Kyron T-314 Research Articles

Investigating in-vitro functionality and in-vivo taste assessment of eco-friendly Tadalafil Pastilles

Tadalafil (TDL) has poor bioavailability due to the less aqueous solubility and bitter taste. Oral solid dosage forms, especially tablets, have a broad market worldwide. Constraints of tablets are a long process, pollution, high processing cost, and requiring more excipient. The research was performed to optimize an eco-friendly immediate-acting pastille of TDL to put forward an alternate formulation to a tablet using advanced data mining tools. Another objective is to assess the taste masking of TDL using the Brief Access Taste Aversion (BATA) model. The amount of PEG-4000, Polyox N-10, and Kyron T-314 were chosen as critical material attributes from failure mode effect analysis. Box-Behnken design (BBD) was utilized to optimize the pastilles and ascertained the significant impact of chosen variables on disintegration time and % CDR at 10 min. The control strategy and optimal region were located using an overlay plot. The pastilles were able to release the drug within 15 min due to faster disintegration. The formulated pastilles were of uniform size, shape, and mechanical strength. The bitter taste of TDL was masked and confirmed by the BATA model. The newer formulation may be helpful in the industry due to its eco-friendly, single-step, and economical process. It unlocks a new direction in the field of oral solid dosage form as an alternative to tablets.

BI-LAMINATED ORAL DISINTEGRATING FILM FOR SYMPTOMATIC TREATMENT OF VIRAL NASOPHARYNGITIS: FORMULATION, CHARACTERIZATION, TASTE MASKING, AND STABILITY STUDIES

Objective: Nasopharyngitis (NP) is one of the most common upper respiratory tract infections (URTIs) brought on by viral infections and requires symptomatic treatment. In this study, a new approach to delivering drugs was developed, which is a bi-laminated oral disintegrating film (ODF) containing dextromethorphan hydrobromide (DEX), phenylephrine hydrochloride (PE), and methylcobalamin (MeCbl) to support the symptomatic treatment of NP. Yet, the extreme bitterness of DEX and PE required a taste-masking technique before ODF formulation to enhance patient compliance. Methods: Various complexing agents were tried at different ratios to mask the bitter taste of the drug(s). DEX-PE ODFs were formulated using the solvent casting procedure. A 31.21 full factorial design was performed to characterize DEX-PE ODFs, where the effects of polymer grade and plasticizer type were evaluated on the disintegration time (DT) and the percentage of drugs released after 10 min (Q10). Results: Complexation with maltodextrin (MD) and ion exchange resin (Kyron T-314) could successfully mask the bitter taste at a ratio of 1:2:2 of drugs, MD, and Kyron T-314, respectively. The ODF optimized formula (F4) recorded the least DT (5±0.5 s) and highest Q10 (96.7±2.1%) and (97.4±1.9%) for DEX and PE, respectively. F4 was then combined with the second film layer containing MeCbl to develop the bi-laminated ODF (B1), which was later evaluated and subjected to stability studies. Conclusion: In conclusion, a taste-masked, bi-laminated ODF could be successfully developed for the symptomatic treatment of NP.

“Fabrication of pellets via extrusion-spheronization for engineered delivery of Famotidine through specialized straws for Paediatrics”

A simple and efficient drug delivery device was designed, viz. specialized straw comprising of famotidine-loaded fast disintegrating pellets. Pediatric dosage forms are designed and developed considering the palatability in children of all ages. This specialized straw was intended for pediatrics presenting with dysphagia or associated symptoms. The pellets were formulated using an extruder spheronization technique incorporated with Kyron T-314 as a super disintegrant. These pellets were characterized for their micromeritic properties, disintegration, and in vitro drug release. The specialized straw was evaluated for various parameters like flow rate of water siphoned through the straw and solvation volume. Pellets were found to have excellent flow properties, disintegration time was found to be 25-30s, and dissolution studies showed 96.1% drug release in 45min. In vitro flow rate was determined to simulate sipping action through this specialized straw. The results indicated that water flowing through the hollow straw at the rate of 13.8±1.3 mLs-1, when tested in prefilled specialized straw, 6.3±1.1 mLs-1 flow rate was observed to be sufficient to dissolve the pellets. Finally, the fast-disintegrating pellets demonstrated excellent in vitro performance and relative ease of manufacturing as compared to other solid dosage forms. Furthermore, the developed specialized straw can be used as a convenient and attractive drug delivery device for pediatrics.

Formulation and Evaluation of Bi-Layer Tablet of Nebivolol and Nateglinide

In the present work, the Bilayered matrix type tablet were prepared by direct and wet granulation technique, in which immediate release layer ( by direct compression) contains Nebivolol and extended release layer (by wet granulation) contains Nateglinide. All the developed bilayer tablets were evaluated for weight variation, friability, thickness and hardness. The percent deviation from the average weight, friability, thickness and hardness was found to be within the prescribed official limits. Release profile of Nebivolol from formulations indicate that lower MCC (Formulations CF1 and CF3) and lactose (Formulation CF3) content displayed higher release rates as compared to formulation with higher MCC and lactose content (Formulation CF2). Also the concentration of KYRON T-314 is also found to influence the release rate of the drug. It was found that formulation containing the highest concentration of superdisintegrants (Formulation CF3) has grater release then other subsequent formulations (Formulations CF1 and CF3). Similarly, the release profile of Nateglinide from formulations indicate that lower HPMC K15M (Formulation CF3) and lactose (Formulation CF3) content displayed higher release rates as compared to formulation with individual HPMC K15M, HPMC K100M, EC (Formulations CF1 and CF2) and higher lactose content (Formulations CF1 and CF2).

Formulation and Optimization of Propranolol Bilayer Tablets: A Potential Approach for Effective Management of Hypertension

The purpose of this investigation is to formulate and evaluate the antihypertensive drug propranolol hydrochloride sustained-release bilayer tablets. In this formulation, one layer provides a loading dose through the immediate release of the drug and the other layer provides a maintenance dose for up to 12 h through controlled release. Different quantities of polymers such as Kyron T-314, Hydroxypropyl methylcellulose- K4M, and ethyl cellulose were used to make bi-layer tablets by direct compression. The compatibility study of pharmaceutical excipients was conducted through Fourier transform infrared spectroscopy studies and no interaction was found. The pre-compression parameter for the angle of repose, bulk density, tapped density and compressibility index was assessed on the produced granules and the findings were good. The tablets were evaluated for the post-compression parameters for thickness, hardness, friability and in vitro release studies. In vitro dissolution study was approved out for 12 h using United States Pharmacopeia dissolution apparatus I using phosphate buffer of pH 1.2 and 6.8 as dissolution medium. Hydroxypropyl methylcellulose- K4M and ethylcellulose were used in combination in all formulations but optimized formulation propranolol hydrochloride tablet 4 showed a higher rate of drug release up to 12 h as compared to the other formulation and optimized formulations propranolol hydrochloride tablet 4 follows the Higuchi model with non-fickian diffusion based on regression coefficient of the kinetics data of cumulative drug release from the dosage form.

Formulation Optimization and Evaluation of Orally Disintegrating Tablets of Moxifloxacin

Oral administration of a pharmacologically active agent is the common and most preferred route among patients suffering from different types of illness. In the market, different type of oral dosage form is available among them tablet is the most favorite and demanded formulation. Further, the tablets, which are easy to use and swallow, are the ideal dosage form like orally disintegrating tablets (ODT’s). The main advantage of this type of formulation is that they can give easily to old aged and under-aged patients. In this research work, ODT’s formulation was manufactured, which get easily disintegrates and gives no bitter taste in the buccal cavity during administration. To achieve this task, moxifloxacin was complexed with suitable ion exchange resins (IER) like Kyron T314. In this course of action, multiple trials were performed using variable percentages or ratio of moxifloxacin and Kyron T 314. The resulting complex powder was characterized by different parameters like IR spectroscopy and differential scanning calorimetry (DSC). Along with the other excipients, drug resin complex (DRC) was used to manufacture the tablets. In this process, two super disintegrants viz. cross povidone and Ac di sol were used, and tablets were prepared by direct compression methodology. The finished product parameters of the tablet were estimated using the different available analytical methodologies. In this research work, it was concluded that the minimum time (19 seconds) for the wetting of tablets was observed when the quantity of crospovidone used was around 10% (MIT05). Additionally, this formulation gives maximum drug release (84.48%) after 120 minutes. Therefore, by using a suitable IER, taste-masked ODT’s of moxifloxacin can be prepared. This method is more efficient and effective in the development of such type of formulations.

Formulation and Evaluation of Oral dispersible Tablet of Paroxetine Hydrochloride

Orodispersible tablets (ODTs) is one such novel approach which helps to increase user acceptance by virtue of rapid disintegration, self-administration without water or chewing. ODTs are solid unit dosage forms like the conventional tablets containing super disintegrants, which help them to disintegrate and/or disperse rapidly in the mouth within few seconds. The orodispersible tablet of Paroxetine hydrochloride was prepared by using direct compression method and the tablet were formulated using various concentration of Kyron T-314 as disintegrating agent, PVP K-30 as binder, F melt Type C as diluent, Sodium Saccharin as sweetening agent, talc as lubricant and Aerosil as glidant respectively. All the batches were prepared according to Factorial design. The prepared tablets were evaluated for various parameters like hardness, dissolution, friability, weight variation, disintegration time. Batch F5 was found to be the best batch as the disintegration time is minimum (26seconds) and better drug release profile. Orodispersible tablets of Paroxetine Hydrochloride were successfully formulated by which first pass metabolism could be avoided and faster onset of action could be achieved.

DEVELOPMENT, EVALUATION AND RP-HPLC METHOD FOR SIMULTANEOUS ESTIMATION OF QUERCETIN, ELLAGIC ACID AND KAEMPFEROL IN A POLYHERBAL FORMULATION

Objective: The current study was planned to develop polyherbal tablet formulation, standardization and evaluation for mitigating the symptoms of polycystic ovarian syndrome (PCOS). To control the issue of PCOS in women by the utilization of newly developed polyherbal tablet formulation.
 Methods: The polyherbal tablets were prepared using a hydroalcoholic extract of the selected medicinal plants viz. Asparagus racemosus, Bauhinia variegata, Caesalpinia bonducella, Saraca asoca, and Symplocos racemosa with the help of a super disintegrant addition technique using crospovidone, kyron T-314 and pregelatinized starch in various percentages. Evaluation assessments such as pre-formulation studies, weight variation, hardness, friability, thickness, disintegration, IR compatibility and simultaneous estimation of quercetin, ellagic acid and kaempferol by RP-HPLC method were done.
 Results: The results reveal that preformulation and evaluation parameters were satisfactory and found to be within an acceptable limit. The Fourier transform infrared spectroscopy (FTIR) compatibility displays no chemical interaction amongst the hydroalcoholic extract of polyherbal formulation and excipients. In simultaneous estimation, the retention time of quercetin, ellagic acid, and kaempferol were found to be 4.86, 6.96 and 10.01 min respectively. The linearity of quercetin, ellagic acid and kaempferol were found in the range of 0-200 µg/ml with correlation coefficients (R2>0.997) within the tested ranges. The LOD and LOQ values of quercetin, ellagic acid and kaempferol were found to be 11.86, 2.63, 5.28 µg/ml and 35.95, 7.98, 16.00 µg/ml respectively. The % RSD values were found to be less than 2 showed the optimized method is precise.
 Conclusion: To conclude, the prepared polyherbal tablet and its quality control analysis revealed satisfactory pharmaceutical properties that fulfill within the limits of pharmacopeial standards. The RP-HPLC method for simultaneous estimation of quercetin, ellagic acid and kaempferol were simple, precise, accurate and consistent for the quantitative analysis and quality control examination of herbal formulations.

Development of medicated chewing gum of taste masked levocetirizine dihydrochloride using different gum bases: in vitro and in vivo evaluation

Objective: The aim of this study was to develop medicated chewing gum (MCG) formulation for taste-masked levocetirizine dihydrochloride (LCZ) that can provide fast drug release into the salivary fluid.Methods: Taste-masked LCZ was first prepared by two methods: cyclodextrin complexation using Kleptose or Captisol and formation of drug resin complex using Kyron T-154 or Kyron T-314 to overcome poor LCZ palatability. MCGs were then prepared using the taste-masked drug, gum base (Artica-T, Chicle, or Health In Gum (HIG), plasticizer (glycerol or soy lecithin at 6 or 8% of the final gum weight). The developed MCGs were evaluated for physical properties, content uniformity, and drug release. Best release MCGs were evaluated thermally to investigate the plasticizer effectiveness and for ex vivo chew out study to confirm adequate drug release. Drug bioavailability was determined for selected formula compared to commercial tablets.Results: Based on taste-masking efficiency, drug/Kleptose complex (1:3 molar ratio) was chosen for incorporation into chewing gums. Physical properties and drug release showed that gum base type, plasticizer type, and level affected not only physical properties but also drug release from MCGs. Thermal study showed decreased glass transition temperature (Tg) with increased plasticizer level. Chew out study confirmed almost complete drug release after a few minutes of chewing. Pharmacokinetic results showed shorter tmax (0.585 vs. 1.375 h) and higher Cmax (0.113 vs. 0.0765 μg/mL) for MCGs than conventional tablets.Conclusion: Results provided evidence that MCGs could be a better alternative to conventional tablet formulations with improved bioavailability and enhanced palatability.

Development and In Vitro Evaluation of Buccal Effervescent Tablet Containing Ropinirole Hydrochloride

The buccal delivery is an attractive route to improve the clinical efficacy of ropinirole hydrochloride (RH) for the treatment of Parkinson and restless syndrome since this drug undergoes extensive first-pass effect, which has only 50% bioavailability after oral administration. The purpose of this study was to develop and optimize the formulation of fast disintegrating buccal effervescent tablets of RH using four types of superdisintegrants. The direct compression method was used to develop four different formulas containing RH using Kyron T-314, crospovidone, croscarmellose sodium, and sodium starch glycolate separately as a superdisintegrant. Sodium bicarbonate and citric acid were added to the formulations to produce effervescence, while sodium carbonate was used as a pH adjusting agent. All the prepared formulas were evaluated, in terms of weight variation, friability, content dose uniformity, hardness, disintegration, and dissolution test. The best formulation was selected for the subsequent study. The obtained results from pre-compression studies were in acceptable range according to British Pharmacopoeia. All formulas passed through the quality control test and significant difference (P < 0.05) was observed for the formula four compared to other formulas, due to the presence of Kyron T-314 as a superdisintegrant in formulation number 4. RH cloud be prepared as a buccal effervescent tablet and superdisintegrant provide fast disintegration of the tablet to exert rapid action.

Formulation and Optimization of Orodispersible Tablet of Loratadine Using Box Behnken Design

In present study Orodispersible tablets (ORDT) of Loratadine were prepared and optimized. Solid dispersion of Loratadine- β cyclodextrin complex were prepared and used in preparation of Orodispersible tablets. Various super-disintegrating agent like Cross carmellose sodium, Cross povidone and Kyron T-314 were employed for faster disintegrating effect. The 24 factorial and Box-Behnken design were utilized to optimize the tablet formulation. The Orodispersible tablet of Loratadine was optimized by Box Behnken Design, where concentrations Kyron T-314, CRP and Pearlitol SD200 were employed and its effect on Disintegration time (DT), Wetting time (WT) and % drug release at 20 min (Q20) was evaluated. Precompression parameters like angle of repose, bulk density, % compressibility, Hausner’s ratio was studies. The different batches of Orodispersable tablets were prepared and evaluated for disintegration time, friability, wetting time and drug release studies. Different batches prepared showed disintegration time in the range of 23 ± 2.52 to 59 ± 2.64, wetting time in between 27± 0.57 to 66.3 ± 3.4, drug release (Q 20) in between 86.1 ± 0.6 to 96.7 ± 0.4 in 20 min., friability less than 1 % and hardness 3.4 to 4.2 Kg/cm2. The optimized formula when compared with marketed product it showed faster disintegration time and rapid drug dissolution in phosphate buffer 6.8. The solid dispersion of Loratadine not only helped improve in solubility but may also help in taste masking. Keywords: Orodispersible tablets, Loratadine, β cyclodextrin Solid dispersion

FORMULATION OF ORALLY DISINTEGRATING TABLETS OF CINNARIZINE BY USING DIRECT COMPRESSION METHOD

Objective: The aim of this work was to formulate and evaluate orally disintegrating tablets of cinnarizine that were prepared by direct compression method using different types of diluents and super disintegrants. The rationale behind this work was to accelerate the disintegration of the tablet to provide rapid dissolution, quick action and enhanced bioavailability of the drug.Methods: The tablets were prepared by direct compression method using different types of diluents as mannitol, microcrystalline cellulose (MCC), and lactose. Different super disintegrants were used such as crospovidone (CP), sodium starch glycolate (SSG) and Kyron T-314; Kyron T-314 was used in different concentrations of 5%, 6%, 7%, and 8%. The prepared formulae (F1-F9c) were subjected to flowability studies and post-compression evaluation studies. The optimized formula was selected depending on the time of disintegration and dissolution; then it was subjected to drug-excipient compatibility study and stability study.Results: Flowability results were ranging from excellent, excellent to good, and good to fair according to the type of the diluent used. All of the prepared tablets showed acceptable hardness, friability, drug content, and disintegration. A rapid disintegration of 11.66±2.25 s with the highest percentage 2 min-drug release of 74.55±3.01% was obtained by using the diluent lactose and the super disintegrant Kyron T-314 (8%) in the formula F9c. The infrared spectroscopic studies of the formula F9c showed no drug-excipient interaction. In addition, the stability study indicated that the optimized formula is a stable formula.Conclusion: Formula F9c of a rapidly disintegrating tablet was easy to be manufactured, and the results showed that this formula had a rapid disintegration, high dissolution profile, no noticeable chemical incompatibility and it was stable upon storage.

Formulation and evaluation of orodispersible tablets of lornoxicam

Orodispersible tablets (ODTs), also known as fast melt, quick melts, fast disintegrating have the unique property of disintegrating in the mouth in seconds without chewing and the need of water. The purpose of this investigation was to develop mouth dissolving tablets of Lornoxicam using KYRON T-314 (Polacrillin Potassium) as a novel superdisintegrant. Mouth dissolving tablets of lornoxicam were prepared by wet granulation technique using KYRON T-314 as superdisintegrant and menthol as subliming agent. The present study demonstrated potentials for rapid absorption, improved bioavailability, effective therapy and patient compliance.
 Keywords: KYRON T-314, Mouth dissolving tablet, Lornoxicam, Subliming agent, Superdisintegrant

Antibiotic evaluation of odontogenic microbiological spectrum of orofacial infection

The present study aimed towards the development of active delivery system for management of hypertension. The Orodispersible tablets (ODTs) containing Telmisartan was developed in order to accomplish enhanced solubility leading to better bioavailability profile. Different ratios, of Telmisartan and PEG 6000 i.e. 1:1, 1:2, 1:3, 1:4 and 1:5 were selected for the formulation of ODT system. A batch process was adopted for the preparation of solid dispersion with each combination of drug and polymer and the finally compressed as tablets by direct compression technique. For the preformulation perspective materials were scrutinized on the basis of solubility profile, drug content, Fourier Transform Infrared (FTIR) spectroscopy and Differential scanning calorimetry (DSC). The drug polymer ratio 1:4 was selected for further compression process. The prepared batches of ODTs were characterized for micromeritic study, thickness, hardness, weight variation, wetting time, disintegration time, drug content and in vitro drug release profile. The evaluation data for all batches was satisfactory out of them formulation TF3 containing 6% kyron T-314 showed the best results with a value of 29.3 sec and 24.1 sec for wetting and disintegration, respectively. This formulation showed superior drug release of 99.93% over a period of 30 minutes.
 Keywords: Telmisartan, PEG 6000, Angioten receptor-II antagonist, Solid dispersion, Kyron T-314

Development and optimization of orodispersible tablets using solid dispersion of Telmisartan

The present study aimed towards the development of active delivery system for management of hypertension. The Orodispersible tablets (ODTs) containing Telmisartan was developed in order to accomplish enhanced solubility leading to better bioavailability profile. Different ratios, of Telmisartan and PEG 6000 i.e. 1:1, 1:2, 1:3, 1:4 and 1:5 were selected for the formulation of ODT system. A batch process was adopted for the preparation of solid dispersion with each combination of drug and polymer and the finally compressed as tablets by direct compression technique. For the preformulation perspective materials were scrutinized on the basis of solubility profile, drug content, Fourier Transform Infrared (FTIR) spectroscopy and Differential scanning calorimetry (DSC). The drug polymer ratio 1:4 was selected for further compression process. The prepared batches of ODTs were characterized for micromeritic study, thickness, hardness, weight variation, wetting time, disintegration time, drug content and in vitro drug release profile. The evaluation data for all batches was satisfactory out of them formulation TF3 containing 6% kyron T-314 showed the best results with a value of 29.3 sec and 24.1 sec for wetting and disintegration, respectively. This formulation showed superior drug release of 99.93% over a period of 30 minutes.

Influence of Various Disintegrants on the Quality of Microcrystalline Cellulose Tablets

The effects of the superdisintegrants sodium starch glycolate, croscarmellose sodium, polacrilin potassium Kyron T-314, and Amberlite IRP 88 on the quality parameters of placebo tablets prepared from microcrystalline cellulose were studied. Sodium starch glycolate was most effective with croscarmellose sodium and Amberlite IRP 88 slightly less. All studied disintegrants gave dosage forms of pharmacopoeial quality. The effects of disintegrant concentration and particle type on tablet hardness were determined. The dosage form hardness increased with increasing disintegrant content for croscarmellose sodium with fibrous particles and decreased for sodium starch glycolate and polacrilin potassium with round and irregularly shaped particles. The tablets were harder if polacrilin potassium was added to the formulation.

Development and Evaluation of Melt-in-Mouth Tablets of Metoclopramide Hydrochloride Using Novel Co-processed Superdisintegrants.

In the present investigation, a novel multifunctional co-processed superdisintegrants consisting of crospovidone and Kyron T-314 were fabricated by solvent evaporation method to develop melt-in-mouth tablets of metoclopramide hydrochloride with a view to enhance patient compliance by direct compression method. The simple physical blends and co-processed mixture of superdisintegrants were characterized for angle of repose, bulk density, tapped density, Carr's index, Hausner's ratio and compatibility studies by FTIR spectroscopy. Melt-in-mouth tablets of metoclopramide hydrochloride were prepared using the physical blends and co-processed mixture of superdisinterants and were evaluated for hardness, friability, in vitro disintegration time, in vitro dispersion time, wetting time, water absorption ratio, drug content, in vitro drug release and accelerated stability study at 40±2° temperature and 75±5% relative humidity. Among the tablets evaluated, formulation F-X prepared by adding co-processed superdisintegrants in ratio of 1:1 showed minimum in vitro dispersion time of 9.71±0.021 s, in vitro disintegration time of 5.70±0.117 s and higher amount of drug release of 99.695±0.29% at the end of 1 min. Formulation F-X was emerged as the overall best formulation based on drug release characteristics in pH 6.8 phosphate buffer compared with the tablets obtained from conventional method of manufacture as well as with marketed preparation. Analysis of drug release data indicated that formulation F-X followed first order kinetics. This study revealed that the co-processed mixture of superdisintegrants have excellent flow properties, high compressibility, render low disintegration time to tablets and have better binding properties as compared to physical blends of superdisintegrants. These materials can be a good substitute for inert superdisintegrants, which are normally used in tablet manufacturing.

Formulation and Evaluation of Rosuvastatin Immediate Release Tablets 10 Mg

Rosuvastatin is a member of the drug class statins, used to treat high cholesterol and to prevent cardiovascular disease. It comes under class II of Biopharmaceutical Classification System. The objective of present study is to develop Rosuvastatin immediate release tablets 10 mg using different types of superdisintegrants to enhance the disintegration time and dissolution of Rosuvastatin calcium to improve bioavailability of the drug. In the present study immediate release formulation of Rosuvastatin calcium was prepared by wet granulation method that are cost effective. Different formulations were made by using various concentrations of superdisintegrants such as Crospovidone, Sodium Starch Glycolate and Kyron T-314 (Polacrillin Potassium). The Prepared formulations were evaluated for the physical characteristics, in vitro dissolution and stability at 40°C/ 75% RH for six months. Among all the formulations F2 (containing 4.5% of super disintegrants i.e., crospovidone) was considered to be the best formulation, which releases up to 102.4% drug in 30 minutes. From this study we can conclude that, formulated tablets of Rosuvastatin containing crospovidone are better and effective than conventional tablets to meet patient compliance.

Optimization of Melt in Mouth Tablets of Palonosetron HCl using 32 Full Factorial Design

Palonosetron HCl is a 5HT3 antagonist licensed for the prevention of acute chemotherapy-induced nausea and vomiting (CINV) associated with highly emetogenic chemotherapy agents (HEC) and the prevention of CINV associated with moderately emetogenic cancer chemotherapy (MEC). It has a substantially longer half-life (Approximately 40 h). So, it was plan to prepare melt in mouth tablet which could rapidly dissolved and absorbed which may produce rapid onset of action. Melt in mouth tablets were prepared by direct compression method using various superdisintegrants like Kyron T314 and Vivasol, and evaluated for pre compression and post compression parameters. A 32 full factorial design was applied systematically to optimize responses. The concentration of Kyron T314 (X1) and concentration of Vivasol (X2) were selected as independent variables and disintegration time (Y1) and wetting time (Y2) as dependent variables. The prepared tablets were evaluated for hardness, friability, disintegration time, wetting time, drug content and in vitro drug release. The results indicated that concentration of (X1) and (X2) significantly affected (Y1) and (Y2). Regression analysis and numerical optimization were performed to identify the best formulation. Similarity (f2) and dissimilarity (f1) study for optimization batch was also carried out. Batch P9 was found to be best batch with 10.43 s. disintegration time, 19.53 s. wetting time and 99.02% drug release in 30 min. There was no drastic change in the result of tablets of optimized batch at end of six month accelerated stability study.

FORMULATION AND EVALUATION OF BILAYER TABLETS OF BACLOFEN USING SYNTHETIC POLYMERS

Aim of study was to develop bilayer drug delivery for treatment of spasticity by delivering loading and maintenance dose for fast achievement of peak plasma concentration and maintaining the same respectively. The prepared drug loaded bilayer tablets were evaluated for pre and post compression parameters. Stability study of the promising formulation was also performed. The tablets were prepared by direct compression and wet granulation method. The loading dose was delivered in the form of immediate release layer prepared by different super-disintegrations and maintenance dose was delivered through sustained release layer prepared by using polymers like HPMC K4, HPMC K15M, HPMC K100, PEO WSR 303 and Precirol. Both the immediate release layer and sustained release layers were separately optimized and then combined to optimize the bilayertablets. No interactions were found between drug and excipients. Formulation containing Kyron T314 shows immediate drug release. Formulation Containing PEO WSR 303 shows sustained release action and bilayer formulations F6 shows releases up to 24 hours. Bilayer tablets with release characteristics offer critical advantages such as, site specificity with improved absorption and efficacy.Key words: Baclofen, Bilayer tablet, sustain release tablet