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In situ gel-forming pharmaceutical compositions and uses thereof for sinus diseases

A composition and drug technology, applied in the direction of drug combination, medical preparations with non-active ingredients, medical preparations containing active ingredients, etc., can solve problems such as undeveloped drugs

Active Publication Date: 2020-03-06
艾威药业公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0008] While multiple drugs have shown promise in anti-biofilm research, no drugs have been developed that combine the antibacterial, antifungal, and anti-inflammatory properties that may be necessary to eradicate pathogens and treat the concurrent inflammatory response of most chronic sinus infections

Method used

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  • In situ gel-forming pharmaceutical compositions and uses thereof for sinus diseases
  • In situ gel-forming pharmaceutical compositions and uses thereof for sinus diseases
  • In situ gel-forming pharmaceutical compositions and uses thereof for sinus diseases

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0069] Example 1. Screening of PVP-I suitable concentration in the prescription

[0070] The composition contains 0.064% (w / w) budesonide and 0.25% (w / w) sodium chloride. Gellan gum concentrations were 0.1%, 0.3%, 0.5% (w / w), and PVP-I concentrations were 0.2%, 0.5%, 0.8%, 1.0% (w / w). Mix different concentrations of gellan gum and PVP-I separately, and study the basic properties of their composition.

[0071] Table 1 prescription dosage

[0072]

[0073] The viscosity of the samples before and after mixing simulated nasal fluid (SNF) was tested under conditions of high shear rate (100 / s) at 25°C and low shear rate (0.1 / s) at 34°C. To simulate the viscosity change of the sample before and after spraying into the nasal cavity, and to simulate the contact of the drug with the simulated nasal fluid, so as to compare the spray ability of the sample and the gel-forming ability when mixed with the nasal cavity simulated fluid. The difference between the sample viscosity at low ...

Embodiment 2

[0084] The prescription screening of embodiment 2.DGG and NaCl dosage

[0085] The weighed micronized budesonide and glycerin were thoroughly mixed, and when no gellan gum was added, 2% of the PVP-I solution and pure water were added to the total weight of the sample. Under stirring conditions, an addition of 1% gellan gum solution was added to the total weight of the sample. Adjust the pH to 4-5.5 with tromethamine and hydrochloric acid. Each group of mother liquors was prepared according to the ingredients shown in Table 5 (without NaCl). 50 μL of sodium chloride solutions of different concentrations were added to 2 mL of the mother liquor, so that the final concentration of sodium chloride was in the range of 0%-0.6%. The sample solutions containing different NaCl concentrations are shown in Table 6.

[0086] Table 5 Prescription Example

[0087]

[0088] Table 6 Prescription Example

[0089]

[0090]

[0091] The viscosity of the samples before and after mixi...

Embodiment 3

[0109] Embodiment 3. Prescription-viscosity curve research

[0110]

[0111]

[0112] The aim of this study was to investigate how different NaCl concentrations in the formulation changed the gel properties of the samples.

[0113] process

[0114] 1) Solution preparation

[0115] Solution 1 (1% DGG solution):

[0116] Add 29.7g of ultrapure water into a 50ml beaker; slowly disperse 0.3g of DGG into the beaker while stirring. Then put the solution into a 90°C water bath and stir for 1 hour to fully expand the gellan gum solution. After 1 hour, the stirring was stopped, the beaker was taken out from the water bath, the stirring was continued, the solution was allowed to cool at room temperature (25° C.), and then the stirring was stopped. This solution is labeled solution 1.

[0117] Solution 2 (2% povidone iodine in water):

[0118] When Solution 1 begins to cool, a 2% povidone-iodine solution in water needs to be prepared.

[0119] Put 39.2g of ultrapure water in...

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Abstract

The present invention provides pharmaceutical compositions comprising an antiseptic and a steroid, useful for treating a clinical symptom in a patients airway (e.g., nose, lung, and sinus), wherein agel containing the antiseptic is formed in situ upon instillation of the compositions onto a body cavity of a subject, as well as methods for using the same.

Description

Background technique [0001] Chronic rhinosinusitis (CRS) is often the result of a mixed inflammatory and infectious process affecting both the nose and paranasal sinuses. It is a debilitating disease that can cause severe physical symptoms and significant impairment of function. The condition is a spectrum of symptoms and a lengthy clinical course that affects as many as 30 million American adults each year. (See Pearlman et al., Review of current guidelines related to the diagnosis and treatment of rhinosinusitis, Current Opinion Otolaryngol Head Neck Surg (June 2008), 16(3), 226-30). Persistent infection can lead to chronic mucosal inflammation, altered nasal ciliary function, and nasal polyposis. Treatment of multidrug-resistant rhinosinusitis remains largely ineffective. The established role of bacterial biofilms in chronic diseases such as CRS, and their robust resistance to conventional medical and surgical treatments, poses a challenge to treating physicians. major p...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/56A61K47/36
CPCA61K9/0043A61K47/32A61K9/08A61K47/36A61K9/10A61K31/56A61K45/06A61K31/155A61K31/58A61K33/18A61P31/02A61P11/02A61K2300/00A61K31/573A61M11/007A61K9/06A61K31/555A61K31/565A61K47/02A61K47/10A61K47/18
Inventor 波·梁
Owner 艾威药业公司
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