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Zanamivir nasal in situ jellies with phase variation property and preparing method thereof

A zanamivir and phase transition technology, which is applied in non-active ingredients medical preparations, antiviral agents, pharmaceutical formulations, etc., can solve the problem of excessive drug clearance, poor oral absorption, and oral bioavailability of only 2%, etc. question

Inactive Publication Date: 2010-06-09
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 medicine that reaches the effective site after administration is less
(2) Potential danger
Therefore, some environmentally sensitive materials have attracted people's attention. The in-situ gel prepared by using environmentally sensitive materials has the advantages of prolonging the drug retention time of the gel, and avoids the inaccurate dosage and inconvenient use. And there is no report about zanamivir in situ gel

Method used

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  • Zanamivir nasal in situ jellies with phase variation property and preparing method thereof
  • Zanamivir nasal in situ jellies with phase variation property and preparing method thereof
  • Zanamivir nasal in situ jellies with phase variation property and preparing method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0022] Prepare ion-sensitive zanamivir nasal in situ gel, the prescription is as follows (see Table 1):

[0023] Table 1 ion-sensitive zanamivir nasal in situ gel prescription (wt%)

[0024]

[0025] Preparation Process:

[0026] The above ion-sensitive polymer was placed in an appropriate amount of deionized water, magnetically stirred in a water bath at 80-100°C to disperse and dissolve, and left to stand in a refrigerator at 4°C (12h) to obtain a clear solution. Dissolve the drug zanamivir and other water-soluble excipients in deionized water, mix the two solutions, adjust the pH to 6.2, and add water to the full amount.

[0027] The rheological properties of the above four formulations were measured at room temperature (20° C.) using a Brookfield DV-III rotational viscometer. The viscosity of the above prescriptions shows a downward trend in varying degrees with the increase of the shear rate, and they belong to pseudoplastic fluids. Prescriptions 1 and 4 have a viscosi...

Embodiment 2

[0032] Prepare temperature-sensitive zanamivir nasal in situ gel, the prescription is as follows (see Table 2):

[0033] Table 2 temperature-sensitive zanamivir nasal in situ gel prescription (wt%)

[0034]

[0035] Preparation Process:

[0036] The above temperature-sensitive polymer was added to a low-temperature phosphate buffer (pH6.5), dispersed and dissolved under magnetic stirring, and left to stand in a refrigerator at 4°C (12h) to obtain a clear solution. Stir the gel property regulator (PEG, PEO, HPMC) at room temperature to dissolve it, and stand still for 12 hours to obtain a clear solution. Dissolve the drug zanamivir and other water-soluble excipients in deionized water, mix the three solutions, adjust the pH to 6.5, and add water to the full amount.

[0037] The rheological properties of the above four formulations at different shear rates were measured at room temperature (20°C) using a Brookfield DV-III rotational viscometer. The viscosity of the above f...

Embodiment 3

[0040] Prepare pH sensitive zanamivir nasal in situ gel, the prescription is as follows (see Table 3):

[0041] Table 3 pH-sensitive zanamivir nasal in situ gel prescription (wt%)

[0042]

[0043]

[0044] Preparation:

[0045] Dissolve the pH-sensitive gel material in distilled water, in which CAP was stirred and dissolved in HCL solution with pH 3.0, and left in a refrigerator at 4°C for 12 hours to obtain a clear solution; Carbopol 934 was dispersed in a certain amount of water, fully Swell to make it a blank matrix; chitosan was dissolved in 0.33M citric acid solution, and stood in a refrigerator at 4°C (12h) to obtain a clear solution. Dissolve the drug zanamivir and other water-soluble excipients in a certain amount of distilled water, mix with the solution prepared by the gel regulator (HPMC, GMO), drop into the pH-sensitive gel solution, adjust the pH to 4.0, and supplement the remaining Measure water to full volume.

[0046] The rheological properties of the...

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Abstract

The invention relates to the new dosage form of zanamivir, which is a nasal in-situ gel with phase transformation property and preparation methods, the invention is made of the original drug of zanamivir, hydrophilic gel materials which are sensitive to environments and assistant materials which can be accepted in pharmacy, after being absorbed by nasal mucosa, the invention can have systemic functions and improve the partial concentration of drugs in respiratory tracts, when room temperature is about 20 DEG C and the invention is in storing state, the invention is in the state of liquid, while after being put into the physiological conditions of nasal cavities, the invention can be quickly formed into gel on the surface of nasal mucosa, so that the detained time of drugs can be prolonged,biological availability can be improved and the compliance of patients can be perfected, and the viscosity of the invention is proper, after being formed into gel, the invention can be detained on the surface of the nasal cavity for a rather long time, which has no nasal ciliary toxicity.

Description

technical field [0001] The invention relates to a new dosage form of zanamivir—nasal in-situ gel with phase transition properties, and a preparation method thereof. Nasal in situ gel of the present invention is made from the prototype drug of zanamivir, environmentally sensitive hydrophilic gel material and other pharmaceutically acceptable adjuvants, and is free at room temperature (20°C) and under storage conditions. In a flowing liquid state, a gel is rapidly formed on the surface of the nasal mucosa under the physiological conditions of the nasal cavity, thereby prolonging the residence time of the drug, increasing the bioavailability, and improving the patient's compliance. Background technique [0002] Zanamivir (zanamivir) was synthesized by von Itzstein of Australia Biota Science Management Co., Ltd. in 1991. It was approved by the U.S. Food and Drug Administration and the European Medicines Agency in 1999, and was marketed by Glaxo Wellcome Company under the trade n...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K31/351A61K9/00A61K9/12A61K47/32A61K47/34A61K47/36A61K47/38A61P31/16A61K47/10
Inventor 甘勇甘莉栾琳张馨欣朱春柳
Owner SHANGHAI INST OF MATERIA MEDICA CHINESE ACAD OF SCI
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