Polymers derived from Xanthomonas campesteris and Cyamopsis tetragonolobus used as retardant materials for the formulation of sustained release floating matrix tablet of atenolol.
The objective of the present study was to develop, optimize, in vitro, and in vivo evaluation of floating matrix tablet of atenolol using polymer blend derived from Xanthomonas campesteris and Cyamopsis tetragonolobus that are characterized by release requirements of sustained-release product and to improve the oral bioavailability of the drug. A 3(2) full factorial design was employed to optimize the tablets, where content of polymer blend (X1) and ratio of xanthan gum-to-guar gum (X2) were considered as independent variables. The effects of independent variables on dependent variables, i.e. floating time, diffusion exponent, and time to release 50% of atenolol were evaluated. The in vivo pharmacokinetic parameters of the optimized formulation were compared with the marketed sustained release formulation of atenolol (Aten(®)). The optimized formulation containing 20% (w/w) of polymer blend and 50:50 ratio of xanthan gum-to-guar gum was able to float more than 12h and showed the desired sustained drug release from the tablets. In vivo retention studies in rabbit stomach showed the gastric residence of tablet up to 6h. The in vivo study of optimized tablets illustrated significant improvement in the oral bioavailability of atenolol in rabbits. It can be concluded that floating matrix tablet of atenolol prepared by using xanthan gum and guar gum has potential for sustained release of the drug as well as improved oral bioavailability through enhanced gastric residence time of formulation in stomach.
Department of Pharmaceutical Sciences, Dibrugarh University, Dibrugarh 786004, Assam, India; Bengal College of Pharmaceutical Sciences & Research, B.R.B. Sarani, Bidhannagar, Durgapur 713212, West Bengal, India.
Sanjay
S
Dey
Department of Pharmaceutical Sciences, Dibrugarh University, Dibrugarh 786004, Assam, India. Electronic address: bhmaz@yahoo.co.in.
Bhaskar
B
Mazumder
Radiopharmaceuticals Laboratory, Board of Radiation and Isotope Technology, Variable Energy Cyclotron Centre, Kolkata 700064, West Bengal, India.
Sankha
S
Chattopadhyay
Radiopharmaceuticals Laboratory, Board of Radiation and Isotope Technology, Variable Energy Cyclotron Centre, Kolkata 700064, West Bengal, India.
Malay Kanti
MK
Das
Regional Radiation and Medicine Centre, Variable Energy Cyclotron Centre, Kolkata 700064, West Bengal, India.
Samarendu
S
Sinha
Regional Radiation and Medicine Centre, Variable Energy Cyclotron Centre, Kolkata 700064, West Bengal, India.
Shantanu
S
Ganguly
Infectious Diseases and Immunology, Indian Institute of Chemical Biology, Jadavpur, Kolkata 700032, West Bengal, India.
Kakali
K
De
Infectious Diseases and Immunology, Indian Institute of Chemical Biology, Jadavpur, Kolkata 700032, West Bengal, India.
Mridula
M
Mishra
D000818:Animals; D001262:Atenolol / Q000008:administration & dosage / Q000737:chemistry* / Q000378:metabolism / Q000493:pharmacokinetics; D001704:Biopolymers / Q000737:chemistry*; D002626:Chemistry, Pharmaceutical / Q000379:methods*; D031293:Cyamopsis / Q000737:chemistry*; D003692:Delayed-Action Preparations; D004355:Drug Stability; D005260:Female; D005753:Gastric Mucosa / Q000378:metabolism; D006244:Hardness; D008297:Male; D011817:Rabbits; D011854:Radiochemistry; D013607:Tablets; D014974:Xanthomonas / Q000737:chemistry*
D001704:Biopolymers; D003692:Delayed-Action Preparations; D013607:Tablets; D001262:Atenolol
Atenolol; Floating matrix tablet; Guar gum; Optimization; Xanthan gum