Unlock instant, AI-driven research and patent intelligence for your innovation.

Ambroxol dry powder for inhalation use with bronchial target

A technology of ambroxol and dry powder, applied in the field of Ming Dynasty, can solve the problems of inability to rapidly relieve the disease of the patient, inconvenient to use and transport, the pain of the patient, etc., and achieves good and fast effect, good targeting, and convenient use and carrying. Effect

Inactive Publication Date: 2020-01-14
HOLLYCON ITAL PTE LTD
View PDF3 Cites 3 Cited by
  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Oral formulations are slow acting, they enter the gastrointestinal tract, are absorbed by the bloodstream, exert systemic effects, and they do not provide rapid relief to patients
Although the parenteral route of administration provides a rapid therapeutic effect, it acts systemically, is relatively difficult to administer and causes pain to the patient
Nebulized inhalers require the use of large-volume nebulizers to aerosolize the liquid and then inhale it, which is difficult to use and transport

Method used

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
View more

Examples

Experimental program
Comparison scheme
Effect test

no. 1 approach

[0034] According to a first embodiment, the method provides a step in which the drug product of ambroxol and / or its hydrochloride is micronized by jet milling (jet milling), thereby obtaining the desired particle size. According to one embodiment, the process gas employed will have a pressure of about 7 bar. The powder thus prepared can be homogeneously mixed with excipients and / or pharmaceutically acceptable dispersants.

[0035] The powder thus obtained is preferably inserted as a single dose hermetically in blisters or capsules made of aluminum in the amounts indicated in the description.

[0036] In a preferred embodiment of the present invention, mannitol is used as an auxiliary material.

[0037] According to another embodiment, the method provides a step a) of mixing ambroxol and / or its hydrochloride with distilled water or distilled water < 20% ethanol.

[0038] The step b) of spray-drying the mixture prepared in step a) in order to obtain fine particles according to...

Embodiment 1

[0048] In this preparation method, a micronizer: DECMCOne model was used. Ambroxol hydrochloride drug was micronized by jet milling.

[0049] The jet mill uses "process gas" 7 bar 0.09Nm3 / min (3.18CFM), the ambient temperature in the white chamber is 20°C, and the temperature in the area dedicated to the micronization device is ≤12°C. Coarse particles are separated from fine particles by grinding and crushing under high pressure and centrifugal force generated by a turbine. Particles meeting the size requirements enter the cyclone separator where they are collected. It is preferred that at least 85% of the particles have a diameter of less than 5 μm, preferably between 3 and 5 μm. Regenerates and evenly distributes excipients and dispersants at a suction level of 50 to 100 μm for good sliding ability. During inhalation, the flow creates turbulence that disperses the particles to form micronized particles that can be inhaled to reach the bronchi. The weight percentage of ac...

Embodiment 2

[0052] In this preparation method, a mini spray dryer BUCHI B-290 was used. Spray dryer nozzle opening: 0.7mm, compressed gas flow: 5~8 bar, 200~800L / h, inlet temperature 115±2℃, liquid feeding speed: 1.8ml / min, atomizing air speed: 473 liters / hour, atomization pressure: 2 bar, air flow: 0.55m 3 / min, drying time ≤ 1.5 seconds. Dissolving ambroxol and / or its hydrochloride in distilled water with or without 20% ethanol, the spray drying method is used with the solution obtained by adjusting the nebulization air speed to control the size of nebulized small droplet particles To prepare particles of micronized powder with good shape. It is preferred that at least 85% of the particles have a diameter of less than 5 μm, preferably 3 to 5 μm, and 40% of the excipient particles mixed uniformly have a diameter of 15 to 100 μm for good sliding ability. During inhalation, the flow creates turbulence that disperses the particles to form micronized particles that can be inhaled to rea...

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
Login to View More

PUM

PropertyMeasurementUnit
diameteraaaaaaaaaa
diameteraaaaaaaaaa
diameteraaaaaaaaaa
Login to View More

Abstract

The present invention relates to a preparation for inhalation use in form of dry powder comprising particles of ambroxol and / or hydrochlorides thereof, and at least a pharmaceutically acceptable excipient and / or dispersant wherein at least 85% of said particles has a geometrical diameter from 3 to 5 [mu]m. The present invention further relates to the methods for preparing such composition and usesthereof. The present invention thanks to the very fine particles of dry powder, as above defined, constitutes a composition for inhalation use with optimum performances which, combined with inhaler action, reaches and acts directly on the bronchi or on the damaged respiratory tract. The local action and the quick absorption of the drug guarantee good features of bioavailability. The decrease in dosing Ambroxol with respect to the other existing oral or injectable formulations allows to reach quickly, locally and safely, the therapeutic target.

Description

technical field [0001] The present invention relates to the preparation that is used for inhalation in dry powder form, and this preparation comprises ambroxol and / or its hydrochloride granule and optional suitable pharmaceutically acceptable adjuvant as single active ingredient, wherein the granule The geometric diameter is equal to or less than 5 μm, wherein at least 85% of the ambroxol and / or its hydrochloride particles in the composition have a geometric diameter of 3 to 5 μm. The invention also relates to processes for the preparation of such compositions and their use. The present invention has the best properties due to the very fine dry powder particles (size equal to or less than 5 μm) for the composition for inhalation use, the composition is combined with the action of the inhaler, directly reaches the bronchi or damaged airways and in the bronchi or Damaged airways act directly. The local action and rapid absorption of the drug guarantee a good bioavailability pr...

Claims

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
Login to View More

Application Information

Patent Timeline
no application Login to View More
Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/72A61K9/14A61K31/137A61K47/26A61K47/18A61P11/10A61J1/00A61M15/00
CPCA61J1/00A61K9/0073A61K9/145A61K31/137A61M15/0028A61P11/10A61K9/0075A61K9/1617A61K9/1623A61K9/19A61K31/7036A61M16/14A61M2202/064A61M15/0005A61M15/0031
Inventor 吴颀吴华欣
Owner HOLLYCON ITAL PTE LTD