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Application of wilforlide A inhalation preparation in medicine for treating lung inflammation

A technology of triptolide A and inhalation preparations, applied in drug combination, drug delivery, antipyretics, etc., to achieve low bioavailability, high safety, and avoid systemic adverse reactions

Active Publication Date: 2022-02-15
SHENZHEN NEPTUNUS PHARMA RES INST CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0007] At present, there are rare reports that WA is made into powder and aerosol products and used to treat lung inflammation

Method used

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  • Application of wilforlide A inhalation preparation in medicine for treating lung inflammation
  • Application of wilforlide A inhalation preparation in medicine for treating lung inflammation
  • Application of wilforlide A inhalation preparation in medicine for treating lung inflammation

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0015] Embodiment 1 contains the preparation of triptolide A (Wilforlide A) powder spray

[0016] References [Que Huiqing, Geng Yingying, Lin Sui, Li Yuanchao. Study on the chemical constituents of Tripterygium wilfordii [J]. Chinese herbal medicine, 2005(11): 1624-1625.] Extracted triptolide A, and micronized it into triptolide after extraction Raw material of rattan lactone A (Wilforlide A, WA).

[0017] Referring to [Feng Li. Development of aztreonam lung inhalation powder aerosol [D]. Chongqing Medical University, 2007.] The method in the article, and according to the characteristics of the drug in this experiment, appropriately modified, weighed triptolide A ( WilforlideA, WA) raw material 2g, glycine 3g, lactose 1g, WA was dissolved in 100mL of absolute ethanol, magnetically stirred for 30min, after WA was completely dissolved, glycine and lactose were dissolved in 30mL of water under magnetic stirring, and slowly added into the ethanol solution of WA, after the solutio...

Embodiment 2

[0020] The influence of embodiment 2 different doses of WA powder aerosol on pulmonary inflammation

[0021] Refer to [Zhang Yaping, Selection of acute pneumonia model in rats induced by lipopolysaccharide inhalation through different routes[J]. Chinese Journal of Experimental Formulas, 2018,24(07):82-88.] part 2.2.1, through nebulization inhalation A method for making an animal model of pneumonia with LPS and making appropriate adjustments. After 3 days of continuous modeling, continue modeling for 4 days, and simultaneously utilize the rat respiratory tract dosing device to give the powder aerosol in embodiment 1 (dose is set to be 0mg / kg, 1mg / kg , 2mg / kg, 4mg / kg, 8mg / kg; dosage is based on active ingredient WA); set non-modeling normal animal group simultaneously as negative control; adopt oral administration of hormone methylprednisolone 10mg / kg as positive control ( hormone group). For the degree of inflammation and index detection methods in each animal group, refer to...

Embodiment 3W

[0032] Embodiment 3WA absorption kinetics in vivo

[0033] Reference [WANG Z, YEUNG S, CHEN S, et al.Bioavailability of wilforlide A inmice and its concentration determination using an HPLC-APCI-MS / MS method[J].JChromatogr B Analyt Technol Biomed Life Sci,2018,1090:65 -72.] The measurement method is to measure the systemic bioavailability of WA through powder spray administration, so as to investigate the degree and risk of systemic distribution of WA after powder spray administration.

[0034] SD rats were divided into groups (4 in each group) and given WA powder aerosol (based on WA content) inhalation administration of 1 mg / kg, 2 mg / kg, 4 mg / kg, 8 mg / kg; intravenous administration of 1 mg / kg. According to the time point of the above reference method, blood was taken, measured, and kinetic parameters were calculated, and the bioavailability of other groups was calculated with AUC0-∞ of intravenous injection as 100%.

[0035] Part of the pharmacokinetic parameters measured a...

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Abstract

The invention discloses application of a wilforlide A inhalation preparation in preparation of a medicine for treating lung inflammation. The lung inflammation particularly refers to inflammation caused by lung infection. The wilforlide A inhalation preparation comprises wilforlide A serving as an active ingredient and pharmaceutic adjuvants, the particle size of micro powder is 1-4 microns, and the daily dosage of the wilforlide A is 1-200mg / 60kg / person.

Description

technical field [0001] The invention relates to the use of triptolide A (Wilforlide A) inhalation preparation in the preparation of medicines for treating pulmonary inflammation. Background technique [0002] Lung infection is a major factor in the pathogenesis of many respiratory infectious diseases, and inflammation of the lungs can cause serious physical damage. In many large-scale epidemics, lung inflammation caused many deaths. In the clinical first aid and treatment of acute infection of the respiratory tract in many countries, the rapid reduction of the inflammatory response can effectively save the patient, leaving enough time for the patient to establish immunity and giving the doctor enough time for treatment. [0003] At present, the first-line medication of this kind of drugs is still hormone drugs. Such drugs are generally administered orally or injected systemically, and high-dose pulse therapy can bring serious adverse reactions, such as high-risk cases of f...

Claims

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Application Information

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IPC IPC(8): A61K9/72A61K31/585A61K47/18A61K47/26A61P11/00A61P29/00
CPCA61K31/585A61P11/00A61P29/00A61K9/0075A61K47/183A61K47/26
Inventor 冯贻东黄传贵
Owner SHENZHEN NEPTUNUS PHARMA RES INST CO LTD