DETERMINATION OF TAMSULOSIN HYDROCHLORIDE RELEASE PHARMACOKINETICS IN PROSTATE GLAND BY A RADIOTRACER METHOD
DOI:
https://doi.org/10.14739/2310-1210.2013.5.18955Keywords:
suppositories, pharmacokinetics, α – adrenogenic blockersAbstract
Introduction: recently in Ukraine prostate diseases have taken one of the leading places among male urological pathologies. Prostate gland hyperplasia is one of the most common ones.
Causes of hyperplasia have not been reliably established so far, however, it has been proved that the poor state of androgen production in men is an integral condition for the development of benign prostatic hyperplasia.
One of the urgent tasks of modern pharmaceutical science is to create new high-performance drugs in such dosage forms that provide optimal therapeutic effect with minimal adverse complications.
Among a large number of drugs for the treatment of prostate diseases a prominent place is occupied by alpha-adrenoblockers – drugs of the first-line treatments that affect the α1А-adrenergic receptors, reduce or completely eliminate the muscle tone of the prostatic urethra and bladder neck.
Tamsulosin hydrochloride is a selective and competitive blocker of postsynaptic α1А-adrenergic receptors. The selectivity of tamsulosin to α1А-adrenergic receptors, which are located in the bladder, is 20 times greater than its ability to interact with α1В-adrenoceptors that are located in vascular smooth muscles.
Objective: to study the pharmacokinetics of tamsulosin hydrochloride release into prostate gland after oral and rectal administration by a radioactive-tracer technique.
Materials and methods of research: tamsulosin hydrochloride substance and suppositories with this substance labeled by 14С with a specific activity of 3.7× 107Bq/mg.
Pharmacokinetic studies of tamsulosin hydrochloride in the prostate were performed after oral and rectal administration. The experiments were carried out on white mature male rats of Wistar line weighing 210 ± 10 g.
Pharmacokinetic studies were performed using a radioactive-tracer technique (tracers) after oral and rectal administration of tamsulosin.
Results and their discussion: after rectal administration the release of tamsulosin hydrochloride is more complete and intensive compared to oral route of administration. Thus, the results of the experiment prove that the preparation reaches the prostate much faster, releases more completely and has a higher bioavailability.
Conclusions: the study of pharmacokinetics of tamsulosin hydrochloride accumulation in prostate gland after oral and rectal administration by a radioactive-tracer technique with the help of α-β-radiometer NRR-610 “Tesla” has been done. The research results proved the advantages of rectal route of drug administration compared with oral.
The obtained results confirm the expediency of creation of the medicinal preparation with alpha-adrenoblocker tamsulosin hydrochloride in the form of suppositories for prostate diseases treatment.
References
Варламова Н.В. Получение и медико-биологические испытания меченого технецием-99m норфлоксацина гидрохлорида / Н.В. Варламова, В.С. Скуридин и др. // Бюллетень сибирской медицины. – 2010. – №6. – С. 1–9.
Кодина Г.Е. Изотопы: свойства, получение, применение / Г.Е. Кодина. – М.: Физматлит, 2005. – С. 311–483.
Котенко К.В. Экспериментальное исследование биокинетики наночастиц оксида цинка у крыс после однократного перорального введения с использованием технологии меченых атомов / К.В. Котенко, И.К. Беляев и др. // Медицинская радиология и радиационная безопасность. – 2011. – Т. 56, №2. – С. 5–10.
Тиктинский О.Л. Андрология / О.Л. Тиктинский, С.Н. Калинина, В.В. Михайличенко. – М.: ООО «Медицинское информационное агентство», 2010. – С. 504–520.
Barry S.J. The development of human benign prostatic hyperplasia with age / Barry S.J., D.S. Coffey, P.C. Walsh etc. // J. Urol. – 2004. – Vol. 132. – P. 474–479.
Dong Z. Tamsulosin versus terazosin for benign prostatic hyperplasia: a systematic review / Dong Z., Wang Z., Yang K., Liu Y., Gao W., Chen W. // Syst Biol Reprod Med. – 2009. – Vol. 55, №4. – P. 129–136.
Narayan P. Long-term effi cacy and safety of tamsulosin for benign prostatic hyperplasia / Narayan P., Tunuguntla H.S. // Rev Urol. – 2005. – Vol. 7, Suppl 4. – P. 42–48.
Downloads
How to Cite
Issue
Section
License
Authors who publish with this journal agree to the following terms:- Authors retain copyright and grant the journal right of first publication with the work simultaneously licensed under a Creative Commons Attribution License that allows others to share the work with an acknowledgement of the work's authorship and initial publication in this journal.
- Authors are able to enter into separate, additional contractual arrangements for the non-exclusive distribution of the journal's published version of the work (e.g., post it to an institutional repository or publish it in a book), with an acknowledgement of its initial publication in this journal.
- Authors are permitted and encouraged to post their work online (e.g., in institutional repositories or on their website) prior to and during the submission process, as it can lead to productive exchanges, as well as earlier and greater citation of published work (See The Effect of Open Access)
