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Aspirin suppository and preparation method thereof

A technology of aspirin and suppositories, which is applied in the field of pharmaceutical preparations, can solve the problems of low dissolution rate and low bioavailability, and achieve the effects of reducing toxicity and side effects, improving safety, and reducing dust flying

Active Publication Date: 2012-11-28
蚌埠丰原涂山制药有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0004] The present invention aims to overcome the defects of low in vitro dissolution rate and low bioavailability of existing aspirin oral preparations, and provides an aspirin suppository suitable for cavity administration and a preparation method thereof

Method used

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  • Aspirin suppository and preparation method thereof
  • Aspirin suppository and preparation method thereof
  • Aspirin suppository and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0015] The preparation of embodiment 1 aspirin suppositories

[0016]

[0017] (1) Sieve 150g of aspirin and 100g of sodium carboxymethylcellulose through 100 mesh and mix well.

[0018] (2) 500 g of polyethylene glycols (300 g of polyethylene glycol 1000 and 200 g of polyethylene glycol 4000) were melted in a water bath at 85°C.

[0019] (3) Add propylene glycol stearate and stearic acid into (2), and stir well.

[0020] (4) Add (1) into (3) and stir evenly to prepare a suppository paste filling.

[0021] (5) When the temperature in (4) drops below 40°C, pour it into the mold, after cooling and solidifying, cut off the overflowing part with a knife, open the plug mold, and push it out.

Embodiment 2

[0022] The preparation of embodiment 2 aspirin suppositories

[0023]

[0024] (1) Sieve 300g of aspirin and 200g of sodium carboxymethylcellulose through 100 mesh and mix well.

[0025] (2) Melt 400 g of polyethylene glycol 4000 and 400 g of glycerin in a water bath at 85°C.

[0026] (3) Add coconut oil ester, stearic acid and carnauba wax to (2), and stir well.

[0027] (4) Add (1) into (3) and stir evenly to prepare a suppository paste filling.

[0028] (5) When the temperature in (4) drops below 40°C, pour it into the mold, after cooling and solidifying, cut off the overflowing part with a knife, open the plug mold, and push it out.

Embodiment 3

[0029] The preparation of embodiment 3 aspirin suppositories

[0030]

[0031] (1) Sieve 150 g of aspirin and 110 g of sodium carboxymethyl cellulose through 100 mesh and mix well.

[0032] (2) Melt 400g of polyethylene glycol 1000 and 300g of gelatin in a water bath at 85°C.

[0033] (3) Add the gooseberry oil ester and stearic acid into (2), and stir well.

[0034] (4) Add (1) into (3) and stir evenly to prepare a suppository paste filling.

[0035] (5) When the temperature in (4) drops below 40°C, pour it into the mold, after cooling and solidifying, cut off the overflowing part with a knife, open the plug mold, and push it out.

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PUM

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Abstract

The invention provides an aspirin suppository suitable for cavitary drug delivery and a preparation method thereof. The suppository is prepared from the following raw materials by weight part: 10-20 of aspirin, 7-12 of sodium carboxymethylcellulose, 14-28 of an oleaginous matrix (such as coconut oil ester, Litsea cubeba oil, palmitate, propylene glycol stearate and the like), 35-95 of a water soluble matrix (such as glycerol, gelatin, polyethylene glycol and the like), and 5-10 of a hardening agent (such as white wax, stearic acid, carnauba wax and the like). The drug provided in the invention can be absorbed directly from an intestinal canal, so that the destruction of a liver first-pass effect during oral administration can be avoided. The drug has the advantages of uniform dispersion, stable dissolution rate, and bioavailability improvement, thus being an effective way of administration.

Description

technical field [0001] The invention relates to the field of pharmaceutical preparations, in particular to an aspirin suppository and a preparation method thereof. Background technique [0002] Aspirin is a salicylic acid antipyretic and analgesic drug, which inhibits the activity of cyclooxygenase by selectively acetylating intracellular cyclooxygenase. It affects the synthesis of prostaglandin, a heat factor in the hypothalamus center, and restores the normal reaction of the body temperature center to regulate body temperature. In addition, aspirin also has the effect of inhibiting platelet aggregation. It is suitable for fever caused by colds; relieves mild to moderate pain; prevents arterial thrombosis and myocardial infarction. [0003] At present, aspirin solid preparations in the market include tablets and capsules, which are all oral preparations, and their dissolution rate in vitro is relatively low, and their plasma concentration and bioavailability are also low; ...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/02A61K31/616A61P29/00
Inventor 薛世静
Owner 蚌埠丰原涂山制药有限公司
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