Controlled Release of Tamsulosin from Nanopore-Forming Granules

doi:10.4333/KPS.2006.36.1.039

Paper

Controlled Release of Tamsulosin from Nanopore-Forming Granules

Published 2006 · Seong-Mi Seo, Hyun-Suk Lee, Jaehwi Lee

Journal of Pharmaceutical Investigation

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3

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0

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Abstract

Tamsulosin or a salt thereof such as its hydrochloride salt has been known to have an adrenaline receptor blocking action for urethra and prostate areas. It has been widely used as a drug which lowers the prostate pressure and improves urinary disturbance accompanied by prostate-grand enlargement, thus for the treatment of prostatic hyperplasia. To avoid dose-dependent side effects of tamsulosin upon oral administration, the development of sustained-release delivery system is essentially required, that can maintain therapeutic drug levels for a longer period of time. The aim of this study was therefore to formulate sustained-release tamsulosin granules and assess their formulation variables. We designed entric coated sustained-release tamsulosin granules for this purpose. Nano-pores in the outer controlled release membrane were needed in order to obtain initial tamsulosin release even in an acidic environment such as gastric region. In our sustained release osmotic granule system, hydroxypropylmethylcellulose in a drug-containing layer was used as a rate controller. The drug-containing granules were coated with hydroxypropylmethylcellulose phthalate (HPMCP) and Eudragit, along with glycerol triacetate as an aqueous nano-pore former. The release of tamsulosin depended heavily on the type of Eudragit such as RS, RL, NE 30D, used in the formulation of controlled release layer. These results obtained clearly suggest that the sustained-release oral delivery system for tamsulosin could be designed with satisfying drug release profile approved by the Korean Food and Drug Administration.

Study Snapshot

Sustained-release tamsulosin granules with nanopores can effectively maintain therapeutic drug levels for longer periods, reducing dose-dependent side effects.

PopulationOlder adults (50-71 years)

Sample size24

MethodsObservational

OutcomesBody Mass Index projections

ResultsSocial networks mitigate obesity in older groups.

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Paper

Controlled Release of Tamsulosin from Nanopore-Forming Granules

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References

Tamsulosin

Tamsulosin has high affinities to 1L -adrenoceptor subtypes in bovine prostate and rat hearts, suggesting an inhibitory effect on prostate contraction.

Antagonistic activity of tamsulosin against human vascular α1‐adrenergic receptors

Tamsulosin hydrochloride effectively inhibits 1Aadrenergic receptors in human blood vessels, with higher doses causing greater inhibition.

Minimally invasive alternative therapeutic options for lower urinary tract symptoms.

Minimally invasive techniques show promise for alleviating lower urinary tract symptoms, but their long-term durability and effectiveness need further large-scale controlled trials.

Overview of α-Blocker Therapy for Benign Prostatic Hyperplasia

-blockers are the most common treatment for benign prostatic hyperplasia, but may have significant cardiovascular side effects.

Adrenergic and cholinergic receptors in the human prostate, prostatic capsule and bladder neck.

Alpha-adrenergic receptor over-stimulation in the prostatic capsule may cause acute urine retention in prostatic patients, supporting the contraindication to cholinergic drugs for retention.

Prazosin concentration monitoring in the treatment of prostatic adenoma

Optimal dosage of Minipress (prazosin) in long-term therapy for benign prostatic hyperplasia can be achieved through monitoring of drug plasma levels.

Citations

Formulation and Evaluation of Sustained Release Extrudes Prepared via Novel Hot Melt Extrusion Technique

Hot-melt extrusion technique (HMET) effectively creates sustained release extrudes for highly dosed, freely soluble drugs, with venlafaxine hydrochloride retaining its crystalline nature and being homogeneously dispersed throughout the polymer matrix.

Development and optimization of a novel oral controlled delivery system for tamsulosin hydrochloride using response surface methodology.

The novel oral controlled-release system for tamsulosin hydrochloride developed using HPMC and HPMCP as coating additives in Surelease aqueous ethylcellulose dispersion successfully achieved a controlled-release pattern.

Optimization of tamsulosin hydrochloride controlled release pellets coated with Surelease and neutralized HPMCP

Optimizing tamsulosin hydrochloride controlled release pellets with a 3:1 ratio of Surelease to neutralized HPMCP and 20% coating level using a full factorial 32 design and optimization technique can successfully achieve controlled release drug delivery.