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Schneiderian membrane medication preparation of isosorbide dinitrate and preparation method thereof

A technology of isosorbide dinitrate and nasal mucosa is applied in the field of nasal mucosa drug delivery preparation and preparation thereof, which can solve the problems of low oral bioavailability and the like, and achieve the effects of abundant capillaries, rapid action and rapid drug absorption.

Active Publication Date: 2010-06-30
SHENYANG PHARMA UNIVERSITY
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

But its oral bioavailability is low, less than 30% of that of intravenous injection

Method used

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Examples

Experimental program
Comparison scheme
Effect test

example 1

[0019] Isosorbide Dinitrate 1.0g

[0020] HP-β Cyclodextrin 30.0g

[0021] Poloxamer 188 0.5g

[0022] Ethylparaben 0.02g

[0023] pH adjuster Adjust pH to 6.0

[0024] Add distilled water to 100mL

[0025] Preparation of Isosorbide Dinitrate Nasal Drops Solution: Take Poloxamer 188 to make a 0.5% solution, add 30.0g HP-β cyclodextrin to dissolve, weigh the prescribed amount of Isosorbide Dinitrate, and mix under stirring conditions Add it to the above-mentioned poloxamer 188 / HP-β cyclodextrin mixed solution to make a solution containing 10.0 mg / mL of isosorbide dinitrate, add 0.02 g of preservative ethyl paraben, stir, and adjust the pH of the solution The value is 6.0, filtered, sterilized, subpackaged, and obtained.

example 2

[0027] Isosorbide Dinitrate 0.5g

[0028] HP-β Cyclodextrin 20.0g

[0029] Tween80 2.0mL

[0030] Chitosan (Mw=100kDa, DDA=84.7%) 1.0g

[0031] Ethylparaben 0.05g

[0032] pH adjuster Adjust pH to 6.0

[0033] Add distilled water to 100mL

[0034] Preparation of Isosorbide Dinitrate Nasal Drops Solution: Take chitosan (Mw=100kDa, DDA=84.7%) to make a 1.0% solution, add 20.0g HP-β cyclodextrin and 2.0mL Tween80 to dissolve, weigh Get the isosorbide dinitrate of recipe quantity, join in above-mentioned chitosan / HP-beta cyclodextrin, Tween80 mixed solution under stirring condition, make the solution containing isosorbide dinitrate 5.0mg / mL, add 0.05g preservative Add ethyl paraben, stir, adjust the pH value of the solution to 6.0, filter, sterilize, and subpackage to obtain.

example 3

[0036] Isosorbide Dinitrate 0.5g

[0037] Polyethylene glycol (Mw=600Da) 15.0mL

[0038] Propylene glycol 5.0mL

[0039] HP-β Cyclodextrin 0.1g

[0040] Ethylparaben 0.04g

[0041] pH adjuster Adjust pH to 6.0

[0042] Add distilled water to 100mL

[0043] Preparation of Isosorbide Dinitrate Nasal Drops Solution: Take HP-β cyclodextrin to make 0.1% solution, add the prescription amount of polyethylene glycol (Mw=600Da), propylene glycol and mix evenly, take the prescription amount of isosorbide nitrate Sorbitate, added to the above-mentioned HP-β cyclodextrin / polyethylene glycol, propylene glycol mixed solution under stirring conditions to make a solution containing isosorbide dinitrate 5.0mg / mL, add 0.04g preservative paraben ester, stirring, adjusting the pH value of the solution to 6.0, filtering, sterilizing, subpackaging, and the product is obtained.

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Abstract

The invention belongs to the medical technology field and discloses a schneiderian membrane medication preparation of isosorbide dinitrate and a preparation method thereof. The schneiderian membrane medication preparation of the isosorbide dinitrate consists of isosorbide dinitrate, pharmaceutical excipients and absorbefacients, the proportion of the weight percentage of the isosorbide dinitrate,the pharmaceutical excipients and the absorbefacients is 0.5-1.0:0.1-30.0:0.1-30.0, and solvent is used for allowance. The preparation method comprises the step of adding the preparation amount of isosorbide dinitrate into solution which is dissolved in advance and contains the sorbefacients with proper concentration and other additives under the agitating condition to prepare the schneiderian membrane medication preparation such as nasal drip solution agents, spraying agents, aerosols, gels and the like. The invention solves the defects of bad oral absorption of the isosorbide dinitrate and large gastrointestinal tract and liver first-pass effect; and the medication preparation has quick absorption and quick effect by utilizing the characteristics of rich schneiderian membrane blood capillary and thin membrane, can be used for the acute exacerbation of angina, coronary heart disease and heart failure and also can be used for the prevention and the treatment of chronic heart failure. The invention has the advantages of good absorption, quick effect, good stability and less side effect.

Description

technical field [0001] The invention relates to the technical field of medicine, and relates to a nasal mucosa administration preparation of isosorbide dinitrate and a preparation method thereof. The nasal mucosa preparation can be used for acute attacks of angina pectoris, and can also be used for the prevention and treatment of chronic heart failure, and has rapid onset of action , good absorption, high curative effect, good stability and few side effects. Background technique [0002] Angina pectoris is the most common and prominent symptom of coronary artery disease patients. In the United States, more than 6 million patients suffer from angina pectoris, and the number is increasing by 350,000 every year. The traditional oral or sublingual route of administration not only cannot avoid the degradation of the gastrointestinal tract and the first-pass effect of the liver, but also once the disease occurs, the patient is often accompanied by symptoms of confusion, which cons...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/34A61K9/08A61K9/12A61K9/00A61P9/10A61P9/04A61K47/40A61K47/36A61K47/34A61K47/10
Inventor 毛世瑞那丽东
Owner SHENYANG PHARMA UNIVERSITY