FORMULATION AND EVALUATION OF DELAYED RELEASE …
FORMULATION AND EVALUATION OF ORODISPERSIBLE TABLETS OF FLUOROQUINOLONE DERIVATIVE
SYNOPSIS FOR
M. PHARM. DISSERTATION
SUBMITTED TO
RAJIV GANDHI UNIVERSITY OF HEALTH SCIENCES,
KARNATAKA
[pic]
BY
NAGABHUSHAN B.S
I M. PHARM.
[pic]
Department of Pharmaceutics
Dayananda Sagar College of Pharmacy
2009
RAJIV GANDHI UNIVERSITY OF HEALTH SCIENCES
BANGALORE, KARNATAKA
ANNEXURE-II
PROFAMA FOR REGISTRATION OF SUBJECTS FOR DISSERTATION
| | | |
|1. |Name of the candidate and address (in block |NAGABHUSHAN B.S |
| |letters) |I M. PHARM., |
| | |DEPARTMENT OF PHARMACEUTICS, |
| | |DAYANANDA SAGAR COLLEGE OF PHARMACY, |
| | |KUMARASWAMY LAYOUT, |
| | |BANGALORE-560078. |
| | | |
| | |PERMANENT ADDRESS |
| | | |
| | |# NO 26, KRUMBIGAL ROAD, |
| | |CHIKKAMAVALLI, |
| | |BANGALORE 560004 |
| | | |
|2. |Name of the institute |Dayananda Sagar College of Pharmacy, Shavige Malleswara Hills, |
| | |Kumaraswamy Layout, |
| | |Bangalore-560078, |
| | |Karnataka. |
| | | |
|3. |Course of study and subject |Master of Pharmacy in Pharmaceutics |
| | | |
|4. |Date of admission to course |21st May -2009 |
|5. |Title of the project: |
| | |
| |“FORMULATION AND EVALUATION OF ORODISPERSIBLE TABLETS OF FLUOROQUINOLONE DERIVATIVE” |
| 6.. |Brief resume of the intended work: |
| | |
| |6.1 Need of the study: |
| | |
| |Oral formulations have wide acceptance and solid dosage forms are popular because of ease of administration, accurate |
| |dosage, self-medication, pain avoidance and most importantly the patient compliance. Tablet is the most popular among all|
| |dosage forms existing today because of its convenience of self administration, compactness and ease of manufacturing; |
| |however, hand tremors, dysphasia in case of geriatric patients, the underdeveloped muscular and nervous systems in young |
| |individuals and in case of uncooperative patients, the problem of swallowing is common phenomenon which leads to poor |
| |patient compliance. Often times people experience inconvenience in swallowing tablet when water is not available, in the |
| |case of the motion sickness (kinetosis) and sudden episodes of coughing during the common cold, allergic condition and |
| |bronchitis1. |
| |To overcome these drawbacks, mouth dissolving tablets (MDT) or orally disintegrating tablets; (ODT) has emerged as |
| |alternative oral dosage forms. These are novel types; of tablets that disintegrate/dissolve/ disperse in saliva within |
| |few seconds. The basic approach used in development of MDT is the use of superdisintegrants, which provide instantaneous |
| |disintegration of tablet after putting on tongue, thereby releasing the drug in saliva. The bioavailability of some drugs|
| |may be increased due to absorption of drugs in oral cavity and also due to pregastric absorption of saliva containing |
| |dispersed drugs that pass down into the stomach. Moreover, the amount of drug that is subject to first pass metabolism is|
| |reduced as compared to standard tablets2. |
| |. |
| | Fluoroquinolones are widely used class of antibacterials as they have a wide spectrum of activity. They are used in |
| |urinary tract infections (norfloxacin, lomefloxacin, enoxacin, ofloxacin, ciprofloxacin, levofloxacin, gatifloxacin, |
| |trovafloxacin), prostatitis (norfloxacin, ofloxacin, trovafloxacin), acute sinusitis (ciprofloxacin, levofloxacin, |
| |gatifloxacin, moxifloxacin (Avelox), trovafloxacin), acute exacerbations of chronic bronchitis (levofloxacin, |
| |sparfloxacin (Zagam), gatifloxacin, moxifloxacin, trovafloxacin), acute exacerbations of chronic bronchitis |
| |(levofloxacin, sparfloxacin (Zagam), gatifloxacin, moxifloxacin, trovafloxacin) and community –acquired pneumonia |
| |(levofloxacin, sparfloxacin, gatifloxacin, moxifloxacin, trovafloxacin) 3. |
| | |
| |In case of chronic bronchitis, patients face difficulty in swallowing the conventional dosage form (tablets). Hence to |
| |overcome this problem, attempts will be made to formulate an orodispersable tablet containing a fluoroquinolone drug. |
| | |
| |6.2 Review of literature |
| | |
| |An attempt was made to improve the onset of action of terbutaline sulfate used in the treatment of asthma. Fast |
| |dissolving tablets of terbutaline sulfate4 were prepared by the direct compression method after incorporating |
| |superdisintegrants in different concentrations. The prepared tablets were evaluated for weight variation, thickness, |
| |hardness, friability, wetting time, drug content, water absorption ratio, in vitro disintegration time and in vitro drug |
| |release. The authors reported that the formulation containing 5% w/w concentration of polyplasdone XL was the best, which|
| |releases up to 99.33% of the drug in 10 min. |
| | |
| |An attempt was made to improve the onset of action of salbutamol sulfate, a bronchodilator, used commonly in the |
| |treatment of asthma. Fast dissolving tablets of salbutamol sulphate5 were prepared using sublimable ingredients. |
| |Evaluation of the tablets showed that all the tablets were found to be within official limits and the disintegration time|
| |for the formulations ranged from 5s to 40s. All the formulation containing microcrystalline cellulose and ammonium |
| |bicarbonate showed the least disintegration time of 5s. |
| | |
| |Khan et al, have formulated a rapid disintegrating tablet (RDT) of the taste-masked ondansetron HCl6. Taste masking was |
| |done by complexing ondansetron HCl with aminoalkyl methacrylate copolymer (Eudragit EPO) in different ratios by the |
| |precipitation method. Drug-polymer complexes (DPCs) were tested for drug content, in vitro taste in simulated salivary |
| |fluid (SSF) of pH 6.2, and molecular property. The complex with drug-polymer ratio of 8:2 did not show drug release in |
| |SSF and hence considered taste masked. Therefore, it was selected. The properties of tablets such as tensile strength, |
| |wetting time, water absorption ratio, in vitro disintegration time, and disintegration in the oral cavity were |
| |investigated. Polyplasdone XL-10 7% wt/wt gave the minimum disintegration time. Tablets of batch F4 containing |
| |spray-dried mannitol and microcrystalline cellulose in the ratio 1:1 and 7% wt/wt Polyplasdone XL-10 showed faster |
| |disintegration, within 12.5 seconds, than the marketed tablet (112 seconds). Taste evaluation of RDT in human volunteers |
| |revealed considerable taste masking with the degree of bitterness below threshold value (0.5) ultimately reaching to 0 |
| |within 15 minutes, whereas ondansetron HCl was rated intensely bitter with a score of 3 for 10 minutes. Tablets of batch |
| |F4 also revealed rapid drug release (t90, 60 seconds) compared with marketed formulation (t90, 240 seconds). Thus, |
| |results conclusively demonstrated successful masking of taste and rapid disintegration of the formulated tablets in the |
| |oral cavity. |
| | |
| |Singh et al, have formulated orodispersible tablets of meloxicam7. The tablets were made by non-aqueous wet granulation |
| |using crospovidone and mannitol. Formulated orodispersible tablets were evaluated for weight variation, friability, |
| |disintegration time, drug content, wetting time, water absorption ratio and in vitro drug release. The results showed |
| |that the presence of a superdisintegrant and mannitol is desirable for orodispersion. All the formulations satisfied the |
| |limits of orodispersion with dispersion. |
| | |
| |Radke et al, have prepared orodispersible tablets of baclofen8 using various concentrations of superdisintegrant agents |
| |like Ac-Di-Sol, crospovidone, sodium starch glycolate by direct compression method. Nine formulations having |
| |superdisintegrants at different concentration levels were prepared. These tablets were evaluated for drug content, weight|
| |variation, friability, hardness, wetting time and in vitro disintegration time. Among the formulations tablets of batch |
| |F3 containing Ac-Di-Sol showed superior organoleptic properties along with excellent in-vitro disintegration time and |
| |drug release as compare to other formulations. It was concluded that superdisintegrants addition technique is a useful |
| |method for preparing orodispersible tablets by direct compression method. |
| | |
| |Ketan et al, have developed orodispersible tablets of atenolol9 containing camphor, kyron-T 314, and lactose were |
| |prepared by direct compression technique. Camphor was sublimed by exposure of tablet to vacuum. The tablets were |
| |evaluated for percentage friability, wetting time, and disintegration time.. The results of multiple linear regression |
| |analysis revealed that for obtaining a rapidly disintegrating dosage form, tablets should be prepared using an optimum |
| |concentration of camphor and a higher percentage of kyron-T 314. The systematic formulation approach helped in |
| |understanding the effect of formulation processing variables. |
| | |
| |Rajitha et al, have formulated orodispersible tablets (ODT) of buspirone10 by wet granulation and direct compression |
| |techniques. The optimized formulation was also prepared by freeze drying method. The influence of superdisintegrants, |
| |crospovidone, croscarmellose sodium and sodium starch glycolate at three levels on disintegration time, wetting time and |
| |water absorption ratio were studied. Tablets were evaluated for weight and thickness variation, disintegration time, drug|
| |content, in vitro dissolution, wetting time and water absorption ratio. The results showed that the tablets containing |
| |crospovidone exhibit quick disintegration time than tablets containing croscarmellose sodium and sodium starch glycolate.|
| |Good correlation was observed between water absorption ratio and DT. Thus rapid disintegrating tablets of buspirone can |
| |be prepared by using crospovidone and other excipients at optimum concentration. |
| | |
| |Singh et al, have prepared fast disintegrating combination tablets of Omeprazole and Domperidone11 by using pertinent |
| |disintegrant. The tablets were prepared using mannitol as diluent and sodium saccharin as sweetening agent along with |
| |three different levels of disintegrant. The superdisintegrant used in this study were Kollidon CL, Ac-Di-Sol and SSG. The|
| |tablets were evaluated for weight variation, hardness, friability, wetting time, water absorption ratio, disintegration |
| |time (DT) and dissolution study. Using the same excipients, the tablets were prepared by direct compression and were |
| |evaluated in the similar way. Drug content was estimated by using HPLC method and also assay of sample was compared with |
| |standard drugs (Omeprazole and Domperidone). From the results obtained, it was observed that the tablet formulation |
| |prepared with 4.76% Ac-Di-Sol (internally cross linked form of sodium carboxymethylcellulose) ie.10 mg showed |
| |disintegration time of 15 seconds in vitro. Also the hardness, friability, dissolution rate and assay of prepared tablets|
| |(batch F7) were found to be acceptable according to standard limits. |
| | |
| |Ravi kumar et al, have developed Orodispersible tablets of haloperidol12 by wet granulation technique using camphor as |
| |subliming agent and sodium starch glycolate together with croscarmellose sodium as superdisintegrants. The porous |
| |granules were then compressed in to tablets. The formulations were evaluated for weight variation, hardness, friability, |
| |drug content, wetting time, in vitro and in vivo dispersion, mouth feel and in vitro dissolution. All the formulations |
| |showed low weight variation with dispersion time less than 45 seconds and rapid in vitro dissolution. The results |
| |revealed that the tablets containing subliming agent had a good dissolution profile. The drug content of all the |
| |formulations was within the acceptable limits. The optimized formulation showed good release profile with maximum drug |
| |being released at all time intervals. It was concluded that fast dissolving tablets with improved haloperidol dissolution|
| |could be prepared by sublimation of tablets containing suitable subliming agent. |
| | |
| |Shishu et al, have formulated taste masked rapidly disintegrating tablets of ofloxacin13. Taste masking was achieved |
| |using a pH sensitive polymer Eudragit E-100 (aminoalkylmethacrylate copolymers). Extrusion followed by crushing technique|
| |was used to prepare taste-masked granules. Taste masked granules were directly compressed into tablets using |
| |microcrystalline cellulose (MCC) as directly compressible filler and sodium starch glycolate (SSG) as a super |
| |disintegrant. The tablets were optimized for tensile strength and fast disintegration characteristics by varying the |
| |amounts of MCC and SSG. Finally the optimized dosage form was subjected to various evaluation tests like pharmacopoeial |
| |tests, in vitro drug release, disintegration time in oral cavity, wetting time and panel testing for taste assessment. |
| |Panel testing data indicated successful formulation of oral fast disintegration tablets with a good taste. |
| | |
| |6.3 Objective of the study: |
| | |
| | |
| |The main objective of the project is to develop an orodispersible tablet containing a fluoroquinolone derivative. |
| |Screening of GRAS listed excipients to select the most effective components to develop an orodispersible tablet. |
| |Selection of appropriate polymer in correct ratio to mask the taste. |
| |Selection of appropriate preparation methodology. |
| |Evaluation of the developed formulation for hardness, friability, drug content, disintegration time etc. |
| |Optimization of the formulations. |
|7. |Materials and methods |
| |7.1 Source of data: |
| |Official Pharmacopoeia, Standard books, International journal of Pharmaceutical sciences, Tropical journal pharmaceutical|
| |research, Indian Journal of Pharmaceutical Sciences, International journal of chemtech research, IJPER, International |
| |journal of pharmtech research, Asian journal of pharmaceutics, Asian journal of pharmaceutical and clinical research, |
| |International journal of pharmacy and Pharmaceutical sciences, AAPS pharmscitech, Pharmaceutical database and internet. |
| |Materials are obtained from authentic dealers. |
| |7.2 Method of collection of the data (including sampling procedure, if any): |
| | |
| |The pharmacological details of the drug will be collected from various standard books, journals and other sources like |
| |research literature databases such as Medline, Pubmed, Science direct, etc. |
| |Experimental data will be collected from the evaluation of designed formulation and then subjecting the formulation to |
| |different studies such as preformulation, hardness, friability, drug content, disintegration time etc. |
| | |
| |7.3. Does it require any investigation or interventions to be conducted or patients or other humans or animals? If so |
| |please describe briefly: |
| |No |
| |7.4. Has ethical clearance been obtained from your institute in case of 7.3 |
| | |
| |Not applicable |
| | |
| |List of references: |
|8. |1. Chandira MR, Mouth dissolving tablet. Pharmaceutical technology transfer, lisensing and regulatory affairs network. |
| | 2009. |
| |2. Sharma S. New Generation of Tablet: Fast Dissolving Tablet. . 2008; 6. |
| | |
| |3. Fluoroquinolone Antibiotics classification, uses and side effects. |
| |http:// 2006. |
| | |
| |4. Rangasamy M, Ayyasamy B, Raju S, Gummadevelly S. Design and evaluation of the fast dissolving tablet of Terbutaline |
| |sulphate. Asian journal of Pharmaceutics 2009; 215-217. |
| | |
| |5. Suresh S, Pandit V and Joshi HP. Preparation and evaluation of mouth dissolving tablets of Salbutamol sulphate. Indian|
| |J Pharm Sci 2007; 69:467-469. |
| | |
| |6. Khan S, Kataria P, Nakhat P, and Yeole P. Taste masking of Ondansetron Hydrochloride by polymer carrier system and |
| |formulation of rapid-disintegrating tablets. AAPS Pharmscitech 2007; 8:E1-E7. |
| | |
| | |
| | |
| | |
| |7. Singh J and Singh R. Optimization and Formulation of orodispersible tablets of Meloxicam. Trop J Pharm Res 2009; |
| |8(2):153-159. |
| | |
| |8. Radke RS, Jadhav JK, Chajeed MR. Formulation and evaluation of orodispersible tablets of baclofen. Int J ChemTech Res|
| |2009; 1(3):517-521. |
| | |
| |9. Ketan RM, Akshay KR, Bhavin VA, Rajesh PK, Ruchi VB, Neha MR, Jignasa MG. Formulation, design and optimization of |
| |orodispersible tablets of Atenolol. Int J PharmTech res 2009; 1(4):1559-1563. |
| | |
| |10. Rajitha K, Shravan Kumar Y, Adukondalu D, Ramesh Gannu and Madhusudan |
| |rao Y. Formation and evaluation of Orally Disintegrating Tablets of Buspirone. International journal of pharmaceutical |
| |sciences and nanotechnology 2009; |
| |1(4):327-334. |
| | |
| |11. Singh SK, Mishra DN, Jassal R, Soni P. Fast disintegrating combination tablets of omeprazole and domperidone. Asian |
| |journal of pharmaceutical and clinical research 2009; 2(4):54 -62. |
| | |
| |12. Ravi kumar, Patil MB, Patil SR, Paschapur MS. Development and characterization of melt-in-mouth tablets of |
| |haloperidol by sublimation technique. International journal of pharmacy and pharmaceutical sciences 2009; 1(1):65-73. |
| | |
| |13. Shishu, Kapoor VR and Kamalpreet. Taste masking and formulation of ofloxacin rapid disintegrating tablets and oral |
| |suspension. Indian J Pharm Educ Res 2009; 43(2):150-155. |
| | | |
|9. |Signature of the candidate | |
| | |(NAGABHUSHAN B.S) |
| | | |
|10. |Remarks of the guide: |Recommended for research and submission of dissertation. |
|11. |Name and Designation (in block letters) | |
| |11.1. Guide |mrs.Brahmani PRIyadarshini S.R., |
| | |ASSociate professor, |
| | |Department of Pharmaceutics, |
| | |Dayananda Sagar College of Pharmacy, |
| | |Kumaraswamy Layout, |
| | |Bangalore-560078. |
| | | |
| | | |
| | | |
| | | |
| |11.2. Signature | |
| |11.3. Co-guide if any |Not applicable |
| |11.4. Signature | |
| |11.5. Head of the department |Dr. B.WILSON, |
| | |Professor & Head, |
| | |Department of Pharmaceutics, |
| | |Dayananda Sagar College of Pharmacy, |
| | |Kumaraswamy Layout, |
| | |Bangalore-560078. |
| | | |
| | | |
| | | |
| |11.6. Signature | |
|12. |12.1. Remarks of the principal | |
| | |Dr. V. Murugan, |
| | |Principal, |
| | |Dayananda Sagar College of Pharmacy, |
| | |Kumaraswamy Layout, |
| | |Bangalore-560078 |
| | | |
| | | |
| | | |
| | | |
| | | |
| |12.2 Signature | |
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