Sains Malaysiana 39(5)(2010): 737–745

Sifat Fizikal dan Kajian In Vitro Tablet Matriks Pelepasan Tertahan Ketoprofen

(Physical Properties and In Vitro Studies of Sustained-Release  Ketoprofen Matrix Tablets)

Ibrahim Ijang

Bahagian Teknologi Perubatan, Agensi Nuklear Malaysia, Bangi

43000 Kajang, Selangor D.E., Malaysia

Mohd Cairul Iqbal Mohd Amin*, Bukhori Abu Bakar

Fakulti Farmasi, Universiti Kebangsaan Malaysia

Jalan Raja Muda Abdul Abdul Aziz, 50300 Kuala Lumpur, Malaysia

Diserahkan: 3 Februari 2009 / Diterima: 20 Januari 2010

ABSTRAK

Penggunaan formulasi tablet pelepasan tertahan untuk dadah anti-inflamatori bukan steroid (DAIBS) seperti aspirin berupaya melindungi lapisan perut dari kesan buruk jus asid tubuh. Kajian ini dilakukan untuk menilai keberkesanan formulasi tablet matriks pelepasan tertahan dengan kepelbagaian kepekatan polimer bersama ketoprofen sebagai model. Tablet dibangunkan dengan menggunakan kaedah granulasi basah yang terdiri daripada polimer hidrofilik (hidroksipropil metilselulosa), polimer hidrifobik bersandar pada pH (Eudragit L100-55) dan polimer tak bersandar pada pH (Eudragit R100) sebagai bahan asas pembentukan matriks pada kepekatan 10%, 20% dan 30%b/b. Semua formulasi dimampatkan dengan menggunakan mesin pentabletan yang mempunyai penebuk berbentuk cembung bersaiz 10 mm. Tablet yang terhasil diuji dari segi keseragaman berat, kekerasan, kerapuhan, ketebalan, % kandungan dadah dan kajian pelepasan in vitro menggunakan kaedah BP 2007. Hasil menunjukkan kadar pelepasan dadah dikawal oleh jenis dan kepekatan polimer di dalam formulasi matriks. Secara umumnya peningkatan kepekatan kandungan polimer di dalam tablet matriks didapati mengurangkan kadar pelepasan dadah. Perbandingan polimer melalui kepekatan yang sama menggunakan t50%, pula mendapati terdapat perbezaan statistik bermakna (P<0.05) pada kadar pelepasan dadah. Berdasarkan kepada pelepasan dadah dalam kajian in vitro, polimer hidrofobik bersandar pada pH (Eudragit L100-55) menunjukkan profil pelepasan dadah secara tertib sifar yang terbaik berbanding polimer yang lain.

Kata kunci: Pelepasan tertahan; tablet matriks; ketoprofen; pelepasan in vitro

ABSTRACT

The use of sustained release tablet formulation for non-steroidal anti-inflammatory drugs (NSAIDs) like aspirin has shown its capability to protect the stomach lining from the adverse effect of gastric juice from the body. This study was carried out to evaluate the efficiency of sustained release matrix tablet formulation using ketoprofen as a model drug with different polymers concentration. The tablets were prepared by the wet granulation method using hydrophilic polymer (hydroxypropyl methylcellulose), hydrophobic pH dependent polymer (Eudragit L100-55) and independent polymer (Eudragit RD 100) as matrix forming retarding materials at 10%w/w, 20%w/w and 30%w/w. All formulations were compressed using 10 mm concave faced punches. The compressed tablets were evaluated for uniformity of weight, friability, hardness, thickness, % drug content and in vitro dissolution test with regard to BP 2007. The results showed that the drug release rate was found to be governed by the type and concentration of polymer in the matrix system. Generally, increasing the polymeric concentration in the matrix tablets will decrease the rate of drug release. When the polymers were compared at similar concentration using t50%, the difference in drug release was found to be statistically significant (p<0.05). Based on the in vitro drug dissolution studies, the hydrophobic pH dependent polymer (Eudragit L100-55) showed a better zero drug release profile compared to other polymers.

Keywords: in vitro dissolution; ketoprofen; matrix tablets; sustained release

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*Pengarang untuk surat-menyurat: email:  mciamin@pharmacy.ukm.my