Powder manufacturing method suitable for inhalation-type drug administration

A manufacturing method and an inhalation-type technology, which can be used in pharmaceutical formulations, medical preparations containing active ingredients, powder delivery, etc., and can solve the problems of easy agglomeration of drug powder particles, inability to achieve rapid dissolution, and inability to quickly absorb effective drug ingredients.

Inactive Publication Date: 2010-10-13
于清
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0014] Example 1: Dissolve 10 grams of 3,6-bis(transmacroyl-4-aminobutyl)-2,5-diketopiperazine powder in 3 liters of 3% ammonia solution to form solution A . And prepare 3 liters of 5% glacial acetic acid solution to form solution B. Mix solutions A and B quickly and thoroughly in a container using a high-speed stirrer to form a suspension C containing micron-sized particles. Suspension C was concentrated by filtering and rinsing with 50 liters of pure water to obtain 500 ml of concentrated suspension D. Solution E was formed by dissolving 6 g of insulin powder in 50 ml of 3% glacial acetic acid solution. After mixing the concentrated suspension D and the glacial acetic acid solution E containing the drug ingredient insulin, the pH value of the suspension was adjusted to 4.0-5.0 with ammonia water to obtain 550 ml of suspension F. The suspension F was dropped into liquid nitrogen to form 510 grams of frozen solid particles, and the frozen solid particles were freeze-dried f...

Embodiment 2

[0015] Example 2: Dissolve 10 grams of 3,6-bis(transmacroyl-4-aminobutyl)-2,5-diketopiperazine powder in 3 liters of 3% ammonia solution to form solution A . And prepare 3 liters of 5% glacial acetic acid solution to form solution B. Solutions A and B are quickly and thoroughly mixed in a container using a high-speed stirrer to form a suspension C containing micron-sized particles. Suspension C was concentrated by filtering and rinsing with 50 liters of pure water to obtain 500 ml of concentrated suspension D. Solution E was formed by dissolving 6 g of insulin powder in 50 ml of 3% glacial acetic acid solution. After mixing the concentrated suspension D and the glacial acetic acid solution E containing the drug ingredient insulin, and adjusting the pH value of the suspension between 4-5 with ammonia water, 550 ml of suspension F was obtained. The suspension F was dried with a spray drier to form 11.3 g of medicated powder suitable for inhalation administration containing th...

Embodiment 3

[0016] Embodiment 3: directly dissolve 10 grams of 3,6-bis(transmacroyl-4-aminobutyl)-2,5-diketopiperazine powder and 6 grams of insulin powder in 5 liters of 3% In the ammonia solution, the solution A is formed, the pH value of the solution is adjusted between 7.5-8.5 with ammonia water, and the solution A is directly dried with a spray dryer to obtain 9.5 grams of medicated powder suitable for inhalation administration containing insulin components.

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PUM

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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...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/70A61K9/14A61K31/495A61P11/02A61P11/00
Inventor 于清
Owner 于清
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