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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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  • Abstract
  • Description
  • Claims
  • Application Information

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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, screen through a large number of experiments, and innovatively use Daphne A in pulmonary drug delivery, Lactose was selected as the carrier material of Daphne A dry powder inhaler DPI

Method used

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

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0022] Embodiment 1: the establishment of the liquid phase condition of genkwa ester A and standard song

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

Embodiment 2

[0024] Embodiment 2: the preparation of genkwa ester A dry powder inhalation

[0025] The lactose used in the prescription is coarse lactose (d>110 μ m) and fine powder lactose (d: 4-11 μ m), after changing the ratio of the two, it is made into a dry powder inhaler (DPI) to investigate the effect of lactose particle size on Daphne genkwa The effect of DPI on the performance of DPI administration in the lungs. The five prescriptions are shown in the table below. Weigh the rough lactose and fine powder lactose of the prescribed amount, and calculate the weight ratio of Daphne A and total lactose as 1:5. Weigh genkwa ester A and mix evenly.

[0026] Table 1 DPI prescription of genkwa ester A with different ratios of rough lactose and fine powder lactose

[0027]

Embodiment 3

[0028] Example 3: Experimental Method for Screening the Prescription of Genkwa Esperidin A Dry Powder Inhalation Preparation by Medicinal Impactor

[0029] Each prescription among the embodiment 2 is made into 20 drug-containing capsules respectively, and each capsule contains powder 50mg. Use the NGI device to simulate human lung administration at a flow rate of 60L / min, rinse the collection trays and adapters with 50% methanol water, centrifuge at 12000r / min for 5min, take the supernatant and put it in a liquid phase vial for Determination of In Vitro Pulmonary Deposition of Daphne A DPI. The amount of drug deposition at all levels of the NGI device was calculated after sample injection. The results are shown in Table 2.

[0030] Table 2: The deposition amount of Daphne-methyl DPI in different formulations in the NGI device

[0031]

[0032]

[0033] Calculation results of in vitro deposition rate FPF

[0034] The in vitro deposition rate (FPF) is the most intuitiv...

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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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