Nimodipime nanometer suspension freeze-dried composition, its preparing method and use

Abstract

A freeze-dried nano-suspension of nimodipine for intravenous injection with low stimulation and high curative effect and stability contains nimodipine, surfactant and scaffolding agent. Its preparing process and application are also disclosed.

Description

technical field [0001] The invention relates to the field of pharmaceutical preparations, in particular to a nimodipine nanosuspension freeze-dried composition, a preparation method and application thereof. Background technique [0002] Nimodipine (molecular formula is C 21 h 26 N 2 o 2 , with a molecular weight of 418.45) belongs to 1,4-dihydropyridine calcium channel antagonists, which can selectively act on cerebral blood vessels, dilate cerebral arteries, increase cerebral blood flow without increasing brain metabolism, and also have anti-platelet aggregation effects . Clinically, it is mainly used for the treatment of cerebral vasospasm, sudden deafness, high blood pressure and migraine after arachnoid hemorrhage. [0003] At present, there are many formulations of nimodipine on the market at home and abroad, mainly including oral agents (such as ordinary tablets, sustained-release tablets, capsules, soft capsules) and injections (small water injections and large i...

AI Technical Summary

Problems solved by technology

Because nimodipine has very little solubility in water (about 1.4ug / ml at 37 degrees), its solid preparations are less dissolved in the gastrointestinal tract, and there is a strong hepatic first-pass effect in addition, resulting in bioavailability after oral administration. Low degree, requiring multiple doses

[0004] Yet, contain the organic solvent of about 30% in the nimodipine injection of clinical use, cause the stimulation of administration and toxic side effect (such as pain, vasculitis etc.)

At the same time, in clinical application, dilution is often required, and the concentration of organic solvents is reduced, resulting in the precipitation of nimodipine and interruption of treatment.

In order to avoid the precipitation of nimodipine in the infusion process, German bayer company uses accessories such as three-way valves to administer drugs through infusion pumps, which undoubtedly increases the cost of use and operational difficulty; Regularity often requires medical staff to pay special attention. Once the drug is precipitated, the drug must be replaced, which makes the dosage difficult to be accurate; and studies have shown that the drug content of nimodipine preparations solubilized by organic solvents is significantly reduced during storage and drug particles will be precipitated.

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