Fast dissolving tablets

Improvement of patient’s compliance has always a challenge towards the development of oral drug delivery system. Different dosage forms are available in the market among all oral dosage form is preferred one. However, the incompliance of pediatric & geriatric patients the scientists worked towards fast dissolving solid dosage form to encounter existing drawbacks with unique palatability and rapid disintegration. The concept of fast dissolving tablet came into existence in late 1970s. Recently, fast dissolving drug delivery systems have started gaining popularity and acceptance as new drug delivery system, because they are easy to administer and lead to better patient compliance. For further improvement in existing technologies and newer technologies has been succeeded and still research is going on in improvement with its preparation methodologies all over the globe. Fast dissolution tablets have faster disintegration and dissolution rate and release within 30 seconds as they come in contact with saliva. These systems also obviate the requirement of carry water during drug administration. As fast dissolving tablets falls under desired expectation of safer, convenient and economical solid dosage forms, several techniques have been developed to improve disintegration quality in the recent past years. This article mainly focuses on patented technologies with recent advancement made so far in the field of the fast dissolving tablets.

Candesartan cilexetil is a prodrug of candesartan – a compound that inhibits binding of angiotensin II to the AT1 – receptor.  It is mainly used in the treatment of hypertension. In the present work attempts were mase to prepare fast dissolving tablets of candesartan cilexetil by sublimation technique. The prepared formulations were evaluated for pre-compressional and post-compressional parameters. The compatibility of drug with other ingredients was checked by FTIR studies, these results revealed that there was no interaction between dug and other excipients. The values of pre-compressional parameters were within prescribed limits and indicated good free flowing properties. In all the formulations the hardness test indicates good mechanical strength. Friability of all formulations was less than 1. Drug content was found to be high (≥ 100.27%) and uniform in all the formulations. The tablet thickness was found to be 3.14 – 3.47. The weight variation results revealed that average percentage deviation was less then ± 7.5 %, which provides good uniformity in all formulations. The disintegration time of the tablets decreased significantly with increase in the concentration of subliming agent. The formulations CSC3, CSM3, CSA3, and CSU3 50 % of drug released in 1.38, 2.55, 4.00 and 3.57 min, and 90 % of drug released in 3.39, 6.04, 7.50 and 7.18 min. The formulation CS (control) released 42.16 % in 60 min. Stability study carried out as per ICH guidelines for three months and results revealed that upon storage disintegration time of tablets decreased significantly (p<0.05). The results concluded that by adopting a systemic formulation approach, an optimum point could be reached in the shortest time with minimum efforts. Sublimation technique would be an effective alternative approach compared with the use of more expensive adjuvants in the formulations of fast dissolving tablets.

Desloratadine is an antagonist at histamine H1 receptors, and an antagonist at all subtypes of the muscarinic acetylcholine receptor. It has a long-lasting effect and in moderate and low doses, does not cause drowsiness because it does not readily enter the central nervous system. The present study is an attempt to formulate and evaluate the fast dissolving tablets of  Desloratadine. Fast dissolving tablets were prepared by direct compression after masking the bitter taste of drug by solid dispersion method with the aid of superdisintegrants. Seven formulations were developed using two different superdisintegrants in varying concentrations in such a way that total weight of the tablet remains the same. The drug-polymer incompatibility was ruled out by FTIR studies. All the formulated tablets were subjected for pre and post-compression evaluation parameters. A comparison of in vitro drug release of best formulation along with F1 formulation having no superdisintegrants is carried out. All the formulated tablets were shown satisfactory results which complies with official limits. Among the seven formulations, F7 was selected as the best formulation as its wetting time was 33 seconds, disintegration time was 29 seconds and %CDR after 8 minutes was 100.1%. F7 was found to be stable at 25°C ± 2 °C,  60°C ± 5°C and 40 °C ± 2 °C and 75 ± 5 % RH . Formulated tablets containing high concentration of croscarmellose sodium are better and effective than conventional tablets to meet patient compliance, give fast relief from allergy and cost effective.

Fast dissolving tablets are the tablets which dissolves rapidly and shows higher bioavailability than conventional tablets. The concept of formulating Fast dissolving tablets of Carvedilol (antihypertensive drug) offer suitable and practical approach in serving the desired objective of faster disintegration and dissolution characteristic with increase bioavailability and to know the effects of two natural superdisintegrants (Hibiscus Rosa, Linseed Mucilage). In the present work solid dispersion were prepared by solvent evaporation method for improving the bioavailability with beta cyclodextrin as a carrier to increase the solubility of the drug. And after compressing the tablet , heat is applied to create pores in tablet as it contain camphor as subliming agent which increase the porosity and cause faster release of drug from the tablet. Comparison between these two natural superdisintegrants was done by taking different ratios individually and in combination. Combination of these two superdisintegrants shows synergistic effect when it is compared to individually. Prepared tablets were subjected to different evaluation parameters such as hardness, friability, weight variation, drug content uniformity, in vitro disintegration time, wetting time, in vitro dissolution studies and stability studies are carried out by using the best formulation. From all the formulations prepared and tested, F11 was found to be the best formulation.

Fast dissolving tablets are the tablet which dissolves rapidly and shows higher bioavailability than conventional tablets. The concept of formulating Fast dissolving tablets of Famotidine (H2 –receptor antagonist) offer suitable and practical approach in serving the desired objective of faster disintegration and dissolution characteristic with increase bioavailability and to know the effects of two synthetic superdisintegrant (Croscarmellose sodium and Sodium starch glycolate). In the present work two methods of solid dispersion were compared for improving the bioavailability i.e. Solvent Evaporation and Fusion method with PVP K30 as a carrier to increase the solubility of the drug. Comparison between these two synthetic superdisintegrant was done by taking different ratios and in combination. Three different combination of these superdisintegrant shows synergistic effect when it is compared to individual. Prepared tablets were subjected to different evaluation parameters such as hardness (2.84±0.15 kg/cm2 to 3.01±0.20 kg/cm2), friability (not more than 0.680±0.0173), weight variation (197.6±1.42 mg to 202.6±1.90 mg), drug content uniformity (97.84±0.35 to 100.23±0.71%), in vitro disintegration time (21.0±0.81 sec to 108.33±0.47 sec), wetting time (29.33±0.47 to 113.33±1.24 sec), in vitro dissolution studies and stability studies are carried out by using the best formulation. From all the formulations prepared and tested, F9 was found to the best formulation.

Fast dissolving tablets are the tablets which dissolves rapidly and shows higher bioavailability than conventional tablets. The concept of formulating Fast dissolving tablets of Loratadine (antiallergic drug) offer suitable and practical approach in serving the desired objective of faster disintegration and dissolution characteristic with increase bioavailability and to know the effects of three synthetic superdisintegrants (Crosscarmeloss sodium, Sodium starch glycolate and Crospovidone). In the present work two methods of solid dispersion were compared for improving the bioavailability i.e Solvent Evaporation and Fusion method with beta cyclodextrin as a carrier to increase the solubility of the drug. Comparison between these three synthetic superdisintegrants was done by taking different ratios individually and in combination. Combination of these three superdisintegrants shows synergistic effect when it is compared to individually. Prepared tablets were subjected to different evaluation parameters such as hardness, thickness, friability, weight variation, drug content uniformity, in vitro disintegration time, wetting time, in vitro dissolution studies and stability studies are carried out by using the best formulation. From all the formulations prepared and evaluated F11 was found to the best formulation. Key words: Fast dissolving tablets, Solid dispersion, Crosscarmeloss sodium, Sodium starch glycolate, Crospovidone, Evaluation parameters.

  Metoprolol Tartrate is effective β-blocker used in the second line treatment for angina and for myocardial infarction. Adult dose as conventional preparations is 25-100 mg daily in single or divided doses, as extended release 100-200 mg once daily. The bioavailability of the drug when formulated as conventional tablets is 40 % due to hepatic metabolism. The present investigation was undertaken with a view to develop a fast dissolving tablet of Metoprolol Tartrate which offers a new range of product having desired characteristics and intended benefits prepared by direct compression method using different concentrations of superdisintegrant. Effect of superdisintegrant on wetting time, drug content, in-vitro drug release, disintegration time has been studied. Disintegration time increased with increase in the level of Croscarmellose sodium while it decreased for Crospovidone, the release was dependent on the aggregate size in the dissolution medium. It is concluded that Metoprolol Tartrate fast dissolving tablets could be prepared using superdisintegrant with improved bioavailability and rapid onset of action.

  Nimodipine is an antihypertensive, calcium channel blocker, vasodilator agent and used in the treatment of various cardiovascular disorders such as angina pectoris, cardiac arrhythmia and hypertension. Oral bioavailability of Nimodipine is around 13% and having half life 9 hrs. In present research work an attempt has been made to prepare fast dissolving tablets of Nimodipine by direct compression technique with β-cyclodextrin complexes using various superdisintegrants. The powder blends were subjected for pre-compressional parameters. The prepared tablets were evaluated for post-compressional parameters. The prepared tablets were characterized by DSC and FTIR Studies. No chemical interaction between drug and excipients was confirmed by DSC and IR studies. The values of pre-compression parameters evaluated were within prescribed limits and indicated good free flowing property. All the post-compressional parameter are evaluated were prescribed limits and results were within IP acceptable limits. The tablets were evaluated for the in-vitro disintegration time and it was observed that the time for all the formulations varied from 19.24 to 48.29 sec. The promising formulations CCP4, CCC4 and CSS1 shows the 90 % of drug released within 5-8 min. Among all the formulation CCP4 (15 % crospovidone) were found to be best and showed a disintegration time of 19.24 sec, 50 % of drug released in 0.96 min, and 90 %  of drug released in 4.78 min. The stability study was conducted as per the ICH guidelines and the formulations were found to be stable, with insignificant changes in hardness, drug content and disintegration time. These results revealed that fast dissolving tablets of the poorly soluble drug, Nimodipine, showing enhanced dissolution and, hence, better patient compliance. Key words: Fast dissolving tablets, Nimodipine, sodium starch glycolate, croscarmellose sodium, crospovidone,  β-cyclodextrin.