Formulation And Evaluation Of Almotriptan Chewable Tablets

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Anil kumar V et al / Int. J. of Pharmacy and Analytical Research Vol-5(3) 2016 [388-399]ISSN:2320-2831IJPAR Vol.5 Issue 3 July- Sep -2016Journal Home page: www.ijpar.comResearch articleOpen AccessFormulation and evaluation of almotriptan chewable tablets1V. Anil kumar*, K.L. Deepthi*, 1R. Kalyani, 1B. Padmasri, 2D.Prasanth1Department of Pharmaceutical Technology, Sri Venkateswara College of Pharmacy, Etcherla,Srikakulam. India.2Department of Pharmacology, Sri Venkateswara College of Pharmacy, Etcherla, Srikakulam, India.*Corresponding Author: V. Anil kumarEmail: anilvadaga@gmail.comABSTRACTIn the present work, Almotriptan chewable tablets were prepared. All the tablets were subjected to weight variation,drug content uniformity, lock length, dissolution, drug excipients interaction and short-term stability studies. Therewas no difference in the position of the absorption bands, hence providing evidence for the absence of any chemicalincompatibility between pure drugs with the excipients. The bulk density and tapped density for all formulation (F1 –F9) varied from 0.423 - 0.485 gm/cm3 and 0.501 - 0.593 gm/cm3 respectively. The results of carr’s consolidate indexor % compressibility index and hausner’s ratio for the entire formulation (F1 – F9) blend range from 15.5- 19.1 and1.10-1.28 respectively, shows fair flow properties. All the tablets show similar color, odour, taste and physicalappearance. There is no impact of different in their organoleptic properties. By using the different excipient, thehardness values ranged from 3.0-3.5 kg/cm2 for formulations (F1-F9) .The entire tablet passes weight variation test,as the average % weight variation was within the Pharmacopeial limit - 7.5%. It was found to be 149mg - 152 mg.The weight of all the tablets was found to be uniform with less deviation. The concentration of the drug in all theformulations with different polymers was found to be 97.35 – 99.58%. It was within the IP limits.Keywords: Almotriptan, Direct compression.INTRODUCTIONChewable release tablets [5, 6]The need for new oral drug delivery systemcontinues, due to poor patient acceptance forinvasive methods, need for exploration of newmarket for drugs and coupled with high cost ofdisease management. Developing new drugdelivery techniques and utilizing them in productdevelopment is critical for pharmaceuticalcompanies to survive this century [5].The oral route of drug administration is themost important method of administering drugs ns intended for oral administration. Someare intended to be swallowed whole, some afterbeing chewed and some after being crushed, someare intended to be dissolved or dispersed in waterwww.ijpar.com 388

Anil kumar V et al / Int. J. of Pharmacy and Analytical Research Vol-5(3) 2016 [388-399]before being taken and some are intended to beretained in the mouth where the active ingredient(s)is/are liberated. Administration of drugs throughoral route is the most common and the easiest wayto administer a drug. But it is a challenge inchildren who have not yet learned to swallowtablets. Hence chewable tablets are formulated toimprove the compliance in children [1].Chewable tablets are the tablets which arerequired to be broken and chewed in between theteeth before ingestion.Chewable tablets areusually uncoated .These are intended to be chewedin the mouth prior to swallowing and are notintended to be swallowed intact. Chewable tabletsare designed for use by the children and suchpersons who may have difficulty in swallowing thetablets [2].Additionally, chewable tablets facilitate morerapid release and hence more rapid absorption ofactive ingredients and provide quick onset of action[4]. A non-dissolving polymer matrix modifiedrelease dosage form containing the drug and otherexcipients that must be chewed but not swallowedto promote release of the drug from the dosageform in the oral cavity.In the manufacture of chewable tablets,measures are taken to: ensure that the tablets areeasily crushed by chewing; ensure that the tabletsare palatable [3].Chewable tablets disintegrate slowly when chewed orallowed to dissolve in the mouth for local action.Chewable tablets are especially useful in the tabletformulations for children and are commonlyemployed in the preparation of multiple vitamintablets .Wherever feasible and practical, the first stepin the formulation of a chewable tablet is to obtain acomplete profile of the active drug. This usually leadsto the most efficient formulation of a stable andquality product as the drug usually dictates the choiceof fillers, carriers, sweeteners, flavor compounds, andother product modifiers. Many of the excipientscommonly used in tablet formulation are especiallyapplicable for use in chewable tablets due to theirability to provide the necessary properties ofsweetness and chew ability. In general, these fall intothe sugar category [6], although a combination ofbland excipients with artificial sweeteners mayprovide a satisfactory alternative .Important aspects ofchewable tablet manufacture are the properincorporation of the coloring agent, assurance ofnecessary particle size distribution) maintenance ofcorrect moisture content, and achievement of propertablet hardness. All of these are the routineresponsibility of the manufacturing department oncethe parameters have been established duringdevelopment [7]. Two common approaches are theuse of low concentrations of light colors and the useof high-intensity mixing of reduced particle sizematerials in order to assure thorough blending.Mannitol is widely used as excipients in chewabletablets for its non-hygroscopic nature of moisturesensitive drugs [8]. Chewable tablet formulation,particularly those containing pharmaceutically activeagents, present issue of the organolepticcharacteristics of odor, taste, appearance and mouthfeel. The formula ingredients and manufacturingprocess both play a role in obtaining the desiredorganoleptic properties [9].AIM AND OBJECTIVEAim To formulate and evaluate tablets Almotriptanchewable tablets using different excipients andselecting best of them.Objective To design the formula for chewable Release tablet.To carry out compatibility studies of drug anddisintegrantsTo incorporate selected model drug candidates inthe formula and prepare tablets.To evaluate the formulated tablets.By physical parameters andBy in-vitro dissolution profile of prepared tablets.METHODOLOGYFormulation of different batchesThe main aim of the present study was toformulate different batches using three varioussuperdisintegrants and other ingredients in varyingconcentrations [10]. So, different batches offormulations were planned accordingly. Accordingto that F1, F2, F3 (with Crospovidone-3%, 5%,7.5%), F4, F5, F6 (with Crosscaramellose-3%, 5%,7.5%), F7, F8, F9 (with Sodium starch glycollate3%, 5%, 7.5%).Table: 1 Formulation of Different Batches (F1-F9)www.ijpar.com 389

Anil kumar V et al / Int. J. of Pharmacy and Analytical Research Vol-5(3) 2016 [388-399]Formulations CodeIngredients ------------Croscarmellose sod. ------ -----SSG------ 5 agnesium stearate 2.251.5AerosilTotal tablet weight 150mgRESULTS AND DISCUSSIONSResultsPreformulation StudyOrganoleptic Properties (Color, odor, taste and appearance)Table2. Results of identification tests of drugCharacteristicsColourOdourTasteResultsWhite amorphous powderCharacteristic odourSlightly bitterMelting point determination: Drug: AlmotriptanTable 3: Results of Melting point determination test of drugReported Melting Point170 - 174Observed Melting Point173Determination of solubilitySoluble in methanol water sparingly soluble in ethanol, propylene glycol, and very slightly soluble inchloroform.www.ijpar.com 390

Anil kumar V et al / Int. J. of Pharmacy and Analytical Research Vol-5(3) 2016 [388-399]DRUG AND EXCIPIENTNCOMPATABILITY STUDIESFig no: 1 FTIR spectrum of Almotriptan pure drugFig no: 2 FTIR spectrum of Almotriptan optimized formulationwww.ijpar.com 391

Anil kumar V et al / Int. J. of Pharmacy and Analytical Research Vol-5(3) 2016 [388-399]UV-SPECTROSCOPY- ANALYSIS OF DRUGUltraviolet Visible (UV-visible) spectroscopyDrug sample showed wavelength of maximum absorption (λ-max) 232nm.Calibration curve of Almotriptan in 0.1N HClWavelength of maximum absorption: 232 nm.Table no 4: standard curve of Almotriptan pH 0.1N HCl at λmax 232nmTable: 4 Calibration Curve of Almotriptan with 0.1NHclS. 60.5340.620www.ijpar.com 392

Anil kumar V et al / Int. J. of Pharmacy and Analytical Research Vol-5(3) 2016 [388-399]0.7y 0.1037x 0.0067R² 0.99880.6absorbance0.50.40.30.20.1001234567conc in µg/mlGraph: 3 Calibration Curve of Almotriptan with 0.1NHclPRE FORMULATION STUDIESTable: 5 Evaluation of tablet blend for formulations (F1 – F9)Formulation Bulk ratio*index* SD(g/cc) SD SD(%) SDAngle ofrepose(ɵ) SDF10.464 0.0630.574 0.0571.23 0.15519.1 0.55629.47 0.688F20.423 0.0430.501 0.0401.16 0.25315.5 0.30527.63 0.287F30.456 0.0660.542 0.0491.22 0.21215.8 0.20825.54 0.168F40.467 0.0680.559 0.0611.25 0.22116.4 0.40126.23 0.425F50.485 0.0640.593 0.0531.10 0.38918.2 0.25127.21 0.458F60.460 0.0680.556 0.0591.21 0.12017.2 0.38629.38 0.446F70.478 0.0500.575 0.0491.24 0.29316.8 0.25628.46 0.541F80.450 0.0870.554 0.0671.28 0.25018.7 0.25825.71 0.181F90.442 0.0680.537 0.0551.27 0.09617.6 0.28729.82 0.510POST FORMULATION STUDIESTable: 6 Evaluation of Chewable Release Tablets for formulations (F1 – F9)Formulation Hardness(kg/cm2) SDF13.2 0.286Friability(%) SDWeight Thickness(mg) SD (mm) SD0.32 0.030 150 0.95 2.20 0.098www.ijpar.com 393 Disintegrationtime(sec) SDDrugcontent(%) SD17 0.1097.80 0.981

Anil kumar V et al / Int. J. of Pharmacy and Analytical Research Vol-5(3) 2016 [388-399]F23.0 0.2800.35 0.040 149 0.78 2.21 0.01714 0.1499.25 0.844F33.4 0.2480.39 0.062 152 0.47 2.16 0.05010 0.0598.13 0.745F43.6 0.2460.32 0.025 150 0.89 2.11 0.09025 0.6599.09 0.947F53.2 0.4860.36 0.061 151 0.35 2.19 0.03020 0.3299.58 0.743F63.5 0.1730.42 0.045 149 0.74 2.13 0.05015 0.4198.26 0.823F73.0 0.1150.38 0.026 150 0.53 2.20 0.07032 0.6397.35 0.935F83.3 0.2180.33 0.047 151 0.87 2.18 0.06824 0.6998.16 0.896F93.5 0.1620.40 0.052 149 0.98 2.14 0.10120 0.1299.05 0.974% FriabilityTable 7: Evaluation of Chewable Release Tablets for formulations (F1 – 1F2F3F4F5F6F7F8F9FormulationsFigure 4: Bar graph comparison friability for formulations (F1- F9)IN VITRO % DRUG RELEASETable: 8 Cumulative % drug releases for formulations (F1 – F9)Percentage Drug Release SDTime in minF1F2F3F4F5F6F7F8F90000000000522.41 0.78535.24 0.52142.21 0.53153.35 23.74 0.46636.98 0.33148.74 0.23455.87 15.86 0.50124.79 0.69552.63 0.26675.68 20.41 0.37443.57 0.33555.36 0.39262.95 35.68 0.46256.24 0.47464.56 0.60273.86 42.85 0.56358.73 0.48274.89 0.51798.16 26.89 0.68039.99 0.55563.98 0.23875.25 30.65 0.50644.85 0.62369.28 0.48882.69 29.48 0.33847.54 0.35562.87 0.49779.98 101530www.ijpar.com 394

Anil kumar V et al / Int. J. of Pharmacy and Analytical Research Vol-5(3) 2016 5510.35569.58 0.50083.74 0.47573.65 0.70696.14 0.71598.08 0.34298.49 0.54077.87 0.58287.63 0.43595.28 0.51898.03 0.18098.86 0.71099.25 0.31385.68 0.57690.59 0.24390.36 0.62697.68 0.540685.69 0.35098.09 ig 8.6: Linear graph comparison between cumulative % drug release for formulations (F1- F3)120100%CDR80F460F540F6200010203040506070TIMEFig 8.7: Linear graph comparison between cumulative % drug release for formulations (F4 - F6)www.ijpar.com 395

Anil kumar V et al / Int. J. of Pharmacy and Analytical Research Vol-5(3) 2016 EFig 8.8: Linear graph cumulative % drug release for formulations (F6)120100%CDR80F760F840F9200020406080TIMEFig 8.9: Linear graph comparison between cumulative % drug releases for formulations (F7- F9)In-vitro drug release kineticsFor understanding the mechanism of drugrelease and release rate kinetics of the drug fromdosage form, the in-vitro drug dissolution dataobtained was fitted to various mathematical modelssuch as zero order, First order, Higuchi matrix, andKrosmeyer-Peppas model. The values are compiledin Table. The coefficient of determination (R2) wasused as an indicator of the best fitting for each ofthe models considered.8.9 Drug release kinetics of Almotirptan8.9.1 Zero order release kineticsTable: 8.8 Zero order release kinetics of almotriptanwww.ijpar.com 396

Anil kumar V et al / Int. J. of Pharmacy and Analytical Research Vol-5(3) 2016 [388-399]Table No 9- R² values for release kinetics% Cumulative drug releaseTime in TIME(min)Fig 8.10: Zero order plot of Almotriptan chewable tablets (F1,F2,F3,F4, ig 8.11: Zero order plot of Almotriptan chewable tablets (F6,F7,F8, F9)www.ijpar.com 397

Anil kumar V et al / Int. J. of Pharmacy and Analytical Research Vol-5(3) 2016 [388-399]8.9.2 First order release kineticsTable: 8.9 First order release kinetics of AlmotriptanLog% drug 1.56971.30141.1556028102.5F1Log%drug remained2F2F31.5F4F51Linear (F1)Linear (F2)0.5Linear (F3)0Linear (F4)020406080Time(min)Linear (F5)Fig.8.12 First order plot of Alomtriptan chewable tablets2.5Log% drug remained2F61.5F7F81F90.5Linear (F6)0Linear (F7)020406080-0.5-1Linear (F8)Linear (F9)Time(min)Fig.8.13 First order plot of Alomtriptan chewable tabletswww.ijpar.com 398

Anil kumar V et al / Int. J. of Pharmacy and Analytical Research Vol-5(3) 2016 [388-399]Table: 8.10 data of drug release kinetic models of almotriptanFORMULATION CODEF1F2F3F4F5F6F7F8F9ZERO CONCLUSIONThe above results suggest that the formulatedimmediate release tablets of Almotriptan exhibitedgood physical parameters. The overall resultsindicated that formulation F6 with croscaramellose(7.5%) had a higher edge compared to otherFIRST formulations containing super disintegrants andpalatability is good. They satisfy all the criteria forchewable release tablets. This direct compressionprocess is simple, reproducible and robust toprepare chewable release tablets of almotriptan andother anti-migraine drugs.REFERENCES[1]. Leon Lachmann , Herbert A , Liberman , Joseph L.Kaing , The theory and practice of Industrial Pharmacy, 293303.[2]. Aulton ME, Wells TI, Pharmaceutics, the Science of Dosage Form Design, Churchill Livingstone, Vingstone,London, 1988, 168.[3]. United States pharmacopoeia (USP 29-NF 24), the official compendia of standards twin brook parkway,rockvillle. Asian Edition, 3, 27, 60-62, 2007, 2675, 2505.[4]. Indian Pharmacopoeia, the controller of publication, Ministry of Health and Welfare. 1, 1996, 1178.[5]. Subhramanyam CVS and Thimasetty J. Laboratory Manual of physical pharmaceutics. 5, 2005, 321-325.[6]. Chavkin et al., United state patents, 5, 753, 255, chewable molded tablets containing medicinally activesubstances, 1998.[7]. Kanig JL nad Rudinc EM, The mechanism of disintegrant action,pharm tech,50-63,CRS,Vienna,Austria, 2006.[8]. Kashid et al, United state patents, 2009/0269393, chewable Bilayer formulation, 2009.[9]. Drug dosage form II (PHR312), advantages of chewable tablets, pharos university, Alexandria, 6, 2011.[10]. Drug dosage form II (PHR312), advantages of chewable tablets, pharos university, Alexandria, 6, 2011.www.ijpar.com 399

Formulation and evaluation of almotriptan chewable tablets 1V. Anil kumar*, K.L. Deepthi*, 1R. Kalyani, 1B. Padmasri, 2D.Prasanth . in the formulation of a chewable tablet is to obtain a complete profile of the active drug. This usually leads to the most efficient formulation of a stable and quality product as the drug usually dictates the choice of fillers, carriers, sweeteners, flavor .

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