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Flurbiprofen acetaminophen solid dispersion and preparation method thereof

A technology of acetaminophen ester and solid dispersion, which is applied in the directions of non-active ingredients medical preparations, pharmaceutical formulations, non-central pain relievers, etc., can solve the problems of low bioavailability and poor solubility, etc.

Inactive Publication Date: 2016-01-06
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 solid dispersion and preparation method thereof
  • Flurbiprofen acetaminophen solid dispersion and preparation method thereof
  • Flurbiprofen acetaminophen solid dispersion and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0033] Embodiment 1: the preparation of flurbiprofen acetaminophen ester

[0034] Weigh 100g (410mmol) flurbiprofen into a round-bottomed flask, add dichloromethane dropwise while stirring until flurbiprofen is completely dissolved in an ice bath, then slowly add the last 45mL (614mmol) dichloromethane Sulfoxide, reacted at room temperature for 6 hours, and evaporated the solvent to obtain 105.5 g of flurbiprofen acyl chloride, with a yield of 98%. Weigh 73g (792mmol) of acetaminophen and place it in a round-bottomed flask, dichloromethane solvent, under ice-bath conditions, slowly add 112mL (803mmol) of triethylamine dropwise, and then the flurbirol dissolved in dichloromethane Fenyl chloride was slowly added dropwise to the acetaminophen solution. Remove the ice bath and react for 6 hours.

[0035] After the reaction, extract with water three times (200mL×3), extract with sodium bicarbonate solution three times (200mL×3), dry the organic phase with anhydrous magnesium sulf...

Embodiment 2

[0043] Take 5g of flurbiprofen acetaminophen ester, dissolve it in ethanol solution, heat PEG400020g to 80°C to form a molten state, slowly add flurbiprofen acetaminophen ester alcohol solution dropwise to the carrier material, stir, and evaporate to dryness Ethanol, quickly moved to -20 ℃ solidified 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 3

[0045] 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.

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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 [BrJPharmacol.1999Nov, 128 (6): 1121-32.]. [0003] Flurbiprofen is an arylpropionic acid non-steroidal an...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K9/14A61K31/216A61K47/34A61K47/32A61K47/38A61P29/00
Inventor 杨凌葛广波邹超宁静洪沫王平
Owner DALIAN INST OF CHEM PHYSICS CHINESE ACAD OF SCI
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