Preparation and<i>in vitro</i>evaluation of slow release ketoprofen microcapsules formulated into tablets and capsules

Khodairy, K. A. El; Eshra, A. G.; Nada, Aly; Mortada, S. A. M.

doi:10.3109/02652049209021251

Cited by 17 publications

(7 citation statements)

References 8 publications

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“…1,7,8) Such prolonged release dosage forms are often utilized to avoid frequent dosing of drugs that show a short biological half life. 6) These systems are available for drugs the plasma concentration of which is critically related to efficacy. That is, such systems can achieve maintenance of drug concentration at the therapeutic range in the body.…”

Section: Discussionmentioning

confidence: 99%

“…Microparticulate dosage forms are often used for controlled drug release. 1,[6][7][8] Further, their gastrointestinal transit can be modified with mucoadhesive polymers. [9][10][11] When the mucoadhesive polymers interact with mucous membranes of the GI tract, they are considered to be localized or trapped at the adhesive sites, which may result in prolonged duration of absorption.…”

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confidence: 99%

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Prolonged Intestinal Absorption of Cephradine with Chitosan-Coated Ethylcellulose Microparticles in Rats.

Takishima

Onishi

Machida

2002

Biological & Pharmaceutical Bulletin

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Cephradine-containing ethylcellulose microparticles (MPC) were prepared by the solvent evaporation method. Chitosan-coated MPC (Chi-MPC) were prepared by doping MPC with viscous chitosan solution and subsequently drying. When fluorescein isothiocyanate (FITC)-labeled chitosan-coated ethylcellulose microparticles without drug were administered intraduodenally, they moved slowly in the intestine, that is, most of them were retained at the upper and middle parts of the small intestine for more than 8 h, which is considered due to mucoadhesive properties of coated chitosan. When MPC and Chi-MPC was incubated at 37°C in the JP 14 second fluid, pH 6.8, both released the drug slowly with similar release rates. Cephradine solution and suspension, MPC and Chi-MPC were administered intraduodenally to investigate intestinal drug absorption. Only Chi-MPC suppressed the initial plasma level and maintained the plasma concentration for a long time up to 24 h, suggesting Chi-MPC would be useful for prolonged intestinal absorption of cephradine.

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Section: Discussionmentioning

confidence: 99%

mentioning

confidence: 99%

Prolonged Intestinal Absorption of Cephradine with Chitosan-Coated Ethylcellulose Microparticles in Rats.

Takishima

Onishi

Machida

2002

Biological & Pharmaceutical Bulletin

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“…MS, MS-P or MS-H (30-50 mg) were added to 300 ml of the JP XIII second ‰uid, pH 6.8, which was stirred at a moderate rate, 60 rpm, to re‰ect the in vivo situation; this rate was similar to that in other release studies. 2,7,10) Aliquots (2 ml) were withdrawn at appropriate times. Immediately after each sampling, the aliquot wasˆltered with a membraneˆlter (0.45 mm in pore diameter) and the same volume of fresh JP XIII second ‰uid at 37°C was supplemented to the test medium.…”

Section: Drug Release Testsmentioning

confidence: 99%

“…Further, frequent dosing of ketoprofen is required for therapeutic maintenance because of its fairly fast elimination from the body. 6,7) . Exposure of the stomach to high levels of ketoprofen can cause gastric damage such as ulceration or bleeding.…”

Section: Introductionmentioning

confidence: 99%

In Vitro and in Vivo Evaluation of Sustained Release Chitosan-Coated Ketoprofen Microparticles

Yamada¹,

Onishi²,

Machida³

2001

YAKUGAKU ZASSHI

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Simple ketoprofen microspheres (MS) were prepared by the dry-in-oil method using ethylcellulose (EC) as a matrix polymer. Further, the microspheres modiˆed by addition of polyethylene glycol (PEG) and hydroxypropyl cellulose (HPC), called MS-P and MS-H, respectively, were prepared. The in vitro release from MS, MS-P and MS-H was examined in the JP XIII second ‰uid, pH 6.8, at 37°C and 60 rpm. Chitosan-coated ketoprofen microparticles (Chi-MP) were prepared by the precipitation of droplets of chitosan solution containing MS, and their adhesion to the rat small intestinal mucosa was tested. The plasma concentrations after duodenal administration were investigated for ketoprofen powder suspension, MS and Chi-MP. The particle size was raised with the increase in amount of ketoprofen added. The drug content and addition of PEG or HPC aŠected the drug release rate. The microspheres with moderate drug content, prepared by addition of modest amount of PEG, exhibited better gradual drug release. Chi-MP showed a good mucoadhesion. The maximum plasma concentration of ketoprofen for Chi-MP was less than one-third of that for ketoprofen powder suspension. Chi-MP tended to show the higher and steadier plasma levels than MS.

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“…KP is a non-steroidal anti-inflammatory drug, and usually applied at a medium dose. [12][13][14] The preparation of a KP-loaded implant tablet has been performed according to a previous report, and the in vitro and in vivo releases have been examined and evaluated.…”

mentioning

confidence: 99%

PLGA Implant Tablet of Ketoprofen: Comparison of in Vitro and in Vivo Releases

Onishi

Takahashi

Machida

2005

Biological & Pharmaceutical Bulletin

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An implant tablet of ketoprofen (KP) was developed in order to achieve its sustained supply for approximately one week, and its release was evaluated in vitro and in vivo. Implant tablets (30 mg) containing 1 and 5 mg of ketoprofen, prepared using poly(DL-lactic acid-co-glycolic acid) copolymer (PLGA; MW 10000; lactic acid : glycolic acid‫1؍‬ : 1 (mol/mol)) as a matrix, exhibited similar week-long sustained release in vitro. Plasma concentration was monitored after the implant tablet (5 mg of KP) and a KP solution (0.5 mg of KP) were administered subcutaneously to rats, and in vivo release rate was analyzed by deconvolution. The release rate from the implant tablet was faster in vivo than in vitro in the initial phase, but much lower in vivo than in vitro in the later phase. The plasma level decreased to the level less than the minimal effective concentration at 96 h after administration. However, the calculated plasma concentration given by convolution based on in vitro release rate was more than 7 times greater than the minimal effective concentration even at 96 h after administration. As the implant displayed the discrepancy between in vitro and in vivo release rates, the improvement of the in vivo release rate is required.

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Preparation andin vitroevaluation of slow release ketoprofen microcapsules formulated into tablets and capsules

Cited by 17 publications

References 8 publications

Prolonged Intestinal Absorption of Cephradine with Chitosan-Coated Ethylcellulose Microparticles in Rats.

Prolonged Intestinal Absorption of Cephradine with Chitosan-Coated Ethylcellulose Microparticles in Rats.

In Vitro and in Vivo Evaluation of Sustained Release Chitosan-Coated Ketoprofen Microparticles

PLGA Implant Tablet of Ketoprofen: Comparison of in Vitro and in Vivo Releases

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