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RAJIV GANDHI UNIVERSITYOF HEALTH SCIENCES, KARNATAKA, BANGALORE. M. PHARM. SYNOPSIS YEAR OF ADMISSION JUNE- 2012 TITLE OF THE SYNOPSIS “STUDIES ON FORMULATION AND EVALUATION OF FLOATING TABLET CONTAINING NIZATIDINE ’’ BY Mr. Rushikesh B. Katkar M.Pharm, Part-I Department of Pharmaceutics UNDER THE GUIDANCE OF Prof. SIDHARTH M. PATIL M.Pharm. DEPARTMENT OF PHARMACEUTICS. KLES’s COLLEGE OF PHARMACY, Akkol Road, NIPANI, KARNATAKA. RAJIV GANDHI UNIVERSITY OF HEALTH SCIENCES KARNATAKA, BANGALORE. ANNEXURE-II PROFORMA FOR REGISTRATION OF SUBJECTS FOR DISSERTATION 1. NAME OF THE CANDIDATE AND ADDRESS Mr. Rushikesh B. Katkar S/o –Bajirao Katkar, A/P : Balinge Tal : Karveer, Dist : Kolhapur Pin code – 416010 MAHARASHTRA 2. NAME OF THE INSTITUTION KLES’s COLLEGE OF PHARMACY Akkol road, NIPANI DIST:- BELGAUM KARNATAKA. 3. COURSE OF STUDY AND SUBJECT Master Of Pharmacy In Pharmaceutics 4. DATE OF ADMISSION JUNE - 2012 5.TITLE OF THE TOPIC “STUDIES ON FORMULATION AND EVALUATION OF FLOATING TABLET CONTAINING NIZATIDINE’’ 2 6.0 BRIEF REVIEW OF THE INTENDED WORK -: 6.1 - Need for the study A peptic ulcer is a break in the inner lining of the esophagus, stomach, or duodenum. A peptic ulcer of the stomach is called a gastric ulcer. Peptic ulcer leads to decrease the pH and mainly acetylcholine and histamine is responsible for development of peptic ulcer(Because of sensation of food). Peptic ulcers can be broadly classified into gastric ulcers and duodenal ulcers. Normally the stomach wall is protected by the mucosa against irritation of gastric acid. When the mucosa is damaged or when the stomach produces so much gastric acid that the protective lining is eroded with subsequent inflammation or necrosis, a local ulcer will develop. Peptic ulcer is usually caused by pepsin and acid a digestive stomach enzyme. The commonest symptom of peptic ulcers is intermittent abdominal pains, especially in the middle of the night or when you are hungry. Causes of peptic ulcers are: 1. Congenital hyperacidity. 2. Mental strain and emotional stress that make the nervous system stimulate the excessive production of gastric acid. 3. Undesirable eating habits, irregular meals or overeating. 4. Smoking and excessive alcohol are direct causes of increased morbidity. 5. Drugs such as aspirin and painkillers for rheumatism irritate and damage gastric mucosa.1 Drugs for peptic ulcers are mainly classified into three categories: 1. Antacids: They neutralize gastric acid, thereby relieving or eliminating the irritation and erosion to the stomach wall and the ulcer sites. Common examples include magnesium trisilicate and aluminum hydroxide. They are available in the form of Chewable pills and liquids. 2. Anticholinergics: They suppress the secretion of gastric acid, reduce Gastro intestinal movement and relieve stomach cramps. Common examples Include propantheline bromide and scopolamine methyl bromide. 3 3. H2 receptor antagonists: They are commonly known as specific drugs. They directly suppress the secretion of gastric acid. common example is cimetidine , ranitidine.2 Nizatidine is used for the treatment of acid-reflux disorders, peptic ulcer disease, active benign gastric ulcer and active duodenal ulcer. Nizatidine is a competitive, reversible inhibitor of histamine at the H2-receptors, particularly those in the gastric parietal cells. By inhibiting the action of histamine on stomach cells, Nizatidine reduces stomach acid production. Nizatidine had no demonstrable anti androgenic action. Full-dose therapy for the problems treated by Nizatidine lasts no longer than 8 weeks. It has been demonstrated that treatment with a reduced dose of Nizatidine is effective as maintenance therapy following healing of active duodenal ulcers. Nizatidine undergoes less extensive hepatic metabolism. Less than 7% of an oral dose is metabolized as N2-monodes-methylnizatidine, an H2-receptor antagonist, which is the principal metabolite excreted in the urine. Other likely metabolites are the N2-oxide (less than 5% of the dose) and the S-oxide (less than 6 % of the dose). Nizatidine is having a half-life of 1-2 hrs. The bioavailability of Nizatidine is approximately 85% with little intersubject variations. The serum concentration reaches its peak (c) within 1-2 hrs after oral administration.3 Oral delivery of drugs is by far the most preferable route of drug delivery due to the ease of administration, low cost of therapy, patient compliance and flexibility in formulation etc. Oral sustained drug delivery formulations show some limitations connected with the gastric emptying time. Variable and too rapid gastrointestinal transit could result in incomplete drug release from the device into the absorption window leading to diminished efficacy of the administered dose. It is evident from the recent research and patent literature that an increased interest in novel dosage forms that are retained in the stomach for a prolonged residence time.4 The floating drug delivery system is oral dosage form designed to prolong the residence time of dosage form, with in the gastrointestinal tract . Such dosage form having density less than that of the gastric fluid floats on the gastric juice for an extended period of time while slowly releasing the drug. On contact with the gastric fluid, the intra gastric floating dosage form forms a water impermeable colloid gel barrier around its surface and maintains bulk density of less than 1, so it remains buoyant in the gastric fluid in stomach until the entire loading dose has been released.5 Gastric emptying of dosage forms is an extremely variable process. The ability to 4 prolong and control the emptying time is a valuable asset for dosage forms which reside in the stomach for a longer period than conventional dosage forms. Drug absorption from the gastro intestinal tract (GIT) is a complex procedure and is subject to many variables. Factors affecting Gastric emptying are 1)Volume of meal 2)composition of meal 3)viscosity of meal 4)Temperature of meal 5)Body posture 6)drug interaction 7)Disease state. The small intestinal transit time is an important parameter for drugs that are incompletely absorbed. Gastro retentive systems can remain in the gastric region for several hours and hence significantly prolong the gastric residence time of drugs. Prolonged gastric retention improves bioavailability, reduces drug waste and improves solubility for drugs that are less soluble in a high pH environment. It has applications also for local drug delivery to the stomach and proximal small intestine.6 Floating drug delivery systems provides better bioavailability for the drugs that are unstable in the intestinal and colonic environment. The controlled gastric retention of solid dosage forms may be achieved by the mechanisms of mocoadhesion, flotation, sedimentation, expansion, modified shape systems.7 Hence, from the study we concluded that, it could play a good role in a therapy for peptic ulcer, which will lead to increase the gastric residence time in stomach. 5 6.2- Review of Literature-: Pannala S et. al. (2011) Have carried out preparation and in-vitro evaluation of Nizatidine immediate release tablets. Immediate release drug-containing core tablets of Nizatidine were prepared by wet granulation method by using avicel, sodium starch glycolate, PVP K-30, HPMC E 5, magnesium stearate. The obtained tablets were evaluated for weight variation, thickness, hardness, drug content, disintegration and in-vitro dissolution studies.7 Thakkar VT, et. al. (2008) Have carried out fabrication and evaluation of Levofloxacin hemihydrate floating tablet. Batches were prepared by direct compression method using gelucire 43/01 and HPMC in different ratios. Invitro release study reveals that the release rate of drug was decreased by increasing the proportion of Gelucire 43/01, 5 to 40%. The release rate of Levofloxacin hemihydrates from matrices was mainly controlled by the hydrophilic and hydrophobic polymer ratio. Optimal batch (F4 containing gelucire 43/01, HPMC K4 M) was selected by regression analysis which followed Higuchi kinetics. 8 Pare A, et. al. (2008) have carried out formulation and evaluation of effervescent floating tablet of Amlodipine besylate. The tablets were prepared in ten different formulations (F1 to F10) by employing different grades of polymers (HPMC K 100M, HPMC K15M & Carbopol 934P) and agents such as sodium bicarbonate and citric acid by direct compression technique. Amlodipine is a potent drug use for the treatment of angina & hypertension. 9 Sharad NS, et. al. ( 2010) Have carried out development and evaluation of floating tablets of Salbutamol sulphate Formulations were prepared by using HPMC sodium bicarbonate and citric acid. Formulations were evaluated for in6 vitro drug release profile, swelling characteristics. The in-vitro drug release followed Korsemeyer-Peppas kinetics and the drug release mechanism was found to be of anomalous type. For the developed formulation, the value of n was found to be 0.6039 while for the marketed formulation the value was 0.5889 indicating the anomalous transport .10 Ramesh B, et. al. (2009) has carried out development and evaluation of gastro retentive Norfloxacin floating tablets. Tablets were prepared by the wet granulation technique using polymers such as hydroxypropylmethylcellulose (HPMC K4M, HPMC K100M) and xanthan gum. Optimized formulations F4 & F9 containing HPMC K4 & HPMC K100M floated with a lag time of less than 1 min and continued to float for 24 hrs. Formulation F16 containing xanthumgum floated with a lag time of 9 min continued to float for 24 hrs.11 Bagherwal A. et. al. (2010) Studies on formulation and evaluation of floating tablets of ciprofloxacin hcl. In the present study, it was aimed to formulate floating tablet of ciprofloxacin hcl with HPMC and carbomer in different proportion (4%, 8% and 12%) by direct compression techniques using polymers lactose, magnesium streate, talc with sodium bicarbonate. All the prepared formulation were found to complies with the official tests like precompression parameter like angle of repose and post compression parameters like shape, tablet dimensions, hardness, friability test, weight variation test, floating test, content uniformity and in-vitro dissolution study. 12 7 6.3 Objectives of the study -: Following are the objectives of the present study -: 1) The current study is to develop an ideal floating drug delivery system. 2) Formulation of floating tablet by suitable method. 3) Evaluation of floating tablet for their physicochemical studies. 4) To carry out stability studies as per as ICH guidelines. 8 7.0 MATERIALS AND METHODS Materials-: Drug : Nizatidine. Polymers :HPMC, HPMC E5, MCC , sodium bicarbonate, citric acid, chitosan.etc. Additives : Magnesium stearate, Talc etc. Binding agent : PVP-K 30, etc. Distntergrant : Sodium starch glycolate etc. Method : Development of Nizatidine floating tablet by Direct compression method or any suitable method or any developed method. 7.1 - Source of Data: a) Journals such as, 1) Indian Drug. 2) Indian Journal of Pharmaceutical Sciences. 3) Indian Journal of Pharmaceutical Education and research. 4) European Journal of Pharmaceutical Sciences. 5) International Journal of Pharmaceuticals. 6) Drug Development & Industrial Pharmacy. 7) Journal of Controlled Release. b) Review articles c) World Wide Web. d) J-gate@Helinet. e) Science Direct, Pub med. f) Library: KLES’s College of Pharmacy. g) E-library: KLES’s College of Pharmacy. 9 7.2 - Method of collection of data 1) Preformulation studies for possible drug or other excipient. 2) Prepration of floating tablet of Nizatidine drug by Direct compression or any suitable method. 3) Evaluation of the various properties of Tablet. Weight variation Thickness of tablet Hardness of tablet Friability % Friability Friability test. Drug content uniformity. In vitro buoyancy studies. Swelling index In vitro dissolution studies 4) Carry out stability studies as per ICH guidelines. 7.3 - Does the study require any investigations or interventions to be conducted on patients or other humans or animals? If so, please describe briefly. “NO” (The study do not requires animal to evaluate Antiulcer activity.) 7.4 - Has ethical clearance been obtained from your institution in case of 7.3? “ NOT APPLICABLE ” 10 8.0 : Reference1) Tripathi K. D. ‘‘Essential of medical pharmacology’’,Jaypee; 2008 :627-640. 2) Satoskar R. S. , Bhandarkar S. D. ,Ainapure S. S. , ‘‘Pharmacology and pharmacotherpeutics’’,S. Chand ;2003:8th :602-609. 3) Barar F.S. K. ‘‘Essential Of pharmacotheraputics’’,S. Chand;2006:537-540. 4) Jain Amit K. , Hatila Umashankar , ‘‘A Review of Floating Drug Delivery System,’’International journal Of pharmaceutical studies and research 2011;2:1-6. 5) Dixit Nikita , ‘‘Floating drug delivery system,journal of current pharmaceutical research;2011 ,7(1):6-20. 6) Mayavanshi AA , Gajjar SS , ‘‘Floating drug delivery system to increase gastric retention Of drugs:A Review,’’Research journal pharmaceutical and technology; 2008.1(4):345-348. 7) Pannala S, Rathnanand M. ‘‘Preparation and in-vitro evaluation of Nizatidine immediate release tablets’’, Int.J. Pharm.Tech.Res 2011; 3(3):1688-92. 8) Thakkar VT, Shah PA, Soni TG, Parmar MY, Gohel MC, Gandhi TR. ‘‘Fabrication and evaluation of Levofloxacin hemihydrate floating tablet.’’, Res Pharm Sci 2008; 3(2):65-72. 9) Pare A, Yadav SK, Patil UK. ‘‘Formulation and evaluation of effervescent floating tablet of Amlodipine besylate’’, Res J Pharm Technol.2008; 1(4):526-30. 10) Sharad NS, Satej SM, Shekhar BW, Maesh RM, Kamla KC. , ‘‘Development and evaluation of floating tablets of Salbutamol sulphate,’’ Int. J. Pharm. Res. Dev 2010; 2(5):1-7. 11 11) Ramesh B, Rongala ASN, Madhusudan RY, Kishan V. Development and evaluation of gastroretentive Norfloxacin floating tablets. Acta Pharm., 2009; 59:211– 21. 12) Bagherwal A. , Kumar D. , Patidar K. ,Sharma P., ‘‘Studies On Formulations And Evaluations Of Floating Tablet Of Ciprofloxacin HCL’’, Pharmaceutical Globale;2010:1(5);1-3. 12 9. SIGNATURE OF THE CANDIDATE 10. REMARKS OF THE GUIDE 11. NAME AND DESIGNATION OF 11.1 Guide Recommended Prof. Sidharth M. Patil M. Pharm. Professor of Pharmaceutics 11.2 Signature 11.3 Co-Guide ( If any) 11.4 Signature 11.5 Head of the Department Prof. J. K. Saboji, M.Pharm Professor & Head Department of Pharmaceutics 11.6 Signature 12. 12.1 Remarks of the Chairman Principal Forwarded to the University for approval 12.2 Signature Principal Prof. J.K.SABOJI KLES’s College of Pharmacy Akkol Road, NIPANI-591237. 13