Sustained release characteristics and pharmacokinetic parameters of ketoprofen suppositories using chitosan

Tarimci, Nilüfer; Ermiş, Dilek

doi:10.1016/s0378-5173(96)04790-4

Cited by 13 publications

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“…15) Ketoprofen chitosan granules loaded polyethylene glycol suppository was examined and compared with conventional form in rabbits. 16) Extensive survey of literature and patent databases did not reveal any microparticles loaded suppository formulation developed of flutamide. Based on these considerations, the main objectives of the present study were: i) To develop flutamide microparticles by ionic gelation method using natural hydrophilic polymers sodium alginate and tamarind kernel powder in combination.…”

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confidence: 99%

Development of Suppositories Containing Flutamide-Loaded Alginate-Tamarind Microparticles for Rectal Administration: In Vitro and in Vivo Studies

Patil¹,

Mahajan

Surana

2015

CHEMICAL & PHARMACEUTICAL BULLETIN

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In the present work the absorption of flutamide from suppositories containing hydrophilic tamarind alginate microparticles after rectal administration in rats was investigated with the purpose of enhancing bioavailability and to avoid hepatic toxicity. Microparticles were developed by ionic gelation method and optimized using one factorial design of response surface methodology. The optimized batch of microparticles had tamarind gum-sodium alginate (1 : 3) ratio and showed entrapment efficiency 94.969% and mucoadhesion strength 94.646% with desirability of 0.961. Suppositories loaded with microparticles were developed by fusion method using poloxamer 407 and poloxamer 188 in combination as suppository base. Kinetic analysis of the release data of microparticle-loaded suppositories showed time-independent release of drug. Higher values of 'n' (>0.89) represent Super Case II-type drug release. The pharmacokinetics of flutamide from flutamide tamarind alginate microparticle-loaded suppository were compared with oral suspension. C max of microparticle-loaded suppository was significantly larger than that of oral suspension (1.711 and 0.859 µg/ mL, respectively).Key words tamarind kernel polysaccharide; sodium alginate; ionic gelation; one factorial design; mucoadhesive microparticle-loaded poloxamer suppository; rectal delivery Adenocarcinoma of the prostate is the second most common cause of death of men world-wide. A nonsteroidal antiandrogen flutamide could be used in combination with medical or surgical castration to provide superior care for patients with metastatic prostate cancer. Large studies have shown a longer disease-free interval and a short survival advantage with maximum androgen blockade compared with monotherapy, especially in younger, healthy patients with minimum metastatic disease.

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confidence: 99%