Oral Dispersible Tablets

The Oral route is the most convenient and accepted for drug administration. Oral route still preferred way of administration of therapeutic agents used to produce systemic effects, and provides high patient compliance. 1 The Demand for formulation of oral disintegrating tablets (ODTs) has increase significantly as it has good impact on the patient compliance. These dosage form are appreciated by populations who have difficulty in the swallowing , called Dysphagia ( difficulty in swallowing ). 2 It is also called as orally disintegrating tablets, fast disintegrating tablets , fast dissolving tablets, mouth dissolving tablets, porous tablets and rapimelts. United states pharmacopoeia also approved these dosage forms as ODTs. European pharmacopoeia has also used the term orodispersible tablet for those tablets which are disperses within 3 minutes in mouth before swallowing. 3 Oral dispersible tablets are some like conventional tablets used in formulation, which

Abstract: The purpose of the present study was to develop oral dispersible tablets containing prednisolone (PDS)-loaded chitosan nanoparticles using microcrystalline cellulose (MCC 101), lactose, and croscarmellose sodium (CCS). The PDS-loaded chitosan nanoparticles were for- mulated by ionotropic external gelation technique in order to enhance the solubility of PDS in salivary pH. Prepared nanoparticles were used for the development of oral fast disintegrating tablets by direct compression method. The prepared tablets were evaluated for disintegration time (DT), in vitro drug release (DR), thickness, weight variation, drug content uniformity, friability, and hardness. The effect of concentrations of the dependent variables (MCC, lactose, CCS) on DT and in vitro DR was studied. Fast disintegrating tablets of PDS can be prepared by using MCC, CCS, and lactose with enhanced solubility of PDS. The minimum DT was found to be 15 seconds, and the maximum DR within 30 minutes was 98.50%. All independent variables selected for the study were statistically significant. Oral fast disintegrating tablets containing PDS nanoparticles could be the better choice for the pediatric patients that would result in better patient compliance. From this study, it can be concluded that fast disintegrating tablets could be a potential drug delivery technology for the management of asthma in pediatrics.

In the present work, oral dispersible tablets of cinnarizine were prepared by direct compression method with a view to enhance patient’s compliance. Five different superdisintegrants viz. crosspovidone, sodium starch glycolate, crosscarmellose sodium and low-substituted hydroxypropylcellulose (L-HPC) and pregelatinized starch were used along with microcrystalline cellulose (Avicel PH 102) and directly compressible mannitol (pearlitol SD-200) which enhances the mouth feel. Fifteen formulations having superdisintegrants at different concentration levels were prepared. These tablets were evaluated for drug content, weight variation, friability, hardness, wetting time and in vitro disintegration time. Among the formulations tablets of batch F9 containing crosspovidone (at 4.5% level) showed superior organoleptic properties along with excellent in-vitro disintegration time and drug release as compared to other formulations. It was concluded that superdisintegrants addition technique is a useful method for preparing oral dispersible tablets by direct compression method.

Amlexanox oral dispersible tablets were prepared using molecular dispersion granulation technique with micronized active due to insoluble nature of the active in water. The process is same for all batches except concentration change. The materials like Amlexanox, sodium lauryl sulfate, microcrystalline cellulose PH 101, croscarmellose sodium and crospovidone were sifted through #40 mesh and Neotame, lemon flavor, tutti frutti flavor, colloidal silicon dioxide and magnesium stearate was sifted through #60 mesh and collected separately in polyethylene bag. 21-23

 Under the pre-formulation studies API characterization and drug–excipient compatibility studies were carried out. The polymer and other excipients are selected based on the satisfactory results produced during drug- excipient compatibility studies to develop new formulation.  The invitro study showed that the formulation B 6 was ideally suitable for oral dispersible tablets.

Granisetron, a selective 5-HT3 receptor antagonist has a good safety profile but a shorter half-life hence is only suited for a multiple-dosage regimen, which increased side effects. Ion-exchange resins were extensively investigated as potential drug release modulators and the ability to get encapsulated along with drugs appeared to be a distinct advantage. Optimized conditions for drug loading using ion-exchange resins Kyron T-114 and Kyron T-134 were evaluated. The microencapsulated drug-resin complexes were incorporated into oral dispersible tablets prepared using crospovidone as a superdisintegrant. The in vitro release profile of the optimized formulation of F4 was investigated, which showed linearity of Higuchi's rate kinetic equation. The shelf life of the optimized formulation was estimated to be 6.7 y, based on accelerated stability study data obtained. The physical and dissolution 3-month stability studies with the three formulations, F4, F5 and F6, showed better disintegration times.

The need for delivering drugs to patients efficiently with minimum side effects has prompted pharmaceutical industries to be engaged in development of new drug delivery systems. Pediatric and geriatric patients find it difficult to swallow solid dosage forms like tablets. Oral dispersible tablet is solid unit dosage form. The objective of present investigation was to prepared oral dispersible tablet of Levocetirizine Dihydrochloride and Montelukast Sodium because it’s active working patients who are busy or travelling, especially those who have no access to water. This review depicts the various aspects of ODT formulation, superdisintegrants and technologies developed for ODT, along with various drugs explored, evaluation tests and marketed formulations in this field. Oral Dispersible tablets are prepared they are required to be evaluated for various parameters.

Oral dispersible tablets are also called as mouth-dissolving tablets, melt-in mouth tablets, fast dissolving tablets, rapimelts, porous tablets, quick dissolving etc. Oral dispersible tablets are those when put on tongue disintegrate instantaneously releasing the drug which dissolve or disperses in the saliva. The faster the drug into solution, quicker the absorption and onset of clinical effect. Some drugs are absorbed from the mouth, pharynx and esophagus as the saliva passes down into the stomach. In such cases, the bioavailability of drug is significantly greater than those observed from conventional tablets dosage form. The advantage of oral dissolving dosage forms are increasingly being recognized in both, industry and academics. Their growing importance was underlined recently when European pharmacopoeia adopted the term “ Orodispersible tablet” as a tablet that to be placed in the mouth where it disperses rapidly before swallowing.

Where, WO is the weight of the tablets before the test and W is the weight of the tablet after the test 45-46. Wetting time: The wetting time of the tablets was measured using simple procedure. A piece of tissue papers of 10cm diameter were placed in a petridish containing 6ml phosphate buffer 6.8. A tablet was carefully placed on the surface of the tissue paper. The time for complete wetting was measured. Three trials for each batch and standard deviation was also determined 7. Water absorption ratio (r): Water absorption ration can be calculated as

Despite of tremendous advancements in drug delivery, the oral route remains the perfect route for the administration of therapeutic agents because of low cost of therapy, ease of administration, accurate dosage, self-medication, pain avoidance, versatility, leading to high levels of patient compliance. Tablets and capsules are the most popular dosage forms. But one important drawback of such dosage forms is ‘Dysphasia’ or difficulty in swallowing. This is seen to afflict nearly 35% of the general population. This disorder is also associated with a number of conditions like:

The convenience of administration and improved patients compliance are important in the design of oral drug delivery s system which remains the preferred route of drug delivery inspite of various disadvantage.one such problem can be solved in the novel drug delivery system by formulating oral disintegrating tablets which disintegrates rapidly without water within few seconds in the mouth due to action of super disintegrants in the formulation. Oral disintegrating tablets are advantageous for pediatric, geriatric mentally ill, nausea patients who have difficulty in swallowing conventional tablets and capsules. Using various excipients, evaluation tests marketed formulation and drugs used in the research area.

dispersible tablets of omeprazole and domperidone with using pertinent disintegrants by direct compression method. The tablets were prepared using mannitol as diluent and sodium sacchairn as sweetening agent along with three different levels of superdisintegrant used in kollidon CL, Ac-Di-Sol, drug and SSG. Omeprazole and domperidone were well resolved and the retention times were around 9.01 and 6.2 respectively. From the results obtained, it can be concluded that the tablet formulation prepared with 4.76% Ac-Di-Sol (internally cross linked form of sodium carboxymethylcellulose) i.e., 10 mg showed disintegration time of 15 seconds in vitro. Also the hardness, friability, dissolution rate and assay of prepared tablets (batch F7) were found to be acceptable according to standard limits.

In the present study Diltiazem hydrochloride odt was prepared with Three different superdisintegrants namely crospovidone, sodium starch glycolate and croscarmellose were used in the formulation of fast dissolving tablets. A total of nine formulations were prepared by direct compression technique microcrystalline cellulose was used as binder . The preformulation studies such as drug polymer compatibility, bulk density, angle of repose and Carr’s index evaluated were found to be within prescribed limits and indicated satisfactory free flowing property . The power blends of of CP-3 batch showed excellent flowability. The data obtained from physicochemical parameters such as hardness, friability, weight variation, drug content, wetting time, in vitro dispersion time and in vitro drug release studies by cp-3 met the requirements of fast dissolving tablet technology.

Most of the marketed fast dissolving tablets consists of non-steroidal anti- inflammatory drugs e.g. Rofecoxib, Ketoprofen and anti hypertensive drugs e.g. Atenolol, Metoprolol, anti emetic drugs e.g. Ondansetron, Granisetron.Disintegrants can help to facilitable drug dissolution and subsequently improvement in bioavailability. Though starch is a good disintegrant it has some problems e.g. high levels required in formulation lack of compressibility which weakens the tablet structure 16 . Therefore, the need of development of a new disintegrant arises which eliminates all disadvantages that starch has. A number of disintegrants, known super disintegrants like sodium starch glycolate (Explotab), crospovidone (Polyplasdone XL), pregelatinized starch(Starch 1500) markedly improve tablet disintegrantion by swelling and or capillary action, cause tablet to break into fragments 17 .The efficiency of these super disintegrants in any fast dissolving dosage forms depend on its selection, concentrations methods of incorporation and steps used for preparation.

Dosage form is a mean used for the delivery of drug to a living body. In order to get the desired effect the drug should be delivered to its site of action at such rate and concentration to achieve the maximum therapeutic effect and minimum adverse effect. Since oral route is still widely accepted route but having a common drawback of difficulty in swallowing of tablets and capsules. Therefore a lot of research has been done on novel drug delivery systems. This review is about oral dispersible tablets a novel approach in drug delivery systems that are now a day’s more focused in formulation world, and laid a new path that, helped the patients to build their compliance level with the therapy, also reduced the cost and ease the administration especially in case of pediatrics and geriatrics. Quick absorption, rapid onset of action and reduction in drug loss properties are the basic advantages of this dosage form. Key words: Fast dissolving/disintegrating tablets, orodispersible tablets, GIT, bioavailability, first pass metabolism, superdisintegrants

In the present investigate is an attempt towards developing a formulation of Anti-migraine drug. The patents for uses and dosage form of Rizatriptan Benzoate will expire in the future so our target was to develop a dosage form as that of innovator product to file an ANDA application . Innovations in the area of Oral Dispersible Tablets are aimed at both increasing the performance of the dosage form by decreasing the disintegration time and increasing the patient compliance by masking the objectionable taste of the ingredient by direct compression technique. It containing Rizatriptan Benzoate as model drug used for the treatment of migraine disease. Formulation were prepared by using different Super disintegrate and suggested nine formulation F01-F09 & prepared Oral Dispersible Tablets F01-F09 by direct compression techniques containing Croscarmellose sodium and Crospovidone as Super disintegrant in different concentration (10.5,13.0 and 15.5mg). Optimized F08 formulation containing concentration of Crospovidone 10.5mg, Pregelatinized Starch 20mg, Aspartame 5mg as sweetener and Peppermint 1mg as flavor, Mannitol 94.77mg, Microcrystalline cellulose Avicel pH 101 37.20mg &Avicel pH 102 5mg, and Mag Stearate 12mg were used and further evaluated. Which having shows good flow properties of powder and final blend, less weight variation, Thickness 2.70-3.20 mm, Hardness 2.7-3.0 N, less disintegration time 11-15 sec and maximum drug content 99.94%. From this study, it can be concluded that Direct Compression technique has low cost, more potential and applicability in future for formulation of Orodispersible Tablet of Rizatriptan benzoate than that of Lyophilization Technique.

Micromedex Healthcare., 2005). However, this becomes a major patient non compliance in the case of children, elderly and bed ridden patients for whom swallowing tablets causes inconvenience (Shu T et al., 2002). Among the dosage forms developed to facilitate ease of medication. The rapid disintegrating tablet (RDT) is one of the most widely employed commercial products (Koizumi K et al., 1997). Hence, present investigation is an attempt to improve patient compliance by formulating antiulcer drug omeprazole in the form of oral dispersible tablets.

Many techniques have been used in the formulation of oral dispersible tablets with the usage of super disintegrants like croscarmellose sodium, crospovidone, sodium starch glycolate, for the DP formulations of different drugs (Susijit Sahoo et al., 2010). The super disintegrants selected for the present study are croscarmellose sodium and micro crystalline cellulose along with the macromolecular inclusion complex namely beta-cyclodextrins for increasing the dissolution rate as well as bioavailability. It was essential to include super disintegrants individually and in combination, hence in the present work an attempt has been made to formulate oral dispersible tablets of aceclofenac with and without using macro molecular inclusion complex (Beta-cyclodextrins) in individual and combination with super disintegrants (Croscarmellose sodium, Microcrystalline cellulose). MATERIALS AND METHODS

The oral route of administration is the better-adapted route of administration of different therapeutic agents. It is generally preferred route due to its advantages such as convenience in case of self-administration, compactness and easy manufacturing. Infact of having so many advantages, the most common drawback of in oral dosage forms like tablets and capsules is difficulty in swallowing, particularly in the case of pediatric and geriatric patients, and mentally disabled patients. To overcome these problems, Pharmaceutical scientists have developed mouth dissolving/disintegrating tablets (MDTs). These Mouth Dissolving Tablets take less than three minutes to dissolve in the oral cavity. Mouth dissolving tablets have good taste and flavour and mask the bitter taste of the drugs. MDTs are most useful for the bed-ridden and patients who have the swallowing problems. Mouth dissolving tablets are also known as oral dispersible tablets, fast disintegrating tablets, orally disintegrating tablets, quick disintegrating tablets, fast-dissolving tablets, rapid dissolving tablets. Mouth dissolving tablets are formulated by two different methods one be patented technology and another one is non patented technology. The advantages of MDTs are a considerable dosage form, onset of action, self-administration, no risk, no pain increased bioavailability of the drug.

Oral Dispersible tablets are well recognised dosage forms presented in the market. Since their introduction to the market in the 1980s, ODTs have become one of the fastest growing segments of the oral drug delivery industry, and their product pipeline is rapidly expanding. An orally disintegrating tablet or orodispersible tablet (ODT) is a drug dosage form available for a limited amount of over-the-counter (OTC) and prescription medications. ODTs is one such novel approach to increase consumer acceptance by virtue of self-administration without water or chewing which disintegrate or dissolve rapidly in the mouth (saliva) within few seconds.The various advantages that they offer to the patients in terms of massive revenues by line extension of products include a variety of advantages. The development of oral dispersible tablets has been formulated for paediatric, geriatric, and bed rest patients and for those people as well as patients who may not have access to water with improved therapeutic efficacy and patient compliance. Several formulations provide an opportunity for product line extension especially for elderly persons will have difficulties in taking conventional oral dosage forms because of hand tremors and dysphasia and swallowing problem in young individuals due to under developed muscular and nervous systems. This article gives a brief review on the ideal properties, significance, characteristics, limitation, choice of drug candidates, challenges in formulation, the fabrication of Oro-dispersible tablets with a detailed concept of fabricating technologies, patented technologies as well as emerging trends or technologies and Evaluation tests of ODTs.