and the nimodipine submicron emulsion injection is obtained. The nimodipine submicron emulsion injection of the invention does not contain auxiliary cosolvents, such as benzoic alcohol, polyethylene glycol, and the like, and has the advantages of high drug-load rate and packaging efficiency, slow release of drugs, good stability, and the like. The preparation process is simple, and a preparation which does not contain any organic solvent is provided, thus radically eliminating the defects of organic solvents, separating out no drugs, reducing the work load of medical care personnel and eliminating the psychological burden of the medical care personnel and patients; in addition, the nimodipine submicron emulsion injection has low cost and stable quality and is suitable for industrialized large scale production.

Description

technical field [0001] The invention relates to the technical field of medicine, in particular to nimodipine submicroemulsion injection and a preparation method thereof. Background technique [0002] Nimodipine is a Ca 2+ Channel blockers. Normally, the contraction of smooth muscle depends on Ca 2+ Enters the cell, causing depolarization of the transmembrane current. Nimodipine effectively blocks Ca 2+ Enter the cell, inhibit the contraction of smooth muscle, and achieve the purpose of relieving vasospasm. Animal experiments have proved that the effect of nimodipine on cerebral arteries is much stronger than that of arteries in other parts of the body, and because of its high lipophilicity, it can easily penetrate the blood-brain barrier. When used in the treatment of subarachnoid hemorrhage, the concentration of cerebrospinal fluid can reach 12.5ng / ml. It can be inferred that it can be used clinically to prevent vasospasm after subarachnoid hemorrhage, but the mechani...

Claims

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Application Information

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IPC IPC(8): A61K9/107A61K31/435A61P9/08
Inventor 李淑斌宁红高娜刘丹魏晓莹
Owner 李淑斌
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