Disintegrating Tablets - Literature review Example

Literature review Rohini, P. et al. (2014) formulated Rosuvastatin, orally disintegrating tablets using direct compression method. They began by preparing fourteen batches using different super disintegrants such as Crospovidone, LycoatRs720, croscaramellose sodium and sodium starch glycolate and in different concentrations. They evaluated the formulations in terms of wetting time, weight variation, friability, drug content, in-vitro dissolution and disintegration time (Rohini, et al, 2014). They found out that the formulation that contains 8% of super disintegrants of sodium starch glycolate and Crospovidone in equal amount was the best formulation that released over 90 percent of the drug in less than 5 minutes. Patel et al (2010) focused on Crosspovidone out of 3 super disintegrant on their study by evaluating the disintegrating time and wetting time. In this study they prepared Rofecoxib tablets through wet granulation technique. They evaluated optimized concentration of Crosspovidone and found out that the concentration of 10% was the best formulation to obtain fast disintegrating tablets (Patel et al, 2010). They used disintegration time and wetting time as the dependent variables and Mannitol and Crosspovidone as independent variable. They compared the best formula with marketed samples and found out that the formula obtained indicated better dissolution compared to marketed products. Mishra DN et al. (2006), used croscarmellose sodium, sodium starch glycolate and mannitol as diluent and Crospovidone as superdisintegrants to prepare rapid disintegrating Valdecoxib tablets. They evaluated the tablets for disintegration time, hardness, in-vitro dissolution analysis, weight and friability. They found out that the quick dissolving tablets of less soluble drug can be prepared using direct compression method by selective superdisintegrants. Madhu B et al., (2006) used spray dried expedients base to prepare orally disintegrating tablets in order to assess the suitability of spray dried excipient base when formulating orally disintegrating tablets (ODT) of high aqueous solubility (Metoclopramide) and low aqueous solubility (Valdecoxib) they used super disintegrants like sodium starch glycolate, kollidon CL, Ac-Di-Sol, mannitol together with aspartame used for sweetening to formulate the tablets. Bhatti A et al. (2007), used taste masked granules which that was made from aminoalkyl methacrylate copolymers by extrusion technique to formulated fast disintegrating oral tablets of Chlorpheniramine maleate. The in vitro discharged profile at a pH of 6.8 show that the significant amount of drug will is not released in the saliva but significant amount (over 80 percent in half an hour) is obtained in more acidic condition of pH 1.2 in the stomach. They used direct compressed method to prepare that tablets using sodium starch glycolate as super - disintegrant. They further evaluated the tablets for fro taste using panel testing method and spectrophotometric technique. They found out that panel testing data obtained from healthy people exhibit successful formation of oral fast disintegrating tablets that disintegrates within 30 second after oral taking. Jain CP et al. (2009) used direct compression technique to prepared Valsartan, rapid dissolving tablets using superdisintegrants and test it for in vitro dissolution and physicochemical properties. They evaluated the disintegration behaviour of the tablet using artificial saliva of pH 5.8. The tablets indicated rapid disintegration and the formulations that which contains Crospovidone had less wetting time. The formulations released from fast dissolving tablets (FDTs) increased with increase in concentration but was highest in the formulation that had Crospovidone. Swamy PV (2007) and a group of other researchers tried to design ODT by use of Meloxicam with an aim enhancing patience compliance. A combination of different superdisintegrants such as sodium starch glycolate-crospovidone and sodium starch glycolate-croscarmellose sodium was used together with mannitol that can be compressed in order to improve the feeling in the mouth. Using in vitro dispersion time that is around ten seconds, two formulas one from every batch were put on test for in vitro drug discharge pattern in a pH of 6.8, the stability at 45 degrees centigrade for a period of three weeks and drug-excipients interaction by use of Infra-Red spectroscopy (Swamy, 2007). From the resulting formulation, two formulation was found to be better that was formulation containing 2 percent of sodium starch glycolate and 1.5 percent of croscarmellose sodium (Swamy, 2007). Setty CM et al (2008) carried out an experiment by developing fast dispersible tablets by compression method by use of several superdisintegrants, croscarmellose and sodium starch glycolate and analyzed their effect on the time it takes to get wet, disintegrate, and amount of drug content in vitro drug release and parameters of its stability (Setty et al, 2008). The results shows that the time it take for the drugs to disintegrate and dissolution parameters decline when the level of croscarmellose sodium increases, while on the other hand, the time it takes to disintegrate and dissolution parameters increases as the level of sodium starch glycolate is increased (Setty et al, 2008). Nevertheless the time it takes the drug to disintegrate fail to reflect dissolution parameter values of Crospovidone drugs and the release of the drugs depends on the total size in dissolution medium. Dandagi et al (2005) tried to formulate dissolving tablets of ofloxacin that are taste masked by a method of direct compression. Two methods were used in the masking of the taste that were addition of sweet substance like aspartame and secondly by mass extrusion method. The superdisintegrants that were used to make the tablets disintegrate fast in the mouth include mannitol, sodium starch glycolate and a mixture of L-HPC and Avicel PH 102 in the ratio 1 to 4 (Dandagi et al, 2005). Disintegration of mannitol, sodium and starch glycolate was fast while disintegration of a combination of L-HPC and Avicel PH 102 was the slowest. Desai et al (2006) prepared ODT of promethazine hydrochloride by use of sodium starch glycolate and cross-carmellose sodium superdisintegrants through the method of direct compression. All the tablets that were prepared exhibited hardness between two to four kg/cm2. The rate of disintegration between the two formulation were different, tablets formulated with sodium starch glycolate disintegrated at a rate of 1 to 3 percent while that formulated with cross-carmellose sodium disintegrated at a rate of 4 to 12 percent in vitro and in vivo in a time of 8 to 10 seconds and 9 to 20 seconds and approximately all the drugs was released from all the formulations in less than two minutes (Desai et al, 2006). Shreenivas and a group of researchers prepared ondansetron hydrochloric tables that can disintegrate in the mouth through a method of direct compression using different superdisintegrants including cross-povidone, croscarmellose sodium, pregelatinized starch, sodium starch glycolate and L-HPC at concentration level of five and ten percent (Shreenivas, Gadad, Dandagi, and Patil, 2006). From all the drugs that were developed, tablets containing ten percent of cross-povidone disintegrate faster at a time of around 10 seconds and wetting time was around 14 seconds, while the formulation containing pregelatinized starch disintegrate slowly at a time of 14 seconds and wetting 24 seconds (Shreenivas, Gadad, Dandagi, and Patil, 2006). Jayadev et al (2011) formulated and designed ODTs that contain antihistamines such as Loratadine using different compositions by direct compression method so as to improve patience compliance. The recipients that were used include Maltodextrin, Mannitol, Micro crystalline cellulose, combination of Mannitol with Starch, Croscarmellose sodium, and Citric acid, the process was evaluated by use of simple analytical technique (Patil, Gopal, Kadam, & Vishwajith, 2011). The taste of the drugs was improved by use of two artificial sweetener that was Aspartame and Mint flavor. All the formulation weight difference, hardness, friability, drug content, wetting and disintegration time were evaluated (Patil, Gopal, Kadam, & Vishwajith, 2011). The results from the study shows that ODT formulated from Loratadine have good physical parameters and disintegrate fast in the mouth without affecting release profile, and effective when used by the elderly and pediatric patients. Furthermore, preparation of drugs using direct compression method using excipients such as a combination of Mannitol with Starch and Micro crystalline cellulose as directly compressible diluents along with super disintegrants like Croscarmellose Sodium was found to be promising in preparing ODTs. Mahajan et al (2004) formulated tablets of sumatripan succinate that can dissolve in the mouth by use of disintegrants sodium starch glycolate, and carboxy methylcellulose sodium by direct compression method. The thickness, weight uniformity, drugs content, water absorption rate, hardness, wetting time, and in vivo and in vitro disintegration time was evaluated using various techniques (Mahajan, Kuchekar, and Badhan, 2004). The drugs disintegrate in vitro in a time between 10 and 15 seconds and in vivo it disintegrate at a time of 12 to 19 seconds. In all the formulations, over 90 percent of the drugs was released in less than 10 minutes. The best disintegration results came from the combination of sodium starch glycolate and carboxy methyl cellulose (Mahajan, Kuchekar, and Badhan, 2004). Rawas-Qalaji et al (2006), studied what will happen if epinephrine is increased on the properties of oral disintegrating sublingual tablets for possible treatment of anaphylaxis. Four different types of tablets with different formulations was prepared, they contain zero percent, six percent, twelve percent, and twenty four percent of epinephrine bitartrate, respectively, and microcrystalline cellulose: low-substituted hydroxypropyl cellulose at a ratio of 9 to 1 were prepared by direct compression method (Rawas-Qalaji, Simons, & Simons, 2006). When compressional force was increased linearly the hardness of all the tablets increases exponentially, furthermore there was a linear increase in disintegration and wetting times of the first formulation and exponential increase in disintegration and wetting times of the remaining formulation respectively. They all passed USP friability test with hardness of 3.1 +/- 0.2 kg (Rawas-Qalaji, Simons, & Simons, 2006). The disintegration times for all the formulation were between 10 to 30 seconds. Shenoy et al (2003) formulated ODT of diclofenac sodium using direct compression method, the tablet ingredients was mixed with superdisintegrants like cross linked carboxymethylcellulose, sodium starch glycolate, and cross linked povidone under different conditions. All the drugs that were developed were evaluated to find the influence of disintegrants and their concentrations on characteristics of rapid dissolving drugs mostly in terms of disintegration time and dissolution rate (Shenoy et al, 2003). The results shows that the tablets containing cross-linked carboxymethylcellulose disintegrate faster and it releases over 90 percent of the drugs in less than 10 minutes. The drugs containing the remaining two superdisintegrants did not show any appreciable difference. The concentration of the superdisintegrants of different formulation also have an effect on the rate of disintegration and in vitro dissolution (Shenoy et al, 2003). The rate of disintegration and dissolution is higher when high level disintegrants are used to formulate the tablets. The hardness and friability of the formulation were also evaluated and it was found that it is independent from the disintegrant concentration. Over the recent past advances in drugs development is aimed at achieving better patience compliance. One of advances in medicine development is development of ODTs. Mahrous et al (2016) formulate ODTs of clopidogrel by the method of direct compression. Three superdisintegrants were used that is Crospovidone, croscarmellose sodium, and sodium starch glycolate and three different disintegrations were used to determine dissolution rate (Mahrous et al, 2016). The formulation hardness, friability, disintegration time and in vitro drug release were evaluated using different techniques. Additionally, interaction of clopidogrel with formulation excipients was analyzed by us of differential scanning calorimetry (DSC) (Mahrous et al, 2016). The results shows that the drugs did not interact with the excipients used. All formulation hardness ranges between 4 to 5 kp. More than 90 percent of the drugs were released within a period of less than 10 minutes according to the in vitro study. Palatability test were carried out using human volunteers and the results shows that the drugs taste were acceptable. The results conclusively shows fast disintegration of the tablets in the mouth and acceptable palatability (Mahrous et al, 2016). References Rohini, P., Pavani, A., & Reddy, R. R. (2014). Formulation and evaluation of orally disintegrating tablets of rosuvastatin. International Journal of Pharmaceutical Sciences Review and Research, 24, 1, 209-214. Madhu B, Dina N. M., shailendra K. S., sengodan G. V. (2006). Spray dried excipient: a novel technique for the formulation of orally disintegrating tablets. Chem Pharm Bull, 54 (1): 99-101 Bindal M, Guruswamy V. L., Mishra D. N., Singh SK. (2006). Spray dried excipient base: A novel technique for the formulation of orally disintegrating tablets. Chem Pharm Bull. 54 (1) Bhatti A., Shishu R., Singh T. (2007). Preparation of tablets rapid disintegrating in saliva containing bitter tastes masked granules by compression method. Ind pharm Sci. 69 (1) 80-84 Jain CP, naruka P. S., Swammy P. G. (2009). Formulation and evaluation of fast dissolving tablest of valsartan. Int j Pharm sci, 1(1):220 - 226 Dandagi, P. M., Sreenivas, S. A., Manvi, F. V., Patil, M. B., Mastiholimath, V. S., & Gadad, A. P. (2005). Taste Masked Ofloxacin Mouth Disintegrating Tablets. Indian Drugs. 42, 52-55. Shreenivas S. A. , Gadad A. P., Dandagi P. M., and Patil M. B. (2006). “Formulation and evaluation of ondensetron hydrochloride directly compressed mouth disintegrating tablets.” Indian Drugs 43.1:35-38. Patil J., Gopal V., Kadam C., & Vishwajith V. (2011). Formulation, design and evaluation of orally disintegrating tablets of Loratadine using direct compression process. International Journal of Pharma and Bio Sciences. 2, 389-400. Mahajan H. S., Kuchekar B. S., Badhan A. C. (2004). “Mouth dissolve tablets of sumatriptan succinate.” Indian Journal of Pharmaceutical Science 66.2:238-240 Rawas-Qalaji M. M., Simons F. E., & Simons K. J. (2006). Fast-disintegrating sublingual tablets: effect of epinephrine load on tablet characteristics. AAPS PharmSciTech. 7. Desai S. A., Kharede S.V., Petkar K. C., Kuchekar B. S. (2006). “Orodispersible tablets of promithazine hydrochloride.” Indian Journal of Pharmaceutical Education and Research 40.3, 172-174. Shenoy, V., Agrawal, S., & Pandey, S. (2003). Optimizing Fast Dissolving Dosage Form of Diclofenac Sodium by Rapidly Disintegrating Agents. Indian Journal of Pharmaceutical Sciences. 65, 197-201. Mahrous, G. M., Kassem, M. G., Ibrahim, M. A., & Auda, S. H. (2016). Formulation and evaluation of orally disintegrating clopidogrel tablets. Brazilian Journal of Pharmaceutical Sciences. 52, 309-318 Swamy, P., Areefulla, S., Shirsand, S., Gandra, S., & Prashanth, B. (2007). Orodispersible tablets of meloxicam using disintegrant blends for improved efficacy. Indian Journal of Pharmaceutical Sciences. 69, 836. Patel B.P., Patel J.K., Rajput G.C., & Thakor R.S. (2010). Formulation and evaluation of mouth dissolving tablets of cinnarizine. Indian Journal of Pharmaceutical Sciences. 72, 522-525. Read More