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Solid dispersions comprising tacrolimus

A technology of active ingredients and compositions, applied in the field of solid dispersion

Active Publication Date: 2011-04-06
VELOXIS PHARMA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

In addition, improved bioavailability may also result in more reproducible (i.e. less variable) release characteristics

Method used

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  • Solid dispersions comprising tacrolimus
  • Solid dispersions comprising tacrolimus
  • Solid dispersions comprising tacrolimus

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0209] Example 1: Immediate release tablet with enhanced bioavailability

[0210] Tablet Composition:

[0211]

％

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

[0212] 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.

[0213] Average disintegration time: 20 minutes. Hardness: 45N.

Embodiment 2

[0214] Example 2: PEG 6000 / poloxamer 188 based immediate release tablet Tablet composition:

[0215] 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

[0216] Magnesium stearate

0.50

0.51

talc

4.50

4.55

Croscarmellose Sodium, Ac-Di-Sol

5.00

5.05

100.00

101.01

[0217] 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 device Phast FS 1.7. 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.

[0218] The magnesium stearate...

Embodiment 3

[0223] Example 3: Enteric Coating of the Immediate Release Tablet of Example 2

[0224] The enteric coating is based on the acrylic polymer Eudragit L30D-55. Eudragit L 30D is supplied as an aqueous latex suspension which forms a water insoluble film when the water evaporates during the coating process. The polymer is insoluble at pH values ​​below 5.0 and readily soluble at pH values ​​above 6.0. Tablets prepared as described in Example 2 were coated with the following film coating composition:

[0225] substance

w / w%

Eudragit L30D-55

40

water

52

triethyl citrate

1.8

Antifoam Lotion

0.2

Talc (fine)

6

total

100

[0226] The amount of film polymer (Eudragit) applied was calculated on the basis of mg of film polymer per cm2 of 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 increm...

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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-0184162 and for tacrolimus analogs see eg EP-A-0444659 and US 6,387,918 (both incorporated herein by reference). [0006] Tacrolimus is a macrolide compound with useful immunosuppressive activity...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K31/436A61K9/16A61K9/14A61P37/06A61K9/20
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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