Karakterisasi Sifat Gastroretentive Matriks Nata De Coco dan Polimer Kitosan yang Mengandung Metformin Hidroklorida

Abstract

Background: Metformin hydrochloride as an anti-diabetic drug in oral administration has low bioavailability (50-60%) and a short half-life (1.5-4.5 hours). Administration of the drug 2-3 times a day can reduce patient compliance. Side effects of metformin reach 30% in the form of gastrointestinal disorders, so the development of sustained release is needed to increase the duration of action and bioavailability of the active substance. Objective: The aim of this study is to make a gastroretentive preparation of metformin hydrochloride from nata de coco and chitosan polymer matrix that can be retained in the stomach and provide sustained release (SR). Method: The stages of the study included preparation by homogenously grinding the ingredients, metformin hydrochloride, chitosan hydrogel, nata de coco pulp, and lactose. Homogeneous preparations were molded into membranes, granules, and printed beads. These dosage forms were examined for their main gastroretentive properties, namely floatability and durability, and other gastroretentive properties such as development properties, mucoadhesiveness, content measurement, and drug release profile were tested on the best dosage form. Results: The molded beads form has the best floating properties and durability compared to membrane and granule forms. F7a molded beads with nata de coco:chitosan polymer ratio (1:2) density 0,80±0,02 g/cm3, weight swelling 12,86%, mucoadhesive 85,80±9,65 dyne/cm3, content 90,46%-107,58%, dissolved 104,05% for 10 hour. F7b molded beads with nata de coco:chitosan polymer ratio (1:1) density 0,82±0,01 g/cm3, weight swelling 20,29%, mucoadhesive 72,23±5,15 dyne/cm3, content 95,71%-116,39%, dissolved 100,94% for 10 hour. F7c molded beads with nata de coco:chitosan polymer ratio (2:1) density 0.74±0,02 g/cm3, weight swelling 25,40%, mucoadhesive 60,87±7,38 dyne/cm3, content 112,69%-120,91%%, dissolved 98,63% for 10 hour. The release profile of F7a, F7b and F7c followed the Higuchi model. The test results showed significant difference dissolution from the variation of dosage ratio of F7a, F7b, and F7c. Conclusion: This study indicates that molded beads of nata de coco and chitosan polymer matrix have the potential to be applied as a gastroretentive drug delivery system.