Formulation and Development of Colon Targeted Drug Delivery of Aceclof

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Formulation and Development of Colon Targeted Drug Delivery of Aceclofenac By ARA PATEL - M. Pharm sem ΙΙ I rd Under the guidance of - Dr. Kamal Singh Rathore & Mr.Gopal Brahmbhatt B.N.Girls’ College of Pharmacy, Udaipur 1

Anatomy of Colon: 

Anatomy of Colon » Ascending Colon » Transverse colon » Descending Colon » Sigmoid Colon Mucosa Submucosa Muscularis externa Serosa 2

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Colon as a Site for Drug Delivery • Colon was considered as BLACK-BOX as most of the drugs are absorbed from upper part of the GI tract. • Promising site for drug delivery » Local disorders » Systemic absorption » Drugs unstable in upper GIT » Drugs poorly absorbed from GIT » Drugs that necessitate targeting at site

Circadian rhythm regulates many body functions in human, viz., metabolism, physiology, behavior, sleep patterns, hormone production, etc.: 

Circadian rhythm regulates many body functions in human, viz., metabolism, physiology, behavior, sleep patterns, hormone production, etc. Diseases displaying circadian rhythm Colon targeted drug delivery systems have a particular mechanism of delivering the drug rapidly and completely after a "lag time," i.e., a period of "no drug release”. It is designed in a manner that the drug is available at the site of action in the right amount 4

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Rational for the Development of Colon Targeted Drug Delivery » Treatment of local pathologies » Chronotherapy (asthma, hypertension, cardiac arrhythmias, arthritis or inflammation ) » Greater responsiveness to the absorption enhancers. » Less enzymatic activity » Site for delivery of delicate drugs (Proteins and Peptides) 5

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Formulation is well protected in stomach. It has minimum side effect. Avoid unnecessary systemic absorption. Could be used to prolong drug delivery. Enhance the absorption of poorly absorbed drug. Improved bioavailability of poorly absorb drug. Reduced dose size & dosage frequency. Improved patient compliance. Advantages 6

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Pharmaceutical Approaches for Targeting Drugs to Colon » pH sensitive system » Time controlled release system » Microbially triggered systems Prodrug approch Polysaccharide based systems Azopolimeric linkage » Osmotically controlled drug delivery systems » Pressure dependent release systems 7

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pH sensitive system pH sensitive polymer + drug core DRUG CORE Colonic pH Release of drug in Colon 8

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Objectives To design and characterize an oral, Colon Targeted drug delivery system of Aceclofenac. It is a chronopharmaceutical approach for the better treatment of rheumatoid arthritis. After that it releases the drug in a controlled manner. Based on this concept that the formulation is designed in such a manner that on leaving the stomach & intestine it reaches at colon and coating layer start to dissolve. 9

METHODOLOGY: 

ACECLOFENAC METHODOLOGY 10

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SL. No. Name of the chemical used Quantity used in mg F1 F2 F3 F4 F5 F6 F7 F8 F9 F10 1 Aceclofenac 201.65 201.65 201.65 201.65 201.65 201.65 201.65 201.65 201.65 201.65 2 Lactose - - 30 15 9.35 46.35 54.35 - - - 3 Microcrystalline Cellulose 64.35 49.65 22 17 - - - 50 49.65 46.65 4 Starch 35 35 35.55 42.55 31.2 31.2 31.2 33.85 35 35 5 Sodium Starch Glycolate ( intra- granular) - - - 2 - - - - 4 4 6 PVPK-30 15 18 15 15 12 12 12 15 15 15 7 Cross Carmellose Sodium - - - 10 10 10 5 6 - 3 8 Cross Povidone - - - - - 3 - - - - 9 Sodium Starch Glycolate 16 16 16 17 16 16 16 16 15 15 10 Aerosil 4 4 4 4 4 4 4 3 4 4 11 Magnesium Stearate 4 4 4 4 4 4 4 3 4 4 12 Talc 1.7 1.7 1.8 1.8 1.8 1.8 1.8 1.5 1.7 1.7 Preparation of Core Tablets 12

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Weighing & Shifting Manual/Machine Machine Drug & Excipients Weighing Balance & vibro shifter Dry Mixing Manual/Machine Machine Time 5 Min Granulation Manual/Machine Machine Wet Granulation High Shear Mixing Granulator Drying Manual/Machine Machine, Granules Fluidized Bed Dryer Total Time 25 Min Sizing Manual/Machine Machine, Vibro shifter Sieve size 20 # Final blending and Lubrication Machine/Manual Manual Time 10 min Different Steps for Formulation 13

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Tablets was compressed by rotary compression tablet punching machine using 10mm Std concave punch. . Compression Tooling B Tooling , 10mm Standard Concave Punch Average weight(mg) 330 ± 5% Thickness(mm) 4.2±0.2 Hardness (kg/cm 2 ) NLT 5kg/cm 2 Friability(%) NMT 1% 14

Evaluation of Tablet Properties: 

Evaluation of Tablet Properties 15

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Results and Discussion 16

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Standard calibration curve for Aceclofenac in Methanol- water 17

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Standard calibration curve for Aceclofenac in pH 7.5 Phosphate buffer Standard calibration curve for Aceclofenac in pH 6.8 Phosphate buffer 18

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Formulation No. Bulk Density Tapped Density Carr’s Index Hausner’s Ratio Total Porosity Angle of Repose F1 0.449 0.507 11.54 1.130 11.53 26.66 F2 0.440 0.507 13.21 1.152 13.20 27.29 F3 0.458 0.530 13.73 1.159 13.72 26.34 F4 0.440 0.496 11.32 1.128 11.32 27.61 F5 0.449 0.496 9.62 1.106 9.61 26.15 F6 0.440 0.496 11.32 1.128 11.32 28.05 F7 0.458 0.519 11.76 1.133 11.76 25.45 F8 0.432 0.486 11.11 1.125 12.73 27.79 F9 0.449 0.507 11.54 1.130 11.53 24.80 F10 0.458 0.507 9.80 1.109 9.80 25.26 EVALUATION OF GRANULES 19

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Formulation Code F1 F2 F3 F4 F5 F6 F7 F8 F9 F10 Tablet hardness 6.29 6.40 6.28 6.42 6.53 6.47 6.20 6.32 6.31 6.44 Friability 0.243 0.304 0.272 0.273 0.303 0.273 0.091 0.303 0.303 0.121 Content Uniformity 99.77 98.11 99.10 100.1 98.77 100.1 101.0 99.44 100.1 99.77 Disintegration time 5:20 6:08 10:46 9:00 9:26 7:25 6:26 2:16 5:06 4:12 EVALUATION OF COMPRESSED TABLETS OF ACECLOFENAC 20

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Dissolution profile for Formulation F1 to F10 21

Conclusion : 

Conclusion 22

SUMMARY: 

SUMMARY Compressed tablets was evaluated for different parameters, and all the results was fall with in the limit. In the present study Colon targeted drug delivery system was designed which intentionally release drug in the Colon region. 23

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Coating of tablets HPMC Ethyl Cellulose Dibutyl Phthalate Ethyl alcohol Dichloro methane Composition of Coating Solution Inlet temperature 45-50ºC Bed temperature 45ºC Humidity below 25% RH Solution spray rate 8-15 RPM Air pressure 1.2-1.5 coating parameter 24

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Thank You 25