<em>Meloxicam (MLX) is a nonsteroidal anti-inflammatory drugs (NSAID) which belong to Biopharmaceutical Classification System (BCS) class II, which have a low solubility level with a high permeability. Therefore, to enchance is solubility level, physical modification of the meloxicam is required. It can be done by the cocrystal formation. Cocrystal contained active ingredients and coformer which bind through the hydrogen bond. This study used malonic acid (MA), since it contained carboxylic group which expected to form hydrogen bonds. Slurry is a method of cocrystal formation by mixing two ingredients, i.e. active ingredients of the drugs and its cofomer, dissolved in a solvent and may be formed due to the heat energy released by the friction between particles and their crusher. This study aimed to determine the characteristic of meloxicam-malonid acid cocrystal by 1:1 mol ratio using PXRD, DSC and FTIR. The result of PXRD charaterization indicated a new peak at angle 9,4° and 18,5°. The result of DSC characterization indicated an endothermic peak with a low melting point at 97,64°C ; 152,62°C ; 176,87°C temperature. The result of FTIR characterization indicated a shirt of the O-H uptake band from at wave number 3126-2980 cm<sup>-1</sup> to 3292-2951 cm<sup>-1</sup>, the N-H uptake band of meloxicam at wave number 3492 cm<sup>-1</sup> to 3525 cm<sup>-1</sup></em>
The aim of this study was to determine the effect of binder and disintegrant excipients toward tablet properties of levofloxacin as the latter tends to suffer brittle fracture upon compression. The excipients used were povidone K-30 as the binder and sodium starch glycolate (SSG) as the disintegrant which the tablets were formulated according to factorial design 22 with two factors and two levels on each factor. Four formulas were prepared by wet granulation method using 2 and 4% of each povidone K-30 and sodium starch glycolate in various compositions. Tablet properties were evaluated for its hardness, friability, and disintegration time as well as dissolution profile. The data obtained was statistically analyzed using Minitab® 17 software to optimize the formulation and resulted in different impacts caused by each excipient. Povidone K-30 exhibited an increment in hardness, friability, disintegration time but a decrease indissolution profile of levofloxacin tablet. SSG decreased hardnessand disintegration time, but increased friability and dissolution profile of levofloxacin tablet. Overlaid contour plot showed that the optimal formula regarding tablet properties of friability, disintegration time, and dissolution profile is in composition of 2.01% povidone K-30 and 2.01% sodium starch glycolate. Keywords: levofloxacin tablet, povidone K-30, sodium starch glycolate, factorial design.
ABSTRACT:The aim of this research was to get optimal formula of levofloxacin tablet prepared with variation of PVP K-30 as binder and vivasol as disintegrant. The making of levofloxacin tablets was done by wet granulation. Tablet was prepared with various levels of PVP K-30 and disintegrant vivasol, compressed using a hydraulic press with 12 mm punch diameter, for 3 seconds. Physical quality (hardness, friability, and disintegration time) and dissolution rate of tablet was evaluated. The optimization of the formula was done by factorial design of 22 factorial experiments with 2 factors (PVP K-30 and vivasol) and 2 levels (2% and 4%). Optimization results showed that elevated levels of PVP K-30 increased tablet hardness, reduced friability of tablet, decreased disintegrating time, and increased dissolution rate of levofloxacin tablets. Meanwhile, elevated levels of vivasol increased the hardness of tablets, decreased the disintegrating time of tablets, decreased the dissolution rate of levofloxacin tablets, but did not affect the friability of tablets. In conclusion, the optimal tablet that meet the specifications of physical quality (hardness, friability, and disintegrating time) and dissolution rate was made by 2.4 to 3.7% of PVP K-30 and 2.0 to 3.2% vivasol as shown in the feasible area of design space. ABSTRAK:Penelitian ini bertujuan mendapatkan formula yang optimal tablet levofloksasin yang dibuat dengan variasi PVP K-30 sebagai pengikat dan vivasol sebagai disintegran. Metode pembuatan tablet levofloksasin dilakukan secara granulasi basah. Formula tablet dibuat dengan variasi PVP K-30 dan disintegran vivasol, dikempa menggunakan alat hidrolik press dengan puch diameter 12 mm, selama 3 detik. Evaluasi mutu fisik (kekerasan, kerapuhan, dan waktu hancur) dan laju disolusi tablet. Optimasi formula dilakukan dengan desain faktorial 22 yaitu eksperimen faktorial dengan 2 faktor (PVP K-30 dan vivasol) dan 2 level (2% dan 4%). Hasil optimasi menunjukkan bahwa peningkatan kadar PVP K-30 meningkatkan kekerasan tablet, menurunkan kerapuhan tablet, dan menurunkan waktu hancur tablet, serta meningkatkan laju disolusi dari tablet levofloksasin. Peningkatan kadar vivasol meningkatkan kekerasan tablet, tidak mempengaruhi kerapuhan tablet, dan menurunkan waktu hancur tablet, serta menurunkan laju disolusi tablet levofloksasin. Kesimpulan penelitian ini menunjukkan bahwa tablet yang optimal serta memenuhi spesifikasi dari mutu fisik (kekerasan, kerapuhan, dan waktu hancur) dan laju disolusi ditunjukkan pada daerah feasible dari design space yaitu kadar PVP K-30 antara 2,4 sampai 3,7 % dan kadar vivasol 2,0 sampai 3,2%.
Salisilamida termasuk golongan obat AINS (anti inflamasi non steroid)memiliki efek analgesik dan antipiretik mirip dengan asam asetil salisilat, namun di dalam tubuh tidak diubah menjadi salisilat. Dalam penggunaan secara oral,salisilamida tidak menimbulkan radang dan pendarahan pada lambung. Salisilamida merupakan senyawaasam lemah (pKa 8,2) yang kelarutannya dipengaruhi oleh pH lingkungan. Pada pemberian secara oral, salisilamida akan melewati saluran cerna pada rentang pH sekitar 1,5–8,0. Menurut persamaan Noyes-Whitney, disolusi obat akan dipengaruhi oleh kelarutannya. Tujuan penelitian ini adalah untuk mengevaluasi hubungan antara kelarutan dan disolusi salisilamida dalam beberapa pH media disolusi. Uji kelarutan dilakukan dalam media disolusi pH 1,2; 4,5; dan 6,5 dengan kekuatan ionik (µ) sebesar 0,2 dalam waterbath suhu 37 ± 0.5 °C sampai terbentuk kelarutan jenuhnya. Uji disolusi dilakukan dalam larutan media disolusi dengan pH yang sama dengan uji kelarutan, menggunakan pengaduk tipe dayung dengan kecepatan 50 rpm pada suhu 37 ± 0.5 °C selama 60 menit. Kadar salisilamida terlarut pada uji kelarutan dan uji disolusi ditentukan dengan menggunakan spektrofotometer pada λmax masing-masing pH media. Kelarutan salisilamida dan nilai efisiensi disolusi dalam 60 menit (ED60) dianalisis dengan ANOVA satu arah padaα 0.05. Hasil penelitian menunjukkan kelarutan salisilamida meningkat seiring dengan meningkatnya pH. Peningkatan kelarutan salisilamida meningkatkan disolusinya
Meloxicam is included in the class II Biopharmaceutical Classification System (BCS). This drug has low solubility and high permeability. The solubility is one of the factors that affect in the dissolution rate of drug. One of the effort to increase dissolution of meloxicam is by forming a solid dispersion system made using melting method. The addition of PEG 6000 and poloxamer 188 carriers determine in the solid dispersion system aims to increase the dissolution rate of meloxicam. The purpose of this study is to characterize the meloxicam solid dispersion system with PEG 6000 and poloxamer 188 matrices at a ratio of 99:1 and 98:2 made by the melting method when compared with the physical mixture and its pure compound using Powder X-Ray Diffaction, DSC and FTIR. The results of meloxicam solid dispersion with a ratio 99:1 and 98:2 showed the disappearance of the typical peak of meloxicam at an angel of 2θ 6.5° and 11.2°. The thermogram data using DSC shows a decrease in melting point of solid dispersion system with a ratio of 99:1 and 98:2 namely 64.33°C and 64.21°C. The result of the characterization of meloxicam solid dispersion with FTIR showed that the identified spectrum were in the spectrum range of meloxicam, PEG 6000, poloxamer 188 indicating there was no incteraction in the meloxicam solid dispersion system.
scite is a Brooklyn-based organization that helps researchers better discover and understand research articles through Smart Citations–citations that display the context of the citation and describe whether the article provides supporting or contrasting evidence. scite is used by students and researchers from around the world and is funded in part by the National Science Foundation and the National Institute on Drug Abuse of the National Institutes of Health.
hi@scite.ai
10624 S. Eastern Ave., Ste. A-614
Henderson, NV 89052, USA
Copyright © 2024 scite LLC. All rights reserved.
Made with 💙 for researchers
Part of the Research Solutions Family.