Improved Pharmacokinetics of Aceclofenac Immediate Release Tablets Incorporating ist Inclusion Complex with Hydroxypropyl-β-Cyclodextrin

Abstract

The present investigation reports the various pharmacokinetic parameters of immediate release aceclofenac tablets incorporating its inclusion complex with hydroxypropyl-β-cyclodextrin. The tablets were prepared using aceclofenac: hydroxypropyl-β-cyclodextrin in a 1:1 molar ratio by the direct compression method (TKN). The results were compared with those of the marketed brand (MKT) and pure drug (TAC). The P-values indicated that mean plasma concentrations were significantly different among all three formulations administered (P<0.05, P<0.01). TKN showed significantly higher plasma levels when compared to the pure drug (P<0.01). The C max and AUC (0-∞) of TKN were significantly higher (P<0.05) compared to the pure drug and marketed formulation. Furthermore, the first-order overall elimination rate constant (K el ) of TKN was also significantly higher (P<0.05) compared to the pure drug and its marketed formulation. These results suggested that tablets prepared by incorporating the AC-HPβCD inclusion complex (TKN) would provide a more rapid onset of pharmacological effects in comparison to the marketed formulation and pure drug.

Optimization of Statistically Designed Aceclofenac Fast Dissolving Tablets Employing Starch Glutamate as a Novel Superdisintegrant

“…Pharmacokinetic studies revealed that the optimized formulation (F2) of aceclofenac fast dissolving tablets reached peak plasma concentration in less time (1 sec) and with increased absorption and relative bioavailability (182.77) when compared to pure drug. These results were in agreement with the results obtained by Dahiya et al [21]. Summary of pharmacokinetic parameters was shown in table 8.…”

Natural Bioactive Thiazole-Based Peptides from Marine Resources: Structural and Pharmacological Aspects

“…Approximately 40% of existing small molecules and 70% of new candidates under development pipelines suffer from the low solubility problem, which is a major reason for their suboptimal drug delivery as well as failures in their development process. Approaches such as cyclodextrin complexation and solid dispersions have been employed to address this challenge and recommend the better formulation over their existing dosage forms [193][194][195][196][197][198]. Likewise, peptides, being biomacromolecules, also exhibit various challenges such as limited water solubility, stability aspects, as well as structural and synthesis complexities, limiting their full exploitation in drug development [199,200].…”

Pharmacokinetics and bioequivalence assessment of optimized directly compressible Aceclofenac (100 mg) tablet formulation in healthy human subjects

“…Henceforth, commonly recommended by the physicians of Asian and European countries [12]. Aceclofenac is a BCS (Biopharmaceutics Class System) class II drug with the log partition coefficient value of 2.170 [13]. The daily recommended dose of aceclofenac in an adult is 100 mg twice daily, necessitating adjustment of doses in hepatic impairments [10].…”