Method for preparing levo-oxiracetam oral instant film agent through hot-melting extrusion

Abstract

The invention discloses a method for preparing levo-oxiracetam oral instant film agent. Levo-oxiracetam, a film-forming material, a plasticizer, a saliva irritant and a corrigent are completely ground and uniformly mixed to form a film through hot-melting extrusion. Water or an organic solvent does not participate in the preparation process, so that the bubble problem caused by the existence of the solvent and the problem of high water content of the film agent are solved, and the uniformity of the levo-oxiracetam oral instant film agent is effectively guaranteed.

Description

technical field [0001] The invention relates to oxiracetam, in particular to a method for preparing levo-oxiracetam oral instant film by hot-melt extrusion. Background technique [0002] Oxiracetam, chemically named 4-hydroxy-2-oxo-1-pyrrolidineacetamide, is a nootropic drug synthesized for the first time in 1974 by the Italian Shi Kebichem company. Aminobutyric acid (GABOB) derivatives, can promote learning, enhance memory, and protect the central nervous system drugs of damaged nerve cells. Its structure is as follows: [0003] [0004] CN102552125A discloses that it can improve the memory and learning function of patients with mental retardation; it is also suitable for memory and mental retardation caused by mild to moderate vascular dementia, senile dementia and traumatic brain injury or as an auxiliary therapeutic drug. CN102600130A discloses its new clinical application for the treatment of epilepsy. At present, oxiracetam mainly includes injections, capsules and...

AI Technical Summary

Problems solved by technology

This type of preparation is directly injected into tissues or blood vessels, and there is no absorption process or the absorption process is very short, so the blood concentration can quickly reach the peak to play a role; Most require higher equipment conditions, and the drugs in the injection are generally dispersed in water as micron-sized solid particles in the molecular state, with a large degree of dispersion, and high-temperature sterilization often results in drug hydrolysis, oxidation, and solid particle coalescence Stability issues such as large size

At the same time, because the injection directly and quickly enters the human body without the protection of the normal physiological barrier of the human body, if the dosage is improper or the injection is too fast, or there is a problem with the quality of the drug, it may bring harm to the patient, or even cause irreparable consequences.

In addition, injection pain, inability to administer drugs by the patient, local induration of injection, and vascular inflammation caused by intravenous injection are all problems in clinical application.

[0006] CN101732251A discloses a liposome of oxiracetam, which is prepared from oxiracetam, phospholipids, cholesterol, Tween 80 and an appropriate amount of osmotic pressure regulator and buffer solution; the liposome has good stability and encapsulation efficiency High, low toxicity and side effects; but the liposome preparation process is complicated, not suitable for large-scale production; more importantly, the curative effect of liposomes in the human body remains to be further studied, and there are few liposome preparations for clinical use in China at present

Although the oral instant film has many advantages, the limitations of its film-forming materials and preparation technology lead to low drug loading, the disintegration time and tensile strength are not easy to control, and most of the time it needs to mask the taste, which restricts the oral instant dissolution. Development and application of film agent

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