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Development of novel fast-dissolving tacrolimus solid dispersion-loaded prolonged release tablet.
Eur J Pharm Sci. 2014 Apr 11; 54:1-7.EJ

Abstract

The goal of this research was to develop a novel prolonged release tablet bioequivalent to the commercial sustained release capsule. A number of tacrolimus-loaded fast-dissolving solid dispersions containing various amounts of DOSS were prepared using the spray drying technique. Their solubility, dissolution and pharmacokinetics in rats were studied. DOSS increased drug solubility and dissolution in the solid dispersions. Compared with the drug powder, the solubility, dissolution and bioavailability of tacrolimus with the fast-dissolving solid dispersion containing tacrolimus/HP-β-CD/DOSS in the weight ratio of 5:40:4 were boosted by approximately 700-, 30- and 2-fold, respectively. Several tablet formulations were accomplished with this solid dispersion in combination with various ratios of HPMC/ethylcellulose. The release behaviour and pharmacokinetic studies in beagle dogs were assessed compared with the commercial prolonged release capsule. A decrease in HPMC/ethylcellulose ratios reduced the dissolution of tacrolimus from the tablets. Particularly, the tacrolimus-loaded prolonged release tablet consisting of fast-dissolving tacrolimus solid dispersion, HPMC, ethylcellulose and talc at the weight ratio of 20:66:112:2 exhibited a dissolution profile similar to that produced by the commercial prolonged release capsule. Furthermore, there were no significant differences in the AUC, Cmax, Tmax and MRT values between them in beagle dogs. Consequently, this tacrolimus-loaded prolonged release tablet might be bioequivalent to the tacrolimus-loaded commercial capsule.

Authors+Show Affiliations

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.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, 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, Yeungnam University, 214-1, Dae-Dong, Gyongsan 712-749, South Korea. Electronic address: csyong@yumail.ac.kr.College of Pharmacy, Yeungnam University, 214-1, Dae-Dong, Gyongsan 712-749, South Korea; 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

24388864

Citation

Cho, Jung Hyun, et al. "Development of Novel Fast-dissolving Tacrolimus Solid Dispersion-loaded Prolonged Release Tablet." European Journal of Pharmaceutical Sciences : Official Journal of the European Federation for Pharmaceutical Sciences, vol. 54, 2014, pp. 1-7.
Cho JH, Kim YI, Kim DW, et al. Development of novel fast-dissolving tacrolimus solid dispersion-loaded prolonged release tablet. Eur J Pharm Sci. 2014;54:1-7.
Cho, J. H., Kim, Y. I., Kim, D. W., Yousaf, A. M., Kim, J. O., Woo, J. S., Yong, C. S., & Choi, H. G. (2014). Development of novel fast-dissolving tacrolimus solid dispersion-loaded prolonged release tablet. European Journal of Pharmaceutical Sciences : Official Journal of the European Federation for Pharmaceutical Sciences, 54, 1-7. https://doi.org/10.1016/j.ejps.2013.12.016
Cho JH, et al. Development of Novel Fast-dissolving Tacrolimus Solid Dispersion-loaded Prolonged Release Tablet. Eur J Pharm Sci. 2014 Apr 11;54:1-7. PubMed PMID: 24388864.
* Article titles in AMA citation format should be in sentence-case
TY - JOUR T1 - Development of novel fast-dissolving tacrolimus solid dispersion-loaded prolonged release tablet. AU - Cho,Jung Hyun, AU - Kim,Yong-Il, AU - Kim,Dong-Wuk, AU - Yousaf,Abid Mehmood, AU - Kim,Jong Oh, AU - Woo,Jong Soo, AU - Yong,Chul Soon, AU - Choi,Han-Gon, Y1 - 2014/01/01/ PY - 2013/10/11/received PY - 2013/11/28/revised PY - 2013/12/24/accepted PY - 2014/1/7/entrez PY - 2014/1/7/pubmed PY - 2014/10/8/medline KW - Bioequivalence in beagle dogs KW - Ethylcellulose KW - Fast-dissolving solid dispersion KW - Hydroxypropyl methylcellulose KW - Prolonged release tablet KW - Tacrolimus SP - 1 EP - 7 JF - European journal of pharmaceutical sciences : official journal of the European Federation for Pharmaceutical Sciences JO - Eur J Pharm Sci VL - 54 N2 - The goal of this research was to develop a novel prolonged release tablet bioequivalent to the commercial sustained release capsule. A number of tacrolimus-loaded fast-dissolving solid dispersions containing various amounts of DOSS were prepared using the spray drying technique. Their solubility, dissolution and pharmacokinetics in rats were studied. DOSS increased drug solubility and dissolution in the solid dispersions. Compared with the drug powder, the solubility, dissolution and bioavailability of tacrolimus with the fast-dissolving solid dispersion containing tacrolimus/HP-β-CD/DOSS in the weight ratio of 5:40:4 were boosted by approximately 700-, 30- and 2-fold, respectively. Several tablet formulations were accomplished with this solid dispersion in combination with various ratios of HPMC/ethylcellulose. The release behaviour and pharmacokinetic studies in beagle dogs were assessed compared with the commercial prolonged release capsule. A decrease in HPMC/ethylcellulose ratios reduced the dissolution of tacrolimus from the tablets. Particularly, the tacrolimus-loaded prolonged release tablet consisting of fast-dissolving tacrolimus solid dispersion, HPMC, ethylcellulose and talc at the weight ratio of 20:66:112:2 exhibited a dissolution profile similar to that produced by the commercial prolonged release capsule. Furthermore, there were no significant differences in the AUC, Cmax, Tmax and MRT values between them in beagle dogs. Consequently, this tacrolimus-loaded prolonged release tablet might be bioequivalent to the tacrolimus-loaded commercial capsule. SN - 1879-0720 UR - https://www.unboundmedicine.com/medline/citation/24388864/Development_of_novel_fast_dissolving_tacrolimus_solid_dispersion_loaded_prolonged_release_tablet_ L2 - https://linkinghub.elsevier.com/retrieve/pii/S0928-0987(13)00488-0 DB - PRIME DP - Unbound Medicine ER -