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Pharmaceutical compositions containing diacerein

A technology of diacerein and formulations, applied in the field of pharmaceutical compositions containing diacerein

Inactive Publication Date: 2011-09-28
TWI BIOTECH
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Although the bioavailability of diacerein is increased to 43%-70% by feeding, incomplete absorption still leads to local effects in the colon

Method used

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  • Pharmaceutical compositions containing diacerein
  • Pharmaceutical compositions containing diacerein
  • Pharmaceutical compositions containing diacerein

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0063] Preparation of solid dispersions

[0064] Typical acceptable ranges for solid dispersion ingredients are shown in Table 3.

[0065] table 3

[0066]

[0067] Process:

[0068] Diacerein is dissolved in a suitable organic solvent to form a drug solution. Carriers such as hydrophilic polymers, hydrophobic polymers, surfactants, water-soluble excipients or waxes, or a combination of the above carriers are then dissolved or dispersed in the drug solution. Solid dispersions can be obtained by spray drying the above solutions, or by coating the solutions on a suitable vehicle (a water soluble material used as a secondary carrier) using a fluidized bed.

Embodiment 2

[0070] complexed with cyclodextrin

[0071] Acceptable ranges for the composition of typical complexes complexed with cyclodextrins are shown in Table 4.

[0072] Table 4

[0073]

[0074] Process:

[0075] Aqueous solutions of cyclodextrins can be prepared in different percentages. Diacerein was added to the above solution to make a saturated solution. The solution was stirred for at least 72 hours and then allowed to stand until precipitation of the insoluble material was complete. The supernatant is filtered and dried via oven, spray drying or freeze drying, or coated on a suitable vehicle (as a diluent) using a fluidized bed.

Embodiment 3

[0077] Matrix System (Tablet)

[0078] The acceptable ranges for the ingredients of a typical tablet matrix system are shown in Table 5.

[0079] table 5

[0080]

[0081] Process:

[0082] API fractions were prepared as described in the above examples. The Diacerein API portion is physically mixed or granulated with the controlled release material and the mixture is then compressed to obtain matrix tablets. Optionally, acidulants or buffers are added to the tablet formulation.

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Abstract

A once-daily controlted-release formulation of diacerein for treating inflammatory or autoimmune diseases or their complications, with reduced adverse side effects and methods of treating such diseases are disclosed.

Description

Background technique [0001] Diacerein (4,5-bis(acetoxy)-9,10-dioxo-2-anthracenecarboxylic acid) is a highly purified anthraquinone derivative. It is known to inhibit the activity of interleukin-1, and has been approved as a Symptomatic Slow-Acting Drug in Osteoarthritis (SYSADOA) in several countries. [0002] Diacerein has a log P value of 2.42 and is practically insoluble in water. Diacerein is completely converted to rhein before entering the circulation. Rhein is excreted by itself via the renal route (20%), or is conjugated in the liver to form rhein glucuronide (60%) and rhein sulfate (20%). Most of these metabolites are excreted through the kidneys. [0003] Diacerein has two main adverse side effects: diarrhea or soft stools and yellow-brown urine. Diarrhea was mild to moderate in severity and occurred within the first two weeks of treatment. Urine staining is due to the presence of metabolites of diacerein in the urine. In vitro and in vivo studies have shown th...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/715
CPCA61K9/1676A61K9/284A61K9/2846A61K9/5078A61K9/146A61K9/2018A61K9/2054A61K9/2866A61K31/235A61K9/2853A61K9/2013A61K47/6951A61P1/02A61P1/04A61P11/00A61P11/06A61P13/12A61P17/00A61P17/02A61P17/06A61P19/00A61P19/02A61P19/10A61P25/00A61P29/00A61P37/00A61P37/02A61P37/06A61P37/08A61P43/00A61P9/10A61P3/10
Inventor 高丹晨吴振森卢威书陈守琼郭姵君陈志明
Owner TWI BIOTECH
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