Unfortunately most superdisintegrants are hygroscopic and readily absorb moisture, which generally rules them out for drugs that are moisturesensitive. Paracetamol employing superdisintegrants introduction oral route is the most preferred route for administration of various drugs because it is regarded as safest, most convenient and economical route1. Rapid disintegrating tablets, superdisintegrants, disintegrants. Improvement by super disintegrants of the properties of tablets containing lactose, prepared by wet granulation. Superdisintegrants disintegrating agents are substances routinely included in the tablet formulations to aid in the break up of the compacted mass when it is put into a fluid. Super disintegrants tablet pharmacy pharmaceutical. Roquette has developed a versatile range of standard disintegration excipients. Mechanism of superdisintegrants superdisintegrants provide quick disintegration. The identification and control of the critical material i. The mechanism of action is a capillary action with a secondary swelling effect. The effects of crospovidone and croscarmellose sodium as. Mrudula hb, derle dv, mechanism of disintegrant action of polacrilin potassium. The electric repulsive forces between particles are the mechanism of disintegration and water is required for it.
Comparison of superdisintegrants in orally disintegrating. The choice of superdisintegrant for a tablet formulation depends largely on the nature of the drug being used. They both are known to have high efficiency in the use of low concentration 25% bb6. Matsya giri 3 1 department of pharmacology, 2 department of pharmacognosy and 3 department of pharmaceutics, swami vivekananda institute of pharmaceutical. Swelling or wicking, acta pharmaceutica sinica b 2012. Incorporation of superdisintegrants at intra and extra granulation stepsin this process part of superdisintegrants are added to intragranular and a part to extragranules. Crospovidones are considerably more compressible relative to other superdisintegrants 79. Superdisintegrants function principally by swelling on absorbing water.
The basic approach used in the formulation of the tablet is the use of superdisintegrants like croscarmellose, sodium starch glycolate, and crospovidone, etc. Effect of a disintegration mechanism on wetting, water. Coprocessed superdisintegrants in recent years drug formulation scientists have recognized that singlecomponent excipients do not always provide the requisite performance to allow certain active pharmaceutical ingredients to be formulated or manufactured adequately. Effect of superdisintegrants and their mode of incorporation. Levocetirizine orodispersible tablet by direct compression. Superdisintegrants are more effective at lower concentrations with greater disintegrating efficiency and mechanical strength 3. Superdisintegrants include sodium starch glycolate, croscarmellose sodium. Superdisintegrants are generally used at a low level in the solid dosage form, typically 1 10 % by weight relative to the total weight of the dosage unit. Orally disintegrating tablets, superdisintegrants,patient compliance. Design of mouth dissolving tablets of rosiglitazone. International journal of pharmaceutics vol 577, 15 march. Peters institute of pharmaceutical sciences, vidyanagar. The article cites the various types of superdisintegrants with their characteristics, mechanism of disintegration and their applications in the formulation of odt. In this mechanism, superdisintegrants swell when they come in contact with water e.
Tablets and hard gelatin capsules constitute a major portion of drug delivery systems that are currently available. The effect of different superdisintegrants and their concentrations on the dissolution of topiramate immediate release tablets v a. The effect of different superdisintegrants and their. Crospovidone is a disintegrating agent at the 2 5% level and is an effective binder disintegrant in tablets prepared using wet granulation. Scribd is the worlds largest social reading and publishing site. This method usually produces better results and more complete mechanism of action. Superdisintegrants provide quick disintegration due to combined effect of swelling and water absorption by the formulation. The penetration of water from the coating solution into the tablet matrix resulted in significant changes in physical properties of the coated tablet cores, such as residual. Effective superdisintegrants provide improved compressibility, compatibility and have no negative impact on the mechanical strength of formulations containing highdose drugs.
The aims of this study are 1 to compare the disintegration efficiency, and 2 to develop a discriminating test model for the 3 classes of superdisintegrants represented by acdisol, primojel, and polyplasdone xl10. Above 8%, disintegration times may actually increase due to gelling and its subsequent viscosity producing effects. Comparison of superdisintegrants in orally disintegrating tablets. Mechanism of superdisintegrants super disintegrants trade name class mechanism crosscarmellose acdisol nymce cross linked cellulose swells 48 fold in superdisintegrants. Mechanism of superdisintegrants there are four major mechanisms for tablets disintegration as follows. Effective superdisintegrants provide improved compressibility, compatibility and have no negative impact on the mechanical strength. Review of disintegrants and the disintegration phenomena parind mahendrakumar desai, celine valeria liew. Study of disintegration mechanisms the disintegration of tablets is a fundamental previous step for the liberation of the active. Also the concentration of the superdisintegrants and the effect of other ingredients like diluents used in the formulation of the tablets in promoting disintegration are. In many cases, it was realized that a synergistic combination of mechanisms had acted together. Effect of superdisintegrants on dissolution of cationic drugs article pdf available in dissolution technologies 152 may 2008 with 973 reads how we measure reads. Other superdisintegrants have a lower crosslink density and, as a result, form gels when fully hydrated, particularly at the higher use levels in odt formulations.
Superdisintegrants includesodium starchglycolate, croscarmellose. Mechanism of action of superdisintegrants a by capillary action disintegration by capillary action is always the first step. Water penetration rate and rate of disintegration force development are. Surface dissolution uv imaging for characterization of superdisintegrants and their impact on drug dissolution. Superdisintegrants international journal of pharmaceutical. As superdisintegrants swell more extensively in basic compared to acidic conditions due to their ionization rojas et al.
In formulation, the concentration of superdisintegrant can be up to 1020%, depends on the dose and characteristic of active ingredient and also the. Superdisintegrants are generally used at a low level in the solid dosage form, typically 1 10 % by weight relative to the total weight. Poor solubility the solubility of the key component in a tablet preparation can affect both the rate and the mechanism of action of tablet disintegration. Superdisintegrants in the development of orally disintegrating tablets. Properties another mechanism of disintegration attempts to explain the of superdisintegrants with special emphasis on correlating these functional properties to disintegrate efficiency and drug release rate. Pdf the desire of improved palatability in orally administered products has prompted the development of numerous. Disintegration by capillary action is always the first step. Functionality comparison of 3 classes of superdisintegrants. Poor solubility the solubility of the major component in a tablet formulation can affect both the rate and the mechanism of tablet disintegration. Superdisintegrants are used to improve the efficacy of solid dosage forms. Review article escalation of drug effectiveness by.
Academic sciencesasian journal of pharmaceutical and clinical. Tablets with high porosity show poor disintegration due to lack of adequate swelling force. Download citation disintegrants and superdisintegrants. International research journal of pharmaceutical and. Criteria for drug selection examples of superdisintegrants 1. Hence disintegration has major role for facilitating drug activity. The mechanism and the extent of sorption of water molecules by tablets containing superdisintegrants and microcrystalline cellulose, following the aqueous film coating of formulated tablets, were investigated. On contact with water the superdisintegrants swell, hydrate, change volume or form and produce a disruptive change in the tablet.
Review of disintegrants and the disintegration phenomena. Disintegrants and superdisintegrants excipients for. Pdf recent trends in role of superdisintegrants to formulation of. Water soluble materials tend to dissolve rather than disintegrate, while insoluble materials generally produce rapidly disintegrating tablets. The tablet disintegrates due to generation of pressure within the tablet. Mechanism of superdisintegrants super disintegrants trade name class mechanism crosscarmellose acdisol nymce cross linked cellulose swells 48 fold in of incorporation of superdisintegrants as shown in table 2. A disintegrant used in granulated formulation processes can be more effective if used both intragranularly.
The objective of this study was to evaluate the functionality and performance of three types of commonly used commercial superdisintegrants, crosslinked croscarmellose sodium xlcmc, crospovidone, and sodium starch glycolate ssg, in the application of odts. Due to swelling of superdisintegrants, the wetted surface of the carrier increases, this promotes the wettability and dispersibility of the system, thus enhancing. Bolhuis and coworkers 5 studied a series of experimental ssg having a relative degree of crosslinking dxl of 0. The improvement of tablet disintegration also has been observed through predictable swelling without gel formation. Examples of superdisintegrants are crosscarmelose, crospovidone, and sodium starch glycolate, which are a crosslinked cellulose, crosslinked polymer, and a crosslinked starch, respectively.
Pdf superdisintegrants in the development of orally. The main mechanism of action of pregelatinized starch is through swelling. The therapeutic activity of these formulations is obtained through a typical manner like disintegration followed by dissolution. For example, the solubility of the drug component could affect the rate and mechanism of tablet disintegration. Due to disintegrating particleparticle repulsive forces 5. The commonly used superdisintegrants are crospovidone and croscarmellose sodium. Swelling is believed to be a mechanism in which certain disintegrating agents such as starch impart the disintegrating effect.
Pdf superdisintegrants in the development of orally disintegrating. Mechanism of superdisintegrants superdisintegrants provide quick disintegration due to combined effect of swelling and water absorption by the formulation. In dosage forms, solid orals gain maximum popularities, about 85%, because of many advantages over others. Hence disintegration has major role for facilitating drug activity and thus gain popularity among other dosage forms. Another mechanism of disintegratn attempts to explain the swelling of tablet made with nonswellable disintegrants. Pdf effect of superdisintegrants on dissolution of. The following mechanisms are responsible for the breaking of. Perhaps the most widely accepted general mechanism of action for tablet disintegration is swelling. Another mechanism of disintegration attempts to explain. Surface dissolution uv imaging for characterization of. Dissolution mechanism mechanism 56,57 the active constituents must be released from the tablet as efficiently as possible to allow its rapid action.
There are seven major mechanisms for tablets disintegration as follows 1. Aug 26, 1983 improvement by super disintegrants of the properties of tablets containing lactose, prepared by wet granulation. Mechanism of disintegration by superdisintegrants there are five major mechanisms for tablet disintegration as follows. The following mechanisms are responsible for the breaking of tablets and bulk contents of capsules into small pieces. Presence of superdisintegrants in oral solid dosage forms is essential for fast tablet disintegration and improved drug dissolution. International research journal of pharmaceutical and applied. In this case, lowest dt for 1% extragranular incorporation of superdisintegrants was 6. The phosphorus content of potato starch is increased by approximately 0. Effect of a disintegration mechanism on wetting, water absorption, and disintegration time of orodispersible tablets pabari rm, ramtoola z school of pharmacy, royal college of surgeons in ireland, 123, st. Unlike other superdisintegrants which are either poorly compressible or noncompressible, crospovidone disintegrants are highly compressible materials as a result. Academic sciencesasian journal of pharmaceutical and. Improvement by super disintegrants of the properties of. Water penetration rate and rate of disintegration force development are generally positively related to disintegrate.
Guyothermann has proposed a particle repulsion theory based on the observation that nonswelling particle also cause disintegration of tablets. When we put the tablet into suitable aqueous medium, the medium penetrates into the tablet and replaces the air adsorbed on the particles, which weakens the intermolecular bond and breaks the. Primarily, this is because almost all disintegrants swell to some extent. Pdf disintegrating agents are substances routinely included in the tablet. Mechanism of superdisintegrants free download as word doc. On the other hand, sufficient swelling force is exerted in the tablet with low porosity. The oral route is the most convenient route for administration of solid dosage form, about 85% of solid dosage administered by oral route because of advantages over others. International journal of biopharmaceutics superdisintegrants. Disintegrants and superdisintegrants are used in tablets and capsules to ensure the rapid break down into their primary particles, facilitating the dissolution or release of the active ingredients. Dec 12, 2005 the aims of this study are 1 to compare the disintegration efficiency, and 2 to develop a discriminating test model for the 3 classes of superdisintegrants represented by acdisol, primojel, and polyplasdone xl10. Superdisintegrants generally are used at a low level in the solid dosage form, typically 110% by weight relative to the total weight of the dosage unit. Mechanism of superdisintegrants tablet pharmacy porosity. Mechanism of disintegrations by superdisintegrants there are five major mechanisms for tablet disintegration as follows.
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