Abstract
In the treatment of type 2 diabetes mellitus a continuous therapy is required which is a more complex one. As in these patients there may be a defect in both insulin secretion and insulin action exists. Hence, the treatment depends on the pathophysiology and the disease state. In the present study, multilayered tablets of pioglitazone hydrochloride 15 mg and metformin hydrochloride 500 mg were prepared in an attempt for combination therapy for the treatment of type 2 diabetes mellitus. Pioglitazone HCl was formulated as immediate release layer to show immediate action by direct compression method using combination of superdisintegrants, namely, crospovidone and avicel PH 102. Crospovidone at 20% concentration showed good drug release profile at 2 hrs. Metformin HCl was formulated as controlled release layer to prolong the drug action by incorporating hydrophilic polymers such as HPMC K4M by direct compression method and guar gum by wet granulation method in order to sustain the drug release from the tablets and maintain its integrity so as to provide a suitable formulation. The multilayered tablets were prepared after carrying out the optimization of immediate release layer and were evaluated for various precompression and postcompression parameters. Formulation F13 showed 99.97% of pioglitazone release at 2 hrs in 0.1 N HCl and metformin showed 98.81% drug release at 10 hrs of dissolution in 6.8 pH phosphate buffer. The developed formulation is equivalent to innovator product in view of in vitro drug release profile. The results of all these evaluation tests are within the standards. The procedure followed for the formulation of these tablets was found to be reproducible and all the formulations were stable after accelerated stability studies. Hence, multilayered tablets of pioglitazone HCl and metformin HCl can be a better alternative way to conventional dosage forms.
Highlights
A drug delivery system (DDS) is defined as a formulation or a device that enables the introduction of a therapeutic substance in the body and improves its efficacy and safety by controlling the rate, time, and place of release of drugs in the body
Solubility of pioglitazone decreases with increase in pH and metformin is freely soluble drug, pioglitazone is formulated as immediate release layer, and metformin is formulated as controlled release layer
Pioglitazone and metformin were obtained as a gift samples from Dr Reddy’s laboratories, Hyderabad and MSN formulations, Hyderabad, respectively, HPMC K4M and crospovidone were procured from Nihal traders, Hyderabad, guar gum is the grounded endosperm of Cyamopsis tetragonolobus, and all the remaining chemicals are of analytical grade
Summary
A drug delivery system (DDS) is defined as a formulation or a device that enables the introduction of a therapeutic substance in the body and improves its efficacy and safety by controlling the rate, time, and place of release of drugs in the body. An appropriately designed controlled-release drug delivery system (CRDDS) can improve the therapeutic efficacy and safety of a drug by precise temporal and spatial placement in the body, thereby reducing both the size and number of doses required. The main objective of controlled/sustained release drug delivery is to make sure of safety and to improve effectiveness of drugs as well as patient compliance. Solubility of pioglitazone decreases with increase in pH and metformin is freely soluble drug, pioglitazone is formulated as immediate release layer, and metformin is formulated as controlled release layer This type of combination will give better compliance [10,11,12,13,14]. It has been used as an appetite suppressant [15,16,17]
Sign-in/Register to view highlights & summary Sign-in/Register to access full text options 
Talk to us
Join us for a 30 min session where you can share your feedback and ask us any queries you have
Schedule a call
