A kind of levooxiracetam oral dispersible film and preparation method thereof

Abstract

The invention relates to an L-oxiracetam oral dispersible membrane and a preparation method thereof. The L-oxiracetam oral dispersible membrane is prepared by adopting materials, such as a composite membrane-forming material, a plasticizer and a filler. After being stuck to the tongue, the L-oxiracetam oral dispersible membrane cannot be easily spit out, and therefore is suitable for old people with dysphagia. Moreover, because the L-oxiracetam oral dispersible membrane can be absorbed through the mucous membrane, the first pass elimination effect is prevented, the bioavailability is increased, the dosage of medication is reduced, and thereby the side effect of the medicine is reduced. The preparation process of the invention is simple, and therefore is suitable for industrialized production.

Description

technical field [0001] The invention relates to a levoxiracetam orodispersible film and a preparation method thereof. Background technique [0002] Oxiracetam is a synthetic cyclic derivative of hydroxyaminobutyric acid (GABOB), which can promote ATP in the brain, promote the synthesis of acetylcholine and enhance the conduction of nerve excitation, and can improve the retrograde amnesia caused by hypoxia. Can enhance memory and improve learning ability. Levo-oxiracetam ((S)-4-hydroxy-2-oxo-1-pyrrolidineacetamide) is the levorotatory form of oxiracetam (Oxiracetam CAS 62613-82-5), a white microcrystalline powder , melting point 135-136°C, optical rotation -36.0° (C=1.00in water), the solubility of levo-oxiracetam is obviously better than that of the mixed body. Levo-oxiracetam is currently not reported as a single drug application. [0003] CN104069074A discloses a freeze-dried preparation of oxiracetam for injection, which is obtained by first forming an aqueous solution...

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.

[0004] 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

Oral dispersible tablets also have the problem of choking, but sucking dispersible tablets has a very slow onset of action, and there is a gritty and bitter taste, which is not conducive to taking

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