DEVELOPMENT AND EVALUATION OF ANTIHYPERTENSIVE



DEVELOPMENT AND EVALUATION OF ANTIHYPERTENSIVE

OCULAR FILMS

SYNOPSIS FOR

M.PHARM DISSERTATION

SUBMITTED TO

RAJIV GANDHI UNIVERSITY OF HEALTH SCIENCES

KARNATAKA

BY

R.S SUDHIRKUMAR.GALLA

M.PHARM

DEPARTMENT OF PHARMACEUTICS

KARNATAKA COLLEGE OF PHARMACY

BANGALORE-560064

(2009-2010)

RAJIV GANDHI UNIVERSITY OF HEALTH SCIENCES,

KARNATAKA, BANGALORE

ANNEXURE -II

| 1 |Name of the Candidate and Address |R.S SUDHIRKUMAR.GALLA |

| | |KARNATAKA COLLEGE OF PHARMACY |

| | |# 33/2 THIRUMENAHALLI |

| | |HEGDE NAGAR MAIN ROAD |

| | |BANGALORE-560064. |

| | | |

| | |PERMANENT ADDRESSS |

| | |S/O G.V RATHNAM |

| | |YERRAGONDAPALEM(POST & M.D) |

| | |PRAKASAM(D.T.) -523327 |

| | |ANDHRA PRADESH |

| | | |

|2 |Name of the Institution |KARNATAKA COLLEGE OF PHARMACY |

| | |# 33/2 THIRUMENAHALLI |

| | |HEGDE NAGAR MAIN ROAD |

| | |BANGALORE-560064. |

| | | |

|3 |Course of Study and Subject |MASTER OF PHARMACY IN |

| | |PHARMACEUTICS |

| 4 |Date of the Admission |29th June 2009 |

| 5 |Title of the Topic: |

| | |

| |DEVELOPMENT AND EVALUATION OF ANTIHYPERTENSIVE |

| |OCULAR FILMS |

|6 | |

| |Brief resume of the intended work: |

| |6.1 Need for the study |

| |Ophthalmic drug delivery is the most comprehensive drug release for localized action and systemic therapy in order to avoid the risk of |

| |eye damage from high blood concentrations of the drug. The unique anatomy, physiology and biochemistry of the eye render this organ |

| |impervious to foreign substances, thus presenting a constant challenge to the formulator to circumvent the protective barriers of the eye |

| |without causing permanent tissue damage. |

| |Glaucoma is a disease that affects the optic nerve and involves loss of retinal ganglion cells in a characteristic pattern. The major risk|

| |factor for most glaucomas and focus of treatment is increased intraocular pressure. Intraocular pressure is a function of production of |

| |liquid aqueous humor by the ciliary processes of the eye and its drainage through the trabecular meshwork. |

| |Topical application of ophthalmically active drugs is the route of administration for treatment of various ocular disorders. It is |

| |generally assured that the intraocular bioavailability of topically applied drugs is extremely poor. This is mainly due to drainage of |

| |excess fluid by the nasolacrimal duct as well as dilution and elimination of the solution by tear turn over. Ocular bioavailability of |

| |drugs is an important parameter influencing the efficacy of ophthalmic preparations. |

| |The present work is to design ideal polymeric ocular drug delivery system to overcome the disadvantages associated with conventional |

| |ophthalmic dosage form to achieve prolonged action, to improve ocular bioavailability and to reduce the frequency of administration. |

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| |6.2 Review of the literature |

| |Yoshiyuki Ohio et al[pic]1 Pharmacokinetic and Pharmacodynamic Analysis of Systemic Effect of Topically Applied Timolol Maleate Ophthalmic|

| |Gelling Vehicle (Rysmon® TG) by using the two phases was used. In one phase, the volunteers instilled a single drop of the 0.5% timolol |

| |maleate ophthalmic gelling vehicle; in the other phase, the volunteers instilled a single drop of the 0.5% timolol maleate ophthalmic |

| |solution. The plasma concentration of timolol and the heart rates were studied during the following 120 min and 60 min, respectively. |

| | |

| |Konstantinos Natsis et al2 are studied Aerobic exercise and intraocular pressure in normotensive and glaucoma patients in the145 |

| |individuals were subdivided into seven groups: normotensives who exercised regularly (Group A); normotensives in whose right eye (RE) |

| |timolol maleate 0.5% (Group B), latanoprost 0.005% (Group C), or brimonidine tartrate 0.2% (Group D) was instilled; and primary glaucoma |

| |patients under monotherapy with β-blockers (Group E), prostaglandin analogues (Group F) or combined anti glaucoma treatment (Group G) |

| |instilled in both eyes. The IOP of both eyes was measured before and after exercise and they observe The IOP is also decreased in glaucoma|

| |patients who are already under anti glaucoma treatment. |

| | |

| |Ashish Prakash gorle et al3studied the Design and Evaluation of Polymeric Ocular Drug Delivery System by Gatifloxacin ocular inserts in|

| |the method of solvent casting method |

| |for preparing the inserts. By using the polymers of chitosan and gellan gum PEG-400 .they observed This insert are vell tolerated by the |

| |rabbit eye. similar potential was also shown by the insert based on gellan gum which showed the additional, remarkable advantages of |

| |increasing the availability in the cul-de-sac. |

| | |

| |Sreenivas sa et al4are studied the Ofloxacin ocular inserts: Design, Formulation and Evaluation they prepared with prolonged release of |

| |drug and mini-mum swelling within cul-de-sac using ofloxacin as a model drug; and hydroxy propyl methyl cellulose, methyl cellulose, poly |

| |vinyl pyrrolidone and poly vinyl alcohol as polymers. PEG-400 was incorporated as plasticizer. hey showed zero-order release of the drug |

| |in the in vitro and in vivo release studies |

| |. |

| |Juan EG et al5 is studied the Effect of Topical Timolol Maleate on the Ophthalmic Artery Blood Pressure by topical timolol maleate 0.5% |

| |on the ophthalmic artery diastolic (OABPd), systolic (OABPS) and mean blood pressure (OABPm) were investigated in 19 healthy subjects |

| |using compression Ophthalmo dynamometry Nineteen healthy volunteers aged 20 to 47 years |

| | |

| |Frais MA et al6 are studied the Ocular reaction to timolol maleate by the Adverse reactions affecting the eyes have been described with |

| |several 1-adrenoreceptor blocking agents, principally practolol. Both propranolol and oxprenolol have been incriminated in causing ocular |

| |symptoms but there are no reported instances of ocular damage due to timolol and the patient reported here developed dryness of the eyes, |

| |which improved subjectively on withdrawal of timolol. |

| | |

| |Attama AA et al7 are studied Sustained Release and Permeation of Timolol from Surface-Modified Solid Lipid Nanoparticles through |

| |Bioengineered Human Cornea by using the surface-modified solid lipid nanoparticles sustained delivery system of timolol hydrogen maleate, |

| |a prototype ocular drug using a human cornea construct. Surface-modified solid lipid nanoparticles containing timolol with and without |

| |phospholipid were formulated by melt emulsification with high-pressure homogenization and Drug transport studies through cornea |

| |bioengineered from human donor cornea cells were carried out using a modified Franz diffusion cell and drug concentration analyzed by |

| |high-performance liquid chromatography. |

| | |

| |Rebuffat P et al8 are studied the trophic effects of the renin-angiotensin system on the rat adrenal zona glomerulosa by stereological and|

| |radio-immunological techniques the effects of renovascular hypertension and of prolonged administration of timolol maleate on the zona |

| |glomerulosa of adult rats and they observed the pure ,-adrenergic blocking agent, suppresses rennin release in the normal rat kidney. |

| | |

| |Türkdemir MH et al9are studied the Volta metric Determination of Timolol Maleate: A b-Adrenergic Blocking Agent by the Investigation of |

| |the electrochemical behavior of timolol |

| | |

| |maleate on a mercury drop electrode reveals the presence of a specific reduction peak of analytical significance. Analysis conditions |

| |affecting the properties of this peak were optimized by a systematic study. The limit of detection of about 2.5 ppb, obtained for the DPV |

| |technique using SMDE, is comparable with the most sensitive techniques. |

| | |

| |Hemanta Kumar Sharma et al10are studied the Preparation and in-vitro evaluation of mucoadhesive microbeads containing Timolol Maleate |

| |using mucoadhesive substances of Dillenia indica L. Microbeads of Timolol Maleate containing NMS were formulated with the aim of |

| |developing new formulation with the fruit of Dillenia indica and Timolol maleate and timolol microbeads by the method of ionotropic |

| |gelation method. |

| | |

| |Jagdish balasubramaniam et al11are studied the In vitro and in vivo evaluation of the Gelrite® gellan gum-based ocular delivery system |

| |for indomethacin and by using the polymers like Bovine serum albumin (BSA), lysozyme and _-globulin and they concluded Indomethacin was |

| |successfully formulated as an in situ gelling system using gellan. The formulated systems provided sustained release of the drug over an |

| |8-hour period in vitro and the developed formulations were devoid of any deleterious effect on the ocular tissues. |

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| |6.3 Main objective of the study: |

| | |

| |The objective of the study is as follows: |

| |To develop an ideal ocular drug delivery system. |

| |Formulation of ocular film by suitable methods. |

| |Evaluation of the prepared formulations |

| |Selected formulations are subjected for invitro release studies. |

| |Stability studies for selected formulations. |

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| |Materials and Methods: |

| |7.1 Source of data |

| |Review of literature from: |

| |Journals such as |

| |Indian Journal of Pharmaceutical Sciences |

| |Journal of Controlled Release |

|7 |Indian Drugs |

| |Web sites : |

| |World wide web. |

| |Science direct. |

| |J-Gate@Helinet. |

| |7.2 Materials |

| |Anti Hypertensive Drug and Polymers will be procured from suitable Pharma grade Manufacturer. Other reagents will be of analytical grade. |

| |7.3 Methods |

| |1) Preparation of Ocular Films by Solvent Casting Technique |

| |2) Evaluation |

| |a) Film Thickness |

| |b) Weight Variation |

| |c) Drug Content |

| |d) Percentage Moisture Absorption |

| |e) Percentage Moisture Loss |

| |f) Folding Endurance |

| |g) Tear Fluid |

| |h)Drug release studies |

| |3) Stability studies as per ICH guidelines |

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| |7.4 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. |

| |. |

| |7.5 Does the study require any investigation or interventions to be |

| |conducted on patients or other humans or animals? |

| |- Does not required - |

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| |7.6 Has ethical clearance been obtained from your institution in case of |

| |7.5? |

| |- Yes – |

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| |List of References |

| |1.Yoshiyuki O, Risa T, Tatuji L, Yasuhiko Y. Cur Eye Res2005; Vol. 30, No. 4, Pg 319-323. |

| |2.Konstantinos N, Asouhidou I, George N, Theodosios C, Vasilios K. Aerobic exercise and Intraocular pressure in nor motensive and |

| |glaucoma patients .BMC ophthalmol 2009 August 13; 9: 6 2415-2426. |

| |3.Ashish P G, Surendra GG. Design and Evaluation of Polymeric Ocular Drug Delivery System. Chem Pharm Bull .2009 June 5; 57(9)914-919. |

|8 |4. Sreenivas SA, Hiremath SP, Godbole AM. Formulation and Evaluation of Ofloxacin Ocular Inserts. Iran j Pharmacol Ther. 2006 January 13; |

| |52: 159-162. |

| |5.Juan EG, Candace F. Effect of Topical Timolol Maleate on the Ophthalmic Artery Blood Pressure. Invest Ophthaimol Vis Sci.1989 June 6; |

| |30: 1095-1096. |

| |6. Frais MA, Bayley TJ. Ocular reaction to Timolol Maleate. Pg med j.1979 December; 55:884-885. |

| |7. Attama AA, Reichl S, Muller GCC .Diclofenac Sodium delivery to the eye. In vitro evaluation of novel solid lipid Nanoparticle |

| |formulation using human cornea construct. Int J Pharm. 2009 April 28; 355:307–313. |

| |8. Rebuffat P, Belloni AS, Mazzocchi G, Vassanelli P, Nussdorfer GG. A Stereological Study of the trophic effects of the Renin-Angiotensin|

| |system on the rat adrenal zona glomerulosa. |

| |J Anat.1979 October 20; 129-3:565-570. |

| |9. Turkdemir MH, Erdogdu G, Aydemir T, Karagozler AA, Karagozler AE. Volta metric Determination of Timolol Maleate: A b-Adrenergic |

| |Blocking Agent. J anal chem.2002; 56:1047-1050. |

| |10. Hemanta K S, Sarangi B, Prasad PS. Preparation and in-vitro evaluation of mucoadhesive microbeads containing Timolol Maleate using |

| |mucoadhesive substances of Dillenia indica L. Arch Pharm Sci Res.2009 October;1 no 2:181-188. |

| |11.Balasubramaniam J ,Shrikant ,Jayanta kP. In vitro and in vivo evaluation of the Gelrite® gellan gum-based ocular delivery system for |

| |indomethacin. Pharmazie..2003 October 14;53:251-261. |

| | |

| | |

| | |

| | |

| |List of References |

| |1.Yoshiyuki O, Risa T, Tatuji L, Yasuhiko Y. Cur Eye Res2005; Vol. 30, No. 4, Pg 319-323. |

| |2.Konstantinos N, Asouhidou I, George N, Theodosios C, Vasilios K. Aerobic exercise and Intraocular pressure in nor motensive and |

| |glaucoma patients .BMC ophthalmol 2009 August 13; 9: 6 2415-2426. |

| |3.Ashish P G, Surendra GG. Design and Evaluation of Polymeric Ocular Drug Delivery System. Chem Pharm Bull .2009 June 5; 57(9)914-919. |

| |4. Sreenivas SA, Hiremath SP, Godbole AM. Formulation and Evaluation of Ofloxacin Ocular Inserts. Iran j Pharmacol Ther. 2006 January 13; |

| |52: 159-162. |

| |5.Juan EG, Candace F. Effect of Topical Timolol Maleate on the Ophthalmic Artery Blood Pressure. Invest Ophthaimol Vis Sci.1989 June 6; |

| |30: 1095-1096. |

| |6. Frais MA, Bayley TJ. Ocular reaction to Timolol Maleate. Pg med j.1979 December; 55:884-885. |

| |7. Attama AA, Reichl S, Muller GCC .Diclofenac Sodium delivery to the eye. In vitro evaluation of novel solid lipid Nanoparticle |

| |formulation using human cornea construct. Int J Pharm. 2009 April 28; 355:307–313. |

| |8. Rebuffat P, Belloni AS, Mazzocchi G, Vassanelli P, Nussdorfer GG. A Stereological Study of the trophic effects of the Renin-Angiotensin|

| |system on the rat adrenal zona glomerulosa. |

| |J Anat.1979 October 20; 129-3:565-570. |

| |9. Turkdemir MH, Erdogdu G, Aydemir T, Karagozler AA, Karagozler AE. Volta metric Determination of Timolol Maleate: A b-Adrenergic |

| |Blocking Agent. J anal chem.2002; 56:1047-1050. |

| |10. Hemanta K S, Sarangi B, Prasad PS. Preparation and in-vitro evaluation of mucoadhesive microbeads containing Timolol Maleate using |

| |mucoadhesive substances of Dillenia indica L. Arch Pharm Sci Res.2009 October;1 no 2:181-188. |

| |11.Balasubramaniam J ,Shrikant ,Jayanta kP. In vitro and in vivo evaluation of the Gelrite® gellan gum-based ocular delivery system for |

| |indomethacin. Pharmazie..2003 October 14;53:251-261. |

| | | |

|9 |Signature of the Candidate | |

| | | |

| | |[ R.S SUDHIRKUMAR.GALLA] |

| | |

|10 |Remarks of the Guide |

| |The topic selected for dissertation is satisfactory. Adequate equipment and chemicals are available to carry out the project work. |

| | | |

|11 | | |

| |Name and Designation | |

| | | | |

| |11.1 |Guide |MRS.BENY BABY,M.PHARM, (PhD) |

| | | |ASST.PROFESSOR |

| | | |DEPARTMENT OF PHARMACEUTICS |

| | | |KARNATAKA COLLEGE OF PHARMACY |

| | | |#33/2, THIRUMENHALLI, |

| | | |HEGDE NAGAR MAIN ROAD, |

| | | |BANGLORE-64. |

| |11.2 |Signature of Guide | |

| | | | |

| | | |[ Mrs.BENY BABY] |

| |11.3 |Co-Guide | |

| | | |Not Applicable |

| |11.4 |Signature of Co-Guide | |

| | | |Not Applicable |

| | | | |

| |11.5 |Head of the Department |DR.K. RAMESH. |

| | | |PRINCIPAL & HEAD OF THE DEPARTMENT |

| | | |DEPARTMENT OF PHARMACEUTICS |

| | | |.KARNATAKA COLLEGE OF PHARMACY |

| | | |#33/2, THIRUMENHALLI, |

| | | |HEGDE NAGAR MAIN ROAD, |

| | | |BANGLORE-64 |

| |11.6 |Signature of HOD | |

| | | | |

| | | | |

| | | |[ DR.K. RAMESH] |

| | | |

|12 |12.1 |Remarks of the Principal |

| | | |

| | |All the required facilities will be provided to carry out dissertation work under the supervision of guide |

| | | | |

| |12.2 |Principal |DR.K. RAMESH. |

| | | |PRINCIPAL |

| | | |KARNATAKA COLLEGE OF PHARMACY |

| | | |#33/2, THIRUMENHALLI, |

| | | |HEGDE NAGAR MAIN ROAD, |

| | | |BANGLORE - 64. |

| | | | |

| | | | |

| |12.3 |Signature of the Principal | |

| | | |[DR.K.RAMESH] |

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