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Ultra-fine dry powder particle suitable for drug administration for lung, and preparation method thereof

A dry powder and granule technology, which can be applied to pharmaceutical formulations, medical preparations without active ingredients, and medical preparations containing active ingredients, etc. It can solve the problems of low particle deposition rate, inconvenient practical application, and easy inactivation of active pharmaceutical ingredients.

Active Publication Date: 2012-01-04
杭州畅溪制药有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Introducing how to utilize volatile salts to prepare fine dry powder particles with excellent aerosolization properties is another object of the present invention. Through the present invention, the existence of ultrafine dry powder particles in the lungs prepared by the existing AIR dry powder preparation technology is solved. The dry powder particle size is too large, the particle density is too small, it is inconvenient for practical application, and it is easy to absorb water and make its aerosolization properties drop sharply, resulting in the technical defect that the active ingredients of the drug are easily inactivated. The dry powder produced by the spray drying technology developed by the company, due to its high particle density, the small geometric size of the particles results in a relatively small deposition rate of the particles in the alveolar area, which cannot be used to deliver proteins, peptides and nucleic acids containing DNA and RNA. drug problem

Method used

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  • Ultra-fine dry powder particle suitable for drug administration for lung, and preparation method thereof
  • Ultra-fine dry powder particle suitable for drug administration for lung, and preparation method thereof
  • Ultra-fine dry powder particle suitable for drug administration for lung, and preparation method thereof

Examples

Experimental program
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Effect test

example 1

[0126] Example 1. Levodopa (Levodopa) dry powder preparation

[0127] Parkinson's disease is an age-related degenerative disorder of the central nervous system, the symptoms of which can be manifested as inactivity, slowness, rigidity of movement and tremor. Oral drug levodopa has a significant effect on early Parkinson's hypokinetic symptoms. However, the current oral dopa drugs have other shortcomings. With the development of the disease, the efficacy of the drug is limited, and the bioavailability of the drug is difficult. It is predicted that these defects caused by oral administration may be completely eliminated by pulmonary inhalation administration.

[0128] An inhalable dry powder containing levodopa can be made in the following manner. In this example, the granules contain 20% (by weight, the same below) of levodopa, 20% of sodium citrate, 10% of calcium chloride, And 50% 1,2-dipalmitoyl-sn-propanetriyl-3-phosphatidylcholine, i.e. Dppc.250 milliliters, the formula s...

example 2

[0136] Example 2. Ketoprofen dry powder preparation

[0137] Ketoprofen is a non-steroidal anti-inflammatory drug approved by the US Food and Drug Administration. Pain-relieving drugs, as commonly used drugs in daily life and medical treatment, have huge market potential, and at the same time, there is an urgent need to improve the curative effect of existing drugs. As we all know, whether it is treating acute pain or penetrating pain, it is very important to make the drug concentration in the blood reach the effective therapeutic level as soon as possible so as to relieve pain. According to the characteristics of the inhalation administration method, the inhalation administration of analgesic drugs will have unique advantages in terms of rapid onset of effect. There is no doubt that there will be benefits for patients.

[0138] Inhalable dry powder containing ketoprofen (Ketoprofen) can be prepared as follows, in this example, the granule contains 20% (by weight) of ketopro...

example 3

[0144] Example 3. Epinephrine dry powder preparation

[0145] Anaphylaxis and death from anaphylaxis are becoming more common, especially in children and young adults, and the rapid onset and severity of symptoms make the treatment of anaphylaxis extremely difficult.

[0146] Intramuscular injection of adrenaline is the most important drug in the treatment of allergies, and it is very effective, but many allergy medicine experts worry about serious consequences and even death caused by delay in administration due to pain caused by intramuscular injection. The inhalation type can completely change the user's fear of needles, and can make the medicine quickly enter the blood to act on the disease.

[0147] Dry powders containing epinephrine can be prepared as follows. In this example, the dry powder granules contain 10% epinephrine (percentage by weight, the same below). 60% DPPC, 20% sodium citrate and 10% calcium chloride. 250 milliliters of solid concentration is 3 grams p...

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Abstract

The invention discloses a superfine drymeal granule suitable for pulmonary administration and a preparation method thereof. The drymeal granule has good air-atomizing property. With smaller geometric dimension, the drymeal granule can deposit in the alveolus area to maximum extent, so the active molecule of the medicine has higher bioavailability. In addition, the drymeal granule can be used for DNA and RNA lung administration. The invention is also designed to introduce how to use volatility salt to prepare the superfine drymeal granule with good air-atomizing property. The invention solves the technique defects of the over size of the drymeal granule, the low density of the granule, inconvenient application and easy inactivation of active drug ingredients caused by the sharp decline of the air-atomizing property resulting from the water absorbability in the lung superfine drymeal granule prepared by the existing drymeal preparation technique. Meanwhile, the invention also solves theproblem that the drymeal produced by the spray drying technology which is developed by Nektar Company, U.S.A, has relatively small deposition rate in the alveolus area and can not be used for transmitting protein, peptide or nucleic acid drugs containing DNA and RNA, and the like, caused by relatively small granule size and relatively high granule density.

Description

technical field [0001] The invention relates to the field of medicine preparation and delivery, in particular to an ultrafine dry powder particle suitable for pulmonary administration and a preparation method thereof. Background technique [0002] Inhalation drug therapy has a long history of use in the medical field. The earliest records of the application of drug therapy through the lungs can be traced back to thousands of years. Hippocrates in ancient Greece and Zhang Zhongjing in ancient China wrote in their works All mentioned the method that reaches the treatment disease by inhaling medicine. However, in the history of the development of medicine, the pulmonary drug delivery method is not the main drug delivery method, and the more commonly used drug delivery methods are still oral and injection. However, oral drugs and injections have their inherent defects. For example, oral drugs participate in the circulation of the body slowly, and it is difficult to reach the le...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K9/14A61K9/72A61K45/00A61K47/02A61K47/12A61K47/24A61K47/26A61K47/34A61K47/36
Inventor 陈晓东
Owner 杭州畅溪制药有限公司
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