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Inhalant, preparation method thereof, and application of inhalantas inhalant carrier with pullulan

A pullulan sugar and inhalant technology, applied in pharmaceutical formulations, medical preparations containing active ingredients, drug delivery, etc., can solve problems such as low lung inhalation efficiency, achieve fast dissolution speed, excellent lubricity, and increase the surface area. glossy effect

Inactive Publication Date: 2013-05-22
SUZHOU HUIREN BIOLOGICAL SCI & TECH
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Lactose has a strong adhesion effect, resulting in low lung inhalation efficiency. Generally speaking, the dose that can actually reach the lungs is only 10% to 30% of the set dose.

Method used

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  • Inhalant, preparation method thereof, and application of inhalantas inhalant carrier with pullulan
  • Inhalant, preparation method thereof, and application of inhalantas inhalant carrier with pullulan
  • Inhalant, preparation method thereof, and application of inhalantas inhalant carrier with pullulan

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0041] Dissolve the pullulan and pharmacologically active substances in the following Table 1 in water according to a certain weight ratio, and then spray-dry under standard working conditions to form drug granules, and the powder spray 1 can be obtained. The lung deposition efficiency was obtained under the standard operation of simulating lung deposition in vitro, expressed as the ratio of microparticles, as shown in Table 1.

[0042] Composition and microparticle ratio of drug particles in powder aerosol 1 in table 1

[0043]

Embodiment 2

[0045] Dissolve the pharmacologically active substances in Table 2 and pullulan in the same aqueous solution at a certain weight ratio, then add adjuvants of the corresponding weight ratio to the solution as required, and spray and dry under standard working conditions to generate drug particles. Get powder spray 2. The lung deposition efficiency was obtained under the standard operation of simulating lung deposition in vitro, expressed in the ratio of microparticles, as shown in Table 2.

[0046] Composition and microparticle ratio of drug particles in powder aerosol 2 in table 2

[0047]

Embodiment 3

[0049] Dissolve the pharmacologically active substances in Table 3 in water, then add adjuvants of corresponding weight ratios as required, and spray-dry to generate drug granules under standard working conditions; the pullulan granules are spray-dried or other known methods (such as ball milling, Jet powder, spray freeze-drying) obtained. The drug granules and the pullulan granules are mixed mechanically according to a certain weight ratio to obtain the compound drug granules, and the powder aerosol 3 can be obtained. Standard detection methods were used to measure the lung deposition efficiency, expressed as the ratio of microparticles, as shown in Table 3.

[0050] Composition and microparticle ratio of drug particles in powder aerosol 3 in table 3

[0051]

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PUM

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Abstract

The invention discloses inhalant, a preparation method thereof, and application of the inhalant as an inhalant carrier with pullulan. The particle diameter of drug particles for lung inhalation in the dry-powder inhalant disclosed by the invention is 0.1-50 mu m, preferably 0.3-15 mu m, more preferably 0.5-5 mu m. Generally, the dosage of drugs inhaled for each time is 0.1 mu g to 500 mg. The effective deposition rate of the inhalant in the lung is increased by 16-400%. The inhalant has high bioavailability and can be used for treating local or systemic diseases. The inhalant disclosed by the invention has important value for increasing the pulmonary delivery efficiency of drugs.

Description

technical field [0001] The invention relates to the field of pharmaceutical preparations, in particular to an inhalant, a preparation method thereof and the application of pullulan as an inhalant carrier. Background technique [0002] Pulmonary drug delivery system (PDDS) refers to a drug delivery system that can deliver drugs to the lungs to produce local or systemic therapeutic effects. As a new drug delivery site, the lung is determined by its physiological structure: an adult has 300-400 million alveoli, with a total area of ​​70-100m 2 , and the alveolar epithelial cells are very thin (0.1-0.2 μm), surrounded by dense capillaries, the drug can be quickly absorbed and directly enter the systemic circulation to achieve the purpose of systemic / targeted therapy. Administration in the form of lung inhalation has obvious advantages: 1. No hepatic first-pass effect, no gastrointestinal degradation; 2. Rapid drug inhalation and rapid onset of action; 3. Can be used to treat lo...

Claims

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Application Information

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IPC IPC(8): A61K9/72A61K47/36A61K45/00
Inventor 李浩莹徐恩宇
Owner SUZHOU HUIREN BIOLOGICAL SCI & TECH
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