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Zanamivir nasal nanometer suspension and preparation method thereof

A nano-suspension, zanamivir technology, applied in non-active ingredients medical preparations, antiviral agents, pharmaceutical formulations, etc., can solve the problem of oral bioavailability of only 2%, fast renal clearance, and bioavailability. It can improve the bioavailability of the drug, prolong the residence time, and make the preparation process simple.

Active Publication Date: 2013-06-19
SHANGHAI INST OF MATERIA MEDICA CHINESE ACAD OF SCI
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

The main problems of zanamivir are its poor oral absorption, fast renal clearance, low tissue permeability, and oral bioavailability is only 2%. few
[0003] At present, inhalants are used abroad for drug administration, produced by GlaxoSmithKline, which effectively solves the problem of rapid drug clearance and low bioavailability, and the bioavailability can reach 10% to 20%. However, dry powder inhalers also exist. There are some disadvantages: (1) the drug that reaches the effective site after administration is less
Dosage form factors: the dosage of nasal drops is inaccurate, and it is unevenly distributed in the nasal cavity, directly reaches the rear part of the effective absorption site, and is quickly cleared from the nasopharyngeal tube; the dosage of spray is accurate, and the distribution in the nasal cavity is even, but still There is a disadvantage of quick removal
Although the gel can prolong the residence time of the drug in the nasal mucosa, its viscosity is relatively high, the dosage is not accurate, it is inconvenient to use, and it is difficult to reach the turbinate after administration, and it mostly stays in the external nasal cavity

Method used

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  • Zanamivir nasal nanometer suspension and preparation method thereof
  • Zanamivir nasal nanometer suspension and preparation method thereof
  • Zanamivir nasal nanometer suspension and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0051] prescription:

[0052] Zanamivir 10%

[0053] Poloxamer 188 5%

[0054] Polyvinylpyrrolidone K-12 5%

[0055] Glycerin 2.6%

[0056] Appropriate amount of acetic acid, adjust the pH value to 4.0

[0057] An appropriate amount of trishydroxymethylaminomethane (30%), adjust the pH value to 6.0

[0058] water balance

[0059] Preparation:

[0060] The zanamivir bulk drug was jet milled (particle size 2 μm). Prepare an aqueous acetic acid solution with a pH value of 4.0, adjust the pH value to 6.0 with 30% aqueous trishydroxymethylaminomethane solution, add the remaining auxiliary materials in the prescription under magnetic stirring, dissolve, and finally make the zanamivir bulk drug under magnetic stirring The powder is added to the above solution to fully dissolve and disperse to prepare a Zanamivir coarse suspension.

[0061] Transfer the Zanamivir coarse suspension to a high-pressure homogenizer, homogenize at a low pressure of 350 bar for 2 weeks, raise the pr...

Embodiment 2

[0064] prescription:

[0065] Zanamivir 20%

[0066] Cremophor EL 12%

[0067] Hypromellose E5 10%

[0068] Propylene Glycol 2.6%

[0069] Chlorobutanol 0.5%

[0070] Appropriate amount of acetic acid, adjust the pH value to 4.0

[0071] Appropriate amount of 1M sodium hydroxide, adjust the pH value to 6.0

[0072] water balance

[0073] Preparation:

[0074] Zanamivir crude drug was pulverized with a ball mill (particle size: 10 μm). Prepare an aqueous acetic acid solution with a pH value of 4.0, add the prescribed amount of chlorobutanol, adjust the pH value to 6.0 with 1M sodium hydroxide aqueous solution after dissolving, add the remaining auxiliary materials in the prescription under stirring, dissolve, and finally dissolve under magnetic stirring Zanamivir crude drug powder is added to the above solution to fully dissolve and disperse to prepare a Zanamivir coarse suspension.

[0075] Transfer the Zanamivir coarse suspension to a high-pressure homogenizer, homog...

Embodiment 3

[0078] prescription:

[0079] Zanamivir 30%

[0080] Sodium Lauryl Sulfate 20%

[0081] Polyvinylpyrrolidone K30 10%

[0082] Mannitol 2.0%

[0083] Chlorobutanol 0.6%

[0084] Proper amount of hydrochloric acid, adjust the pH value to 4.0

[0085] An appropriate amount of Tris (30%), adjust the pH value to 6.0

[0086] water balance

[0087] Preparation:

[0088] Zanamivir crude drug was pulverized by mechanical grinding method (particle size 14 μm). Prepare an aqueous solution of hydrochloric acid with a pH value of 4.0, add the prescribed amount of chlorobutanol, adjust the pH value to 6.0 with 30% aqueous solution of trishydroxymethylaminomethane after dissolving, add the remaining auxiliary materials in the prescription under magnetic stirring, and dissolve , and finally, under magnetic stirring, the zanamivir bulk drug powder is added to the above solution to fully dissolve and disperse to obtain a zanamivir coarse suspension.

[0089] Transfer the Zanamivir coa...

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Abstract

The invention relates to a zanamivir nasal nanometer suspension and a preparation method thereof. A preparation recipe of the invention comprises the following ingredients in percentage by weight: 5 to 50 percent of effective treatment amount of zanamivir, 1 to 40 percent of surface active agents, 1 to 40 percent of suspending aid, 0 to 20 percent of other pharmaceutically acceptable additives and the balance water. The invention adopts a high-pressure homogenizing method for preparing the zanamivir nasal nanometer suspension. The zanamivir nasal nanometer suspension of the invention has the characteristics of small medication volume, long mucous membrane detention time, good exertion of local and whole body effect and the like.

Description

technical field [0001] The invention relates to the field of pharmaceutical preparations, in particular to a zanamivir nanosuspension for nasal administration and a preparation method thereof. Background technique [0002] Zanamivir (zanamivir), synthesized by Australia Biota Science Management Company in 1991 [1] , was approved by the US Food and Drug Administration and the European Medicines Agency in 1999, and was marketed by GlaxoWellcome under the trade name Relen-za, which is used for the prevention and treatment of Type A and Type B influenza. The chemical name of zanamivir is 4-guanidino-2-deoxy-2,3-didehydro-N-acetylneuraminic acid, and the molecular formula is C 12 h 20 N 4 o 7 , molecular weight 333.2, white to off-white powder. Zanamivir is a water-soluble polar small molecule that can specifically inhibit viral neuraminidase, and its plasma protein binding rate is less than 10%. Completely excreted within 24 hours after a single administration, the total c...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K9/10A61K31/351A61K47/32A61K47/36A61K47/38A61P31/16
Inventor 甘勇张馨欣甘莉朱春柳
Owner SHANGHAI INST OF MATERIA MEDICA CHINESE ACAD OF SCI
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