RAJIV GANDHI UNIVERSITY OF HEALTH SCIENCES,
“FORMULATION AND EVALUATION OF ORO-DISPERSIBLE TABLETS OF AMLODIPINE BESYLATE”
SYNOPSIS FOR
M.PHARM DISSERTATION
SUBMITTED TO
RAJIV GANDHI UNIVERSITY OF HEALTH SCIENCES
KARNATAKA
[pic]
BY
ALEAKHYA. K.
I M.PHARM
DEPARTMENT OF PHARMACEUTICS
PES COLLEGE OF PHARMACY
BANGALORE-560050
(2011)
RAJIV GANDHI UNIVERSITY OF HEALTH SCIENCES,
BANGALORE, KARNATAKA
ANNEXTURE –II
PROFORMA OF REGISTRATION OF SUBJECT OF DISSERTATION
| | |ALEAKHYA.K. |
|1. |NAME OF THE CANDIDATE AND ADDRESS |DEPT. OF PHARMACEUTICS, |
| | |PES COLLEGE OF PHARMACY, |
| | |HANUMANTHA NAGAR |
| | |BANGALORE -50 |
| | |aleakhyak@ |
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| | |PERMANENT ADDRESS |
| | |D/O K.VENKATESWARA RAO, |
| | |SAI DEEPA ROCK DRILLS, PLOT NO. 106., |
| | |PHASEII.,I.D.A.,CHERLAPALLY, |
| | |HYDERABAD-51 |
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| | |HYDERABAD- 51 |
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|2. |NAME OF THE INSTITUTION |PES COLLEGE OF PHARMACY |
| | |HANUMANTH NAGAR, |
| | |BANSHANKARI 1st STAGE, |
| | |BANGALORE-50 |
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|3. |COURSE OF THE STUDY AND SUBJECT |MASTER OF PHARMACY |
| | |IN PHARMACEUTICS |
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|4. |DATE OF ADMISSION TO THE COURSE | |
| | |11th July 2011 |
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|5. |TITLE OF THE TOPIC: |
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| |“FORMULATION AND EVALUATION OF ORO-DISPERSIBLE |
| |TABLETS OF AMLODIPINE BESYLATE” |
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|6. |BRIEF RESUME OF THE STUDY: |
| |6.1Need For the Study: |
| | |
| |Hypertension is the term used to describe high blood pressure. Normal B.P is 120/80mmHg. Antihypertensives are a class of |
| |drugs that are used to treat hypertension. They are classified into Diuretics, Sympatholytics, Vasodilators, Calcium channel |
| |blockers, Angiotensin II receptor blockers, Potassium channel blockers. |
| | |
| |Amlodipine besylate is a besylate salt of amlodipine, and is a long-acting calcium channel blocker. This is one of the |
| |popular and widely used drug which has gone off patent. The market size of this drug is 2 billion dollars. Presently, |
| |Amlodipine besylate is available only as tablets in 2.5, 5 and 10 mg for oral administration. |
| | |
| |The basic pharmacokinetics of this drug are: It has a half-life of 30-50 hours, has a high protein binding of 95-98%, |
| |Bioavailability is 60-65% and undergoes slow but extensive hepatic metabolism. |
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| |Despite of its popularity, as Amlodipine is available only in tablet form, the drug is not found useful to certain population|
| |like geriatrics and hospitalized patients. Orally disintegrating technique is one which meets the need of such population and|
| |is also convenient and of patient compliance. |
| | |
| |The present project work is planned for finding a best formulation that uses orally disintegrating technique for an |
| |antihypertensive drug. The aim of this study is to develop orally disintegrating tablet form of Amlodipine drug, challenges |
| |in formulation, evaluation methodologies and future aspects. |
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| |REVIEW OF LITERATURE: |
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| |Jangam VK et al., formulated and evaluated oro-dispersible tablets of Carvedilol by direct compression using Lactose and |
| |super disintegrants like Crospovidone and Sodium starch glycolate. Complete dissolution was not observed due to insolubility |
| |of Carvedilol. So solid dispersion of Carvedilol was prepared using PVP K-30 and 2%, 5%, 10% and 15% super disintegrants. |
| |Crospovidone in the concentration of 15% gave faster disintegration time in 16 sec. and shows 100% drug release within 15 |
| |min. 1 |
| | |
| |Kabra AO et al., aimed towards the formulation and in vitro evaluation of rapidly disintegrating tablets by direct |
| |compression technology using Captopril as a model drug. Rapidly disintegrating tablet of Captopril was formulated using three|
| |super disintegrants in different concentrations i.e. 4%w/w, 8%w/w and 12%w/w and one disintegrants having concentration i.e. |
| |2% w/w/, 4% w/w and 6% w/w like Croscarmellose sodium, Crospovidone, Sodium starch glycolate and Indion 414. All the batches |
| |were prepared by direct compression method using the Cadmach Single punch tablet compression machine using 8 mm flat punch. |
| |Disintegration time and drug release were taken as the basis to optimize the immediate release tablet. |
| |Prepared tablets were evaluated for thickness, hardness, friability, uniformity of weight, disintegration time, |
| |wetting time and dissolution study. Crospovidone in the concentration of 12 % gave faster disintegration in 22 |
| |seconds and shows and 80% drug release in 10 min at gastric pH is selected as the optimized formulation. The selected |
| |formulation was subjected to stability |
| |studies for thirty days which showed stability with regard to the release |
| |pattern.2 |
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| |Senthil A et al., prepared orally disintegrating tablets of Metaprolol tartarate by direct compression method using different|
| |concentration of Crospovidone as super disintegrants and different diluents. Tablets were prepared with different diluents |
| |like Mannitol, Lactose, Dibasic calcium phosphate at different concentration and tablets were evaluated. The tablet |
| |containing 6% |
| |Crospovidone and with spray dried lactose as a diluent was found to be the optimized combination due to its fast in vitro |
| |dispersion when compared to other formulations, with wetting time below 1minute.3 |
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| |Bharadwaj V et al., prepared fast disintegrating tablets of Amlodipine besylate by using super disintegrants Kollidon CL, |
| |Ac-Di-Sol and Sodium starch glycolate in varying concentrations 2%, 4%, 6%. Tablets were evaluated for weight variation, |
| |hardness, friability, disintegration time. Using the same excipients, the tablets were prepared by direct compression and |
| |evaluated. It was found that tablet prepared with Ac-Di-Sol showed average disintegration time of 16seconds in vitro that is |
| |faster than other super disintegrants used in the study.4 |
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| |Howida KI et al., developed Valsartan ODT at 40 mg dose using freeze drying technique and evaluated. Among the prepared 27 |
| |tablet formulas, formula no.6 containing 4:6 Valsartan: Mannitol and 2% Pectin was selected to be tested in vivo. Oral |
| |bioavailability of two 40mg Valsartan tablets were compared with the conventional tablets after administration of a single |
| |dose to four healthy volunteers. Valsartan was monitored in plasma by HPLC. Apparent rate of absorption of Valsartan from |
| |prepared tablets was significantly higher than conventional tablets.5 |
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| |Naik PS et al., developed Metaprolol succinate fast dissolving tablets by dry granulation using PVP in Isopropyl Alcohol as |
| |binder. Camphor and Ammonium Bicarbonate were used as subliming agents in 10% and 20% |
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| |concentration. Croscarmellose sodium (Ac-Di-Sol) and Sodium starch glycolate were used as super disintegrants (2%, 4%, 8%) |
| |separately. Sodium starch glycolate and Ac-Di-Sol hastens the disintegration of tablets due to its wicking action on contact |
| |with water. Both when used in combination have a synergistic effect on the disintegration time and dissolution of tablets.6 |
| | |
| |Pandey S et al., developed taste masking ODT that showed rapid onset of action as the dosage form is disintegrated prior to |
| |reaching the stomach and is ideal for acute diseases like hypertension and heart failure. Lisinopril was chosen and the drug |
| |is slightly bitter in taste and produces non compliance to patients especially geriatric patients. It concluded that beta |
| |cyclodextrins were useful for masking the taste as well as enhancing the solubility of the drug. Super disintegrants were |
| |helpful in formulation of fast dissolving tablets. Croscarmellose sodium is suitable for the formulation of the ODT’s.7 |
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| |Bhowmik D et al., worked on the fundamental principle, used in the development of fast dissolving tablets that is used to |
| |maximize its pore structure. They have evaluated spray dried materials and plastic materials for development of such tablets.|
| |Vaccum drying and freeze drying techniques have been tried to maximize pore structure. Freeze drying yielded a fragile and |
| |hydroscopic product. So vaccum drying technique was adopted after adding subliming agent to increase the porosity of tablets |
| |and that the tablet disintegrates quickly.8 |
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| |Bhowmik D et al., prepared fast dissolving tablets of Telmisartan by using super disintegrants Crospovidone, Ac-Di-Sol and |
| |Sodium starch glycolate at three different concentrations of 5%, 7.5%, 10%. The tablets were prepared by direct compression |
| |method and the prepared blend and tablets were evaluated for their physicochemical properties and in vitro dissolution study.|
| |The evaluation studies were performed such as weight variation, thickness, |
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| |hardness, disintegrating time, wetting time, and in vitro drug release and stability study. The disintegration time of fast |
| |dissolving tablets were increased by the addition of concentration of super disintegrants.9 |
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| |Jain CP et al., developed fast dissolving tablets of Valsartan using different super disintegrants by direct compression |
| |method. Effect of disintegrant on disintegration behavior of tablet in artificial saliva, pH 5.8 was evaluated. Wetting time |
| |of formulations containing Crospovidone was least and tablets showed fastest disintegration. The drug release from the |
| |tablets increased with increasing concentration of super disintegrants and was found to be highest with formulations |
| |containing Crospovidone.10 |
| | |
| |Raghavendra Rao N G et al., developed rapidly disintegrating Chlorthalidone oral tablets by direct compression using |
| |co-grinding and solid dispersion methods. The major problem with the drug is limited aqueous solubility which may hinder |
| |dissolution. So, the solid dispersions and co-grinding method were followed to increase solubility and bioavailability. The |
| |tablet formulation containing Polyvinyl pyrrolidine K-12 solid dispersion showed maximum drug release than Chlorthalidone |
| |Polyvinyl pyrrolidine K-12 co-grinding method. The dissolution profile of best solid dispersion formulation was compared with|
| |co-grinding method formulation. The prepared tablets were evaluated for hardness, friability, wetting time, disintegration |
| |time, and in vitro drug release. The study revealed that solid dispersion of the drug with the hydrophilic carrier Polyvinyl |
| |pyrrolidine can enhance the dissolution rate of Chlorthalidone tablets.11 |
| | |
| |Ranch KM et al., developed oro-dispersible tablets of Atenolol by using Camphor, Kyron-T314 and Lactose by direct compression|
| |technique. Tablets were evaluated for friability, wetting time and disintegration time. It was revealed that, tablets |
| |prepared using an optimum concentration of Camphor |
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| |and a higher % of Kyron-T314 disintegrated rapidly.12 |
| | |
| |Bandari S et al., have given some of the ODT technologies available. They are - Lyophilization is a process that includes |
| |removal of solvent from a frozen suspension. The tablet has rapid disintegration and dissolution but has low mechanical |
| |strength and poor stability. Molding includes moistening, dissolving/dispersing the drug with a solvent and then molding the |
| |moist mixture into tablets. It results in high porous structure. They also have low mechanical strength. Cotton candy process|
| |involves formation of matrix of polysaccharides by the action of melting and spinning. It offers good mechanical strength. |
| |Sublimation involves the presence of highly porous structure in tablet matrix and offers good porosity and disintegration of |
| |tablet. Some other techniques are Zydis technology, Phase transition process melt granulation.13 |
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| |6.3 Main objectives of the study: |
| |To carry out compatibility studies of drug and super disintegrants. |
| |To design and develop Oro-dispersible tablets of an anti hypertensive drug, Amlodipine Besylate. |
| |To carry out pre-compression and post-compression parameters. |
| |To carry out stability studies as per ICH guidelines. |
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| |MATERIALS AND METHODS: |
| |7.1 Source of data: |
| |The data will be obtained from the literature survey, internet source and experimental work, which includes formulation of |
| |Oro-dispersible tablets by using various super disintegrants, evaluation of pre-compression and post- compression parameters,|
| |evaluation of drug content and stability studies. |
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| |7.2 Method of collection of data (including sampling procedures if any) |
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| |The data will be collected from prepared formulations subjected to different evaluation techniques, estimation of water |
| |absorption ratio, wetting time, disintegration time, in-vitro drug release and stability studies. |
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| |7.3 DOES THE STUDY REQUIRE ANY INVESTIGATIONS OR INTERVENTIONS TO BE CONDUCTED ON PATIENTS OR OTHER HUMANS OR ANIMALS? |
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| |– NO – |
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| |7.4 HAS ETHICAL CLEARENCE BEEN OBTAINED FROM YOUR INSTITUTION IN CASE OF 7.3? |
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| |-Not applicable- |
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| |LIST OF REFERENCES: |
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| |Jangam VK, Javvaji H, Tadikonda R, Gollapudi R. Formulation and in vitro evaluation of oro-dispersible tablets of Carvidilol.|
| |Int J Adv Pharm Sci. 2011;2(1):50-54. |
| | |
| |Kabra AO, Shah FB, Wanare RS. Formulation and in vitro evaluation of rapidly disintegrating tablets using Captopril as a |
| |model drug. Int J Pharm Sci Rev Res. 2011;7(2):206-10. |
| | |
| |Senthil A, Hima Bindu S, Thakkar HKRB, Jamsheer AK, Vontoor BN. Development and evaluation of orally disintegrating tablets |
| |of Metoprolol tartarate by direct compression method using different diluents. Int Res J Pharm. 2011;2(1):118-25. |
| | |
| |Bharadwaj V, Shukla V, Goyal N, Salim MD, Sharma PK. Formulation and evaluation of fast disintegrating sublingual tablets of|
|7. |Amlodipine besylate using different super disintegrants. Int J Pharm & Pharm Sci. 2010;2(3):89-92. |
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| |Howida KI, Doaa AE-S. Valsartan Orodispersible Tablets: Formulation, in vitro/in vivo characterization. AAPS Pharm Sci Tech. |
| |2010;2(1):189-96. |
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| |Naik PS, Kurup NS. Design and optimization of fast dissolving tablets containing Metaprolol by sublimation method. Int Res J|
| |Pharm. 2010;1(1):346-57. |
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| |Pandey S, Viral D, Goyani M. Formulation and evaluation of taste masked fast disintegrating tablets of Lisinopril. Int J |
| |Pharm Tech Res. 2010;2(2):1639-43. |
| | |
| |Bhowmik D, Chiranjib, Jaiswal J, Dubey V, Chandira M. Fast dissolving tablet: A review on revolution of novel drug delivery |
| |system and new market opportunities. Der Pharmacia Lettre. 2009;1(2):262-76. |
| | |
| |Bhowmik D, Jayakar B, Sampath Kumar K. Design and characterisation of fast dissolving tablet of Telmisartan. Int J Pharm |
| |Recent Res. 2009;1(1):31-40. |
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| |Jain CP, Naruka PS. Formulation and evaluation of fast dissolving tablets of Valsartan. Int J Pharm & Pharm Sci. |
| |2009;1(1):219-26. |
| | |
| |Raghavendra Rao NG, Kota RK, Setty CM, Purushotham Rao K. Formulation and evaluation of fast dissolving Chlorthalidone |
| |tablets. Int J Pharm & Pharm Sci. 2009;1(1):79-87. |
| | |
| |Ranch KM, Koli AR, Bhavin VA, Parikh RK, Vyas RB, Maniyar NR, Modi JG. Formulation, design and optimization of |
| |oro-dispersible tablets of Atenolol. Int J Pharm Tech Res. 2009;1(4):1559-63. |
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| |Bandari S, Mittapalli RK, Gannu R, Yamsani MR. Oro-dispersible tablets: An overview. Asian J Pharm. 2008;2(1):2-11. |
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|8. | |
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| | |(ALEAKHYA.K) |
|9. |SIGNATURE OF CANDIDATE | |
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|10. |REMARKS OF THE GUIDE |Recommended |
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|11 |NAME AND DESIGNATION OF: | |
| | |Dr. MANJULA TALLURI |
| |11.1 GUIDE: |Professor , |
| | |Department of Pharmaceutics, |
| | |P.E.S College of Pharmacy, |
| | |Bangalore-560050. |
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| |11.2 SIGNATURE: | |
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| |11.3 CO-GUIDE: | |
| | |-NOT APPLICABLE- |
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| |11.4 SIGNATURE: | |
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| |11.5 HEAD OF THE DEPARTMENT: |Dr. SATISH C.S |
| | |Professor & Head, |
| | |Department of Pharmaceutics, |
| | |P.E.S College of Pharmacy, |
| | |Bangalore-560050. |
| | | |
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| |11.6 SIGNATURE: | |
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| | |Prof. Dr. S. MOHAN |
|12 |12.1 REMARKS OF THE CHAIRMAN& PRINCIPAL: |Principal & Director |
| | |P.E.S College of Pharmacy, |
| | |Bangalore-560050. |
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| |12.2 SIGNATURE: | |
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