FORMULATION DEVELOPMENT AND EVALUATION OF LANSOPRAZOLE DR ODT

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About Authors:
Mr. Rajat Kumar Pandeya
M. Pharm., Dept. of Pharmaceutics,
Noida Institute of Engg. & Technology
Greater Noida, India.
rajatkumar.pandeya@gmail.com

ABSTRACT :
Oral disintegrating tablets (ODTs) have received ever-increasing demand during the last decade, and the field has become a rapidly growing area in the pharmaceutical industry. Upon introduction into the mouth, these tablets dissolve or disintegrate in the mouth in the absence of additional water for easy administration of active pharmaceutical ingredients. The popularity and usefulness of the formulation resulted in development of several ODT technologies. This review describes various formulations and technologies developed to achieve fast dissolution/dispersion of tablets in the oral cavity. In particular, this review describes in detail FDT technologies based on lyophilization, molding, sublimation, and compaction, as well as approaches to enhancing the ODT properties, such as spraydrying, moisture treatment, sintering, and use of sugar-based disintegrants. In addition, taste-masking technologies, experimental measurements of disintegration times, and clinical studies are also discussed.

Reference Id: PHARMATUTOR-ART-1421

INTRODUCTION
Gastroesophageal   reflux   disease   or   GERD occurs when the lower esophageal sphincter (LES) does not close properly and stomach contents leak back, or reflux, into the esophagus. The LES is a ring of muscle at the  bottom  of  the  esophagus  that  acts  like  a  value between the esophagus and stomach. The esophagus carries food from the mouth to the stomach.

When refluxed stomach acid touches the lining of the esophagus, it causes a burning sensation in the chest or throat called heartburns. The fluid may even be tested in the back of the mouth, and this is called acid indigestion.  Occasional heartburn is  common  but  does not  necessarily  mean  one  has  GERD.  Heartburn  that occurs  more  than  twice  a  week  may  be  considered GERD, and it can eventually lead to more serious health problems.
Anyone,  including  infants,  children and pregnant women, can have GERD. Lansoprazole  is  one  of  the  classes  of  proton pump   inhibitors,   which   reduce   gastric   acidity,   an important factor in healing acid-related disorders such as gastric ulcer, duodenal ulcer and reflux oesophagitis. It is used to treat gastro-oesophageal reflux  disease,  ulcers, acid-related   dyspepsia   and   as   an   adjuvant   in   the eradication of H. pylori.2,3,4

Granules are of great interest to the pharmaceutical industry for variety of reasons. Pelletized products not only offer flexibility in dosage form design and development, but are also utilized to improve safety and efficacy  of  bioactive  agents.  The  focal  intent  of  the present cram was to develop a stable, pharmaceutically equivalent, robust and delayed release micro pellet formulation of Lansoprazole.

MATERIALS AND METHODS MATERIALS
Lansoprazole was obtained as gift sample from Active Pharmaceutical Ingredient, Sugar Granules, MCC , HPC and Mg Carbonate   from Alkem Research Centre.

METHODS
Preparation of Lansoprazole microGranules
The prototype microGranules of lansoprazole were prepared using MCC Sphere to optimize the various parameters such as inlet temperature, outlet temperature and air pressure of Fluid Bed Coater. Then formulations of delayed release microGranules of lansoprazole were done using HPC as a release retardant in different concentrations (table 1).

Drug Loading
MCC Spheres  were  sieved  through  30#40  and 33%  of Granules  was  taken for  drug loading from total batch size. Required quantity of drug was taken and dispersed in specified ml of purified water solution and stirred for 10 minutes. The required quantity of MCC Spheres was taken and dispersed in specified ml of purified water and stirred for 10 minutes to obtain a clear solution.  Purified water Solution was mixed with dispersed MCC Sphere solution with stirring. Granules were loaded using dispersion both in to FBC bowl and coated.

Barrier coating
Required  quantity  of  Drug  loaded  Granules  was taken for Barrier coating. Required quantity of HPMC was taken and dissolved in specified ml of purified water and stirred until a clear solution was obtained and coating was done (table 2).

Enteric coating
Specified quantity of Barrier coated Granules were taken for Enteric coating. Required quantity of Eudragit L30 D55, Talc, Titanium Dioxide, Iron oxide Red and citric acid (Table 2)were taken and dispersed in specified ml of purified water and stirred for 10 minutes to obtain a clear solution. The prepared dispersion was mixed with Eudragit solutions with required quantity of Water solution for pH adjustment and coating was done.

Evaluation of powder blend and Granules
The formulated powder blend were evaluated for compatibility, particle size shape analysis using Malvern particlesizer (MS 2000)5, angle repose6, hausner’s ratio, compressibility index, bulk density, true density and Granule density5, flow rate, Carr’s Index.

Compression of Tablets
The prepared blend was compressed in round shaped tablet 20mg . The weight of tablet 140-160mg , Hardness 60-80N , thickness 2.50-2.60mm and DT is 2-4 min.

In-vitro Dissolution studies
The   release   of   drug   from   the   developed formulations in the environment of gastrointestinal tract was   determined   using   the   USP   XXIII   dissolution apparatus   II   (Electro   lab   TDT   –   08L).   Tablets equivalent to 20 mg of Lansoprazole in beaker containing 900 ml of 0.1N HCl of dissolution media maintained at 37 ± 0.5°C and 100 rpm. After 1 hour the medium was drained without losing the Granules and 900 ml of pre heated buffer solution of pH 6.8 added, study was further continued for 60 minutes at 75 rpm.  Aliquot  of samples  were withdrawn at  every  15 minutes  each  time  which  was  replaced  by  the  same amount of fresh medium.
The samples were Centrifuge at 5000 rpm for 5 minutes of the above solution, and clear supernatant liquid was used. Correction factors for each aliquot were considered in calculation of release profile. Absorbance of sample after proper dilution was measured at  285  nm  using  HPLC  Dionex  (chromeleon)  against blank. Concentration of drug was determined from the standard plots of the drug in buffer and the percentage drug release was calculated at each sampling time.

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