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

[0006] It is an object of the present invention to provide a dosage form for oral administration of POE 4 inhibitors whose solubility is slight, which form can be produced without great technical complexity, which takes account of the low solubility of the PDE 4 inhibitor whose solubility is slight, and which results in rapid, acceptable bioavailability of the POE 4 inhibitor whose solubility is slight, so as to attain serum levels which are required in order to obtain the desired pharmacological effect quickly without side effects becoming manifest.

[0007] It has now been found, surprisingly, that this object can be achieved by a dosage form for oral administration of a PDE 4 inhibitor whose solubility is slight, employing polyvinylpyrrolidone (PVP) as binder for the dosage form. Compared with dosage forms in which no PVP is employed as binder, the dosage form of the invention shows distinctly improved pharmacokinetic properties. Thus, in particular in relation to the bioavailability of the PDE 4 inhibitor whose solubility is slight, a faster absorption and thus faster onset of the pharmacological effect is observed with the dosage forms of the invention compared with dosage forms without PVP. The oral dosage form of the invention is preferably a solid dosage form in tablet or pellet form. It is preferably a solid oral dosage form with immediate release of the active ingredient (immediate release solid oral dosage form).

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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