Survey
* Your assessment is very important for improving the workof artificial intelligence, which forms the content of this project
* Your assessment is very important for improving the workof artificial intelligence, which forms the content of this project
FORMLULATION AND EVALUATION OF ANTI-AMOEBIC SUPPOSITORIES SYNOPSIS FOR M.PHARM DISSERTATION SUBMITTED TO RAJIV GANDHI UNIVERSITY OF HEALTH SCIENCES KARNATAKA BY B.NAGA VAIDYANATHA REDDY I M.PHARM UNDER THE GUIDANCE OF Dr. K .RAMESH PROFESSOR, HEAD OF THE DEPARTMENT DEPARTMENT OF PHARMACEUTICS KARNATAKA COLLEGE OF PHARMACY BANGALORE-560064 (2011-2012) RAJIV GANDHI UNIVERSITY OF HEALTH SCIENCES KARNATAKA, BANGALORE. ANNEXURE II PROFORMA FOR REGISTRATION OF SUBJECT FOR DISSERTATION 1 Name of the Candidate and Address B.NAGA VAIDYANATHA REDDY KARNATAKA COLLEGE OF PHARMACY # 33/2 THIRUMENAHALLI HEGDE NAGAR MAIN ROAD BANGALORE-560064. PERMANENT ADDRESS: S/0: B.SIVABALI REDDY, H.NO-25-645, SRINIVASANAGAR, NANDYAL Dist: KURNOOL, State: ANDRAPRADESH-518002 2 KARNATAKA COLLEGE OF PHARMACY Name of the Institution # 33/2 THIRUMENAHALLI HEGDE NAGAR MAIN ROAD BANGALORE-560064. 3 Course of the Study and Subject MASTER OF PHARMACY (PHARMACEUTICS) 4 Date of Admission 5 Title of the Topic FORMULATION AND EVALUATION OF ANTI –AMOEBIC SUPPOSITORIES 8thJULY 2011 1 6. Brief Resume of the Intended Work: 6.1 Need for the study The rectal route of drug delivery have been recognized as an alternative to the oral route in situations such as when the patient is comatose, unable to swallow or when the drug produces nausea or vomiting. There are several therapeutic reasons why a drug should be administered rectally than orally. One of these is that, it is possible to avoid partly hepatic first pass elimination following rectal administration. The rectal venous drainage is such that the upper part is connected with the portal system and the lower part directly with the systemic circulation. However there is no sharp distinction between these drainages, since the rectal veins are linked by an extensive anastomoses network. It has been accepted that atleast 50-70% of a drug suitable for rectal administration is absorbed via the above direct pathway. It is well recognized that drug absorption after rectal administration is in agreement to a considerable extent with the pH partition theory. In the light of this, efforts have been made in recent times to present a good number of drugs in suppository form. Rectal administration of anti-amoebic is accepted as effective prophylaxis against infection associated with surgery and as treatment of established infection. Since observation of the therapeutic effect is known to be faster by the rectal route of administration and overcomes the gastric irritation problems rectal suppositories were deemed as appropriate. Anti-amoebic in the form of rectal therapy for localized action is readily achieved and it may be feasible for rectal therapy to overcome the limitations and to realize its potential advantages. 2 6.2 Review of the literature: Nitroimidazole resistant vaginal trichomoniasis treated with intravaginal paromomycin (50mg) and trichomoniasis but resulted in severe local side effects. Paromomycin useful for different cases of nitroimidazole resistance tricomonas vaginalis vaginitis to exact dose findout.1 The bioavailability of drugs from suppositories is taken into consideration. The factors affecting bioavailability, the avoidance of first-pass effects, the role of absorption promoters, a sustained-release effect and selected therapeutic indications for the application of suppose.2 Volumetric methods were used to metronidazole with calf thymus DNA determined binding constant (k) binding site size (s). This method interaction of metronidazole with surface-conform DNA and peak current of metronidazole at the biosensor for metronidazole determination. This method applied with high precision and accuracy compared with spectroscopic methods for estimation of the total metronidazole drug content in pharmaceutical dosage forms.3 Antibacterial metronidazole used in most common therapy in the treatment of bacterial vaginosis (B.V.) this are different formulation is available creams, gels, vaginal lavages and vaginal suppositories. The aim to realize vaginal mucoadhesive tablets by including bio adhesive polymer as chitosan (FG90C), polyvinyl pyrrolidone (PVPK90) poly carbophill (pcppa) the characterized by studies of DSC, friability, hardness, mucoadhesion in vitro release and antibacterial activity. The polymers FG90C and PVPK90 (1:1 ratio) suitable formulating of metrodinazole traditional dosage forms for vaginal topical administration of in vitro bacterial inhibitor studies by using diffusion method.4 The physical and release properties of metronidazole suppositories are influenced by the bases and adjuvants employed. Tween 80 and sodium salicylate used to formulate only immediate-release suppositories while methyl cellulose also used in sustained release metronidazole suppositories bases are witepsol , polyethylene glycol, PEG 1500, PEG 6000 by using fusion method.5 3 Administration of anti microbial suppositories is accepted as effective prophylaxis against infection associated with surgery and as treatment of established infection. This study shows that in gravely ill patients metronidazole administration as suppositories gives perfectly adequate therapeutic serum concentration of the drug, but that achieve these concentration rapidly the first suppository should be given with an intravenous loading dose.6 PEG-metronidazole conjugates with in vitro and in vivo studies carried out by using metronidazole a drug used for treatment of protozoal infections. By using different conjugated to linear (or) branched polymers of polyethylene glycol 5000-OH, PEG- 20,000 -OH, Mpeg-10,000 –NHS, Mpeg-20,000-NHS. Finally the MET solubility, stability, release characterstics, and in vivo studies carried out I.V. &S.C. administration and pharmacokinetic properties up on conjugation.7 To evaluate the efficacy and tolerability of vaginal pessary treatment of vaginitis. The method involved in phase-3 studies using one vaginal pessary the reduction occurred in symptoms and signs of vaginitis the gynecological and microbiological evaluation carried out, by using microscopy and candida albicons culture. The combination of metronidazole and miconazole treatment of the most common causes of vaginitis.8 Extensively used beta- lactam antibiotics and 5- nitro imidazole used anaerobic bacteria antibiotic resistance gram negative bacilli of beta- lactam classified as 1) production 2) alteration 3) changes in outer membrane permeability. The 5- nitroimidazole molecule reduction of nitro group in the absence of oxygen the identified in bacteroides fragilis group spp. The mechanisms of resistance is critical for both the selection of antimicrobial therapy and the design of new antimicrobial agents. To review the mechanisms for and the prevalence of beta-lactam and metronidazole resistance in strain belonging to the B. fragi.9 The suppositories properties mainly depend the properties of bases.these bases properties mainly affect the formulation and evaluation of the suppositories.10 4 6.3 OBJECTIVE OF THE STUDY: The objective of the study is as follows: 1) The current study is to develop an ideal rectal drug delivery system. 2) Formulation of suppositories by suitable method. 3) Characterisation of formulated suppositories. 4) Evaluation of suppositories for their physicochemical studies. 5) Stability studies for selected formulations. 7 Materials and Methods: 7.1 Source of data: Review of literature resourced from: Journal such as . Indian journal of pharmaceutical sciences . Journal of controlled release . Indian drugs . Science direct Websites: . Word Wide Web . J-Gate@Helinet. 7.2 Method of collection of data (including sampling procedures if any): The data will be collected from prepared formulations subjected to different evaluation techniques, scale-up techniques and stability studies obtained from ICH guidelines 5 7.3 Materials Anti-amoebic drug and bases will be procured / obtained from pharma grade suitable manufacturer. All the other reagents will be of analytical grade. 7. 4 Methods 1) Preparation of suppositories by hot melting. 2) Thermal analysis. 3) Evaluation a) Visual evaluation. b) Melting point. c) Liquefaction time d) Mechanical strength. e) Solidification. f)Drug release studies 7.5 Does the study require any investigation or interventions to be conducted on patients or other humans or animals? -Does not required- 7.6 Has ethical clearance been obtained from your institution in case of 7.5? - NO – 6 8 List of References 1. Poppe AJ. Anti microbial-resistant vaginal trichomoniasis treated with paromomycin. Eur J Obstet Gynecol Reprod Biol. 2001 May 30; 96: 119- 20. 2. Hermann TW. Bioavailability of drugs from suppositories. Int J pharm 1995Jan 30; 123: 1-11. 3. Xiaohua J, Xiangqin L. Voltammetry of the interaction of metronidazole with DNA its analytical applications. Bio electrochem 2006 Aug 24; 68:206-12. 4. Luana P, Valeria A, Cinzia P, Stefania S, Carlo R. Metronidazole mucoadhesive tablets for vaginal administration. Int J Pharm 2009 May 18; 377:120-27. 5. Adegboye TA, Ltiola OA. Physical and Release Properties of Metronidazole Suppositories.Trop J Pharma Res. 2008 march 19; 7(1): 887-96. 6. Barker EM, Aitchison JM, Cridland JS, Baker LW. Rectal administration of metronidazole in severely patients. Br Med J 1983 July 30; 287: 311-13. 7. Cinzia B, Manuela B, Gianfranco P, Maria V. Metronidazole –PEG conjugates in vitro and in vivo properties. IL Farmaco 2005 July 22; 60: 783-8. 8. Fabio P, Aroldo C, Geraldo D, Iara L, Luis B, Alvaro P. Metronidazole and miconazole nitrate in treatment of vaginitis. Int J Gynaecol obstet 2008 April 10; 102: 287-92. 9. Hong F, Charlotta E, Maria H, Carlerik N. metronidazole resistant Bacteroides Fragilis group. Int J Antimicrob Agents 2002 Feb 12; 19: 361-70. 10. Lieberman A. Pharmaceutical dosage forms: Edited by Rieger M, Banker S, Martin, Gilberts. Disperse system. Second ed. New york.Academic Press s2005; p: 446-96. 7