Dry powder inhalant for anesthesia and preparing method thereof

Abstract

Disclosed is a dry powder inhalant for anesthesia. The dry powder inhalant for the anesthesia is prepared by the following steps that dexmedetomidine hydrochloride injection and ketamine hydrochloride are used as raw materials, a certain amount of carriers, active protective agents, lubricating agents and pH adjusting agents are added, and pretreatment, mixing, drying, total mixing and injected packing are conducted. According to the dry powder inhalant for the anesthesia, special medicine feeding channels do not need to be established, in the medicine taking process, patients are painless, the compliance is good, the stability in the product storing process is good, pH changing and impurity increment in the storing process are low, the impurity increment within the expiry date is only 0.06%, the expiry date of products reaches above 36 months, the flowability of the powder is good, the angle of repose is less than 42 degrees, the content uniformity is good, the content RSD of a plurality of points is less than 1%, the preparing process is simple and easy to operate, and the dry powder inhalant for the anesthesia is worthy of market promotion.

Description

technical field [0001] The invention mainly relates to the technical field of pharmacy, in particular to a dry powder inhaler for anesthesia and a preparation method thereof. Background technique [0002] At present, the commonly used sedative drugs before examination in China are oral chloral hydrate or midazolam, and intramuscular injection of sodium lumina. The efficacy and use of these sedatives have the following problems: (1) chloral hydrate oral agent: it is the most commonly used sedative agent for children before examination in outpatient clinics. Because its mouthfeel is very bitter, many children refuse to take it or cause vomiting after taking it. Increased risk of aspiration, even life threatening. In addition, the metabolites of chloral hydrate are active and sometimes cause delayed awakening; at the same time, the drug has an obvious first-pass effect, and the sedative effect is uncertain, which often leads to sedation failure, and many children often need re...

AI Technical Summary

Problems solved by technology

The efficacy and use of these sedatives have the following problems: (1) chloral hydrate oral agent: it is the most commonly used sedative agent for children before examination in outpatient clinics. Because its mouthfeel is very bitter, many children refuse to take it or cause vomiting after taking it. Increased risk of aspiration, even life-threatening

In addition, the metabolites of chloral hydrate are active and sometimes cause delayed awakening; at the same time, the first-pass effect of the drug is obvious, and the sedative effect is uncertain, which often leads to sedation failure, and many children often need repeated medications

(2) Oral midazolam: the sedative effect is not good, and the success rate is only 60-75%

(3) Lumin sodium intramuscular injection: the success rate of sedation is about 80%, but it is accompanied by painful stimulation, which will cause harm to children

[0003] Dexmedetomidine hydrochloride is the dextro isomer of medetomidine, which is a derivative of imidazoles. It is a highly selective α2 receptor agonist, and its chemical name is: (+)-4-(S) -[1-(2,3-Dimethylphenyl)ethyl]-1H-imidazole hydrochloride acts on α2 receptors in the nucleus of the locus coeruleus of the brainstem to produce a good sedative effect, but 2ug / kg alone After sedation with dexmedetomidine, it is easy to be awakened by external stimuli, and the awakening rate can reach about 50%, resulting in failure of sedation; large doses of dexmedetomidine hydrochloride (>2ug / kg) can cause bradycardia

[0004] Ketamine is an NMDA receptor antagonist, which has analgesic, sedative and sympathetic stimulation effects, but generally its use requires a large dose, which is likely to cause blood pressure to rise and there is restlessness in the recovery period

[0005] To sum up, the research on dexmedetomidine hydrochloride and ketamine in the prior art still cannot meet the needs of clinical use, and there is an urgent need to develop a dry powder inhalation preparation that is convenient for clinical use, has a rapid onset of effect, is safe and effective; at present, Dry powder inhalers still have problems such as poor storage stability, large pH changes, difficult to control impurities, short shelf life, poor powder fluidity, resulting in large differences in finished product loading, and poor content uniformity in the preparation process, resulting in increased medication risks.

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