Superdisintegrants

The Main goal of the present study was to develop and evaluate the orally disintegrating mini-tablets (ODMTs) containing Salbutamol sulphate for the treatment of respiratory disorders like Asthma and Chronic obstructive pulmonary diseases. The problems associated with conventional oral dosage forms are associated with slow down onset of action and lag time, while parenterals and aerosol despite of quick-outset of action strongly affect the patient compliance. Quick release tablets are highly accepted rapid increasing drug delivery systems and thus, an attempt was made to improve the onset of action of drug. To reach this goal, selective superdisintegrants like Crospovidone and Sodium starch glycolate were used in different ratios. Micromeritic properties of the powder were within the limit confirmed by free flowing. ODMTs were compressed in order to have sufficient mechanical strength and integrity to withstand handling, shipping and transportation. The tablets were prepared by direct compression method and physicochemical properties were evaluated. FTIR and DSC studies were confirms no chemical interaction between the excipients and drug. Out of six formulations prepared tablet F3 resulted a least dissolution and disintegration time. Hence, concluded that ODMTs give the better effect to the asthma patients and may serve as a successful strategy for enhancing the bioavailability of drug.

The Mouth Dissolving Drug Delivery Systems was an advancement that came into existence in the early 1970’s and combats over the use of the conventional tablets, syrups, capsules which are the other oral drug delivery systems. Orally disintegrating dosage forms can address the pharmaceutical needs of the paediatric and geriatric patient group having difficulties in swallowing the conventional solid oral dosage forms. Orally disintegrating dosage forms also have the advantage of self medication, pain avoidance hence better patient compliance. Taste masking of bitter drugs is an important parameter. Orally disintegrating dosage forms may have an added advantage of bypassing first pass metabolism. Acyclovir is an antiviral drug used for the treatment of herpes simplex virus (HSV), mainly HSV-1 and HSV-2 and varicella zoster virus. It is a BCS class III drug. Hence an orally disintegrating tablet formulation of acyclovir was prepared by direct compression techniques after incorporating superdisintegrants croscarmellose sodium , sodium starch glycolate and Crossprovidone . Eight formulations were prepared. Tablet containing sodium starch glycolate and croscarmellose sodium showed excellent in vitro dispersion time and drug release as compared to other formulation. After   study of eight formulations F8 showed short dispersion time with maximum drug release in 25 min. It is concluded that fast disintegrating acyclovir tablets could be prepared by direct compression using superdisintegrants.

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.

Oral drug delivery has been known for decades as the most widely utilized route of administration among all the routes. United State Food and Drug Administration (FDA) defined ODT as “a solid dosage form containing medicinal substance or active ingredients which disintegrate rapidly usually within a matter of second when placed upon the tongue. Propranolol is a nonselective beta-adrenergic blocker and is almost completely absorbed following oral administration. However , most of drug is undergoes high first-pass metabolism by the liver and on average, only about 25% of propranolol reaches the systemic circulation. The present study investigated to development of novel fast dissolving tablet of Propranolol HCL which was by first pass metabolism, provide rapid onset of action and increasing the bioavailability of the drug. The fast dissolving tablets were prepared by Direct compression method by using different superdisintegrant like Crosspovidone, crosscarmellose sodium, sodium starch glycolate etc. The advantage of this formulation is such that in case of hypertension attack patient can take the drug without the usage of water. Therefore the main objective of the present work is to develop orodispersible tablets of Propranolol hydrochloride to improve bioavailability, disintegration time, dissolution efficacy and patient compliance.

The purpose of this research was to develop mouth dissolve tablets ofdomperidone andpantoprazole, were prepared by direct compression technique. Pantoprazole inhabits gastric acid formation and thereby it is very efficient for the treatment of gastric and duodenum ulcers. Domperidone, an antiemetic drug, has been used as an add-on treatment in adults and children. The tablets were prepared using microcrystalline cellulose as diluent and  aspartames as sweetening agent along with three different levels of disintegrant. The superdisintegrant used in this study were CCS and SSG. The tablets were evaluated for weight variation, hardness, friability, wetting time, water absorption ratio, disintegration time (DT) and dissolution study. formulation prepared with 30% of CCS showed Disintegration time of 20seconds in vitro. Also the hardness, friability, dissolution rate of prepared tablets (batch F6) were found to be acceptable according to standard limits.

An immediate action of Metformin HCl is essential for emergency treatment of diabetes. With an objective of finding the best suitable disintegrant for immediate release tablet of Metformin HCl, different formulations were prepared by incorporating varying ratios of three widely used superdisintegrants both by intra and extra granularly. Wet granulation method was adopted to formulate the tablets by using Maize Starch as diluent; Povidone k-30 as binder; Sodium Starch Glycolate/Kollidon CL/Crosscarmellose Sodium as superdisintegrants in different concentration (2-3.5%), Aerosil-200 as flow promoter and Magnesium Stearate as lubricant. To evaluate the rheological properties of powdered blend, some pre-compression characteristics including bulk and tapped densities, compressibility index, Hausner’s ratio, angle of repose were studied. The compressed tablets were evaluated for hardness, thickness, diameter, friability, drug content, weight variation, in vitro dispersion time, in vitro disintegration time, in vitro wetting time and finally for in vitro dissolution studies. It was found that wetting time, dispersion time and the disintegration time of the tablets were governed by the type and quantity of the superdisintegrants. In vitro drug release data obtained at phosphate buffer at pH 6.8 also found reliant on successful incorporation of right disintegrating agent. Higher the disintegrant ratio in the formulation, lower the disintegration time and hence, higher percentage of drug release was obtained. Based upon results of different studies, Sodium Starch Glycolate has been proven successful in rapid disintegration of tablets and enhancing dissolution behavior.

Armodafinil is very slightly soluble in water; hence the drug may be slowly or incompletely dissolved in the gastro intestinal tract. So the rate of dissolution and therefore its bioavailability is less. In the present study an attempt has been made to prepare immediate release tablets of Armodafinil by using different superdisintegrants (croscarmellose sodium, pregelatinized starch and Avicel pH 101 to increase the rate of drug release from dosage form or the dissolution rate and hence its bioavailability. The prepared granules and tablets were evaluated for their physiochemical properties and in-vitro dissolution study was conducted for the prepared tablets. The in-vitro dissolution studies shows the release in the following order of superdisintegrants is croscarmellose sodium> Pregelatinized starch> Avicel PH 101. It was concluded that the immediate release tablets with proper hardness, disintegration time and with increase rate of dissolution can be made using croscarmellose sodium as superdisintegrants (F9). The formulation F9 was selected as an optimized formulation for stability study and the in-vitro dissolution study showed that was no difference in percent of drug released between 1st month and 3rd month sample.

  Fast dissolving drug delivery system offers a solution for those patients having difficulty in swallowing tablet. In the present study, an attempt has been made to formulate fast dissolving tablets of Pantoprazole Sodium Sesquihydrate using superdisintegrants such as Croscarmellose sodium (Ac‐Di‐Sol), Sodium starch glycolate (Explotab) and Crosspovidone by direct compression technique. The prepared tablets were evaluated for hardness, friability, wetting time, weight variation, in vitro disintegration time and in vitro dissolution study. The hardness of the tablets was in the range of 3.0 ‐ 4.0 Kg/cm². The percentage friability of the tablets was less than one. Weight variation test results showed that the tablets were deviating from the average weight within the permissible limits of ±7.5 %. Drug content uniformity study results showed the uniform dispersion of the drug throughout the formulation i.e. 98.54% to 101.23%. Tablets containing Crosspovidone (F9) showed better disintegrating character along with the rapid release (99.83% drug within 4 minutes). No appreciable difference was found between the formulations containing other two superdisintegrants. Crosspovidone was found to be better suited for the formulation of mouth dissolving tablet of Pantoprazole Sodium Sesquihydrate compared to other superdisintegrarnts used in the study.

  Fast dissolving, fast melting, chewable and orally dissolving or disintegrating tablets are solid dosage forms that disintegrate rapidly and dissolve in the mouth withoutwater. The principle challenge with orally disintegrating tablets (ODTs) is to develop tablet formulations for standard direct compression processes that deliver rapid disintegration, pleasant mouth feel and high breaking force for tablet robustness. Superdisintegrant affect a range of formulation parameters, including the rate of disintegration, tablet breaking force, and mouth feel. The emphasis on the availability of drug highlights the importance of the relatively rapid disintegration of a tablet as a criterion for ensuring uninhibited drug dissolution behavior. Number of factors affects the disintegration behavior of tablets. The development of fast dissolving or disintegrating tablets provides an opportunity to take an account of tablet disintegrants. Superdisintegrants are generally used at a low level in the solid dosage form, typically 1 – 10 % by weight relative to the total weight of the dosage unit. Key words: Tablet Disintegrants, Superdisintegrants, Kyron T-314.