Thymopentin inhalation powder aerosol and preparation method thereof

A technology for inhaling powder and thymus, which is applied in the field of thymopentin inhalation powder and its preparation, can solve the problems of thymopentin not easy to degrade, low bioavailability, large energy consumption, etc., to achieve rich blood flow, biological High utilization and pain relief effect

Inactive Publication Date: 2015-04-22
陈长潭
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Since thymopentin is very water-soluble, it is difficult to be absorbed through the nasal mucosa barrier, and the bioavailability is low
In addition, thymopentin in dry powder preparations of thymopentin is not easy to degrade and has good solubility, but the process is complicated and consumes a lot of energy

Method used

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  • Thymopentin inhalation powder aerosol and preparation method thereof
  • Thymopentin inhalation powder aerosol and preparation method thereof
  • Thymopentin inhalation powder aerosol and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0044] Embodiment 1: the preparation of thymopentin inhalation powder spray

[0045] Grind 1g of Thymopentin finely, and use an ultrafine pulverizer to perform ultrafine pulverization to obtain an ultrafine dry powder with a particle diameter of 1 μm; grind 21.28g of mannitol, 106.42g of leucine, and 1.3g of poloxamer 188 at a high speed Pulverizer, high-speed grinding and pulverization, to obtain micropowder with a particle size of 60 μm ~ 80 μm; mix thymopentin ultrafine dry powder and auxiliary materials according to the method of equal increase, fill No. 5 capsules, each filling 130mg, and make 1000 capsules, namely The Thymopentin inhalation spray that gets the content of every dose of principal agent is 1mg.

Embodiment 2

[0046] Embodiment 2: the preparation of thymopentin inhalation powder spray

[0047] Grind 1g of Thymopentin finely, and use an ultrafine pulverizer to perform ultrafine pulverization to obtain an ultrafine dry powder with a particle size of 5 μm; grind 42.5g of mannitol, 85.2g of leucine, and 1.3g of poloxamer 188 at a high speed Pulverizer, high-speed grinding and crushing to obtain a particle size of 60 μm micropowder; Thymopentin ultrafine dry powder and auxiliary materials are mixed according to the method of equal increase, and filled with No. 5 capsules, each filled with 130mg, made into 1000 capsules, that is Thymopentin inhalation spray with a content of 1 mg main drug.

Embodiment 3

[0048] Embodiment 3: the preparation of thymopentin inhalation powder spray

[0049] Grind 0.5g of thymopentin finely, and ultrafinely pulverize with an ultrafine pulverizer to obtain an ultrafine dry powder with a particle diameter of 2 μm; mix 85.4g of mannitol, 42.7g of leucine, and 1.4g of poloxamer 188 with a high-speed Grinding and pulverizing with a high-speed grinding machine to obtain a micropowder with a particle size of 80 μm; mix the thymopentin ultrafine dry powder and auxiliary materials according to the method of equal increase, fill No. 5 capsules, each filling 130mg, and make 1000 capsules. The content of each main drug is 0.5 mg thymopentin inhalation spray.

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Abstract

The invention relates to the technical field of medicinal chemistry, and particularly relates to a thymopentin inhalation powder aerosol and a preparation method thereof. The medicine of the thymopentin inhalation powder aerosol is inhaled in a form of micropowder, and is directly carried into the lung to take effect; the toxic or side effects on the whole body caused by the medicine are reduced; the thymopentin inhalation powder aerosol is convenient to use and relatively low in price; the medicine is relatively good in stability; the thymopentin inhalation powder aerosol has the advantages of large absorbing surface, abundant blood in the absorbing part, and relatively low enzyme activity, relatively thin epithelial barrier and high membrane permeability by pulmonary inhalation; the first-pass effect of the liver can be avoided; the thymopentin inhalation powder aerosol is convenient to use; the pain of patients caused by needle administration is removed; the compliance of the patients is improved; and the thymopentin inhalation powder aerosol has the characteristics of being rapid to absorb, good in stability and high in bioavailability on treatment of viral upper respiratory infection.

Description

technical field [0001] The invention relates to the technical field of medicinal chemistry, in particular to a thymopentin inhalation powder and a preparation method thereof. Background technique [0002] Thymopentin is a chemically synthesized oligopeptide composed of five amino acids, arginine, lysine, aspartic acid, valine, and tyrosine. Thymopentin is the immune active part of thymopoietin Ⅱ, which has the function of regulating and enhancing the immune function of human cells. [0003] The ways to realize the immunomodulatory effect of thymopentin include: (1) Inducing and promoting the differentiation, proliferation and maturation of T cells; (2) Regulating the proportion of T cell subsets, which is CD 4 + / CD 8 + Tend to normal (including two-way regulation of hypersensitive state of immune function and patients with low immune function); (3) enhance the immune function of red blood cells; (4) increase the phagocytosis of macrophages; (5) increase natural killing ...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/72A61K38/08A61P37/04A61P37/02
Inventor 黄阿三李仁祥孙立新陈玉叶吴乾方
Owner 陈长潭
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