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Current Trends in Biotechnology and Pharmacy Vol. 7 (1) 535-543 January 2013, ISSN 0973-8916 (Print), 2230-7303 (Online) 535 Development and Evaluation of Controlled Release Verapamil Hydrochloride Pellets by PAN Coating Process S.Vidyadhara 1* , M.Bhanu Prasad 2 , R.L.C. Sasidhar 1 and T. Bala Krishna 1 1 Chebrolu Hanumaiah Institute of Pharmaceutical Sciences. Guntur. A.P. 2 Department of Biotechnology, Acharya Nagarjuna University, Guntur. A.P. *For Correspondence - svidyadhara@gmail.com Abstract The present investigation was mainly focused on the development of controlled release pellets of verapamil HCl with ethyl cellulose and hydroxylpropyl methyl cellulose phthalate (HPMCP) by employing pan coating technique. Ethyl cellulose 7cps a high viscosity grade controlled release polymer was mainly used as coating agent for regulating the drug release from pellets. HPMCP, an enteric coating polymer was used in the present study to regulate the drug release at varied G.I pH conditions. An attempt was made to optimize the composition of these two polymers to achieve the controlled release of drugs from the pellets. Low viscosity hydroxypropyl methylcellulose (HPMC E5) was used a film former in the present investigation. Croscaremellose sodium was used as disintegrant to create channels in the coating for drug release. Povidone was used as binder to achieve uniform drug layering in the present investigation. It was observed that increase in the concentration of polymers ethyl cellulose and resulted in delay in the drug release. The increase in the hydroxypropyl methylcellulose phthalate polymeric concentration in formulations showed initial delay in drug release and has no effect on further drug release. Key words: Verapamil hydrochloride, controlled release, pellets, pan coating. Introduction Multiparticulate dosage forms (MPDF) are receiving a immense attention as alternative drug delivery system for oral drug delivery even though single unit dosage forms have been widely used for decades. The most commonly used pharmaceutical solid dosage forms today include granules, pellets, tablets and capsules, out of which tablets being the most popular dosage form, accounting for 70% of all ethical pharmaceutical preparations produced. The most increasingly interesting area in the development of MPDF’S is incorporation into tablets instead of hard gelatin capsules in order to make it more economical to the consumers and gaining more attention currently. The present research work focuses on the pelletized form of multiple units, they are prepared by process called Pelletization which is referred to as a size enlargement process and the final product obtained is called pellets. Pellets provide a reduction in the dosage regimen and gastrointestinal irritation moreover controlling the drug release and increasing the absorption of the active ingredient. Also one of the advantageous properties of the pellet formulations is being good candidates for the delivery of the drug substances due to minimizing the dose dumping effect. The reproducibility of the release characteristics from pellet formulations is also much better with respect to the single-unit dosage forms. They are suitable systems for film coating with respect to the low surface area-volume ratios. Also, resistance to external factors such as moisture, air and light are the most advantageous properties of these dosage forms (1-4). In the present investigation pan coating is employed for the preparation of verapamil HCl Controlled Release Verapamil Hydrochloride Pellets
Current Trends in Biotechnology and Pharmacy Vol. 7 (1) 535-543 January 2013, ISSN 0973-8916 (Print), 2230-7303 (Online) 536 pellets. In pan coating method, a core material is coated with the drug substance following a secondary coating process in which the release controlling polymer material is introduced (5-6). The coating process for pellets is carried out primarily in order to modify the release of the drug from the pelletized drug delivery systems. The some of the Coating equipments used for the pan coating processes are standard coating pan and the perforated coating pan. Verapamil hydrochloride is a calcium channel blocker and a class IV antiarrythmic drug. It is a white crystalline powder, soluble in water; sparingly soluble in alcohol, freely soluble in methyl alcohol. A 5% solution in water has a pH of 4.5 to 6.5.Verapamil is approximately 90% absorbed from the GI tract but the bioavailability is only about 20% due to first-pass metabolism in the liver. It has terminal elimination half-life of 2 to 8 hours and prolonged after repeated oral doses. its plasma protein binding is up to 90% (7). The present investigation was mainly focused on the development of controlled release pellets of verapamil HCl with ethyl cellulose and hydroxylpropyl methyl cellulose phthalate by employing pan coating technique. Ethyl cellulose 7cps a high viscosity grade controlled release polymer was mainly used as coating agent for regulating the drug release from pellets. HPMCP, an enteric coating polymer was used in the present study to prevent burst effect of the drug from pellets during the first two hours of the dissolution. An attempt was made to optimize the composition of these two polymers to achieve the controlled release of drugs from the pellets. HPMC E5 was used a film former in the present investigation. Croscaremellose sodium was used as disintegrant to create channels in the coating for drug release. Povidone was used as binder to achieve uniform drug layering in the present investigation (8-9). Experimental Section Materials: Verapamil HCl was obtained as a gift sample from Pellet Pharma Ltd. The excipients povidone k-30 and ethyl cellulose(EC) 7cps were obtained as gift samples from pellet Pharma Ltd., HPMC E 5 was obtained as gift sample from Dow Chemicals Asia pvt., Ltd., Mumbai. hydroxylpropyl methyl cellulose phthalate (HPMCP), talc, isopropyl alcohol, propylene glycol were obtained as gift samples from Loba chemi pvt ltd., Mumbai. Preparation of verapamil HCl controlled release pellets by pan coating technique: Equal quantities of verapamil HCl and crosscarmellose sodium were taken in to bowl and mixed manually. To the mixer another equivalent quantity of verapamil HCl was added and mixed with the help of gloved hand and remaining quantity of drug was loaded in to the blender and mixed with the powder for 10 mins. Preparation of povidone solution: Isopropyl alcohol, PVP K-30 and Tween 80 were taken into stainless steel the tank and switched on the propeller type stirrer and mixed for 10mins. The solution was filtered through nylon cloth in to SS tank. Drug loading: Sugar pellets were loaded into the pan. On to the sugar pellets verapamil HCl and crosscarmallose blends prepared, earlier were loaded while spraying the povidone solution by using 1.2 mm spray gun nozzle. Pan was allowed to rotate for about 10 mins until uniform drug loading occurs. The coating pan was operated at an rpm of 15-20. The pellets bed was agitated to avoid sticking to coating pan. The pellets were kept under rotation for 30 minutes to avoid sticking. The drug loaded pellets from the pan were spread on to the trays uniformly and dried at 60°C temperature for about 3hrs. After drying the pellets were sifted by using vibro sifter to remove fines and collected the uniform sized pellets. Preparation of HPMCE 5 solution:HPMC- E 5 and water were taken into the stainless steel tank and mixed for 10mins with propeller type stirrer. The solution was filtered through nylon cloth into SS tank. Vidyadhara et al
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