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High-porosity dry powder inhaler carrier and supersaturated synthesis method and applications thereof

A dry powder inhaler, high porosity technology, used in medical preparations containing active ingredients, powder delivery, aerosol delivery, etc., can solve the problems of crystalline drug distribution, unevenness, poor absorption, etc. Controllable, improved uniformity, and high practicability

Inactive Publication Date: 2017-07-07
谭淞文
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Due to the improvement of spray drying parameters, the mixing degree of each drug component has been improved, and the product particles can reach a smaller particle size after spray drying treatment, which meets the standard requirements; but because spray drying granulation has higher requirements for solute solubility Large, the drug product cannot be fully dissolved in water, resulting in crystallization of the product and uneven distribution of the drug, and poor absorption. At the same time, the particle size range of the spray-dried granulation is wide, usually 1-20 microns (with a median particle size of 10 microns For example), the size uniformity is not high, which affects the drug delivery efficiency of pulmonary medication
[0005] In order to improve the porosity of the carrier particle material for adsorbing drug particles, a flower-shaped particle material has been described in the prior art, which is published in the 7th issue of "Nature Nanotechnology" in 2012 by Jun Ge et al. "inorganic hybrid nanoflowers" protein material, indicating that the porous flower-shaped granular material can greatly improve the loading capacity, efficiency and shelf life of the drug when used as a drug carrier; but the protein carrier material cannot be used as a drug carrier for the lungs. The carrier material also cannot use this method to synthesize flower-shaped granular materials similar to this form

Method used

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  • High-porosity dry powder inhaler carrier and supersaturated synthesis method and applications thereof
  • High-porosity dry powder inhaler carrier and supersaturated synthesis method and applications thereof
  • High-porosity dry powder inhaler carrier and supersaturated synthesis method and applications thereof

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Embodiment 1

[0037] This embodiment provides a high-porosity dry powder inhaler carrier, which is a flower-shaped porous dry powder particle with a rough surface. The median diameter of a single particle under the electron microscope is 0.5-50 microns (controlled by the parameters of the preparation method), and the drug molecule The carrying capacity is 5-50% mass fraction, and the way of carrying drug molecules includes physical contact adsorption, micropore capillary action adsorption, and intermolecular force adsorption; the N of the high-porosity dry powder inhaler carrier before carrying drug molecules 2 The adsorption specific surface area is 10-100 square meters per gram, and the BET pore size distribution range includes micro (50 nanometers); the high-porosity dry powder inhaler carrier is in N after loading drug molecules 2 The specific surface area of ​​adsorption decreases to 1-50% of the original value, and the change of microscopic morphology is mainly reflected in the decrea...

Embodiment 2

[0046] This embodiment provides a method for preparing a high-porosity dry powder inhaler carrier, comprising the following steps:

[0047] S1: Mix 50 grams of lactose with 50 grams of water (1:1 mass fraction ratio);

[0048] S2: Heating the mixed solution to 99 degrees, stirring and dissolving to obtain a 1g / g lactose solution;

[0049] S3: Quickly add high-temperature lactose solution to 1L ethanol solvent at 20 degrees (1:20 volume fraction ratio);

[0050] S4: after standing at room temperature for 5 minutes, centrifuge to separate the solid, and dry it with wind at room temperature.

Embodiment 3

[0052] This embodiment provides a method for preparing a high-porosity dry powder inhaler carrier, comprising the following steps:

[0053] S1: Mix 10 grams of lactose with 100 grams of water (mass fraction ratio of 1:10);

[0054] S2: spray drying at 150 degrees to prepare lactose supersaturated solid phase sample particles;

[0055] S3: quickly add lactose particles into 400mL ethanol solvent at 25 degrees (mass fraction ratio of 1:40);

[0056] S4: The solid was separated after standing at room temperature for 30 minutes, and dried at 40°C for 2 hours to constant weight.

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Abstract

The invention relates to a high-porosity dry powder inhalant carrier and its supersaturated synthesis method and application. The carrier is a flower-shaped porous dry powder particle with a rough surface. The median diameter of a single particle under an electron microscope is 0.5-50 microns. The carrying capacity of drug molecules is 5-50% mass fraction, and the N2 adsorption specific surface area of ​​the carrier is 10-100 square meters per gram, containing micro, medium and macro pores. For the first time, the present invention combines supersaturated synthesis technology and flower-shaped material preparation technology, and applies it to the field of dry powder inhalants. Using the synthesis method provided by the invention, the high-porosity dry powder inhalant carrier is prepared with controllable size and high performance. The porosity nanopore system is used for the adsorption, carrying and transportation of nano-level and molecular-level components, with good uniformity, stability and transmission efficiency. The invention realizes efficient, high-quality, cheap and practical mass production of nano- and micron-level high-porosity dry powder inhalant carrier materials.

Description

technical field [0001] The invention relates to the technical field of drug carriers, in particular to a high-porosity dry powder inhaler carrier and its supersaturated synthesis method and application. Background technique [0002] Dry powder inhaler is a commonly used spray for lung medication. It is composed of drug molecules and carrier particles, in which the drug molecules act on the lungs, and the carrier material is used to carry the drug molecules to achieve the effect of drug delivery. The carrier used as a dry powder inhaler has strict health requirements and must be a material that can be absorbed by the respiratory tract and lung cells or has no effect, such as sugars and sugar alcohols; considering the size of the lung terminal channel, direct drugs or carriers The shape of the material is preferably particles with a size of 1-5 microns. At the same time, based on the structure of the respiratory tract of the lungs, the carrier material for the front-end delive...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/16A61K9/72A61K47/26A61K47/36A61K47/18A61K45/00A61K31/405A23L29/30
CPCA61K9/0073A61K9/1617A61K9/1623A61K9/1652A61K31/405A61K45/00
Inventor 谭淞文谭松林谭越谭旭
Owner 谭淞文
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