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Glimepiride is an oral antidiabetic drugs which is practically insoluble in water. The formation of β-cyclodextrin inclusion complex was able to increase the solubility of glimepiride. This study aim to prepare, characterize and formulation of inclusion complex tablets in order to meet the requirement in Pharmacopeia. The inclusion complex were prepared in a molar ratio of 1:1 and 1:2 by freeze drying method, after that characterized include FTIR spectroscopy and scanning electro microscope (SEM). Further, it was formulated into tablets by direct compression technique using primogel and crospovidone as super disintegrants. The tablets were evaluated include weight uniformity, hardness, friability, disintegration, and dissolution. The dissolution studies of inclusion complex were performed by using USP II apparatus. The result of FTIR and SEM provided evidence of the formation of complexes after utilizing freeze-drying methods. The tablet evaluation containing inclusion complex glimepiride-β cyclodextrin with primogel and cropovidone as disintegrant showed that increased concentration of disintegrant will increase disintegration time of the tablets. All of formulas meet the requirements in the Pharmacopoeia. The inclusion complex of glimepiride-β cyclodextrin successfully used for enhancing the solubility of glimepiride and the tablets meet the requirement in Pharmacopeia.

16,22 ± 0,39 % and 7,61 ± 0,12 kg, respectively

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Backround: Glibenclamide is an oral antidiabetic drug which is practically insoluble in water. Formation of β-cyclodextrin inclusion complex was able to increase glibenclamide solubility. Objective: Aims of this study are to characterize, formulate and evaluate inclusion complex tablets of glibenclamide to meet the requirements in Pharmacopeia. Methods: Inclusion complex was prepared in a 1: 1 and 1: 2 molar ratio by spray drying method. Characterization were performed by using Fourier Transform Infrared (FTIR) spectroscopy and Scanning Electron Microscope (SEM). Further, it was formulated into tablets by direct compression technique using primojel and crospovidone as disintegrants. Uniformity weight, hardness, friability, disintegration, and tablets were evaluated include dissolution. Dissolution studies of inclusion complex were performed by using United States Pharmacopeia (USP) II apparatus. Drug concentration dissolution was determined with high pressure liquid chromatography (HPLC). Result: Result of FTIR and SEM provided evidence of glibenclamide and β-cyclodextrin complex formation after using spray drying methods. The tablet evaluation with primojel and crospovidone as disintegrant showed that increase concentration of disintegrant would increase disintegration time of the tablets. All of the formulas meet the requirements in the Pharmacopoeia. Conclusion:The inclusion complex of glibenclamide-β cyclodextrin successfully used for enhancing the solubility of glibenclamide. The tablets meet the requirements in Pharmacopeia.Latar Belakang: Glibenklamid merupakan obat antidiabetes oral yang sukar larut dalam air. Pembentukan komplek inklusi dengan β-siklodekstrin diharapkan mampu meningkatkan kelarutan glibenklamid. Tujuan Penelitian: Penelitian ini bertujuan untuk mengkarakterisasi, memformulasi dan mengevaluasi tablet hasil komplek inklusi glibenklamid supaya memenuhi persyaratan Farmakope. Metode: Komplek inklusi dibuat dengan perbandingan rasio molar glibenklamid dan β-siklodekstrin 1 : 1 dan 1 : 2 dengan menggunakan metode spray drying. Hasil komplek inklusi dikarakterisasi meliputi spektroskopi FTIR dan SEM. Selanjutnya kompleks tersebut diformulasi menjadi tablet dengan teknik kempa langsung menggunakan primojel dan crospovidon sebagai disintegran. Tablet yang dihasilkan dievaluasi keseragaman bobot, kekerasan, kerapuhan, waktu hancur dan disolusi. Uji disolusi tablet hasil