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Pharmaceutics 2017, 9(3), 23; https://doi.org/10.3390/pharmaceutics9030023

Effect of Polymers on the Physicochemical Properties and Biological Performance of Fenoprofen Calcium Dihydrate-Triacetyl-β-Cyclodextrin Complex

1
Pharmaceutics and Pharmaceutical Technology Department, Future University, Cairo 11311, Egypt
2
Pharmaceutics Department, October 6 University, Giza 12511, Egypt
*
Author to whom correspondence should be addressed.
Received: 22 May 2017 / Revised: 15 June 2017 / Accepted: 19 June 2017 / Published: 3 July 2017
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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. View Full-Text
Keywords: fenoprofen calcium dehydrate; triacetyl-β-cyclodextrin; hydroxypropylmethyl cellulose; ethyl cellulose; sustained release fenoprofen calcium dehydrate; triacetyl-β-cyclodextrin; hydroxypropylmethyl cellulose; ethyl cellulose; sustained release
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This is an open access article distributed under the Creative Commons Attribution License which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited. (CC BY 4.0).
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Ammar, H.O.; Makram, T.S.; Mosallam, S. Effect of Polymers on the Physicochemical Properties and Biological Performance of Fenoprofen Calcium Dihydrate-Triacetyl-β-Cyclodextrin Complex. Pharmaceutics 2017, 9, 23.

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