Zanamivir capsule type inhalation aerosol powder and preparation method thereof

A technology for inhaling powder aerosols and Mivir capsules, which is applied in the directions of antiviral agents, pharmaceutical formulations, and medical preparations containing active ingredients, etc. The problems of poor hygroscopicity and high hygroscopicity can achieve the effect of simple and easy preparation process, low hygroscopicity and good particle fluidity.

Active Publication Date: 2012-05-30
SHANDONG NEWTIME PHARMA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, the zanamivir powder aerosol mentioned in this document has poor particle fluidity, high hygroscopicity, and low indicators such as content uniformity, emptying rate and effective part deposition.

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0047] The preparation of embodiment 1 zanamivir inhalation powder

[0048] Zanamivir Ultrafine Powder 100g

[0049] Grind Lactose 100g

[0050] Crystalline Lactose 300g

[0051] A total of 20,000 capsules are made

[0052] Pulverize the raw material of zanamivir, weigh the ultrafine powder of zanamivir in the prescription, mix it with the ground lactose in the prescription, and then mix it with the crystalline lactose in the prescription, measure the content, calculate the filling amount, and fill it with microcapsules. Machine filled in No. 3 capsules.

[0053] Example 1 Sample Test Results

[0054] 1. Particle size of dry powder: The particle size of zanamivir is 3.31 μm±0.11 μm.

[0055] 2. Angle of repose: 49°.

[0056] 3. Moisture: The relative weight gain is 2.1%.

[0057] 4. Content uniformity: ±3.0%.

[0058] 5. Evacuation rate: 99.8%.

[0059] 6. The amount of drug deposition in the effective site: 29%.

[0060] 7. Irritability to respiratory mucosa: no obv...

Embodiment 2

[0061] The preparation of embodiment 2 zanamivir inhalation powder aerosol

[0062] Zanamivir Ultrafine Powder 100g

[0063] Grind Lactose 200g

[0064] Crystalline lactose 200g

[0065] A total of 20,000 capsules are made

[0066] Pulverize the raw material of zanamivir, weigh the ultrafine powder of zanamivir in the prescription, mix it with the ground lactose in the prescription, and then mix it with the crystalline lactose in the prescription, measure the content, calculate the filling amount, and fill it with microcapsules. Machine filled in No. 3 capsules.

[0067] Example 2 Sample Test Results

[0068] 1. Particle size of dry powder: The particle size of zanamivir is 3.67μm±0.41μm.

[0069] 2. Angle of repose: 55°.

[0070] 3. Moisture: The relative weight gain is 4.8%.

[0071] 4. Content uniformity: ±3.1%.

[0072] 5. Evacuation rate: 99.1%.

[0073] 6. The amount of drug deposition in the effective site: 31%.

[0074] 7. Irritability to respiratory mucosa: ...

Embodiment 3

[0075] The preparation of embodiment 3 zanamivir inhalation powder aerosol

[0076] Zanamivir Ultrafine Powder 100g

[0077] Grind Lactose 40g

[0078] Crystalline Lactose 360g

[0079] A total of 20,000 capsules are made

[0080] Pulverize the raw material of zanamivir, weigh the ultrafine powder of zanamivir in the prescription, mix it with the ground lactose in the prescription, and then mix it with the crystalline lactose in the prescription, measure the content, calculate the filling amount, and fill it with microcapsules. Machine filled in No. 3 capsules.

[0081] Example 3 Sample Test Results

[0082] 1. Particle size of dry powder: The particle size of zanamivir is 3.97μm±0.44μm.

[0083] 2. Angle of repose: 48°.

[0084] 3. Moisture: The relative weight gain is 2.9%.

[0085] 4. Content uniformity: ±3.9%.

[0086] 5. Evacuation rate: 99.8%.

[0087] 6. The amount of drug deposition in the effective site: 20%.

[0088] 7. Irritability to respiratory mucosa: n...

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Abstract

The invention relates to a zanamivir capsule type inhalation aerosol powder and a preparation method thereof. The capsule type inhalation aerosol powder comprises a capsule shell and a capsule content, wherein the capsule content is composed of 5 parts by weight of zanamivir super micropowder, 10-18 parts by weight of inhalation crystallization lactose and 2-10 parts by weight of inhalation grinding lactose 40M, and average particle size of the zanamivir super micropowder is less than 5mu m and particle size of an excipient is within the range of 40-100mu m. The zanamivir capsule type inhalation aerosol powder provided by the invention has a simple preparation process, good mobility, low hygroscopicity, high content uniformity and high deposit rate on an effective part.

Description

technical field [0001] The invention relates to a medicine for preventing and treating influenza virus, in particular to a zanamivir capsule-type inhalation powder and a preparation method thereof. Background technique [0002] Zanamivir, chemical name is 5-acetamido-4-[(aminoiminomethyl)-amino]-2-[(1R,2R)-2,6-anhydro-3,4,5 - Trideoxy-D-glyceryl-D-galactose-2-enolic acid, an analog of neuraminidase (NA), based on the lipid membrane of the virus hemagglutinin and crystals of NA X-ray detection of the structure was synthesized, which is a slow-binding high-affinity competitive inhibitor of influenza virus NA. Zanamivir can effectively inhibit influenza A and B viruses, and has the same therapeutic effect on the viral epidemic of many neuraminidase-dependent pathogenic bacteria. [0003] Zanamivir has the advantages of high selectivity, low toxicity, strong activity, small dosage, wide range of action and good preventive effect. However, due to its instability in the gastroi...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/72A61K31/351A61P31/16
Inventor 赵志全张丽萍刘阿利
Owner SHANDONG NEWTIME PHARMA
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