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Salts of the CGRP antagonist BIBN4096 and inhalable powdered medicaments containing them

a technology of bibn4096 and bibn4096, which is applied in the field of salts, can solve the problems of inability to administer orally using conventional preparations, increased stress, and compatibility problems

Inactive Publication Date: 2005-07-07
BOEHRINGER INGELHEIM PHARMA GMBH & CO KG
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Benefits of technology

Achieves a bioavailability of about 60% through inhalation, with improved pharmacokinetic properties and particle characteristics, enabling rapid absorption and high plasma levels, and simplifies industrial-scale processing with enhanced dispersibility and stability.

Problems solved by technology

It cannot be administered orally using conventional preparations as the substance has only limited bioavailability by oral route both in the form of the active substance base and also in the form of its salts.
Moreover, the carrier results in additional stress on the lungs as well as the occurrence of undesirable interactions, which may lead to problems of compatibility.
As a result, such particles may often be of complex composition in terms of their crystal properties as a result of this mechanical step.

Method used

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  • Salts of the CGRP antagonist BIBN4096 and inhalable powdered medicaments containing them
  • Salts of the CGRP antagonist BIBN4096 and inhalable powdered medicaments containing them
  • Salts of the CGRP antagonist BIBN4096 and inhalable powdered medicaments containing them

Examples

Experimental program
Comparison scheme
Effect test

example 5

Spray Parameter Suitable for an Aqueous BIBN4096 Solution (Modified BÜCHI Spray Tower)

[0084]

Concentration solution2 g / 100 gsolvent:0.012 mol / L sulphuric acidDroplet size Q(5.8)39%(Reference solution: H2O at ambienttemperature)X507.0 μmvolumetric flow “spray rate”0.54 L / hspray pressure3.3-3.5 bar overpressure (N2)(nozzle type)(BÜCHI spray nozzle 0.7 mm,Art. No. 04364)Mass flow Spray gas nozzle type2.1 kg / h(BÜCHI spray nozzle 0.7 mm,Art. No. 04364)Inlet temperature150° C.Outlet temperature101° C.volumetric flow “drying gas”35 standard m3 / hcross section of drying tower105 mm

example 6

Spray Parameter Suitable for an Qqueous BIBN4096 Solution (Modified BÜCHI Spray Tower)

[0085]

Concentration solution5 g / 100 gsolvent:0.02 mol / L citric acidDroplet size Q(5.8)55%(Reference solution: H2O at ambienttemperature)X505.5 μmvolumetric flow “spray rate”0.54 L / hspray pressure4.4-4.6 bar overpressure (N2)(nozzle type)(BÜCHI spray nozzle 0.7 mm,Art. No. 04364)Mass flow Spray gas nozzle type2.8 kg / h(BÜCHI spray nozzle 0.7 mm,Art. No. 04364)Inlet temperature150° C.Outlet temperature 99° C.volumetric flow “drying gas”35 standard m3 / hcross section of drying tower105 mm

example 7

Spray Parameter Suitable for an Aqueous BIBN4096 Solution (Modified BÜCHI Spray Tower)

[0086]

Concentration solution10 g / 100 gsolvent:0.06 mol / L tartaric acidDroplet size Q(5.8)60%(Reference solution: H2O at ambienttemperature)X505.3 μmvolumetric flow “spray rate”0.54 L / hspray pressure4.7-4.9 bar overpressure (N2)(nozzle type)(BÜCHI spray nozzle 0.7 mm,Art. No. 04364)Mass flow Spray gas nozzle type3 kg / h(BÜCHI spray nozzle 0.7 mm,Art. No. 04364)Inlet temperature150° C.Outlet temperature101° C.volumetric flow “drying gas”35 standard m3 / hcross section of drying tower105 mm

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Abstract

The invention relates to salts of the active substance base 1-[N2-[3,5-dibromo-N-[[4-(3,4-dihydro-2-(1H)-oxoquinazolin-3-yl)-1-piperidinyl]carbonyl]-D-tyrosyl]-L-lysyl]-4-(4-pyridinyl)-piperazine [BIBN4096] of formula I, the preparation thereof, a process for preparing an inhalation powder containing a salt of the active substance BIBN4096 as well as the inhalation powders which can be obtained by the process.

Description

RELATED APPLICATIONS [0001] Benefit of U.S. Provisional Application Ser. No. 60 / 362,268, filed on Mar. 6, 2002 is hereby claimed.FIELD OF THE INVENTION [0002] The invention relates to salts of the substance 1-[N2-[3,5-dibromo-N-[[4-(3,4-dihydro-2(1H)-oxoquinazolin-3-yl)-1-piperidinyl]carbonyl]-D-tyrosyl]-L-lysyl]-4-(4-pyridinyl)-piperazine [BIBN4096] of formula I, which are stable in their amorphous state under normal conditions (T<50° C., relative humidity<75%), processes for preparing them, the use of these salts for preparing a pharmaceutical composition of the inhalation powder type, particularly for preparing a pharmaceutical composition with CGRP-antagonistic properties, as well as a process by means of which in a single step the thermodynamically stable or stabilised salts of the active substance in their amorphous state can be processed to form microparticles. [0003] In the process according to the invention the salts are obtained in the form of spherically nanostructu...

Claims

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Application Information

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Patent Type & Authority Applications(United States)
IPC IPC(8): A61K38/00C07D401/14C07K5/06C07K5/065
CPCA61K38/00C07K5/06191C07K5/06078C07D401/14
Inventor TRUNK, MICHAELWEILER, CLAUDIUS
Owner BOEHRINGER INGELHEIM PHARMA GMBH & CO KG
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