FORMULATION AND EVALUATION OF PREDNISOLONE TABLET FOR COLON TARGETED D

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FORMULATION AND EVALUATION OF PREDNISOLONE TABLET FOR COLON TARGETED DRUG DELIVERY SYSTEM.:

FORMULATION AND EVALUATION OF PREDNISOLONE TABLET FOR COLON TARGETED DRUG DELIVERY SYSTEM . Chetan Singh Chauhan*, Pushpendra Singh Naruka, Rajendrapal Singh Rathore, Viralkumar Badadwal Journal of Chemical and Pharmaceutical Research J. Chem. Pharm. Res., 2010, 2(4):993-998 PRESENTED BY :- MOHIT TRIVEDI M.PHARM 2 ND SEM. MATUSHREE V.B.MANVAR COLLEGE OF PHARMACY DUMIYANI 1 GUID ED BY :- Dr. H. M. Tank Mr. Sandip Patel

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ABSTRACT INTRODUCTION MATERIALS AND METHOD EVALUATION PARAMETER RESULT AND DISCUSSION CONCLUSION AKNOWLADGEMENT REFERENCES CONTENTS:- 2

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The purpose of this study was to prepare prednisolone pH-dependent release tablets and evaluate their advantages as a colon targeted drug delivery system. prednisolone insoluble in water and unstable in gastric environment was formulated into pH-dependent tablets coated with combinations of two methacrylic acid copolymers Eudragit L100 and Eudragit S100. The influence of core tablet compositions, polymer combination ratios and coating levels on the in vitro release rate of prednisolone from coated tablets was investigated . ABSTRACT:- 3

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The results showed that less than 10% drug was released in 0.1 N HCl within 2 hr, and about 90% of the drug was released in the pH 7.2 phosphate buffer within 6 hr. Colon drug delivery is advantageous in the treatment of colonic disease and oral delivery of drugs unstable or susceptible to enzymatic degradation in upper GI tract . In this study coated tablets that is resistant to gastric and small intestinal pH conditions but can be easily dissolved in colonic pH. CONT… 4

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The results of the present study have demonstrated that the pH-dependent tablet system is a promising vehicle for preventing rapid hydrolysis in gastric environment and improving oral bioavailability of prednisolone for the treatment of ulcerative colitis . KEYWORDS :- Prednisolone, colon targeted drug delivery, enteric coating, In vitro dissolution, pH Dependent delivery system. CONT… 5

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Colon targeted delivery systems have been the focus point of formulation laboratories because the colon is considered as a suitable site for delivery of both conventional and labile molecules, and it is also a site for some specific diseases, such as, ulcerative colitis, Crohn’s disease, bowel cancer, some infections, and constipation, which require local delivery of the drug. Various approaches have been used for oral delivery of drug to the colon which includes time-dependent delivery, pH-dependent systems and bacteria-dependent delivery. 6 INTRODUCTION:-

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Oral ingestion has long been the most convenient and commonly employed route of drug delivery. pH-dependent systems are vary useful for colon-targeted delivery of drug, there has always been controversy about their usefulness for the intended purpose mainly because of, a) High GI pH variability among individuals. b) Lack of proper coating material that would dissolve at the desired pH of the colon, thus bypassing the effect of the stomach and the small intestine on the dosage form. CONT … 7

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Methacrylic acid copolymers such as Eudragit L100, and Eudragit S100 have commonly been used as pH-dependent polymers for coating solid dosage forms (because of their solubility at pH 6.0 or higher, and 7.0 or higher , respectively),none of them is suitable for use alone for coating of dosage forms that would start releasing the drug specifically at pH 6.5, which is generally considered as the suitable pH for colon-targeted delivery. CONT … 8

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Prednisolone is an anti inflammatory drug, for oral administration in the treatment of diseases of colon (ulcerative colitis, Crohn’s disease, carcinomas and infections). The absolute oral bioavailability is 75-98 %. It has a half life of 2 - 4 hr. CONT … 9

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Prednisolone IP, Micro crystalline cellulose CCS, SSG Aerosil, Isopropyl alcohol, Talc, Magnesium stearate , Eudragit L100, Eudragit S 100, DEP, TIO2 . Lincoln Pharmaceutical Ltd MATERIALS:- 10

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FORMULATION:- 11

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PREPARATION OF CORE TABLET DRUG + EXICIPIENT PASS THROUGH SEIVE NO # 40 COLLECT IT & MIX IN POLYTHENE BAG 12 METHOD:-

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13 Add lubricated granules Compressed into tablet by single rotary machine

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It was done by using the standard coating pan, where fixed numbers of tablets were coated each time by atomizing the polymeric coating solution through the means of spray gun. The scale-up variables including pan loading, pan speed, number of spray guns, spray rate, and inlet airflow etc. were considered. About 500 tablets of prednisolone tablet were taken and allow to coatings in pan coater at 30 rpm & temp. Coating was carried out with spraying method and dried with same. COATING OF THE TABLETS:- 14

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Table–3 Evaluation of uncoated tablet EVALUATION OF TABLETS:- 15

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The in-vitro dissolution studies were carried out using USP dissolution apparatus type II in different medium. Acid stage: Two hours in 900 ML 0.1N HCL at 75 rpm. Buffer stage: Three hour in 900 ML pH 4.5 phosphate buffers at 75 rpm, 1 hour in 900 ML pH 7.2 simulated colonic fluid at 75 rpm. Dissolution test was carried out for a total period of 6 hours. Analysis for prednisolone was done by UV detected at 247 nm IN-VITRO DRUG RELEASE STUDIES:- 16

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Table 4: Cumulative percentage drug release of prednisolone PH dependent Tablets 17

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The expected in vitro release pattern selected for the colon targeting was not more than 10% of drug release up to the end of 5hrs.Eudragit L-100 and Eudragit S-100 were used in different concentration; 5%, 7% and 10% coating level. The batch SF1 and SF2 with 5% coating showed a release of more than 10% in less than five hours i.e. 19.1 % & 16.2 % respectively, which is not acceptable. Hence these formulations were excluded from further studies. However the SF7 and SF8 formulation showed a release of less than 10% in the first five hour of dissolution study. The drug release was directly related to the concentration of polymer in solution and the % coating level. Percent of drug release vs. time plot shows that the dissolution rate was inversely proportional to the coating level applied. A significant difference was observed in the percentage of drug released for different coating level. All the coated tablets with variable coating levelshowed a nearly complete drug release in the 6 hr. RESULTS AND DISCUSSION:- 18

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In the formulation SF3 ,SF4 and SF5 where 7% polymer coating was applied in the ratio 3:2,1:1,2:3. The % drug release after 5hr was 18.96 %, 11.56 %, 12.1 % respectively. For formulation SF6, SF7 and SF8 where, 10% coating in the ratio 3:2, 1:1, 2:3; was applied. The drug release at 5th hr and 6th hour 10.4% 95.4% respectively in the formulation SF5 observed. In the SF7 & SF8 polymer was able to control the drug release after 5th hr the drug release was well within the desired limits of less than 10% i.e. 6.7% and 5.6%. The drug released from these formulations at the end of dissolution run was 98.2% & 99.1%. It was observed that the drug release was controlled by increase the coating level. Based on the above studies, the optimum formulation, formulation SF8 coated with Eudragit L100–Eudragi S100 at a combination ratio of 2:3 and at the coating level of 10%, was chosen for studying the effect of pH of the buffer media on the release profiles, as shown in Figure. As anticipated, the release Cont… 19

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Figure - Comparative in vitro release profiles for coated prednisolone tablets 20

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The present study was carried out to investigate the ability of methacrylate co-polymers for targeting the drug release in colon. From results obtained in the present study, it was concluded that the resulted optimum formulation was the one coated with 10% coating level of Eudragit L100 and Eudragit S100. The in vitro studies showed that this formulation successfully deliver the maximum amount of drug in intact form to the colon. The combined action of the superdisintegrant; cross carmellose sodium and sodium starch glycollate have been contributed to such a fast disintegration property. It prevents the drug release in the stomach and intestine so we can solve the problem of side effect of anti inflammatory drug in this area & also prevents ulcerative colitis. 21 CONCLUSION:-

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[9]Banker, G.S., Anderson, N.R., Tablets. In: Lachman L, Lieberman, HA, Kanig, JL, eds, The Theory and Practice of Industrial Pharmacy. Philadelphia, PA: Lea & Febiger; 1986, 3rd Ed: 293- 345. [10] Yano H., Hirayama F., Kamada H. Journal of Controlled Release, 2002, 103-112. [11] Lorenzo, M.L, Remunan, C., VilaJato, J.L., Alonson, M.J., J. Control Release., 1998, 52,109–118. [12] Rubinstein, A., Radai, R., Ezra, M., Pathak, S., Rokem J.S. Pharm. Res., 1993, 258–263. [13] Khan, M., Prebeg Z., Kurjakovic, N., Journal of Controlled Release., 1999, 58,215-222. [14] Krishnaiah, Y., Satyanaryana, S., Rama Prasad, Y.V., Drug Dev. Ind. Pharm., 1999, 25,651- 657. [15] Oosegi, T., Onishi, H., Machida, Y., International Journal of Pharmaceutics., 2008, 80-88. 23

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