Studies on biological macromolecules lipid-Gelucire based gastroretentive multiparticulate.
Studies on biological macromolecules lipid-Gelucire based sustained release gastroretentive multiparticulates of metformin hydrochloride (MH) were developed by dispersing MH in melted Gelucire 39/01 and 43/01 using the melt granulation technique while fast release solid dispersions gastroretentive multiparticulates of glibenclamide (GLB), poorly soluble drug were developed using Gelucire 50/13 and PEG 200, 400, 4000, 6000 as carrier at different ratios. Percent drug entrapment of MH was 99.6±0.35% and in vitro floating ability was 11.3±0.47h. Model dependent analysis shows that zero order kinetics was followed while drug release mechanism was anomalous diffusion controlled. Combination of ethylcellulose, methylcellulose and microcrystalline cellulose with Gelucire were explored for release of drug, floatability and consistency for optimized formulation. While GLB multiparticulates showed entrapment efficiency of 99.8±0.11%, in vitro buoyancy for 11±0.2h and improved solubility and dissolution rate. Zero order kinetics was promising for all formulations. Model independent analysis f2 value for GIV was 40 while for M II was 54. Characterization was done by SEM, FTIR and PXRD. RP-HPLC method was adopted for simultaneous pharmacokinetic analysis of the drugs in rat plasma. In IVIVC studies confirm increased bioavailability of drugs in combination form and followed level A correlation using the diabetic type II Wistar rat.
Department of Pharmaceutics, College of Pharmacy, IFTM, Moradabad 244102, Uttar Pradesh, India; Uttar Pradesh Technical University, Lucknow, India. Electronic address: p23upadhyay@yahoo.com.
Prashant
P
Upadhyay
Department of Pharmaceutics, IIT-Banaras Hindu University (BHU), Varanasi, Uttar Pradesh 221010, India.
Jayanta Kumar
JK
Pandit
Department of Pharmaceutics, IIT-Banaras Hindu University (BHU), Varanasi, Uttar Pradesh 221010, India.
Arun Kumar
AK
Wahi
D000818:Animals; D001682:Biological Availability; D004058:Diffusion; D016503:Drug Delivery Systems; D005223:Fats / Q000008:administration & dosage* / Q000737:chemistry; D065569:Gastrointestinal Absorption; D006801:Humans; D007700:Kinetics; D008055:Lipids / Q000008:administration & dosage / Q000737:chemistry; D008687:Metformin / Q000008:administration & dosage* / Q000737:chemistry; D009821:Oils / Q000008:administration & dosage* / Q000737:chemistry; D011092:Polyethylene Glycols / Q000737:chemistry; D051381:Rats; D012995:Solubility
D005223:Fats; D008055:Lipids; D009821:Oils; C071184:Gelucire 50-13; D011092:Polyethylene Glycols; D008687:Metformin
Bioavailability; Biological macromolecules; Gastroretentive multiparticulates; In vitro–in vivo correlation (IVIVC); Lipid-Gelucire