Powder manufacturing method suitable for inhalation-type drug administration

Abstract

The invention relates to a powder manufacturing method capable of accurately controlling aerodynamic force size of power particles and is suitable for inhalation-type drug administration. In the method, after 3,6-double (4-double fumaryl aminobutyl)-2,5-diketopiperazine or salt substituent thereof is dissolved into alkaline solution, drug is directly added into the solution, or the alkaline solution and the acid solution are mixed under high shearing environment to form injectable suspension, and then drug is added; and the solution or the injectable suspension is dried to prepare drug particles suitable for aerodynamic force size (0.5-10 micrometers). The drug particles are transported to positions, such as patient nasal cavity, bronchus, lungs and the like by a dry powder inhaler; the characteristics that drug particles are quickly dissolved in human body environment with the pH value of 6.4-8 and drug particles are stable when pH value is less than or equal to 6.4 or more than 8 are utilized to realize quick and effective adsorption of drug.

Description

technical field [0001] The present invention relates to the preparation method of powder suitable for inhalation administration, especially using 3,6-bis(4-bisfumarylaminobutyl)-2,5-diketopiperazine and its salt substitutes as medicine Method for manufacturing pharmaceutical powder of the carrier. Background technique [0002] Due to the large mucosal surface area of ​​the human nasal cavity, bronchi and lungs, and the drug particles can quickly penetrate the mucosal tissue and be absorbed by the human body, and can avoid the first-pass effect of the liver. Therefore, compared with oral administration and subcutaneous injection, inhalation Administration has the therapeutic advantage of more rapid administration. At present, there are many inhalation drug delivery systems that can deliver chemical drug ingredients or biological drug ingredients to the nasal cavity, bronchi, and lungs of patients through dry powder inhalers or nebulizers, and directly treat lesions in the na...

AI Technical Summary

Problems solved by technology

However, drug powder particles with an aerodynamic diameter of 0.5-10 microns are usually easy to agglomerate, which further increases the difficulty of precisely controlling the aerodynamic size of drug particles to achieve precise drug delivery

Most of the inhalation drug delivery systems currently on the market cannot precisely control the aerodynamic size of drug particles. After patients inhale these drugs, usually only a small number of particles have a suitable aerodynamic size (between 0.5-10 microns) and can be deposited to the mucosal surface and then absorbed by the body, so usually inhalation administration requires a large dose, and precise administration cannot be achieved

[0004] In addition, at present, many inhaled drug particles cannot be quickly dissolved in the human body environment with a pH value between 6.4-8, and the effective drug ingredients carried by them cannot be quickly absorbed by the human body through the mucosal tissue, and the respiratory system does not give full play to drug delivery. Rapid advantage; and the solid particles remaining on the mucosal surface will cause side effects such as respiratory system lesions