BIOAVAILABILITY STUDY OF PHYSICAL MIXTURE OF CARBAMAZEPINE AND AMINO ACIDS
Objective: This study aimed to evaluate the bioavailability of physical mixture (PM) of carbamazepine (CBZ) and amino acids (glycine, alanine,
and lysine), includes a parameter tmax, Cmax and AUC0-12.
Methods: PM made by weighing CBZ with amino acids (glycine, alanine, and lysine) equimolar and mix both components with a mortar until a
homogeneous mixture. PM obtained was characterized using differential thermal analysis (DTA), Fourier transform infrared (FTIR) and optical
microscopy. Bioavailability was conducted after obtaining ethical clearance from Faculty of Veterinary Airlangga University to five New Zealand
Rabbits for each treatment. CBZ levels in blood plasma were determined by HPLC analysis method.
Results: The results of the DTA thermogram and infrared spectra showed that CBZ compound mixed with the components of the constituent amino
acids. Time achieve maximum levels value (tmax) PM of CBZ-GLY, CBZ-ALA, and CBZ-LYS, respectively, for 5.09, 3.85, and 3.93 hours faster than the tmax
value of CBZ at 6.14 hours. Cmax value of PM CBZ-LYS at 4.85 mg/mL higher than CBZ at 2.56 mg/mL and AUC0-12 value PM CBZ-LYS at 37.31 hrs ug/mL
greater than CBZ at 20.59 Î¼g hrs/mL.
Conclusion: From the research can be concluded that PM able to improve the bioavailability of CBZ. The value tmax of PM CBZ-amino acids (GLY, ALA,
and LYS) faster than CBZ. PM of CBZ-LYS provides Cmax and AUC0-12 value greater than CBZ compounds.
Keywords: Carbamazepine, Glycine, Alanine, Lysine, Physical mixture, Bioavailability.
Ja yasutha J, Bhargavdilip S, Kishore K, Ramasany C. Comparasion
of efficacy and safety of Carbamazepine and Eslicarbamazepine
in adult partial and generalized seizures. Asian J Phram Clin Res
Koester LS, Bertuol JB, Groch KR, Xavier CR, Moellerke R,
Mayorga P, et al. Bioavailability of carbamazepine: beta-cyclodextrin
complex in beagle dogs from hydroxypropylmethylcellulose matrix
tablets. Eur J Pharm Sci 2004;22(2-3):201-7.
Ansel HC, Popovich NG, Allen LV. Pharmaceutical Dosage Form and
Drug Delivery System. 9th ed. Malvern: Williams and Wilkins; 2011.
Jatwani S, Rana AC, Singh G. An overview on solubility enhancement
techniques for poorly soluble drugs and solid dispersion as an eminent
strategic approach. Int J Pharm Sci Res 2011;3(4):942-56.
Chandaramouli Y, Gandhimathi R, Yasmeen BR, Vikram A, Mahitha B,
Imroz SM. Review on cocrystal as an approach with never implications
in pharmaceutical field. Int J Med Chem Anal 2012;2(2):91-100.
Isadiartuti D, Budiati T, Martodihardjo S. Solubility and dissolution
study of physical mixture of carbamazepine and amino acids. Int J
Pharm Pharm Sci 2014;6(1):301-6.
Bhise SB, Rajkumar M. Effect of HPMC on solubility and dissolution
of carbamazepine form III in simulated gastrointestinal fluids. Asian J
Kobayashi Y, Ito S, Itai S, Yamamoto K. Physicochemical properties
and bioavailability of carbamazepine polymorphs and dihydrate. Int J
Shargel L, Wu-Pong S, Yu ABC. Applied Biopharmaceutical
Pharmacokinetics. 5th ed. Boston: The McGraw Hill Companies; 2005.
p. 371-91, 411-8.
Sinko PJ, Singh Y. Martinâ€™s Physical Pharmacy and Pharmaceutical
Sciences: Physical Chemical and Biopharmaceutics Principles in the
Pharmaceutical Sciences. 6th ed. Baltimore: Lippincott Wiliams &
Ali W, Badawi AA, Mahdy MA, Hanan ME. Formulation and evaluation
of carbamazepine 200 mg immediate release tablets using polyethylene
glycol 6000. Int J Pharm Pharm Sci 2013;5(1):114-9.
Grzesiak AL, Lang M, Kim K, Matzger AJ. Comparison of the four
anhydrous polymorphs of carbamazepine and the crystal structure of
form I. J Pharm Sci 2003;92(11):2260-71.
Prajapati ST, Gohel MC, Patel LD. Studies to enhance dissolution
properties of carbamazepine. Indian J Pharm Sci 2007; 69(3):427-30.
Carino SR, Sperry DC, Hawley M. Relative bioavailability estimation
of carbamazepine crystal forms using an artificial stomach-duodenum
model. J Pharm Sci 2006;95(1):116-25.
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