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Novel fenofibric acid-loaded controlled release pellet bioequivalent to choline fenofibrate-loaded commercial product in beagle dogs.
Int J Pharm. 2015 Jul 25; 490(1-2):273-80.IJ

Abstract

The objective of this study was to develop a novel fenofibric acid-loaded controlled release pellet showing enhanced, or equivalent to, bioavailability compared with two commercially available products containing fenofibrate or choline fenofibrate. The effect of solubilizing agents on drug solubility and the impact of fillers on core properties were investigated. Among them, magnesium carbonate most improved drug solubility, and κ-carrageenan provided the best spherical cores. The fenofibric acid-loaded pellet was prepared with magnesium carbonate and κ-carrageenan employing the extrusion/spheronizing technique followed by coating with ethylcellulose. Furthermore, dissolution and pharmacokinetic study in beagle dogs were performed compared to the fenofibrate-loaded commercial tablet (FCT) and choline fenofibrate-loaded commercial mini-tablet (CFCM). This fenofibric acid-loaded pellet showed controlled release of the drug in phosphate buffer (pH 6.8) and 0.025 M sodium laurylsulfate within 4h. Furthermore, this pellet and CFCM exhibited similar dissolution profiles. Plasma concentrations greater than 1,000 ng/ml were maintained from 30 min to 8h, suggesting a sustained release pattern. Also, the fenofibric acid-loaded pellet gave significantly higher AUC and Cmax values than FCT, indicating that it improved the bioavailability of fenofibrate due to enhanced solubility and sustained release. In addition, this pellet and CFCM were not significantly different in terms of pharmacokinetic parameters including AUC, Cmax and Tmax. Thus, this pellet was bioequivalent to CFCM in beagle dogs. In conclusion, this fenofibric acid-loaded controlled release pellet would be a potential alternative to the choline fenofibrate-loaded commercial product.

Authors+Show Affiliations

College of Pharmacy & Institute of Pharmaceutical Science and Technology, Hanyang University, 55 Hanyangdaehak-ro, Sangnok-gu, Ansan 426-791, South Korea; Pharmaceutical Research Centre, Hanmi Pharm. Co., Paltan-myeon, 893-5 Hwaseong, Gyeonggi-Do 445-913, South Korea.College of Pharmacy & Institute of Pharmaceutical Science and Technology, Hanyang University, 55 Hanyangdaehak-ro, Sangnok-gu, Ansan 426-791, South Korea.College of Pharmacy & Institute of Pharmaceutical Science and Technology, Hanyang University, 55 Hanyangdaehak-ro, Sangnok-gu, Ansan 426-791, South Korea.College of Pharmacy & Institute of Pharmaceutical Science and Technology, Hanyang University, 55 Hanyangdaehak-ro, Sangnok-gu, Ansan 426-791, South Korea.College of Pharmacy & Institute of Pharmaceutical Science and Technology, Hanyang University, 55 Hanyangdaehak-ro, Sangnok-gu, Ansan 426-791, South Korea.College of Pharmacy & Institute of Pharmaceutical Science and Technology, Hanyang University, 55 Hanyangdaehak-ro, Sangnok-gu, Ansan 426-791, South Korea; Pharmaceutical Research Centre, Hanmi Pharm. Co., Paltan-myeon, 893-5 Hwaseong, Gyeonggi-Do 445-913, South Korea.College of Pharmacy, Yeungnam University, 214-1 Dae-Dong, Gyongsan 712-749, South Korea.College of Pharmacy, Yeungnam University, 214-1 Dae-Dong, Gyongsan 712-749, South Korea.Pharmaceutical Research Centre, Hanmi Pharm. Co., Paltan-myeon, 893-5 Hwaseong, Gyeonggi-Do 445-913, South Korea. Electronic address: jswoo@hanmi.co.kr.College of Pharmacy & Institute of Pharmaceutical Science and Technology, Hanyang University, 55 Hanyangdaehak-ro, Sangnok-gu, Ansan 426-791, South Korea. Electronic address: hangon@hanyang.ac.kr.

Pub Type(s)

Journal Article
Research Support, Non-U.S. Gov't

Language

eng

PubMed ID

26024820

Citation

Kim, Kyung Soo, et al. "Novel Fenofibric Acid-loaded Controlled Release Pellet Bioequivalent to Choline Fenofibrate-loaded Commercial Product in Beagle Dogs." International Journal of Pharmaceutics, vol. 490, no. 1-2, 2015, pp. 273-80.
Kim KS, Jin SG, Mustapha O, et al. Novel fenofibric acid-loaded controlled release pellet bioequivalent to choline fenofibrate-loaded commercial product in beagle dogs. Int J Pharm. 2015;490(1-2):273-80.
Kim, K. S., Jin, S. G., Mustapha, O., Yousaf, A. M., Kim, D. W., Kim, Y. H., Kim, J. O., Yong, C. S., Woo, J. S., & Choi, H. G. (2015). Novel fenofibric acid-loaded controlled release pellet bioequivalent to choline fenofibrate-loaded commercial product in beagle dogs. International Journal of Pharmaceutics, 490(1-2), 273-80. https://doi.org/10.1016/j.ijpharm.2015.05.059
Kim KS, et al. Novel Fenofibric Acid-loaded Controlled Release Pellet Bioequivalent to Choline Fenofibrate-loaded Commercial Product in Beagle Dogs. Int J Pharm. 2015 Jul 25;490(1-2):273-80. PubMed PMID: 26024820.
* Article titles in AMA citation format should be in sentence-case
TY - JOUR T1 - Novel fenofibric acid-loaded controlled release pellet bioequivalent to choline fenofibrate-loaded commercial product in beagle dogs. AU - Kim,Kyung Soo, AU - Jin,Sung Giu, AU - Mustapha,Omer, AU - Yousaf,Abid Mehmood, AU - Kim,Dong Wuk, AU - Kim,Young Hun, AU - Kim,Jong Oh, AU - Yong,Chul Soon, AU - Woo,Jong Soo, AU - Choi,Han-Gon, Y1 - 2015/05/27/ PY - 2015/03/25/received PY - 2015/05/13/revised PY - 2015/05/22/accepted PY - 2015/5/31/entrez PY - 2015/5/31/pubmed PY - 2016/3/24/medline KW - Bioavailability KW - Bioequivalence KW - Controlled release pellet KW - Dissolution KW - Fenofibric acid SP - 273 EP - 80 JF - International journal of pharmaceutics JO - Int J Pharm VL - 490 IS - 1-2 N2 - The objective of this study was to develop a novel fenofibric acid-loaded controlled release pellet showing enhanced, or equivalent to, bioavailability compared with two commercially available products containing fenofibrate or choline fenofibrate. The effect of solubilizing agents on drug solubility and the impact of fillers on core properties were investigated. Among them, magnesium carbonate most improved drug solubility, and κ-carrageenan provided the best spherical cores. The fenofibric acid-loaded pellet was prepared with magnesium carbonate and κ-carrageenan employing the extrusion/spheronizing technique followed by coating with ethylcellulose. Furthermore, dissolution and pharmacokinetic study in beagle dogs were performed compared to the fenofibrate-loaded commercial tablet (FCT) and choline fenofibrate-loaded commercial mini-tablet (CFCM). This fenofibric acid-loaded pellet showed controlled release of the drug in phosphate buffer (pH 6.8) and 0.025 M sodium laurylsulfate within 4h. Furthermore, this pellet and CFCM exhibited similar dissolution profiles. Plasma concentrations greater than 1,000 ng/ml were maintained from 30 min to 8h, suggesting a sustained release pattern. Also, the fenofibric acid-loaded pellet gave significantly higher AUC and Cmax values than FCT, indicating that it improved the bioavailability of fenofibrate due to enhanced solubility and sustained release. In addition, this pellet and CFCM were not significantly different in terms of pharmacokinetic parameters including AUC, Cmax and Tmax. Thus, this pellet was bioequivalent to CFCM in beagle dogs. In conclusion, this fenofibric acid-loaded controlled release pellet would be a potential alternative to the choline fenofibrate-loaded commercial product. SN - 1873-3476 UR - https://www.unboundmedicine.com/medline/citation/26024820/Novel_fenofibric_acid_loaded_controlled_release_pellet_bioequivalent_to_choline_fenofibrate_loaded_commercial_product_in_beagle_dogs_ L2 - https://linkinghub.elsevier.com/retrieve/pii/S0378-5173(15)00487-1 DB - PRIME DP - Unbound Medicine ER -