Midazolam medicament composition as well as preparation method and application thereof

Abstract

The invention belongs to fields of pharmacy and pharmaceutics and relates to a midazolam medicament composition as well as a preparation method and application thereof. Particularly, the midazolam medicament composition comprises midazolam and / or pharmaceutically acceptable salts of midazolam, serving as main medicament components, and pharmaceutically acceptable auxiliary materials, wherein the content of the main medicament components is 0.2%-2%. The midazolam medicament composition provided by the invention is administered through an orifice, so that the bioavailability and curative effectof the midazolam medicament are improved, and favorable compliance can be achieved.

Description

technical field [0001] The invention belongs to the field of pharmacy and pharmacy, and relates to a midazolam pharmaceutical composition, a preparation method and application thereof. Background technique [0002] Midazolam is a benzodiazepine sedative-hypnotics with anti-anxiety, sedative, hypnotic, muscle relaxation, anticonvulsant and antiepileptic effects. Midazolam is a lipophilic substance that forms a stable water-soluble salt in an acidic solution with pH<4, and its hydrochloride or maleate is often used in clinical preparations. After entering the human body, midazolam salt can regain its high lipophilicity under the condition of physiological pH value, and can quickly pass through the blood-brain barrier, so the effect is rapid. [0003] Currently commercially available midazolam preparations include tablets and injections, which are clinically used for pre-anesthesia medication, spinal anesthesia and local anesthesia auxiliary medication, and operations durin...

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Problems solved by technology

[0007] The patent application with publication number CN 1830447A discloses a midazolam oral film, which improves the controllability of the midazolam dosage and is easy to use, but it cannot fundamentally improve the midazolam The disadvantage of low oral bioavailability

[0008] Publication No. CN 1929816A discloses a high-concentration midazolam administered through the nasal cavity, which avoids the first-pass effect, but also has shortcomings, because the given drug is a high-concentration midazolam Midazolam solution, its stability is a crucial issue, and the separation of medicine at the site of administration is difficult to avoid. The inventors use high-concentration midazolam solution (50mg / ml, propylene glycol and glycerol solubilization) When administering toad mucosa, it was found that once the drug solution came into contact with the mucous membrane, a large amount of drug was precipitated immediately

In addition, the local irritation caused by drug precipitation also exists objectively. In addition, the combined drug mentioned in the patent may cause spit-and-pharynx phenomenon when administered intranasally. Lun is extremely bitter, so it is difficult to avoid bringing discomfort to patients, especially children

[0009]Although as early as the early 1980s, people have carried out many studies on the in vivo behavior of midazolam after administration, so far, no There are better reports or products on the market of midazolam in terms of convenience and good bioavailability

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