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Search Results: 1 - 10 of 44 matches for " Piroxicam "
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Caboxymetylcellulose/Gelatin Blends Loaded with Piroxicam: Preparation, Characterization and Evaluation of in Vitro Release Profile  [PDF]
Vivia Buzzi, Marli Brudner, Theodoro Maciel Wagner, Giovana C. Bazzo, Ana Paula Testa Pezzin, Denise Abatti Kasper Silva
Journal of Encapsulation and Adsorption Sciences (JEAS) , 2013, DOI: 10.4236/jeas.2013.34012

Piroxicam is a non-steroidal anti-inflammatory drug (NSAID) exhibiting analgesic and antipiretic properties and widely used in the management of chronic diseases. Associated with these use, there are registers of adverse reactions. Microparticle formulations in hydrogel matrix can be used to form a semi-permeable barrier which enables their actions and can reduce the effects. This work presents a study on the effect of gelatin/carboxymethyl cellulose (Gel/CMC) semi-IPN matrix composition on the retention and kinetic behavior of releasing this drug. The microparticles were obtained through the emulsion-crosslinking method using 23 factorial planning and the piroxicam was added as solid particles. In order to characterize the interaction between matrix-active agent and quantification of the drug, the following techniques were applied: SEM, DSC and XRD. SEM micrographs revealed microparticles with regular and spherical shape and that in some compositions the drug is partially absorbed and not encapsulated. Beyond that DSC and XRD analyses indicate that the piroxicam remained in the matrixes, maintains the same crystalline form. The factorial planning analysis indicated that matrix obtained a maximum encapsulation efficiency (EE%) of 10.64% and became possible to create a response surface graph using a EE% as answer. In addition to this, release kinetics analyses demonstrated that the release process seems to be governed by distinctly kinetic models, considering the composition of the sample. In some samples the release can be driven by Fickinianan diffusion, others by anomalous transport or swelling.

Derivatization of enolic OH of piroxicam: a comparative study on esters and sulfonates
Jayaselli, J.;Cheemala, J. Manila Sagar;Geetha Rani, D. P.;Sarbani Pal,;
Journal of the Brazilian Chemical Society , 2008, DOI: 10.1590/S0103-50532008000300019
Abstract: a number of ester and sulfonate derivatives of piroxicam were prepared via acylation/sulfonation of the enolic oh of piroxicam. all the compounds were evaluated for their chemical stability and cyclooxygenase inhibiting properties. data suggested that esters could be useful for the development of potential prodrugs. the sulfonate derivatives prepared for the first time were found to be stable. one of them showed a moderately selective cox-2 inhibition over cox-1 and would have lower gastrointestinal side effects than piroxicam due to the masked enolic oh group. a plausible mechanism for the acylation/sulfonation process has been proposed that involves participation of the pyridine moiety of piroxicam. molecular structure of one of the ester was established for the first time by the crystal structure analysis from x-ray powder data.
Método analítico para a determina??o de meloxicam em plasma humano por cromatografia líquida de alta eficiência (CLAE)
Porta, Valentina;Ferraz, Humberto Gomes;Souza, Tatiane Maria de Lima;Kano, Eunice Kazue;Serra, Cristina Helena dos Reis;
Revista Brasileira de Ciências Farmacêuticas , 2005, DOI: 10.1590/S1516-93322005000200009
Abstract: a simple, rapid and specific high-performance liquid cromatographic (hplc) method was developed and validated to estimate meloxicam (cox-2 inhibitor) levels in human plasma. piroxicam was used as internal standard. reversed phase chromatography was conducted using a synergi rp-max (150 x 4.6 mm) column at 30 oc and a mobile phase of acetonitrile and 0.025 mol/l ph 4,5 phosphate buffer (40:60, v/v), at a flow rate of 1ml/min. analytes were detected at 364 nm. plasma samples were acidified with 1 mol/l hydrochloric acid and extracted with tert-butyl methyl ether, evaporated to dryness, reconstituted in 250 ml of mobile phase and injected in the column. the retention time of meloxicam and piroxicam were 3.35 and 4.19 minutes, respectively. this method showed to be linear in the range of 50 - 4500 ng/ml (r2 = 0.9995), a loq of 50 ng/ml and accuracy of 114%. the analytical method showed suitable specificity, sensitivity, linearity, precision and accuracy, and can be used in bioequivalence or pharmacokinetics studies involving meloxicam.
The effect of piroxicam on the formation of postoperative, intraabdominal adhesion in rats
Maghsoudi Hemmat,Askary Behnam
Saudi Journal of Gastroenterology , 2008,
Abstract: Background/Aims: Peritoneal adhesions are fibrous bands of tissues formed between organs that are normally separated and/or between organs and the internal body wall after peritoneal injury. Antiinflammatory agents were used to reduce the initial inflammatory response to tissue injury and, hence, the subsequent formation of adhesion. The aim of this study was to investigate the effect of intraperitoneal instillation of piroxicam on intraperitoneal adhesions. Methods: Eighty Wistar rats were subjected to standardized lesion by using the scraping model and were randomly divided into four groups. Group I (control) received no treatment; groups II, III, and IV received 10-12.5 mL of 0.05, 0.1, and 0.2 mg/mL piroxicam solution, respectively, after surgery. On the 14th postoperative day, the adhesion intensity score, inflammatory cell reaction, and the number of adhesion bands were determined. Results: There were no rats with grade 0 adhesions in the control group. There were 10 rats (50%) with grade 2 and eight rats (40%) with grade 3 adhesions. The adhesion intensity ( P < 0.0001) and the number of adhesion bands ( P < 0.001) were significantly lower in groups III and IV. No significant difference was observed in the adhesion intensity or the number of adhesion bands between groups I and II. Conclusions: Intraperitoneal instillation of piroxicam solution might be useful for preventing peritoneal adhesions.
Modification and Validation of an HPLC Method for Quantification of Piroxicam
Muthanna F. Abdulkarim,Ghassan Z. Abdullah,M.H.F. Sakeena,Mallikarjun Chitneni
International Journal of Drug Delivery , 2011,
Abstract: Piroxicam is a NSAID that is widely used in the treatment of joint pain and osteoarthritis. The objectives of the study were to modify and validate HPLC method so as to obtain an accurate, sensitive and precise method to quantify piroxicam concentrations without interference from the other ingredients presence in the formulation. The method published by Owen et al. was adapted and modified to suit the above requirements. The modification was carried out on the mobile phase as the mobile phase used by the authors was not able to separate the drug peak from the interference of the formulation excipients. The modified mobile phase consisted of 5 mM of disodium hydrogen phosphate adjusted to pH 3 with concentrated ortho phosphoric acid, methanol, acetonitrile and glacial acetic acid at ratios of 27:20:52:1 respectively. The method was validated and found to be specific, precise, accurate and reproducible even when run at different times of the same day or on different times on different days. The limit of detection and quantification were determined to be 0.035 μg/ml and 0.0625 μg/ml respectively. It could be concluded that this method could be used to determine piroxicam concentration in the samples collected from in vitro study of permeability through the synthetic membrane and excised rat skin. Keywords: Piroxicam, HPLC, Quantification analysis, Modification.
Hollow microspheres for gastroretentive floating- pulsatile drug delivery: preparation and in vitro evaluation
Maryam Maghsoodi,Elham Hemati,Bahram Qadermazi,Zahra Yari
Advanced Pharmaceutical Bulletin , 2011,
Abstract: Purpose: A multiparticular floating-pulsatile drug delivery system was developed for time and site specific drug release of piroxicam. A blend of floating and pulsatile principles of drug delivery system would have the advantage that a drug can be released in the upper GI tract after a definite time period. Methods: Hollow microspheres were prepared by the emulsion solvent diffusion method using Eudragit S as an enteric acrylic polymer with piroxicam at various polymer/drug ratios in a mixture of dichloromethane and ethanol. Developed formulations were evaluated for yield, encapsulation efficiency, particle size, shape, apparent density, buoyancy studies and dissolution studies. Results: The obtained microballoons were spherical with no major surface irregularity and mean particle size ranging from 250 to 380 for different batches. Formulations show a slight amount of relaese ranging from 0.7 to 11% in acidic medium (SGF) with complete release of drug in simulated intestinal fluid (SIF) in less than 3 h. Encapsulation efficiency of different formulations varied from 90 to 98%. The optimum loading amount of drug in the particles was found to impart suitable floatable properties to the microballoons. With increasing polymer/drug ratio, buancy of the microballoons increases accompanied by simultaneous reduction of apparent particle density. Conclusion: A pulsatile release of piroxicam was demonstrated by a simple drug delivery system which could be useful in chronopharmacotherapy of rheumatoid arthritis.
Effect of Polyvinylpyrrolidone on Complexation and Dissolution Rate of Beta Cyclodextrin and Hydroxypropyl Beta Cyclodextrin Complexes of Piroxicam
Otra Kumar,A. Prameela Rani
International Journal of Pharmaceutical and Phytopharmacological Research , 2012,
Abstract: Complexation of Piroxicam with β-Cyclodextrin and hydroxypropyl-β-Cyclodextrin in the presence and absence of polyvinylpyrrolidone and the effect of polyvinylpyrrrolidone on the solubilizing efficiency of Cyclodextrins and on the dissolution rate of Piroxicam from the Cyclodextrin complexes were investigated. The phase solubility studies indicated the formation of Piroxicam-β-Cyclodextrin and Piroxicam-hydroxypropyl-β-Cyclodextrin inclusion complexes at a 1:1 M ratio in solution, both in the presence and absence of polyvinylpyrrolidone. The complexes formed were quite stable. The solubility and dissolution rate of Piroxicam were markedly enhanced by complexation with β-Cyclodextrin and hydroxypropyl- β-Cyclodextrin. Piroxicamhydroxypropyl-β-Cyclodextrin(1:2) inclusion complex gave a 36.52-fold increase in the dissolution rate of Piroxicam. Addition of polyvinylpyrrolidone resulted in higher complexation efficiency and markedly enhanced solubilizing efficiency of β-Cyclodextrin and hydroxypropyl-β-Cyclodextrin. Solid inclusion complexes of Cyclodextrins with polyvinylpyrrolidone gave several times higher rates of dissolution than those of Piroxicam and its complexes with Cyclodextrins alone.
Kulkarni Parthasarathi Keshavarao,Dixit Mudit,Panner Selvam,Achin Jain
International Research Journal of Pharmacy , 2012,
Abstract: The aim of the present study was to enhance the dissolution rate of piroxicam (PX) using its solid dispersions (SDs) with polyethylene glycol (PEG) 6000. The phase solubility behavior of piroxicam in presence of various concentrations of PEG 6000 in distilled water was obtained at 37 °C. The solubility of PX increased with increasing amount of PEG 6000 in water and demonstrating that the reaction conditions became more favorable as the concentration of PEG 6000 increased. The SDs of PX with PEG 6000 were prepared using 1:1, 1:2,1:3,1:4 and1:5 (PX/PEG 6000) ratio by Hot-melt method and solvent evaporation method. Evaluation of the properties of the SDs was performed by using dissolution, Fourier-transform infrared (FTIR) spectroscopy, differential scanning calorimetry (DSC). The SDs of PX with PEG 6000 exhibited enhanced dissolution rate of PX and the rate increased with increasing concentration of PEG 6000 in SDs. Mean dissolution time (MDT) of PX decreased significantly after preparation of SDs and physical mixture with PEG6000. The FTIR spectroscopic studies revealed that there is no chemical interaction and drug was stable. The DSC studies indicated the microcrystalline or amorphous state of PX in SDs with PEG 6000.
Design, Synthesis, Antinociceptive and Anti-Inflammatory Activities of Novel Piroxicam Analogues
Amanda Silva de Miranda,Walfrido Bispo Júnior,Yolanda Karla Cupertino da Silva,Magna Suzana Alexandre-Moreira,Rosane de Paula Castro,José Ricardo Sabino,Luciano Morais Li?o,Lídia Moreira Lima,Eliezer J. Barreiro
Molecules , 2012, DOI: 10.3390/molecules171214126
Abstract: In this paper we report the design, synthesis, antinociceptive and anti-inflammatory activities of a series of benzothiazine N-acylhydrazones 14a–h, planned by structural modification of piroxicam (1), a non steroidal anti-inflammatory drug. Among the synthesized analogues, compounds 14f (LASSBio-1637) and 14g (LASSBio-1639) were identified as novel antinociceptive and anti-inflammatory prototypes, active by oral administration, acting by a mechanism of action that seems to be different from that of piroxicam, since they were inactive as an inhibitor of cyclooxygenase (COX-1 and COX-2) at concentrations of 10 mM.
Effect of preparation conditions on morphology, drug content and release profiles of poly(hydroxybutyrate) microparticles containing piroxicam
Bazzo, G. C.;Lemos-Senna, E.;Gon?alves, M. C.;Pires, A. T. N.;
Journal of the Brazilian Chemical Society , 2008, DOI: 10.1590/S0103-50532008000500016
Abstract: in this study, poly(hydroxybutyrate) microparticles containing piroxicam were prepared by the oil-in-water emulsion-solvent evaporation method. the effects of some process conditions on drug content were determined using a 23 factorial design. the piroxicam loading efficiency varied from 5.5 to 89.8 %. hollow and irregular microparticles with drug crystals on their surfaces were obtained when 5 ml of chloroform was used as the internal phase. in the release study, all of the piroxicam was released to the dissolution medium (phosphate buffer ph 7.4) after 8 h. small spherical microspheres with a rough and porous polymeric matrix were obtained when 20 ml of dichloromethane was used as the internal phase and isopropanol was added to the external aqueous phase. these microspheres controlled the piroxicam release for approximately 50 h. the results demonstrated that it is possible to obtain microparticles with specific characteristics by the optimization of the process conditions.
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