Nimodipine injection composition, and preparation method and application thereof

A technology for nimodipine injection and composition, applied in the field of nimodipine injection composition and preparation thereof, can solve the problems of poor cyclodextrin biocompatibility, poor industrialization, long production cycle and the like, and achieve stable Good sex, convenient medication, large drug loading effect

Inactive Publication Date: 2013-11-20
SHANGHAI TIANSHILI MEDICAL TECH
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

The preparation reported in this study introduces more toxic benzyl alcohol, resulting in the result of taking care of one thing and losing another, and it is still not an ideal preparation
In addition, the Chinese patent application CN200410022169.3, the title of the invention is "Nimodipine Injection Emulsion and Its Preparation Method" and CN200510081668.4, the title of the invention is "Nimodipine Emulsion Injection and Its Preparation Method". Nimodipine has poor solubility in oil, resulting in a low drug loading directly into an emulsion. In order to ensure an effective dosage, a larger volume of emulsion needs to be infused, which will bring certain side effects
Foreign scholars (Ghareb M.Soliman, et al. Tailoring the of nimodipinedrug delivery using nanocarriers based on A B miktoarm star polymers, Biomaterials, 2010, 31(32): 8382) developed nimodipine polymer micellar solution in order to reduce the local irritation of commercially available nimodipine injection, but the preparation produced The cycle is long (stirred in the dark for 24 hours), and on the other hand, more than 20% of the medicine cannot be wrapped (retained by the microporous membrane of 0.45 micron), indicating that the industrialization degree of the preparation process is poor
In addition, the nimodipine cyclodextrin inclusion compound is prone to a series of allergic reactions and renal toxicity due to the poor biocompatibility of the cyclodextrin, and its applicability is poor.

Method used

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  • Nimodipine injection composition, and preparation method and application thereof
  • Nimodipine injection composition, and preparation method and application thereof
  • Nimodipine injection composition, and preparation method and application thereof

Examples

Experimental program
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Effect test

Embodiment 1

[0037] The present invention will now be described in detail in conjunction with the embodiments and drawings, but the implementation of the present invention is not limited thereto. Embodiment 1: A kind of composition of nimodipine injection

[0038] Preparation of Nimodipine Injection:

[0039] Weigh 4 grams of nimodipine, add 95 grams of polyethylene glycol 400, stir and dissolve at 60 ° C, then use polyethylene glycol 400 to make up to 100 ml; adjust the pH value to 4.50 with citric acid; add 0.2 grams Activated carbon was used for the needle, adsorbed at 60°C for 30 minutes, then filtered with a capsule filter, divided into 1ml / branch, sealed, and sterilized in a high-pressure steam sterilizer at 121°C for 15 minutes to obtain nimodipine Injection. Preparation of emulsion:

[0040] Weigh 100 grams of caprylic triglyceride for injection, 100 grams of soybean oil, heat in a water bath to 70°C, add 12 grams of egg yolk phospholipids for injection, cut to dissolve, stir an...

Embodiment 2

[0043] Embodiment 2: a kind of composition of nimodipine injection

[0044] Preparation of Nimodipine Injection:

[0045] Weigh 1 g of nimodipine, add it to 76 g of polyethylene glycol 400, stir and dissolve at 70°C, then use polyethylene glycol 400 to make the volume to 100 ml; add 0.01 g of activated carbon for needles, Adsorb at high temperature for 60 minutes, then filter with a microporous membrane, pack into 2ml / branch, seal, and sterilize with a circulating steam sterilizer at 100°C for 30 minutes to obtain nimodipine injection.

[0046] Preparation of emulsion:

[0047] Weigh 100 grams of caprylic triglyceride for injection, 100 grams of soybean oil, heat in a water bath to 80°C, add 12 grams of soybean lecithin for injection, shear to dissolve, stir and mix to obtain the oil phase; measure 700 grams of water for injection milliliter, add 22.5 grams of glycerin, stir to dissolve, and heat to 80°C to obtain the water phase; mix the oil phase and the water phase at a t...

Embodiment 3

[0050] Embodiment 3: A kind of composition of nimodipine injection

[0051] Preparation of Nimodipine Injection:

[0052] Weigh 5 grams of nimodipine, add it to 80 grams of polyethylene glycol 400, stir and dissolve at 80 ° C, then use polyethylene glycol 400 to make the volume to 100 ml; adjust the pH value to 3.5 with hydrochloric acid; add 0.1 g of Activated carbon for needles, adsorbed at 80°C for 45 minutes, then filtered with a microporous membrane, divided into 1ml / branch, sealed, and sterilized in a high-pressure steam sterilizer at 121°C for 15 minutes to obtain nimodipine injection liquid.

[0053] Preparation of emulsion:

[0054] Weigh 50 grams of caprylic triglyceride for injection, 50 grams of soybean oil, heat in a water bath to 65°C, add 30 grams of egg yolk phospholipids for injection, cut to dissolve, stir and mix to obtain the oil phase; measure 800 grams of water for injection milliliter, add 26 grams of glycerin, stir to dissolve, and heat to 65°C to ob...

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Abstract

The invention relates to the field of medicinal preparations. In order to increase the solubility of nimodipine in water, nimodipine injection sold on the market at home and abroad contains a great amount of organic solvent, but the high total content of organic solvent causes overlarge stimulation to blood vessels during direct injection, and a series of adverse effects such as phlebitis and the like are easily caused. The invention aims to provide a nimodipine injection composition, and a preparation method and application thereof. The preparation method comprises the following steps of: dissolving the nimodipine in a small amount of organic solvent for injection to obtain injection; and mixing with a small volume of emulsion to obtain the nimodipine injection composition. When the nimodipine injection composition is used, the injection in the composition is mixed with the small volume of emulsion, and intravenous injection is performed, or the composition mixed solution is dispersed in 5 percent glucose or physiological saline for intravenous drip. The injection composition has the advantages of high loading rate, low consumption of auxiliary materials, low toxicity, high stability, convenience in administration and the like; and during clinical administration, a three-way valve is not needed for assistance, a medicine is prevented from being separated out in the infusion process, and the administration safety is effectively improved.

Description

technical field [0001] The invention relates to pharmaceutical preparation technology, in particular to a composition of nimodipine injection and a preparation method and application thereof. Background technique [0002] Nimodipine, chemical name: (±)-2,6-dimethyl-4-(3-nitrophenyl)-1,4-dihydropyridine-3,5-dicarboxylic acid-(1-methyl Ethyl)-(2-methoxyethyl) ester, a light yellow crystalline powder, insoluble in water. It is a dihydropyridine calcium antagonist, which can easily pass through the blood-brain barrier and act on cerebrovascular and nerve cells. It can selectively act on cerebrovascular smooth muscle, expand cerebral blood vessels, increase cerebral blood flow, and significantly reduce ischemia caused by vasospasm. Acute brain injury, while increasing cerebral blood flow without affecting brain metabolism. It is clinically used to prevent and treat ischemic nerve damage caused by cerebral vasospasm after subarachnoid hemorrhage, as well as senile brain function...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K9/107A61K31/4422A61P9/10A61P25/06A61P27/16
Inventor 高保安金文斌
Owner SHANGHAI TIANSHILI MEDICAL TECH
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