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Cinobufagin dry power inhaler and preparation method and application thereof

A cinobufacin-based, dry powder inhaler technology, which is applied in pharmaceutical formulations, powder delivery, respiratory diseases, etc., can solve problems that have not been reported in research, and achieve the goal of reducing toxic and side effects, fast onset of action, and rapid absorption Effect

Active Publication Date: 2013-08-28
南京南药医药科技有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

There is no report on the study of Cinobufacien-based dry powder inhalation with anti-lung tumor effect

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0022] Preparation of inhalation: Cinobufin base was pulverized to D 90 = less than 5 microns, mixed with lactose having a particle size of 80-110 microns in a mass ratio of 1:9, packing the drug powder into capsules or blisters or dry powder inhalers to obtain an inhaler.

Embodiment 2

[0024] Preparation of inhalation: Cinobufin base was pulverized to D 90 = 4 microns, mixed with lactose with a particle size of 80-125 microns and leucine with a particle size of 35-70 microns in a ratio of 10:90:3, packed into capsules or blisters or dry powder inhalers, to obtain inhalant.

Embodiment 3

[0026] Preparation of inhalation: Cinobufin base was pulverized to D 90 = 4 microns, mixed with leucine with a particle size of 80-150 microns in a ratio of 1:9, packed into capsules or blisters or dry powder inhalers to obtain an inhaler.

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PUM

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Abstract

The invention relates to a cinobufagin dry power inhaler, in particular to a dry power inhaler made of cinobufagin, a preparation method of the dry power inhaler and application of the dry power inhaler in preparation of drugs for treating tumors of lung. The cinobufagin dry power inhaler is characterized by consisting of the cinobufagin and medically acceptable auxiliary materials, and the mass ratio of the cinobufagin to the medically acceptable auxiliary materials is 1: 0.03 - 1:110. The cinobufagin is prepared to be the dry powder inhaler, therefore, the cinobufagin can be directly acted on pulmonary lesions, the happening of adverse actions is reduced, the bioavailability of the drug is enhanced, the defects of oral formulation including slow effect, liver first-pass effect to liver,low bioavailability and the like are overcome, and synchronously the problems of injection including inconvenience for use, bad compliance of patients and the like are also solved.

Description

Technical field: [0001] The invention relates to a dry powder inhaler, specifically a dry powder inhaler made of cinobufaction base, a preparation method of the dry powder inhaler and an application in the preparation of a drug for treating lung tumors. Background technique: [0002] Cinobufin toxin base is the main active ingredient in toad venom. It belongs to cardiac glycosides and is a fat-soluble substance. The molecular formula is: C 26 h 34 o 6 , has pharmacological effects such as anti-tumor, analgesic and cardiotonic, anti-inflammatory and immune-enhancing. At present, oral preparations containing cinobufaction base have been applied clinically, and have good curative effects on liver cancer, lung cancer, gastric cancer, etc., and have synergistic effects on chemotherapy and radiotherapy. However, oral preparations need to go through the first-pass effect of the liver, the onset of action is slow, and the bioavailability of the preparations is low. Although the ...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K9/72A61K9/14A61K31/585A61K47/26A61P11/00A61P35/00
Inventor 张振海陈彦贾晓斌刘璇杜萌
Owner 南京南药医药科技有限公司
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