Novel Extended-Release Multiple-Unit System of Imidafenacin Prepared by Fluid-Bed Coating Technique
| Autor: | Young Wook Choi, Eun Seok Lee, Chang Hyun Kim, Myung Joo Kang, Taek Hwan Shin, Min Su Goh, Myoung Jin Ho, Sung Hyun Im |
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| Rok vydání: | 2018 |
| Předmět: |
Male
Polymers Chemistry Pharmaceutical Acrylic Resins Pellets Pharmaceutical Science 02 engineering and technology Aquatic Science Imidafenacin 030226 pharmacology & pharmacy Polyvinyl alcohol 03 medical and health sciences chemistry.chemical_compound Dogs Hypromellose Derivatives 0302 clinical medicine Differential scanning calorimetry Pharmacokinetics Drug Discovery medicine Animals Ecology Evolution Behavior and Systematics Chromatography Ecology Chemistry Imidazoles General Medicine 021001 nanoscience & nanotechnology Controlled release Antispasmodic Agent Drug Liberation Solubility Methacrylic acid Delayed-Action Preparations 0210 nano-technology Agronomy and Crop Science medicine.drug |
| Zdroj: | AAPS PharmSciTech. 19:2639-2645 |
| ISSN: | 1530-9932 |
| DOI: | 10.1208/s12249-018-1100-6 |
| Popis: | The objective of this study was to formulate once-a-day extended-release (ER) pellet system of imidafenacin (IDN), a recently approved urinary antispasmodic agent with twice-a-day dosing regimen. The sugar sphere pellets were firstly layered with IDN and hypromellose and then coated with Eudragit RS (copolymers of acrylic and methacrylic acid esters), employed as a release modifier, using a fluid-bed coater. Solid-state characterizations using solid-state X-ray diffraction and differential scanning calorimeter indicated that the antispasmodic agent was homogeneously layered onto the pellets in an amorphous state. Drug release from multiple-unit ER system was effectively retarded in proportion to the amount of Eudragit RS in the outer layer, with a high correlation value above 0.86. In a pharmacokinetic evaluation in beagle dogs, the plasma concentration profile of IDN was markedly protracted by ER pellets, exhibiting delayed the time needed to reach the maximum drug concentration and the elimination half-life in plasma, compared to the commercial immediate release form (Uritos® tablet, Kyorin Pharmaceutical Co., Ltd., Japan). Therefore, the novel ER pellets can be a promising tool for oral IDN therapy, providing a once-a-day dosing regimen, and thus, improving patient compliance. |
| Databáze: | OpenAIRE |
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