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Edit Comment Close Premium member Presentation Transcript SUPERDISINTEGRANTS…..: SUPERDISINTEGRANTS….. Present By Mr.Uday B. Pawar M.Pharm. Pharmaceutics. 1CONTENTS: CONTENTS Introduction Advantages & Disadvantages Classification Mechanism of superdisintegrants Factors affecting superdisintegrants Method of addition of superdisintegrants Comparative study of superdisintegrants Newer Super disintegrants Conclusion References 2 INTRODUCTION: INTRODUCTION Disintegrants are substances or mixture of substances added to the drug formulation that facilitate the breakup or disintegration of tablet or capsule content into smaller particles that dissolve more rapidly. Superdisintegrants are generally used at a low concentration in the solid dosage form, typically 1– 10 % by weight relative to the total weight of the dosage unit. Eg. Superdisintegrants are crosscarmelose, crosspovidone, and sodium starch glycolate. 3PowerPoint Presentation: The superdisintegrants include a particulate agglomerate of coprocessed starch or cellulose and a sufficient amount of an augmenting agent to increase the compactibility. The augmented superdisintegrant provides a fast disintegration of a solid dosage form when incorporated in sufficient quantity. For many solid dosage forms disintegration occurs prior to drug dissolution and superdisintegrants such as crospovidone, SSG, croscarmellose sodium are now frequently used in tablet formulations to improve the rate and extent of tablet disintegration and thus increase the rate of drug dissolution. 4ADVANTAGES : ADVANTAGES Remarkable tendency on wetting causing rapid Disintegration. No lump formation on disintegration. Compatible with commonly used therapeutical agents and excipients. Work equally effective in hydrophilic and hydrophobic formulations. Provides good mechanical strength to the tablet facilitating easy packing and transportation. 5DISADVANTAGES: DISADVANTAGES More hygroscopic (may be a problem with moisture sensitive drugs) Some are anionic and may cause some slight in-vitro binding with cationic drugs (not a problem in-vivo.) 6CLASSIFICATION: CLASSIFICATION Structural Type (NF Name) Description Trade Name Modified starches (Sodium starch glycolate) The carboxymethyl groups induce hydrophilicity and cross-linking reduces solubility. Explotab Primojel Modified cellulose (Crosscarmelose, NF) Sodium carboxymethyl cellulose, which has been cross-linked to render the material insoluble. Ac-Di-Sol Nymcel Primellose Solutab. Cross-linked polyvinylpyrrolidone (Crospovidone, NF) It has high molecular weight and cross-linking render the material insoluble in water. Crospovidone Kollidon Polyplasdone 7MECHANISM OF SUPERDISINTEGRANTS: MECHANISM OF SUPERDISINTEGRANTS There are four major mechanisms : Swelling Wicking (capillary) Deformation Repulsion 8Mechanism By Swelling: Mechanism By Swelling Swelling is believed to be a mechanism in which certain disintegrating agents (such as starch) impart the disintegrating effect. By swelling in contact with water, the adhesiveness of other ingredients in a tablet is overcome causing the tablet to fall apart . 9 Wicking (capillary action): Wicking (capillary action) Tablet porosity provides pathways for the penetration of fluid into tablets. The disintegrant particles (with low cohesiveness & compressibility) themselves act to enhance porosity and provide these pathways into the tablet. Liquid is drawn up or “wicked” into these pathways through capillary action and rupture the interparticulate bonds causing the tablet to break apart. 10Deformation: Deformation During tablet compression Disintegrant particles get deformed and these deformed particles get into their normal structure when they come into contact with aqueous media. This increase in size of the deformed particles produce a breakup of the tablet. 11Repulsion: Repulsion 12MECHANISM OF SUPERDISINTEGRANTS : MECHANISM OF SUPERDISINTEGRANTS Super disintegrants Trade name Class Mechanism Crosscarmellose Ac-Di-Sol Nymce Cross linked cellulose Swells 4-8 fold in <10sec. Crosspovidone Crosspovidone Polyplasdone Crosslinked PVP Swells very little and act by capillary action. Sodium starch glycolate Explotab Primogel Crosslinked starch Swells 7-12 folds in <30 seconds Soy Polysaccharide Emcosoy Natural Swells 7-12 folds in <30 seconds Indion 414 Indion 414 Cross-linked acrylic copolymer Remarkable swelling tendency -No lump formation 13FACTORS AFFECTING SUPERDISINTEGRANTS: FACTORS AFFECTING SUPERDISINTEGRANTS Effect of fillers Effect of binder Effect of lubricants Effect of surfactants:- SURFACTANTS REMARKS Sodium lauryl sulfate Good-various drugs Poor-various drugs Polysorbate 20 Good Polysorbate 40 and 60 Poor Polysorbate 80 Good Tweens Poor Poly ethylene glycol Poor (GOOD- decrease in disintegration time, POOR- increase in disintegration time) 14METHOD OF ADDITION OF SUPERDISINTEGRANTS: METHOD OF ADDITION OF SUPERDISINTEGRANTS There are two methods of incorporating disintegrating agents into the tablet:- Internal Addition ( Intragranular ) II. External Addition (Extra granular) III. Partly Internal and External 15COMPARATIVE STUDY OF CURRENT SUPERDISINTEGRANTS: COMPARATIVE STUDY OF CURRENT SUPERDISINTEGRANTS 1. Croscarmellose Sodium :- Synonyms: (Ac-Di-Sol) Ac-Di-Sol super disintegrant facilitates rapid disintegration and drug dissolution at low use levels in tablets, capsules, granules, and other rapidly disintegrating dosage forms. Ac-Di-Sol is recognized for superior quality, consistency, and stability and is the standard by which super disintegrants are compared. Croscarmellose sodium is a cross linked polymer of carboxymethyl cellulose sodium. 16PowerPoint Presentation: Cross linking makes it an insoluble, hydrophilic, highly absorbent material, resulting in excellent swelling properties and its unique fibrous nature gives it excellent water wicking capabilities. Croscarmellose sodium provides superior drug dissolution and disintegration characteristics, thus improving bioavailability of formulations. 17PowerPoint Presentation: Typical Properties of Ac-Di-Sol: - Typical Average Particle Size NMT 2%200 mesh NMT 10%325 mesh PH 5.9 - 7.0 Degree of Substitution 0.63 -0.85 Settling Volume (ml) 10 – 30 Water Soluble Substances (%) NMT 5.5 Loss on Drying (%) NMT 6.0 18PowerPoint Presentation: Applications: - In tablet formulations, croscarmellose sodium may be used in both direct-compression and wet-granulation processes. -When used in wet granulations the croscarmellose sodium is best added in both the wet and dry stages of the process (intra- and extra granularly) so that the wicking and swelling ability of the disintegrant is best utilized. - Concentrations of up to 5% w/w of croscarmellose sodium may be used as a tablet disintegrant although normally 2% w/w is used in tablets prepared by direct compression and 3% w/w in tablets prepared by a wet-granulation process 19PowerPoint Presentation: 2. CROSPOVIDONE,NF :- The insoluble grades of Kollidon (Crospovidone) are manufactured by apolymerization process that yields crosslinked insoluble polyvinylpyrrolidone in the form of a “popcorn” polymer. The polymerisation is performed using anaqueous system. No organic solvents are involved at any stage . Crospovidone, NF, is a synthetic, insoluble but rapidly swellable, cross-linked homopolymer of N-vinyl-2-pyrrolidone 20PowerPoint Presentation: Product Range: Polyplasdone XL: Polymer has the largest average particle size (100-130 μ) and provides the fastest disintegration. Polyplasdone XL-10: Polymer has a finer average particle size (30-50 μ), which enhances content uniformity in the formulation of small tablets (less than 300 mg) and in intragranular applications while still providing rapid disintegration. Polyplasdone INF-10: Polymer has the finest average particle size (5-10 μ) of the Polyplasdone grades and is a highly adsorptive material. 21Features and Benefit of various grade crosspovidone: Features and Benefit of various grade crosspovidone Features Benefits Two particle sizes for disintegration ( Polyplasdone XL & XL-10) - Polyplasdone XL-10 disintegrant also gives smoother mouth feel in quick dissolve and chewable formulations compared to other disintegrants with larger particle size. Granular particles -Provides good flow properties during tablet manufacturing. Porous particle morphology -Swells rapidly and wicks water into the particle and tablet by capillary action, hence providing fast disintegration at low use level. -Highly compressible material providing hard, non-friable tablets. Excellent for use with poorly compressible drug actives. Non-gelling - Completely insoluble with relatively high cross-link density. -Does not form gels that can impede disintegration, dissolution and drug release. -Excellent disintegration performance even after cycles of wetting and drying. 22Chemistry : Chemistry Chemical Description Polyvinylpolypyrrolidone , pharmaceutical grade CAS Registry No. 9003-39-8 CAS Registry Name 2-Pyrrolidinone, 1-ethenyl, homopolymer Chemical Formula (C6H9NO)n Synonyms Crosslinked polyvinylpyrrolidone (PVP), Insoluble PVP, Polyvinylpolypyrrolidone (PVPP), Crospovidone , Crospovidonum 23PHYSICAL PROPERTIES: PHYSICAL PROPERTIES Solubility &Viscosity Swelling & Hydration Particle Size & Particle Size Distribution Flow Property 24Swelling & Hydration :- Fig.shows the difference in swell volume under acidic conditions (pH 1.5 and 5.0) compared to neutral pH forPolyplasdone disintegrants and other common super disintegrants. :- : Swelling & H y dration :- Fig. shows the difference in swell volume under acidic conditions (pH 1.5 and 5.0) compared to neutral pH forPolyplasdone disintegrants and other common super disintegrants . :- 25PowerPoint Presentation: Particle Size & Particle Size Distribution:- Products Typical average partical size Polyplasdone XL 100 – 130 Polyplasdone XL-10 30 – 50 Polyplasdone INF-10 5 – 10 Polyplasdone Crospovidone is available in 3 particle sizes for optimum performance . 26PowerPoint Presentation: Flow Property Polyplasdone XL and XL-10 polymers have good flow properties . Property Polyplasdone INF-10 XL-10 XL Angle of Repose (degrees) 41 30 35 Flowability Index 45 50 47 27PowerPoint Presentation: Properties Polyplasdone INF-10 XL-10 XL Appearance White to off white, free-flowing powder White to off white, free-flowing powder White to off white, free-flowing powder Bulk Density (g/cm3)* 0.4 0.3 0.3 Tap Density (g/cm3)* (1000 taps) 0.5 0.5 0.4 Specific Surface Area (m2/g)* 2.0-2.5 1.2-1.4 0.6-0.8 % Adsorptive Activity 30-50 ------ ---- pH (1g/100 ml DI water) 5.0 - 8.0 5.0 - 8.0 5.0 - 8.0 % Moisture 5.0 Maximum 5.0 Maximum 5.0 Maximum % Ash 0.1 Maximum 0.1 Maximum 0.1 Maximum Heavy Metals (ppm, as Lead) 10 Maximum 10 Maximum 10 Maximum Product Specifications & Typical Properties 28PowerPoint Presentation: Pharmaceutical applications of Crospovidone:- Polyplasdone XL-10 disintegrant is well suited for quick dissolve and chewable tablets as it provides rapid disintegration, smooth mouth feel and hard tablets with low friability. Depending on the structure of the active, Polyplasdone polymers can be used to improve solubility, and hence, enhance bioavailability. Polyplasdone INF-10 polymer absorbs water, gases and toxins and is therefore used in some countries to treat gastrointestinal disorders and as an anti-diarrheal agent in human and veterinary applications . 29 Research Article : Research Article Formulation, Evaluation and Comparision of Fast-Dissolving Tablet of Nimesulide by Using Crospovidone as Superdisintegrant Method-Direct Compression . Concentration-2%,4%,8%,12% Compared with markated product 30PowerPoint Presentation: Formulation of fast-dissolving tablet of Nimesulide Ingredients(mg) F1 F2 F3 F4 Nimesulide 100 100 100 100 Crospovidone 4 8 16 24 MCC 50 50 50 50 D-manitol 30 26 18 10 Aspartame 10 10 10 10 Talc 4 4 4 4 Mg.stearate 2 2 2 2 31In vitro dissolution profile: In vitro dissolution profile 32PowerPoint Presentation: 3. Sodium Starch Glycolate:- Nonproprietary name:- BP.SodiumStarchGlycolate PhEur: Carboxymethylamylum natricum USP: Sodium starch glycolate Synonyms:- Carboxymethyl starch, Explotab,Primojel Chemical name:- Sodiumcarboxymethylstarch [9063-38-1] Moleculer weight:- 500000-1000000 33PowerPoint Presentation: Disintegration Mechanism:- Primojel promotes water penetration into the tablet and develops a disintegration force needed to push the particles apart. Eg. dicalcium phosphate dihydrate High swelling capacity results in its high disintegration rate and efficiency. Suitable for a variety of tablet and capsule formulations. 34Water uptake of loose disintegrant powder: Water uptake of loose disintegrant powder 35PowerPoint Presentation: Drug dissolution rate: After the fast disintegration of tablets or capsules containing Primojel, the active ingredient will dissolve rapidly as a result of the hydrophilic nature of Primojel, and the counteracting effect of Primojel on the effects that hydrophobic lubricants have on drug dissolution rate and in vivo drug absorbtion rate. Stability and storage condition: Sodium starch glycolate is stable and should be stored in well closed container to protect it wide variation in humidity and temperature that may cause caking . 36PowerPoint Presentation: Application in pharmaceutical formulation:- Sodium starch glycolate is widely used in oral pharmaceuticals as a disintegrant in capsule and tablet formulation. It is commonly used in tablets prepared by either direct compression or wet granulation process. The usual concentration employed in a formulation is between 2-8% with the optimum concentration about 4% although in many cases 2% is sufficient. Increasing the tablet compression pressure also appears to have no effect on disintegration time. 37 Newer Super Disintegrants : Newer Super Disintegrants Isapghula Husk:- It is a natural substance as disintegrant. It consists of dried seeds of the plant known as plantago ovata. It contains mucilage which is present in the epidermis of the seeds. The mucilage is used as binding agent in the granulation of material for compressed tablets. A Plantago ovata seed husk has high swellability and gives uniform and slightly viscous solution hence it is used as thickening and suspending agent. 38PowerPoint Presentation: Research Article Effect of Natural and Artificial Superdisintegrants in the Formulation of Fast Dissolving Diclofenac Tablet In the present study, the effects of a natural superdisintegrant Plantago ovata and synthetic superdisintegrants like sodium starch glycolate (SSG), Crosspovidone and Croscarmellose sodium (Ac-di-sol) were compared in the formulations of fast dissolving tablets (FDT). Method- direct compression method. -Evaluation parameter-weight variation, hardness, thickness, disintegration time, wetting time, water absorption ratio, -In vitro disper-sion, In vivo disintegration time, friability and dissolution. 39PowerPoint Presentation: Swelling index -To compare the swelling property of Plantago ovata with Sodium starch glycolate (SSG), Crosspovidone (CP) and Ac-di-sol. Among all the super disintegrants, Plantago ovata showed the highest swelling index. Diclofenac is a non-steroidal anti-inflammatory drug and used for in the treatment of rheumatoid arthritis, osteoarthritis, and ankylosing spondilitis. This natural superdisintegrants showed better disintegrating property than the most widely used synthetic super disintegrants like SSG, Crosspovidone and Ac-di-sol in the formulations 40PowerPoint Presentation: Ion exchange resins( Indion 414):- The INDION 414 has been used as a superdisintegrant for ODT. It is chemically cross-linked polyacrylic, with a functional group of – COO – and the standard ionic form is K+. It has a high water uptake capacity. Indion 414, an ion exchange resin, as a new superdisintegrant for pharmaceutical dosage forms. Indion 414 is a pharmaceutical grade weak acid cation exchange resin. Model drugs belonging to various classes were taste masked and formulated into palatable mouth dissolve tablets. Experiments were carried out to evaluate the disintegrant property of Indion 414 by incorporating Indion 414 in fast disintegrating dosage form like mouth dissolve tablets. 41PowerPoint Presentation: SPECIFICATIONS FOR INDION 414:- Parameter Specification Particle size distribution Retained on 100 BSS mesh 1% maximum Retained on 100 BSS mesh 30% maximum Moisture content 10% maximum Sodium content 0.2% maximum Potassium content 20.6 to 25.1% pH of 10% slurry 7-9 Iron content, as Fe 100 ppm, maximum Heavy metals, as Pb 20 ppm, maximum Arsenic content 3 ppm maximum 42Research Article: Research Article Indion 414 as superdisintegrant in formulation of melt in mouth meloxicam tablets These delivery systems either dissolve or disintegrate in the mouth rapidly, without requiring any water to aid in swallowing so it is easy to take for any age patient, regardless of time or place. Indion 414 is a high-purity pharmaceutical grade ion exchange resin and is safe for oral consumption, cost-effective and is easily available. The present work was aimed to formulate and evaluate efficacy of Indion 414 as superdisintegrant in formulation of melt in mouth meloxicam tablets. FTIR spectra of meloxicam and Indion 414 was obtained to study the compatibility with Indion 414. 43PowerPoint Presentation: Formulation of melt in mouth meloxicam tablets Ingredients (mg) Formulations F1 F2 F3 F4 Meloxicam 15 15 15 15 Indion 5 - - - Crospovidone - 5 - - Croscarmallose sodium - - 5 - Sodium Starch Glycolate - - - 5 Magnesium stearate 2 2 2 2 Talc 4 4 4 4 44PATENT: PATENT Patent for aminoalkanoylated cellulose as a superdisintegrant. The inventors are N.H. Aloorkar and M.S. Bhatia. The patent application number is 2610/MUM/2010 A. The international classification numbers are A61K31/00 and A61K9/00. 45Superdisintegrant Performance – A Case Study with Croscarmellose Sodium : Superdisintegrant Performance – A Case Study with Croscarmellose Sodium Purpose:- To investigate factors influencing croscarmellose sodium functionality with special emphasis on developing a discriminating model tablet formulation to evaluate product brand-to-brand variability. Parameter Studied:- particle size distribution, water uptake, and swelling properties of five brands of croscarmellose sodium in either neutral water or 0.1 N HCl 46PowerPoint Presentation: Observation:- Media with acidic pH had a negative impact, but to different extents, on both the water uptake and swelling of all croscarmellose sodium brands due to the presence of carboxymethyl sodium substituents. A tablet matrix composed of lactose (75% w/w) and dicalcium phosphate (25% wt/wt) was used to compare the functional equivalency of the five brands of croscarmellose sodium. The tablet disintegration times were inversely proportional to the swelling ability of superdisintegrant in the testing medium regardless of medium temperature and disintegrant concentration. 47PowerPoint Presentation: Conclusion:- The particle size, total degree of substitution, and the ratio of basic to acidic substituents are important factors that should be considered during product optimization. The tablet matrix composed of lactose and dicalcium phosphate at a weight ratio of 3:1 can be used as a model formulation for product lot-to-lot consistency and product brand-to-brand comparison purposes. 48CONCLUSION: CONCLUSION There are many superdisintegrants, which show superior disintegration, the search for newer disintegrants is ongoing and researchers are experimenting with modified natural products, like formalincasein, chitin, chitosan, polymerized agar acrylamide, xylan, smecta, key-jo-clay, crosslinked carboxymethylguar and modified tapioca starch. Studies have suggested that the water insoluble superdisintegrants show better disintegration property than the slightly water soluble agents,since they do not have a tendency to swell. Superdisintegrants that tend to swell show slight retardation of the disintegration property due to formation of viscous barrier. 49PowerPoint Presentation: There is no particular upper limit regarding the amount of superdisintegrant as long as the mechanical properties of the tablet are compatible with its intended use. The superdisintegrant may be used alone or in combination with other superdisintegrants. Thus, overviews of various types of superdisintegrants which are available have been discussed. The ease of availability of these agents and the simplicity in the direct compression process suggest that their use would be a more economic alternative in the preparation of ODT than the sophisticated and patented techniques . 50 REFERENCES: REFERENCES Anisal Quadir and Karl Kolter , Comparative study of current Superdisintegrants , Excipients performance, supplement to pharmaceutical technology , 2006, 38-39. Wayne Camarco , Dipan ray and Ann Druther , Selecting super disintegrating for orally disintegrating formulation, Excipients performance , supplement to pharmaceutical technology 2006, 28-32 Karl Kolter Comparative Study of Current Superdisintegrants , Pharm Technol 2007 51PowerPoint Presentation: ArthurH.Kibbe, In, Handbook of pharmaceutical excipients III rd ed n p.no.160 Gohel MC, Jogani PD. A review of co-processed directly compressibleexcipients. J Pharm Pharm Sci .2005,8,76Y,93. 11. Amin Purnima, Prabu Namita, Wadhwani Anita, Ind. Jour. Phar.Sci , 2006,68(1) ,117-119 Amin Purnima, Prabunamita, Wadhwani Anita Indion 414 as super disintegrantsin formulation of mouth dissolve tablet, Indian j. Pharm. Sci . 2006,68 (1), 117-119 52PowerPoint Presentation: International Journal of Pharmaceutical Sciences and Drug Research 2009; 1(3): 172-175 172 International Journal of Pharmaceutical Research 2009 1(4) 63-67 Prajapati S.T., Prajapati V.D., Acharya S.R. and Patel C.N., Characterization of disintegration properties of plantago ovata Mucilage in the formulation of Dispersible tablet, Ind.j.pharm.Edu. And Rese . 2006, 40(3), 208-211. 53PowerPoint Presentation: THANK YOU 54 You do not have the permission to view this presentation. In order to view it, please contact the author of the presentation.