DESIGN AND EVALUVATION OF TOPICAL

ETORICOXIB GEL

M.Pharm. Dissertation Protocol

Submitted to the

Rajiv Gandhi University of Health Sciences, Karnataka.

Bangalore.

By

c.SOUJANYA

B.Pharm.

under the guidance of

Mr. P. RAVI PRAKASH,

Assistant. Professor,

Dept. of Pharmaceutics.

DEPARTMENT OF PHARMACEUTICS

N.E.T. PHARMACY COLLEGE, RAICHUR.

2007

Rajiv Gandhi University of Health Sciences, Karnataka

Bangalore

ANNEXURE II

PROFORMA FOR REGISTRATION OF SUBJECTS FOR DISSERTATION

1 / Name of candidate and address (In Block Letters) / C.SOUJANYA D/O C.MAHA RUDRAPPA, H-NO. 7-137, (MAMATALA KOVELA), SRINIVASA COLONY, MAHABUBNAGAR, ANDHRA PRADESH,
2 / Name of the Institute / N.E.T.PHARMACY COLLEGE,
RAICHUR.
3 / Course of study and subject: / M.PHARM. PHARMACEUTICS.
4 / Date of admission of course: / 12-06-2007
5 / Title of the topic:
DESIGN AND EVALUATION OF TOPICAL ETORICOXIB GEL
6 / Brief Resume of this intended work:
6.1 Need of the study Enclosure-I
6.2 Review of Literature Enclosure-II
6.3 Objectives of study Enclosure-III
7 / Materials and Methods:
7.1 Source of data Enclosure-IV
7.2 Method of collection of data (Including Sampling procedure, if any)
Enclosure-V
7.3 Does the study require any investigation or interventions to be conducted on patients of humans or animals ? If so, please describe briefly.
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7.4 Has ethical clearance been obtained from your institution in case of 7.3 ?
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8. / List of references Enclosure- VI
9 / Signature of the candidate
10 / Remarks of the Guide / The proposed work can be carried out in the laboratory
11 / Name and designation of
(in block letters)
11.1 Guide
11.2 Signature / MR. P. RAVI PRAKASH, Asst. Professor. Dept. of Pharmaceutics,
N.E.T.Pharmacy College,
Raichur-584103.
11.3 Co-Guide (if any)
11.4 Signature / ------
------
11.5 Head of Department
11.6 Signature / PROF. H. DODDAYYA,
Dept. of Pharmaceutics,
N.E.T.Pharmacy College,
RAICHUR-584103.
12 / 12.1 Remarks of the Chairman and Principal
12.2 Signature / PROF. H. DODDAYYA,
Principal,
N.E.T.Pharmacy College,
RAICHUR-584103

ENCLOSURE-I

6) Brief resume of the work.

6.1) Need for the study:

The purpose of topical dosage is to conveniently deliver drugs to a localized area of the skin1. topical creams and gels for the regional therapy of non-steroidal anti-inflammatory drugs(NSAIDs) have been used in many countries, and an effective therapy requires sufficient drug concentrations to evoke a desired pharmacological effect within target tissues. Recent studies2 have shown that after topical application, significant levels of anti-inflammatory drugs were found in deep tissues such as facia, muscle, and synovium, which is a desirable feature for the relief of local symptoms, while reducing potential systemic side effects.

Gels are semisolid systems that consists of either suspensions of small inorganic particles or large organic molecules interpenetrated by a liquid. Gels can either be water based (aqueous gels) or organic solvent based (organogels)3. gels for dermatological use have several favorable properties such as being thixotropic, greaseless, easily spreadable, easily removable, emollient, nonstaining, compatible with several exipients, and water-soluble or miscible4.

Etoricoxib is a non-steroidal anti-inflammatory drug (NSAID), which is a potent and highly selective cyclooxygenase-2 inhibitor5. NSAIDs are used mainly to treat pain and arthritis6. Etoricoxib produces dose dependent inhibition of COX-2 without inhibition of COX-1. It is indicated for osteoarthritis, rheumatoid arthritis, primary dysmenorrheal, post operative dental pain, low-back ache etc.7

Etoricoxib when presented in the form of topical gel can reduce local inflammations. Although the gel formulation of etoricoxib is highly useful there is lack of literature on the formulation and evaluation of etoricoxib gel. Hence in the present workis planned to prepare and evaluate etoricoxib gel for topical application

ENCLOSURE-II

Review of literature:

  1. Chowdary et al. (1998)8 reported eight topical drug delivery systems belonging to anhydrous, cream (o/w and w/o), water soluble and gel categories for Ciprofloxacin. Overall, the gels prepared by PEG, CMC sodium exhibited higher antimicrobiologicl activity when compared to cream and anhydrous bases.

2. Arul et al. (1998)9 reported the formulation and evaluation of keterolac tromethomine gels prepared by using various concentrations of carbopol. The anti-inflammatory activity was compared with marketed gel formulation.

3. Ilango et al. (1998)10 the effect of polymer concentration on in vitro Nimesulide release from carbopol 940, HPMC gels and SLS at different concentrations.. HPMC and Carbopol based Nimesulide gels showed promiosing diffusion behavior and exhibited good anti inflammatory effect in rats.

4. Amin et al. (1998)11 reported the preparation and evaluation of ketorolac tromethamine gels for ocular anti inflammatory effect in rabbits. They were prepared by using Carbopol 940, HPMC, Sodium CMC, etc. Carbopol gel showed the maximum in vitro release rate. All gels exhibited no ocular irritation and good anti inflammatory effect.

5. Padamwar et al. (2003)12 reported the preparation and evaluation of sericin gels containing choline salicylate. The rheological and adhesive properties of sericin were suitable for the preparation of sericin gels containing choline salicylate.

6. Jagtap et al. (2003)13evaluated the efficacy, safety and tolerability of Valdecoxib (1%) gel in adult patients with painful inflammatory joint disease. They found that Valdecoxib gel is effective in reducing the inflammation satisfactorily. The laboratory values were found with in normal limits. There were no reports of any hypersensitivity reactions.

7. Mandip singh et al. (2005) 14formulated and evaluated topical formulation of spantideII with and without n-methyl-2-pyrrolidone(nmp) as penetration enhancer. The in vivo studies indicatedthat spantide II formulations in nmp were effective in significantly reducing allergic contact dermatitis (ACD) response.

8. Gendy AEL et al. (2002)15formulated and evaluated different gel and ointment formulations of flurbiprofen using carbopol 934P (CAB), poloxamer 407 (POL), and eudragit S100 (EUD) as gel bases, while emulsion (EML) and polyethylene glycol (PEG) ointments were employed. It has been reported that the CAB and POL gels could be the vehicles of choice for rapid release and onset of flurbiprofen after topical application.

ENCLOSURE-III

6.3) Objectives of the study.

The present study is planned with the following objectives:

1) To prepare the Etoricoxib topical gels using different gelling agents.

2) To evaluate the gels with respect to various physicochemical parameters.

3) To evaluate the gels for in vitro release studies.

4) To carry out stability studies of different temperature and humidity conditions.

ENCLOSURE-IV

7) Materials and Methods

7.1) Source of data.

Primary data: This data will be collected by conducting laboratory experiments and recording the observation.

Secondary data: This will be collected from various journals and textbooks.

ENCLOSURE-V

7.2. Method of collection of data:

The data for the study is planned to collect from the laboratory based experiments, which include the following –

The gels of Etoricoxib will be prepared by using polymers like carbopol, HPMC, HPC, Sodium alginate, Sodium CMC, etc. Attempts will be made to use cost effective and natural polymers.

The gels will be evaluated for various physicochemical characteristics like drug content, viscosity, spreadability, etc. They will also be evaluated for in vitro drug release studies using diffusion cells. Finally they will be subjected to stability studies of different conditions of temperature and humidity.

ENCLOSURE-VI

8) List of references :

  1. David AO; Anton HA. Topical Drug Delivery Formulations. David AO; Anton HA; Eds; Marcel Dekker. Inc.: NewYork, 1990;P.1.
  1. Monteiro-Riviere NA; Inman AD; Riviere JE; McNeill SC; Francoeur; ML Pharm. Physicochemical and release studies of Naproxen in poloxamer gels. Res.1993; 10: 1326.
  1. B. Anand; Pisal SS; Paradkar AR; Mahadik KR. Applications of organogels in pharmaceuticals, J Sci Ind Res. 2001; 60(4): 311-318

.

  1. Klich CM Jels and Jellies In; Swarbrick J; Boylan JC; eds. Encyclopedia of pharmaceutical technology. Vol6.New York. NY:Marcel Dekker Inc.1992; 6: 415 –439.

5. Deborah J; Cochrane B; Jarvis G; Keating; Adis new drug profile; etoricoxib. Drug 2002; 62(18): 2637.

6. Capone ML; Tacconelli S; Sciulli MG; Patrignani P. Clinical pharmacology of selective COX-2 inhibitors. Int J Immunopathol Pharmacol. 2003; 16(2):Suppl:49-58.

7. Matsumato AK; Cavanaugh PF Jr. Etoricoxib. Drug today (Barc) 2004; 5: 395-414.

8. Chowdary KPR; Appan Kumar P. Release and antimicrobial activity of ciprofloxacin from topical drug delivery systems. The Eastern Pharmacist. 1998; 7: 135-136.

9. Arul B; Satyamurthy D. Formulation and evaluation of ketorolac tromethamine gels. The Eastern Pharmacist. 1998; 7:135-136.

10. Ilango R; Kavimani S; Senthil kumar K; Deepa KR; Jaykar B. Formulation and evaluation of transdermal preparations of Nimesulide. The Eastern Pharmacist. 1998;11: 123-125.

11. Amin PD; Tayade PT; Davse VV. Evaluation of keterolac tromethamine gels for ocular anti-inflammatory activity in rabbits. The Eastern Pharmacist 1998; 12: 127-130.

12. Padamwar MN; Pawar AP. Preparation and evaluation of sericin gels containing choline salicylate. Indian Drugs 2003; 9:526-531.

13. Jagtap SA; Chincholi S; Taneja PK; Ismail ND; Ram S; Sarvagad SB; Dongre N; Desai A. Evaluation, efficacy, safety and tolerability of Valdecoxib gel (1%) in adult patients with painful inflammatory joint disease. J Indian Med Assoc. 2003; 101(12): 764, 766, 727.

14. Loice kikwai; Jayachandra Babu R; Renata prado; Alexandra Kolot; Armstrong Cheryl A; Ansel John C; Mandip Singh. In vitro and in vivo evaluation of topical formulations of Spantide II. AAPS Pharma Sci Tech 2005; 6: E565-E572.

15. Gendy AME; Jun HW; Kassem AA. In vitro release studies of Flurbiprofen from different topical formulations. Drug Dev Ind Pharm. 2002; 28: 823-831.