Original Article FORMULATION DEVELOPMENT AND CHARACTERIZATION OF GASTRORETENTIVE DRUG DELIVERY SYSTEMS OF LORATADINE SRINU NAIK SAPAVATU a , RAJENDRA KUMAR JADI b* a Department of Chemical Engineering, University College of Technology, Osmania University, Hyderabad 500007, Telangana State, India, b Department of Pharmacy, University College of Technology, Osmania University, Hyderabad 500007, Telangana State, India Email: rajendra.rajaji@gmail.com Received: 02 Aug 2019, Revised and Accepted: 23 Sep 2019 ABSTRACT Objective: The main objective of the research work is to develop a single unit non-effervescent drug delivery system of Loratadine (LTD) by direct compression process to prolong the gastric residence time (GRT). Methods: LTD non-effervescent floating tablets were prepared with different polymers like hydroxypropyl methylcellulose (HPMC) K15M, HPMC K100M (i.e.: 1:1, 1:2, 1:3) as release retardants. Glyceryl behenate (Compritol 888 ATO) and Glyceryl palmitostearate (Precirol ATO 5) were used (1:1, 1:2, 1:3) as low-density lipids to impart buoyancy for longer period. Results: The drug (LTD) and excipient (i.e. HPMC, low-density lipid aids, etc.,) interaction studies were carried out by Fourier Transform Infrared Spectroscopy (FTIR) and there was no likely interaction involving them. The developed LTD floating matrix tablets were characterized by pre and post-compression parameters and all results were found within the pharmacopoeial limits. The cumulative percentage of drug release ranges from 56.87±0.25 % (F12) to 99.87±0.09 % (F2). The drug release profiles of the all formulations (F1 to F12) were subjected to various pharmacokinetic parameters and the optimized formulation (F3) followed the Korsmeyer Peppas (R 2 =0.996) model with non-Fickian diffusion (n>0.5). The obtained data by radiographic images of F3 formulation showed the GRT of 6±0.5 h (n=3). Conclusion: Hence, from all evaluation studies, it was evident that F3 formulation was optimized (99.82±1.63 % drug release in 12 h). Keywords: Buoyant, Non-effervescent, Low-density lipids, Direct compression © 2019 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.2019v11i6.35194 INTRODUCTION Oral directions of drug administration have broad recognition of up to 50-60% of whole dosage forms [1]. Oral drug delivery (i.e.: tablets, capsule, powders, emulsions, suspensions, etc.,) is considered as the most common, most popular, convenient and safe (when compared to parental route) [2]. Solid dosage forms are more popular because of ease of administration, accurate dosage, self- medication, pain avoidance and most importantly the patient compliance [3-5]. The majority accepted solid dosage forms are tablets and capsules; one of the important drawbacks of solid dosage forms; especially solids are not recommended to pediatrics, geriatrics and unconscious patients [6-8]. Gastrointestinal physiology offers additional flexibility in dosage form design than the popularity of other routes [9, 10]. The term extended-release (i.e. controlled release, sustained release, etc,) formulations are used to categorize drug delivery systems (DDS) that are considered to accomplish or extend phase of time subsequent for administration of a single dose and as an alternative to multiple dosage, having a benefit that the drug release was long- standing and it has been noticeable to pharmaceutical manufacturing [11-15]. LTD is a lipophilic, non-sedating H1 blocker and used to treat seasonal allergic rhinitis having low bioavailability (40%), and biological half-life (8 h). So, patients can avoid frequent administrations in a day [16-20]. Such frequent drug administration may reduce patient obedience and therapeutic effectiveness [21-25]. To overcome the above-mentioned problems it is required to convey the single dose for an extended period. Besides, LTD shows the greatest solubility at acidic pH and it is an appropriate candidate for the expansion of gastroretentive drug delivery systems (GRDDS). The aim of extended release (ER) DDS is to be customized in such a method with the intention; extra residence time in the stomach to release the drug before the absorption window. The goal of GRDDS is to provide a beneficial quantity of the drug to the appropriate location in the body and sustain the required drug concentration. To avoid the problems associated with the delivery of LTD, we planned to formulate LTD in an extended-release floating matrix formulation. This will allow us to reduce the frequency of administration and enhances patient compliance. To achieve the goal we have used low- density lipids or floating aids like compritol and precirol that can allow the formulation to stay on top of the gastric contents. It will avoid the first-pass metabolism and will improve the bio-availability of the formulation. MATERIALS AND METHODS Materials Loratadine received as a gift sample from Hetero Labs Ltd, Hyderabad, India. HPMC K15 M and HPMC K100 M procured from B and K Technologies, China. Compritol and precirol were purchased from Gattefosse, Germany. MCC–(Avicel PH 200), Aerosil and Magnesium stearate from SD Fine Chemicals Ltd., Mumbai. Hydrochloric acid from Merck specialities Pvt. Ltd. Mumbai, India Methods Pre-compression characterization Drug excipient compatibility studies Fourier transform infrared spectroscopy (FTIR) The drug excipient compatibility study was carried out by FTIR with in the frequency range of 4000–400 cm- 1 and 4 cm -1 resolution. The IR spectra for the test samples were obtained using the KBr disk method using an FTIR (Star Tech Labs Pvt. Ltd., Hyderabad) [26]. Differential scanning calorimetry (DSC) The differential thermal analyzer was used to find out the presence of any interaction among drug and excipients. About 5-15 mg of the sample was taken in pierced DSC aluminium pan and scanned in the temperature range of 50-300 °C and the heating rate was 10 °C/min.; nitrogen served as purged gas and the system was cooled down by liquid nitrogen [27]. I In nt te e r rn na a t ti io o n na al l J Jo ou u r rn na a l l o of f A Ap pp p l li ie e d d P Ph h a ar rm m a ac ce e u u t ti ic cs s ISSN- 0975-7058 Vol 11, Issue 6, 2019