Solubility Enhancement of Aceclofenac by Solid Dispersion

Abstract

The aim of the study was to improve the solubility of aceclofenac, which is poorly water soluble drug belongs to BCS class-II. Aceclofenac appears to be particularly well tolerated among the NSAIDs, with a lower incidence of gastrointestinal adverse effects. For poorly soluble orally administered drugs, the rate of absorption is often controlled by the rate of dissolution. To improve the solubility of drug by solid dispersions were prepared with different methods like physical mixture, kneading method and solvent evaporation method with various carriers like poloxamer188, poloxamer407 and PEG 6000 in different ratios from 1:1 to 1:5. The prepared formulations were evaluated for physicochemical characteristics, characterized by differential scanning calorimetry (DSC), X-ray diffraction (XRD), in-vitro dissolution studies and saturation solubility. Based on the evaluation parameters poloxamer407 in ratio of 1:5 through solvent evaporation method was optimized and formulated into tablets by direct compression method.These tablets showed a higher in-vitro dissolution drug release which is 99.62% in 30 minutes when compared with pure drug which showed 26.62% in 60 minutes, whereas marketed tablet (Hifenac) shows 99.64±0.10% in 40 minutes. Hence it was concluded that solid dispersion of aceclofenac drug by using polaxamer 407 with solvent evaporation method enhances solubility, absorption rate and increase bioavailability of the aceclofenac drug.

Safety and Pharmaceutical Evaluation of a Novel Natural Polymer, Ocicum, as Solubility and Dissolution Enhancer in Solid Dispersion

“…The release of aceclofenac was increased by increasing polymer ratios and a slightly higher drug release was observed with 1:3 dispersions when compared to the other ratios. Though the increase in dissolution of aceclofenac in the present experiments was in accordance with the earlier-reported higher dissolution of aceclofenac with Poloxamer 407 [16], yet the magnitude of the increased drug release was higher in solid dispersions prepared using Ocicum than that prepared using the Poloxamer 407. However, the improved dissolution profiles of ACF with Ocicum are exclusive to this research work.…”

“…The binary solid dispersions are simpler formulations, as they contain drug and polymer to capture the effect only of the polymer on the solubility and the dissolution of aceclofenac. Poloxamer 407, a synthetic polymer was selected for comparison, as it has shown significant improvement in the solubility and dissolution of aceclofenac [ 16 ] and other poorly soluble drugs [ 17 , 18 , 19 ].…”

Pembentukan dan Karakterisasi Multikomponen Kristal Aseklofenak – Asam Suksinat Dengan Metode Solvent Drop Grinding.

“…Penelitian mengenai usaha perbaikan kelarutan dan disolusi aseklofenak sudah banyak dilaporkan. Dispersi padat dengan beberapa polimer [9], kompleks inklusi dengan siklodekstrin-β [10], pembentukan nanokarier (nanoemulsi dan nanosuspensi) [11]. Pembentukan kompleks inklusi dengan siklodekstrin mengalami kendala terkait bobot molekul.…”

“…Akan tetapi, sistem dispersi ini dalam masa penyimpanan yang relatif singkat menunjukkan penurunan laju disolusi karena perubahan kristalinitasnya. Sistem dispersi tersebut tidak stabil terhadap suhu dan kelebapan, sehingga cukup sulit untuk diproduksi secara komersil [9].…”