Biowaiver Monographs for Immediate Release Solid Oral Dosage Forms: Diclofenac Sodium and Diclofenac Potassium

Chuasuwan, B.; Binjesoh, V.; Polli, James E.; Zhang, H.; Amidon, Gordon L.; Junginger, Hans E.; Midha, K. K.; Shah, Vinod P.; Stavchansky, Salomon A; Dressman, Jennifer B.; Barends, D. M.

doi:10.1002/jps.21525

Cited by 144 publications

(104 citation statements)

References 50 publications

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“…Diclofenac is a non-steroidal anti-inflammatory drug with analgesic, anti-inflammatory and antipyretic properties, was chosen as the model compound [5]. It is reported that absorption of diclofenac occurs throughout the intestinal tract [6].…”

Section: Introductionmentioning

confidence: 99%

Determination of Regional Intestinal Permeability of Diclofenac and Metoprolol Using a Newly-Developed and Validated High Performance Liquid Chromatographic Method

Kaynak¹,

Buyutuncel²,

Cagler³

et al. 2015

Trop. J. Pharm Res

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Section: Introductionmentioning

confidence: 99%

Determination of Regional Intestinal Permeability of Diclofenac and Metoprolol Using a Newly-Developed and Validated High Performance Liquid Chromatographic Method

Kaynak¹,

Buyutuncel²,

Cagler³

et al. 2015

Trop. J. Pharm Res

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“…Diclofenac potassium is claimed to dissolve faster and hence absorbed faster, than the sodium salt and is recommended for the treatments that need short onset of action, mainly for its analgesic properties 21 . Although there were differences between IC 50 values of sodium and potassium salts of diclofenac, a statistical evaluation was not performed (Table 1).…”

Section: Discussionmentioning

confidence: 99%

PCB-153 İle İnkübe Edilen Sığır Miyometriumu Üzerine Diklofenak Potasyum ve Diklofenak Sodyumun Tokolitik Etkisi

Daş¹,

Aksoy²,

Yavuz³

et al. 2013

Kafkas Univ Vet Fak Derg

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SummaryIn this study, the tocolytic effects of the potassium and sodium salts of diclofenac, a non-steroidal anti-inflammatory drug (NSAID), on cattle myometria were investigated in the presence of an estrogenic polychlorinated biphenyl congener 2,2 ' ,4,4' ,5,. The uterine samples were obtained from newly slaughtered, non-pregnant cattle more than two years old and in the anoestrus stage. Eight groups were constituted for testing (each group contained 8 strips from two animals, with 4 from each); there were four control groups (diclofenac potassium 24 h and 48 h; diclofenac sodium 24 h and 48 h) and four groups for PCB-153 (diclofenac potassium 24 h and 48 h; diclofenac sodium 24 h and 48 h). The control groups were incubated in physiological salt solution (PSS) for 24 or 48 hours and the PCB-153 groups were incubated in PSS which contained 100 ng/mL of PCB-153, for either 24 h or 48 h. After the incubation period, the strips were hung and incubated in the tissue bath system until spontaneous contractions occurred. Oxytocin (OT) was administered at 0.5 nM to the strips in all groups for the stimulation of spontaneous contractions. Diclofenac potassium and diclofenac sodium were then administered cumulatively in the range of 1x10 -7 to 7x10 -4 M to the strips of all groups to the maximum inhibitory effect was observed. After each application, isometric uterine contractions were recorded for 20 min. Mean peak amplitude (P MAX ), frequency (beats per minutes, BPM) and area under the curve (AUC) values of the myometrial contractions, which are criteria for determining drug effects, were calculated from the curve and evaluated statistically. The inhibitory concentration 50 (IC 50 ) values were calculated for the BPM, P MAX and AUC values of the myometrial contractions. Finally, the tocolytic effects of diclofenac potassium and diclofenac sodium on the contractions of cattle uterine strips pre-incubated with PCB-153, were determined. Keywords: Diclofenac potassium, Diclofenac sodium, PCB-153, Cattle, Tocolysis PCB-153 İle İnkübe Edilen Sığır Miyometriumu Üzerine Diklofenak Potasyum ve Diklofenak Sodyumun Tokolitik Etkisi ÖzetBu çalışmada, steroid yapıda olmayan ağrı kesici ve yangı giderici ilaçlardan (non steroidal anti-inflammatory drugs, NSAIDs) diklofenakın potasyum ve sodyum tuzlarının poliklorlu bifenil (PCB)'lerden östrojenik etkili 2,2' ,4,4' ,5,5'-hekzaklorobifenil (PCB-153) varlığında sığır uterus düz kaslarını gevşetici etkisi araştırılmıştır. Uterus örnekleri mezbahada iki yaşın üzerinde, yeni kesilen, anöstrüs evresinde, gebe olmayan ineklerden sağlanmıştır. İlaçların etkisini ortaya koymak için, dört kontrol (diklofenak potasyum 24 ve 48 saat, diklofenak sodyum 24 ve 48 saat) ve dört PCB-153 (diklofenak potasyum 24 ve 48 saat, diklofenak sodyum 24 ve 48 saat) olmak üzere sekiz ayrı grup oluşturulmuştur. Her bir grup iki farklı hayvandan dörder olmak üzere toplam sekiz miyometrium şeridi içermektedir. Kontrol grupları ayrı ayrı 24 ve 48 saat süre ile fizyolojik tuz solüsyonu (physiological salt saline, P...

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“…Since DS has pH dependent solubility such as 0.14 mg DS is soluble in 1 mL of pH 5.8 phosphate buffer and 5.15 mg DS soluble in 1 mL pH 7.4 phosphate buffer at 23±2°C, 29 a pH value which DS is less soluble in the external phase was selected in order to increase encapsulation efficiency. 22 Lowering the external pH from 7.4 to 5.8 (F4) resulted with an increase on encapsulated DS by 32% and from this point on all other nanoparticle formulations (F5 and F6) were prepared with pH 5.8 external phase which allows less DS escape to outer aqueous phase depending on less solubility.…”

Section: Encapsulation Efficiencymentioning

confidence: 99%

<i>In Situ</i> Hydrogel Formulation for Intra-Articular Application of Diclofenac Sodium-Loaded Polymeric Nanoparticles

Küçüktürkmen

Öz

Bozkır

2017

tjps

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Objectives: The world's population is getting older and the number of people suffering from arthritis is a major problem according to World Health Organization's data. In this respect, the need for more efficient treatment for arthritis becomes an urgent issue. In this research, nanoparticle bearing in situ gelling hydrogel formulation was developed for prolonged local delivery of diclofenac sodium (DS). Materials and Methods: Emulsion-solvent evaporation technique was used for the preparation of nanoparticles. Particle size, encapsulation efficiency, morphology, and drug release profile of DS loaded biodegradable nanoparticles as well as gel viscosity and gelation time of in situ gelling hydrogel formulations were optimized to increase the time interval between each dose application for enhanced patience compliance. Results:The spherical nanoparticles with a mean particle diameter of 168 nm was obtained and confirmed by both transmission electron microscope and atomic force microscope. Different types of surfactants were tested in the first emulsification step of nanoparticle production process and Arlacel ® -C significantly increased the encapsulation efficiency to 89.7%. Thirty days prolonged in vitro release of DS was achieved by using the combined formulation of polymeric nanoparticles and in situ hydrogel prepared by using poloxomer 407 and chitosan. Conclusion: Local administration of DS with this novel delivery system could be considered of having potential to minimize side effects associated with decreased amount of drug in dosage form compared to conventional oral dose. Key words: Diclofenac sodium, drug delivery, PLGA, Poly(ε-caprolactone), thermosensitive hydrogel, poloxamers ABSTRACT ÖZ Amaç: Dünya Sağlık Örgütü'nün verilerine göre dünya çapında insanların yaş ortalaması ve bağlantılı olarak artrit hastalığından mağdur olan insan sayısı da artmaktadır. Bu açıdan bakıldığında, artrit tedavisi için daha etkili tedavilerin gerekliliği önemli hale gelmiştir. Bu araştırmada, diklofenak sodyumun (DS) uzatılmış lokal taşınımı için nanopartikül içeren in situ hidrojel formülasyonları geliştirilmiştir. Gereç ve Yöntemler: Nanopartiküllerin hazırlanmasında emülsiyon-çözücü buharlaştırma yöntemi kullanılmıştır. DS yüklü nanopartiküllerin partikül büyüklüğü, enkapsülasyon etkinliği, morfolojisi ve ilaç salım profilleri ile in situ hidrojelin jel viskozitesi ve jelleşme süresi, hasta uyuncunu artırmak için her bir dozun uygulanması arasındaki zamanı artırmak amacıyla optimize edilmiştir. Bulgular: Ortalama partikül büyüklüğü 168 nm olan küresel nanopartiküller elde edilmiş ve geçirimli elektron mikroskobu ve atomik kuvvet mikroskobu ile desteklenmiştir. Nanopartikül üretim sürecinin ilk emülsifikasyon adımında farklı sürfaktanlar denenmiş ve Arlacel ® -C diklofenak sodyumun enkapsülasyon etkinliğini %89.7'ye yükseltmiştir. DS'nin 30 güne uzatılmış in vitro salımı, nanopartiküllerin ve poloksamer 407/kitozan ile hazırlanmış in situ hidrojelin kombine kullanılmasıyla başarılmıştır. Sonuç: DS'nin bu yenilikçi taşıy...

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Biowaiver Monographs for Immediate Release Solid Oral Dosage Forms: Diclofenac Sodium and Diclofenac Potassium

Cited by 144 publications

References 50 publications

Determination of Regional Intestinal Permeability of Diclofenac and Metoprolol Using a Newly-Developed and Validated High Performance Liquid Chromatographic Method

Determination of Regional Intestinal Permeability of Diclofenac and Metoprolol Using a Newly-Developed and Validated High Performance Liquid Chromatographic Method

PCB-153 İle İnkübe Edilen Sığır Miyometriumu Üzerine Diklofenak Potasyum ve Diklofenak Sodyumun Tokolitik Etkisi

<i>In Situ</i> Hydrogel Formulation for Intra-Articular Application of Diclofenac Sodium-Loaded Polymeric Nanoparticles

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