Research Article ISSN: 2754-5008 Open Access Formulation of Extended-Release Ranolazine Tablet and Investigation Its Stability in the Accelerated Stability Condition At 40⁰C And 75 % Humidity Research and Development Section, Dr. Abidi Pharmaceutical Company, Tehran, Iran Farzad Khajavi Journal of Pharmaceutical Research & Reports *Corresponding author Farzad Khajavi, Research and Development Section, Dr. Abidi Pharmaceutical Company, Tehran, Iran. Tel: +98-21-44504787. E-mail: farzadchemistry@gmail.com Received: December 24, 2020; Accepted: January 02, 2021; Published: January 07, 2021 Volume 2(1): 1-3 Keywords: Eudragit, Ranolazine, Drug release, Extended-release tablet, Stability Introduction The goal of controlled delivery systems is to reduce the frequency and / or to increase the effectiveness of the drug by localization at the target site, thereby reducing the dose required to provide uniform drug delivery [1]. Drug release from the dosage form is controlled mainly by the properties of polymer and drug used in the preparations [2]. Cellulose ethers are found to accommodate a large percentage of drugs and are easy to use in tablets. They are also very stable over a wide range of conditions. In the presence of strong acid, water and heat a cellulose ether polymer will degrade by chain scission causing a loss of average molecular weight or viscosity. HPMC is often used to prepare matrix of sustain-release (SR) tablets because the polymer is non-toxic, easy to handle and do not require any special manufacturing technology [3-6] . It was evident that HPMC 2208 (methocel K4M premium) and carboxy vinyl polymers can release drugs for longer time by quickly forming a gel layer [1]. Eudragit ® L100 is an anionic copolymer of methacrylic acid and methyl methacrylate with ratio of the free carboxyl groups to the ester groups of approximately 1:1. The polymer is insoluble in acid medium, hence when used in a coating layer of drug formulation, it will protect the acid-unstable-drug from degradation once it reaches the stomach [7-9]. In this work we formulated Ranolazine 500 mg extended-release tablet with the using of Eudragit L100-55 as a retarding agent. The stability results of tablets show that the formula is stable in this condition. Experimental Materials HCl, NaOH were purchased from Merck. Ranolazine from Aurobindo Pharmaceutical Co. Ltd., Microcrystalline Cellulose from Accent (India), Hydroxypropylmethyl Cellulose (HPMC 5 cps) from NIPPON SODA Co., LTD. (Japan), Eudragit L100-55 from Ashland (Belgium) and Magnesium stearate from Behansar Co. were provided. Ranexa Extended-release tablet 500 mg (Menarini Pharmaceutical Company (Italy)) were provided and used as reference tablets. Preparation of matrix tablets Tablet preparation The ready to press powder of tablets was prepared by wet granulation method. The drug substance is kneaded with the internal phase (that contains Microcrystalline Cellulose, Eudragit L100-55, and Hydroxypropylmethyl Cellulose) after passing through 20 mesh screen for 15 minutes. This frst mixture is kneaded with binder solution (prepared by dissolving of NaOH in purifed water). The wet mass is dried in hot-air chamber at 50 °C, protected from light. The next step is passing the dried produced mass through oscillating granulator with 16 mesh screen. The dry granular mass is mixed with the Magnesium Stearate after passing through 80 mesh screen for about 5 minutes. After that, powder was compressed using a mini rotary press machine (Kambert Machinery Co. PVT. LTD. India) with 16 mm diameter oval concave punch. Determination of tablet hardness and thickness The hardness of tablets was determined using hardness tester (Pharma Test PTB-311F, D-63512 Hain burg, Germany). The mean of the tablet hardness was calculated for ten tablets. The thickness of tablets was determined using a digital caliper (CE ISO 9001, Guanglu Electrical Co., LTD. China) and the results were expressed as mean values of ten determinations. In vitro drug release studies An in-vitro release of Ranolazine tablets was studied using USP ABSTRACT Formulation of Ranolazine in the form of extended-release tablet in 500 mg dosage form was performed using Eudragit L100-55 as a retarding agent. Drug- release profles were investigated in comparison with the reference Ranexa extended-release 500 mg tablet. F2 and f1 were calculated as 64.16 and 8.53, respectively. According to Peppas equation, the release of drug is controlled by difusion (n=0.5). Te tablets were put into accelerated stability condition (40⁰C, 75% humidity) for 3 and 6 months. Te dissolution release profles and other physical and chemical characteristics of the tablets confrmed the robustness and stability of formulation in this condition. J Pharma Res Rep, 2021