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Nasal in-situ gel of scopolamine with phase change property

A technology of scopolamine and in-situ gel, which is applied in the field of pharmaceutical preparations, can solve the problems of inconvenient use, limited development, and impact on bioavailability, and achieve the effects of avoiding inconvenience, prolonging contact time, and improving bioavailability

Inactive Publication Date: 2006-08-02
FUDAN UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, because the surface of the nasal mucosa contains a large number of nasal cilia and nasal mucus, their movement results in a very short residence time (about 15-30min) of the drug on the surface of the nasal mucosa, and the bioavailability is still affected to a certain extent.
Although some bioadhesive preparations such as nasal gels can prolong the residence time of drugs in the nasal mucosa, their viscosity is high, preparation is difficult, and there are defects such as inaccurate dosage and inconvenient use, which seriously limit the application of this dosage form. develop

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0023] The ion-sensitive scopolamine nasal in-situ gel was prepared according to the ratio shown in Table 1.

[0024] Prescription 1

Prescription 2

Prescription 3

Prescription 4

Scopolamine

deacetylation knot

cold glue

sodium alginate

Osmolality regulation

weight loss

preservatives

pH regulator

distilled water

0.1%

0.2%

-

Mannitol 5%

Chlorhexidine acetate

0.01%

Triethanolamine

pH to 6.5

Add water to

100%

0.5%

0.8%

-

Sorbitol 4%

Thimerosal

0.01%

NaOH adjustment

pH to 6.5

Add water to

100%

1%

-

1%

Mannitol 5%

Ethylparaben

0.03%

pH adjustment with KOH

to 6.5

Add water to

100%

2%

-

6%

Sorbitol 4%

Chlorobutanol

0.5%

Triethanolamine

pH to 6.5

Add water to

100% ...

Embodiment 2

[0034] The temperature-sensitive scopolamine nasal in-situ gel was prepared according to the ratio in Table 2.

[0035] Prescription 11

[0036] Prescription 15

[0037] The preparation method of prescriptions 11-17 is to add a certain amount of hydrophilic matrix into low-temperature phosphate buffer (pH6.5-7.4), stir to disperse evenly, and then place it in a refrigerator at 4°C for more than 24 hours until the polymer Completely dissolved to obtain a clear blank matrix, the drug and other additives are formulated into a solution or suspension, and fully mixed with the blank matrix to form a drug-containing in-situ gel.

[0038] Since the aqueous solution of the nonionic surfactant poloxamer has the property of being reversely gelled by heating, the gels prepared by prescriptions 11 and 12 are light yellow suspensions at low temperature (4°C). The entanglement and stacking effect of the gel is intensified and the gel occurs, and the solution-gel trans...

Embodiment 3

[0044] Prepare pH-sensitive scopolamine nasal in-situ gel according to the proportioning in Table 4 respectively.

[0045] Prescription 18

Prescription 19

Prescription 20

Prescription 21

Prescription 22

Scopolamine

CAP

AEA

Carbopol 940P

HPMC or MC

NaOH

CMCNa

preservatives

pH regulator

distilled water

2%

40%

-

-

-

-

-

1N Hcl to adjust pH

to 4.0

Benzyl alcohol 0.5%

Add water to 100%

5%

10%

-

-

1%

-

-

1N Hcl to adjust pH

to 4.0

Phenylethyl alcohol 0.5%

Add water to 100%

10%

-

9%

-

-

-

1%

1N Hcl to adjust pH

to 4.5

benzalkonium chloride

0.02%

Add water to 100%

5%

-

1%

-

-

-

2%

1N Hcl to adjust pH

to 4.0

Chlorobutanol

0.5%

Add water to 100%

0.1%

-

...

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PUM

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Abstract

The present invention belongs to the field of medicine preparation, and is nasal in-situ gel of scopolamine with phase change property as one new kind of nasal medicine preparation form. The medicine preparation is prepared with scopolamine or its pharmaceutically acceptable salt or ester derivative, hydrophilic gel and pharmaceutically essential supplementary material. It is water solution of scopolamine containing environment sensitive polymer material, and is liquid at normal state and forms gel on the surface of nasal mucous membrane fast after nasal cavity administration. It has delayed medicine elimination, raised bioavailability, no preparation and use inconvenience like that of common high viscosity gel preparation and no toxicity on nasal cilium.

Description

technical field [0001] The invention belongs to the field of pharmaceutical preparations, and relates to a new dosage form of nasal medicine-scopolamine nasal in-situ gel with phase transition properties. Specifically, it is an aqueous solution of scopolamine containing environmentally sensitive polymers, which is in a liquid state under normal conditions, and quickly forms a gel on the surface of the nasal mucosa after nasal administration, thereby delaying drug elimination and improving bioavailability. Background technique [0002] Airsickness and seasickness are commonly referred to as motion sickness or motion sickness, and are mainly a disease caused by low-frequency noise or infrasound produced by the engine of an airplane or boat when a person takes an airplane or boat. Symptoms include nausea, vomiting, and loss of appetite. [0003] Scopolamine is an anticholinergic drug with a chemical name of 6β, 7β-epoxy-1αH, 5αH-tropane-3α-ol (-) tropinate. It mainly plays th...

Claims

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Application Information

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IPC IPC(8): A61K31/46A61K9/00A61K9/06A61P11/02
Inventor 蒋新国曹师磊
Owner FUDAN UNIV
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