Core in Cup Ethylmorphine Hydrochloride Tablet for Dual Fast and Sustained Pain Relief: Formulation, Characterization, a
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Research Article Core in Cup Ethylmorphine Hydrochloride Tablet for Dual Fast and Sustained Pain Relief: Formulation, Characterization, and Pharmacokinetic Study Aliaa Nabil ElMeshad,1,3 Khaled M. Abdel-Haleem,2 Nabaweya A. Abdel Gawad,1,2 Mohamed Ahmed El-Nabarawi,1 and Nermin M. Sheta2
Received 1 May 2020; accepted 7 July 2020 Abstract. Ethylmorphine hydrochloride (EtM) is a derivative of morphine used as analgesic to treat severe pain in case of cancer and bone injury. This study aimed to formulate and evaluate core in cup tablets containing 2 doses of EtM, the cup was formulated as lyophilized oro-dispersible tablet (ODT) for immediate release (IR), and the core was formulated as directly compressed tablet for sustained release (SR). Factorial design was adopted for the optimization of tablets prepared via lyophilized form and direct compression techniques: a 41.22 design was used for the former, while a 32 one was used for the latter. All prepared tablets showed acceptable physical properties which were in accordance with pharmacopeial standards. Two lyophilized ODTs (F9 and F10) formulae were selected as the cup for instant release. While one directly compressed tablet formula (S6) was selected based on the in vitro release profile to represent the sustained core, the outcome was 2 core in cup tablets, namely B1 and B2 which were evaluated for their in vivo absorption and showed a maximum plasma concentration (Cpmax) of 354.12 ± 17.55 ng/mL and 350.82 ± 12.15 ng/mL respectively attained after 3.0 h which were twofolds significantly higher in comparison to the market tablet with Cpmax of only 172.05 ± 12.53 ng/mL attained after 2.20 ± 0.24 h. KEYWORDS: Core in cup tablet; Ethyl morphine hydrochloride; Lyophilized orodispersible tablet; Sustained release tablet.
INTRODUCTION Ethylmorphine hydrochloride (EtM) is a potent narcotic analgesic and antitussive drug that undergoes metabolism in the liver by ethylmorphine-N-demethylase enzyme into morphine. It acts by diminishing pain by blocking the transmission of pain signals to the brain and thus is used to relieve muscle spasms and cramps in addition to severe pain of bone and cancer. EtM is highly water-soluble drug (2.610 g/ L at 20°C) which possesses fast absorption and elimination (1). The oral route is one of the most acknowledged routes for drug administration and has been used for both traditional and novel delivery of drugs due to ease of administration and enhanced compliance. In fact, the conventional dosage form usage has been declined by time in comparison to modified release one due to benefits of dose frequency reduction and improved compliance (2,3). Immediate release (IR) tablets are designed to disintegrate and release their main active ingredients with 1
Department of Pharmaceutics and Industrial Pharmacy, Faculty of Pharmacy, Cairo University, Kasr El Eini St., Cairo, 11562, Egypt. 2 Department of Pharmaceutics and Industrial Pharmacy, Faculty of Pharmacy, October 6 University, Giza, Egypt. 3 To whom correspondence should be addressed. (e–mail: a
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