Abstract
The aim of this study was to formulate and prepare compression-coated tablets for colonic release (CR-tablets), and to evaluate the bioavailability of ketoprofen following the administration of a single dose from mini-tablets with immediate release (IR-tablets) compared to CR-tablets. CR-tablets were prepared based on time-controlled hydroxypropylmethylcellulose K100M inner compression-coating and pH-sensitive Eudragit® L 30D-55 outer film-coating. The clinical bioavailability study consisted of two periods, in which two formulations were administered to 6 volunteers, according to a randomized cross-over design. The apparent cumulative absorption amount of ketoprofen was estimated by plasma profile deconvolution. CR-tablets were able to delay ketoprofen’s release. Compared to IR-tablets used as reference, for the CR-tablets the maximum plasma concentration (Cmax) was lower (4920.33±1626.71 ng/mL vs. 9549.50±2156.12 ng/mL for IR-tablets) and the time needed to reach Cmax (tmax) was 5.33±1.63 h for CR-tablets vs. 1.33±0.88 h for IR-tablets. In vitro-in vivo comparison of the apparent cumulative absorption amount of ketoprofen showed similar values for the two formulations. Therefore, the obtained pharmacokinetic parameters and the in vitro-in vivo comparison demonstrated the reliability of the developed pharmaceutical system and the fact that it is able to avoid the release of ketoprofen in the first part of the digestive tract.
Highlights
A particular type of pharmaceutical system for colonic release is the chronopharmaceutical system with pulsatile release
This study aimed at (I) developing a ketoprofen colonic drug delivery system, pH and time dependent, by double-coating: the first step was compression-coating of ketoprofen mini-tablet cores (IR-tablets) with a layer based on a matrix-forming polymer (HPMC) and the second step was film-coating of the compression-coated tablets with an enteric outer film based on EL55 (Eudragit® L 30D-55), a methacrylic polymer
Other groups of researchers found similar results: Patel et al (2016) coated ketoprofen core tablets using a mixture of Eudragit® S100 and Eudragit® L100 and obtained compression-coated tablets with 4 h lag time and more than 80% drug release; Devi and Sharma (2015) prepared compression-coated ketoprofen tablets using amylose/ethyl cellulose mixture and observed that during 5 h the system released less than 20% ketoprofen, but reached 76.31% drug release; Alencar et al (2017) found that Eudragit® S100 coated pellets compressed into tablets were able to release less than 20% ketoprofen for 4 h, but to allow the release of approximately 90% of the drug until the end of the dissolution study
Summary
A particular type of pharmaceutical system for colonic release is the chronopharmaceutical system with pulsatile release. The use of pulsatile release systems may be advantageous for adapting the treatment to chronopharmacological needs (for example, in the treatment of cardiovascular diseases, asthma, arthritis, ulcers) (Biswas et al, 2015; Vonica, Tomuță, Leucuța, 2011) or to target a drug to a specific site in the digestive tract, for example in the colon (Hashem et al, 2011; Veerareddy, Vemula, 2012). Chronotherapeutical systems include among them the compression-coated tablets. The drug core of compression-coated tablets is usually represented by a mini-tablet which offers the advantages of reduced size, regular shape and smooth surface, providing excellent support for coating with various polymers. Compression-coated tablets as colonic release systems are usually obtained by coating the drug cores by compression-coating (Fukui, Miyamura, Kobayashi, 2001a, 2001b; Fukui et al, 2001). The polymers in the coating layers are usually soluble or insoluble matrix-forming polymers, capable of controling
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