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Fulltext Comparative bioavailability study of a generic sustained release diclofenac sodium tablet

Magosso E, Yuen KH, Choy WP, Ling SSN, Ng BH, Ur-Rahman N, et al.

Med J Malaysia, 2004 Aug;59(3):352-6.
PMID: 15727381

The bioavailability of a generic diclofenac sodium sustained release tablet preparation (Zolterol, SR) was compared with the innovator product, Voltaren, SR. Twelve healthy adult male volunteers participated in the study, which was conducted according to a randomized, two-way crossover design with a wash out period of one week. The bioavailability of diclofenac was compared using the parameters area under the plasma concentration-time curve (AUC(0-infinity)), peak plasma concentration (Cmax) and time to reach peak plasma concentration (Tmax). No statistically significant difference was observed for both logarithmically transformed AUC(0-infinity), Cmax values and Tmax value of the two preparations.

Matched MeSH terms: Anti-Inflammatory Agents, Non-Steroidal/pharmacokinetics*
Bioequivalence assessment of two enteric-coated aspirin brands, Nu-Seals and Loprin, after a single oral dose of 150 mg in healthy male adults

Bukhari NI, Zafar A, Shamsi Wu, Bashir MA, Mirza AA

Therapie, 2005 Mar-Apr;60(2):167-73.
PMID: 15969319

AIM: The bioequivalence of aspirin from two enteric-coated brands, Nu-seals and Loprin, identified as the reference (R) and test (T) products, respectively, was assessed.

METHODS: A two-period randomised crossover design with a washout interval of 15 days was used in this study. The study results were determined in 16 healthy volunteers, all males with ages ranging from 19-28 (23.33 +/- 3.74) years and bodyweights of 52-92 (65.89 +/- 11.39) kg. After oral ingestion of 150mg of the either brand with 200 mL of water, serial blood samples were obtained over a period of 24 hours. Plasma, harvested from blood was analysed for the concentration of salicylic acid, a deacetylated metabolite of aspirin, by a validated high performance liquid chromatography (HPLC) method. Pharmacokinetic parameters were determined for both formulations by an interactive computer-assisted PK II procedure. A general linear model for repeated measures and 90% confidence intervals (CI) was employed to assess the sequence of treatment effects and to exclude differences between the parameters due to the product and period of administration, respectively.

RESULTS: The observed 90% CI ratios (Loprin/Nu-seals) for peak concentration, time to reach the peak and area under the plasma-concentration time curve from zero to infinity of 1.03,1.08; 1.04,1.05 and 1.01,1.15, respectively, were within the bioequivalence range (0.80,1.25) stipulated by the US Food and Drug Administration.

CONCLUSION: On the basis of the findings, the test (Loprin) and reference drug (Nu-seals) were deemed bioequivalent.

Matched MeSH terms: Anti-Inflammatory Agents, Non-Steroidal/pharmacokinetics*
Formulation of diclofenac for dermal delivery

Goh CF, Lane ME

Int J Pharm, 2014 Oct 1;473(1-2):607-16.
PMID: 25091375 DOI: 10.1016/j.ijpharm.2014.07.052

Diclofenac (DF) was first synthesized in the 1960's and is currently available as ophthalmic, oral, parenteral, rectal and skin preparations. This review focuses on the administration of DF to the skin. As a member of the non-steroidal anti-inflammatory (NSAID) group of drugs the primary indications of DF are for the management of inflammation and pain but it is also used to treat actinic keratosis. The specific aims of this paper are to: (i) provide an overview of the pharmacokinetics and metabolism of DF following oral and topical administration; (ii) examine critically the various formulation approaches which have been investigated to enhance dermal delivery of DF; and (iii) identify new formulation strategies for enhanced DF skin penetration.

Matched MeSH terms: Anti-Inflammatory Agents, Non-Steroidal/pharmacokinetics
Effects of microwave on drug-release responses of spray-dried alginate microspheres

Mardziah RE, Wong TW

Drug Dev Ind Pharm, 2010 Oct;36(10):1149-67.
PMID: 20380595 DOI: 10.3109/03639041003695063

Microspheres prepared from rigid guluronic acid- (MG) and flexible mannuronic acid-rich (MC) alginate will undergo different drug release changes with respect to the influence of microwave on the matrix. An in-depth understanding of their differences in drug release changes is attainable through investigating cross-linking agent-free alginate microspheres prepared by spray-drying technique.

Matched MeSH terms: Anti-Inflammatory Agents, Non-Steroidal/pharmacokinetics
Development of gelatin microspheres loaded with diclofenac sodium for intra-articular administration

Saravanan M, Bhaskar K, Maharajan G, Pillai KS

J Drug Target, 2011 Feb;19(2):96-103.
PMID: 20380621 DOI: 10.3109/10611861003733979

We have previously reported on the targeting of diclofenac sodium in joint inflammation using gelatin magnetic microspheres. To overcome complications in the administration of magnetic microspheres and achieve higher targeting efficiency, the present work focuses on the formulation of gelatin microspheres for intra-articular administration. Drug-loaded microspheres were prepared by the emulsification/cross-linking method, characterized by drug loading, size distribution, scanning electron microscopy (SEM), Fourier transform infrared (FT-IR) spectroscopy, differential scanning calorimetry (DSC), X-ray diffraction (XRD), gas chromatography, and in vitro release studies. The targeting efficiency of microspheres was studied in vivo in rabbits. The microspheres showed drug loading of 9.8, 18.3, and 26.7% w/w with an average size range of 37-46 µm, depending upon the drug-polymer ratio. They were spherical in nature and free from surface drug as evidenced by the SEM photographs. FT-IR, DSC, and XRD revealed the absence of drug-polymer interaction and amorphous nature of entrapped drug. Gas chromatography confirms the absences of residual glutaraldehyde. The formulated microspheres could prolong the drug release up to 30 days in vitro. About 81.2 and 43.7% of administered drug in the microspheres were recovered from the target joint after 1 and 7 days of postintra-articular injection, respectively, revealing good targeting efficiency.

Matched MeSH terms: Anti-Inflammatory Agents, Non-Steroidal/pharmacokinetics
Gamma-scintigraphic study of the gastrointestinal transit and in vivo dissolution of a controlled release diclofenac sodium formulation in xanthan gum matrices

Billa N, Yuen KH, Khader MA, Omar A

Int J Pharm, 2000 May 15;201(1):109-20.
PMID: 10867269

A xanthan gum matrix controlled release tablet formulation containing diclofenac sodium was evaluated in vitro and was found to release the drug at a uniform rate. The gastrointestinal transit behaviour of the formulation as determined by gamma scintigraphy, using healthy male volunteers under fasted and fed conditions, indicated that gastric emptying was delayed with food intake. In contrast, the small intestinal transit remained practically unchanged under both food statuses. Therefore, the delay in caecal arrival observed in the fed state can be attributed to the delay in gastric emptying. Rate of diclofenac sodium absorption was generally higher in the fed state compared to the fasted state, however the total amount absorbed under both food statuses remained practically the same. The rate of in vivo dissolution of the drug in the fed state was faster compared to that in the fasted state. Thus, at the time of caecal arrival, in vivo dissolution was complete in the fed state, unlike in the fasted state, where almost 60% of the drug was delivered to the colon.

Matched MeSH terms: Anti-Inflammatory Agents, Non-Steroidal/pharmacokinetics*
Development and In Vitro Evaluation of Aceclofenac Buccal Film

Almurisi SH, Mohammed A, Qassem F, Jehad H, Jassim A, Al-Japairai K, et al.

Curr Drug Discov Technol, 2024;21(3):46-55.
PMID: 37807409 DOI: 10.2174/0115701638262447230920061222

AIM: This study aimed to formulate and characterize aceclofenac buccal film formulations made of different polymers and evaluate the effects of polymer type on buccal film properties.
MATERIALS AND METHODS: Five polymer types, namely hydroxypropyl methylcellulose (HPMC), sodium carboxymethylcellulose (SCMC), polyvinyl alcohol (PVA), Eudragit S100, and Eudragit SR100, were used to prepare aceclofenac buccal film formulation either separately or combined by solvent-casting method. These formulations were evaluated in terms of physical appearance, folding test, film weight and thickness, drug content, percentage of elongation, moisture uptake, water vapor permeability, and in vitro drug release.
RESULTS: The addition of Eudragit polymer in most of the produced buccal films was unacceptable with low folding endurance. However, the dissolution profile of buccal films made from PVA and Eudragit SR100 provided a controlled drug release profile.
CONCLUSION: Buccal films can be formulated using different polymers either individually or in combination to obtain the drug release profile required to achieve a desired treatment goal. Furthermore, the property of the buccal films depends on the type and concentration of the polymer used.

Matched MeSH terms: Anti-Inflammatory Agents, Non-Steroidal/pharmacokinetics
Fulltext Topical piroxicam in vitro release and in vivo anti-inflammatory and analgesic effects from palm oil esters-based nanocream

Abdulkarim MF, Abdullah GZ, Chitneni M, Salman IM, Ameer OZ, Yam MF, et al.

Int J Nanomedicine, 2010 Nov 04;5:915-24.
PMID: 21116332 DOI: 10.2147/IJN.S13305

INTRODUCTION: During recent years, there has been growing interest in use of topical vehicle systems to assist in drug permeation through the skin. Drugs of interest are usually those that are problematic when given orally, such as piroxicam, a highly effective anti-inflammatory, anti-pyretic, and analgesic, but with the adverse effect of causing gastrointestinal ulcers. The present study investigated the in vitro and in vivo pharmacodynamic activity of a newly synthesized palm oil esters (POEs)-based nanocream containing piroxicam for topical delivery.
METHODS: A ratio of 25:37:38 of POEs: external phase: surfactants (Tween 80:Span 20, in a ratio 80:20), respectively was selected as the basic composition for the production of a nanocream with ideal properties. Various nanocreams were prepared using phosphate-buffered saline as the external phase at three different pH values. The abilities of these formulae to deliver piroxicam were assessed in vitro using a Franz diffusion cell fitted with a cellulose acetate membrane and full thickness rat skin. These formulae were also evaluated in vivo by comparing their anti-inflammatory and analgesic activities with those of the currently marketed gel.
RESULTS: After eight hours, nearly 100% of drug was transferred through the artificial membrane from the prepared formula F3 (phosphate-buffered saline at pH 7.4 as the external phase) and the marketed gel. The steady-state flux through rat skin of all formulae tested was higher than that of the marketed gel. Pharmacodynamically, nanocream formula F3 exhibited the highest anti- inflammatory and analgesic effects as compared with the other formulae.
CONCLUSION: The nanocream containing the newly synthesized POEs was successful for trans-dermal delivery of piroxicam.

Matched MeSH terms: Anti-Inflammatory Agents, Non-Steroidal/pharmacokinetics
Sunitinib-ibuprofen drug interaction affects the pharmacokinetics and tissue distribution of sunitinib to brain, liver, and kidney in male and female mice differently

Lau CL, Chan ST, Selvaratanam M, Khoo HW, Lim AY, Modamio P, et al.

Fundam Clin Pharmacol, 2015 Aug;29(4):404-16.
PMID: 26011058 DOI: 10.1111/fcp.12126

Tyrosine kinase inhibitor sunitinib (used in GIST, advanced RCC, and pancreatic neuroendocrine tumors) undergoes CYP3A4 metabolism and is an ABCB1B and ABCG2 efflux transporters substrate. We assessed the pharmacokinetic interaction with ibuprofen (an NSAID used by patients with cancer) in Balb/c male and female mice. Mice (study group) were coadministered (30 min apart) 30 mg/kg of ibuprofen and 60 mg/kg of sunitinib PO and compared with the control groups, which received sunitinib alone (60 mg/kg, PO). Sunitinib concentration in plasma, brain, kidney, and liver was measured by HPLC as scheduled and noncompartmental pharmacokinetic parameters estimated. In female control mice, sunitinib AUC0→∞ decreased in plasma (P < 0.05), was higher in liver and brain (P < 0.001), and lower in kidney (P < 0.001) vs. male control mice. After ibuprofen coadministration, female mice showed lower AUC0→∞ in plasma (P < 0.01), brain, liver, and kidney (all P < 0.001). However, in male mice, AUC0→∞ remained unchanged in plasma, increased in liver and kidney, and decreased in brain (all P < 0.001). The tissue-to-plasma AUC0→∞ ratio was similar between male and female control mice, but changed after ibuprofen coadministration: Male mice showed 1.6-fold higher liver-to-plasma ratio (P < 0.001) while remained unchanged in female mice and in kidney (male and female mice) but decreased 55% in brain (P < 0.05). The tissue-to-plasma partial AUC ratio, the drug tissue targeting index, and the tissue-plasma hysteresis-like plots also showed sex-based ibuprofen-sunitinib drug interaction differences. The results illustrate the relevance of this DDI on sunitinib pharmacokinetics and tissue uptake. These may be due to gender-based P450 and efflux/transporters differences.

Matched MeSH terms: Anti-Inflammatory Agents, Non-Steroidal/pharmacokinetics*
Designing novel bioconjugates of hydroxyethyl cellulose and salicylates for potential pharmaceutical and pharmacological applications

Abbas K, Amin M, Hussain MA, Sher M, Bukhari SNA, Jantan I, et al.

Int J Biol Macromol, 2017 Oct;103:441-450.
PMID: 28526350 DOI: 10.1016/j.ijbiomac.2017.05.061

This deals with fabrication of macromolecular prodrugs (MPDs) of salicylic acid (SA) and aspirin (ASP) based on a hydrophilic cellulose ether, hydroxyethyl cellulose (HEC). Degrees of substitution (DS) of SA and ASP per HEC repeating unit (HEC-RU) were achieved ranging from 0.60 to 2.18 and 0.53 to1.50, respectively. The amphiphilic HEC-SA conjugate 2 assembled into nanowire-like structures, while HEC-ASP conjugate 6 formed nanoparticles (diameter 300-00nm) at a water/DMSO interface. After oral administration in rabbit models, conjugates 2 and 6 showed plasma half-life of 6.96 and 7.01h with maximum plasma concentration (Cmax) of 15.27 and 23.01μg L-1, respectively, and each reached peak plasma concentration (tmax) at 4.0h. Immunomodulatory assays (interleukin 6 and tumor necrosis factor-α values) revealed that anti-inflammatory properties of SA and ASP were unaltered in conjugates. Swelling inhibition of 61 and 71% was observed for conjugates 2 and 6, respectively, in a carrageenan induced paw edema test. Cytotoxic profiling (MTT assay) showed that conjugates were safe for administration in the concentration range of 2-10mM up to 24h. Thermal analyses revealed that Tdm values of SA and ASP conjugates were increased by 99 and 154̊C, respectively, indicating extraordinary thermal stability imparted to drugs after MPD formation.

Matched MeSH terms: Anti-Inflammatory Agents, Non-Steroidal/pharmacokinetics
Fulltext In vitro permeation and in vivo anti-inflammatory and analgesic properties of nanoscaled emulsions containing ibuprofen for topical delivery

Abdullah GZ, Abdulkarim MF, Salman IM, Ameer OZ, Yam MF, Mutee AF, et al.

Int J Nanomedicine, 2011;6:387-96.
PMID: 21499428 DOI: 10.2147/IJN.S14667

As a topical delivery system, a nanoscaled emulsion is considered a good carrier of several active ingredients that convey several side effects upon oral administration, such as nonsteroidal anti-inflammatory drugs (NSAIDs).

Matched MeSH terms: Anti-Inflammatory Agents, Non-Steroidal/pharmacokinetics*
Carbopol 934, 940 and Ultrez 10 as viscosity modifiers of palm olein esters based nano-scaled emulsion containing ibuprofen

Abdullah GZ, Abdulkarim MF, Mallikarjun C, Mahdi ES, Basri M, Sattar MA, et al.

Pak J Pharm Sci, 2013 Jan;26(1):75-83.
PMID: 23261730

Micro-emulsions and sometimes nano-emulsions are well known candidates to deliver drugs locally. However, the poor rheological properties are marginally affecting their acceptance pharmaceutically. This work aimed to modify the poor flow properties of a nano-scaled emulsion comprising palm olein esters as the oil phase and ibuprofen as the active ingredient for topical delivery. Three Carbopol ® resins: 934, 940 and Ultrez 10, were utilized in various concentrations to achieve these goals. Moreover, phosphate buffer and triethanolamine solutions pH 7.4 were used as neutralizing agents to assess their effects on the gel-forming and swelling properties of Carbopol ® 940. The addition of these polymers caused the produced nano-scaled emulsion to show a dramatic droplets enlargement of the dispersed globules, increased intrinsic viscosity, consistent zeta potential and transparent-to-opaque change in appearance. These changes were relatively influenced by the type and the concentration of the resin used. Carbopol ® 940 and triethanolamine appeared to be superior in achieving the proposed tasks compared to other materials. The higher the pH of triethanolamine solution, the stronger the flow-modifying properties of Carbopol ® 940. Transmission electron microscopy confirmed the formation of a well-arranged gel network of Carbopol ® 940, which was the major cause for all realized changes. Later in vitro permeation studies showed a significant decrease in the drug penetration, thus further modification using 10% w/w menthol or limonene as permeation promoters was performed. This resulted in in vitro and in vivo pharmacodynamics properties that are comparably higher than the reference chosen for this study.

Matched MeSH terms: Anti-Inflammatory Agents, Non-Steroidal/pharmacokinetics
Absorption of andrographolides from Andrographis paniculata and its effect on CCl(4)-induced oxidative stress in rats

Akowuah GA, Zhari I, Mariam A, Yam MF

Food Chem Toxicol, 2009 Sep;47(9):2321-6.
PMID: 19540299 DOI: 10.1016/j.fct.2009.06.022

A simple and validated high-performance liquid chromatography (HPLC) method with UV detection has been used to determine the content of andrographolide (AP) and 14-deoxy-11,12-didehydroandrographolide (DIAP) in rat plasma after oral dose of methanol extract (1 g/kg body weight) of Andrographis paniculata leaf. An increase in plasma concentration of AP and DIAP was observed from 30 min to 3 h after oral administration of the extract. The maximum plasma concentrations of AP and DIAP were 1.42+/-0.09 microg/ml and 1.31+/-0.04 microg/ml, respectively. Fourteen days oral treatment of rats with the methanol extract (1 g/kg body weight) followed by CCl(4) administration preserved catalase (CAT), and superoxide dismutase (SOD) activities in erythrocytes, whereas plasma lipid peroxidation, alanine transaminase (ALT) and aspartate transaminase (AST) activities were restored to values comparable with control values. Treatment of rats with CCl(4) did not showed significant alteration (p>0.05) in plasma total antioxidant status (TAS) as compare to values of control group.

Matched MeSH terms: Anti-Inflammatory Agents, Non-Steroidal/pharmacokinetics*

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