Development, In-Vitro and Ex-Vivo Evaluation of Muco-Adhesive Buccal Tablets Of Hydralazine Hydrochloride

Hydralazine hydrochloride is an anti-hypertensive drug. The drug has poor oral bioavailability (BA) of about 30- 50% due to extensive first-pass metabolism. Hence, the buccal delivery was used to enhance the BA of hydralazine hydrochloride. Buccal muco-adhesive tablets were prepared by direct compression technique, using carbopol 934P, HPMC K₄M, sodium alginate and sodium carboxy methyl cellulose (NaCMC) as muco-adhesive polymers. Prepared formulations were evaluated for physico-chemical characterization, ex-vivo residence time and in-vitro release studies. The some of the parameters viz hardness, thickness, weight variation are showing the values within the pharmacopeial limits. However, the swelling and bio-adhesive strength were increased with increasing polymer concentrations. From the in-vitro release studies, F9 buccal tablets prepared with NaCMC exhibited better release (96.56%, 6 h) profile than all other formulations and considerd as optimized. The release mechanism from kinetic methods suggests that, the drug release follows zero-order kinetics with diffusion mechanism. Thus, the buccal tablets of hydralazine hydrochloride showed enhanced BA and were further confirmed by in-vivo studies.

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Materials

Hydralazine hydrochloride was obtained as a gift sample from Stride’s lab, Bangalore India. Carbopol 934P was obtained from S.D. Fine Chemicals, Mumbai. Hydroxy propyl methyl cellulose (HPMC K4M) and sodium carboxy methyl cellulose (Na-CMC) was obtained from Loba chemicals, Mumbai. Micro crystalline cellulose (MCC) obtained from Laksmi chemicals, India PEG 6000 obtained from India glycol Pvt Ltd., Mumbai, India. All other ingredients used in formulations were of analytical grade.

Kumara Swamy Samanthula , Mahendra Kumar,Agaiah Goud Bairi, Shobha Rani Satla
Braz. J. Pharm. Sci. 2022;58: e18635
https://doi.org/10.1590/s2175-97902020000318635