Mouth Dissolving Tablets Research Articles

Formulation, development and optimization of mouth dissolving tablets of Rizatriptan benzoate

Rizatriptan benzoate, a drug used to treat migraine needs quick action, for which mouth dissolving tablets (MDTs) of the drug may be suitable. However, the bitter taste of drug pose a major challenge to the development of MDTs of the drug. In the present study, MDTs were developed after masking the bitter taste of the drug through solid dispersion. The solid dispersions of Rizatriptan benzoate were prepared with PEG 6000 and mannitol in various ratios and the taste of the formulations was evaluated by willing volunteers and the most acceptable formulation was chosen for development of the MDTs. The MDTs were developed and optimized by using the sequential simplex optimization technique. Disintegration time, hardness and friability of the tablets were considered as the parameters for the optimization of formulations. The optimized formulation showed a disintegration time of 15 s, hardness of 5.2 kg/cm2 and friability of 0.5 %. The drug release of 99 % was achieved within 15 min in simulated saliva fluid. Therefore, the MDTs developed in this study could meet the dual need of effectively masking the bitter taste of the drug as well as deliver it quickly, for speedy onset of action and better therapeutic efficacy.

A review on fast dissolving tablet

These tablets are distinguished from conventional sublingual tablets, lozenges, and buccal tablets which require more than a minute to dissolve in the mouth. In the literature, ODTs also are called orally disintegrating, orodisperse, mouth-dissolving, quick-dissolve, fast-melt, and rapid-disintegrating tablets. Over the past three decades, orally disintegrating tablets (ODTs) have gained much attention as a preferred alternative to conventional oral dosage forms such as tablets and capsules. An ODT is a solid dosage form that disintegrates and dissolves in the mouth (either on or beneath the tongue or in the buccal cavity) without water within 60 seconds or less. The desire of improved palatability in orally administered products has prompted the development of numerous formulations with improved performance and acceptability, and the field has become a rapidly growing area in the pharmaceutical industry. The unique property of mouth dissolving tablet is that they are rapidly disintegrating and/or dissolving and release the drug as soon as they come in contact with saliva, thus obviate the requirement of water during administration. This article reviews the earlier applications and methodologies of taste masking and also emphasize on the recent developments and approaches of bitterness reduction for orally used pharmaceuticals. Apart from the conventional methods of fabrication, this review also provides the detailed concept of some unique patents; technologies developed and marketed formulations of Mouth Dissolving Tablets (MDTs).

Formulation variable study and optimization of taste masked mouth dissolving tablets using design of experiment

Background: Aim of present work is to prepare and optimized mouth dissolving tablets (MDTs) by using tasteless complex of levocetirizine. Materials and Methods: Formulation and optimization of tablets was done by using computer optimization technique. Formulated taste masked complex of drug was characterized by taste evaluation, percentage drug loading, thermal analysis and X-ray diffraction pattern. Optimization of MDTs was done by considering concentration of binder (polyvinylpyrrolidone [PVP] K30) and super-disintegrant (Kyron T-314) as independent variables whereas wetting time (WT), friability (Fr) and amount of drug release in 15 m (Q 15 ) as dependent variables. Response surface plots and contour plots were drawn, and optimum formulations were selected by feasibility and grid searches. Result and Discussion: By using 3 2 central composite design (CCD) optimized batch was obtained for which value of independent variable, PVP K30 (X1) and Kyron T-314 (X2) was 15 mg and 21 mg respectively and for dependent response, that is, Fr, WT and Q 15 to be 0.42%, 11.8 s. and 91.16% respectively. Validation of optimization study indicated very high degree of prognostic ability of response surface methodology (RSM). By analyzing the observed value to predicted value for Fr, WT and Q 15 the regression coefficient value was found to be 0.950, 0.961 and 0.957. Linearity of plot concluded that desired predicted response of all check-point batches were close to the predicted values and show the validity of data. Conclusion: Hence, optimized formulated batches were formulated by proper balancing of concentration of independent variables to attain desired dependent response using 3 2 CCD. Thus, 3 2 CCDs is an efficient tool in optimization experiments. High degree of outcome obtained using RSM concludes that 3 2 CCD is quite efficient in optimizing drug delivery systems that exhibit nonlinearity in response.

Formulation and Evaluation of Mouth Dissolving Tablets of Tramadol Hydrochloride

Purpose: To prepare, and evaluate in vitro and in vivo tramadol hydrochloride mouth dissolving tablets (MDT).Methods: Tramadol HCl MDT were prepared by direct compression using Pharmaburst as coprocessed excipient and compared with a reference product (Rybix ODT, 50 mg). Physicochemical parameters including hardness, friability, weight variation, disintegration time and dissolution studies were determined for all the formulations. In-vivo studies were performed for the optimized formulation (F13), using as reference, a commercial product (Trambax IR, 50 mg), by a two-way crossover design under fasting conditions on eight healthy adult human subjects. Drug-plasma concentrations obtained from the bioequivalence study for test and reference products were analyzed in each subject by high performance liquid chromatography (HPLC), and basic pharmacokinetic parameters, including Cmax, Tmax, AUC0-t, AUC0-∞, t½ and λz, were calculated.Results: The tablet formulation prepared with Pharmaburst (F13) showed good flow properties, low disintegration time (15 s) and improved drug release (99 % at 30 min) compared with those of the reference product (88 % at 30 min) and passed 6 months accelerated stability test. Bioequivalence of the test product with that of the reference product under fasting conditions was established by computing 90 % confidence interval for the In-transformed pharmacokinetic parameters of Cmax, AUC0-t and AUC0-∞ for tramadol. The 90 % confidence intervals for Cmax were 99.70 - 114.31, for AUC0-t 97.31 - 108.87 and for AUC0-∞ 97.17 - 109.75. This confidence interval, in each case, was within bioequivalence criteria limitConclusion: A suitable preparation of tramadol HCl MDT that is bioequivalent with a reference commercial product under fasting condition can be obtained when Pharmaburst is used as a disintegrant.Keywords: Bioequivalence, dissolution, Mouth dissolving tablets, Pharmaburst, Tramadol hydrochloride, Disintegration time

A review on fast dissolving tablets

Fast dissolving tablets are also called as mouth-dissolving tablets, melt-in mouth tablets, Orodispersible tablets, rapimelts, porous tablets, quick dissolving etc. Fast dissolving tablets are those when put on tongue disintegrate instantaneously releasing the drug, which dissolve or disperses in the saliva. The faster the drug dissolved into solution, quicker the absorption and onset of clinical effect. Oral routes of drug administration have wide acceptance up to 50-60% of total dosage forms. Solid dosage forms are popular because of ease of administration, accurate dosage, self-medication, pain avoidance and most importantly the patient compliance.

Formulation and Evaluation of Mouth Dissolving Tablets of Buclizine HCl by Direct Compression Technique.

Aim of novel drug delivery system is to enhance safety and efficacy of drug molecule to achieve better patient compliance. One of the above advances is the formulation of mouth dissolving tablets (MDTs) which dissolve instantaneously. Within a few seconds the releasing of drug without the need of water. Main objective of this paper was to prepare and develop MDTs of Buclizine (BZ HCl) with sufficient mechanical integrity, content uniformity, and acceptable palatability to assist patients of any age for easy administration. Buclizine HCl is an anti-allergic drug used for management of allergic reactions. The MDTs of Buclizine HCl were prepared by direct compression method. The effect of varying concentrations of different superdisintegrants such as crospovidone, croscarmellose sodium, and sodium starch glycolate on disintegration time and dissolution rate was studied. The prepared tablets were evaluated for hardness, friability, disintegration time and in-vitro drug release. Results obtained conclusively demonstrated successful rapid disintegration of the formulated tablets and acceptable palatability.

A REVIEW ON MOUTH DISSOLVING TABLETS

Mouth Dissolving Tablets (MDTs) have received ever-increasing demand during the last decade and the field has become a rapidly growing area of research in the pharmaceutical industry. Upon introduction into the mouth, these tablets dissolve or disintegrate in the mouth in the absence of additional water for easy administration of active pharmaceutical ingredients. The popularity and usefulness of the formulation resulted in development of several MDT technologies. This review describes various formulations and technologies developed to achieve fast dissolution/dispersion of tablets in the oral cavity. In particular, this review describes in detail MDT technologies based on lyophilization, moulding, sublimation and compaction, as well as approaches to enhance the MDT properties, such as spray drying, moisture treatment, sintering, and use of sugar-based disintegrants.

IN-VITRO AND IN-VIVO CHARACTERIZATION OF MOUTH DISSOLVING TABLET: AN UPDATED REVIEW

Mouth dissolving tablets (MDTs) has extended much attention as a preferred alternative to conventional oral dosage form. It provides an advantage particularly for pediatric and geriatric populations who have difficulty in swallowing conventional tablets and capsules. MDTs have the unique property of rapidly disintegrating and/ or dissolving or releasing the drug as soon as they come in contact with saliva, thus obviating the requirement of water during administration. The current review describes the ideal characteristics, significance, limitations and mainly lays emphasis on the in-vitro and in-vivo characterization of MDT. Keywords: Mouth dissolving tablets, disintegration, in-vivo and in-vitro evaluation, dysphagia.

MOUTH DISSOLVING TABLETS: A REVIEW

Conventional dosage forms like tablets and capsules are now days facing the problems like dysphagia, resulting in the high incidence of non compliance and making the therapy ineffective. To obviate the problems associated with conventional dosage forms, mouth dissolving tablets have been developed having good hardness, dose uniformity, easy administration and serves as the first choice of dosage form for paediatrics, geriatrics and travelling patients. The MDTs were developed with an aim of having sufficient hardness, integrity and faster disintegration without water. Fast dissolving Tablets are disintegrating and/or dissolve rapidly in the saliva without the need for water. Some tablets are designed to dissolve in saliva remarkably fast, within a few seconds, and are true fast-dissolving tablets. Others contain agents to enhance the rate of tablet disintegration in the oral cavity, and are more appropriately termed fast-disintegrating tablets, as they may take up to a minute to completely disintegrate. This tablet format is designed to allow administration of an oral solid dose form in the absence of water or fluid intake. Such tablets readily dissolve or disintegrate in the saliva generally within <60 seconds. Keywords: Mouth dissolving tablet, Disintegration, Patented technologies, Marketed MDTs Â

Formulation and in Vitro Evaluation of Mouth Dissolving Tablet of Olanzapine Using Solid Dispersion Technique

In the present investigation solid dispersion of olanzapine has been prepared to improve its solubility. Further, using solid dispersion, mouth dissolving tablet was prepared to overcome the problem of swallowing. A Simplex Lattice design was applied using three factors, i.e. superdisintegrants like croscarmellose sodium(X 1 ) crospovidone(X 2 ), and sodium starch glycolate(X 3 ) in tablet formulation. Disintegration time and T 50 (Time required to 50% drug release) taken as responses. Solid dispersion showed significant enhancement in solubility of olanzapine. For mouth dissolving tablet, batch containing 5% croscarmellose sodium alone had minimum disintegration time (44 sec.) and faster drug release (T 50 : 40 sec) compared to other batches.

Development and Characterization of Mouth Dissolving Tablet of Zolmitriptan

ObjectiveTo formulate and Characterize Mouth Dissolving Tablet of Zolmitriptan to produce the intended benefits. MethodsTablets were prepared using a direct compression method employing superdisintegrants such as Kyron T-314, Crospovidone, Croscarmellose Sodium, and Sodium Starch Glycolate. Tablets of Zolmitriptan prepared using Kyron T-314 exhibited the least friability and disintegration time 35 seconds. To decrease the disintegration time further, a sublimation technique was used along with the superdisintegrants for the preparation of Mouth Dissolving Tablet (MDTs). The addition of camphor as a subliming agent lowered the disintegration time 10 seconds further, but the percent friability was increased. A 32 full factorial design was employed to study the joint influence of the amount of superdisintegrant (Kyron T-314) and the amount of sublimating agent (Camphor) on the percent of friability and the disintegration time. ResultsThe results of multiple linear regression analysis revealed that an effective MDT of Zolmitriptan requires higher percentages of Kyron T-314 and camphor should be used. The approach using the optimization technique helped to produce a detailed understanding effect of formulation parameters. An optimized formulation was found to have good hardness, wetting time, disintegration time. Release kinetic model study indicated that all the formulations follow zero order kinetics. It also indicated that batch F1, F2, F5 and F8 releases the drug at constant rate as well as fast rate as per the Weibull model which was also confirmed by Hixson-Crowell model. Stability studies indicated that there are no significant changes in hardness, Percentage friability, drug content and in-vitro disintegration time and cumulative percentage drug release. ConclusionsThus, it was concluded that by adopting a systematic formulation approach, Zolmitriptan Mouth dissolving tablet could be formulated using superdisintegrants in combination with a vacuum-drying technique for improved therapeutic efficacy.

Formulation and evaluation of aceclofenac mouth-dissolving tablet

Aceclofenac has been shown to have potent analgesic and anti-inflammatory activities similar to indomethacin and diclofenac, and due to its preferential Cox-2 blockade, it has a better safety than conventional Non steroidal anti-inflammatory drug (NSAIDs) with respect to adverse effect on gastrointestinal and cardiovascular systems. Aceclofenac is superior from other NSAIDs as it has selectivity for Cox-2, a beneficial Cox inhibitor is well tolerated, has better Gastrointestinal (GI) tolerability and improved cardiovascular safety when compared with other selective Cox-2 inhibitor. To provide the patient with the most convenient mode of administration, there is need to develop a fast-disintegrating dosage form, particularly one that disintegrates and dissolves/disperses in saliva and can be administered without water, anywhere, any time. Such tablets are also called as “melt in mouth tablet.” Direct compression, freeze drying, sublimation, spray drying, tablet molding, disintegrant addition, and use of sugar-based excipients are technologies available for mouth-dissolving tablet. Mouth-dissolving tablets of aceclofenac were prepared with two different techniques, wet granulation and direct compression, in which different formulations were prepared with varying concentration of excipients. These tablets were evaluated for their friability, hardness, wetting time, and disintegration time; the drug release profile was studied in buffer Phosphate buffered Saline (PBS) pH 7.4. Direct compression batch C3 gave far better dissolution than the wet granulation Batch F2, which released only 75.37% drug, and C3, which released 89.69% drug in 90 minutes.

Formulation design and optimization of tastemasked mouth-dissolving tablets of Tramadol hydrochloride

The aim of the present study was to mask the extremely bitter taste of Tramadol HCL, an opioid analgesic, and to formulate a tablet which can rapidly disintegrate in saliva (rapidly disintegrating tablet). The crucial aspect in the formulation of mouth-dissolving tablets is to mask the bitter taste and to minimize the disintegration time. Taste masking was done using sweetening agent and D-mannitol and taste-masked pellets were prepared by extrusion spheronization technique. Prepared pellets were tested for drug content, taste evaluation in oral cavity and molecular property. Pellet shows significant taste masking, confirmed by in vitro taste evaluation; therefore, it was selected for further study. Pellets were evaluated for density, angle of repose, Carr’s index, Hausner’s ratio and sphericity while tablets were evaluated for disintegration and in vitro dissolution. A 32 full factorial design and statistical models were applied to optimize the effect of two factors, i.e. superdisintegrant sodium starch glycolate and taste-masking agent (D-mannitol). In this study, response surface methodology was used for designing of the experiment, generation of mathematical models and optimization study. Taste evaluation of pellets in human volunteers revealed considerable taste masking with a degree of bitterness below threshold value (2.0) within 10 s, whereas Tramadol HCl was rated intensely bitter with a score of +4 for 10 s. The size of the pellets varied from 0.895 to 1.423 mm for different batch and found to be a spherical. Disintegration time of different formulations varied from 30 to 60 s. It was observed that the responses, i.e. disintegration time and sphericity were affected by both the factors. The statistical models were validated and can be successfully used to prepare optimized taste-masked mouth-dissolving tablets of Tramadol HCl with adequate disintegration and shape. Key words: 32 factorial design, rapidly disintegrating tablet, response surface methodology, taste-masked granule, Tramadol HCL

Formulation design and optimization of taste-masked mouth-dissolving tablets of Tramadol hydrochloride

Formulation design and optimization of taste-masked mouth-dissolving tablets of Tramadol hydrochloride

Formulation Design and Optimization of Novel Taste Masked Mouth-Dissolving Tablets of Tramadol Having Adequate Mechanical Strength

The purpose of this work was to develop novel taste masked mouth-dissolving tablets of tramadol that overcomes principle drawback of such formulation which is inadequate mechanical strength. Tramadol is an opioid analgesic used for the treatment of moderate to severe pain. Mouth-dissolving tablets offer substantial advantages like rapid onset of action, beneficial for patients having difficulties in swallowing and in conditions where access to water is difficult. The crucial aspect in the formulation of mouth-dissolving tablets is to mask the bitter taste and to minimize the disintegration time while maintaining a good mechanical strength of the tablet. Mouth-dissolving tablets of tramadol are not yet reported in the literature because of its extreme bitter taste. In this work, the bitter taste of Tramadol HCl was masked by forming a complex with an ion exchange resin Tulsion335. The novel combination of a superdisintegrant and a binder that melts near the body temperature was used to formulate mechanically strong tablets that showed fast disintegration. A 3(2) full factorial design and statistical models were applied to optimize the effect of two factors, i.e., superdisintegrant (crospovidone) and a mouth-melting binder (Gelucire 39/01). It was observed that the responses, i.e., disintegration time and percent friability were affected by both the factors. The statistical models were validated and can be successfully used to prepare optimized taste masked mouth-dissolving tablets of Tramadol HCl with adequate mechanical strength and rapid disintegration.

Ternary complexation of carvedilol, β-cyclodextrin and citric acid for mouth-dissolving tablet formulation

The purpose of this study was to improve the solubility and dissolution rate of carvedilol by forming a ternary complex with beta-cyclodextrin and citric acid and to formulate its mouth-dissolving tablets. The rationale for preparing mouth-dissolving tablet of carvedilol was to make the drug available in a soluble form in the mouth, which would facilitate its absorption from the buccal cavity. This would help to overcome its first-pass metabolism and thereby improve bioavailability. Phase solubility studies revealed the ability of beta-cyclodextrin and citric acid to complex with carvedilol and significantly increase its solubility. Ternary complexation of carvedilol was carried out with beta-cyclodextrin and citric acid by physical mixing, kneading and spray drying methods and the prepared complexes were characterized by Fourier transform infra red spectroscopy, differential scanning calorimetry, powder X-ray diffractometry, scanning electron microscopy and complexation efficiency. The complex obtained by the spray drying method resulted in highest complexation efficiency and a 110-fold increase in the solubility of carvedilol. The mouth-dissolving tablets formulated using the spray dried complex with suitable excipients showed 100 % dissolution within five minutes. Accelerated stability studies of mouth-dissolving tablets carried out as per ICH guidelines revealed that the tablets were stable.