Liquid medicine composition of rosiglitazone

A technology for rosiglitazone and a composition, which is applied in the directions of drug combination, metabolic diseases, aerosol delivery, etc., can solve the problems of low solubility of rosiglitazone, single dosage form, inconvenient taking of solid preparations, etc., and achieves increased drug use Compliance and patient compliance, novel dosage forms, and beneficial effects on long-term treatment

Active Publication Date: 2013-05-29
BEIJING HUMANWELL JUNWEI PHARM TECH CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0005] Rosiglitazone is a relatively ideal hypoglycemic drug. The drug is currently on the market in most countries around the world, but it has a single dosage form, and only tablets are used clinically. The usual dosage is 4mg per day, taken in a single dose
Existing solid preparations usually require water when taken, and in many cases, such as for the elderly or when going out, the taking of solid preparations is inconvenient
However, due to the low solubility of rosiglitazone, it is a great challenge for the development of its liquid formulations

Method used

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  • Liquid medicine composition of rosiglitazone
  • Liquid medicine composition of rosiglitazone
  • Liquid medicine composition of rosiglitazone

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0049] Example 1, Rosiglitazone maleate liquid composition

[0050] formula:

[0051]

[0052] Preparation method: Dissolve the prescription amount of rosiglitazone maleate with glycerin and 1,2-propanediol, then add stevioside and menthol, shake well, and make the volume constant with phosphate buffer to get it.

[0053] In this embodiment, the phosphate buffer is a solution containing sodium dihydrogen phosphate and disodium hydrogen phosphate at 0.05 mol / L each and adjusting the pH to 5.5 with phosphoric acid solution or sodium hydroxide solution.

Embodiment 2

[0054] Example 2, Rosiglitazone maleate liquid composition

[0055] formula:

[0056]

[0057] Preparation method: add ethanol and 1,2-propanediol to the prescription amount of rosiglitazone maleate until it is completely dissolved and clear, then add menthol, stevioside, and citric acid, and dilute with phosphate buffer to get it.

[0058] In this embodiment, the phosphate buffer is a solution containing 0.1 mol / L of sodium dihydrogen phosphate and disodium hydrogen phosphate each and adjusting the pH to 6.5 with phosphoric acid solution or sodium hydroxide solution.

Embodiment 3

[0059] Example 3. Rosiglitazone maleate liquid composition

[0060] formula:

[0061]

[0062] Preparation method: Add the prescription amount of rosiglitazone maleate to ethanol until it is completely dissolved and clear, then add Tween-80 and mix well, add cinnamon oil and sorbitol, and make the volume constant with phosphate buffer.

[0063] In this embodiment, the phosphate buffer is a solution containing 0.25 mol / L of sodium dihydrogen phosphate and disodium hydrogen phosphate each and adjusting the pH value to 4.5 with phosphoric acid solution or sodium hydroxide solution.

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PUM

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Abstract

The invention discloses a liquid medicine composition of rosiglitazone or pharmaceutical salt thereof. The liquid medicine composition comprises a curing and / or preventing effective quantity of rosiglitazone or pharmaceutical salt, cosolvent, phosphate and water thereof. The composition disclosed by the invention has the advantages as shown in the specification.

Description

Technical field [0001] The invention belongs to the field of pharmacy, and relates to a drug for treating hyperglycemia, in particular to a liquid composition containing rosiglitazone or its medicinal salt. The composition can be used to administer the oral mucosal route for rapid absorption and lower blood sugar. Background technique [0002] Rosiglitazone is a thiazolidinedione, which is an effective insulin sensitizer. The chemical name of maleic acid is (±)-5-[[4-[2-(methyl-2-pyridylamino)ethyl [Oxy]phenyl]methyl]-2,4-thiazolidinedione (Z)-2-butenedioate, the structure is as follows: [0003] [0004] Rosiglitazone maleate was approved by the US FDA in May 1999. It is a potent oral treatment for type 2 (non-insulin-dependent) diabetes. It is a highly selective and powerful peroxidase. Proliferation-activated receptor gamma (PPAR gamma) agonists, which bind to and activate PPAR gamma, thereby increasing the synthesis of a variety of proteins. These proteins are involved in th...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K9/12A61K31/4439A61P3/10
Inventor 高永良王炳璋
Owner BEIJING HUMANWELL JUNWEI PHARM TECH CO LTD
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