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Salmeteroxinamic acid ester particles for inhalation and preparation method of salmeteroxinamic acid ester particles

A technology of xinaate and microparticles, which is applied in the field of salmeterol xinaate microparticles for inhalation and its preparation, which can solve the problems of undisclosed active ingredients such as the method of sub-salmeterol micronization, and achieve fine particle size , Avoid powder clogging, high product yield effect

Pending Publication Date: 2021-06-11
SHENZHEN HAIBIN PHARMA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0005] CN105412049A discloses a preparation method of a dry powder inhaler pharmaceutical composition. In this method, the coating powder and the pharmaceutical active ingredient are individually micronized and then mixed to obtain a dry powder inhaler pharmaceutical composition. Tero specific micronization method

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0024] Embodiment 1, the micronization of salmeterol

[0025] 1.0 g of salmeterol was pulverized using an experimental McONE jet mill provided by Dec, Switzerland. The pulverization pressure was 1.2 MPa, and the feeding speed was 0.2 g / min. The D90 of the obtained product was 20.28 μm.

[0026] The particle size measurement of salmeterol adopts the following method. The salmeterol in Example 1 is fully dispersed in a small amount of water, and the particle size is measured by marlven-Mastersizer 2000 as follows. The detailed results are shown in Table 1.

[0027] Table 1

[0028] D10 D50 D90 Salmeterol 1.186 5.378 20.280

Embodiment 2

[0029] Embodiment 2, the micronization of salmeterol co-crushing agent

[0030] 1.0g of salmeterol and 19.0g of α-lactose hydrate were mixed by a three-dimensional mixer, and pulverized using a jet mill with a pulverization pressure of 0.6Mpa and a feed rate of 0.5g / min. The particle size of the obtained product was D90 is 6.956 μm.

[0031] Use the SYMPATEC laser particle size analyzer to measure the particle size of the lactose used. The operation is as follows: operate and install the instrument HELOS (H2969) and RODOS, adjust the flow rate to 4.0bar, open the software, measure the background value, load the sample, and start the measurement. The results are shown in Table 2.

[0032] Table 2

[0033] D10 D50 D90 α-lactose monohydrate 11.43 74.19 148.28

[0034] The particle size measurement of salmeterol and co-pulverizing agent micronized products adopts the following method: dissolve the above-mentioned co-micronized sample in a small amount of...

Embodiment 3

[0040] Embodiment 3, salmeterol and co-crushing agent micronized product prepare dry powder inhalation product

[0041] According to the above-mentioned measurement results, each component was weighed, and the co-micronized product of salmeterol and lactose was obtained according to the method of Example 2, transferred to a high-speed mixer and mixed for 5 minutes, and finally mixed for 10 minutes in a three-dimensional mixer, according to each A unit dose of 25 mg (containing 250 micrograms of flutica propionate) is dispensed and administered through an applicator.

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Abstract

The invention belongs to the technical field of pharmaceutical preparations, and particularly relates to a salmeteroxinamic acid ester microparticle for inhalation and a preparation method thereof, and the salmeteroxinamic acid ester microparticle for inhalation comprises the following components: salmeteroxinamic acid ester and a co-crushing agent in a mass ratio of 1: (10-70). The preparation method comprises the following steps: firstly, according to the mass ratio, mixing salmeteroxamic acid ester with the co-crushing agent for 0.5-1 hour; smashing the mixture obtained in the step 1) in a self-airflow smashing mode, wherein the smashing pressure is 0.6 Mpa, the feeding speed is 0.5 g / min, and obtaining the salmeteroxinamic acid ester particles for inhalation. Compared with independent crushing, the method provided by the invention has the advantages of higher feeding speed and higher product yield, powder blockage in the crushing cavity and the airflow channel is avoided, and the obtained product has smaller particle size.

Description

technical field [0001] The invention belongs to the technical field of pharmaceutical preparations, and in particular relates to salmeterol xinacate microparticles for inhalation and a preparation method thereof. Background technique [0002] Dry powder inhalation preparation (DPI) is a very valuable route of administration, which has the advantages of low dosage, less systemic side effects, fast onset, good therapeutic effect and patient compliance. [0003] Salmeterol is a long-acting selective β2-adrenoceptor agonist with obvious bronchodilation effect. Salmeterol products include: salmeterol inhalation aerosol, salmeterol powder inhalation, salmeterol plate, for the long-term treatment of reversible airway obstruction and chronic bronchitis of asthma. [0004] At present, respiratory drug delivery usually has strict requirements on the particle size of the drug, such as pulmonary drug delivery, which usually requires the particle size of the drug to be less than or equa...

Claims

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Application Information

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IPC IPC(8): A61K9/72A61K9/14A61K47/26A61K31/137A61K31/56A61K31/58A61K31/573A61P11/06A61P11/00
CPCA61K9/145A61K31/137A61K31/56A61K31/573A61K31/58A61P11/00A61P11/06A61K2300/00
Inventor 卢兆强罗劲松闻聪欧阳陵
Owner SHENZHEN HAIBIN PHARMA
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