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INTRODUCTION: GIT tract and drug which could be used for colonic
Now a day, various routes of administration have diseases is the best candidate for colon targeting.
been explored for the effective delivery of the drug. Ornidazole fulfills these criteria [9,10].
The oral route is considered to be most convenient
for the administration of drugs to patients. On oral MATERIALS AND METHOD:
administration of conventional dosage forms drug Ornidazole , HPMC K4 M,Eudragit S100, Xanthan
normally dissolves in the gastro-intestinal fluids and gum, PVP K-30,Mg.stearate,Talc and MCC were
is absorbed from these regions of the gastro-intestinal purchased from Research Lab Fine Chem. Ltd.
tract, which depends upon the physicochemical Mumbai .
properties of the drug [1-3]. It has a serious drawback
in conditions where localized delivery of the drug in DRUG POLYMER COMPATIBILITY STUDIES
the colon is required or in conditions where a drug 1. Drug polymer compatibility studies were carried
needs to be protected from the hostile environment of out using FTIR.
upper GIT. Dosage forms that deliver drugs in the 2. The study was carried out on individual pure drug
colon rather than upper GIT has number of and its physical mixture with the selected polymers
advantages. Oral delivery of drugs in the colon is under study.
valuable in the treatment of various diseases of colon
like colon cancer, ulcerative colitis, Crohn's disease PREPARATION OF COLON TARGETED
and inflammatory bowel disease [4-6], IBS where by ORNIDAZOLE TABLETS
high local concentration can be achieved while Ornidazole, Hpmc K4 M, Xanthan gum, PVP K-30
minimizing side effects. Colon targeted drug delivery and microcrystalline cellulose, were taken in required
is used to deliver the substances that are degraded by quantities mixed and passed through #60 sieves,
the digestive enzymes in the stomach such as proteins lubricated with magnesium stearate and talc then was
and peptides. During the past decades research is compressed into tablets by compressed on tableting
going on in developing the methods to target the drug machine (Rimek Mini Press-II, Karnavati
to the specific region [7,8]. Engineering Ltd.) by using 9 mm punch. The tablets
were further coated with Eudragit S 100 solution of
Ornidazole is insoluble in acidic media and it is coating solution. A coating solution of Eudragit S
poorly absorbed from upper GIT tract. But it is 100 was prepared in a mixture of Isopropyl alcohol,
soluble in alkaline media and it is almost completely acetone (1:1). The coating of matrix tablet was
absorbed from colon. More ever Ornidazole causes prepared by immersion in the coating solution
gastric Irritation in stomach when administered followed by deep coating technique.
orally. Drug which is poorly absorbed from upper
From FTIR study it can concluded that the drug Ornidazole have maintained its identity without losing its
characteristic properties in formulation blend.
Table 2: showing physicochemical properties of colon targeted tablets batches FB1to FB9
Drug
Hardness Weight variation
2 Thickness (mm) % Friability Content
Batch (kg/cm (mg)
(%)
FB1 4.6 3.46 ±0.05 353.2 ±2.19 0.46 ±0.15 98.15
FB2 4.5 3.5 ±0.1 355.5 ±2.64 0.35 ±0.18 98.75
FB3 4.6 3.4 ±0.15 354.3 ±2.45 0.43 ±0.05 97.56
FB4 4.5 3.5 ±0.1 352.5 ±2.25 0.6 ±0.1 96.45
FB5 4.3 3.5 ±0.2 353.9 ±2.58 0.5 ±0.1 98.50
FB6 4.4 3.4 ±0.4 352.7 ±1.65 0.6 ±0.1 98.73
FB7 4.5 3.5 ±0.2 354.8 ±2.04 0.36 ±0.11 97.30
FB8 4.7 3.4 ±0.05 354.15 ±1.78 0.48 ±0.10 96.94
FB9 4.5 3.5 ±0.36 353.2 ±1.75 0.59 ±0.07 98.49
All the tablet formulations were subjected for drug release study. All tablets have shown smooth
evaluation according to various official specifications appearance.
and other parameters. Shape, thickness, hardness, Formulated colon targeted tablet has showed smooth
friability, weight variation, thickness and, in vitro flat surface and was white in colour colon targeted
tablet was found to be 3.4-3.5 mm. weight variation limit (95 to 105 %) indicates that all batches passed
was found within the pharmacopoeia limits of ±10%. the % Drug Content test. Results for all above tests
Hardness colon targeted tablet was found to be 4.3 to were tabulated in table no.2.
4.7 kg/cm2 . Friability value of colon targeted tablet
was found to be 0.35 to 0.60% indicates that core b) In Vitro Dissolution Study
tablet possess good mechanical strength. Result for % In vitro Drug Release Study of colon targeted batches
Drug Content for all batches was found to be from FB1to FB9
96.56 to 98.75 % which was within the approved
Design-Expert® Software
Factor Coding: Actual Time for25% drug release (hrs)
Time for25% drug release (hrs) 100
Design Points
6
6
4
X1 = A: HPMC K 4 M 90
X2 = B: Xanthan gum
B: Xanthan gum (mg)
80
4.5 55 5.5
70
60
40 45 50 55 60
A: HPMC K 4 M (mg)
Fig.7: A counter plot showing relationship between various levels of independent variables to gain fixed value
of 25% drug release.
Design-Expert® Software
Factor Coding: Actual
Time for25% drug release (hrs)
Design points above predicted value
Design points below predicted value
6
4
6.5
5.5
4.5
3.5
100 60
90 55
80 50
70 45
B: Xanthan gum (mg) A: HPMC K 4 M (mg)
60 40
Fig.8: A response surface plot showing effect of concentration of independent variables on the 25% drug
release.
Design-Expert® Software
Factor Coding: Actual Drug release (%)
Drug release (%) 100
Design Points
94.17
71.15
X1 = A: HPMC K 4 M 90
X2 = B: Xanthan gum
B: Xanthan gum (mg)
80
85
5
80
90
70
60
40 45 50 55 60
A: HPMC K 4 M (mg)
Fig.9: A counter plot of showing relationship between various levels of independent variables to gain fixed
value of Drug Release (%).
Design-Expert® Software
Factor Coding: Actual
Drug release (%)
Design points above predicted value
Design points below predicted value
94.17
71.15
95
X1 = A: HPMC K 4 M
X2 = B: Xanthan gum
90
80
75
70
100 60
90 55
80 50
70 45
B: Xanthan gum (mg) A: HPMC K 4 M (mg)
60 40
Fig.10: A response surface plot showing effect of concentration of independent variables on Drug Release
(%).
Model
Response Sum of Degree of Mean F R
P value significant/non-
model square freedom square value square
significant
Drug Release <
363.99 12 168.03 47.14 0.9041 Significant
(%) 0.0001
Time for 25%
Drug release 6.00 12 2.54 20.71 0.0003 0.8056 Significant
(hrs)
CONCLUSION:
From the IR study and physical observation it could ACKNOWLEDGEMENT:
be concluded that there was no significant Drug- The authors are thankful to Hazrat
Excipients interaction. So Formulations were MaulanaG.M.Vastanvi Sahab, President, Akbar Patel
subjected to Evaluation of all physicochemical Sir Coordinator of JamiaIslamia Ishaatul Uloom’s Ali
parameters. Developed film coated colon targeted Allana College of Pharmacy Akkalkuwa,Dist-
tablets possessed the required physicochemical Nandurbar for providing the work facilities.
parameters such as hardness, friability, weight
variation, drug content. Optimization study indicates REFERENCES:
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