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ISSN 0974 – 9446
FORMULATION AND EVALUATION OF ORALLY DISINTEGRATING TABLETS OF SERTRALINE Suhas M. Kakade1*, Vinod S. Mannur1, Ravindra V. Kardi1, Ketan B. Ramani1, Ayaz A. Dhada1 Department of Pharmaceutics, K.L.E. University’s college of pharmacy, J.N.M.C. Campus, Belgaum – 590010, India. Email: email@example.com
ABSTRACT There is an increasing demand for more patient compliant dosage form and a novel method is the development orally disintegrating tablets which dissolve or disintegrates instantly on the patient tongue or buccal mucosa. It is suited for tablets undergoing high first pass metabolism and is used for improving bioavailability with reducing dosing frequency to minimize side effect and make it more cost effective. Sertraline is practically slightly soluble in water, its rapidly and extensively absorbed after oral administration, the absolute bioavailability is only approximately 44% due to extensive hepatic first pass metabolism. Hence the main objective of the study was to formulate orally disintegrating tablets of sertraline to achieve a better dissolution rate and further improving the bioavailability of the drug. Orally disintegrating tablets prepared by direct compression and using super disintegrants like crospovidone, croscarmellose sodium and sodium starch glycolate designate, designated as three different groups of formulation ( A, B and C) respectively were prepared and evaluated for the precompression parameters such as bulk density, compressibility, angle of repose etc. The prepared batches of tablets were evaluated for hardness, weight variation, friability, drug content, disintegration time and in-vitro dissolution profile and found satisfactory. Among the three groups, group (C) containing crospovidone emerged as the best formulation and showed maximum dissolution rate with 98.49% drug release in 15 min. All three groups of formulations released the drug at faster rates than that of marketed conventional tablets of sertraline. Key-words : Sertraline, Superdisintegrants, Orally disinintegrating tablets.
International Journal of Pharma Research and Development – Online
Sertraline is a selective serotonin reuptake inhibitor (SSRI) used as an adjuvant in the treatment of depression and anxiety disorder. The absolute bioavailability is only approximately 44% due to extensive hepatic metabolism. However.2 To improve the quality of life and treatment compliances of such patients fast disintegrating or orally disintegrating tablets dosage form is abetter alternative for oral medication. Methods: Prepration of orally disintegrating tablets: Sertraline orally disintegrating tablets were prepared by direct compression method. All chemicals and reagents used were of analytical grade.1 Difficulty in swallowing is experienced by patient such as pediatric. Hydrabad.3 Orally disintegrating tablets are solid dosage form containing medical substances which disintegrate rapidly. usually within few seconds when placed upon tongue requiring no additional water to facilate swallowing. Direct compression dose not require the use of water or heat during the formulation procedure and is the ideal method for moisture and heat-labile medications. disabled and mentally ill. Evaluation of orally disintegrating tablets of sertraline: All the batches of tablets were evaluated for various parameters like weight variation. then finally 1mg Magnesium Sterate and 1mg Aerosil was added material was slightly compressed on the 8mm flat-faced punch using a Rimek tablet press machine. disintegration and dissolution and results reported in Table 2. Ltd. including motion sickness and sudden episodes of allergic attacks. MATERIALS AND METHODS Materials: Sertraline was obtained as a gift sample from Sai Ram Organics Pvt.4 It is suited for tablets undergoing high first pass metabolism and is improving bioavailability with reducing dosing frequency to minimize side effect. which may produce the rapid onset of action in the treatment of depression and anxiety disorder. hence resulting in higher incidence of non-compliance and ineffective therapy. The aim of purpose work was to formulate and characterization orally disintegrating tablets of sertraline for rapid dissolution of drug and absorption. drug content. Compositions of various formulations are shown in Table 1. Crospovidone and Lactose spray dried were gift sample from Signet Chemical Corporation. hardness. Ahmedabad. The total weight of the formulation was maintained 200mg.5 Various techniques can be used to formulate orally disintegrating tablets or fast dissolving tablets. All the ingridents of the orally disintegrating tablets of sertraline were weighed and mixed in mortar with the help of pestle. Croscarmellose sodium. the low aqueous solubility it is rapidly and extensively absorbed after oral administration.: IJPRD/2010/PUB/ARTI/VOV-1/ISSUE-12/FEB/007 ISSN 0974 – 9446 INTRODUCTION AND MATERIALS & METHODS INTRODUCTION Recent advance in novel drug delivery system aims to enhance the safety and efficacy of the drug molecule by formulating a dosage form being for the administration. Sodium starch glycolate and Microcrystalline cellulose were gift samples from Sunrise Remedies. geriatric. Mumbai.6 Direct compression one of the techniques requires the incorporation of a superdisintegrants into the formulation the use or highly water soluble excipients to achieve fast tablet disintegration.ijprd. India. 2 International Journal of Pharma Research and Development – Online www. Different concentration of excipients was used to prepare different groups of orally disintegrating tablets.com . friability. bedridden.Publication Ref No.
8) was taken as the dissolution medium at 50 rpm and 370C±0. Mumbai.ijprd. Friability test: Six tablets from each batch were examined for friability using Roche Fribilator (Tropical Equipment Pvt. Content uniformity test: Five tablets were weighed and powdered. R = 100 (Wa – Wb)/Wb Where Wb and Wb are the weight before and after water absorption. Mumbai. The samples were analyzed spectrophotometrically at 270 nm. The tablet was placed on the tissue paper and allowed to wet completely.: IJPRD/2010/PUB/ARTI/VOV-1/ISSUE-12/FEB/007 ISSN 0974 – 9446 Weight variation test: Twenty tablets were taken and their weight was determined individually and collectively on a digital weighting balance. The wetted tablet was removed and reweighted. 3 International Journal of Pharma Research and Development – Online www. In vitro disintegration time: The disintegration test was performed using an USP disintegration apparatus. Wetting time: A piece of tissue paper folded twice was kept in a Petri dish (inter diameter 5.Publication Ref No. Five millilitres of aliquots were periodically withdrawn and the sample volume was replaced with an equal volume of fresh dissolution medium. the solution was filtered suitably diluted and the drug content was analyzed using UV spectrometer at 270 nm. In vitro dissolution testing: Dissolution study was conducted for all the formulation using USP type-II apparatus (Electolab.com . Hardness test: The hardness of the tablet was determined using Monsanto Hardness Tester. dedusted and reweighted and % friability was calculated. respectively. The tablets were taken out. R was determined according to the following equation.). The time required for complete wetting of the tablet was then recorded. The dissolution test was performed using 500 ml of phosphate buffer (PH 6. Ltd. The tablet was placed on the tissue paper and allowed to wet completely. %Friability = (Loss in weight/Initial weight) x 100 Water absorption ratio: A piece of tissue paper folded twice was kept in a Petri dish (internal diameter 5. The average weight of one tablet was determined from the collective weight. 10 mg of equivalent of sertraline was weighed and dissolved in suitable quantity of methanol.5cm) containing 6ml of purified water. India) and the equipment was run for 4min at 25 revolutions per minute.50C. Water absorption ratio. The time reported to obtain complete disintegration of six tablets were recorded and average was reported.50C. India. with distilled water at 24±0.5cm) containing 6ml of purified water.
89. Ito. Mouth Dissolving Tablets: A Novel Drug Delivery System. T. Brown. Yuki.49%. Paul. Bull.23-0. Seager. Ltd. B. Drug Delivery Technol.. J. 193-198. The result in vitro disintegration were within the prescribe limit and comply with the criteria for orally disintegrating tablets. A. Bull... friability. International Journal of Pharma Research and Development – Online 4 www.. The cumulative % of drug release increased in 15 min with increased in the concentration of superdisintegrant. 1999. 7-9.15% with crospovidone. 35. 1998. Masanobu. ACKNOWLEDMENT We acknowledge generous help of Sai Ram Organics Pvt. H.com . 2002.. Kathleen. solubility enhancement of sertraline required and is under investigation. Kozo. the value were with 18-43sec. croscarmellose sodium and sodium starch glycolate respectively.45-37.. 375-82. 50(9). Studies of rapidly disintegrating tablets in the oral cavity using co-grinding mixtures of mannitol with crospovidone.. Hyderabad. 5.36% and 86. 2002.S. S. drug content.4–4. India. The loss in total weight of the tablets due to friability was in the range of 0. The drug content in different formulation was highly uniform and in the range of 97-99%. Pharmacol. M.. T. Evalution of the disintegration time of rapidly disintegrating tablets via a novel method utilizing a CCD camera. All above properties and value were near to boundary of standard limit. India for providing gift samples of sertraline and superdisintegrants respectively.. 32nd Edn. 2003.. Mumbai.61%. 1181-1186. REFERENCES 1. H. Chem. Chem. Pharm. P.. (Figure No. India. Pharm. 4.B. In vitro dissolution studies are shown in table 2 and fig.1).: IJPRD/2010/PUB/ARTI/VOV-1/ISSUE-12/FEB/007 ISSN 0974 – 9446 RESULT AND DISCUSSION Sertraline orally disintegrating tablets were prepared by direct compression method.. 2004. B and C) of formulation with variation of tablet excipent were prepared with each group containing three different formulations. Ltd. CONCLUSION In the present study it can be concluded from the characterization of orally disintegrating tablets of sertraline that formulation containing crospovidone is most acceptable. Y.. Table 2 shows the data obtained from the evaluation of tablets.S. 2. K.. Martindale the complete drug reference.. Hironaka. And Sunrise Remedies Pvt. wetting time.. 6..C. C.S... 1-4. Ahmadabad. Mahajan.ijprd. Wetting time is used as an indicator of the ease of tablet disintegration and found to be 17-32sec. disintegration and dissolution which were reported in Table no 2. UK. Kuchekar. 50. Three different groups (A. 3 and 4. Shu. All the tablets maintained hardness in the range 3. Junko. T. A. T. 3. K. D. Suzuki. Yutaka.. 91. Water absorption ratio ranged from 18. Pharmaceutical press. H. Signet Chemical Corporation. 307-308. At 10% superdisintegrant level the drug release at the end of 15 min. It was observed that to further increase the drug release from orally disintegrating tablets. were found to be 98. Ryoji.1kg/cm2.. All batches of the tablets were preliminarily evaluated for various physical parameters such as hardness.. Sean. Drug-delivery product and the zydis fast dissolving form. 50(4). Pharm. Pharma Times. water absorption ratio. 2.Publication Ref No. Badhan.
Badhan.. J. G. Indian Drugs.H.. D. Ramesh. 8.C.Y. J. 592-598. The theory and practice of industrial pharmacy.S. C. 41(10).. Shravan K. Adhukondalu. 10.. Lachman. Int. Y. Madhusudan. Mouth Dissolving Tablets of Salbutamol Sulphate: A Novel Drug Delivery system...A.. Jachion. H..: IJPRD/2010/PUB/ARTI/VOV-1/ISSUE-12/FEB/007 ISSN 0974 – 9446 7. L. Formulation and Evaluation of Orally Disintegrating Tablets of Buspirone. Liberman. J. Reynier. Piccerellel.ijprd. 9.. 2004.L. B. 3rd Edn. G. Pharm. A. Rajitha.. 2004.. Mahajan. 293-294. 2003. Kanig. Eouani..S.Publication Ref No. P. Varghese Pub. Pharm. P.. 1(4). House: Bombay. Kuchekar.P.com .. 29-41. Determination of the In vitro Disinetgration Profile of Rapidly Disintegrating Tablets and Correlation with Oral Disinetgration. 372-334. J. and Nanotechnol. Abdelbary.. 292. 2009. Int... K. J.. FIGURES & TABLES Table 1: Formulation of Sertraline Orally Disintegrating Tablets Ingredients Group A A1 Sertaline Lactose (Spray Dried) MCC Crospovidone Croscarmellose Sodium SSG Aspartame Aerosil Mg Stearate 50 96 40 10 2 1 1 A2 50 91 40 15 2 1 1 A3 50 86 40 20 2 1 1 Group B B1 50 96 40 10 2 1 1 B2 50 91 40 15 2 1 1 B3 50 86 40 20 2 1 1 Group C C1 50 96 40 10 2 1 1 C2 50 91 40 15 2 1 1 C3 50 86 40 20 2 1 1 5 International Journal of Pharma Research and Development – Online www.. Prinderre. Sci. H.
44 ± 0.7 ± 0.34 ± 0.36 78.01 4.com .87 ± 0.45 ± 1.4 ± 0.638 33 ± 1.26 82.67 ± 0.04 99.09 ± 1.73 91.02 97.89 ± 1.00 26.33 ± 0.01 Friabilit y (%) Drug content (%) Disinteg ration time (sec.23 ± 0.36 30.33 ± 1.61 ± 0.07 98.00 32.61 19.138 43 ± 0.12 4.8 ± 0.00 22.89 ± 1.40 ± 0.02 3.43 ± 0.59 34.00 24.00 ± 0.: IJPRD/2010/PUB/ARTI/VOV-1/ISSUE-12/FEB/007 ISSN 0974 – 9446 Table 2: Evaluation data of the prepared sertraline orally disintegrating tablets Evaluati on Paramet ers Hardnes s (kg/cm2) Group A A1 A2 A3 B1 Group B B2 B3 C1 Group C C2 C3 3.528 38 ± 2.653 20 ± 2.) Wetting time (sec.25 0.76 34 ± 2.9 ± 0.6 ± 0.38 ± 0.01 ± 1.) i e sc 30 25 20 15 10 5 0 A1 A2 A3 B1 B2 B3 C1 Disintegration time Wetting time C2 C3 For m ulation Figure 1: Disintegration time and Wetting time of Sertraline orally disintegrating tablets 6 International Journal of Pharma Research and Development – Online www.05 98.33 ± 0.00 0.01 98.00 17.1 ± 0.00 0.25 0.12 27.00 18.39 ± 0.71 91.00 22.03 3.09 ± 1.04 99.00 ± 1.00 25.1 ± 0.Publication Ref No.936 89.01 99.15 50 45 40 35 Tm ( e .23 98.90 0.06 3.) Water absorpti on ratio % Cumulat ive drug release 0.123 24 ± 2.03 98.01 36.37 ± 1.965 21 ± 1.ijprd.06 3.345 26 ± 2.45 ± 2.56 ± 0.5 29.6 ± 0.49 85.84 ± 2.7 ± 0.89 0.34 ± 1.03 97.58 28.35 0.58 37.79 ± 1.11 88.135 18 ± 1.55 18.03 3.00 23.18 0.26 86.01 3.
ijprd.Publication Ref No.: IJPRD/2010/PUB/ARTI/VOV-1/ISSUE-12/FEB/007 ISSN 0974 – 9446 % Cumulative drug release 100 80 60 40 20 0 0 3 6 9 12 15 18 Time in minutes A1 A2 A3 Figure 2: Drug release profile of group ‘A’ tablets 100 % Cumulative drug release 80 60 40 20 0 0 3 6 9 12 15 18 Time in minutes B1 B2 B3 Figure 3: Drug release profile of group ‘B’ tablets 100 % Cumulative drug release 80 60 40 20 0 0 3 6 9 12 15 18 Time in minutes C1 C2 C3 Figure 4: Drug release profile of group ‘C’ tablets 7 International Journal of Pharma Research and Development – Online www.com .
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