The therapeutic activity of these formulations is obtained through a typical manner like disintegration followed by dissolution. Spironolactone is a drug derived from sterols that exhibits an incomplete oral absorption due to its low water solubility and slow dissolution rate. As tableting becomes more advanced, formulators prefer direct compression blends. The functionality and performance of three types of commercial superdisintegrants were evaluated in the application of orally disintegrating tablets. Dissolution of poorly soluble drugs can be improved by wetmilling their suspensions and drying the suspensions to form nanocomposites. Mechanisms for tablet disintegration are swelling, porosity and capillary action. International journal of pharmaceutical sciences and research 2010. 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. Superdisintegrants, utility in dosage forms journal of. Clove oil9 provide symptomatic relief from nausea and vomiting, good. Due to swelling of superdisintegrants, the wetted surface of the carrier increases, this promotes the wettability and dispersibility of the system, thus.
Orally disintegrating tablets8 provides immediate action, convenient dosing and improves patient compliance. International journal of biopharmaceutics superdisintegrants. Incorporation of superdisintegrants at intra and extra granulation stepsin this process part of superdisintegrants are added to intragranular and a part to extragranules. Various superdisintegrant along with their mechanism of. Similarly, various natural substances like gum karaya, modified starch and agar have been used as. The global superdisintegrants market size was valued at around usd 258. The commonly used superdisintegrants are crospovidone and croscarmellose sodium. Tablets with high porosity show poor disintegration due to lack of adequateswelling force. The polymer has a small particle size distribution that imparts a smooth mouth feel to dissolve quickly. Effective superdisintegrants provide improved compressibility, compatibility and have no negative impact on the mechanical strength of formulations containing highdose drugs.
However, they are of limited use when tablets are prepared with crushing strength of more than 4 kg 1819. The effects of crospovidone and croscarmellose sodium as. John c carter,carter pharmaceutical consulting, inc. International research journal of pharmaceutical and. Superdisintegrants are the materials primarily used in the pharmaceutical preparation of tabl. Formulation and evaluation of orally disintegrating. This method usually produces better results and more complete mechanism of action. Design of orodispersible tablets of losartan potassium. In this mechanism, superdisintegrants swell when they come in contact with water e. 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. Disintegrants and superdisintegrants excipients for. Formulation development, evaluation and comparative study. The following mechanisms are responsible for the breaking of. Hence disintegration has major role for facilitating drug activity.
On analyzing the behavior of disintegration time in the oral cavity as well as wetting time by surface free energy we came to know. Superdisintegrants are used to improve the efficacy of solid dosage forms. International research journal of pharmaceutical and applied sciences irjpas available online at. Mechanism of superdisintegrants tablet pharmacy porosity. Comparative study on effect of natural and synthetic super. The present work was aimed at formulation development, evaluation and comparative study of the effects of superdisintegrants in cefixime 50 mg oral disintegrating tablets. Mechanism of superdisintegrants super disintegrants trade name class mechanism crosscarmellose acdisol nymce cross linked cellulose swells 48 fold in free download as word doc. They both are known to have high efficiency in the use of low concentration 25% bb6. Swelling is believed to be a mechanism in which certain disintegrating agents such as starch impart the disintegrating effect. Peters institute of pharmaceutical sciences, vidyanagar. With improved bioavailability vishwakarma, divya, patel, natvarlal, patel, kanu on.
In spite of the increased focus and interest generated in the area of controlled release and targeted drug delivery system in recent years, tablet dosage forms that are intended to be swallowed whole, disintegrate, and release their medicaments rapidly in the gastrointestinal tract still remain the formulation of choice from both a manufacturing as well as a patient. On analyzing the behavior of disintegration time in the oral cavity as well as wetting time by surface free energy we came to know, that for a faster wetting a molecule should have high polar component of surface free energy and the agents which meet these special requirements are called as superdisintegrants. Effect of superdisintegrants and their mode of incorporation on. Both superdisintegrants are waterinsoluble and swell in water. 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. Superdisintegrants are generally used at a low level in the solid dosage form, typically 1 10 % by weight relative to the total weight. Unlike other superdisintegrants, which rely principally on swelling for disintegration, polyplasdone crospovidones use a combination of mechanisms to provide rapid disintegration. Although polyplasdone crospovidones swell by 95% to 120% upon contact with water, swelling is not the only mechanism for tablet disintegration. Superdisintegrants shrivastava priyanka and sethi vandana department of pharmaceutics, lloyd college of pharmacy, greater noida, u. Fast dissolving tablet of metoprolol tartrate using superdisintegrants. Pdf superdisintegrants in the development of orally. Pdf orodispersible tablets disintegrate andor dissolve rapidly in the saliva. From table 2 and 3 it is clear that nature and method of incorporation of superdisintegrants has a great effect on the dt of carbamazipine tablets.
Dissolution mechanism mechanism 56,57 the active constituents must be released from the tablet as efficiently as possible to allow its rapid action. Tablets and capsules which need rapid disintegration, the inclusion of the right disintegrant is a prerequisite for optimal bioavailability. Superdisintegrants are generally used at a low level in the solid dosage form, typically 1. The superdisintegrants used for the present study were sodium starch.
This is achieved by decreasing the disintegration time which in turn enhances drug dissolution rate. Fast dissolving tablet of metoprolol tartrate using. Pdf the desire of improved palatability in orally administered products has. The carboxymethyl group induces hydrophilicity while crosslinking minimizes solubility in. There are four major mechanisms for tablets disintegration as follows swelling.
By swelling in contact with water, the adhesiveness of other ingredients in a tablet is overcome causing the tablet to fall apart. The choice of superdisintegrant for a tablet formulation depends largely on the nature of the drug being used. Perhaps the most widely accepted general mechanism of action for tablet. Different classes of dispersants and their concentration can affect both nanoparticle aggregation in the suspensions and drug dissolution from the nanocomposites. Comparison of superdisintegrants in orally disintegrating. Functional assessment of four types of disintegrants and. Using a digital video camera to examine the disintegration process of tablets containing the same wtwt percentage concentration of the disintegrants, ac. Pdf superdisintegrants in the development of orally disintegrating. Superdisintegrants in the development of orally disintegrating tablets. The prepared granules of different formulations were free.
Scribd is the worlds largest social reading and publishing site. Superdisintegrants improve disintegration efficiency and decrease use levels compared to traditional disintegrants. Tablets and hard gelatin capsules constitute a major portion of drug delivery systems that are currently available. Ssg is a sodium salt of a carboxymethyl ether of starch fig. Although not all effective disintegrants swell in contact with water, swelling is believed to be a mechanism in which certain disintegrating agents such as starch impart the disintegrating effect. It acts by wicking, swelling and possibly some deformation recovery. The article cites the various types of superdisintegrants with their characteristics, mechanism of disintegration and their applications in the formulation of odt. In general, all of these provide rapid disintegration at low use levels in both wet and dry granulations and direct compression tablet processes. 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. Thus, a new disintegrant class called superdisintegrants has emerged in the market. Roquette has developed a versatile range of standard disintegration excipients.
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. Mechanism of superdisintegrants free download as word doc. Superdisintegrants which were added to the drug formulations facilitated the breakup or disintegration of tablet content into smaller particles that dissolved more rapidly. Table 1 presents the physical properties of the two superdisintegrants quadir and kolter, 2006, shah and augsburger, 2001, shah and augsburger, 2002. The three most common classes of superdisintegrants are.
In this study, formulations of spironolactone with four disintegrants named as croscarmellose sodium. In formulation, the concentration of superdisintegrant can be up to 1020%, depends on the dose and characteristic of active ingredient and also the. The following mechanisms are responsible for the breaking of tablets and bulk contents of capsules into small pieces. This technique is useful for preparation of odt because of the availability of improved excipients especially the superdisintegrants. The influence of superdisintegrants on immediate release. Anup megotia, meenu nagpal, upendra k jain, varun dept. Due to disintegrating particleparticle repulsive forces 5. Crospovidones are considerably more compressible relative to other superdisintegrants 79. Perhaps the most widely accepted general mechanism of action for tablet disintegration is swelling. Department of pharmaceutics, bapatla college of pharmacy, bapatla, andhra pradesh, india. Mechanism of disintegrations by superdisintegrants there are five major mechanisms for tablet disintegration as follows.
Taste masking by ion exchange resin and its new application. 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. The rate of swelling is highest among all the superdisintegrants and is effective at %. Hence disintegration has major role for facilitating drug activity and thus gain popularity among other dosage forms. 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. It is free flowing, completely soluble, neutral polymer composed of sugar units and is approved for use in food. The objective of the present article is to highlight the various kinds of superdisintegrants along with their role in tablet disintegration and drug release, which are being used in the. In dosage forms, solid orals gain maximum popularities, about 85%, because of many advantages over others.