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New clopidogrel napadisilate salt and its solid dispersion with improved stability and bioequivalence to the commercial clopidogrel bisulphate salt in beagle dogs.
Int J Pharm. 2011 Aug 30; 415(1-2):129-39.IJ

Abstract

The purpose of this study was to develop a novel clopidogrel napadisilate-loaded solid dispersion with improved stability and bioequivalence to the clopidogrel bisulphate-loaded commercial product. Clopidogrel napadisilate prepared in this study appeared as a white crystalline powder unlike clopidogrel base. However, this salt did not improve the solubility of clopidogrel, even with improved stability compared to clopidogrel bisulphate. To improve the solubility of clopidogrel napadisilate, a novel clopidogrel napadisilate-loaded solid dispersion was prepared by the spray-drying technique using HPMC and colloidal silica, and the physicochemical properties, dissolution and bioavailability in beagle dogs were evaluated compared to the clopidogrel bisulphate-loaded commercial product. The solid dispersion composed of clopidogrel napadisilate, HPMC and colloidal silica at a weight ratio of 11.069/3/3.5 improved solubility by 6.5-fold compared to clopidogrel napadisilate, even if it did not improve drug solubility compared to clopidogrel bisulphate. However, unlike clopidogrel bisulphate, this formulation improved the stability of clopidogrel. Furthermore, the clopidogrel napadisilate solid dispersion-loaded tablet showed similar dissolution to the clopidogrel bisulphate-loaded commercial product and was bioequivalent to the commercial product in beagle dogs. Thus, this clopidogrel napadisilate-loaded solid dispersion could be a promising candidate for improving the stability and bioavailability of clopidogrel.

Authors+Show Affiliations

College of Pharmacy, Yeungnam University, 214-1 Dae-Dong, Gyongsan 712-749, South Korea.No affiliation info availableNo affiliation info availableNo affiliation info availableNo affiliation info availableNo affiliation info availableNo affiliation info available

Pub Type(s)

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

Language

eng

PubMed ID

21645599

Citation

Kim, Yong-Il, et al. "New Clopidogrel Napadisilate Salt and Its Solid Dispersion With Improved Stability and Bioequivalence to the Commercial Clopidogrel Bisulphate Salt in Beagle Dogs." International Journal of Pharmaceutics, vol. 415, no. 1-2, 2011, pp. 129-39.
Kim YI, Kim KS, Suh KH, et al. New clopidogrel napadisilate salt and its solid dispersion with improved stability and bioequivalence to the commercial clopidogrel bisulphate salt in beagle dogs. Int J Pharm. 2011;415(1-2):129-39.
Kim, Y. I., Kim, K. S., Suh, K. H., Shanmugam, S., Woo, J. S., Yong, C. S., & Choi, H. G. (2011). New clopidogrel napadisilate salt and its solid dispersion with improved stability and bioequivalence to the commercial clopidogrel bisulphate salt in beagle dogs. International Journal of Pharmaceutics, 415(1-2), 129-39. https://doi.org/10.1016/j.ijpharm.2011.05.059
Kim YI, et al. New Clopidogrel Napadisilate Salt and Its Solid Dispersion With Improved Stability and Bioequivalence to the Commercial Clopidogrel Bisulphate Salt in Beagle Dogs. Int J Pharm. 2011 Aug 30;415(1-2):129-39. PubMed PMID: 21645599.
* Article titles in AMA citation format should be in sentence-case
TY - JOUR T1 - New clopidogrel napadisilate salt and its solid dispersion with improved stability and bioequivalence to the commercial clopidogrel bisulphate salt in beagle dogs. AU - Kim,Yong-Il, AU - Kim,Kyung Soo, AU - Suh,Kwee-Hyun, AU - Shanmugam,Srinivasan, AU - Woo,Jong Soo, AU - Yong,Chul Soon, AU - Choi,Han-Gon, Y1 - 2011/05/27/ PY - 2011/03/01/received PY - 2011/05/13/revised PY - 2011/05/23/accepted PY - 2011/6/8/entrez PY - 2011/6/8/pubmed PY - 2011/12/13/medline SP - 129 EP - 39 JF - International journal of pharmaceutics JO - Int J Pharm VL - 415 IS - 1-2 N2 - The purpose of this study was to develop a novel clopidogrel napadisilate-loaded solid dispersion with improved stability and bioequivalence to the clopidogrel bisulphate-loaded commercial product. Clopidogrel napadisilate prepared in this study appeared as a white crystalline powder unlike clopidogrel base. However, this salt did not improve the solubility of clopidogrel, even with improved stability compared to clopidogrel bisulphate. To improve the solubility of clopidogrel napadisilate, a novel clopidogrel napadisilate-loaded solid dispersion was prepared by the spray-drying technique using HPMC and colloidal silica, and the physicochemical properties, dissolution and bioavailability in beagle dogs were evaluated compared to the clopidogrel bisulphate-loaded commercial product. The solid dispersion composed of clopidogrel napadisilate, HPMC and colloidal silica at a weight ratio of 11.069/3/3.5 improved solubility by 6.5-fold compared to clopidogrel napadisilate, even if it did not improve drug solubility compared to clopidogrel bisulphate. However, unlike clopidogrel bisulphate, this formulation improved the stability of clopidogrel. Furthermore, the clopidogrel napadisilate solid dispersion-loaded tablet showed similar dissolution to the clopidogrel bisulphate-loaded commercial product and was bioequivalent to the commercial product in beagle dogs. Thus, this clopidogrel napadisilate-loaded solid dispersion could be a promising candidate for improving the stability and bioavailability of clopidogrel. SN - 1873-3476 UR - https://www.unboundmedicine.com/medline/citation/21645599/New_clopidogrel_napadisilate_salt_and_its_solid_dispersion_with_improved_stability_and_bioequivalence_to_the_commercial_clopidogrel_bisulphate_salt_in_beagle_dogs_ L2 - https://linkinghub.elsevier.com/retrieve/pii/S0378-5173(11)00507-2 DB - PRIME DP - Unbound Medicine ER -