Preparation process of compound dry powder inhaler for glucocorticoids and beta2 receptor agonists

A technology for glucocorticoid and dry powder inhaler, which is applied to the preparation of glucocorticoid and β2 receptor agonist compound dry powder inhaler composition, and the preparation field of indacaterol and mometasone compound dry powder inhaler composition. Solve the problems of reducing FPF value and preparation stability, the fluidity of preparation composition, and preparation stability, etc., to achieve the effect of improving the stability of FPF and preparation, convenient operation, and lower production cost

Active Publication Date: 2018-11-09
SHANGHAI FANGYU HEALTH PHARMA TECH CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

The electrostatic force, van der Waals force, capillary force, etc. generated by the specific active ingredients of the drug and the composition of the excipients will affect the force of the dispersed state of the drug; these forces will have an impact on the use of the preparation, such as reducing the FPF value and the stability of the preparation Sex, when the patient uses it, the active ingredients of the drug will be deposited in the mouth and throat in large quantities, causing local side effects, etc.
[0007] The study found that the particle size of the active substance, the chemical properties and the particle size of the carrier will cause the difference in the fluidity of the preparation composition, as well as the difference in the FPF value of the preparation and the stability of the preparation.

Method used

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  • Preparation process of compound dry powder inhaler for glucocorticoids and beta2 receptor agonists
  • Preparation process of compound dry powder inhaler for glucocorticoids and beta2 receptor agonists
  • Preparation process of compound dry powder inhaler for glucocorticoids and beta2 receptor agonists

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0040] Get the indacaterol maleate and mometasone furoate of 10g respectively, carry out jet milling, feeding nozzle pressure 1.1MPa, pulverizing nozzle pressure is 1.1MPa, obtains the indacaterol maleate of micronization (D10= 0.35 μm, D50=1.2 μm, D90=2.0 μm), mometasone furoate (D10=0.23 μm, D50=1.1 μm, D90=1.9 μm).

[0041] Ingredients: indacaterol maleate 0.8g (micronized), mometasone furoate 0.6g (micronized), lactose 90g and mannitol 10g (the particle size after mixing lactose and mannitol is D10=1.2μm, D50 = 35 μm, D90 = 150 μm).

[0042] Process 1:

[0043] Mix indacaterol maleate, mometasone furoate, lactose and mannitol, put the mixed sample in a wet granulator, the vertical rotation speed is 10r / s, finish mixing after 10min, let it stand for 1 hour, and the obtained sample Place in a sample processor with 75% humidity for 2 hours. The dry powder is filled into size 3 capsules in 25 mg aliquots.

[0044] Process 2:

[0045] Mix indacaterol maleate, mometasone furo...

Embodiment 2

[0058] Get 10g of indacaterol acetate and mometasone furoate, carry out airflow pulverization respectively, adjust feed nozzle pressure 0.5MPa, pulverize nozzle pressure and be 0.5MPa, obtain micronized indacaterol acetate (D10=0.70 μ m, D50=2.50 μm, D90=3.20 μm), mometasone furoate (D10=0.84 μm, D50=2.30 μm, D90=3.80 μm).

[0059] Ingredients: indacaterol acetate 0.6g (micronized), mometasone furoate 0.3g (micronized), lactose monohydrate 16g, lactose 63.9g.

[0060] Process 1:

[0061] Mix indacaterol acetate, mometasone furoate, lactose monohydrate and lactose (the particle size after mixing lactose monohydrate and lactose is D10=0.8 μm, D50=20 μm, D90=101 μm), and the mixed sample is In the high-speed shearing machine, the vertical rotation speed is 18r / s, the mixing is completed after 10min, and the sample is left to stand for 1 hour, and the obtained sample is put into a sample processor with a pressure of 500Pa for 24 hours. The dry powder is filled into size 3 capsul...

Embodiment 3

[0072] Process 1:

[0073] Take 10g of indacaterol maleate and mometasone furoate monohydrate respectively, carry out airflow pulverization respectively, adjust the feeding nozzle pressure to 0.5MPa, and crush the nozzle pressure to 0.4MPa to obtain micronized indacaterol maleate Terol (D10=1.1 μm, D50=3.8 μm, D90=5.5 μm) and mometasone furoate monohydrate (D10=0.58 μm, D50=1.5 μm, D90=3.2 μm).

[0074] Indacaterol maleate (0.6g), mometasone furoate monohydrate (1.0g) and lactose monohydrate (80g, D10=2.2μm, D50=53μm, D90=98μm) were mixed, and the mixed sample In the mixer, the vertical rotation speed is 4r / s, and the mixing is completed after 16min, and left to stand for 1 hour, and the obtained sample is put into a sample processor with a humidity of 58% for 72 hours. The dry powder is filled into size 3 gelatin capsules in 25 mg aliquots.

[0075] Process 2:

[0076] Take 10 g of indacaterol maleate and mometasone furoate monohydrate respectively, and carry out jet milli...

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Abstract

The invention relates to a preparation process of a compound dry powder inhaler for glucocorticoids and beta2 receptor agonists. The process comprises the following steps: (a) performing micronizationon glucocorticoids and beta2 receptor agonists; (b) mixing the micronized product in the step (a) with a drug carrier, or mixing the micronized product in the step (a) with a drug carrier and an additive; and (c) adding the composition in the step (b) into a sample handling room for handling, thereby obtaining the pharmaceutical composition of the dry powder inhaler. The sample handling room is an environment of which the humidity is 45-75% or an environment of which the pressure is not higher than 500Pa; the handling time is 2-72 hours; the glucocorticoids are mometasone furoate or pharmaceutically acceptable salts thereof; and the beta2 receptor agonists are indacaterol or pharmaceutically acceptable salts thereof. The process disclosed by the invention is simple, convenient to operateand low in production cost.

Description

field of invention [0001] The invention belongs to the technical field of pharmaceutical preparations, in particular to a glucocorticoid and beta 2 A preparation process of a receptor agonist compound dry powder inhaler composition, in particular relates to a preparation process of a compound dry powder inhaler composition of indacaterol and mometasone. technical background [0002] In recent years, due to the aggravation of air pollution, the incidence of asthma and chronic obstructive pulmonary disease (COPD) has gradually increased. Since the drugs currently used for anti-asthma and COPD can only control the occurrence of symptoms, but cannot completely cure them, the number of patients with asthma and COPD is increasing significantly every year. [0003] Inhaled corticosteroids (ICS) and long-acting beta 2 The combination of receptor agonist (LABA) is one of the main compound forms in the treatment of asthma and COPD. The combined application of LABA and ICS can not o...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K45/00A61K9/72A61K31/58A61K31/4704A61P11/06
CPCA61K45/00A61P11/06A61K9/0075A61K31/4704A61K31/58A61K2300/00
Inventor 金方文斌斌梅丽闻聪
Owner SHANGHAI FANGYU HEALTH PHARMA TECH CO LTD
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