Abstract
Objective: The present study aimed to develop a new SR metformin hydrochloride (MH) gastroretentive formulation with novel excipient (NE), which has better floatation and can be prepared with more simple pharmaceutical techniques for the treatment of diabetes Mellitus.
 Methods: A gastro-retentive floating matrix tablet (GFT) formulation of MH was prepared using various concentrations of PEO (Polyox WSR-303) and hydroxypropyl methylcellulose K100M (HPMC K100 M) and Floating agent (novel excipient) to achieve desirable TFT, FLT and drug release. The wet granulation method was selected using isopropyl alcohol as a binder for the preparation of tablets. D-optimal non-simplex mixture design was used for the selection of suitable polymer concentrations and floating agents. Release kinetics was used to determine the mechanism of drug release.
 Results: It was observed that GFT with optimum quantities of PEO, HPMC K100M, and the floating agent showed 100 % of drug release in 24h with FT up to 24h and minimum FLT of less than 2 min. Formulation with an in vitro release profile slower to the marketed sample was prepared.
 Conclusion: A sustained-release (GFT) of MH tablets using PEO-, HPMC K100M, and an effervescent system was successfully prepared. AGFT formulation with an in vitro release profile slower to the marketed sample that releases MH for 24h may suitable for once-daily dosing can be prepared.
Highlights
Oral administration is the most common route for drug delivery due to ease of administration and full control of administration by the patient, together with a high degree of flexibility on dosing
PEO component of the matrix limits the initial release of the drug and imparts gastric retention through swelling, while the HPMC component lowers the amount of PEO required while still allowing the swelling to occur
Using PEO and HPMC in combination would be beneficial in achieving prolonged gastro retention along with sustained delivery of highly soluble drugs like metformin hydrochloride (MH)
Summary
Oral administration is the most common route for drug delivery due to ease of administration and full control of administration by the patient, together with a high degree of flexibility on dosing. Due to its ability to lower blood glucose levels, it is widely used to treat non-insulin-dependent type 2 diabetes mellitus (T2DM) It lowers blood glucose concentration and glycosylated hemoglobin A1c levels by inhibiting hepatic gluconeogenesis and improves the insulin sensitivity of peripheral tissues without causing hypoglycemia or weight gain, in contrast to other antidiabetic drugs. These pharmacological advantages have made MH the first choice for the treatment of T2DM. To increase the bioavailability of MH, it would be beneficial to develop a floating gastro-retentive matrix tablet with prolonged gastric retention time and gradual drug release of the drug at the absorption site [6, 7]
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