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Medicine-containing slow-release granules for nasal mucosa and application of medicine-containing slow-release granules

A technology of sustained-release microparticles and nasal mucosa, applied in pharmaceutical formulations, microcapsules, drug delivery, etc., can solve problems such as drug delivery, inability to stably act on lesions for a long time, and achieve stable release effects.

Inactive Publication Date: 2019-08-20
PUYI (SHANGHAI) BIOTECHNOLOGY CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0009] In order to solve the problem that the above-mentioned existing treatment methods cannot act on the lesion for a long-term and stable administration, the present invention aims to provide a drug-containing sustained-release microparticle for nasal mucosa and its application.

Method used

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  • Medicine-containing slow-release granules for nasal mucosa and application of medicine-containing slow-release granules
  • Medicine-containing slow-release granules for nasal mucosa and application of medicine-containing slow-release granules
  • Medicine-containing slow-release granules for nasal mucosa and application of medicine-containing slow-release granules

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0063] Use polylactic acid glycolic acid copolymer PLGA (75 / 25, molecular weight 18000) and mometasone furoate according to the weight ratio of 2:1, respectively dissolve in acetone, prepare 500ml solution, PLGA, mometasone furoate share the solution 15 wt%. Use the spray drying method to make particles, the normal particle size distribution is D(10)=4μm, D(50)=18μm, D(90)=40μm, see the particle size distribution diagram for details figure 1 .

[0064] Take 1.5 mg of microparticles, use a drug dissolution tester to dissolve the sample in a PBS solution at 37°C, and use HPLC to test the amount of dissolved drug, such as Figure 2A As shown, within 30 days, the maximum amount of drug dissolution in the first 3 days was 22.5 μg / d, and then gradually stabilized and slowed down, and the degradation was basically completed in 30 days, with an average release rate of 12 μg / d.

Embodiment 2

[0066] Poly(lactic-co-glycolic acid) copolymer PLGA (molecular weight 6000) and mometasone furoate were dissolved in acetone at a weight ratio of 2:1 to prepare a 500ml solution. PLGA and mometasone furoate accounted for 15wt% of the solution. Microparticles were produced by spray drying, and the particle diameters were D(10)=4 μm, D(50)=18 μm, and D(90)=40 μm.

[0067] Take 1.5 mg of microparticles, use a drug dissolution tester to dissolve the sample in a PBS solution at 37°C, and use HPLC to test the amount of dissolved drug, such as Figure 2B As shown, within 20 days, the maximum amount of drug dissolution in the first 3 days was 31 μg / d, and then gradually stabilized and slowed down, and the degradation was basically completed in 20 days, with an average release rate of 21 μg / d.

Embodiment 3

[0069] Use polylactic acid polyethylene glycol / polyethylene glycol polylactic acid copolymer PLA-PEG (PEG molecular weight 6000,

[0070] PLA:PEG is 30:1, Mw=48000) and mometasone furoate are respectively dissolved in acetone according to the weight ratio of 3:2, and are prepared into 500ml solution, PLA-PEG, mometasone furoate account for 15wt% of the solution altogether . Microparticles were produced by spray drying, and the particle diameters were D(10)=4 μm, D(50)=18 μm, and D(90)=40 μm.

[0071] Take 1.5 mg of microparticles, use a drug dissolution tester to dissolve the sample in a PBS solution at 37°C, and use HPLC to test the amount of dissolved drug, such as Figure 2C As shown, within 30 days, the maximum amount of drug dissolution in the first 3 days was 39 μg / d, and then gradually stabilized and slowed down, and the release was basically completed within 30 days, with an average release rate of 15 μg / d.

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Abstract

The invention relates to medicine-containing slow-release granules for nasal mucosa. The medicine-containing slow-release granules comprise medicines and a biodegradable polymer, wherein the medicinesare 0.1-40% by weight in the medicine-containing slow-release granules, the biodegradable polymer is 60-99.9% by weight of the medicine-containing slow-release granules, the granule size of the medicine-containing slow-release granules is 0.5-250[mu]m, and the granule size is in normal distribution. The invention further provides an application of the medicine-containing slow-release granules. The medicine-containing slow-release granules for nasal mucosa can be directly applied to meatus nasi diseased regions. Specially, the medicines and the biodegradable polymer are mixed to prepare the granules in different size, and the size of the granules and the distribution of the granule size are controlled, so that control of the release time of the medicines can be achieved.

Description

technical field [0001] The invention relates to drug-containing microparticles, more particularly to a drug-containing sustained-release microparticle for nasal mucosa and its application. Background technique [0002] The sinuses are multiple air-filled bony cavities around the nasal cavity, which communicate with the nasal cavity through small tubes. The epidermal mucosal cells in the nasal cavity and paranasal sinuses of normal people continuously secrete clear liquid, and then the cilia on the mucosal cells pulsate regularly, and these secretions flow from the nasal sinuses, through the nasal cavity, to the nasopharynx and throat Then swallowed into the esophagus and stomach. The average adult secretes about 1 liter of mucus every day. These mucus are used to maintain the humidity inside the nasal cavity and sinuses, and at the same time absorb dust and foreign objects in the air to protect the health of the respiratory tract. Once due to the invasion of viruses, bacte...

Claims

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Application Information

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IPC IPC(8): A61K9/52A61K45/00A61K47/34
CPCA61K9/0004A61K9/0019A61K9/0043A61K9/5031A61K45/00
Inventor 晏伟夏佩佩魏征
Owner PUYI (SHANGHAI) BIOTECHNOLOGY CO LTD
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