The Dissolution study of ketoprofen inclusion in skimmed milk

SINAPATI, Numa, Prof.Dr. Achmad Fudholi, DEA.,Apt

2008 | Tesis | S2 Ilmu Farmasi

Ketoprofen, merupakan asam propionic yang menjadi bagian dari golongan obat nonsteroid anti-inflamasi yang kurang larut dalam air dan berpotensi tinggi terhadap iritasi pada lambung selama masa terapi. Formula yang berbeda sudah dilakukan untuk mengurangi indikasi ketoprofen terhadap iritasi lambung, termasuk disperse padat atau inklusi pada hidrofilik karier. Pada penelitian ini, susu skim dipilih sebagai pembawa/karier karena mengandung permukaan bahan aktif dan kandungan asam amino. Inklusi ketoprofen pada susu skim dilakukan dengan menggunakan vakuum evaporator. Formula yang dibuat berdasarkan jumlah yang berbeda terhadap susu skim yang digunakan. Lima formula susu skim yang digunakan antara lain 50 ml (F1), 100 ml (F2), 150 ml (F3), 200 ml (F4) dan 250 ml (F5). Suspensi yang diperoleh kemudian dikeringkan dalam oven pada suhu 50 ⁰C, kemudian disaring dengan penyaring berukuran 150 μm. Setiap formula yang ada kemudian dicampur dengan bahan-bahan lain dan digranulasi menggunakan air. Granul-granul lalu dikeringkan dalam oven, dan dicampur dengan lubrican. Granul-granul tersebut ditimbang seberat 500 mg dan dikempakan secara manual. Karakteristik fisik tablet dievalusi. Hasil yang diperoleh menunjukkan bahwa seluruh formula-formula memenuhi persyaratan, kecuali formula ke 5 menunjukkan kerkerasan (3.9 kg). Waktu hancur untuk semua formula memenuhi persyaratan kecuali formula 4, yaitu 43,20 menit. Hasil Dissolusi Efisiensi (DE) pada waktu 120 menit, menunjukkan bahwa formula 3 memiliki tingkat disolusi yang lebih baik dibandingkan dengan formula lainnya. Dapat disimpulkan, bahwa untuk memperoleh tingkat disolusi yang lebih baik, perlu optimasi jumlah susu skim untuk inclusinya.

Ketoprofen is a propionic acid belonging to the non-steroid anti-inflamatory drugs. It is moderately hydrophobic and poorly soluble in water. It has a high potential for gastric irritation during chronic therapy. Different formulation approaches have been investigated to decrease the gastric irritation of ketoprofen including solid dispersion or inclusion in hydrophilic carriers. In this study, skimmed milk was chosen as a carrier due to its surface active agent and amino acid content. Ketoprofen inclusion in skimmed milk was performed using vacuum evaporation technique. The formulas were designed based on the different amount of skimmed milk used. Five formulas were prepared containing different volume of skimmed milk i.e. 50 ml (F1), 100 ml (F2), 150 ml (F3), 200 ml (F4) and 200 ml (F5) of skimmed milk. Suspension obtained were further dried in the oven at 50 degree Celsius, and then sieved at a size of 150 μm. Each of these formulas were then mixed with the other ingredients and granulated using water. The granules were dried in the oven and mixed with the lubricant. The granules were weighed to 500 mg and compressed manually to tablet form. The physical characteristics of the tablet were evaluated followed by the evaluation of the dissolution rate. The results showed that all the formulas were within the range of ideal physical properties except formula 5 showed decrease in hardness 3.9kg. Disintegration time showed that all formulas were within the range, except formula 4 showed the longest time (43.20 mins). Dissolution efficiency (DE) was calculated to evaluate the dissolution rate. Dissolution efficiency results at 120 minutes showed that formula 3 showed better dissolution rates compared to the other formulas. Formula 2 was next in line to formula 3. It can therefore be concluded that, in order to obtain better dissolution rate, the amount of skimmed milk in the inclusion should be optimized.

Kata Kunci : Obat Nonsteroid,Ketoprofen,Susu Skim,Inklusi, Ketoprofen, skimmed milk, inclusion.