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Spirolactone and hydrochlorothiazide pharmaceutical composition solid preparation

A technology of ester hydrochlorothiazide lipid and ester hydrochlorothiazide lipid, which is applied in the direction of drug combination, pharmaceutical formulation, liposome delivery, etc., can solve the problems of liposome stability and poor encapsulation efficiency, and achieve improved bioavailability, Better results, longer cycle times

Inactive Publication Date: 2011-09-21
HAINAN SHU ER PHARMA RES
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0011] After a long period of serious research and a large number of screening experiments, the inventor finally screened the combination of egg yolk lecithin, cholesterol and sodium glycocholate, and unexpectedly found that egg yolk lecithin, cholesterol and glycocholate The combination of the three materials of sodium bicarbonate solves the technical problems of poor stability and encapsulation efficiency of liposomes, and obtains unexpected preparation effects, thereby providing liposomes with good quality

Method used

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  • Spirolactone and hydrochlorothiazide pharmaceutical composition solid preparation
  • Spirolactone and hydrochlorothiazide pharmaceutical composition solid preparation
  • Spirolactone and hydrochlorothiazide pharmaceutical composition solid preparation

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0052] The preparation of embodiment 1 spironolactone hydrochlorothiazide liposome capsule

[0053] Prescription (1000 capsules)

[0054]

[0055]

[0056] Preparation Process

[0057] (1) 150g egg yolk lecithin, 75g cholesterol and 25g sodium glycocholate are dissolved in the mixed solvent of 4:1 isopropanol and acetone in 5000ml volume ratio, obtain lipid solution;

[0058] (2) Place the above-mentioned lipid solution in a pear-shaped bottle, and remove the mixed solvent by rotary evaporation in a constant temperature water bath at 45° C. to form a uniform lipid film;

[0059] (3) Disperse 25g of spironolactone and 25g of hydrochlorothiazide in 800ml of water, add it into a pear-shaped bottle and shake gently, so that the lipid film is eluted and dispersed in a hydration medium for dissolution, to obtain a liposome suspension;

[0060] (4) Place the above-mentioned suspension in an ultrasonic instrument and sonicate to a translucent colloidal solution;

[0061] (5) ...

Embodiment 2

[0065] The preparation of embodiment 2 spironolactone hydrochlorothiazide liposome capsules

[0066] Prescription (1000 capsules)

[0067]

[0068] Preparation Process

[0069] (1) 250g egg yolk lecithin, 125g cholesterol and 75g sodium glycocholate are dissolved in the mixed solvent of 4:1 isopropanol and acetone in 9000ml volume ratio, obtain lipid solution;

[0070] (2) Place the above-mentioned lipid solution in a pear-shaped bottle, and remove the mixed solvent by rotary evaporation in a constant temperature water bath at 55° C. to form a uniform lipid film;

[0071] (3) Disperse 25g of spironolactone and 25g of hydrochlorothiazide in 800ml of water, add it into a pear-shaped bottle and shake gently, so that the lipid film is eluted and dispersed in a hydration medium for dissolution, to obtain a liposome suspension;

[0072] (4) Place the above-mentioned suspension in an ultrasonic instrument and sonicate to a translucent colloidal solution;

[0073] (5) Filter the...

Embodiment 3

[0077] The preparation of embodiment 3 spironolactone hydrochlorothiazide liposome capsules

[0078] Prescription (1000 capsules)

[0079]

[0080] Preparation Process

[0081] (1) 400g egg yolk lecithin, 200g cholesterol and 100g sodium glycocholate are dissolved in a mixed solvent of 4:1 isopropanol and acetone in a volume ratio of 20000ml to obtain a lipid solution;

[0082] (2) Place the above-mentioned lipid solution in a pear-shaped bottle, and remove the mixed solvent by rotary evaporation in a constant temperature water bath at 50° C. to form a uniform lipid film;

[0083] (3) Disperse 50g of spironolactone and 50g of hydrochlorothiazide in 1500ml of water, add it into a pear-shaped bottle and shake gently, so that the lipid film is eluted and dispersed in a hydration medium for dissolution, to obtain a liposome suspension;

[0084] (4) Place the above-mentioned suspension in an ultrasonic instrument and sonicate to a translucent colloidal solution;

[0085] (5) ...

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Abstract

The invention discloses a spirolactone and hydrochlorothiazide liposome preparation which is prepared mainly from the following the ingredients in parts by weight: 1 part of spirolactone, 1 part of hydrochlorothiazide, 3-15 parts of egg phosphatidylcholine, 1-8 parts of cholesterol, and 0.5-5 parts of sodium glycyl-cholate. The invention further discloses a spirolactone and hydrochlorothiazide pharmaceutical composition solid preparation which is prepared by adding other excipient commonly used on pharmacy with the spirolactone and hydrochlorothiazide liposome preparation. The invention improves the product quality of the preparation and reduces the toxic and side effects.

Description

technical field [0001] The invention relates to a compound preparation of spironolactone hydrochlorothiazide, in particular to a solid preparation of spironolactone hydrochlorothiazide pharmaceutical composition, which belongs to the technical field of medicine. Background technique [0002] Spironolactone, whose chemical name is 17b-hydroxy-3-oxo-7a-(acetylthio)-17a-pregna-4-ene-21-carboxylic acid g-lactone, molecular formula: C 24 h 32 o 4 S, molecular weight: 416.57, structural formula: [0003] [0004] Spironolactone is similar in structure to aldosterone and is a competitive inhibitor of aldosterone. Acts on the distal convoluted tubule and collecting duct to block Na + -K + and Na + -H + Exchange, result Na + , Cl - and increased water excretion, K + , Mg 2+ and H + Decreased excretion, Ca 2+ The effect is variable. Since spironolactone only acts on the distal convoluted tubule and collecting duct, and has no effect on other segments of the renal tubu...

Claims

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Application Information

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IPC IPC(8): A61K31/585A61K31/549A61K9/127A61K47/24A61K47/28A61P9/12
Inventor 陶灵刚
Owner HAINAN SHU ER PHARMA RES
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