Cefixime has been formulated in cocrystal form with nicotinamide (coformer). SEF-NIK cocrystals were prepared at a mole ratio of 1:1 using a liquid-assisted grinding method. The cocrystals were characterized using DSC, FTIR, SEM, and PXRD. The characterization results showed that cocrystals were formed between cefixime and nicotinamide. The results of the solubility test, dissolution rate and permeability of the SEF-NIK cocrystal showed a significant increase compared to pure cefixime. Based on these results, the SEF-NIK cocrystal was continued for pharmacodynamic studies with in vitro antibacterial activity studies. This study aims to determine the effect of cocrystallization techniques on the antibacterial activity of cefixime. The test was carried out using two methods, namely the Agar Diffusion Test and the Broth Dilution Test. The results showed that cocrystallization of cefixime with nicotinamide did not inhibit its effectiveness against Escherichia coli bacteria, but its effectiveness was better than pure cefixime. In the agar diffusion method, the inhibition zones of cefixime and SEF-NIK cocrystals against Escherichia coli bacteria were 6.2 mm and 8.6 mm, respectively. On the fifth day of the broth dilution test method, the OD values of Escherichia coli bacteria in the cefixime and SEF-NIK cocrystals were 1.330 and 1.064, respectively.
Keywords: cefixime, liquid-assisted grinding, antibacterial activity
Abstrak
Sefiksim telah berhasil dibuat dalam bentuk kokristal dengan nikotinamida (koformer). Kokristal SEF-NIK dibuat dengan perbandingan mol 1:1 menggunakan metode liquid-assisted grinding. Kokristal dikarakterisasi menggunakan DSC, FTIR, SEM, dan PXRD. Hasil karakterisasi menunjukkan bahwa terbentuk kokristal antara sefiksim dan nikotinamida. Hasil uji kelarutan, laju disolusi, dan permeabilitas kokristal SEF-NIK menunjukkan peningkatan yang signifikan dibandingkan dengan sefiksim murni. Berdasarkan hasil penelitian tersebut, kokristal SEF-NIK dilanjutkan ke tahap uji farmakodinamik yakni uji aktivitas antibakteri secara in vitro. Penelitian ini bertujuan untuk mengetahui pengaruh dari teknik kokristalisasi terhadap aktvitas antibakteri sefiksim. Pengujian dilakukan menggunakan dua metode yakni Agar Diffusion Method (difusi agar) dan Broth Dilution Method (dilusi cair). Hasil penelitian menunjukkan bahwa kokristalisasi sefiksim dengan nikotinamida tidak menghambat efektivitasnya terhadap bakteri Escherichia coli, akan tetapi efektivitasnya lebih baik dibandingkan sefiksim murni. Pada metode difusi agar, zona hambat sefiksim terhadap bakteri Escherichia coli sebesar 6,2 mm sedangkan kokristal SEF-NIK lebih besar yakni 8,6 mm. Pada metode dilusi cair, hasil pengukuran OD bakteri Escherichia coli hari kelima pada sefiksim sebesar 1,330 sedangkan pada kokristal SEF-NIK sebesar 1,064.
Kata Kunci: sefiksim, liquid-assisted grinding, aktivitas antibakteri