Influence of different viscosity grade Methocel and Ethocel polymers for the development of controlled release dimenhydr
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Influence of different viscosity grade Methocel and Ethocel polymers for the development of controlled release dimenhydrinate matrix tablets Zeb‑un‑Nisa1 · Muhammad Harris Shoaib1 · Rabia Ismail Yousuf1 · Syed Imran Ali2 · Zafar Alam Mahmood1 · Sabahat Jabeen1 · Faaiza Qazi1 Received: 1 February 2020 / Revised: 6 June 2020 / Accepted: 18 September 2020 © Springer-Verlag GmbH Germany, part of Springer Nature 2020
Abstract Dimenhydrinate is a therapeutic agent used for the treatment of nausea and vomiting. A conventional dose of dimenhydrinate is 50 mg per 8 h. Once-daily controlled release tablets of dimenhydrinate were formulated intended to treat emesis. The tablets were formulated using hydrophilic polymers Methocel® and hydrophobic polymers Ethocel® and subsequently analyzed for pre-compression and post-compression characteristics, % moisture uptake, dissolution profiles and release behavior of the drug. Identification of active ingredient and compatibility of blends were analyzed through FT-IR. Drug release kinetics of dimenhydrinate was assessed at pH 1.2, 4.5 and 6.8. The results of release profiles were evaluated for different kinetic models including model dependent and model independent. The optimized formulation K100M 30% showed ideal pre-compression properties and in vitro characteristics. Tablets exhibited a controlled drug release pattern due to the formation of a viscous gel layer followed by erosion. Furthermore, zero-order best described the release pattern with the value of r2 ˃ 0.99. Once-daily tablets released 98–100% drug in 24 h. Significantly more concentration and higher viscosity grade of hydrophilic polymer ensured the required pattern of drug release. Keywords Dimenhydrinate · Controlled release · Methocel® · Ethocel® · Drug release kinetics · FT-IR
Introduction Dimenhydrinate, an antiemetic agent, is a salt of 8-chlorotheophylline and diphenhydramine. Chemically, it consists of 8-chlorotheophylline and 2(diphenylmethoxy)N,N-dimethylethylamine (1:1) (Fig. 1). It is classified as first-generation * Muhammad Harris Shoaib [email protected]; [email protected] Extended author information available on the last page of the article
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antihistamine, as the drug crosses the cell membranes conveniently, leading to its enhanced bioavailability [1]. The half-life is 5 h, and the conventional dose of dimenhydrinate is 50 mg per 8 h. Controlled release tablets are designed which release the drug at a rate that maintains plasma concentration unchanged with time [2]. The ideal drug delivery system comprises minimum doses to deliver the drug at the site in stipulated time to minimize unwanted side effects. Controlled release dosage units are more drug proficient, and release pattern normally is zero order [3, 4]. Generally, controlled release therapy is required to maintain blood or plasma concentration of drugs for a longer period; controlled release dosage units indeed have more advantages which include steady state with a lesser number of
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