OPTIMIZATION FORMULATION AND EVALUATION OF SUSTAINED RELEASE TABLETS OF ASPIRIN AND ATORVASTATIN

About Authors:
Kalpen N. Patel*, Maulika S. Patel, Divya Thakkar, Manan Patel, Kaushal Raval
Shree Krishna Institute of Pharmacy, Shankhalpur,
Bechraji, Mahesana, Gujarat, India.
*kalpenpharma@gmail.com

ABSTRACT
Sustained releases tablets have been used for reduced the dosing frequency and maintain the plasma drug concentration level within narrow therapeutic range. Aspirin used as antiplatelate agent and Atorvastatin is HMG-CoA reductase inhibitor which lowers the plasma concentration of cholesterol. Here in present study sustained release tablets of Aspirin and Atorvastatin prepared by using cellulose acetate phthalate (CAP) and microcrystalline cellulose (MCC) as a polymers. The sustain release tablet of Aspirin And Atorvastatin were prepared by wet granulation method and were substituted for film coating to mask the spotting from Atorvastatin and for protection from light. From the dissolution profile of F2B2 gives controlling the release up to 12 hrs with required value i.e. - 55.85 % for Aspirin and 54.78 % for Atorvastatin in 4 hrs respectively and 100.70 % for Aspirin and 100.60 % for Atorvastatin in 12 hrs respectively. The result of stability studies of batch F2B2 indicate that it is stable at 400C / 75 % ±0.5 % relative humidity as there was no significant differences observe for dissolution and average drug content data after two months.

Reference Id: PHARMATUTOR-ART-1373

INTRODUCTION
Oral drug delivery has been known for decades as the most widely utilized route of administered among all the routes that have been employed for the systemic delivery of drug via various pharmaceutical products of different dosage forms. The reasons that the oral route achieved such popularity may be in part attributed to its ease of administration and the belief that oral administration of the drug is well absorbed¹.

All the pharmaceutical products formulated for systemic delivery via the oral route of administration irrespective of the mode of delivery (immediate sustained or controlled release) and the design of dosage forms (either solid dispersion or liquid) , must be developed within the intrinsic characteristics of GI physiology, pharmacokinetics , pharmacodynamics and formulation design is essential to achieve a systemic approach to the successful development of an oral pharmaceutical dosage form.^2,3

The basic rational for controlled drug delivery is to alter the pharmacokinetic and pharmacodynamics of pharmacological active moieties by using novel drug delivery system or by modifying the molecular structure and physiological parameters inherent in the selected route of administration. It is desirable that the duration of drug action becomes more a design property of a rate controlled dosage form and less or not at all a property of the drug molecules properties, inherent kinetics. Thus optional design of controlled release systems necessitates a thorough understanding of the pharmacokinetics and pharmacodynamics of the drugs.

The goal in designing sustained or controlled delivery system is to reduce the frequency of the dosing or to increase effectiveness of the drug by localization at the site of action, reducing the dose required or providing uniform drug delivery. So sustained release dosage form is a dosage form that release one or more drugs continuously in predetermined pattern for a fixed period of time, either systematically or to a specified target organ.

MATERIALS AND METHODS:
Collection of Materials:
Aspirin was collected from Siddharth Cargo Chem. product Ltd. Mumbai, Atorvastatin was collected from Dr. Reddy’s Lab., Hyderabad, Microcrystalline cellulose and Cellulose acetate phthalate were collected from Reliance cellulose Pvt. Ltd., Polyethylene glycol 8000, Corn starch, Talcum, Acetone, Methylene chloride, Hydroxy propyl methyl cellulose, Polyethylene glycol 6000, Isopropyl alcohol were collected from Loba chemi and Titanium dioxide was collected from Berje, Chemical, Mumbai.

Preparation of Sustained Release Tablets of Atorvastatin and Aspirin ^{4, 5, 6}
Preparation Procedure for Granules of Aspirin ^{7, 8, 9}
The Aspirin avicel and cornstarch were blended and placed in Hobart mixer. And passed through 40 # sieve. Cellulose acetate phthalate dissolved in acetone. And corbowax 8000, dissolved in methylene chloride are blended until uniform viscous mixture is obtained. The cap and PEG mixture was slowly added to aspirin blend with constant stirring until uniform with granular mass was obtained. The material was discharged on to trays and dried at 1250 F. for 1-2 hrs. The dried run rate was screen through 20 # sieve the formulation of Aspirin granules are described in Table no. 1.

Table No. 1: Formulation of Granules of Aspirin According To MCC: CAP Different Ratio

Preparation Procedure for Granules of Atorvastatin^{10, 11}
The atorvastatin avicel and cornstarch were blended and placed in Hobart mixer. And passed through 40 # sieve. Cellulose acetate phthalate dissolved in acetone. And corbo waxes 8000, dissolved in methylene chloride are blended until uniform viscous mixture is obtained. The cap and PEG mixture was slowly added to atorvastatin blend with constant stirring until uniform with granular mass was obtained. The material was discharged on to trays and dried at 1250 F. For 1-2 hrs.

For Tablet preparation equivalent quantity of Atorvastatin and ENT enteric coated granules of aspirin were mixed (13% and 87% respectively) and blended with 1% talc and compressed on rotary press, the formulation of Atorvastatin granules are described in Table no. 2.

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