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Stable fasudil hydrochloride injection and preparation method thereof

A technology of fasudil hydrochloride and injection, which is applied in the directions of non-active ingredient medical preparations, medical preparations containing active ingredients, and pharmaceutical formulas, can solve the problems of increasing the content of insoluble particles, and achieve lower dosage and clarity. Good quality and stability

Active Publication Date: 2016-09-07
中润药业有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

The pharmaceutical composition of fasudil hydrochloride improves the stability of the preparation to light by adding a certain amount of cysteine ​​hydrochloride, but cysteine ​​hydrochloride is only stable under acidic conditions, and is stable under neutral and alkaline conditions. It is easy to form water-insoluble cystine precipitates, which increases the content of insoluble particles in the injection

Method used

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  • Stable fasudil hydrochloride injection and preparation method thereof
  • Stable fasudil hydrochloride injection and preparation method thereof
  • Stable fasudil hydrochloride injection and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0041] Every 1000 described fasudil hydrochloride injections, its formula consists of:

[0042]

[0043] The stabilizer is composed of N-carboxymethyl chitosan and reduced glutathione in a mass ratio of 1:0.25.

[0044] Preparation:

[0045](1) Take the prescribed amount of water for injection and use a polyvinyl chloride exchange column containing diethylaminoethyl dextran gel to remove pyrogens, then feed carbon dioxide to saturation, and set aside;

[0046] (2) Fasudil hydrochloride, N-carboxymethyl chitosan, reduced glutathione, anhydrous citric acid, sodium citrate dihydrate and sodium chloride were mixed in the prescribed amount, and added The water for injection with 90% of the prescription volume treated in step (1) is stirred until dissolved, and the pH is adjusted to 5.0 with hydrochloric acid or sodium hydroxide, and then 3 g of medicinal charcoal that is frozen in a refrigerator at -10 ° C is added, and stirred and adsorbed for 15 minutes , filter and decarbon...

Embodiment 2

[0049] Every 1000 described fasudil hydrochloride injections, its formula consists of:

[0050]

[0051] The stabilizer is composed of N-carboxymethyl chitosan and reduced glutathione in a mass ratio of 1:0.25.

[0052] The preparation method is the same as in Example 1.

Embodiment 3

[0054] Every 1000 described fasudil hydrochloride injections, its formula consists of:

[0055]

[0056] The stabilizer is composed of N-carboxymethyl chitosan and reduced glutathione in a mass ratio of 1:0.25.

[0057] The preparation method is the same as in Example 1.

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Abstract

The invention belongs to the field of pharmaceutical preparation, and particularly relates to stable fasudil hydrochloride injection and a preparation method thereof. The fasudil hydrochloride injection comprises fasudil hydrochloride, stabilizers, anhydrous citric acid, sodium citrate dihydrate, sodium chloride and water for injection, wherein the stabilizers comprise N-carboxymethyl chitosan and reduced glutathione according to the mass ratio of 1:(0.05-0.35). The preparation method includes the steps: dissolving components in the formula by the water for injection after pyrogen removal; adjusting pH (potential of hydrogen); adding medicinal carbon for stirring adsorption to further remove pyrogen and perform discoloration; performing filtration and decarburization; performing filtration, sterilization, sub-package, potting and sterilization to obtain the fasudil hydrochloride injection. The fasudil hydrochloride injection has fine light stability and simple in formula, insoluble particles are effectively suppressed, the preparation process is easily operated, and industrialization is facilitated.

Description

technical field [0001] The invention belongs to the field of pharmaceutical preparations, in particular to a stable fasudil hydrochloride injection and a preparation method thereof. Background technique [0002] Fasudil hydrochloride, chemical name is hexahydro-1-(5-sulfonylisoquinoline)-1(H)-1,4-diazepine hydrochloride, a RHO kinase inhibitor and novel intracellular Ca 2+ antagonist. The drug can dilate blood vessels by increasing the activity of myosin light chain phosphatase, reduce the tension of endothelial cells, improve the microcirculation of brain tissue, protect ischemic brain tissue, and at the same time antagonize inflammatory factors, protect nerves against apoptosis, and promote neuroprotection. regeneration. Clinically, it is mainly used to prevent and improve vasospasm caused by various reasons, selectively expand the spasmed blood vessels, and improve the state of heart and brain ischemia. Existing studies have shown that Fasudil hydrochloride has certa...

Claims

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Application Information

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IPC IPC(8): A61K9/08A61K31/551A61K47/36A61K47/12A61K47/42A61P9/08A61P9/10A61P25/00
CPCA61K9/0019A61K9/08A61K31/551A61K47/12A61K47/36A61K47/42
Inventor 魏林华魏林友崔旭升
Owner 中润药业有限公司
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