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

A technology of zanamivir and phase transition, which is applied in the direction of medical preparations containing non-active ingredients, medical preparations containing active ingredients, organic active ingredients, etc., which can solve the problems of low bioavailability, fast renal clearance, and drug clearance. Too fast and other problems

Inactive Publication Date: 2008-07-30
SHANGHAI INST OF MATERIA MEDICA CHINESE ACAD OF SCI
View PDF0 Cites 13 Cited by
  • 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

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
View more

Image

Smart Image Click on the blue labels to locate them in the text.
Viewing Examples
Smart Image
  • 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] Prescription 1

Prescription 2

Prescription 3

Prescription 4

Zanamivir

sodium alginate

deacetylated gellan gum

osmotic regulator

preservatives

pH regulator

Deionized water

1.2

6

Glycerin 1.8

Chlorobutanol 0.5

Adjust pH to 6.2 with HCL

margin

1.6

0.8

Sorbitol 4.5

Thimerosal 0.01

Adjust pH to 6.2 with HCL

margin

1.7

0.3

Glycerin 2

Chlorobutanol 0.5

Adjust pH to 6.2 with HCL

margin

1.1

1.5

Mannitol 5

Ethylparaben 0.02

Adjust pH to 6.2 with HCL

margin

[0025] Preparation Process:

[0026] The above ion-sensitive polymer was placed in an appropriate amount of deionized water, ...

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] Prescription 5

Prescription 6

Prescription 7

Prescription 8

Zanamivir

Poloxamer 407

Poloxamer 188

polyethylene glycol (molecule

Volume 6000~

11000)(PEG)

polyoxyethylene

(PEO)

Hypromellose

prime (HPMC)

osmotic regulator

preservatives

pH regulator

Deionized water

1.6

20

5

2

---

---

Sodium chloride 0.9

Benzalkonium Chloride 0.03

NaOH adjustment

pH to 6.5

margin

1.6

35

---

---

---

2

Sorbitol 4.5

Chlorobutanol

0.5

Triethanolamine

Regulate pH to 6.5

margin

1.6

---

28

...

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] Prescription 9

Prescription 10

Prescription 11

Zanamivir

Cellulose Acetate Phthalate (CAP)

Kabop 934

Chitosan

Hypromellose (HPMC)

Glyceryl Monooleate (GMO)

osmotic regulator

preservatives

1.6

30

---

---

0.5

---

Glycerin 1.5

Benzoic acid 0.02

1.6

---

0.8

---

1

---

Glycerin 2

Chlorobutanol 0.5

1.6

---

3

---

3

Mannitol 4.5

Thimerosal 0.01

[0043] pH regulator

Deionized water

Adjust pH to 4.0 with HCL

margin

Adjust pH to 4.0 with HCL

margin

Adjust pH to 4.0 with HCL

margin

[0044] Preparation:

[0045] Dissolve the pH-sensitive gel material...

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
Login to view more

PUM

No PUM Login to view more

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

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
Login to view more

Application Information

Patent Timeline
no application Login to view more
Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/00A61K9/12A61K31/351A61K47/32A61K47/34A61K47/36A61K47/38A61P31/16A61K47/10
Inventor 甘勇甘莉栾琳张馨欣朱春柳
Owner SHANGHAI INST OF MATERIA MEDICA CHINESE ACAD OF SCI
Who we serve
  • R&D Engineer
  • R&D Manager
  • IP Professional
Why Eureka
  • Industry Leading Data Capabilities
  • Powerful AI technology
  • Patent DNA Extraction
Social media
Try Eureka
PatSnap group products

Browse by: Latest US Patents, China's latest patents, Technical Efficacy Thesaurus, Application Domain, Technology Topic.

© 2024 PatSnap. All rights reserved.Legal|Privacy policy|Modern Slavery Act Transparency Statement|Sitemap