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Studies on preparation of carbamazepine (CBZ) supersaturatable self-microemulsifying (S-SMEDDS) formulation and relative bioavailability in beagle dogs.
Pharm Dev Technol. 2011 Aug; 16(4):415-21.PD

Abstract

The main purpose of this work was to develop a supersaturatable self-microemulsifying drug delivery system (S-SMEDDS) of carbamazepine (CBZ). S-SMEDDS of CBZ was prepared and drug precipitation behavior, dissolution rate in vitro and particle size distribution were evaluated. The relative bioavailability of S-SMEDDS formulation of CBZ was evaluated in beagle dogs compared with a commercial tablet. The results showed that the presence of a small amount of polymeric precipitation inhibitor (PVP) effectively sustained the supersaturated state by retarding precipitation kinetics. The mean particle size of S-SMEDDS formulation after dispersion was about 33.7?nm and the release rate from S-SMEDDS was significantly higher than the commercial tablet in vitro. In pharmacokinetic parameters of S-SMEDDS formulation, AUC(0?t) and C(max) were 9.83???2.47??g?ml(?1)?h and 4.96???1.16??g?ml(?1), compared to the conventional tablet which were 1.67???1.19??g?ml(?1)?h and 0.74???0.19??g?ml(?1), respectively. AUC(0-t) of S-SMEDDS increased nearly five times compared to the market tablet with the same administration dose of 200?mg. On the other hand, AUC(0?t) of S-SMEDDS with a dose of 50?mg was about 85.9% compared to the commercial tablet with a dose of 200?mg. Thus, it was concluded that S-SMEDDS provide an effective approach for improving the extent of absorption of CBZ with a low surfactant level.

Authors+Show Affiliations

Institute of Pharmacology and Toxicology, Academy of Military Medical Sciences, Beijing, China.No 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

20433250

Citation

Zhang, Nan, et al. "Studies On Preparation of Carbamazepine (CBZ) Supersaturatable Self-microemulsifying (S-SMEDDS) Formulation and Relative Bioavailability in Beagle Dogs." Pharmaceutical Development and Technology, vol. 16, no. 4, 2011, pp. 415-21.
Zhang N, Zhang W, Jin Y, et al. Studies on preparation of carbamazepine (CBZ) supersaturatable self-microemulsifying (S-SMEDDS) formulation and relative bioavailability in beagle dogs. Pharm Dev Technol. 2011;16(4):415-21.
Zhang, N., Zhang, W., Jin, Y., & Quan, D. Q. (2011). Studies on preparation of carbamazepine (CBZ) supersaturatable self-microemulsifying (S-SMEDDS) formulation and relative bioavailability in beagle dogs. Pharmaceutical Development and Technology, 16(4), 415-21. https://doi.org/10.3109/10837451003774419
Zhang N, et al. Studies On Preparation of Carbamazepine (CBZ) Supersaturatable Self-microemulsifying (S-SMEDDS) Formulation and Relative Bioavailability in Beagle Dogs. Pharm Dev Technol. 2011;16(4):415-21. PubMed PMID: 20433250.
* Article titles in AMA citation format should be in sentence-case
TY - JOUR T1 - Studies on preparation of carbamazepine (CBZ) supersaturatable self-microemulsifying (S-SMEDDS) formulation and relative bioavailability in beagle dogs. AU - Zhang,Nan, AU - Zhang,Weidong, AU - Jin,Yinghua, AU - Quan,Dong-qin, Y1 - 2010/04/30/ PY - 2010/5/4/entrez PY - 2010/5/4/pubmed PY - 2012/2/11/medline SP - 415 EP - 21 JF - Pharmaceutical development and technology JO - Pharm Dev Technol VL - 16 IS - 4 N2 - The main purpose of this work was to develop a supersaturatable self-microemulsifying drug delivery system (S-SMEDDS) of carbamazepine (CBZ). S-SMEDDS of CBZ was prepared and drug precipitation behavior, dissolution rate in vitro and particle size distribution were evaluated. The relative bioavailability of S-SMEDDS formulation of CBZ was evaluated in beagle dogs compared with a commercial tablet. The results showed that the presence of a small amount of polymeric precipitation inhibitor (PVP) effectively sustained the supersaturated state by retarding precipitation kinetics. The mean particle size of S-SMEDDS formulation after dispersion was about 33.7?nm and the release rate from S-SMEDDS was significantly higher than the commercial tablet in vitro. In pharmacokinetic parameters of S-SMEDDS formulation, AUC(0?t) and C(max) were 9.83???2.47??g?ml(?1)?h and 4.96???1.16??g?ml(?1), compared to the conventional tablet which were 1.67???1.19??g?ml(?1)?h and 0.74???0.19??g?ml(?1), respectively. AUC(0-t) of S-SMEDDS increased nearly five times compared to the market tablet with the same administration dose of 200?mg. On the other hand, AUC(0?t) of S-SMEDDS with a dose of 50?mg was about 85.9% compared to the commercial tablet with a dose of 200?mg. Thus, it was concluded that S-SMEDDS provide an effective approach for improving the extent of absorption of CBZ with a low surfactant level. SN - 1097-9867 UR - https://www.unboundmedicine.com/medline/citation/20433250/Studies_on_preparation_of_carbamazepine__CBZ__supersaturatable_self_microemulsifying__S_SMEDDS__formulation_and_relative_bioavailability_in_beagle_dogs_ L2 - https://www.tandfonline.com/doi/full/10.3109/10837451003774419 DB - PRIME DP - Unbound Medicine ER -