Physicochemical, pharmacokinetic, and pharmacodynamic characterization of isradipine tablets for controlled release

Venkatesh, D. Nagasamy; Meyyanathan, S. N.; Shanmugam, R.; Kamatham, Srinivas Sumanth; Campos, J.; Dias-Ferreira, João; Cardoso, Juliana Cordeiro; Severino, Patrícia; Souto, Eliana B.

doi:10.1080/10837450.2020.1839495

Cited by 5 publications

(6 citation statements)

References 56 publications

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“…Avicel PH 101, magnesium stearate, and talc were added to the granules to obtain a blend that was compressed on a 10-station rotation tablet machine of 12 mm concave punches (Rimek, Ahmedabad, India). The compression force was kept constant at 9000 N [ 16 ]. The composition of the final tablets is given in Table 7 .…”

Section: Methodsmentioning

confidence: 99%

“…The Carr’s compressibility index (%) of the granules ( Table 6 ) was calculated as previously described [ 16 ] and using the following Equation (8):

…”

Section: Methodsmentioning

confidence: 99%

“…The resulting tablets were dedusted and reweighed. The friability was calculated as the percentage of weight loss using the following Equation (10) [ 16 ]:

…”

Section: Methodsmentioning

confidence: 99%

“…In this case, drug release is controlled by the hydration of HPMC. A gelatinous layer at the matrix surface, through which the loaded drug diffuses, is created [ 16 ].…”

Section: Introductionmentioning

confidence: 99%

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Effect of Hydrophilic Polymers on the Release Rate and Pharmacokinetics of Acyclovir Tablets Obtained by Wet Granulation: In Vitro and In Vivo Assays

Venkatesh

S.N.Meyyanathan²,

Kovačević³

et al. 2022

Molecules

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This study aims to evaluate the feasibility of producing acyclovir-containing modified release matrix tablets by a wet granulation method based on the type and concentration of two pharmaceutical-grade hydrophilic matrix polymers (i.e., hydroxypropyl methylcellulose (HPMC), carbomers, and their combinations) commonly used in biomedical applications. The mechanical properties of the tablets and in vitro and in vivo performance were studied. The physicochemical properties of the raw materials and corresponding physical mixtures were characterized by differential scanning calorimetry, showing that the hydrophilic polymers did not influence the physicochemical properties of the drug. The wet granulation process improved the flow and compression properties of the obtained granules. This method enabled the preparation of the matrix tablets of acyclovir with appropriate mechanical properties concerning hardness and friability. The drug release kinetics was governed by the type and concentration of the hydrophilic polymers composing the matrices. The study has proven that HPMC-composed tablets were superior in modified drug release properties compared to carbomer- and HPMC/carbomer-based tablets. Mathematical analysis of the release profiles, determined in a medium adjusted to pH 1.2 followed by pH 7.4, revealed that the drug released from the hydrophilic tablets followed non-Fickian first-order kinetics. An optimal HPMC-based formulation submitted to accelerated stability studies (40 °C, 75% RH) was stable for three months. A complete cross-over bioavailability study of the selected acyclovir-loaded sustained release tablets and marketed immediate-release tablets were compared in six healthy male volunteers. The extent of drug absorption from the sustained release tablets was significantly greater than that from immediate-release pills, which may improve the drug’s antiviral properties attributed to the lower elimination rate and enhanced acyclovir half-life.

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Section: Methodsmentioning

confidence: 99%

“…The Carr’s compressibility index (%) of the granules ( Table 6 ) was calculated as previously described [ 16 ] and using the following Equation (8):

…”

Section: Methodsmentioning

confidence: 99%

“…The resulting tablets were dedusted and reweighed. The friability was calculated as the percentage of weight loss using the following Equation (10) [ 16 ]:

…”

Section: Methodsmentioning

confidence: 99%

“…In this case, drug release is controlled by the hydration of HPMC. A gelatinous layer at the matrix surface, through which the loaded drug diffuses, is created [ 16 ].…”

Section: Introductionmentioning

confidence: 99%

See 2 more Smart Citations

Effect of Hydrophilic Polymers on the Release Rate and Pharmacokinetics of Acyclovir Tablets Obtained by Wet Granulation: In Vitro and In Vivo Assays

Venkatesh

S.N.Meyyanathan²,

Kovačević³

et al. 2022

Molecules

Self Cite

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“…Furthermore, the duration required for the tablet to completely dissolve was monitored and recorded as an integral component of the experiment. [23][24] In vitro dissolution studies:…”

Section: Pharmaceutical Informationmentioning

confidence: 99%

"Development And Assessment of Immediate Release Nitrofurantoin Tablet and Sustained Release Trimethoprim Tablet: Formulation, Characterization and Comparative Evaluation"

Kute,

Singh

2023

ijmst

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The research includes an examination of material properties, an investigation into the compatibility of the drug and excipients, the development of analytical techniques, and the determination of tablet production methods for immediate and sustained release layers. The methodology for material characterization encompassed the analysis of the pharmaceuticals' solubility in various aqueous solutions and buffers. The evaluation of the compatibility between excipients and medications was conducted utilizing FT-IR spectroscopy. Furthermore, calibration curves were devised by the research team for Nitrofurantoin and Trimethoprim, enabling the quantification of these pharmaceutical substances via UV spectrophotometry. The preparation of the tablets involved the utilization of direct compression and moist granulation methods, respectively, for the immediate and sustained release layers. This required the application of a variety of excipients and polymers. The tablets underwent a thorough evaluation in a controlled laboratory environment, which encompassed assessments of their dimensions, resistance to deformation, mass variability, and susceptibility to fracturing, concentration of active component, breakdown time, and solubility. The findings demonstrated that the regression coefficients in the calibration curves were substantial, thereby validating the accuracy of the drug concentration estimations. The results of the solubility studies indicate that Nitrofurantoin becomes more soluble in acidic environments. However, it should be noted that the solubility of both Trimethoprim and Nitrofurantoin is influenced by various solvents and buffers. An investigation into the compatibility of pharmaceuticals and the excipients was conducted through the utilization of FT-IR spectroscopy to ascertain such compatibility or interaction. A micromeritics analysis of granule flow parameters unveiled batch-specific variations in flow characteristics which will impact the manufacturing procedure. Upon scrutinizing the tablets, discrepancies in multiple measurements were discovered among various samples, suggesting the possibility of atypical tablet characteristics. Nitrofurantoin and Trimethoprim exhibited a progressive release from their tablets over time in various samples, as indicated by the drug release profiles observed in vitro; this suggests that the tablets have distinct release kinetics. Nevertheless, the medication release data exhibited irregularities in its presentation, such as sporadic inputs, absent values, and potentially erroneous statistics. The presence of these inconsistencies has the potential to compromise the dependability and comprehension of the results. In brief, the research provides extensive knowledge regarding the development, examination, and assessment of Nitrofurantoin rapid release tablets and Trimethoprim sustained release tablets.

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A review on 1,4-dihydropyridines as anti-tuberculosis agent

Jindal

Sohal

Malhi

2022

Materials Today: Proceedings

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Physicochemical, pharmacokinetic, and pharmacodynamic characterization of isradipine tablets for controlled release

Cited by 5 publications

References 56 publications

Effect of Hydrophilic Polymers on the Release Rate and Pharmacokinetics of Acyclovir Tablets Obtained by Wet Granulation: In Vitro and In Vivo Assays

Effect of Hydrophilic Polymers on the Release Rate and Pharmacokinetics of Acyclovir Tablets Obtained by Wet Granulation: In Vitro and In Vivo Assays

"Development And Assessment of Immediate Release Nitrofurantoin Tablet and Sustained Release Trimethoprim Tablet: Formulation, Characterization and Comparative Evaluation"

A review on 1,4-dihydropyridines as anti-tuberculosis agent

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