Crospovidone

The aim of present research work is to formulate and evaluate Oral dispersible tablets of frovatriptan using various diluents and superdisintegrants and to optimize the formulation. Frovatriptan is a triptan drug  used for the treatment of migraine headaches. The drug excipient compatibility study was done and  no interactions were found, DSC & XRD studies were carried out. The tablets were formulated by direct compression method using Spray dried lactose, Manito, Microcrystalline cellulose (MCC), Starch as diluents and Crospovidone, Cross-Carmel lose sodium, Sodium starch glycol ate as superdisintegrants. The pre-compression parameters like bulk density, tapped density, Carr’s Index, Haunters ratio and angle of repose were determined and all the formulations were found to be within IP limits. The post compression parameters like the hardness, thickness, friability, weight variation, and disintegrating time, wetting time, water absorption ratio and drug content for all the formulations were carried out and results were found to be as per USP limits. In-vitro drug release and kinetics studies were carried out for all the formulations, of those the formulation F33 containing Cross providing (5%) and mannitol as diluent, has shown better release and follows first order kinetics. The formulations were optimized by 22 factorial design and the ANOVA study was carried out and normal plot, half normal plot and overlay plot were plotted. The tablets were stored at 40±2ËšC/75 ± 5% RH for three months to assess the stability of optimized formulation.

The present study involved preparation of solid dispersions of Olmesartan medoxomil to improve the aqueous solubility and dissolution rate in order to enhance bioavailability. Olmesartan is a BCS Class II anti-hypertensive drug, having low aqueous solubility and low bioavailability of 26%.  In the present study, solid dispersions of Olmesartan with different carriers like Poloxamer 407, PEG 4000  and crospovidone in different ratios (1 : 1, 1 : 2, 1 : 3, 1 : 4) were prepared by solvent evaporation method.  The formulations were further characterized for percentage yield, drug content, in vitro release study,  and stability study. In vitro release studies revealed that the solid dispersions prepared by solvent evaporation method crospovidone (1 : 4) was considered as the best formulation because of its faster drug release among all formulations.  Infrared spectroscopy (IR) studies revealed that no interactions exist between drug and polymer. Powder X-ray diffraction studies showed a significant decrease in crystalline nature of drug in solid dispersions. In conclusion, solid dispersions of Olmesartan in crospovidone (1:4) have shown to be a promising approach to enhance the bioavailability of Olmesartan.

Enalapril maleate is the maleate salt of enalapril, a derivative of two amino acid, L-alanine and L-proline. Enalapril maleate is angiotensin converting enzyme (ACE) inhibitor. It lowers blood pressure by reducing peripheral vascular resistance without relatively increasing cardiac output, rate or contractility. All grades of essential hypertension especially in patients with diabetes and other chronic renal diseases like glomerulosclerosis can be treated with Enalapril. It is also indicated in the treatment of heart failure. Enalapril maleate is having a half life of 11 hrs. The bioavailability of Enalapril maleate tablets is approximately 55 % and food does not affect absorption. Hence, an attempt was made for preparations of a FDT of enalapril maleate were formulated by direct compression technique using co-processed superdisintegrant like Crospovidone and Croscarmellose sodium in different ratios. The prepared were evaluated for various pharmaceutical characteristics viz. hardness, % friability, weight variation, drug content, in-vitro dissolution profiles. Results showed that the direct compression technique by using co-processed superdisintegrants successfully used for enhancing the solubility of Enalapril Maleate. The prepared tablets were characterized using FTIR and finally the prepared tablets were evaluated for various pharmaceutical characteristics such as hardness, % friability, weight variation, drug content all the results were within the I.P Limit. Crosspovidone and CCS containing tablets rapidly exhibit high capillary activity and pronounced hydration with a little tendency to gel formation and disintegrate the tablet rapidly. The formulations prepared by co-processed superdisintegrants showed rapid % drug release due to fast disintegration of tablets. The formulation PM 3 and CP 6 shows 99% drug released within 20 minutes. The results of stability studies revealed no change in physical appearance, hardness, drug content and in vitro dissolution profiles, thus indicating that formulation was stable. Thus Results showed that the direct compression technique by using co-processed superdisintegrants successfully used for enhancing the solubility of Enalapril maleate.

In the present work Tadalafil fast disintegrating tablets were prepared with poloxamer as carrier to enhance the solubility of Tadalafil and in order to disperse at faster rate in the mouth. Chemically Tadalafil is (6R,12aR)-6-(1,3-Benzodioxol-yl) 2,3,6,7,12,12a hexahydro-2-methylpyrazino[10,20:1,6] pyrido [3,4-b]indole-1,4-dione used in erectile dysfunction. In this current work Tadalafil fast disintegrating tablets were formulated from F1-F12 by direct compression method by taking 1:1, 1:2 and 1:3 ratio of poloxamer as a water soluble polymer and super disintegrating agents such as crospovidine, croscarmellose sodium, sodium starch glycolate and kryon. There after FT-IR studies were performed and it was observed that there were no incompatible reactions found between the Tadalafil and excipients used in formulations. Then all the formulations of Tadalafil fast disintegrating tablets F1-F12 were evaluated for pre and post compressional parameters including in-vitro dissolution studies. In which formulation F-12, containing (1:3) ratio of drug-poloxamer and kryon as super disintegrating agent was shown significant changes in wetting time (13±2.09sec), dispersion time (36±3.605sec) and fastest percentage drug release of 99.27±2.78 within 30 minutes was observed.

Oral fast disintegrating films (OFDF) is an emerging technology brings out “formulations taken without water” with quick onset of action and improved patient compliance. The present aim of study is to enhance the dissolution rate of the dosage form by using the different superdisintegrants and co-processed superdisintegrants. The films were prepared by solvent casting method using hydrophilic polymers that rapidly dissolves on the tongue or buccal cavity, delivering the drug to the systemic circulation. The polymer was used  HPMC E15, PEG 6000 as plasticizer, citric acid as the saliva stimulating agent, sucrose as the sweetening agents and sodium starch glycolate, crosscarmelose sodium and crospovidone as the superdisintegrants and tween 80 as surfactant . The FTIR reports suggest that drug and excipients were compatible. These oral disintegrating films were evaluated for various evaluation parameters. The in-vitro dissolution studies were conducted as per USP II with sinker. There were three ODFs prepared by using different types of the superdisintegrants, two were prepared by using the co-processed superdisintegrants and one was without any superdisintegrants. Among all formulation, the F6 shown the better in-vitro drug release profile which was prepared by using co-procesed superdisintegrants. It can be concluded that the co-processed superdisintegrants enhances the dissolution rate by comparing with other formulation.

The present study was an attempt to prepare and evaluate Zolmitriptan 9 different oral disintegrating tablets using superdisintegrants like SSG, Crospovidone and Croscarmellose sodium. Formulations were evaluated for their micromeretic properties and post compression studies and found to be within the limits. Based on the disintegrating time and dissolution studies F9 was found to be best formulation. It was found that the sodium starch glycolate is much more effective than the other super disintegrating agents in the preparation of Zolmitriptan oral disintegrating tablets. DSC and FTIR data revealed that no interactions takes place between the drug and polymers used in the optimized formulation.

The present research work was to design and develop an optimized oro-dispersible tablet dosage form of an anti-psychotic drug, Olanzapine by using direct compression technology.  Total number of nine formulations were prepared as per the standard experimental design protocol using Design Expert Software (Version 8.0.5, Stat-Ease, Inc.). Independent variables such as the amount of the amount of Crospovidone XL 10 (A) and the amount of Avicel PH 102 (B) were optimized by application of Response surface methodology using Central Composite Design. The dependent variables selected were in-vitro dispersion time and wetting time of the tablets. All the evaluated physical parameters of the oro-dispersible tablets were practically within control. The direct compression method used to prepare the oro-dispersible tablets in this study is relatively simple, safe and economic. A stable, effective and pleasant tasting mouth dissolving tablet, which has a good balance over all the physical parameters was formulated.

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.

The pivotal motif of the present research work is to develop immediate release tablets of Fexofenadine hydrochloride. The rate of dissolution and bioavailability of the Fexofenadine HCL may be increased by using superdisintegrant in its immediate release tablets. Direct compression method was adapted to prepare the tablets by using lactose, microcrystalline cellulose as filler, crospovidone and sodium starch glycolate as superdisintegrant in different concentration (2-8%). Tablet were prepared and evaluated for Hardness, friability, weight variation, content uniformity, wetting time, disintegration time and in-vitro drug release. Disintegration time decreased with increase in the level of crospovidone. Whereas, disintegration time increased with increase in the level of sodium starch glycolate. The results indicate that the selected batch of tablet formulation containing crospovidone provides DT between 3-6 minutes with sufficient crushing strength and accepted friability. It was concluded that immediate release tablet for Fexofenadine hydrochloride can be formulated for fast treatment of allergic rhinitis

  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.