Karakterisasi Sifat Gastroretentive Matriks Nata De Coco dan Polimer Natrium Karboksimetil Selulosa yang Mengandung Metformin Hidroklorida

Abstract

Background: Metfomin Hydrochloride when administered orally about 40% of the dose is absorbed in the upper small intestine (duodenum and jejenum) and only 10% is absorbed in the ileum therefore it has a low bioavailability of 50-60%, administration of metformin by immediate release the most common side effects are nausea and vomiting and discomfort in the stomach, Gastroretentive Drug Delivery System is a system approach designed to extend the residence time of drugs in the stomach to increase drug bioavailability. Objective: Making a gastroretentive preparation of metformin HCl from nata de coco matrix and Na CMC polymer that can be retained in the stomach and is able to provide sustained release. Method: Metformin HCl gastroretentive printed beads were prepared using nata de coco pulp, mucilago Na CMC 10% in distilled water and lactose in different ratios. The mixture of nata de coco pulp, mucilago Na CMC, and lactose containing metformin HCl was printed using a 1,2 cm diameter beverage pipette and dried at room temperature for 5×24 hours. The floating, swelling, integrity, and release properties of the printed beads were tested using the USP dissolution apparatus paddle method in artificial stomach medium pH 1,2 for 12 hours. The mucoadhesive properties were tested using 1×1 cm rat gastric mucosa with a DuNuoy tensiometer. Results: The experimental results showed that F8a (1:2) F8b (1:1) and F8c (2:1) printed beads provided good characteristics as a gastroretentive drug delivery system with slow or gradual drug release. Floating properties before the occurrence of gastric emptying time (2-3 hours) shown from Floating Lag Time 36±5,65 minutes, 8±5,40 minutes, 34±9,62 and Floating Duration Time 12 hours, printed beads have unqualified swelling properties because the preparation is not larger than the diameter of the pylorus at (2-3 hours), mucoadhesive properties show the results of 67,26±0,15 dyne/cm2 where these results have better mucoadhesive strength than other formulas. The printed beads are able to provide a slower and gradual release or meet the requirements of sustained release marked in formulas F8a and F8b at 12 hours 80,01% and 81,55% with a sustained release requirement of 12>75%. Conclusion: nata de coco-Na CMC printed beads have good gastroretentive properties with the best release profiles being F8a, F8b and F8c, respectively.