Preparation method of fluticasone propionate particles and applications of the particle

A technology of fluticasone propionate and microparticles, which is applied to inhalation aerosols and inhalation powder aerosols, to prepare fluticasone propionate microparticles with a particle size D98 below 5 μm, and to prepare nasal sprays, which can solve the problem of small batches of raw materials and environmental pollution High roundness, low energy consumption and low production cost

Active Publication Date: 2014-02-19
CHONGQING HUAPONT PHARMA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0006] However, mechanical pulverization means have great problems for the industrial production of medicines. One is to rely on expensive pulverization equipment, such as ball mills, high-pressure homogenizers, etc., and the cost is relatively high; The batc

Method used

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  • Preparation method of fluticasone propionate particles and applications of the particle
  • Preparation method of fluticasone propionate particles and applications of the particle

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0041] Embodiment 1 preparation of fluticasone propionate microparticles

[0042] method:

[0043] 1) Preparation of fluticasone propionate solution A: add 10 g of fluticasone propionate to 550 g of polyethylene glycol 400, heat and stir to dissolve completely, and obtain solution A;

[0044] 2) Preparation of anti-solvent B: Take 2.05g of Tween 80 and 1.91g of benzalkonium chloride, dissolve them in water, add water to 17050g, and obtain anti-solvent B;

[0045] 3) Mixing method of solution A and anti-solvent B: under stirring, add solution A into anti-solvent B, and keep stirring for 10 minutes to obtain a suspension.

[0046] result:

[0047] Detected with a laser particle size analyzer, the D98 of the fluticasone propionate particles in the suspension is 3.47 μm, see figure 1 .

Embodiment 2～6

[0049] According to the operation method of Example 1 and the types and amounts of each material in Table 1, fluticasone propionate microparticles were prepared.

[0050] The particle size of the obtained product fluticasone propionate microparticles is shown in Table 1.

[0051] Table 1 The types, dosage and particle size of each material used in the preparation of fluticasone propionate microparticles

[0052]

Embodiment 7

[0067] Get the suspension containing fluticasone propionate microparticles obtained in 880g embodiment 1, 0.5g Tween 80, 2.5g phenethyl alcohol, 5g glucose, 1.2g microcrystalline cellulose, 2.5g sodium carboxymethylcellulose, 0.2g BHT, add water to 1000g, stir, mix evenly, the liquid medicine that mixes is filled with brown glass bottle, and every bottle filling capacity is 16g, and spray pump head is installed, gets fluticasone propionate nasal spray.

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Abstract

The invention discloses a preparation method of fluticasone propionate particles having a D98 particle size smaller than 5 [mu]m. By utilization of a recrystallization method, a fluticasone propionate raw material is dissolved in a solvent to prepare a solution, and the solution is added into water containing a surfactant to precipitate the fluticasone propionate particles having the needed particle size. Compared with traditional methods, the preparation method provided by the invention has high yield, low production cost, no dependence on special equipment, and low energy consumption. The preparation method provided by the invention is free from duct generation. Reagents used in the preparation method are nontoxic, harmless and environmental friendly. Products have small particle sizes, narrow particle size distribution, high roundness and good fluidity, and are particularly suitable to be used as raw materials for medicinal preparations.

Description

technical field [0001] The invention belongs to the field of pharmacy, and in particular relates to a method for preparing fluticasone propionate particles with a particle size D98 below 5 μm, and the use of the fluticasone propionate particles in preparing nasal sprays, inhalation aerosols and inhalation powders. Background of the invention [0002] Fluticasone propionate is an adrenal hormone drug used to prevent and treat conditions such as rhinitis or asthma. [0003] Common dosage forms of fluticasone propionate are nasal spray, inhalation aerosol and inhalation powder. In these preparations, fluticasone propionate enters the human body through the respiratory tract. In order to make it reach the lesion and be effectively absorbed and utilized, there are stricter requirements on the particle size of fluticasone propionate. For example, the standard of fluticasone propionate nasal spray in the United States Pharmacopoeia is: the particle size of fluticasone propionate r...

Claims

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Application Information

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IPC IPC(8): C07J31/00A61K31/56A61K9/12A61K9/72A61P11/02A61P11/06
Inventor 兰洁陈李平张凌远管璐晗
Owner CHONGQING HUAPONT PHARMA
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