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Solid dispersions comprising tacrolimus

A technology of solid dispersion and tacrolimus, applied in medical preparations containing active ingredients, organic active ingredients, liquid delivery, etc.

Active Publication Date: 2006-11-08
VELOXIS PHARMA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Additionally, the increased bioavailability may also lead to more reproducible (i.e. not as good as Prograf  variable) release characteristics

Method used

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  • Solid dispersions comprising tacrolimus

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0207] Example 1: Immediate release tablet with enhanced bioavailability

[0208] ％

mg

Tacrolimus

0.50

1.00

Lactose 200 mesh

49.75

100.00

PEG 6000

34.48

69.30

Poloxamer 188

14.78

29.70

Magnesium stearate

0.50

1.01

total

100.00

201.01

[0209] Tacrolimus was dissolved in polyethylene glycol 6000 and poloxamer 188 (w / w ratio 70:30) at 70°C. The solution was sprayed onto 250 g of lactose in a fluidized bed Strea-1. The granulated product was sieved through a 0.7mm sieve and mixed with magnesium stearate in a Turbula mixer for 0.5 minutes. The mixture is compressed into 8 mm tablets (200 mg tablet, compound cup shape) containing 1 mg of active ingredient.

[0210] Average disintegration time: 20 minutes. Hardness: 45N.

Embodiment 2

[0211] Example 2: PEG 6000 / poloxamer 188 based immediate release tablet

[0212] substance

％

mg

Tacrolimus

1.98

2.00

Lactose monohydrate, lactose 200 mesh

40.50

40.91

PEG 6000

33.26

33.60

Poloxamer 188, Lutrol 68

14.40

14.40

Magnesium stearate

0.50

0.51

Talc

4.50

4.55

Croscarmellose Sodium, Ac-Di-Sol

5.00

5.05

100.00

101.01

[0213] Tacrolimus was dissolved in PEG 6000 at a temperature above 80°C. Poloxamer 188 was added and the solution was heated to a temperature above 80°C. The solution was sprayed onto 200 g of lactose monohydrate in a fluidized bed Phast FB100 using a dosing unit Phast FS1.7. The resulting granules were sieved with a Comill (sieve size 1397) at 4500 rpm and mixed with croscarmellose sodium in a Turbula mixer for 3 minutes.

[0214] The magnesium stearate and talc were sifted thro...

Embodiment 3

[0218] Example 3: Enteric Coating of the Immediate Release Tablet of Example 2

[0219] substance

[0220] The amount of film polymer (Eudragit) applied is based on each cm 2 Calculated in mg of film polymer on the tablet surface. The thickness of the enteric coating is 80 μm. Determination of the film thickness used was based on the measurement of the tablet height increments with a digital micrometer. The film coating process was carried out in a Phast FB100 fluidized bed equipped with a Wurster-like insert, inlet air temperature 50°C, inlet airflow 100 cbm / hour, product temperature 38°C, feed rate 15 g / min.

[0221] The coated tablets were cured in an oven at 30°C for 48 hours. Alternatively, the coated tablet can be more efficiently cured at 40°C for 24 hours.

[0222] Enteric-coated tablets were subjected to in vitro dissolution testing using two different dissolution media / test methods.

[0223] time (hours)

[0224] time (minutes)

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Abstract

A pharmaceutical composition comprising tacrolimus (FK-506) dissolved and / or dispersed in a hydrophilic or water-miscible vehicle to form a solid dispersion or solid solution at ambient temperature have improved bioavailability.

Description

[0001] The present invention relates to a solid dispersion containing tacrolimus or its analogues with improved bioavailability, more specifically, a solid solution or solid dispersion of tacrolimus in a hydrophilic vehicle; comprising a solid solution or Pharmaceutical compositions of solid dispersions; and dosage forms comprising solid solutions or solid dispersions. Background of the invention [0002] Tacrolimus, also known as FK-506 or FR-900506, has the same 44 h 69 NO 12 The corresponding chemical tricyclic structure is shown below: [0003] [0004] Tacrolimus exists as white crystals or crystalline powder. It is practically insoluble in water, freely soluble in ethanol, and readily soluble in methanol and chloroform. [0005] For the preparation of tacrolimus see EP-A-0 184 162 and for tacrolimus analogs see eg EP-A-0 444 659 and US 6,387,918 (both incorporated herein by reference). [0006] Tacrolimus is a macrolide compound with useful...

Claims

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Application Information

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IPC IPC(8): A61K31/436A61K9/14A61K9/16A61K9/20A61P37/06
CPCA61K9/1611A61K9/1617A61K9/1623A61K9/1641A61K9/1652A61K9/2009A61K9/2013A61K9/2018A61K9/2027A61K9/2031A61K9/2054A61K9/2077A61K9/2095A61K9/2846A61K9/2893A61K31/00A61K31/436A61K31/4745A61P31/00A61P37/00A61P37/06A61K9/0053A61K9/10A61K31/439
Inventor P·赫尔姆T·诺灵
Owner VELOXIS PHARMA
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