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Published on March 10, 2014

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PowerPoint Presentation: FORMULATION AND EVALUATION OF FAST DISINTEGRATING SUBLINGUAL TABLETS OF LOSARTAN POTASSIUM Under the guidance of Prof. (Dr.)T.N.K. Suriyaprakash , M.Pharm ., Ph.D Principal, Al Shifa College of Pharmacy. KERALA UNIVERSITY OF HEALTH SCIENCES Presented by MUHAMMED ISHAD PM Reg No : 103270018 PowerPoint Presentation: Plan of work N eed of work Literature review Introduction D rug and excipients profile Summary and conclusion Bibliography Aim and objective Result and discussions CONTENTS PowerPoint Presentation: Introduction Fast disintegrating sublingual tablets is defined as a solid dosage form that contains medicinal substances and disintegrates rapidly (within few seconds) without water when kept under the tongue . Advantages: Ease of administration to patients who refuse to swallow a tablet, such as pediatric, geriatric patients and psychiatric patients. Convenience in administration of drug and accurate dosing as compared to liquid formulations. Water is not required for swallowing the dosage form , Good mouth feels property helps to change bitter pill, particularly for pediatric patients. Fast disintegration of medicament and absorption which will leads to rapid, onset of action. PowerPoint Presentation: Disadvantages: Since sublingual administration of drugs interferes with eating. Sublingual medication cannot be used when a patient is unconscious. PowerPoint Presentation: Sublingual route is capable of producing a rapid onset of action. The drug is released in to saliva and its subsequent spreading may cause the drug to be absorbed across the oral cavity. S timulation of salivary secretion oxygen is consumed and vasodilator substances are produced, and the glandular blood flow increases. The salivary glands consist of lobules of cells which secrete saliva through the salivary ducts into the mouth. The three pairs of salivary glands are the Parotid, Sub mandibular and the Sublingual which lies on the floor of the mouth. High permeability and the rich blood supply, the sublingual route is capable of producing a rapid onset of action which makes it an appropriate route for drugs with short delivery period and in frequent dosing regimen. Mechanism of Sublingual Absorption . PowerPoint Presentation: Factors affecting the sublingual absorption. PowerPoint Presentation: This system is produced using standard tablet technology by direct compression of excipients . Simplest means of production of a pharmaceutical tablet. It reduces, 1) Capital 2) L abour 3) E nergy costs for manufacture 4) Avoidance of water for granulation for water sensitive drug substances. Technique used for preparation of fast disintegrating sublingual tablets PowerPoint Presentation: Crospovidone ( Kollidon CL,Polyplasdone XL ) Croscarmellose sodium (Ac-Di-Sol, Nymce ZSX, Primellose , Solutab , Vivasol ) Sodium starch glycolate ( Explotab , Primogel , Vivastar P) Sodium alginate ( Kelcosol , Keltone , Protanal ) Low hydroxypropyl cellulose Commonly Used Superdisintegrants PowerPoint Presentation: LITERATURE REVIEW Sharma et al, [29] has done formulation and evaluation of fast disintegrating sublingual tablets of glipizide : an attempt to treat diabetic coma using different superdisintegrants . Bayrak et al, [30] studied the formulation of zolmitriptan sublingual tablets prepared by direct compression with different polymers.The tablets disintegrated rapidly, and dissolution tests revealed that zolmitriptan was dissolved from the formulation within the limits . Aghera et al, [32] has studied Formulation and evaluation of sublingual tablets of losartan potassiumSublingual tablets of Losartan Potassium were prepared to improve its bioavailability, pre-systemic metabolism in the gastrointestinal tract and hepatic first pass elimination PowerPoint Presentation: DRUG PROFILE Losartan potassium Description: A white to off-white crystalline powder. Therapeutic Category : Antihypertensive Agents Angiotensin II Receptor Antagonists Bioavailability: 33% Metabolism : Hepatic Volume of distribution: 34L Half life: 1.5–2 hours. PowerPoint Presentation: Polymers used Crospovidone : Description: Crospovidone is a white to creamy-white, finely divided, freeflowing,practically tasteless, odorless or nearly odourless, hygroscopic powder . PowerPoint Presentation: Croscarmellose sodium: Synonyms: Ac-Di-Sol. Description: White or greyish white powder. Odourless and tasteless. Insoluble in water. Practically insoluble in acetone, ethanol and toluene. Magnesium stearate: Magnesium stearate is widely used in cosmetics, foods, and pharmaceutical formulations. It is primarily used as a lubricantin capsule and tablet manufacture. Description: Magnesium stearate is a very fine, light white powder. Faint odour. PowerPoint Presentation: Sodium starch glycolate : Synonyms: Explosol . Explotab . Description: Sodium starch glycolate is a white to off-white, odorless , tasteless, free flowing powder. It does not melt, but chars at approximately 200 o C. It is sparingly soluble in ethanol (95%) but practically insoluble in water. PowerPoint Presentation: The need for sublingual administration is that, In the case of liquid oral dosage form ,there is always the problem of dosing the drug accurately, As for parenteral it is painful, Dysphagia in case of tablet. Hence the utility of a newer route should be investigated Fast disintegrating sublingual tablet I mprove its bioavailability to avoid pre-systemic metabolism in the gastrointestinal tract and hepatic first pass elimination. NEED OF WORK PowerPoint Presentation: AIM AND OBJECTIVES AIM: Formulation and evaluation of fast disintegrating sublingual tablets of losartan potassium. Avoiding the first pass metabolism and improve its bioavailability to avoid pre-systemic metabolism in the gastrointestinal tract and hepatic first pass elimination with reduction in dosing frequency. . PowerPoint Presentation: OBJECTIVE OF STUDY: Compare it with marketed formulation . To report stability of fast disintegrating sublingual tablets of losartan potassium PowerPoint Presentation: PLAN OF WORK Formulation of FDST PowerPoint Presentation: EXPERIMENTAL WORK PREFORMULATION STUDY PHYSICAL PROPERTIES: Organoleptic properties: Colour , odour and appearance Melting point Solubility: D istilled water, phosphate buffer pH 6.8. PowerPoint Presentation: COMPATIBILITY STUDY S tudy was carried out by using FTIR Drug & excipients were prepared in the proportion of 1:1 The scanning was 200-400 nm. FTIR of the pure drug, polymer and their combinations were obtained. To find out any interaction was there between drug and the polymer. Absence of characteristic bands of the drug would indicate the interaction with polymers PowerPoint Presentation: CALIBRATION CURVE OF LOSARTAN POTASSIUM Stock solution of 1mg/ml was prepared in phosphate buffer pH 6.8 Diluted with 6.8 phosphate buffer to obtain the known std solutions in the range of 1-6 mcg/ml Absorbance was measured using shimadzu UV-Visible spectrophotometer in wavelength of 250nm The absorbance values were plotted against concentrations of losartan potassium PowerPoint Presentation: INGREDIENTS   F1 F2 F3 F4 F5 F6 F7 F8 F9 LOSARTAN POTASSIUM 20 20 20 20 20 20 20 20 20 SODIUM STARCH GLYCOLATE 25 30 35             CROSCARMELLOSE SODIUM       25 30 35       CROSPOVIDONE             25 30 35 MICROCRYSTALLINE CELLULOSE 88 83 78 88 83 78 88 83 78 MANNITOL 50 50 50 50 50 50 50 50 50 SODIUM SACCHARIN(5%) 10 10 10 10 10 10 10 10 10 MAGNESIUM STEARATE 5 5 5 5 5 5 5 5 5 TALC 2 2 2 2 2 2 2 2 2 TOTAL WEIGHT OF TABLET 200 200 200 200 200 200 200 200 200 UNIT FORMULA FOR DIFFERENT FORMULATION PowerPoint Presentation: FORMULATION DEVELOPMENT PowerPoint Presentation: PRE COMPRESSION STUDIES: 1) Angle of repose θ = tan -1 (h/r) 2) Bulk density Bulk density (Po) = mass / untapped volume 3) Tapped density Tapped density (Pt) = mass / tapped volume 4) Compressibility index C.I. = (Tapped density ‐Bulk density)/(Tapped density) x 100 5) Hausner ratio Hausner ratio = tapped density / bulk density PowerPoint Presentation: POST COMPRESSION STUDIES: Hardness. Thickness. Drug content. Weight variation test. Friability. Wetting Time. Water Absorption Ratio. Disintegration test. Dissolution Studies. Accelerated Stability Studies. PowerPoint Presentation: 1) Organoleptic properties: PREFORMULATION STUDY PHYSICAL PROPERTIES: Organoleptic properties Observations Colour White to Off white Description Crystalline powder 2) Melting point:   Drug name Melting point Observed(°C) Reported(°C)   LOSARTAN POTASSIUM   183.5-184.5°C   184°C PowerPoint Presentation: 3) Solubility study: Solvent Solubility 1) Distilled water 42mg/100ml 2) pH 6.8 phosphate buffer solution 38mg/100ml PowerPoint Presentation: COMPATIBILITY STUDY BY FTIR   Functional groups Wave number standard (cm -1 ) Wave number Observed (cm -1 ) OH 3100-3600 3130.57 CH Stretching (Aromatic) 3000-3100 3003.27   CH Stretching (Aliphatic) 2850-3000 2963.12 C-O 1050-1150 1110.75 C=C stretch   1400-1600 1600 Al-CH-bend 1350-1480 1454.3 PowerPoint Presentation: Inference: Major peaks observed in individual drug spectrum also observed in spectrum of drug with polymer, therefore no incompatibility between drug & different polymers. PowerPoint Presentation: CALIBRATION CURVE OF LOSARTAN POTASSIUM S tandard curve of Losartan potassium ( pH – 6.8 phosphate buffer ) Concentration (μg/ml) Absorbance (nm) 1 0.01 2 0.031 3 0.051 4 0.07 5 0.093 6 0.111 PowerPoint Presentation: Formulation Angle of repose Bulk density g/cm 3 Tapped density g/cm 3 Compressibility index (%) Hausner’s ratio F1 27˚.23’ 0.45 0.54 16.66 1.20 F2 26˚.22’ 0.40 0.48 16.6 1.20 F3 27˚.10’ 0.44 0.52 15.38 1.18 F4 26˚.75’ 0.46 0.51 9.80 1.10 F5 25˚.16’ 0.44 0.53 16.98 1.20 F6 25˚.13’ 0.43 0.52 17.30 1.20 F7 24˚.35’ 0.42 0.51 17.64 1.21 F8 27˚.10’ 0.43 0.52 17.30 1.20 F9 26˚.12’ 0.48 0.54 11.11 1.12 PRE COMPRESSION STUDIES: PowerPoint Presentation: POST COMPRESSION STUDIES: Formulation Hardness kg/cm 2 Thickness (mm) Drug content (%) Weight variation (mg) Friability (%) Wetting time (sec) Water absorption ratio (%) F1 3.5 3.12 97.82 185.04-206.84 0.47 28 63.91 F2 3.7 3.03 98.17 184.5 - 207.5 0.40 29 75.13 F3 3.5 2.94 98.32 184.26-205.12 0.47 28 68.60 F4 3.4 2.90 97.28 184.7 -207.44 0.59 29 79.65 F5 3.8 3.10 97.56 184.63-204.49 0.60 26 78.17 F6 3.5 3.12 96.26 185 -204.98 0.53 26 82.05 F7 3.8 2.81 98.25 184.88-203.86 0.40 20 80.21 F8 3.7 3.10 98.32 184.85-204.81 0.42 18 82.27 F9 3.8 3.21 98.44 184.88-205.86 0.40 15 84.71 PowerPoint Presentation: Disintegration studies: Formulation Disintegration time (sec) F1 44 F2 48 F3 43 F4 51 F5 49 F6 50 F7 31 F8 28 F9 20 PowerPoint Presentation: This results showed that F9 has minimum disintegration time. Hence it will disintegrate first compare to other formulations. PowerPoint Presentation: Dissolution Studies: Dissolution studies were carried out for all the formulation in USP paddle method (Apparatus 2) using Phosphate buffer 6.8 D issolution medium (900 mL) at 50 rpm and 37 + 0.5 o C. Samples were periodically withdrawn at suitable time intervals ( 0,5,10,15,20,25mints) and volume replaced with equivalent amounts of plain dissolution medium. The samples were analysed spectrophotometrically at 250 nm. PowerPoint Presentation: Comparative Drug Release Profile at different concentration of SSG . Time in minutes Cumulative % drug release F1 F2 F3 0 0 0 0 5 63.86 65.46 68.67 10 65.77 70.80 74.60 15 75.06 81.70 83.70 20 79.91 86.90 88.81 25 80.12 89.08 91.08 PowerPoint Presentation: 2) Comparative Drug Release Profile at different concentration of CCS Time in minutes Cumulative % drug release F4 F5 F6 0 0 0 0 5 34.56 37.60 69.78 10 55.62 65.66 79.86 15 68.45 76.67 85.16 20 76.65 85.60 88.87 25 78.45 86.40 89.45 PowerPoint Presentation: 3) Comparative Drug Release Profile at different concentration of CP Time in minutes Cumulative % drug release F7 F8 F9 0 0 0 0 5 62.74 67.28 68.76 10 70.34 76.80 83.08 15 76.71 85.30 91.56 20 83.71 91.20 96.38 25 85.45 93.40 97.56 PowerPoint Presentation: 4) Comparative Drug Release Profile of F3(SSG-17.5%),F6(CCS-17.5%), F9(CP-17.5%) PowerPoint Presentation: The results indicate that the drug release of all the formulations were found to be above 60% in five minutes except for formulations ( F4 and F5 ). The release rate of the three superdisintegrants were in the order of Crospovidone > Sodium Starch Glycolate > Croscarmallose . PowerPoint Presentation: Comparative In vitro dissolution profile and disintegration of best formulation (F9) with marketed product (MP). F9 Marketed product Disintegration time (sec) Dissolution Disintegration time (sec) Dissolution Time (sec) % drug release Time (sec) % drug release 20 0 0 41 0 0 5 68.76 5 22.44 10 83.08 10 38.94 15 91.56 15 55.44 20 96.38 20 66.86 25 97.56 25 70.78 PowerPoint Presentation: ACCELERATED STABILITY STUDIES Strength : 20 mg Storage Condition : 40±2°C, 75±5% RH Sl no: Condition Initial 1 Month 2 nd Month 3 rd Month 1 Drug content 98.40 97.8 97.6 97.3 2 Dissolution 97.56 97.54 97.51 97.49 3 DT in seconds 20 21 21 22 4 Description White to off white tablet. PowerPoint Presentation: It can be inferred from the above data that there is no significant change in product performance upon stability and thus the product is Stable. PowerPoint Presentation: SUMMARY AND CONCLUSION The purpose of the study was to formulate and evaluate Fast Disintegrating Sublingual Tablets of Losartan Potassium. The results of Fourier Transmission Infra-Red spectroscopy confirm that both drug and excipients including polymers are compatible with each other and are devoid of interactions. The results of precompression studies like angle of repose, bulk density, tapped density, compressibility index and hausner’s ratio reveals that the prepared powder blends of all formulations possess good flow properties. The tablets were prepared by direct compression method using superdisintegrants like Sodium starch glycolate (F1 to F3), Croscarmallose (F4 to F6), Crospovidone (F7 to F9) in different concentrations of 12.5% ,15% ,17.5% and 25% Mannitol is used as both binder and sweetener, sodium saccharin for additional taste masking and Microcrystalline cellulose as diluent. The tablets obtained were of uniform shape and size. PowerPoint Presentation: The prepared tablets were subjected to post compression evaluations and the results indicate that, The hardness, thickness of all the tablets are uniform, which ensures that all the tablets were of uniform size and shape with good resistance against mechanical damage. The tablets of all formulations contains uniform amount of drug, which ensures content uniformity for tablets of all formulations. The tablets were within the limits of weight variation test, which in turn indicate uniform distribution of contents of the powder blends of each formulations. The friability of all the tablets was found to be ˂ 1%, which indicates the good mechanical resistance. The tablets of all formulations were found to have minimum wetting time and maximum water absorption ratio which is the desired characteristic of fast disintegrating sublingual tablets, which enables faster disintegration of tablets . The disintegration time of all tablets were found to be less than three minutes, which ensures faster disintegration. PowerPoint Presentation: Conclusion: It was concluded, that Losartan potassium can be successfully formulated as fast disintegrating sublingual tablets using various superdisintegrants (Sodium starch glycolate , croscarmellosesodium , crospovidone ) in different concentrations ( 12.5,15%,17.5% each) by direct compression method. The formulation containing 17.5% of crospovidone (F9) as superdisintegrant was found to be outstanding than other formulations including marketed product in terms of disintegration time and rate of dissolution. PowerPoint Presentation: BIBLIOGRAPHY Zhang H, Zhang J, Streisand JB. Oral Mucosal Drug Delivery: Clinical Pharmacokinetics and Therapeutic Applications. ClinPharmaco 2002: 41(20):661-680. A Short Review on “A Novel Approach in Oral Fast Dissolving Drug Delivery System and Their Patents”M.D . Nehal Siddiqui, GarimaGarg and Pramod Kumar Sharma, Advance in biological Reaserch 5 (6): 291-203, 2011. Sublingual mucosa as a route for systemic drug delivery,neha narang1, jyotisharma , International Journal of Pharmacy and Pharmaceutical Sciences,Vol 3, Suppl 2, 2011. Birudaraj R, Berner B, Shen S. Buccal permeation of buspirone : Mechanistic studies on transport pathways. J Pharm Sci 2005; 94: 70-78. Price TM, Blauer KL, Hansen M, Stanczyk F, Lobo R, Bates GW. Singledose pharmacokinetics of sublingual versus oral administration of micronized 17 beta- estradiol . Obstet Gynecol. 1997; 89: 340-345. PowerPoint Presentation: 6) urosaki Y, Takatori T, Nishimura H, Nakayama T, Kimura T . Regional variation in oral mucosal drug absorption permeability and degree of keratinization in hamster oral cavity. Pharm Res 1991; 8: 1297 ‐ 1301. 7) Ghosh TK, Chatterjee DJ, Pfister WR. Quick dissolving oral dosage forms: Scientific and regulatory considerations from a clinical pharmacology and biopharmaceutical perspective. In: Ghosh TK and Pfister WR ( Eds ). Drug Delivery to the Oral Cavity Molecules to Market. NY, USA: CRC Press, 2005: 337 ‐ 356. 8) Richman MD, Fox D, Shangraw RF. Preparation and stability of glyceryltrinitrate sublingual tablets prepared by direct compression. J Pharm Sci 1965; 54(3): 447 ‐ 451. 9) Mary Elizabeth RN, Martelli BS. Sublingual and buccal medication administration. Encyclopedia of Nursing and Allied Health, 20050229. 10) Lea L. Sublingual Administration. Colon Health 1996; 13. Shojaie AH. Buccal mucosa as a route for systemic drug delivery: A review. J Pharm PharmSci 1998; 1(1):15 ‐ 30

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