Journal of Applied Pharmaceutical Science 02 (08); 2012: 118-123
The dosage form begins to disintegrate immediately aftercoming into contact with saliva, with complete disintegrationnormally occurring within 30–50 s after administration. Thesolutions containing the active ingredients are swallowed, and theactive ingredients are then absorbed through the gastrointestinalepithelium to reach the target and produce the desired effect(Dobetti
2001). Target groups for oral FDTs are wide-ranging people of all ages who can have trouble in swallowing conventional tabletsand capsules. This includes children and the elderly who eitherhave trouble and cannot swallow or have not learned to swallowthe conventional solid dosage forms. In addition, psychiatricpatients as well as hospitalized or bedridden patients sufferingfrom a variety of disorders such as stroke, thyroid disorders,Parkinson’s disease and other neurological disorders such asmultiple sclerosis and cerebral palsy (Sastry
2000) also finddifficulty in swallowing tablets and require ‘fast-melt’ tabletsbecause of their physical condition. The convenience and ease of using FDTs is also important to normal consumers, with someadults preferring these dosage forms as they are easy to handle andswallow, can be taken without water and have a rapid onset of action (Ciper
2008). For example, patientsand travellers with a limited access to water would also find suchFDTs extremely beneficial (Sastry
2005). Besides improving patient compliance, FDTs have beeninvestigated for their potential in increasing the bioavailability of poorly water soluble drug through enhancing the dissolution profileof the drug (Ahmed
1998).Fast dissolving tablets are prepared by various techniques,mainly direct compression (Bi
2009) and compression molding (Ford,1986); thus, they exhibit different disintegration behaviour. Thebasic approach used in the development of the fast
dissolvingtablets is the use of superdisintegrants. Sodium starch glycolate,and crospovidone were screened in the present study. Anotherapproach used in developing FDT is by maximizing the porestructure of the tablets. Freeze
drying and vacuum
dryingtechniques have been tried by researchers to maximize the porestructure of tablet matrix. Freeze drying is cumbersome and ityields a fragile and hygroscopic product. Usuallysuperdisintegrants are added to a drug formulation to ease thebreakup or disintegration of tablet into smaller particles that candissolve more rapidly than in absence of disintegrants (Abdelbary
2004).Amlodipine besylate is a long
acting calcium channelblocker used in the treatment of chronic stable angina, vasospasticangina and hypertension (Brunton
2005). Amlodipine is asparingly soluble orally administered drug and the rate of absorption is often controlled by the rate of dissolution. The rate of dissolution can be increased by incorporating the drug in a fastdissolving dosage form (Sinko, 2006). The simplicity and costeffectiveness of the direct compression process have positionedthis technique as an alternate to granulation technologies. In thepresent study we have developed an effective and stable FDT of Amlodipine besylate formulated by direct compression methodwith adequate hardness, low disintegration time and pleasant taste.Another purpose was to study the influence of superdisintegrantswhen used alone and in combination.
MATERIALS AND METHODSMaterials
Amlodipine Besylate (ADB) and MicrocrystallineCellulose (MCC) were procured from Yarrow Pharmaceuticals,Mumbai, India. Magnesium Stearate, Lactose was procured fromVijlac Pharmaceuticals, Hyderabad, India. Crospovidone waspurchased from DMV Fronterra excipients, Cuddalore, India. Talcand Sodium Saccharine was procured from Navdeep finechemicals, Mumbai, India. All other chemicals and reagents usedwere of laboratory or analytical grade.
Preparation of Amlodipine Fast Disintegrating tablets
Fast disintegrating tablets containing 10 mg of amlodipinebesylate were prepared by direct compression method and thevarious formula used in the studies are shown in (table 1). Soliddispersion equivalent to 10 mg of drug and colloidal siliconedioxide was mixed in a polyethylene cover. It was then mixedwith Microcrystalline Cellulose, sodium starch glycolate, lactoseand talc in another polyethylene cover. Vanilla flavour and sodiumsaccharin was added to the above material in geometrical dilutionmethod. Magnesium Stearate was added to the above mixture andmixed well for not more than three minutes. Superdisintegrantslike crospovidone and sodium starch Glycolate were used aloneand finally the effect of combination of superdisintegrants wasstudied. The prepared solid dispersion was evaluated for variousparameters like angle of repose, bulk density, compressibility indexand hausner ratio. After evaluation of the solid dispersion thetablets were compressed with single station punching machine(Cadmach TB-024) using 6 mm flat punches set.
Evaluation of Amlodipine Fast Disintegrating Tablets
Evaluation of Pre-compression parameters of powder
Prior to compression, powder were evaluated for theirflow and compressibility parameters. Flow properties of powder
Formulation of Fast Dissolving Tablets of Amlodipine Besylate.
Sl.No IngredientsWeight in mg/tabF1 F2 F3
1Amlodipine besylateSolid dispersion equivalentto 10 mg of drug30 30 302Microcrystalline Cellulose(MCC PH 101)55 55 553 Lactose 41.75 44.30 37.34 Crospovidone 7.00 ----- 7 .005 Sodiumstarch glycolate ----- 4.20 4.206 Colloidal Silicone dioxide 2.80 2.80 2.807 Vanilla flavour 1.00 1.00 1.008 Sodiumsaccharine .75 1.00 1.009 Purified Talc 1.00 1.00 1.0010 MagnesiumStearate 0.70 0.70 0.70
140 mg 140mg 140mg