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FORMULATION AND EVALUATION OF ENTERIC COATED TABLETS OF PROTON PUMP INHIBITER:

FORMULATION AND EVALUATION OF ENTERIC COATED TABLETS OF PROTON PUMP INHIBITER By N.RAJU BALAJI INSTITUTE OF PHARMACEUTICAL SCIENCES NARSAMPET,WARNAGAL

CONTENTS:

CONTENTS INTRODUCTION MATERIALS & METHODS EVALUATION OF TABLETS CONCLUSION

INTRODUCTION:

INTRODUCTION Oral site specific drug delivery systems have attracted a great deal of interest recently for the local treatment of a variety of bowel diseases and also for improving systemic absorption of drugs , which are unstable in stomach . Delivery of therapeutic agent into the intestinal region could be accomplished by the application of an enteric coating on a solid dosage form. Several approaches have been attempted and reported during the last decade to develop new methodologies for site specific drug release , including PH sensitive drug release , and time controlled release .

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Among these , the time controlled release systems such as sustained or delayed dosage are very promising. Nevertheless, due to the potentially large variation of gastric emptying time of dosage form in humans. Esomeprazole magnesium trihydrate , is a classical example of proton pump inhibitors and is approved by FDA for the treatment of symptometic gastrointestinal reflux disease , short time treatment and maintaince of erosive esophagitis . A number of eneric coating polymers are available and capable of protecting the drug core from the aggressive environments of the stomach. Being soluble at higher pH values , these polymers dissolve in the intestine and release, the polymers dissolve in the intestine and release the core for ready action

MATERIALS AND METHODS :

MATERIALS AND METHODS MATERIALS Esomeprazole magnesium trihydrate , Eudragit L -30 D-55 Hydroxy propyl methyl cellulose phthalate Cellulose acetate phthalate Acryl –EZE Opadry( colorcon , goa,india)

DRUG EXCIPIENT INTERACTION STUDY:

DRUG EXCIPIENT INTERACTION STUDY Acvtive drug blended with individual excipients were taken in 1;1ratio,filled in closed vials and placed in stability chambers at 35 c / 60 % RH for a period of 4 weeks . Samples are analyzed by IR

PREPARATION OF CORE TABLETS:

PREPARATION OF CORE TABLETS Dummy granules for tablets were prepared by wet granulation method. The respective ingredients were passed through a sieve no.60 (250 micro meters) and blended with a turbula mixer. Activation of pvp k-30 was done using isopropyl alcohol and the prepared granules were dried . The dried granules were mixed with drug and compressed on a 10 station tablet machine using 7 mm biconvex round shaped die and punches.

PREPARATION OF ENTERIC COATED TABLETS:

PREPARATION OF ENTERIC COATED TABLETS Seal coat of opadry was applied to the tablets up to a weigh gain of 3%. Then the seal coated tablets were enteric coated with different enteric coating material such as eudragit L-30 D-55, Hydroxy propyl methyl cellulose phthalate Cellulose acetate phthalate, Acryl-EZE

EVOLUATION OF GRANULES:

EVOLUATION OF GRANULES Bulk density Tapped density Carr’s index Angle of repose

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The bulk density and tapped density were calculated as the ratio of the granules mass and the respective volumes . Carr`s index was calculated using the equation ; I= Dt -Db/ Dt *100 Where Dt = the tapped density of the powder Db = the bulk density of the powder The angle of repose was calculated using the equation H=height of the pile R=radius of the base of the conical pile

EVALUTATION OF TABLETS:

EVALUTATION OF TABLETS Hardness Friability test Uniformity of weight Disintegration time Drug content studies In vitro dissolution tests Stability studies

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Hardness-The tablet crushing strength was tested by commonly used Monsanto type tablet hardness tester . Friability test -Tablet strength was tested by Roche friabilitor . Uniformity of weight – Disintegration time - Disintegration time was determined using the disintegration apparatus USP in 0.1 HCL for 2 hours and then in phosphate buffer ph 6.8 maintaining the temperature at 37 +- 2 c

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Drug content studies – The amount of drug was determined by injecting 20 microliters of in a HPLC system consisting of a phenomenax C18 analytical column . The compounds were eluted at a flow rate of 1.0ml/min using a mobile phase of acetonitrile ; phosphate buffer ph 6.8 (60;40 v/v) .The column effluent was moniterd at 203 nm. In-vitro dissolution tests apparatus – USP XII type II media – 0.1 N HCl and 6.8 pH buffer tem – 37 +/- o.5 0 c speed – 100 rpm The samples were analyzed by HPLC

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Stability tests -The stability studies were carried out at 25 c +- 2 c /60 % RH , 35 c +- 2 c /60% +-5 % RH and 40 c +_2 c /75 % +- 5 % RH for selected formulation for three methods. Stastical evaluation - The data were statiscally analyzed by one way analysis of variance (ANOVA) and students t –test .

Results and discussions:

Results and discussions The observed IR spectra did not show any alteration in IR peaks , suggesting no possible interaction between excipients and Esomeprazole . Considering the dissolution in general and stability in particular , the pH of the core tablet was basified using sodium bicorbonate (50 mg). Five different core tablets (f1-f5)of esomeprazole were prepared with varying concentration of diluents (dibasic calcium phosphate and mannitol ) Based on the disintegration test f1 formulation was selected for further enteric coating as this had shown minimum disintegration time .

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The granules used for preparing the f1 formulation s exhibited ideal preparations for tablet compression Bulk density (0.47+- 0.05%g/cc) Tapped density(0.58+-0.03 g/cc) Angle of repose(29.65 +-1.25) Carr`s index (18.96+0.89) Moreover physical properties of compressed tablets exhibited good physical integrity Friability *(0.27+-0.06) Weight variation(181.25 +- 5.83)

CONCLUSION:

CONCLUSION Esomeprazole core tablets were prepared and stabilized using sodium bi corbonate as a stabilizer . Enteric coat was done using using four different enteric coating materials to achieve 5%weight gain . Evolution of these tablets indicates that the tablets coated with HPMCP and CAP failed the disintegration test in 0.1 n HCL . The study that indicates that out of the four polymers studied , methacrylic acid polymers are most suitable for enteric coating . These provide greater protection to the core under acidic condition while at the same time show the fastest drug release under intestinal pH. The above formulations were found to be stable for three months.

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