Comparative in vitro dissolution and in vivo bioequivalence of two diclofenac enteric coated formulations

Basmenji, S.; Valizadeh, Hadi; Zakeri–Milani, Parvin

doi:10.1055/s-0031-1300554

Cited by 3 publications

(2 citation statements)

References 27 publications

Supporting

Mentioning

Contrasting

Order By: Relevance

“…shedding of L-selectin has been demonstrated not only in vivo in both humans and mice [5,11], but also in vitro, where the concentration of NSAIDs required to induce L-selectin shedding in human neutrophils [5,12] are within the range (micromolars) reached in plasma by oral administration of NSAIDs in humans [49,50].…”

Section: Inhibition Of Cell Adhesion By Nsaidsmentioning

confidence: 99%

NSAIDs: Learning new tricks from old drugs

Dı́az-González

Sánchez-Madrid

2015

Eur J Immunol

View full text Add to dashboard Cite

Nonsteroidal anti-inflammatory drugs (NSAIDs) comprise a heterogeneous group of pharmacological agents used for the symptomatic treatment of fever, pain, and inflammation. Although the main mechanism of action of NSAIDs consists of inhibiting prostaglandin synthesis by blocking the enzyme cyclooxygenase (COX), clinical, and experimental data strongly indicate the existence of additional mechanisms. Some of the COX-independent effects are related to the ability of NSAIDs to penetrate biological membranes and disrupt important molecular interactions necessary for a wide array of cellular functions, including cell adhesion. These effects, in particular those that interfere with L-selectin function in neutrophils during the inflammatory response, may contribute to the antiinflammatory properties that NSAIDs exert in vivo. Recent contributions in this field have shown that the anti-L-selectin effect of NSAIDs is related to the NADPH-oxidasedependent generation of superoxide anion at the plasma membrane. These findings might represent a novel approach for developing new and effective anti-inflammatory compounds with a better safety profile than the currently available NSAIDs.Keywords: L-selectin r Non-steroidal anti-inflammatory drugs r NADPH oxidase IntroductionNonsteroidal anti-inflammatory drugs (NSAIDs) are a heterogeneous group of therapeutic agents widely used for the symptomatic treatment of rheumatic disorders. Since the early seventies of last century, it has been widely accepted that the main mechanism of action of these compounds, which is also responsible for the main side effect of gastric mucosal damage, is inhibition of cyclooxygenase (COX), a key enzyme in prostaglandin synthesis [1]. Prostaglandins are group of hormone-like lipid compounds with a wide variety of strong physiological effects, including regulation of inflammation, pain sensitization, and platelet aggregation, among many others. However, a growing body of evidence suggests that NSAIDs have additional anti-inflammatory properties (reviewed in [2]). Some of these effects appear to be related to the ability of NSAIDs to penetrate biological membranes, as evaluated in vitro using membrane mimetic models, cell cultures, Correspondence: Prof. Federico Díaz-González e-mail: federico.diaz.gonzalez@gmail.com and molecular dynamic simulation systems [3,4], where they disrupt normal signaling events and modify important processes necessary for cellular function, including cell adhesion [5,6].The ability of NSAIDs to interfere with either cell adhesion, for example, by cleavage of epithelial cell adhesion molecule protein on tumor cells [6], or with leukocyte adhesion pathways essential for the inflammatory response, such as causing L-selectin shedding on neutrophil [5], has been described. Interestingly, this antiadhesive effect of NSAIDs has also been shown to influence platelet adhesion, and it has been suggested that coagulation, hemostasis, and thrombus formation could be modulated by these compounds independently of the release of proinflammat...

show abstract

Section: Inhibition Of Cell Adhesion By Nsaidsmentioning

confidence: 99%

NSAIDs: Learning new tricks from old drugs

Dı́az-González

Sánchez-Madrid

2015

Eur J Immunol

View full text Add to dashboard Cite

show abstract

“…Many authors have evaluated the influence of different formulations on physical, chemical and pharmacokinetic parameters of drugs and came to the conclusion that in vitro/in vivo correlation exists, [8][9][10] although other authors have claimed that such studies are not warranted. 11,12 Accordingly, the aim of this study was to evaluate the correlation.…”

Section: Introductionmentioning

confidence: 99%

Bioequivalence trial of Diclofenac sodium tablets: Effects of Eudragit and tablet preparation, formulation characterization, release profiles, and bioavailability measurements

Kecman¹,

Jokanovic²

2018

PONS

View full text Add to dashboard Cite

Objective. The study was aimed to evaluate the effects of changing excipients, including type of Eudragit polymer, on release and absorption profiles in vitro and in vivo, of tablets containing the antiinflammatory drug, diclofenac sodium. Methods. Formulation 1 consisted of diclofenac sodium tablets containing Eudragit L30, and Formulation 2 consisted of diclofenac sodium tablets containing Eudragit L100, and both formulations contained different excipients. Tablets were assessed, in vitro, for weight, hardness, diameter, thickness, mass uniformity, disintegration and dissolution profiles and drug content. Tablets were also assessed in vivo by gavage in healthy rabbits and assessing diclofenac sodium plasma concentrations and pharmacokinetic parameters. Results. Results showed that in vitro analyses demonstrated non-equivalence while in vivo analyses demonstrated equivalence. This suggests that although different types of Eudragit and excipients modulated the in vitro dissolution and release profiles of diclofenac sodium, in vivo absorption in rabbits remained similar representing bioequivalence. Conclusion. It is needed to conduct evaluations of bioequivalence of diclofenac sodium oral preparations at both in vitro and in vivo conditions.

show abstract

Single Dose Bioequivalence Study of Two Brands of Olanzapine 10 mg Tablets in Iranian Healthy Volunteers

et al. 2013

View full text Add to dashboard Cite

This single dose, randomized, open label, 2-period and crossover study in healthy Iranian adult volunteers was conducted to compare the bioavailability of 2 branded formulations of olanzapine 10 mg tablets. 24 volunteers received one tablet of each olanzapine 10 mg formulation. Drugs were administered after a 12 h overnight fast in each of 2 treatment days which separated by a 2-week washout period. Serial blood samples were collected over a period of 72 h. Plasma was analyzed using a validated high performance liquid chromatography method with ultraviolet detection in the range of 2-24 ng/mL with a lower limit of quantitation of 1.25 ng/mL. A non-compartmental method was employed to determine the pharmacokinetic properties (Cmax, Tmax, AUC0-t, AUC0-∞ and T1/2) to test to bioequivalence. Cmax, AUC0-t and AUC0-∞ were used to test the bioequivalence after log-transformation of plasma data. The mean (SD) Cmax, AUC0-t and AUC0-∞ for the test formulation were 15.82 (3.15) ng/mL, 447.19 (100.64) ng.h/L and 570.75 (130.55) ng.h/L respectively. Corresponding values for the test formulation were 15.72 (4.25) ng/mL, 440.37 (98.75) ng.h/mL and 558.66 (129.57) ng.h/mL. For test formulation vs. the reference formulation, the 90% CIs of the least squares mean test/reference ratios of Cmax, AUC0-t and AUC0-∞ were 97.6-110.0%, 96.4-109.4% and 97.3-109.2%. In these volunteers, based on the FDA regulatory definition, results from the pharmacokinetic analysis suggested that the test and reference formulations of olanzapine 10 mg tablets were bioequivalent.

show abstract

Comparative in vitro dissolution and in vivo bioequivalence of two diclofenac enteric coated formulations

Cited by 3 publications

References 27 publications

NSAIDs: Learning new tricks from old drugs

NSAIDs: Learning new tricks from old drugs

Bioequivalence trial of Diclofenac sodium tablets: Effects of Eudragit and tablet preparation, formulation characterization, release profiles, and bioavailability measurements

Single Dose Bioequivalence Study of Two Brands of Olanzapine 10 mg Tablets in Iranian Healthy Volunteers

Contact Info

Product

Resources

About