Abstract
Background: Fenoprofen calcium dehydrate (FCD) is counted as a non-steroidal, anti-inflammatory, anti-arthritic drug. FCD is slightly water soluble. It is indicated for mild pain relief, where the suggested dosage is 200 mg orally every 4 to 6 h. Aim: Reduce dissolution efficiency, reach an extended therapeutic effect and reduce the frequency of the drug side effects. Method: Combination of the co-evaporated drug:triacetyl-β-cyclodextrin complex prepared in a ratio of 1:3 and either of two polymers—hydroxylpropylmethyl cellulose (HPMC) or ethyl cellulose (EC)—in the same formulation. In vitro dissolution studies were carried in simulated gastric (pH 1.2) and intestinal (pH 6.8) fluids, by using the USP dissolution tester (rotating paddle apparatus). The FCD in vitro release from EC/drug complex was markedly retarded. Interaction between fenoprofen, TA-β-CD, EC, HPMC in the solid state were confirmed by FT-IR, DSC, XRD and SEM. In vivo studies assessed the anti-inflammatory and analgesic activities and the results were compared with the market product Nalfosab® Capsules. Results: Remarkable inhibition of inflammation and nociception after 24 h was attained for EC/drug complex. Conclusions: EC/drug complex has a sustained effect due to high remaining amount after elapsing with remarkable inhibition of inflammation.
Highlights
Fenoprofen calcium dihydrate (FCD) is counted as a nonsteroidal, anti-inflammatory, anti-arthritic drug
Above observations, hydroxylpropylmethyl cellulose (HPMC)/drug marked decrease in the characteristic peak peak of drug. These results the of existence a new solidwith phase with degree lower degree of crystallinity, These results showed theshowed existence a new of solid phase lower of crystallinity, that could that by could created by the molecularof interaction of the and the drug complex be created thebemolecular interaction the HPMC
ethyl cellulose (EC)/drug complex showed higher percentage inhibition of the rat paw edema induced by carrageenan after both 12 and 24 h
Summary
Fenoprofen calcium dihydrate (FCD) is counted as a nonsteroidal, anti-inflammatory, anti-arthritic drug. FCD is slightly soluble in water, with pKa 4.5 at 25 ◦ C. FCD is highly recommended to treat mild to moderate pain at a dosage of 200 mg orally every 4 to 6 h. Fenoprofen calcium is about 99% bound to plasma proteins. Fenoprofen calcium dehydrate (FCD) is counted as a non-steroidal, anti-inflammatory, anti-arthritic drug. It is indicated for mild pain relief, where the suggested dosage is 200 mg orally every 4 to 6 h. The FCD in vitro release from EC/drug complex was markedly retarded. Results: Remarkable inhibition of inflammation and nociception after 24 h was attained for EC/drug complex. Conclusions: EC/drug complex has a sustained effect due to high remaining amount after elapsing with remarkable inhibition of inflammation
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