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Process for preparation of oral pharmaceutical compositions comprising biphosphonates

A composition and drug technology, applied in the direction of drug combination, medical preparations containing active ingredients, active ingredients of phosphorus compounds, etc., can solve the problems of increasing the risk of forming complexes

Inactive Publication Date: 2004-06-23
F HOFFMANN LA ROCHE & CO AG
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

The risk of complex formation is further increased by the abrasive action of certain pharmaceutical excipients

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0019] Embodiment 1 (comparative example 1):

[0020] Ibandronate 2.5 mg capsules (batch size 45.000 capsules) were prepared after granulation in a high speed blender / granulator.

[0021] component g

[0022] Sodium ibandronate 120.24

[0023] Lactose 7934.76

[0024] Polyvinylpyrrolidone 202.50

[0025] Cross-linked polyvinylpyrrolidone (disintegrant) 562.50

[0026] Stearic acid (lubricant) 180.00

[0027] The content of active substance in each capsule corresponds to 2.5 mg of free acid.

[0028] Lactose, ibandronate and polyvinylpyrrolidone were mixed in a high speed mixer / granulator (Diosna type) for 2 minutes at a fill factor of 50%, followed by granulation with water for 8 minutes. The wet granules were dried in a fluidized bed (Aeromatic type equipment), passed through a 0.8 mm sieve, mixed with a disintegrant and a lubricant (Rhoenrad type agitator, mixing time 10 minutes), and processed in a capsule machine (MG2 / G23 type). ) in size 2 hard gelatin capsules bu...

Embodiment 2

[0032] Embodiment 2 (comparative example):

[0033] Ibandronate 1.0 mg capsules (batch size 5000 capsules) were prepared after granulation in a high speed blender / granulator.

[0034] component g

[0035] Sodium ibandronate 5.345

[0036] Lactose 999.655

[0037] Polyvinylpyrrolidone 22.500

[0038] Cross-linked polyvinylpyrrolidone (disintegrant) 62.500

[0039] Stearic acid (lubricant) 10.00

[0040] The active substance content in each capsule is equivalent to 1.0 mmg of free acid.

[0041] Lactose, ibandronate and polyvinylpyrrolidone were mixed in a high speed mixer / granulator (Diosna type) for 2 minutes and then granulated with water for 10 minutes. The wet granules were dried in a fluidized bed (Aeromatic type equipment), passed through a 0.8 mm sieve, mixed with a disintegrant and a lubricant (Rhoenrad type mixer, mixing time 10 minutes) and processed in a capsule machine (KFM Harro Hofliger type). ) enclosed in size 2 hard gelatin capsules.

[0042] Specified ...

Embodiment 3

[0046] Ibandronate 1.0 mg tablets (batch size 60.000 tablets) were prepared after granulation in a fluid bed.

[0047] component g

[0048] Sodium ibandronate 64.14

[0049] Lactose 4405.86

[0050] Polyvinylpyrrolidone 150.00

[0051] Cross-linked polyvinylpyrrolidone (disintegrant) 300.00

[0052] Stearic acid (lubricant) 120.00

[0053] Microcrystalline Cellulose 900.00

[0054] Colloidal SiO 2 (Glidant) 60.0

[0055] The active substance content in each tablet corresponds to 1.0 mg of free acid.

[0056] Lactose and 600 g of microcrystalline cellulose were granulated in a fluidized bed (Aeromatic type) with an aqueous solution containing polyvinylpyrrolidone and ibandronate. The wet granules were dried in a fluidized bed (Aeromatic type equipment), passed through a 1.0 mm sieve, mixed with disintegrant, lubricant, flow regulator and 300 g of microcrystalline cellulose (Turbula type mixer, mixing time 5 minutes) and Tablets are converted in a tablet press (Korsch t...

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PUM

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Abstract

The invention relates to a process for the preparation of bisphonate-containing pharmaceutical compositions for oral application, wherein the active substance is wet-granulated in manner known per se in a fluidised-bed granulator using adjuvants which have no abrasive action and wherein the wet granulate is then dried in the fluidised bed, screened through a screen having a suitable mesh width and further processed by techniques known per se to form pharmaceutical compositions.

Description

technical field [0001] The present invention relates to a preparation method of a pharmaceutical composition for oral administration, which contains aminoalkyl-1,1-diphosphonic acid derivatives or their physiologically safe salts (hereinafter referred to as bisphosphonate compounds) as active substance. Background technique [0002] Bisphosphonates are crucial in the treatment of bone diseases and certain disorders of calcium metabolism, such as hypercalcemia, osteoporosis, tumor osteolysis, Paget's disease, etc. [0003] Pharmaceutical formulations often have to meet stringent requirements for content, content uniformity and purity. The specific properties of the active substance may adversely affect the content, uniformity and purity of the dosage form to be administered. Bisphosphonates are known to be a class of substances that strongly tend to form complexes with polyvalent metal ions. Common pharmaceutical preparations for oral use are often produced in equipment an...

Claims

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Application Information

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IPC IPC(8): A61K9/16A61K9/20A61K9/28A61K9/48A61K31/66A61K31/663A61K47/12A61K47/26A61K47/32A61K47/38A61P3/14A61P19/08A61P19/10
CPCA61K9/2013A61K9/4858A61K31/663A61P19/00A61P19/08A61P19/10A61P3/14A61K9/16
Inventor 罗尔夫-迪特尔·加贝尔约恩·默克尔海因里希·伍格
Owner F HOFFMANN LA ROCHE & CO AG