Stable 3-n-butylphthalide3-n-butylphthalide high-capacity injection and preparation method thereof

A technology of injection and butylphthalide, which is applied in the field of large-capacity injection of butylphthalide and its preparation, can solve problems such as product quality impact, difficult operation of dilution, and difficulty in clinical application, so as to make up for market gaps and avoid safety risks Effect

Pending Publication Date: 2019-12-10
CHENGDU SHIBEIKANG BIOLOGICAL MEDICINE TECH CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

When this dosage form is used for intravenous injection, it needs to be compatible with glucose injection or sodium chloride injection. It is difficult to operate when it is diluted in clinical application. It is difficult in clinical application and activated carbon is used in the preparation process, which has a certain impact on product quality.
[0008] In summary, the butylphthalide preparation process disclosed in the prior art is relatively complicated, or it is inconvenient for clinical application, and the injection preparation process uses activated carbon, which cannot completely reduce the patient's incompatibility to activated carbon, and the quality is not completely stable. Well meet the needs of clinical application of this product

Method used

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  • Stable 3-n-butylphthalide3-n-butylphthalide high-capacity injection and preparation method thereof
  • Stable 3-n-butylphthalide3-n-butylphthalide high-capacity injection and preparation method thereof
  • Stable 3-n-butylphthalide3-n-butylphthalide high-capacity injection and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0050] Embodiment 1, large-volume injection of butylphthalide, comprising racemic butylphthalide or L-butylphthalide, polyethylene glycol-15-hydroxystearate, sodium chloride and water for injection.

[0051] Prescription 1, calculated in 1000ml

[0052]

[0053]Preparation process: Add half of the prescribed amount of polyethylene glycol-15-hydroxystearate into the prescribed amount of racemic butylphthalide or L-butylphthalide at 60-65°C, stir and mix thoroughly; then add the prescribed amount Measure one-third of the water for injection and stir to make a milky solution. Dissolve the remaining polyethylene glycol-15-hydroxystearate of the prescription quantity in water for injection of one-third of the prescription quantity, stir, slowly add the milky solution, stir, then add the sodium chloride of the prescription quantity, set Make up to 1000ml, stir, filter with ultrafiltration membrane, fill with nitrogen protection, pack in 100ml per bottle / bag, and sterilize.

Embodiment 2

[0054] Embodiment 2, large volume injection of butylphthalide, comprising racemic butylphthalide or L-butylphthalide, polysorbate-80, sodium chloride, EDTA-2Na, pH regulator and water for injection.

[0055] Prescription 2, calculated in 1000ml

[0056]

[0057] Preparation process: at 60-65°C, add the prescribed amount of polysorbate-80 into the prescribed amount of racemic butylphthalide or L-butylphthalide, stir, and mix thoroughly; then add 70% of the prescribed amount of water for injection, stir, and prepare Get solution, add sodium chloride, EDTA-2Na of recipe quantity, be settled to 1000ml, stir, add pH adjuster (hydrochloric acid and / or sodium hydroxide), adjust pH to 6.5, ultrafiltration membrane ultrafiltration, according to each bottle 100ml per bag, dispensed and sterilized.

Embodiment 3

[0058] Embodiment 3, large volume injection of butylphthalide, comprising racemic butylphthalide or L-butylphthalide, poloxamer 188, sodium chloride, pH regulator and water for injection.

[0059] Prescription 3, calculated in 1000ml

[0060]

[0061]

[0062] Preparation process: at room temperature, add the prescribed amount of poloxamer 188 to the prescribed amount of racemic butylphthalide or L-butylphthalide, stir, and mix thoroughly; then add 70% of the prescribed amount of water for injection, and stir to prepare a solution , add the prescribed amount of sodium chloride, set the volume to 1000ml, stir, add pH adjuster (disodium hydrogen phosphate and / or sodium dihydrogen phosphate), adjust the pH to 6.5, ultrafiltration membrane ultrafiltration, nitrogen protection, press 100ml per bottle / bag, sterilized.

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Abstract

The invention relates to a stable 3-n-butylphthalide high-capacity injection and a preparation method thereof. The stable 3-n-butylphthalide high-capacity injection contains dl-3-n-butylphthalide or l-3-n-butylphthalide, a surface active agent, an osmotic pressure regulator, a pH regulator, a stabilizer, and water for injecting, wherein the surface active agent is selected from one or more of polyethylene glycol-15-hydroxystearate, polysorbate-80, poloxamer188 and lecithin. The 3-n-butylphthalide high-capacity injection is stable in quality, does not contain activated carbon, and has few particles and higher safety, and the quantity of the particles does not increase along with storage time; the content of 3-n-butylphthalide is high, and therefore the 3-n-butylphthalide high-capacity injection can be directly applied to intravenous injection, and accordingly meets requirements for clinical drug delivery; and a preparation technology is simple, ensures the stability of the injection andis high in operability, and thus industrial production is easily achieved.

Description

technical field [0001] The invention belongs to the field of pharmaceutical preparations, and in particular relates to a stable large-capacity injection of butylphthalide and a preparation method thereof. Background technique [0002] Butylphthalide: (3-n-butylphthalide, NBP for short), full name 3-butyl-1(H)-isobenzofuranone, also known as apigenin A, is extracted from celery seed, It can also be artificially synthesized. Butylphthalide is an oily liquid that is insoluble in water and has a strong celery smell. The molecule contains a chiral carbon atom, so it exists in two optical isomers, namely L-butylphthalide and D-butylphthalide. Butylphthalide can reduce the infarction after focal cerebral ischemia, increase the cerebral blood flow in the ischemic area and improve the microcirculation in the cerebral ischemic area, protect the mitochondrial function, reduce the degree of neurological damage, and improve the cerebral ischemia. Energy metabolism, etc., act on multipl...

Claims

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Application Information

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IPC IPC(8): A61K9/08A61K31/365A61K47/14A61K47/26A61K47/10A61K47/24A61K47/02A61P9/10
CPCA61K9/08A61K9/0019A61K31/365A61K47/14A61K47/26A61K47/10A61K47/24A61K47/02A61P9/10
Inventor 岑国栋杨茂廷谭少军罗厚华
Owner CHENGDU SHIBEIKANG BIOLOGICAL MEDICINE TECH CO LTD
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