Chemical-pharmaceutical analysis of original and generic tamsulosin preparations

Drugs based on a1-adrenergic blockers are currently used as a first line of treatment for lower urinary tract symptoms (LUTS). Blockage of a1a-adrenergic receptors leads to relaxation of smooth muscles in prostatic stroma which leads to a decrease in obstruction symptoms. Tamsulosin blocks a1a- and α1d-adrenergic receptors, which allows it to effectively diminish all LUTS, while circulatory adverse events are rare because of its low activity towards α1b-adrenergic receptors. However, therapeutic efficacy of drugs belonging to this group is possible only when required serum drug concentration is reached and maintained for a necessary period of time. These characteristics are defined by properties of a pharmaceutical form no less, or sometimes even more than by properties of an active ingredient itself. They are influenced by a choice of excipients which define drug release profile. Properties of a pharmaceutical form may radically change after substitution of one excipient by another, after substitution of solvent used for this pharmaceutical form, due to altered temperature regimen without following optimization of composition or manufacturing flaws...