ArticlePolymers2021
Design and Evaluation of Losartan Potassium Effervescent Floating Matrix Tablets: In Vivo X-ray Imaging and Pharmacokinetic Studies in Albino Rabbits.
Article in Polymers, 2021. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 15 papers.
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Who cites it
15 citing papers in PubMed, 30 citations in OpenAlex.
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- Development and characterization of gastro-floating sustained-release granules for enhanced bioavailability of patchouli oil.Heliyon · 2024Article
- Expanding the Manufacturing Approaches for Gastroretentive Drug Delivery Systems with 3D Printing Technology.Pharmaceutics · 2024Review
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- Formulation and Preparation of Losartan-Potassium-Loaded Controlled-Release Matrices Using Ethocel Grade 10 to Establish a Correlation between In Vitro and In Vivo Results.Pharmaceutics · 2024Article
- Nanofabrication of Losartan Potassium Sustained Release Floating Microspheres using Different Grades of Ethyl Cellulose and its Insight on Release Profiles.Current pharmaceutical design · 2024Article
- Diltiazem Hydrochloride Floating Matrix Tablet: Formulation andCardiovascular & hematological disorders drug targets · 2024Article
- Design and evaluation ofDrug delivery · 2023Article
- Merging konjac glucomannan with other copolymeric hydrogels as a cutting-edge liquid raft system for dual delivery of etoricoxib and famotidine.Drug delivery · 2023Article
- Development of Computational In Silico Model for Nano Lipid Carrier Formulation of Curcumin.Molecules (Basel, Switzerland) · 2023Article
- Losartan Potassium and Verapamil Hydrochloride Compound Transdermal Drug Delivery System: Formulation and Characterization.International journal of molecular sciences · 2022Article
- Recent Progress on Modified Gum Katira Polysaccharides and Their Various Potential Applications.Polymers · 2022Review
- Preparation and Characterization of Hydrophilic Polymer Based Sustained-Release Matrix Tablets of a High Dose Hydrophobic Drug.Polymers · 2022Article
- Improved gastric residence time of famotidine by raft-forming drug delivery system using DOE.International journal of immunopathology and pharmacologyArticle
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Authors and funding
8 authors at 5 institutions in 2 countries.
Funding
Abstract
Losartan potassium (LP) is an angiotensin receptor blocker used to treat hypertension. At higher pH, it shows poor aqueous solubility, which leads to poor bioavailability and lowers its therapeutic effectiveness. The main aim of this research was to develop a direct compressed effervescent floating matrix tablet (EFMT) of LP using hydroxyl propyl methylcellulose 90SH 15,000 (HPMC-90SH 15,000), karaya gum (KG), and an effervescent agent, such as sodium bicarbonate (SB). Therefore, an EFMT has been developed to prolong the stomach residence time (GRT) of a drug to several hours and improve its bioavailability in the stomach region. The blended powder was evaluated for pre-compression characteristics, followed by post-compression characteristics, in vitro floating, water uptake studies, and in vitro studies. The optimized formulation of EFMT was investigated for in vivo buoyancy by X-ray imaging and pharmacokinetic studies in Albino rabbits. The results revealed that the parameters of pre- and post-compression were within the USP limits. All tablets showed good floating capabilities (short floating lag time <1 min and floated for >24 h), good swelling characteristics, and controlled release for over 24 h. The Fourier-transform infrared (FTIR) and differential scanning calorimetry (DSC) spectra showed drug-polymer compatibility. The optimized formulation F3 (HPMC-90SH 15,000-KG) exhibited non-Fickian diffusion and showed 100% drug release at the end of 24 h. In addition, with the optimized formulation F3, we observed that the EFMT floated continuously in the rabbit's stomach area; thus, the GRT could be extended to more than 12 h. The pharmacokinetic profiling in Albino rabbits revealed that the relative bioavailability of the optimized LP-EFMT was enhanced compared to an oral solution of LP. We conclude that this a potential method for improving the oral bioavailability of LP to treat hypertension effectively.
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