TASTE ABATEMENT AND CHARACTERIZATION OF DISPERSIBLE TABLETS OF ARTEMETHER PREPARED BY HOT MELT EXTRUSION Original Article YOGESH A. SONAR 1* , MRUDULA H. BELE 2 , NITIN H. SONAR 3 , VISHAL S. BAGUL 4 , PRASHIK S. SHIMPI 5 1,2 Pharmaceutics Department of NDMVP Samaj’s College of Pharmacy, Nashik, 422002, 3,4,5 Received: 02 May 2017, Revised and Accepted: 10 Oct 2017 R C Patel Institute of Pharmaceutical Education and Research, Shirpur, 425405 Email: yshsonar@gmail.com ABSTRACT Objective: The aim of this study was to formulate and evaluate a taste-masked formulation using hot melt extrusion approach for artemether. Methods: Taste masking of artemether was done by preparing solid dispersion with coating polymer kollicoatsmartseal 30D using hot melt extrusion. The prepared solid dispersion was subjected to taste masking evaluation like sensory evaluation parameters against five levels set for taste evaluation using artemether as control standard along with in vitro release studies in simulated salivery fluid. After taste evaluation of solid dispersion was subjected to the formulation of dispersible tablets by direct compression method. The final taste masking evaluation of dispersible tablets of solid dispersion containing artemether were done by a sensory evaluation panel of nine members along with in vitro release study in simulated salivary and gastric fluid. Results: The percent drug content was found 35.09±0.06 % in solid dispersion. The drug excipients compatibility studies performed with the help of FTIR instrument and DSC that indicates there were no interactions between drug and polymers. Solid dispersions (1:1, 1:2, 1:3 drug polymer ratio) of artemether were evaluated by sensory evaluation panel from which 1:3 drug: polymer solid dispersion was found more palatable. Release rate study in simulated salivary fluid shown no release but shows release of drug in simulated gastric fluids which indicates that the drug was taste masked. The optimized batch of dispersible tablets (F1) were subjected for evaluation parameters like dispersion time (70±1.90), wetting time (63±1.86), etc. Dissolution studies of optimized formulation indicated that the polymer does not allow drug to release in simulated salivery pH 6.8 but shows immediate release in simulated gastric pH which also confirms taste masking efficiency of polymer. Final optimized F1 batch evaluated for taste masking evaluation by sensory evaluation panel using pure drug as control standard found to be palatable. Conclusion: It may be concluded that kollicoatsmartseal 30D could mask the taste of the drug in salivary pH and shows drug release at gastric pH which confirms its efficiency for taste masking. Keywords: Artemether, Kollicoatsmartseal 30D, Hot-melt extrusion, Taste masking, Solid dispersion © 2017 The Authors. Published by Innovare Academic Sciences Pvt Ltd. This is an open access article under the CC BY license (http://creativecommons.org/licenses/by/4.0/) DOI: http://dx.doi.org/10.22159/ijap.2017v9i6.19555 INTRODUCTION Worst the taste of the medication, the better the cure was once the prevailing attitude. Today this trend has changed and great importance is placed on the organoleptic characteristics of pharmaceutical products [1]. Oral administration of pharmaceuticals is one of the most popular method of drug delivery [2]. Organoleptic characteristics of pharmaceutical products, i.e. Taste, odor, and appearance are essential factors in assessing the patient acceptability; out of these organoleptic characteristics of taste is an important parameter governing patient compliance [3]. Some active pharmaceutical ingredients (API's) are generally associated with an unpleasant taste. The formulations containing such APIs are poorly accepted by patients and the adherence to treatment is adversely affected. Bad taste is a primary barrier while administering drugs to children. Most of the pediatricians reported that the taste and palatability were the greatest hurdles to complete treatment. Therefore. It is necessary to discover robust approaches to formulate the dosage forms to mask the unpleasant taste of the API to improve the ease of administration and palatability. Oral administration of bitter drugs with an acceptable degree of palatability is a key issue for health care providers, especially for pediatric patients. Taste masking in the present day pharmaceutical industry has become a potential tool to improve patient compliance and commercial success of the product [3-6]. The taste of any substance can be improved by two basic manipulations; either by reducing the drug solubility or by altering the ability of the drug to interact with taste receptors [7]. Artemether (ARM) drug used for the prevention of malaria and is included in the WHO list of essential medicines. Artemether is essential for rapid clearance of parasitemia and rapid resolution of symptoms. It reduces parasite numbers by a factor of approximately 10,000 in each asexual cycle, which is more than other current antimalarial (which reduce parasite numbers 100–1000-fold per cycle). Artemether is active against P. vivax as well as chloroquine sensitive and chloroquine resistant strains of P. falciparum and is also indicated in the treatment of cerebral malaria [8-12]. The objective of this study was to developed taste masked formulation of artemether which is intensely bitter in taste and is a critical problem, especially in the pediatric population. Hence, to increase the palatability of the drug it is necessary to mask the taste and to formulate a suitable dosage form to enhance patient compliance and adherence to treatment. On this background, this research was designed to address the question, whether it is possible to mask the intensely bitter taste of the poorly water soluble drug ‘Artemether’ by hot melt extrusionusing the kollicoatsmartseal 30D as a polymer for taste abatement? Oro-dispersible tablets (ODTs) entered the market in the 1980s as an alternative to tablets and it also provides an advantage particularly for pediatric and geriatric populations who have difficulty in swallowing conventional tablets and capsules MATERIALS AND METHODS [13]. Materials Artemether was received as a gift sample from ajanta pharma limited. aurangabad and IPCA laboratories limited. ratlam, India. kollicoatsmartseal 30 D was received as a gift sample from the BASF chemical company, mumbai, India. Potassium dihydrogen phosphate procured from modern Scientifics, nashik-India. Materials were used as received. Methods Preparation of drug: polymer solid dispersion by hot melt extrusion (HME) The HME was optimized by trial and error method with the help of data obtained from previous work. It was optimized first using International Journal of Applied Pharmaceutics ISSN- 0975-7058 Vol 9, Issue 6, 2017