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      Feasibility of optimizing trimetazidine dihydrochloride release from controlled porosity osmotic pump tablets of directly compressed cores

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          Abstract

          The aim of this study was to develop and optimize Trimetazidine dihydrochloride (TM) controlled porosity osmotic pump (CPOP) tablets of directly compressed cores. A 2 3 full factorial design was used to study the influence of three factors namely: PEG400 (10% and 25% based on coating polymer weight), coating level (10% and 20% of tablet core weight) and hole diameter (0 “no hole” and 1 mm). Other variables such as tablet cores, coating mixture of ethylcellulose (4%) and dibutylphthalate (2%) in 95% ethanol and pan coating conditions were kept constant. The responses studied ( Y i ) were cumulative percentage released after 2 h ( Q% 2h), 6 h ( Q% 6h), 12 h ( Q% 12h) and regression coefficient of release data fitted to zero order equation (RSQ zero), for Y 1, Y 2, Y 3, and Y 4, respectively. Polynomial equations were used to study the influence of different factors on each response individually. Response surface methodology and multiple response optimization were used to search for an optimized formula. Response variables for the optimized formula were restricted to 10% ⩽  Y 1 ⩽ 20%, 40% ⩽  Y 2 ⩽ 60%, 80% ⩽  Y 3 ⩽ 100%, and Y 4 > 0.9. The statistical analysis of the results revealed that PEG400 had positive effects on Q%2h, Q%6h and Q%12h, hole diameter had positive effects on all responses and coating level had positive effect on Q% 6h, Q% 12h and negative effect on RSQ zero. Full three factor interaction (3FI) equations were used for representation of all responses except Q% 2h which was represented by reduced (3FI) equation. Upon exploring the experimental space, no formula in the tested range could satisfy the required constraints. Thus, direct compression of TM cores was not suitable for formation of CPOP tablets. Preliminary trials of CPOP tablets with wet granulated cores were promising with an intact membrane for 12 h and high RSQ zero. Further improvement of these formulations to optimize TM release will be done in further studies.

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          Clinical spectrum of the osmotic-controlled release oral delivery system (OROS), an advanced oral delivery form.

          S. Gupta, Robert Conley, Gayatri Sathyan (2006)
          The osmotic-controlled release oral delivery system, OROS, is an advanced drug delivery technology that uses osmotic pressure as the driving force to deliver pharmacotherapy, usually once-daily, in several therapeutic areas. The purpose of this review is to discuss the evolution of OROS technology and examine the many therapeutic areas where OROS products are being used. A search of Medline and EMBASE were performed using the keywords 'OROS' and 'osmotic delivery' for the period January 1990 to June 2005. Data were also obtained from the manufacturers' websites and associated publications. OROS technology has evolved over the last 30 years, resulting in four systems: the elementary osmotic pump; the two-layer osmotic push-pull tablet; the advanced longitudinally compressed tablet multilayer formulation; and, the L-OROS system. OROS technology is employed for drug delivery in many therapeutic areas including: cardiovascular medicine, endocrinology, urology, and central nervous system (CNS) therapeutics. Two calcium channel blockers utilizing OROS technology for the treatment of hypertension are nifedipine and verapamil. Glipizide extended-release is used for the treatment of type 2 diabetes. Doxazosin is used for the treatment of benign prostatic hyperplasia, and oxybutynin for overactive bladder. Most recent developments are with drugs that affect the CNS, including the use of methylphenidate for treatment of attention deficit hyperactivity disorder, paliperidone extended-release and OROS hydromorphone, which are under clinical development for schizophrenia and chronic pain, respectively. Drug delivery using the various OROS products can result in an improved safety profile, stable drug concentrations, uniform drug effects, and reduced dosing frequency. OROS technology has also enabled the use of an effective starting dose, without the need for dose titration, which allows the achievement of symptom control much earlier than that observed with immediate-release preparations. Such attributes can enhance patient compliance and convenience, thereby ensuring efficacy and improving patient outcomes.
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            The effect of trimetazidine on cardiac function in diabetic patients with idiopathic dilated cardiomyopathy.

            Nian-Sheng Tang, Lian-Qun Cui, Hong-Jie Zhang … (2013)
            Trimetazidine is an anti-ischemic metabolic agent which improves myocardial glucose utilization. Whether it may improve cardiac function and physical tolerance in diabetic patients with idiopathic dilated cardiomyopathy is still not confirmed. In this study we have investigated the effectiveness of trimetazidine in these patients. Volunteers with diabetes and idiopathic dilated cardiomyopathy were recruited for participation in this study. Patients were randomized into two groups. One group received trimetazidine (20mg, t.i.d.) for 6 months (n=40), while another group received a placebo during the same period (n=40). All patients received an echocardiographic examination, 6-minute walk test and an inflammation biochemical analysis (C reactive protein) at baseline and after 6 months of treatment. No significant adverse events or changes in clinical or biochemical parameters were detected through the study. After 6 months, TMZ-treated patients had a significant improvement in systolic function as compared with control patients associated with an increased ratio of E/A. C reactive protein concentrations remained stable throughout the study in trimetazidine group at baseline and at the 6 month on follow up. In comparison, it increased significantly in the control group at the 6-month follow up. The NT-pro BNP levels did not change in the control group, whereas they significantly decreased in the trimetazidine group. The physical activity tolerance level improved in the trimetazidine group compared to the control group. Trimetazidine treatment was associated with a significant improvement of cardiac function and physical tolerance. Results also suggested that the inflammatory response was decreased in trimetazidine group as compared with control patients. Copyright © 2012 Elsevier Inc. All rights reserved.
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              Once-daily propranolol extended-release tablet dosage form: formulation design and in vitro/in vivo investigation.

              Yaw-Bin Huang, Yi-Hung Tsai, Wan-Chiech Yang … (2004)
              The purpose of this study was to develop and optimize the propranolol once-daily extended release formulations containing HPMC, Microcrystalline cellulose (MCC) and lactose. In vitro studies, the response surface methodology and multiple response optimization utilizing the polynomial equation were used to search for the optimal formulation with specific release rate at different time intervals. The constrained mixture experimental design was used to prepare systematic model formulations, which were composed of three formulation variables: the content of HPMC (X(1)) MCC (X(2)) and lactose (X(3)). The drug release percent at 1.5, 4, 8, 14 and 24 h were the target responses and were restricted to 15-30, 35-55, 55-75, 75-90 and 90-110%, respectively. The results showed that the optimized formulation provided a dissolution pattern equivalent to the predicted curve, which indicated that the optimal formulation could be obtained using response surface methodology. The mechanism of drug release from HMPC matrix tablets followed non-Fickian diffusion. In the vivo study, the MRT was prolonged for matrix tablets when compared with commercial immediate release tablets. Furthermore, a linear relationship between in vitro dissolution and in vivo absorption was observed in the beagle dogs.
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                Author and article information

                Contributors
                Basant A. Habib
                Journal
                Journal ID (nlm-ta): J Advanc Res
                Journal ID (iso-abbrev): J Advanc Res
                Title: Journal of Advanced Research
                Publisher: Elsevier
                ISSN (Print): 2090-1232
                ISSN (Electronic): 2090-1224
                Publication date PMC-release: 11 June 2013
                Publication date (Print): May 2014
                Publication date (Electronic): 11 June 2013
                Volume: 5
                Issue: 3
                Pages: 347-356
                Affiliations
                Department of Pharmaceutics and Industrial Pharmacy, Faculty of Pharmacy, Cairo University, Egypt
                Author notes
                [* ]Corresponding author. Tel.: +20 1002019293; fax: +20 223628246. basant_a_habib@ 123456yahoo.com
                Article
                Publisher ID: S2090-1232(13)00079-9
                DOI: 10.1016/j.jare.2013.05.005
                PMC ID: 4294720
                PubMed ID: 25685502
                SO-VID: a36c41c3-6cba-4a79-b061-362e87f85c7a
                Copyright © © 2013 Production and hosting by Elsevier B.V.
                License:

                This is an open access article under the CC BY-NC-ND license (http://creativecommons.org/licenses/by-nc-nd/3.0/).

                History
                Date received : 4 May 2013
                Date revision received : 29 May 2013
                Date accepted : 30 May 2013
                Categories
                Subject: Original Article

                Keywords: trimetazidine,controlled porosity osmotic pump tablets,factorial design,response surface methodology
                Data availability:
                Keywords: trimetazidine, controlled porosity osmotic pump tablets, factorial design, response surface methodology

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