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pharm tox

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1Continental J. Pharmacology and Toxicology Research 2: 1 - 5, 2008.© Wilolud Online Journals, 2008.A COMPARATIVE EVALUATION OF 0.3% EYE DROPS AND IN SITU FORMING GEL OF PEFLOXACINMESYLATE IN EXPERIMENTALLY INDUCED PSEUDOMONAS CONJUNCTIVITISSuman Yadav
1
and Nayyar Parvez
2
 
1
Department of Chemistry, Advanced Institute of Technology, MD University Rohtak, Distt. Faridabad, Haryana, India.
2
Department of Pharmaceutics, Advanced Institute of Pharmacy, MD University Rohtak, Distt. Faridabad, Haryana, India.ABSTRACTThe authors evaluated and compared the efficacies of eye drops and in situ forming gel of pefloxacinmesylate in
 pseudomonas
induced conjunctivitis in 40 rabbits. The in-situ forming gel of pefloxacinmesylate was formulated as a liquid and when administered in the cul-de-sac, it gets converted to gel.The objective of the present research work was to demonstrate the in vivo activity of in situ gellingformulation and compared with marketed eye drops. No difference was obtained in all parameters of conjunctivitis on day 0, between in situ gelling formulation (Group I) and marketed eye drops (GroupII), indicating that severity of conjunctivitis was similar initially between the two groups. Comparisonof scores obtained with marketed eye drops and in situ gel formulation indicated that in situ gellingformulation was faster in relieving symptoms of conjunctivitis. The findings of the present studyindicate that in situ forming gel of pefloxacin mesylate is a potential delivery system for the treatmentof 
 pseudomonas
induced conjunctivitis.KEY WORDS: Pefloxacin mesylate, conjunctivitis, in situ forming gel.INTRODUCTION
Pseudomonas aeruginosa
(
P.aeruginosa
) causes severe and rapid ocular infection and is one of the most common cause of bacterial conjunctivitis (Wilson and Ahearn, 1977).The mainstay of medical therapy for
P.aeruginosa
induced conjunctivitis is aminoglycosides. But they suffer fromdisadvantages of limited spectrum, poor ocular penetration, high cost and side effects (Fuginele
et al
, 1965, Bowe
et al
,1991). Emergence of aminoglycoside resistant
 pseudomonas
strain is an added drawback for their use in
P. aeruginosa
 conjunctivitis Flouroquinolones are one of the promising group of antibiotics, already demonstrated to possess good anti-pseudomonas activity. This group includes enoxacin, norfloxacin, ciprofloxacin, ofloxacin, and more recently gatifloxacin.These antibiotics are currently being used topically to treat conjunctivitis and corneal ulcers, but suffers from disadvantagesof having less ocular penetration on the topical use when corneal epithelium is intact and low intra-ocular penetration whengiven orally or parenterally.Pefloxacin is newer flouroquinolone bactericidal antibiotic (1-ethyl, 6-flouro, 7-[4-methyl] –1-piperanyzyl-4-oxo-1, 4-dihydro-3-quinolen carboxylic acid), and has been proved to possess superior antibacterial activity in vivo and has betterpharmacokinetic propereties as compared to other quinolones, including norfloxacin, ciprofloxacin and ofloxacin. Althoughpefloxacin has been advocated primarily for oral and parenteral uses, it has the potential for topical ophthalmic use to treatocular infections (Gonzalez
et al
, 1989; Hobden
et al
, 1990; Sultana
et al
, 2004).The authors evaluated and compared efficacies of pefloxacin mesylate eye drops and in situ forming gels in rabbit model of experimentally induced
 pseudomonas
conjunctivitis.MATERIALS AND METHODSPermission for the use of animals for the study was obtained from Jamia Hamdard Animal Ethics Committee. Forty healthyadult albino rabbits of either sex, weighing 1 to 2 kg, having sterile cultures of conjunctival swabs taken from both eyes wereselected for the study. The rabbits were observed for one week to rule out any systemic and ocular diseases, particularlyinfections. They were divided randomly into two groups of 20 rabbits each. The research was carried out at Jamia hamdard,New Delhi, India. ( P<0.05)
 
2Suman Yadav
 
and Nayyar Parvez: Continental J. Pharmacology and Toxicology Research 2: 1 - 5 , 2008Table 1: Mean score
±
S.D. for grading of parameters of conjunctivitis viz. Redness, Lacrimal secretion, Mucoid discharge,Response to ocular therapy and Swelling of eyelid in Group I of rabbits treated with marketed eye drops, n = 20.S.No Parameter Mean score + S.D.Day 0 Day 3 Day 51. Redness4
±
0 0.947
±
0.458 0.421
±
0.512 Lacrimal secretion3
±
0 0.75
±
0.436 0.2
±
0.4023 Mucoid discharge3
±
0 0.4
±
0.656 0.15
±
0.3664 Response toocular stimulus2
±
0 0.3
±
0.477 0.15
±
0.3665 Swelling of eyelid2
±
0 0.15
±
0.307 0.05
±
0Table 2: Mean score
±
S.D. for grading of parameters of conjunctivitis viz. Redness, Lacrimal secretion, Mucoid discharge,Response to ocular therapy and Swelling of eyelid in Group II of rabbits treated with in situ forming gel, n = 20.S.No Parameter Mean score + S.D.Day 0 Day 3 Day 51. Redness4
±
0 0.157
±
0.41 0.05
±
02 Lacrimal secretion3
±
0 0.2
±
0.402 0.05
±
03 Mucoid discharge3
±
0 0.15
±
0.366 0.05
±
04 Response toocular stimulus2
±
0 0.2
±
0.41 0.05
±
05 Swelling of eyelid2
±
0 0.05
±
0 0.05
±
0Table. 3 Significance “t” test results of Group I (marketed eye drops) vs. Group II (in-situ forming gel) for improving thesymptoms of conjunctivitis in rabbit eye, viz. Redness, Lacrimal secretion, Mucoid discharge, Response to ocular therapyand Swelling of eyelid.S.No Parameter Significance t test results of Group I vs. Group II.Day 0 Day 3 Day 51. Redness P > 0.999t = 0NSP < 0. 0001t = 5.747ESP = 0.0024t = 3.253ES2 Lacrimal secretion P > 0.999t = 0NSP = 0.0002t = 4.148ESP = 0.1034t = 1.669NS3 Mucoid discharge P > 0.999t = 0NSP = 0.1449t = 1.488NSP = 0.2293t = 1.222NS4 Response toocular stimulusP > 0.999t = 0NSP = 0.4814t = 0.7710NSP = 0.2293t = 1.222NS5 Swelling of eyelid P > 0.999t = 0NSP = 0.1534t = 1.457NSP > 0.999t = 0NSES = Extremely significant ; NS = Non significant.Inoculation and Induction of conjunctivitisA sub-culture from a recently isolated strain of 
P.aeruginosa
sensitive to pefloxacin was obtained from B.V.Patel ChestInstitute, Delhi University, New Delhi, India. Bacterial conjunctivitis was induced in rabbits eye by exposing them tobacterial strains.
 
3Suman Yadav
 
and Nayyar Parvez: Continental J. Pharmacology and Toxicology Research 2: 1 - 5, 2008Grading of conjunctivitis and confirmation of diagnosisConjunctival swabs were taken from animals and sent to microbiology laboratory of our institution for confirmation of 
P.aeruginosa
as causitive microorganismParameters of conjunctivitis were graded as follows: Redness of the mucous membrane of the eye was observed visually andgrades were given from 0 to 4 i.e., 0 = absent; 1 = mild; 2 = moderate; 3= severe; 4= extensive; Lacrimal secretion: It wasgraded from 0 to 3 as 0 = normal; 1= slightly more than normal and 2 = more than normal; 3= severe; Mucoidal discharge:Whitish to yellowish white semi-solid discharge if any was noted and recorded as a grade of 0 to 3 in which 0 = absent; 1 =little; 2 = more and 3 = extensive ; Response to ocular stimulus : It was assessed by throwing torch light on the eye from aparticular distance and noticing the response to this stimulus. It was graded from 0 to 2 as 0 = normal; 1 = fast; 2 = very fast;Swelling of eye lid: It was graded from 0 to 2 as 0 = absent; 1 = slight; 2 = prominent.Grading of parameters of conjunctivitis in Group I and II of animals are shown in Tables 1 and 2.Drug formulation and therapyGroup I rabbits were treated with marketed eye drops of pefloxacin mesylate containing 0.3% w/v of drug and group II rabbitwere treated with in situ forming gel of pefloxacin mesylate containing 0.18 % of drug, 0.6 % of polymer Gelrite, 0.010 %propyl paraben, 0.05 % methyl paraben in boric acid buffer of pH 4.7.Criteria of conjunctivitis response to drug therapyDecrease in redness, mucoid discharge, lacrimal secretion, response to ocular stimulus and swelling of eyelid were taken aspositive response to therapy. Observations were made to note any ocular or systemic side effects in all the rabbits.Treatment effects were compared with those of the marketed formulations, and significance was determined using unpaired ttest. Significance levels were determined for P< 0.05, for two tailed test. The theoretical ‘t’ value is 2.306 (i.e., the table ‘t’value) at this level of degrees of freedom. Treatment was given significance (S) if “t” value exceeded the table “t” value andif it did not exceed then treatment was considered as non significant (NS). Results of the unpaired t test are shown in Table 3.RESULTSNo difference was obtained in all parameters of conjunctivitis on day 0, between in situ gelling formulation (Group I) andmarketed eye drops ( Group II), indicating that severity of conjunctivitis was similar initially between the two groups.Comparison of scores obtained with marketed eye drops and in situ gel formulation indicated that in situ gelling formulationwas faster in relieving symptoms of conjunctivitis. Results are shown in Tables 1 and 2.
Figure 1 Scores of conjunctivitis of marketed eyedrops and in situ gelling formulations on day 3 oftherapy.
00.10.20.30.40.50.60.70.80.91
RednessLacrimalsecretionMucoiddischargeResponseto ocularstimulusSwelling ofeyelid
Parameters of conjunctivitis
   S  c  o  r  e  s  o   f  c  o  n   j  u  n  c   t   i  v   i   t   i  s
marketed eyedropsin situ gellingformulations

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