Dry powder inhalant with lung cancer-resistant activity

A dry powder inhaler, anti-lung cancer technology, applied in the field of biomedicine, to achieve the effects of high safety, low adverse reactions, and increased concentration

Active Publication Date: 2017-02-22
NANJING UNIVERSITY OF TRADITIONAL CHINESE MEDICINE
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0008] The purpose of the present invention is to solve many problems such as toxicity caused by Daphne A in the treatment of lung cancer, overcome the obstacles in application, scr

Method used

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  • Dry powder inhalant with lung cancer-resistant activity
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  • Dry powder inhalant with lung cancer-resistant activity

Examples

Experimental program
Comparison scheme
Effect test

Example Embodiment

[0022] Example 1: The liquid phase conditions of Daphne A and the establishment of the standard song

[0023] The experiment uses Daphne ketone A crude drug, the structural formula is as figure 1 , Establish liquid analysis conditions, chromatographic column: Merck C18 column (4.6mm×250mm, 5μm), mobile phase: methanol-water (82:18), column temperature 40℃, flow rate 1.0mL / min, detection wavelength 233nm, The injection volume is 20μL. Take the peak area (A) as the ordinate and the concentration (C) as the abscissa to perform linear regression to obtain the standard curve equation: A=19910C-12788(r 2 =1, the accuracy, precision and recovery rate are good, in line with the requirements of the analytical method), the linear range is 2.5-80μg / mL.

Example Embodiment

[0024] Example 2: Preparation of Daphne geniella dry powder inhalant

[0025] The lactose used in the formulation is coarse lactose (d>110μm) and fine powdered lactose (d: 4-11μm). By changing the ratio of the two, a dry powder inhalant (DPI) is made to investigate the effect of lactose particle size on Daphne The effect of Ester A DPI on the pulmonary administration performance, five prescriptions are shown in the table below. Weigh the prescription amount of coarse lactose and fine powdered lactose, and each recipe is based on the weight parts of Daphne A and total lactose 1:5 Weigh Daphne geni and mix well.

[0026] Table 1 Different ratios of coarse lactose and fine powdered lactose DPI prescription

[0027]

Example Embodiment

[0028] Example 3: The experimental method for screening the prescription of the medicinal impactor on the dry powder inhalation preparations

[0029] Each prescription in Example 2 was made into 20 medicated capsules, and each capsule contained 50 mg of powder. Use the NGI device to simulate human lung drug delivery at a flow rate of 60L / min. Wash each collection tray and adapter with 50% methanol water. After centrifugation at 12000r / min for 5 minutes, take the supernatant and place it in a liquid phase vial. Determination of the amount of genitalium DPI in the lungs in vitro. Calculate the amount of drug deposition at each stage of the NGI device after sample injection. The results are shown in Table 2.

[0030] Table 2: The amount of deposits of different formulations of DPI in the NGI device

[0031]

[0032]

[0033] Calculation results of in vitro deposition rate FPF

[0034] In vitro deposition rate (FPF) is the most intuitive indicator for investigating the aerodynamic part...

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Abstract

The invention discloses a dry powder inhalant with lung cancer-resistant activity. The dry powder inhalant with the lung cancer-resistant activity comprises yuanhuacine and a lactose carrier, wherein the lactose carrier is prepared from rough lactose with the diameter being more than 110 microns and fine lactose with the diameter being 4 to 11 microns. According to the dry powder inhalant with the lung cancer-resistant activity, the yuanhuacine and the inhalable lactose are innovatively mixed to prepare the dry powder inhalant for treating lung cancer, the medicine is directly given to a target part locally and accurately, the concentration of the medicine at the target point is increased, the toxic and side effects of other tissues are reduced and the curative effect is improved. An optimal prescription process is screened out by using a new-generation medicinal impactor to simulate a pulmonary administration method, so that more medicines are settled in the lung, an in-situ administration effect is achieved, and the lung tissue targeting aim is fulfilled. The dry powder inhalant with the lung cancer-resistant activity can obviously increase the concentration of the medicines in the lung tissue, improve the curative effect of treating the lung cancer, reduce the distribution of the medicines in the heart, liver, spleen, kidney, brain and reproductive system and reduce the toxicity on other tissues.

Description

technical field [0001] The invention belongs to the biomedicine technology, and in particular relates to a dry powder inhalation preparation with genkwa ester A as an active ingredient. The preparation can improve drug efficacy, concentrate drug concentration, and reduce toxic and side effects on non-target parts. Background technique [0002] Lung cancer is one of the most common malignant tumors. Globally, the morbidity and mortality of lung cancer are on the rise, especially in developing countries such as China. In my country, the morbidity and mortality of lung cancer rank first among all malignant tumors, among which the morbidity and mortality of males rank first, the incidence of females ranks second (only lower than breast cancer), and the mortality rate ranks first. The first one. The environmental pollution caused by the rapid development of industrialization and the high smoking rate have made the harm of lung cancer to Chinese residents gradually increasing. In ...

Claims

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Application Information

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IPC IPC(8): A61K9/72A61K47/26A61K31/357A61P35/00
CPCA61K9/0075A61K31/357A61K47/26
Inventor 陈志鹏李曼范亲李伟东段金廒
Owner NANJING UNIVERSITY OF TRADITIONAL CHINESE MEDICINE
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