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Nimodipine lipid microsphere injection and preparation method thereof

A nimodipine lipid and injection technology, which is applied in the direction of pharmaceutical formulations, oil/fat/wax non-active ingredients, medical preparations containing active ingredients, etc., can solve the problem of low solubility of nimodipine in the oil phase. To avoid the hepatic first-pass effect, improve bioavailability, and increase stability

Active Publication Date: 2009-07-22
沈阳信康药物研究有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0005] The main problem that nimodipine preparation technology exists is that the solubility of nimodipine in oil phase is not high, affects the drug effect of medicine

Method used

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  • Nimodipine lipid microsphere injection and preparation method thereof
  • Nimodipine lipid microsphere injection and preparation method thereof
  • Nimodipine lipid microsphere injection and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0052] Taking the production of 1,000 bottles of the nimodipine lipid microsphere injection product of the present invention as an example, the used raw materials and auxiliary materials and their mass ratios are:

[0053] Nimodipine 4g

[0054] Lecithin for Injection 60g

[0055] Soybean Oil for Injection 250g

[0056] Medium Chain Fatty Acid for Injection 250g

[0057] Glycerin 125g

[0058] Tween-80 5g

[0059] Sodium Oleate 1.5g

[0060] Add water for injection to 5000ml

[0061] In the proportioning of the raw materials used in the present embodiment, the mass percentages of the medicinal active ingredients and the auxiliary materials are:

[0062] Nimodipine 0.08%

[0063] Lecithin for Injection 1.2%

[0064] Soybean Oil for Injection 5%

[0065] Medium Chain Fatty Acids for Injection 5%

[0066] Glycerin 2.5%

[0067] Tween-80 0.1%

[0068] Sodium Oleate 0.03%

[0069] Water for injection was added to 100%.

[0070] Its preparation method is as follows:

...

Embodiment 2

[0082] Taking the production of 1,000 bottles of the nimodipine lipid microsphere injection product of the present invention as an example, the used raw materials and auxiliary materials and their mass ratios are:

[0083] Nimodipine 4g

[0084] Lecithin for Injection 25g

[0085] Soybean Oil for Injection 100g

[0086] Medium Chain Fatty Acid for Injection 100g

[0087] Glycerin 50g

[0088] Tween-80 7.5g

[0089] Sodium Oleate 2g

[0090] Add water for injection to 5000ml

[0091] In the proportioning of the raw materials used in the present embodiment, the mass percentages of the medicinal active ingredients and the auxiliary materials are:

[0092] Nimodipine 0.08%

[0093] Lecithin for Injection 0.5%

[0094] Soybean Oil for Injection 2%

[0095] Medium Chain Fatty Acids for Injection 2%

[0096] Glycerin 1%

[0097] Tween-80 0.15%

[0098] Sodium Oleate 0.04%

[0099] Water for injection was added to 100%.

[0100] The preparation method is the same as that...

Embodiment 3

[0102] Taking the production of 1,000 bottles of the nimodipine lipid microsphere injection product of the present invention as an example, the used raw materials and auxiliary materials and their mass ratios are:

[0103] Nimodipine 4g

[0104] Lecithin for Injection 115g

[0105] Soybean Oil for Injection 400g

[0106] Medium Chain Fatty Acid for Injection 400g

[0107] Glycerin 150g

[0108] Tween-80 10g

[0109] Sodium Oleate 2.5g

[0110] Add water for injection to 5000ml

[0111] In the proportioning of the raw materials used in the present embodiment, the mass percentages of the medicinal active ingredients and the auxiliary materials are:

[0112] Nimodipine 0.08%

[0113] Lecithin for Injection 2.3%

[0114] Soybean Oil for Injection 8%

[0115] Medium Chain Fatty Acids for Injection 8%

[0116] Glycerin 3%

[0117]Tween-80 0.2%

[0118] Sodium Oleate 0.05%

[0119] Water for injection was added to 100%.

[0120] The preparation method is the same as tha...

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Abstract

The invention provides a nimodipine lipid microsphere injection, which is prepared from the following components in percentage by weight: 0.08 percent of nimodipine, 0.5 to 2.3 percent of lecithin for injection, 2 to 8 percent of soybean oil for injection, 2 to 8 percent of medium chain fatty acid for injection, 1 to 3 percent of glycerin, 0.1 to 0.2 percent of tween-80, 0.03 to 0.05 percent of sodium oleic acid, and the balance being water for injection. The preparation method comprises steps of preparation of an oil phase, preparation of water phase, preparation of colostrum, homogenization and canning. In the nimodipine lipid microsphere injection, the soybean oil for injection and the medium chain fatty acid for injection are used to prepare the oil phase, the nimodipine is a fat soluble drug and can be better dissolved in the oil phase, the lipid microsphere in which the soybean oil for injection is the main component has solvent characteristics, is non-toxic, and can guide the fat soluble drugs to be dissolved in emulsion particles and perform the metabolism along with lipid oil drops and slowly release, thereby maintaining the effective blood concentration, lowering toxic and side effects of the drugs, increasing the solubility and stability of the nimodipine drug, improving the drug-loading rate and reducing the hydrolysis of the drugs.

Description

technical field [0001] The invention relates to the technical field of western medicine preparation, in particular to a nimodipine lipid microsphere injection and a preparation process thereof. Background technique [0002] Nimodipine (NMD for short) is a 1,4-dihydropyridine derivative. The chemical name is 3,5-pyridinedicarboxylic acid-1,4-dihydro-2,6-dimethyl-4-(3-nitrophenyl)-2-methoxyethyl-1-methylethyl ester . In 1988, it was used in clinical practice in China. In the past 20 years, nimodipine's effects of dilating cerebral blood vessels and improving cerebral blood supply have been affirmed and applied in clinical practice. It is mainly used as a vasodilator and in the treatment of cardiovascular and cerebrovascular diseases, neurological and endocrine diseases . [0003] At present, the commonly used nimodipine preparations in clinical practice include tablets, capsules and injections. Nimodipine is a poorly water-soluble drug with low solubility and strong liver ...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/16A61K31/4422A61K47/44A61P9/10A61P5/00A61P25/00
Inventor 唐星黄惠锋任延成宋莹王亚轩
Owner 沈阳信康药物研究有限公司
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