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Epalrestat dropping pills and preparation thereof

A technology of epalrestat and dripping pills, applied in the field of drug preparation, can solve the problems of further improvement of bioavailability, single dosage form, etc., and achieve the effects of being beneficial to labor protection, rapid drug effect and high bioavailability

Inactive Publication Date: 2008-08-13
HAINAN JINXING PHARMA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0004] But now only tablets and capsules of epalrestat are in use, the dosage form is relatively single, and its clinical utilization needs to be further improved

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0030] For every 1000 drop pills, 5g of epalrestat, 9g of polyethylene glycol 4000, 6g of polyethylene glycol 6000, 1mg of tert-butyl-4-hydroxyanisole and 0.1g of Tween 80 were used.

[0031] The preparation method is:

[0032] (1) Grinding and finely grinding epalrestat raw materials to more than 150 mesh;

[0033] (2) Take polyethylene glycol 4000, polyethylene glycol 6000 and tert-butyl-4-hydroxyanisole by prescription, heat to the eutectic point of the three, make it melt and mix uniformly;

[0034] (3) Lower the above eutectic solution to 80-85°C and keep it warm, add epalrestat powder and Tween 80, and stir evenly.

[0035] (4) Transfer the above solution into a dripping device for dripping. The temperature of the solution is controlled at 80-85° C., drop into frozen liquid paraffin, remove the liquid paraffin, and dry in the air.

[0036] Detect the semi-finished products, and pack them after passing the test.

Embodiment 2

[0038] For every 1000 drop pills, 7.5g epalrestat, 27g polyethylene glycol 4000, 10.5g polyethylene glycol 6000, 2.5mg tert-butyl-4-hydroxyanisole and 0.2g Tween 80 were used.

[0039] Preparation method is the same as embodiment 1

Embodiment 3

[0041] For every 1000 drop pills, 10.0g epalrestat, 40.0g polyethylene glycol 4000, 30g polyethylene glycol 6000, 3.0mg tert-butyl-4-hydroxyanisole and 0.25g Tween 80 were used.

[0042] Preparation method is the same as embodiment 1

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PUM

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Abstract

The invention discloses an Epalrestat pill, which is characterized in that the invention comprises an Epalrestat, a Carmowax carrier, an antioxidant and a surfactant. The pill has favorable stability and high bioavailability.

Description

technical field [0001] The invention relates to an epalrestat dropping pill, which belongs to the technical field of medicine preparation. Background technique [0002] Epalrestat was first listed in Japan in 1992. It is a reversible non-competitive aldose reductase inhibitor (ARI) of carboxylic acids. Chronic complications of nerves, blood vessels, heart, and organs are the direct causes of blindness, lower limb gangrene, uremia, cerebral apoplexy or myocardial infarction, and even life-threatening. [0003] It is now known that certain metabolic pathways and signal transduction pathways play a very important role in the occurrence and development of diabetic complications. For example, under normal circumstances, only about 5% of the glucose in the cell enters the polyol channel, but in the state of diabetes, the polyol channel is activated, and about 30% of the glucose enters this channel, which can cause the depletion of NADPH in the cell and indirectly activate DAG- P...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/20A61K31/426A61K47/34A61P3/10A61K47/10A61K47/26
Inventor 刘全胜马明夏兵曹俊
Owner HAINAN JINXING PHARMA
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