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Flurbiprofen acetaminophen ester solid dispersion and preparation method thereof

A technology of acetaminophen ester and solid dispersion, which can be used in pharmaceutical formulations, drug delivery, non-central analgesics, etc., and can solve problems such as poor solubility and low bioavailability

Inactive Publication Date: 2013-01-16
DALIAN INST OF CHEM PHYSICS CHINESE ACAD OF SCI
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Starting from the actual market application, this project adopts solid dispersion technology with strong operability to solve the problem of low bioavailability in vivo of flurbiprofen acetaminophen ester due to poor solubility

Method used

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  • Flurbiprofen acetaminophen ester solid dispersion and preparation method thereof
  • Flurbiprofen acetaminophen ester solid dispersion and preparation method thereof
  • Flurbiprofen acetaminophen ester solid dispersion and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0023] Take 5 g of flurbiprofen acetaminophen ester, dissolve it in ethanol solution, heat 20 g of PEG4000 to 80° C. to form a molten state, slowly drop the flurbiprofen acetaminophen ester alcohol solution into the carrier material, stir, and volatilize Dry ethanol and quickly move to -20°C to solidify for 4h. The resultant was taken out, pulverized, and dried. That is, solid dispersion powder is obtained. The solid dispersion of the inventive process has an in vitro cumulative dissolution rate of 93.5±3.1% (n=6) within 45 minutes. Six samples were measured in parallel.

Embodiment 2

[0025] Take flurbiprofen acetaminophen ester 5g, dissolve in appropriate ethanol, dissolve PVP-S630 in ethanol, heat at 60°C, mix the above two solutions evenly, stir for 2 hours, evaporate the ethanol, and quickly move to Curing at -20°C for 8 hours. The resultant is taken out, pulverized, and dried to obtain a solid dispersion powder. The solid dispersion of the inventive process has an in vitro cumulative dissolution rate of 94.4±3.6% (n=6) within 45 minutes. Six samples were measured in parallel.

Embodiment 3

[0027] Take flurbiprofen acetaminophen ester 5g, kollidon VA64 20g, mix evenly, melt and extrude at 160°C, the mixture of drug and carrier is fully mixed in the extruder, dispersed, solidified, crushed and sieved to obtain Solid dispersion. The solid dispersion of the inventive process has an in vitro cumulative dissolution rate of 88.4±2.8% (n=6) within 45 minutes. Six samples were measured in parallel.

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Abstract

The invention relates to flurbiprofen acetaminophen ester solid dispersion and a preparation method thereof. Anti-inflammatory and analgesic prodrugs mainly comprise brand new compounds of flurbiprofen acetaminophen ester, and the flurbiprofen acetaminophen ester solid dispersion is prepared by adding hydrophilic carrier materials and by respectively adopting a solvent method, a solvent-melting method and a melting method and can be further prepared into oral tablets or capsules by being mixed with proper adjuvants. By the flurbiprofen acetaminophen ester solid dispersion and the preparation method thereof, solubility and dissolving-out speed of drugs can be obviously increased, the solubility of the drugs in water is increased by 10-100 times as compared with that of crude drugs, cumulative dissolving-out percentage of the drugs in dissolving-out media in 45 minutes is substantially increased accordingly, and finally oral absorbability of the drugs is improved.

Description

technical field [0001] The invention belongs to the field of pharmaceutical manufacturing, and in particular relates to a flurbiprofen paracetamol solid dispersion and a preparation method thereof. Background technique [0002] Non-steroidal anti-inflammatory analgesics (NSAIDs) are the fastest-growing drugs in the world, and are widely used to treat arthritis, especially various inflammatory pains caused by osteoarthritis and rheumatoid arthritis. Different types of NSAIDs have the same mechanism of action [Curr.Opin.Rheum.1996,8:169–175], all of which inhibit the activity of cyclooxygenase, thereby inhibiting the formation of the inflammatory response factor prostacyclin from arachidonic acid (PGI1), prostaglandins (PGE1, PGE2) and thromboxane A2 (TXA2). Such drugs are more likely to cause side effects such as gastrointestinal ulcers, bleeding, and even perforation [Br J Pharmacol.1999 Nov,128(6):1121-32.]. [0003] Flurbiprofen is an arylpropionic acid non-steroidal ant...

Claims

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Application Information

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IPC IPC(8): A61K9/00A61K31/216A61P29/00
Inventor 杨凌葛广波洪沫宁静邹超
Owner DALIAN INST OF CHEM PHYSICS CHINESE ACAD OF SCI
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