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In vitro and in vivo evaluation of novel immediate release carbamazepine tablets: complexation with hydroxypropyl-β-cyclodextrin in the presence of HPMC.
Int J Pharm. 2011 May 16; 409(1-2):75-80.IJ

Abstract

Carbamazepine (CBZ)-hydroxypropyl-β-cyclodextrin (HP-β-CD) complex in the presence of HPMC was prepared and characterized by differential scanning calorimetry (DSC) and X-ray diffractometer intended for improving the dissolution rate of CBZ. The phase-solubility method was used to investigate the effect of HP-β-CD and HPMC on the solubility of CBZ. Tablets of the resulting complex were prepared using direct compression method and the bioavailability was evaluated in beagle dogs using a UPLC/MS/MS method. The results showed solubility of CBZ was increased up to 95 times by complexation with HP-β-CD in the presence of 0.1% HPMC. The results of DSC and X-ray diffraction proved a formation of complex between CBZ and HP-β-CD. Dissolution rate of CBZ was notably improved from complex tablets with more than 97.39% released within 10 min; whereas for the commercial tablets, around 60% was released within 30 min. Using commercial tablets as the reference formulation, the bioavailability of complex tablets was considerably increased by 1.5-fold (P<0.05) and T(max) was reduced to 0.88 h compared with 1.25 h for commercial tablets. Furthermore, a lower inter-subject variability (49.9%) was observed compared with that of the commercial tablets (39.7%). It is evident from the results herein that complexation with HP-β-CD in the presence of HPMC is a feasible way to prepare a rapidly acting and better absorbed CBZ oral product.

Authors+Show Affiliations

School of Pharmacy, Shenyang Pharmaceutical University, Mailbox 59#, 103 Wenhua Road, Shenyang 110016, Liaoning Province, PR China. kouwen1224@126.comNo affiliation info availableNo affiliation info availableNo affiliation info availableNo affiliation info availableNo affiliation info availableNo affiliation info available

Pub Type(s)

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

Language

eng

PubMed ID

21371541

Citation

Kou, Wen, et al. "In Vitro and in Vivo Evaluation of Novel Immediate Release Carbamazepine Tablets: Complexation With Hydroxypropyl-β-cyclodextrin in the Presence of HPMC." International Journal of Pharmaceutics, vol. 409, no. 1-2, 2011, pp. 75-80.
Kou W, Cai C, Xu S, et al. In vitro and in vivo evaluation of novel immediate release carbamazepine tablets: complexation with hydroxypropyl-β-cyclodextrin in the presence of HPMC. Int J Pharm. 2011;409(1-2):75-80.
Kou, W., Cai, C., Xu, S., Wang, H., Liu, J., Yang, D., & Zhang, T. (2011). In vitro and in vivo evaluation of novel immediate release carbamazepine tablets: complexation with hydroxypropyl-β-cyclodextrin in the presence of HPMC. International Journal of Pharmaceutics, 409(1-2), 75-80. https://doi.org/10.1016/j.ijpharm.2011.02.042
Kou W, et al. In Vitro and in Vivo Evaluation of Novel Immediate Release Carbamazepine Tablets: Complexation With Hydroxypropyl-β-cyclodextrin in the Presence of HPMC. Int J Pharm. 2011 May 16;409(1-2):75-80. PubMed PMID: 21371541.
* Article titles in AMA citation format should be in sentence-case
TY - JOUR T1 - In vitro and in vivo evaluation of novel immediate release carbamazepine tablets: complexation with hydroxypropyl-β-cyclodextrin in the presence of HPMC. AU - Kou,Wen, AU - Cai,Cuifang, AU - Xu,Shuying, AU - Wang,Huan, AU - Liu,Jing, AU - Yang,Dan, AU - Zhang,Tianhong, Y1 - 2011/03/01/ PY - 2010/11/28/received PY - 2011/01/25/revised PY - 2011/02/20/accepted PY - 2011/3/5/entrez PY - 2011/3/5/pubmed PY - 2011/8/13/medline SP - 75 EP - 80 JF - International journal of pharmaceutics JO - Int J Pharm VL - 409 IS - 1-2 N2 - Carbamazepine (CBZ)-hydroxypropyl-β-cyclodextrin (HP-β-CD) complex in the presence of HPMC was prepared and characterized by differential scanning calorimetry (DSC) and X-ray diffractometer intended for improving the dissolution rate of CBZ. The phase-solubility method was used to investigate the effect of HP-β-CD and HPMC on the solubility of CBZ. Tablets of the resulting complex were prepared using direct compression method and the bioavailability was evaluated in beagle dogs using a UPLC/MS/MS method. The results showed solubility of CBZ was increased up to 95 times by complexation with HP-β-CD in the presence of 0.1% HPMC. The results of DSC and X-ray diffraction proved a formation of complex between CBZ and HP-β-CD. Dissolution rate of CBZ was notably improved from complex tablets with more than 97.39% released within 10 min; whereas for the commercial tablets, around 60% was released within 30 min. Using commercial tablets as the reference formulation, the bioavailability of complex tablets was considerably increased by 1.5-fold (P<0.05) and T(max) was reduced to 0.88 h compared with 1.25 h for commercial tablets. Furthermore, a lower inter-subject variability (49.9%) was observed compared with that of the commercial tablets (39.7%). It is evident from the results herein that complexation with HP-β-CD in the presence of HPMC is a feasible way to prepare a rapidly acting and better absorbed CBZ oral product. SN - 1873-3476 UR - https://www.unboundmedicine.com/medline/citation/21371541/In_vitro_and_in_vivo_evaluation_of_novel_immediate_release_carbamazepine_tablets:_complexation_with_hydroxypropyl_β_cyclodextrin_in_the_presence_of_HPMC_ L2 - https://linkinghub.elsevier.com/retrieve/pii/S0378-5173(11)00177-3 DB - PRIME DP - Unbound Medicine ER -