Oral dosage form containing a PDE 4 inhibitor as an active ingredient and polyvinylpyrrolidone as excipient

Abstract

Dosage forms for oral administration of a PDE4 inhibitor whose solubility is slight are described. They contain PVP as a binder.

Description

TECHNICAL FIELD [0001] The present invention relates to the field of pharmaceutical technology and describes a dosage form for oral administration of a PDE 4 inhibitor as active ingredient in tablet or pellet form for treating diseases such as asthma or airway obstructions. The invention additionally relates to processes for producing the dosage form. PRIOR ART [0002] Cyclic nucleotide phosphodiesterase (PDE) inhibitors (specifically of type 4) are currently of special interest as a new generation of active ingredients for treating inflammatory disorders, especially inflammations of the airways such as asthma or airway obstructions (such as, for example, COPD=chronic obstructive pulmonary disease). A number of PDE 4 inhibitors is currently undergoing advanced clinical testing. [0003] In WO00 / 50011 and WO01 / 32165, which relate to dosage forms with controlled or sustained delivery of a PDE 4 inhibitor, it is pointed out that unwanted CNS side effects may become manifest on delivery of...

AI Technical Summary

Benefits of technology

The use of PVP in the dosage form improves bioavailability and absorption rates of PDE 4 inhibitors with low solubility, achieving required serum levels quickly while minimizing side effects.

Problems solved by technology

However, production of dosage forms with controlled or sustained release of slightly soluble active ingredients may be technically complicated, reference being made thereto for example in U.S. Pat. No. 5,286,494.

With medicinal substances which are slightly soluble in water, therefore, the bioavailability is frequently limited by the solubility or rate of dissolution.

This makes it very difficult to produce suitable dosage forms.

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