OPTIMASI FORMULA TABLET NIFEDIPIN GELLING FLOATING-GASTRORETENTIVE MENGGUNAKAN MATRIKS HPMC K4M, CARBOPOL 940, DAN EUDRAGIT RSPO

Wa Ode Sitti Musnina, S.Si, Prof. Dr. Suwaldi Martodihardjo., M.Sc., Apt.

2013 | Tesis | S2 Ilmu Farmasi

Nifedipin memiliki waktu paruh eliminasi yang relatif pendek (4 jam). Nifedipin dalam bentuk sediaan rilis segera (konvensional) memberikan respon hipotensif. Nifedipin diabsorpsi dengan cepat dan hampir sempurna (90%) dalam lambung. Berdasarkan sifat absorpsinya yang baik dalam lambung, nifedipin dapat dibuat dalam bentuk sediaan lepas lambat gelling floating-gastroretentive. Rancangan formula pada penelitian ini ditentukan menggunakan model desain faktorial dengan 3 faktor yaitu: HPMC K4M (A), Carbopol 940 (B), dan Eudragit RSPO (C) sehingga didapatkan 8 rancangan formula. Kekerasan tablet, durasi floating, bobot kumulatif nifedipin yang terlepas pada menit ke 360 (C360) dan nilai efisiensi disolusi pada menit ke 360 (ED360) digunakan sebagai parameter optimasi. Berdasarkan hasil pengolahan data, persamaan dan contour plot didapatkan untuk masing–masing parameter tersebut, sehingga formula optimal dapat ditentukan. Berdasarkan pendekatan nilai desirability dihasilkan formula optimal dengan komposisi matriks yaitu HPMC K4M 39,39 mg, Carbopol 940 33,64 mg dan Eudragit RSPO 10 mg. Formula optimal yang dihasilkan memiliki kekerasan tablet 4,9 Kg, durasi floating 1350 menit, C360 8,4% dan ED360 sebesar 3,8%. Kinetika pelepasan obat dari tablet nifedipin yang dihasilkan pada formula optimal mengikuti persamaan orde nol.

Nifedipine has a relatively short elimination half-life (4 hours). Nifedipine in immediate-release dosage forms has hypotensive response. Nifedipine is absorbed rapidly and almost perfectly (90%) in the stomach. Based on the absorption properties in the stomach, nifedipine can be prepared in the sustained-release dosage forms as gelling floating-gastroretentive. Formulas used in this study were determined by using factorial design with the use of three factors, i.e. HPMC K4M (A), Carbopol 940 (B), and Eudragit RSPO (C) so that eight formulas were obtained. Tablet hardness, duration of floating, amount of drug which is released up to 360 minute (C360), and dissolution efficiency up to 360 minutes (DE360) were used as parameters of optimization. Based on the data obtained, they were analyzed using equation to find the contour plots. Moreover, the contour plots were used to determine the optimum formula. Based on desirability values, optimum formula with 39,39 mg of HPMC K4M, 33,64 mg of Carbopol, and 10 mg of Eudragit RSPO was obtained. The results of optimum formula had 4.9 Kg of tablet hardness, 1350 minutes of floating time, 8.4% of C360, and 3.8% of ED360. Release kinetics of the optimum formula of nifedipine tablet is fitted to zero-order equation.

Kata Kunci : nifedipin, formula optimal tablet gelling floating, HPMC K4M, Carbopol 940, Eudragit RSPO