Solubilized ibuprofen

A technology of mixture and potassium carbonate, applied in the direction of anhydride/acid/halide active ingredients, microcapsules, capsule delivery, etc., can solve the problems that do not mention the importance of water content ibuprofen dehydrate or hydrate

Inactive Publication Date: 2008-05-07
LOSAN PHARMA GMBH
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

In particular, however, there is no description of solubilized ibuprofen granules, which are prepared by inverting in particular at least two basic adjuvants and, if desired, adding highly water-soluble adjuvants together with ibuprofen, or specifically introducing - References to technical advantages, which will surprise those skilled in the art, such as the compressibility of this class of solubilized ibuprofen compounds
With the exception of WO 2004 / 035024, there is no mention of the importance of water content or whether it involves solubilized ibuprofen dehydrate or hydrate

Method used

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  • Solubilized ibuprofen

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1-15

[0134] The examples outlined in Table 1 were carried out in a heatable and coolable mixing vessel.

[0135]

Example

base and excipients a)

heating b)

product

temperature c)

notes d)

1

0.95 mole NaOH

2.0% Mannitol

(ambient temperature)

81℃

Vigorously exothermic; add 1 mole

Water; granular powder, very weak

compressibility of

2

1.0 mol Na 2 CO 3

0.4 mol KCl

8% Povidone K25

38℃

41℃

Add 0.5 moles of water before solubilization

And add 1.5 molar after solubilization

Er water; granule powder, good

compressibility of

3

1.0 mole K 2 CO 3

65℃

86℃

Add 0.2 moles of water, hygroscopicity

fine powder, very good

Compressibility, v...

Embodiment 16

[0146] a) 6.18 kg (30 moles) of ibuprofen, 2.25 kg (30 moles) of glycine and 1.2 kg (30 moles) of ground sodium hydroxide were mixed in a mixing vessel. The temperature of the vigorously stirred mixture was raised to 68° C. over 20 minutes while the mixture was transformed into a viscous mass. A 1 g sample of pellets dissolved in 100 mL of 37°C water within 35 seconds, thus indicating that solubilization was complete. 540 g of water were added to the warm mass within 5 minutes, and the mass was converted to coarse granules within 10 minutes with slow stirring. After 15 minutes at 60° C., the granules were sieved through a sieve with a mesh size of 1.5 mm. The obtained granules (granule A) had a loss on drying of 11.2% w / w at 105°C for 30 minutes. Granular samples stored in a desiccator at 25°C and 75% relative humidity for 2 months absorbed only 0.3% w / w of water. A portion of the granules was dried in a drying oven at 60°C until the loss on drying (105°C, 30 minutes) was 6...

Embodiment 17

[0154] Mix 206 kg (1000 moles) of ibuprofen with 16 kg (400 moles) of ground sodium hydroxide, 47.7 kg (450 moles) of sodium carbonate, 13.8 kg (100 moles) of potassium carbonate, 10 kg of povidone K25 and 7 kg of sucrose monohard The fatty acid esters are mixed vigorously in a mixing vessel. The temperature of the mixture was raised to about 50°C and within 30 minutes slightly sticky granules formed. 1 g of granule sample was dissolved in 100 mL of 37° C. water within 25 seconds. The solubilized granules were transferred to a fluid bed granulator and sprayed in 100 liters of water at an inlet air temperature of about 30°C. The moisture content of the granules obtained was 8.8% w / w, measured according to the loss on drying method at 70° C. for 30 minutes. The granules were stored for 3 months at 25°C and 75% relative humidity, and their water uptake was 2.8% (w / w).

[0155] The granules obtained are mixed with 1.5% magnesium stearate in a fluidized bed granulator and compre...

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Abstract

The present invention relates to a process for the preparation of solubilized ibuprofen, preferably in granular form, comprising the steps of: providing a mixture comprising solid ibuprofen and a first base, said first A base is selected from sodium hydroxide, potassium hydroxide, sodium carbonate, potassium carbonate, sodium glycinate, potassium glycinate and third generation sodium and potassium phosphates and mixtures thereof, and ibuprofen and the first base are mixed in a substantially dry state response. The granules and pharmaceutical compositions obtained and the dosage forms prepared therefrom are distinguished by their high solubility and fast disintegration and dissolution in aqueous media, good flowability and compressibility, fast onset of analgesic action.

Description

field of invention [0001] The present invention relates to solubilized ibuprofen, in particular solubilized ibuprofen in the form of granules, pharmaceutical dosage forms comprising solubilized ibuprofen and processes for the preparation of solubilized ibuprofen and ibuprofen granules. Background of the invention [0002] Due to its action and high tolerability at doses of 200mg and 400mg, ibuprofen is one of the most commonly used drugs for pain relief. Based on the amount of ibuprofen produced globally, annual consumption is estimated to be about 30 billion tablets. Given its lower cost, available dosage forms mainly include ibuprofen in acid form. However, ibuprofen has poor and highly pH dependent solubility. Since the solubility only increases at a pH above 6.5, the active ingredient is dissolved and absorbed only in the intestinal tract and not in the stomach. Depending on the pH conditions in the gut, absorption may also be delayed for physiological reasons. This ...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/50A61K31/19
Inventor P·格鲁贝尔
Owner LOSAN PHARMA GMBH
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