Formulation & Evaluation of Fast dissolving Buccal films of Sertraline

The hydrochloride of Sertraline is a white crystalline powder; slightly soluble in water and freely soluble in ethanol [1]. It is a drug of selective serotonin reuptake inhibitors (SSRI) that is chemically unrelated to other SSRIs, tricyclic, tetracyclic, or other available antidepressant drugs. Sertraline inhibit the inactivation of serotonin (5hydroxytryptamine or 5-HT) by blocking its absorption in the central nervous system [2]. SSRIs are used to treat depressions and effective for obsessive-compulsive disorder, posttraumatic stress disorder, premenstrual dysphoric mood disorder, panic disorder, generalized anxiety disorder and bulimia. The films were prepared from polymers such as polyvinyl pyrrolidone, Carbopol 934P in different ratios by solvent casting method. Propylene glycol or PEG 400 as plasticizers and mannitol or sodium saccharin as sweeteners were also included. Satisfactory results were obtained when subjected to physico-chemical tests such as weight variation, thickness and folding endurance. Films were also subjected to in vitro drug release studies by using USP dissolution apparatus. In vitro release studies indicated 90-95% release within 1 hr. *Corresponding author, Mailing address: Apoorva Mahajan (PGPM 1 Year) International school of Business & Finance, 15 A, Ring Road, Lajpat Nagar-4, New Delhi 24. E mail: [email protected] Contact No. 08447234658 Fax No. 01140430020 Article History:-----------------------Date of Submission: 06-01-2012 Date of Acceptance: 25-01-2012 Conflict of Interest: NIL Source of Support: NONE F U L L L e n g t h R e s e a r c h P a p e r C o v e r e d i n I n d e x C o p e r n i c u s w i t h I C V a l u e 4 .6 8 f o r 2 0 1 0 Int. J. Drug Dev. & Res., Jan-March 2012, 4 (1): 220-226 Covered in Scopus & Embase, Elsevier 220 esophagus as the saliva passes down into the stomach. In such cases, bioavailability of drug is significantly greater than those observed from conventional tablet dosage form [2]. Most fastdissolving delivery system films must include substances to mask the taste of the active ingredient. This masked active ingredient is then swallowed by the patient's saliva along with the soluble and insoluble excipients. Improved patient compliance is a primary benefit of the fast-dissolving drug delivery systems. Fast dissolving buccal films provide ease of administration for patients who are mentally ill, disabled and uncooperative; requires no water; have quick disintegration and dissolution of the dosage form. They can be unobstructive and can be designed to leave minimal or no residue in the mouth after administration and also provides a pleasant mouth feel. This delivery system has no risk of chocking. It allows high drug loading and has the ability to provide advantages of liquid medication in the form of solid preparation [3]. Fast dissolving buccal film is a drug delivery film that is placed on a mucosal or in oral cavity. They provide suitability for a wide variety of drugs. It has improved bio-availability for certain therapeutic ingredients. It has small size for improved patient compliance. As most of the drugs are unpalatable, fast dissolving buccal films usually contain a medicament in taste masked form. Films has ability to dissolve rapidly without the need for water provides an alternative to patients with swallowing disorders as a result of extremities and dysphasia, and to patients suffering from nausea, such as those patients receiving chemotherapy. It is the newest frontier in drug delivery technology that provides a very convenient means of taking medications and supplements. There are multiple fast-dissolving over the counter and prescribed products on the market worldwide, most of which have been launched recently. There have also been significant increases in the number of new chemical entities under development using a fast-dissolving drug delivery technology. Sertaline an antidepressant drug, which exhibits only 44% of oral bioavailability because of extensive first pass metabolism and has low solubility [4]. In view of all the above reasons, this study will be an attempt to optimize the therapeutic effect of sertraline by formulating as fast mouth dissolving films for sublingual use. Following are the structure and values of various parameters given for Sertraline in Table 1. IUPAC NAME: (1S,4S)-4-(3,4-dichlorophenyl)-Nmethyl-1,2,3,4--tetrahydronaphthalen-1-amine4. Table 1: Determination of values of different parameters for Sertraline Parameters Value Molecular weight 342.69 Melting point 246-249 oC[1] Log P 5.06[3] pKa 9.545 Half life 26 hrs Protein binding 98.5%[3-4] Bioavailability 44%[4] Dose 12.5200 mg daily[3] Water solubility 4mg/ml[5] The present study aims to improve the bioavailability of sertraline with reduced systemic effects by using a novel approach of fast dissolving buccal films • To formulate a suitable delivery system for delivery of sertraline. • To characterize and evaluate the delivery system