Benefits Of Tablets That Disintegrate In Water Biology Essay

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Schiermeier S et al. 2002 mentioned fast dispersible tablets disintegrate either rapidly in water, to form a stabilized suspension, or disperse instantaneously in the mouth to be swallowed without the aid of water. A direct compression method was used to prepare these two types of tablets containing coated ibuprofen as a high dosed model drug to develop an orodispersible tablet, a rotatable central composite design was applied to predict the effects of the quantitative factors mannitol and crospovidone as well as compression force on the characteristics of the tablet.

Shishu et al. 2007 prepared rapidly disintegrating tablets of chlorpheniramine maleate using taste masked granules. The taste masked granules were prepared using aminoalkyl methacrylate copolymers (Eudragit E-100) by the extrusion method. in vitro release profile obtained at pH 6.8 indicate that perceivable amount of drug will not be released in saliva while high percent release (more than 80% in 30 min) would be obtained at acidic pH 1.2 of the stomach. These taste masked granules were directly compressed into tablets using sodium starch glycolate as a super disintegrant.

Malke S et al. 2007 fast dissolve tablets of oxcarbazepine were prepared containing Avicel PH 102 as a diluent and Ac-Di-Sol as a superdisintegrants by wet granulation process. A modified disintegration method was used for studying disintegration. Since the drug is poorly water soluble, drug release was tested in various media and the effect of surfactant on drug release was studied.

Madgulkar AR et al. 2007 studied the efficacy of Indion 414 and Amberlite IRP 88 as superdisintegrants in mouth dissolve tablets of Nimesulide. Formulations also contain camphor. Tablets were prepared by wet granulation method. The compressed tablets were stored at 50°C for two hours to bring about sublimation of camphor. The tablets were evaluated for parameters like hardness, friability, weight variation, drug content, in vitro dispersion time, in vivo dispersion time and drug release. Indion 414 was found best compared to Amberlite IRP 88.

Swamy PV et al. 2007 designed orodispersible tablets of meloxicam with a view to enhance patient compliance. A combination of superdisintegrants i.e., sodium starch glycolate-crospovidone and sodium starch glycolate-croscarmellose sodium were used with directly compressible mannitol to enhance mouth feel. Based on in vitro dispersion time (approximately 10 sec), two formulations (one from each batch) were tested for in vitro drug release pattern (in pH 6.8 phosphate buffer), short term stability (at 45°C for 3 weeks) and drug-excipients interaction (IR spectroscopy). Among the two formulations, the formulation containing 2% w/w/ sodium starch glycolate and 1.5% w/w croscarmellose sodium was found to be better formulation.

Sharma S et al. 2008 prepared fast dissolving tablets of promethazine theoclate by direct compression after incorporating superdisintegrants Ac-Di-Sol, sodium starch glycolate, and crospovidone in different concentrations. Different types of evaluation parameters for tablets were used. Tablets containing Ac-Di-Sol showed superior organoleptic properties, along with excellent in vitro and in vivo dispersion time and drug release, as compared to other formulations.

Patel DM et al. 2008 developed fast dissolving tablets of etoricoxib; a 32 full factorial design was applied to investigate the combined effect of 2 formulation variables: amount of menthol and crospovidone. Granules containing etoricoxib, menthol, crospovidone, aspartame and mannitol were prepared by wet granulation technique. Menthol was sublimed from the granules by exposing the granules to vacuum. The porous granules were then compressed in to tablets. Alternatively, tablets were first prepared and later exposed to vacuum. The result of multiple regression analysis indicated that for obtaining fast dissolving tablets; optimum amount of menthol and higher percentage of crospovidone should be used.

Setty CM et al. 2008 prepared aceclofenac fast dispersible tablets by direct compression method using different superdisintegrants, croscarmellose sodium, sodium starch glycolate, and crospovidone and their effect on wetting time, disintegration time, drug content, in vitro release and stability parameters had been studied. Disintegration time and dissolution parameters decreased with increase in the level of croscarmellose sodium. Whereas, disintegration time and dissolution parameters increased with increase in the level of sodium starch glycolate in tablets. However the disintegration time values did not reflect in the dissolution parameter values of crospovidone tablets and release was dependent on the aggregate size in the dissolution medium.

Mundada AS et al. 2008 developed a technique to mask the bitter taste of roxithromycin by complexation technique and prepared dispersible tablet of taste masked granules. Weak cation exchange resins Indion 214 and Amberlite IRP 64, polymer carbopol 934 P were used in formulation of complexes with the drug. The loading process was optimized for the pH loading solution and resin or polymer: drug ratio. The complexes were evaluated for bulk density, angle of repose, taste masking, and in vitro drug release. Amberlite IRP 64 was found to be better complexing agent for masking bitter taste of roxithromycin.

Mulla JA et al. 2008 developed fast dissolving tablets of promethazine hydrochloride using direct compression after incorporating superdisintegrants such as Ac-Di-Sol, Explotab, and Polyplasdone XL in different concentrations. The prepared tablets were evaluated for different pharmacopoeial tests. Tablets containing Ac-Di-Sol showed better disintegrating character along with rapid release.

Mohapatra A et al. 2008 developed orally disintegrating tablets of metformin hydrochloride using direct compression and wet granulation method. Tablets prepared with direct compression using starch 1500 and microcrystalline cellulose showed erosion behavior rather than disintegration and also did not give good mouth feel. Thus Pearlitol SD 200 (spray dried mannitol) was used to prepare tablets by wet granulation (10% PVP in IPA as binder). The strong saline and slight bitter taste of the drug was masked using nonnutritive sweetener and flavor.

Furtado S et al. 2008 Orodispersible tablets of famotidine were prepared using camphor as subliming agent and sodium starch glycolate together with crosscarmellose sodium as superdisintegrants. The formulations were evaluated for weight variation, hardness, friability, drug content, wetting time, in vitro and in-vivo dispersion, mouth feel and in vitro dissolution. All the formulations showed low weight variation with dispersion time less than 30 seconds and rapid in vitro dissolution. The results revealed that the tablets containing subliming agent had a good dissolution profile.

Singh J et al. 2008 optimize an orodispersible formulation of indomethacin using a combined approach of subliming agent and superdisintegrant. The tablets were made by non-aqueous wet granulation technique with superdisintegrant incorporated both intragranularly and extragranularly. A 23 factorial design was used to investigate the effects amount of subliming agents namely camphor and ammonium bicarbonate and taste masking and soothening hydrophilic agent mannitol as independent variables and disintegration time and crushing strength as dependent responses. The volatilization time of eight hours at 50°C was optimized by conducting solid-state kinetic studies of optimized formulations. Optimized orodispersible tablets were evaluated for wetting time, water absorption ratio, porosity and in vitro and in vivo disintegration tests. Results show that higher levels of camphor and mannitol and a lower level of ammonium bicarbonate are desirable for orodispersion.

Mahapatra A et al. 2009 develop and characterize mouth dissolving tablets of Levocetirizine hydrochloride using sublimation technique. Mouth dissolving tablets of Levocetirizine hydrochloride using different concentrations of Pearlitol SD 200 (spray dried mannitol) and menthol were developed using direct compression technique. The technique is to increase the porosity of the tablets whereby menthol, a subliming material was removed by sublimation from compressed tablets. A high porosity was achieved due to the formation of many pores where menthol particles previously existed in the compressed tablets prior to sublimation of the menthol. Along with usual physical properties, the wetting time of tablets also measured. In-vitro and in vivo disintegration time of tablets were determined.

Kawtikwar P.S et al. 2009 prepare bitter less fast dissolving tablet of Tizanidine Hydrochloride using Eudragit E 100 as a taste masking agent. Mass extrusion was the technique used for preparing taste masked granules. The tablet was prepared with three super disintegrates e.g. sodium starch glycolate, crosscarmellose sodium and crospovidone. The blend was examined for angle of repose, bulk density, tapped density and hausner ratio. The tablets were evaluated for hardness, drug content and friability and disintegration time. The disintegration in oral cavity was also tested and was found to be 22 sec. Other tablets were prepared by using camphor as sublimating agent. It was concluded that tablets prepared by addition of superdisintegrant has less disintegration time than those prepared by sublimation method.

Modasiya M.K et al. 2009 prepare fast disintegrating tablets of Piroxicam in the oral cavity with enhanced dissolution rate. The tablets were prepared with three super disintegrates i.e. sodium starch glycolate, Ac-Di-Sol and low molecular weight hydoxy propyl methylcellulose. The blend was examined for angle of repose, bulk density, tapped density, compressibility index and Hausner's ratio. The tablets were evaluated for hardness, tensile strength, and drug content, friability and were found satisfactory. The disintegration time in the oral cavity was also tested. The rapidly disintegrating tablets with proper hardness, rapidly disintegrates in the oral cavity with enhanced dissolution, which is achieved by using selected superdisintegrants.

Patel B et al. 2009 fast dissolving tablets of glipizide were prepared by direct compression method with a view to enhance patient compliance. Two superdisintegrants viz, crospovidone and croscarmellose sodium (4%, 5%, 6%) with different binders viz, pvp k-30 and pregelatinized starch (3%) were used. The prepared batches of tablets were evaluated for hardness, friability, weight variation, disintegration, wetting time, drug content and in vitro dissolution studies. Based on evaluating parameters, Formulation prepared by using 5% croscarmellose sodium with 3% PVP K30 was selected as optimized formulation. Finally, the optimized formulation was compared with marketed conventional formulation. Stability studies were carried out at 25°C / 60% RH and 40°C / 75% RH for optimized formulation for 2 months. Stability studies on the optimized formulation indicated that there was no significant change found in physical appearance, disintegration time and wetting time of the tablets.

Singh J et al. 2009 formulate and optimize an orodispersible formulation of meloxicam using a 22 factorial design for enhanced bioavailability. The tablets were made by non-aqueous wet granulation using crospovidone and mannitol. A 22 factorial design was used to investigate the amount of crospovidone and taste masking, soothening hydrophilic agent (mannitol), as independent variables, and disintegration time as dependent response. Formulated orodispersible tablets were evaluated for weight variation, friability, disintegration time, drug content, wetting time, water absorption ratio and in vitro drug release. All the formulations satisfied the limits of orodispersion with a dispersion time of less than 60 sec.

Radke R.S et al. 2009 prepare orodispersible tablets of baclofen using various concentrations of superdisintegrant agents like Ac-Di-Sol, crospovidone, sodium starch glycolate by direct compression method. Nine formulations having superdisintegrants at different concentration levels were prepared. These tablets were evaluated for drug content, weight variation, friability, hardness, wetting time and in vitro disintegration time. Among the formulations tablets of batch F3 containing Ac-Di-Sol showed superior organoleptic properties along with excellent in-vitro disintegration time and drug release as compare to other formulations. It was concluded that superdisintegrants addition technique is a useful method for preparing orodispersible tablets by direct compression method.

Jain C.P. et al. 2009 fast dissolving tablets of valsartan were prepared using different superdisintegrants by direct compression method. FDTs were evaluated for physicochemical properties and in vitro dissolution. Effect of disintegrant on disintegration behavior of tablet in artificial saliva, pH 5.8 was evaluated. Wetting time of formulations containing Crospovidone was least and tablets showed fastest disintegration. The drug release from FDTs increased with increasing concentration of superdisintegrants and was found to be highest with formulations containing Crospovidone.

Shirsand S.B. et al. 2009 fast dissolving tablets of clonazepam were prepared by direct compression method with a view to enhance patient compliance. Three superdisintegrant, viz., crospovidone, croscarmellose sodium and sodium starch glycolate in different ratios with microcrystalline cellulose (Avicel PH-102) along with directly compressible mannitol (Pearlitol SD 200) to enhance mouth feel. The prepared batches of tablets were evaluated for hardness, friability, drug content uniformity, wetting time, water absorption ratio and in vitro dispersion time. Based on in vitro dispersion time (approximately 13 s), three formulations were tested for the in vitro drug release pattern (in pH 6.8 phosphate buffer), short-term stability (at 40°/75% relative humidity for 6 mo) and drug-excipients interaction (IR spectroscopy). Among the three promising formulations, the formulation prepared by using 10% w/w of crospovidone and 35% w/w of microcrystalline cellulose emerged as the overall best formulation.

Rangasamy M et al. 2009 fast dissolving tablets of terbutaline sulfate were prepared by the direct compression method after incorporating superdisintegrants such as Explotab, Ac-Di-Sol and Polyplasdone XL in different concentrations. The prepared tablets were evaluated for weight variation, thickness, hardness, friability, wetting time, drug content, water absorption ratio, in vitro dispersion time, in vitro disintegration time and in vitro drug release. Among all, the formulation F9 (containing 5% w/w concentration of Polyplasdone XL) was the best formulation, which releases up to 99.33% of the drug in 10 min.

Srinivas Reddy et al. 2002 investigated orally disintegrating tablets of levocetirizine dihydrochloride formulated with different superdisintegrants (sodium starch glycollate, croscarmellose sodium, and crosspovidone) using mannitol as a diluent. Tulsion-335®,Indion-204®, and poly kyron T -134® cation exchange resins were used as taste-masking agents. The drug and resin complex was prepared by the kneading method. Ten formulations were prepared with varying combinations of superdisintegrants and ion-exchange resins by the wet granulation technique, using polyvinylpyrrolidone K-30 as the binder. The prepared tablets were evaluated for degree of taste masking, weight variation, hardness, friability, in vitro and in vivo disintegration time, content uniformity, and water absorption ratio. Dissolution studies were performed in two dissolution media: O.IN HCI and distilled water. The corresponding dissolution rates were compared with the marketed formulation. Differential scanning calorimetry studies were carried out on the drug-resin complexes. Prepared tablets were good in appearance and showed acceptable results for hardness and friability. In vitro and in vivo disintegration times for the optimum formulation (F-I) were found to be 22 and 55 s, respectively. Relatively acceptable taste was achieved with both Indion-204 and Tulsion-335. Rapid disintegration time was achieved in tablets containing crosspovidone as the superdisintegrant. Dissolution studies indicated the formation of the complex of drug and resin. Differential scanning calorimetry studies indicated the formation of drug-resin complex.

N. Kanaka Durga devi et al. 2004 studied orally disintegrating tablets of Montelukast sodium a potent, selective and orally acting leukotriene receptor antagonist that acts by inhibiting physiological actions of the cysteinylleukotrienes (LTC4, LTD4 and LTE4). It is used in the prophylaxis and treatment of asthma. AS precision of dosing and patient's compliance become important prerequisite for asthma management, there is a need to develop formulations for this drug which overcomes problems such as difficulty in swallowing, inconvenience in administration while travelling and patient's acceptability. The tablets were prepared with three superdisintegrants i.e polyplasdone XLlO,Ac-Di-Sol and Primojel. The pure drug and formulation blend was examined for angle of repose, bulk density, tapped density, Compressibility index and Haussner's ratio. The tablets were evaluated for hardness, tensile strength, drug content, friability and were found satisfactory. The disintegration time in the oral cavity was also tested and was found to be around 9sec. Based on dissolution rate the disintegrants can be rated as Polyplasdone XLIO > Ac-di-sol > PrimojeL Hence polyplasdone XLIO was recommended as suitable disintegrant for the preparation of direct compression melt- in-mouth tablets of Montelukast sodium. All the dissolution parameters were calculated and compared with market tablet. An increase in the dissolution rate was observed with M8 formulation when compared to market one. It was concluded that the rapidly disintegrating tablets with proper hardness, rapid disintegration in the oral cavity with enhanced dissolution rate can be made using super disintegrants.

Yu-Shi Shen et al. 2006 designed orally disintegrating tablet formulation of olanzapine (ODT olanzapine) to get dissolve rapidly upon contact with saliva. A manic patient who has an esophageal stricture and chronic pharyngitis, two conditions that impede the swallowing of medications. She was successfully treated for her mania with this orally disintegrating formulation. This case report shows that ODT olanzapine may be useful in the psychiatric management of manic and other patients for whom olanzapine is appropriate, and who have an underlying medical condition that impedes swallowing oral medications.

Keny RV et al. 2004 investigated mouth disintegrating tablets of rizatriptan benzoate to produce the intended benefrts. Mouth disintegrating tablets of rizatriptan benzoate were prepared using superdisintegrants crosspovidone, carboxy methyl cellulose calcium, Indion 414 and Indion 234 using the direct compression method. The tablets prepared were evaluated for thickness, uniformity of weight, content uniformity, hardness, friability, wetting time, in vitro and in vivo disintegration time, mouth feel, in vitro drug release and assay by high performance liquid chromatography. The tablets disintegrated in vitro and in vivo within 4 to 7 s and 6 to 19 s, respectively. Almost 90% of drug was released from all formulations within 20 min. The drug release from the formulations followed first order kinetics. Stability studies of the tablets at 40+/- 2 degrees /75%+/-5% RH for 1 month showed non significant drug loss. The formulation containing combination of crosspovidone and Indion 234 was found to give the best results. Apart from fulfilling all official and other specifications, the tablets exhibited higher rate of release.

Sankar V et al. 2010 formulated Cetirizine oro-dispersible tablets for quick onset of action and for maximum bioavailability. Tablets were prepared using cetirizine along with camphor and mannitol in the proportion of 1:1:1, 1:1:3, and 1:1:6. The flow property of granules was found to be good for the formulation CZ2 (l: 1 :3). The hardness and friability of all the formulations were found to be within the standard limit for orodispersible tablets. Disintegration time was found to be rapid in formulation CZ2 (l:1:3).The in vitro dissolution time was found to be 100% in 11 minutes for the formulation CZ2 (l: 1 :3).

Javakar B et al. 2003 investigated Etoricoxib mouth dissolving tablets. toricoxib is a new non-steroidal anti-inflammatory drug (NSAID) with selective cox-2 inhibitory activity, selective inhibition of cox-2 provides anti-inflammatory and analgesic activity it is commonly used for osteo-arthritis, rheumatoid arthritis, primary dysmenorrhoea, post operative dental pain and acute gout. The main criteria for mouth dissolving tablets are to disintegrate or dissolve rapidly in oral cavity with saliva in 15 see to 60 see with need of water. The disintegrants used should fulfill the criteria by disintegrating the tablets in specified time limit. In the present investigation variety of super disintegrants like primogel, kollidone, Ac-Di-sol, L-HPMC, L- HPC, were selected and tablets were prepared by direct compression method in different concentration like 4% and 8%. The prepared tablets were evaluated for weight variation, hardness, friability, in vitro disintegration time, wetting time, in vitro dissolution study, etc. Formulation f-9 shows the lowest disintegration time (44 see) and wetting time (52 see). In vitro dissolution studies revealed that formulation F-9 containing 8% L-HPC showed 97% drug release at the end of 20 min.

Barabanti P et al. 1999 formulated Sumatriptan fast disintegrating tablet. Sumatriptan is the first serotonin (5-hydroxytryptamine [5-HT](lB/ID)) receptor agonist specifically designed for the acute treatment of migraine. A new sumatriptan fast disintegrating/rapid release tablet (FDTIRRT) using RT technology has been developed to enhance tablet disintegration and dispersion in the stomach with the intention of speeding absorption and onset of effect, hence mitigating the effects on the gastrointestinal dysmotility that typically accompanies the attack. Sumatriptan FDTIRRT is bioequivalent to conventional tablets, although it provides slightly faster absorption during early post-dose interval. Clinical trials indicate that sumatriptan FDTIRRT is rapidly effective in terms of freedom from pain and return to normal activities, both with early and late treatment. The drug is well tolerated. In an oral formulation, which is the patients' preferred dosing route, sumatriptan FDTIRRT may therefore constitute an advance in the management of acute migraine attacks.

Lew MF et al. 2002 examined orally disintegrating tablet of Selegiline a potent, selective and irreversible inhibitor of monoamine oxidase type B. It is delivered in an innovative formulation that largely bypasses the gut and first-pass hepatic metabolism by allowing transbuccal absorption. Selegiline orally disintegrating tablet dissolves in the mouth within seconds and is rapidly absorbed directly into the systemic circulation, increasing parent drug bioavailabilityand lowering plasma metabolites compared with conventional oral formulations. Adding selegiline orally disintegrating tablet to levodopa in patients experiencing 'wearing-off episodes significantly decreases off time and increases dyskinesia-free 'on' time. Adding selegiline orally disintegrating tablet to levodopa also significantly improves Unified Parkinson's Disease Rating Scale motor scores and patients' and physicians' ratings of disease severity. Selegiline orally disintegrating tablet has been demonstrated to be safe and well tolerated in placebo-controlled clinical trials.

Masareddy RS et al. 2006 made an attempt to study two different methods direct

compression and sublimation in formulation of mouth dissolving tablets of clozapine. Total four formulations using various superdisintegrants and subliming agents were prepared. All prepared formulations were evaluated for physico-chemical parameters. The formulations exhibited good disintegration properties with total disintegration time in the range of 25 to 35 s. Comparative evaluation of two methods showed direct compression method is a better alternative to sublimation method as its formulations rapidly disintegrate in oral cavity. In vitro cumulative percentage drug release for formulations prepared by direct compression with explotab superdisintegrants shows 99.79 while sublimation method using camphor 93.58 release in 12 min. Kinetic studies indicated that all the formulations followed first order release with diffusion mechanism.

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