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Preparation, characterization and in vivo evaluation of formulation of baicalein with hydroxypropyl-beta-cyclodextrin.
Int J Pharm. 2006 Apr 07; 312(1-2):137-43.IJ

Abstract

The interaction of 2-hydroxypropyl-beta-cyclodextrin (HP-beta-CD) and a poorly water-soluble flavonoid, baicalein (Ba), chemically 5,6,7-trihydroxy flavone in solution and solid-state was studied. Ba/HP-beta-CD solid systems were prepared by freeze-drying method. The formation of Ba/HP-beta-CD complex in aqueous solution was demonstrated by UV spectroscopy, while Ba/HP-beta-CD co-lyophilized product was characterized by differential scanning calorimetry (DSC) and X-ray diffractometry (XRD). Through complexation with HP-beta-CD, the solubility of Ba in neutral aqueous solution was improved significantly. The phase-solubility profile was AP-type, indicating the formation of higher-order complexes or complex aggregates. Ba/HP-beta-CD solid powders were amorphous and show a significantly improved dissolution rate in comparison with free Ba. Comparison of the pharmacokinetics between Ba/HP-beta-CD co-lyophilized product and free Ba was also performed in rats. The concentration of Ba and its mainly conjugated metabolite, 7-O-glucuronide of baicalein (BG) in rat plasma was determined by HPLC method. The in vivo results show that Ba/HP-beta-CD co-lyophilized product exhibits the similar pharmacokinetics as that of free Ba after intravenous administration. Ba/HP-beta-CD co-lyophilized product displays earlier tmax and higher Cmax of BG than free Ba after oral dosing. By comparing the AUC0-infinity of BG between oral dosing, the relative bioavailability of Ba/HP-beta-CD co-lyophilized product to free Ba was 165.0%, which highlighted the evidence of significantly improved bioavailability of formulation of Ba with HP-beta-CD.

Authors+Show Affiliations

College of Pharmaceutical Sciences, Zhejiang University, Hangzhou 310031, PR China.No affiliation info availableNo affiliation info availableNo affiliation info available

Pub Type(s)

Journal Article

Language

eng

PubMed ID

16459034

Citation

Liu, Jun, et al. "Preparation, Characterization and in Vivo Evaluation of Formulation of Baicalein With Hydroxypropyl-beta-cyclodextrin." International Journal of Pharmaceutics, vol. 312, no. 1-2, 2006, pp. 137-43.
Liu J, Qiu L, Gao J, et al. Preparation, characterization and in vivo evaluation of formulation of baicalein with hydroxypropyl-beta-cyclodextrin. Int J Pharm. 2006;312(1-2):137-43.
Liu, J., Qiu, L., Gao, J., & Jin, Y. (2006). Preparation, characterization and in vivo evaluation of formulation of baicalein with hydroxypropyl-beta-cyclodextrin. International Journal of Pharmaceutics, 312(1-2), 137-43.
Liu J, et al. Preparation, Characterization and in Vivo Evaluation of Formulation of Baicalein With Hydroxypropyl-beta-cyclodextrin. Int J Pharm. 2006 Apr 7;312(1-2):137-43. PubMed PMID: 16459034.
* Article titles in AMA citation format should be in sentence-case
TY - JOUR T1 - Preparation, characterization and in vivo evaluation of formulation of baicalein with hydroxypropyl-beta-cyclodextrin. AU - Liu,Jun, AU - Qiu,Liyan, AU - Gao,Jianqing, AU - Jin,Yi, Y1 - 2006/02/03/ PY - 2005/08/31/received PY - 2006/01/05/revised PY - 2006/01/09/accepted PY - 2006/2/7/pubmed PY - 2006/8/30/medline PY - 2006/2/7/entrez SP - 137 EP - 43 JF - International journal of pharmaceutics JO - Int J Pharm VL - 312 IS - 1-2 N2 - The interaction of 2-hydroxypropyl-beta-cyclodextrin (HP-beta-CD) and a poorly water-soluble flavonoid, baicalein (Ba), chemically 5,6,7-trihydroxy flavone in solution and solid-state was studied. Ba/HP-beta-CD solid systems were prepared by freeze-drying method. The formation of Ba/HP-beta-CD complex in aqueous solution was demonstrated by UV spectroscopy, while Ba/HP-beta-CD co-lyophilized product was characterized by differential scanning calorimetry (DSC) and X-ray diffractometry (XRD). Through complexation with HP-beta-CD, the solubility of Ba in neutral aqueous solution was improved significantly. The phase-solubility profile was AP-type, indicating the formation of higher-order complexes or complex aggregates. Ba/HP-beta-CD solid powders were amorphous and show a significantly improved dissolution rate in comparison with free Ba. Comparison of the pharmacokinetics between Ba/HP-beta-CD co-lyophilized product and free Ba was also performed in rats. The concentration of Ba and its mainly conjugated metabolite, 7-O-glucuronide of baicalein (BG) in rat plasma was determined by HPLC method. The in vivo results show that Ba/HP-beta-CD co-lyophilized product exhibits the similar pharmacokinetics as that of free Ba after intravenous administration. Ba/HP-beta-CD co-lyophilized product displays earlier tmax and higher Cmax of BG than free Ba after oral dosing. By comparing the AUC0-infinity of BG between oral dosing, the relative bioavailability of Ba/HP-beta-CD co-lyophilized product to free Ba was 165.0%, which highlighted the evidence of significantly improved bioavailability of formulation of Ba with HP-beta-CD. SN - 0378-5173 UR - https://www.unboundmedicine.com/medline/citation/16459034/Preparation_characterization_and_in_vivo_evaluation_of_formulation_of_baicalein_with_hydroxypropyl_beta_cyclodextrin_ L2 - https://linkinghub.elsevier.com/retrieve/pii/S0378-5173(06)00039-1 DB - PRIME DP - Unbound Medicine ER -