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Azithromycin pharmaceutical composition, and preparation method and application of azithromycin pharmaceutical composition

A technology for azithromycin and composition, applied in the field of azithromycin composition and preparation thereof, can solve problems such as unfavorable drug quality control, complex granulation process parameters, uneven granules, etc., and achieves the consistency and reliability of curative effect, high blood drug concentration and the like. Good consistency and small clinical individual differences

Active Publication Date: 2020-07-31
BEIJING SIHUAN PHARMA +2
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

But this method has the following defects, one is that the dry granulation operation is complicated, the parameters of the granulation process are complicated, and the obtained particles are not uniform, which affects the quality uniformity of the preparation and is not conducive to the quality control of the drug; the other is that there is a lot of dust in the preparation process , cleaning is difficult; third, dry granulation destroys the appearance and particle size of azithromycin crystals, which adversely affects the dissolution and absorption of the drug
[0008] At present, no technical solution has been found that can directly mix azithromycin dihydrate without granulation treatment to meet clinical needs

Method used

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  • Azithromycin pharmaceutical composition, and preparation method and application of azithromycin pharmaceutical composition
  • Azithromycin pharmaceutical composition, and preparation method and application of azithromycin pharmaceutical composition
  • Azithromycin pharmaceutical composition, and preparation method and application of azithromycin pharmaceutical composition

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1-3

[0054] The preparation of the azithromycin compositions of different particle sizes of embodiment 1-3

[0055] The particle diameter of the azithromycin bulk drug of Examples 1-3 is shown in Table 2.

[0056] The particle size determination method comprises the following steps: with reference to the particle size distribution determination method ("Chinese Pharmacopoeia" 2015 edition four general rules 0982 third method dry method measurement) (Malvern Mastersizer 3000 or a laser particle size analyzer with comparable performance), an appropriate amount of this product is taken, Make the shading rate of the detector between 0.5%-15%, the gas source pressure is 0.5bar, the sampling speed is 50%, the Venturi tube type is standard, the hopper gap is 1.0mm, check according to the law, and take 3 consecutive measurements average value.

[0057] Table 2

[0058] parameter Comparative example 1 Example 1 Example 2 Implementation 3 Dv(10) / μm 75.3 75.3 57.1 ...

Embodiment 4

[0060] The influence of embodiment 4 different preparation processes on the particle size of azithromycin

[0061] Detection method: After the azithromycin composition of comparative example 1 and embodiment 1 is dispersed in water with its insoluble medium, it is placed under a polarizing microscope (59XF, Shanghai Optical Instrument Factory) for detection, and the transmitted light is 50 times, and the azithromycin is observed in different samples. particle size.

[0062] The measurement results are shown in Table 3 and figure 1 and figure 2 .

[0063] table 3

[0064] Particle size (μm) ① ② ③ ④ ⑤ ⑥ Comparative example 1 69.4 62.9 66.9 76.4 66.3 59.3 Example 1 382.6 244.5 471.0 639.2 355.2 405.4

[0065] It can be seen from the polarizing microscope pictures that after the azithromycin API is dispersed in water in an insoluble medium, it can be seen that the particle size of the API is between 350 μm and 600 μm. After dry granul...

Embodiment 5

[0066] Example 5 Azithromycin Particle Size Effects on Blood Drug Concentration

[0067] 12 cases / group of healthy adult subjects were selected, half male and half male, and a randomized, open-label, single-dose experiment was adopted to monitor for 72 hours (T=72 hours). Table 4 shows the pharmacokinetic parameters of azithromycin in plasma after the subjects took the test preparations of azithromycin capsules of Comparative Example 1 and Examples 1-3 once orally.

[0068] Table 4

[0069] parameter (unit) Comparative example 1 Example 1 Example 2 Implementation 3 Dv(90) / μm 553 553 310 359 C max (ng / mL)

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Abstract

The present invention provides an azithromycin pharmaceutical composition. In the composition, azithromycin has a particle size of 40-400 [mu]m and a D90 particle size of 200-400 [mu]m. The composition solves a problem of large individual differences in human body blood concentration of the azithromycin, and a preparation method has advantages of simple operation, suitability for large-scale industrial production, etc.

Description

technical field [0001] The invention belongs to the field of medicine, and in particular relates to an azithromycin composition, a preparation method thereof and an application thereof. Background technique [0002] Azithromycin (Azithromycin, also known as azithromycin, azithromycin) is a macrolide antibiotic approved by the FDA in 1991. [0003] [0004] Azithromycin is a bitter insoluble drug, which is usually prepared into coated tablets or capsules. Azithromycin dissolves slowly in the gastrointestinal tract after oral administration, which makes it difficult or limited for the drug to be absorbed by the body. [0005] The raw material for preparing the azithromycin preparation is its dihydrate, and the crystal form of the hydrate is stable and non-hygroscopic. However, there are defects such as uneven crystal particle size distribution, product agglomeration, and poor fluidity, which in turn affect the quality uniformity and preparation of pharmaceutical preparati...

Claims

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Application Information

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IPC IPC(8): A61K31/7052A61K45/00A61P31/04A61P11/00A61P11/02A61P11/04A61P27/02A61P15/00
CPCA61K31/7052A61K45/00A61P11/00A61P11/02A61P11/04A61P15/00A61P27/02A61P31/04A61K2300/00
Inventor 贾卫哺李巧霞赵小龙
Owner BEIJING SIHUAN PHARMA
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