Peningkatan Laju Disolusi Ketoprofen Dengan Teknik Co-Grinding Menggunakan Polimer Hydroxypropyl Methylcellulose E6

Abstract

PENDAHULUANKetoprofen merupakan obat golongan antiinflamasi nonsteroid (NSAIDs), turunan ABSTRACT: Improvement of the dissolution rate of ketoprofen as a model for a poorly water-soluble drug by solid state co-grinding technique with hydrophilic polymer hydroxypropyl methylcellulose E6 (HPMC) using mortar grinder apparatus have been investigated. Three different formulations prepared with varying drug : carrier ratio 1:2, 1:1, and 2:1 (w/w). The physical mixture prepared with ratio 1:1 (w/w). X-ray diffraction showed a decrease of the peak intensity of ketoprofen. DSC analysis showed a decrease of the melting point of ketoprofen. FTIR analysis showed no chemical interaction between drug and polymer. In this investigation, it was found that solubility tended to increase with an increase in the amount of polymer used. Solid dispersion ratio 1:2 showed the highest solubility (6,5 fold). However, unlike the solubility results, the dissolution rate increased with decreases in polymer concentration due to thick diffusion layer formation of the polymer. Solid dispersion ratio 2:1 showed the highest dissolution (2.1 times).ABSTRAK: Telah dilakukan peningkatan laju disolusi ketoprofen sebagai model zat aktif yang sukar larut air dengan teknik penggilingan bersama (co-grinding) dengan polimer hidrofilk hydroxypropyl methylcellulose E6 (HPMC) menggunakan alat mortar grinder. Tiga formula disiapkan dengan perbandingan zat aktif : polimer 1:2, 1:1, dan 2:1 (b/b), dan campuran fisik dibuat dengan menggunakan perbandingan 1:1 (b/b). Difraktogram sinar-X menunjukkan terjadinya penurunan intensitas puncak ketoprofen. Termogram DSC menunjukkan terjadinya penurunan titik leleh ketoprofen. Analisis FTIR menunjukkan tidak terdapat interaksi kimia antara zat aktif dengan polimer. Pada penelitian ini didapatkan bahwa kelarutan obat meningkat dengan meningkatnya konsentrasi polimer. Dispersi padat rasio 1:2 menunjukkan peningkatan kelarutan terbesar (6,5 kali). Tidak seperti kelarutan, laju disolusi ketoprofen meningkat dengan menurunnya kosentrasi polimer karena terbentuknya lapisan difusi yang tebal oleh polimer. Dispersi padat resio 2:1 menunjukkan peningkatan disolusi tertinggi (2,1 kali). J u r n a l S a i n s F a r m a s i & K l i n i s (p-ISSN: 2407-7062 | e-ISSN: 2442 diterbitkan oleh Ikatan Apoteker Indonesia -Sumatera Barat homepage: http://jsfkonline.org Jur nal Sains Farmasi & Klinis , 3(2),[193][194][195][196][197][198][199][200][201] Keywords Pembuatan campuran fisikaCampuran fisika ketoprofen dan hydroxypropyl methylcellulose E6 (HPMC) pada perbandingan berat 1:1, dibuat dengan cara mencampur kedua bahan dengan menggunakan spatula. terdispersi secara merata dipermukaan HPMC E6. Analisis Spektrofotometri FT-IR Analisis Analisis Termal (DSC)Hasil ini sekaligus menunjukkan bahwa terjadi interaksi antara ketoprofen dan HPMC yang akan menghasilkan senyawa yang lebih amorf.Pengujian disolusi ketoprofen, campuran fisik dan hasil penggilingan ketoprofen -HPMC E6 dilakukan dengan menggunakan alat disolusi tipe II, dengan kece...

Combination of Dissolving Microneedles with Nanosuspension and Co-Grinding for Transdermal Delivery of Ketoprofen

“…This method has been described in Section Differential Scanning Calorimetry (DSC) Analysis of Co-grinded Ketoprofen. The properties can be seen when the material is subjected to heat [ 17 ]. Figure 6 A,B display an endothermic peak of ketoprofen at 95.8 °C, which is associated with the melting point of ketoprofen.…”

“…SEM was conducted to find the polymorphism and morphology of the prepared CG ketoprofen, referring to method Section SEM (Scanning Electron Microscopy). Based on the results shown in Figure 7 A, it can be seen that ketoprofen was a crystalline solid with large irregular lumps and a hollow texture [ 17 ]. The pure powder of PVP ( Figure 7 B) produced a ball-shaped morphology with an uneven surface, as previously described [ 35 ].…”

“…A total of 5 mL of sample solution was pipetted at 5, 10, 15, 30, 45, and 60 min, and upon each pipetting, the dissolution medium was replaced with a new one with the same volume and temperature when pipetting. Next, the sample solution was analyzed by a UV-Vis spectrophotometer at its maximum absorption wavelength [ 17 ]. The analytical spectrophotometric condition was used referring to the method section UV-Vis Spectrophotometric Condition.…”

“…NS is a colloidal dispersion of submicron drug particles with a size < 1 µm [ 16 ]. Co-grinding is a method used to increase drug solubility by grinding solid drug compounds together with hydrophilic polymers [ 17 ]. Co-grinding is a simple and environmentally friendly technique because it does not use organic solvents [ 18 ].…”

“…Co-grinding is a simple and environmentally friendly technique because it does not use organic solvents [ 18 ]. Co-grinding has also been carried out for the drug ketoprofen, as previously performed by Hilaliyati [ 17 ]. They found that co-grinding ketoprofen with hydroxy propyl methyl cellulose can improve the physicochemical properties of ketoprofen and its dissolution rate in a phosphate buffer medium of pH 7.4.…”