Post-compression Parameters Research Articles

Formulation, In-vitro and In-vivo Evaluation of Chronology-based Mucoadhesive Drug Delivery System of an Antihypertensive Drug

Current research aimed to prepare and estimate chronology-based mucoadhesive PDDS of antihypertensive drug losartan potassium through formulation of fast-dissolving core tablet and incorporation of core tablet to polymer coating to formulate bioadhesive PDDS through direct compression system. The coating was done by using polymers ethyl cellulose and carbopol 934. Pre-compression and post-compression parameters, drug release, lag time and mucoadhesive examination was assessed for the formulation. The expected lag time for hypertension is 8 hours; hence, this lag time was achieved by using a bioadhesive pulsatile system. The optimized formulation showed 8 hours lag time with appropriate mucoadhesion for an equivalent period. Moreover, in-vitro as well as in-vivo mucoadhesion investigations reflected the positive outcomes. Consequently, the BPDDS was the finest preventative substitute for drugs with the highest absorption in the stomach and for drugs used to treat diseases related to circadian rhythm

Fast Dissolving Tablets of Promethazine Theoclate: Optimization by Box Behnken Design

HThe current work was planned to optimize promethazine theoclate fast-dissolving tablets using Box Behnken design. The effect of three independent factors, the concentration of camphor (sublimating agent), sodium starch glycolate (superdisintegrant) and β-cyclodextrin (solubility enhancer) on two responses, disintegration time and percent drug release was studied. A total of 27 formulations were prepared and tested for various precompression and postcompression parameters. The correlation between factors and responses was established by plotting contour plots. The independent variables, the concentration of camphor and sodium starch glycolate, have a significant influence on response disintegration time, whereas the factor, concentration of β-cyclodextrin, has an effect on the response and percent drug release.

Formulation Development and Evaluation of Ubidecarenone Chewable Tablet

Background: Coenzyme Q10 has a role in mitochondrial transport system and can be utilized as a supplement in migraine prevention. This study's objective is to assess Coenzyme Q10's effectiveness when used in conjunction with conventional medications to prevent migraines. Adding 300mg of coenzyme Q10 each day to prescription medications, while another group of patients continued receiving standard care. Over the course of a three-month treatment period, data on attack frequency, headache pain intensity, monthly migraine days, and associated symptoms like nausea, vomiting, phonophobia, and photophobia were analyses. Ubidecarenone, a medicinal component. The goal is to produce Ubidecarenone in a 300 mg chew-able tablet form. In vitro release studies and organoleptic properties, such as taste and flavour, will be evaluated. investigations in the early stages, tests for medicine excipient compatibility, and analyses of the water content Quality Assurance for the Process Hausner's Ratio, Bulk Density, Tapped Density, Comprehensibility Index, and Angle of Repose for calculating derived properties for medications and mixtures. ingredients that have been optimised for their concentrations, such as tastes, sweeteners, disintegrants, wetting agents, glidants, and lubricants. putting the best possible ingredients together to make a chew able pill. Evaluation of chewable tablets for post compression parameters including uniformity of weight, thickness, hardness, brittleness, friability, dissolution, assay, and in vitro drug release properties. An evaluation of the optimised batch's palatability is required. The intention is to create chewable tablets of ubidecarenone. Method: The wet granulation method is used to make chewable tablets of ubidecarenone. Mannitol is used as a diluent, crospovidone as a disintegrant agent, sodium starch as a disintegrate agent, saccharin sodium as a sucrose sweetener, orange flavour, peppermint oil as a flouring agent, and colloidal silicon dioxide as a gliding. The Ubidecarenone (300 mg) is one of the best first-line treatments for migraine prevention.

Exploring magnesium myristate for its dual functionality as a binder and lubricant in the formulation of tablet.

Purpose: To explore 'magnesium myristate' for its dual functionality as a lubricant and binder in the formulation of tablets. Methods: Using (DoE), tablet formulations using magnesium myristate and conventional excipients (magnesium stearate and PVP K30) were developed by wet granulation technique. The prepared granules and formulated tablets were evaluated for pre- and post-compression parameters, respectively. Results: Magnesium myristate exhibited excellent flow properties. The optimized formulations containing magnesium myristate exhibited increased hardness and in vitro drug release in comparison to conventional excipients. f2 similarity index for in vitro drug release showed no significant variations with optimized formulations and with the marketed formulations. Conclusion: Magnesium myristate shows a promising replacement for conventional excipients as both a lubricant and binder in tablet formulation.

Formulation and evaluation of floating tablet of nimesulide by direct compression method

Nimesulide has been used versatile on fever, pain, inflammation, rheumatoid arthritis, tendinitis, thrombophlebitis and trauma. Common drawbacks of conventional tablet dosage forms of nimesulide show an irritant effect on the stomach due to its weakly acidic nature along it has short duration of action leading to poor bioavailability. A Floating drug delivery system for Nimesulide leads to overcoming the problem related to an irritant on the stomach by avoiding direct contact with the mucosa. Thus, this study was designed and performed to formulate and evaluate the floating tablet of Nimesulide and determine the release pattern of the prepared formulation. Tablets were prepared by direct compression method using different polymers (HPMC, carbopol, and guar gum), either in an individual or in combination. The formulation blend was subjected to various pre-formulation and post-formulation studies including floating lag time, total floating time, hardness, friability, drug content, weight uniformity, and in-vitro dissolution. According to pre- pre-formulation study, the flow property was found to be good to passable. Similarly, all post-compression parameters of floating tablets were found to be within acceptable limits except the friability test of F1 and F2 formulations. The tablet’s floating lag time was determined to be in the range of 7-153.5 seconds, and the total floating time was in the range of 4-7 hrs. From the data of dissolution, carbopol showed a slower release of drugs than that of HPMC and guar gum. The use of carbopol as a floating polymer showed release of drugs from dosage form was 84.46% in 7 hrs and 99.10% in 3 hrs with the use of HPMC, 96.39% in 4 hrs with the use of guar gum. A combination of HPMC and guar gum released drugs in a slow release of drugs only for 3 hrs i.e. 98.02% in 3 hrs, the combination of carbopol and HPMC slowly released drugs for 6 hrs i.e. 90.43% in 6 hrs, and the combination of carbopol and guar gum showed maximum slow release of drugs for greater than 7 hrs i.e.74.16% in 7hrs. Hence, among all the formulations, F7 with the combination of carbopol and guar gum as polymer showed a maximum slowed release effect for greater than 7 hrs, which can be taken as the best batch.

OPTIMIZATION AND CHARACTERIZATION OF FAST DISSOLVING TABLETS OF CANDESARTAN CILEXETIL PREPARED FROM SPHERICAL AGGLOMERATES

The primary objective of this study was to develop a rapidly dissolving tablet containing an antihypertensive drug, candesartan cilexetil (CAND). The research work focused on improving solubility and in vitro dissolution of drugs using spherical agglomeration technique. Spherical agglomerates of CAND were developed using PVPK-30 as polymer and dichloromethane as bridging liquid. A spherical agglomerate of CAND was used to formulate fast dissolving tablet (FDT) with different superdisintegrants like Crospovidone and Cross carmellose sodium. The prepared powder blend was evaluated for different pre-compression parameters like solubility, compressibility index, Hausner’s ratio and flow property and post-compression parameters including in vitro dissolution study. The solubility of prepared agglomerates was found to be 0.15 to 0.91 mg mL-1, and it was higher than the pure drug (0.00071 mg mL-1). In vitro drug release study of optimized batch of FDT has shown 95.47 % of drug release. From the results, it was revealed that the prepared FDT using the agglomeration technique might be used to enhance the solubility and bioavailability of CAND to augment acute and chronic hypertension therapy.

FORMULATION DEVELOPMENT AND INVITRO EVALUATION OF PERAMPANEL IMMEDIATE RELEASE TABLETS

The aim of the present study is to develop and evaluate the immediate release tablet of Perampanel by direct compression method. The superdisintegrant crospovidone (CP), croscarmellose sodium (CCS) and sodium starch glycolate (SSG) were used for immediate release of drug from tablet. The prepared tablets were evaluated for all pre-compression parameters and post-compression parameters. The drug excipients interaction was investigated by FTIR. All formulation showed compliances with Pharmacopoeial standards. The study reveals that formulations prepared by direct compression F3 exhibit highest dissolution using crospovidone showed faster drug release 99.13 % over the period of 45min.

DEVELOPMENT OF CONTROLLED RELEASE FORMULATIONS OF DEXLANSOPRAZOLE TO IMPROVE BIOAVAILABILITY

The present work was aimed to development of controlled release formulations of Dexlansoprazole to improve bioavailability. Dexlansoprazole is the proton pump inhibitor that suppresses gastric acid secretion by specific inhibition of the H+/K+-ATPase in the gastric parietal cell. By acting specifically on the proton pump, Dexlansoprazole blocks the final step in acid production, thus reducing gastric acidity. Construction of calibration curve of Dexlansoprazole and to investigate the drug and polymer interaction studies by FTIR and DSC. To prepare the different controlled release formulations of Dexlansoprazole tablets with different polymers such as acrylic acid polymer such as Carbopol-974P, HPMC grades for prevalence HPMC-K4M, HPMC-K15M, HPMCK100M, Natural Polymers akin to Xanthan gum, Guar gum, Sodium Carboxy Methyl Cellulose, and Pectin by Direct Compression method. Evaluation of Dexlansoprazole pre compression parameters such as Bulk density, Tapped density, Hausner’s ratio, Carr’s index, Angle of repose. Evaluation of post-compression parameters of Dexlansoprazole controlled release tablets such as Weight variation, Hardness, Friability test, Thickness, Drug Content and In-vitro dissolution studies. Evaluation of in-vitro dissolution uniqueness of all the formulations of Dexlansoprazole by using USP dissolution apparatus type-II (paddle). To study the mechanism of drug dissolution by applying kinetic parameters. To perform the stability studies of optimized formulations of Dexlansoprazole as per ICH guidelines.

Formulation and Drug Release Study of Rivaroxaban Oral Disintegrating Tablets Using Various Super-Disintegrants

This study aims to improve Rivaroxaban's solubility, dissolution, and bioavailability. Orally disintegrating tablets (ODTs) made with super-disintegrants like crospovidone, sodium starch glycolate, and cross-carmellose sodium will do this. Tablet preparation used direct compression and formulation optimization with design expert software. After a thorough factorial design and evaluation of pre- and post-compression parameters, the F3 batch, which contained Rivaroxaban (7.97%), Crospovidone (3.59%), Croscarmellose sodium (5.18%), Sodium Starch Glycolate (5.18%), Lactose Anhydrous (31.08%), Mannitol (15.94%), MCC (27.89%), SSF (1.59%), and Talc (1.59%), was the best. The enhanced tablet formulation (F3) showed positive qualities, including 3.3 kg/cm² hardness, 23 seconds disintegration time, and 99% drug release after 30 minutes. The innovative Rivaroxaban orally disintegrating tablet (ODT) method disintegrated and dissolved faster than market forms. Rivaroxaban's physical and chemical properties were assessed before formulation. The medication was colorless, scentless, crystalline, and melted at 227°C-229°C, as described in published research. The pharmaceutical was found to be a BCS Class II drug with low water solubility and high solubility in acetate buffer pH 4.5 and 0.1 N Hydrochloric acid. Fourier-transform infrared spectroscopy (FTIR) confirmed no drug-polymer-excipient interactions. Every batch of tablets exhibited uniform thickness (3.5 mm to 3.8 mm) and diameter (10.31 mm to 10.36 mm), indicating good compression without adhering to shaping tools. All samples had a 3-5 kg cm-² hardness, indicating strong mechanical properties. The Roche friability method showed that all batches had good abrasion resistance, ranging from 0.1% to 0.5%. Variations in croscarmellose sodium and crospovidone on tablet disintegration time and hardness were examined using design expert software. The ANOVA showed important factors affecting these attributes. Data-driven polynomial equations predict tablet disintegration time and hardness. These models reveal formulation parameters that affect tablet performance. Thus, the improved F3 batch of rivaroxaban orally disintegrating tablets (ODTs) improves solubility, dissolving, and bioavailability. This may improve treatment outcomes.

Effect of Croscormellose Sodium in Sustained Release Layer of Valsartan in Bilayer Tablet with Clopidogrel as Immediate Drug Release and Valsartan as Sustained Drug Release

The aim of the study was to design and evaluate bilayer tablets of clopidogrel as immediate release and quick relief and valsartan for sustained release and check the effect of croscarmellose sodium (2%) in Carbopol for sustained release action. Bilayer tablets was prepared using direct compression method. Super disintegrants such as Crospovidone, Croscarmellose sodium were evaluated for immediate release of clopidogrel. Polymers HPMC K4, guar gum, ethyl cellulose and carbopol for controlling release of Valsartan. The compressed bilayer tablets were evaluated for weight variation, thickness, hardness, friability, drug content and in vitro drug release in 0.1N HCl and phosphate buffer pH 6.8. All the pre and post compression parameters were found to be within the acceptable limits. The formulations were optimized based on results of dissolution and formulations CF5 for immediate release & VF11 for sustained release. VF11 was formulated with addition of superdisentigrant and showed better controlled release and dissolution similar to VF8. The release kinetics of Valsartan was subject to curve fitting analysis in order to identify the best fit kinetic model. The regression analysis proves that VF11 follow first order release and drug release by diffusion process based on Fick’s law of diffusion. The data for stability studies infer no considerable change in drug content, dissolution rates and other quality control test were within limits.
 Keywords: Bilayer tablets, clopidogrel, valsartan, direct compression method.

Physicochemical reports of gliclazide-carplex solid dispersions and tablets prepared with directly compressible co-processed excipients

ObjectivesThe main goal of this research was to develop better tablet formulations by utilizing solid dispersions (SDs) and coprocessing excipients composite to achieve a better release rate of poor water-soluble gliclazide. MethodsThe solvent evaporation method made SDs of gliclazide with different carriers carplex 67, carplex 80, and carplex FPS 500 (weight ratio, 1:1). The drug release patterns of the SDs were all evaluated and optimized. The SDs were illustrated by using scanning electron microscopy (SEM), differential scanning calorimetry (DSC), X-ray powder diffraction (PXRD), and Fourier transform infrared spectroscopy (FTIR). Tablet batches FGC-1 to 8 were made using gliclazide-carplex 67 solid dispersions (GC67-SDs) and the co-processed composite of excipients, namely starch-MCC-povidone (SMP) and lactose-MCC-povidone-sodium starch glycolate (LMPS), prepared with coprocessing technology. We evaluated these batches by conducting physicochemical tests and comparing them to the existing commercial brand. ResultsIn a water medium, the release of gliclazide from SDs peaked within the first 30 min, showing a roughly 5∼6-fold increase compared to plain gliclazide. This quick dissolution rate may be due to the amorphization of the drug, which improved the specific surface area, and increased wettability caused by the hydrophilic properties of carplex particles. This has been confirmed through SEM, DSC, FTIR, and PXRD analysis. All FGC formulations had satisfactory pre-compression factor results, while the post-compression parameters indicated good mechanical strength and homogeneity across the blend. All produced tablets met the weight variation, friability, and disintegration time limit set by the compendia. Through in vitro drug release testing, it was discovered that all FGC tablet batches had consistent and nearly identical release results compared to SDs of gliclazide. However, the FGC-5 to 8 batches containing LMPS composites were determined to be the most effective formulations. In the first 30 min in a water medium, the percentage of drug generated from the FGC-8 tablets involving GC67-SDs and co-processed composite LMPS-4 is approximately 3.5 times higher than the average release of currently marketed products (MPs). After storing the selected FGC tablet batches for three months at 40 °C and 75 % RH, there were no noticeable alterations in the amount of drug and drug release profiles across the batches. ConclusionBased on these findings, it appears that using the carplex silica-based SDs approach, along with gliclazide and co-processing excipients composite, could result in significant benefits compared to the current commercial brands. This approach could be effectively utilized to create solid dosage forms for drugs that have low solubility in water.

Design and evaluation of herbal tablet formulation (HTF) of leaves of Carica papaya linn, Moringa oleifera linn and fruit of Carrissa carandus lam

The objective of the research paper to design and development of herbal tablet formulation (HTF) of leaves of Carica Papaya Linn (LCPL) & Moringao leiferaLinn (LMOL) and fruit part of Carrissa CarandusLam (FCCL).Powdered leaves of Carica Papaya Linn & Moringao leifera Linn and fruit part of Carrissa Carandus Lam was macerated in 80% hydro-ethanolic solution for 72 hours .To identify the active constituents, phyto-chemical screening was performed. The extracts were evaluated for the flavonoid and phenolic content by qualitative and quantitative measurement. The Leaves of LCPL& LMOL and fruit of FCCL was extracted by maceration process. Preliminary phytochemical screening was performed. The LCPL showed the presence of flavonoids, phenol, proteins, glycosides, and alkaloids. The LMOL has shown the presence of phenolic compounds, flavonoids, carbohydrates, proteins, amino acids, terpenoids and tannins. The FCCL has shown the presence of phenolic compounds, flavonoids, carbohydrates, terpenoids, glycosides, alkaloids and tannins. Total flavonoid content and phenolic content was present as gallic acid and Iso-quercetin respectively. The herbal tablet formulation was prepared by wet granulation method utilizing the different proportion of the plant extract. The evaluation of Herbal tablet formulation stated that HTF-3 formulation has shown the best result in pre-compression and post-compression parameters. The hydro ethanolic extract of LCPL, LMOL and FCCL show the presence of different flavonoid and phenolic content i.e., Iso-quercetin, gallic acid. The Three different batches of HTF were prepared and result data indicates that developed formulation has been approved, suitable for oral administration and pharmacological evaluation.

Formulation and evaluation of oral dispersible tablet of nimesulide by direct compression method

Based on Biopharmaceutics Classification System (BCS), nimesulide is a class II drug, characterized by low solubility and high permeability. Thus, its dissolution represents a limiting step in the drug absorption process which directly affects the bioavailability of the drug. Oral Dispersible tablets (ODTs) of nimesulide overcome the problem related to dissolution by enhancing the rate of dissolution by decreasing the disintegration time and making it easy to administer to patients who refuse to swallow a tablet. In the present study, different formulations of nimesulide were prepared to vary the concentration of superdisintegrants: crospovidone, croscarmellose sodium, sodium starch glycolate along with other excipients: PVP K-30, Aerosil, Mannitol, and Magnesium stearate by direct compression method. Precompression and post-compression parameters were evaluated and also the effect of different concentrations of superdisintegrants on the release profile of Nimesulide ODT was studied. The final data revealed that a combination of 10% crospovidone and 8.33% SSG i.e. formulation B4 was found best combination with the lowest dispersion time of 40 seconds, lowest disintegration time of 19.16 seconds, and lowest wetting time of 15 seconds as compared to other formulations. All other studied parameters were found to be satisfactory for all ODT formulations for Nimesulide. It was concluded that Nimesulide can be successfully formulated as oral dispersible tablets using various superdisintegrants in different concentrations by direct compression method. The optimized batch can be subjected to real-time and accelerated stability studies to determine the shelf life for commercial use.

Formulation and Evaluation of Paracetamol Tablet to Assess Binding Property of Limonia acidissima Pectin

Plants acts as a major source of medicines and are used to formulate various pharmaceutical preparations. Apart from this they act as excellent pharmaceutical aids and excipients.Limonia acidissima is nutritious, easily available, cheap but underutilized fruit. The aim of present research is to isolate the pectin from dried fruit pulp of Limonia acidissima and to assess its binding property. Pectin was extracted by boiling dried fruit pulp powder with water for 7 hrs at pH 3.2 adjusted with citric acid and using ethanol as precipitating agent. Binding property of pectin was assessed using paracetamol as a model drug. Paracetamol granules were prepared by wet granulationmethod. Granules were prepared using starch as disintegrant, calcium carbonate as filler, talc as glidant, Magnesiumstearate as lubricant and varying concentration of pectin as binder and were compressed into respective tablets.A reference batch of starch as binder was prepared to carry out the comparative study and to assess the binding property of pectin. Total four batches of formulation were prepared using different concentrations of pectin. For each formulation pre compression and post compression studies were performed and compared to range asper pharmacopoeias. Tablets were evaluated based on Weight uniformity, Tablet Hardness, Friability, Disintegration and In vitro drug release. The results obtained for all pre-compression and post compression parameters were found within acceptable range of pharmacopoeias. Limonia acidissima pectin can act as excellent binder in dosage forms. In vitro dissolution studies were revealed that batch F3 showed 99.64 % of drug release. In pharmaceutical dosage form like tablet, Limonia acidissima pectin acts as an excellent binder since it is of natural origin and Limonia acidissima fruits were available easily at very low costand proved to be better alternative for synthetic binder.

Formulation development and evaluation of omeprazole buccal tablets

Omeprazole is a medication used in the treatment of gastroesophageal reflux disease (GERD), peptic ulcer disease, and Zollinger–Ellison syndrome. It is also used to prevent upper gastrointestinal bleeding in people who are at high risk. The Mucoadhesive buccal tablets were prepared by direct compression method using Sodium Alginate, HPMC K4M and SCMC as mucoadhesive polymer. The compatibility studies of drug and excipients were performed by FT-IR spectroscopy. After examining the flow properties of the powder blends the results are found to be within prescribed limits and indicated good flowing property, hence it was subjected to tablet compression. The tablets were evaluated for post compression parameters like weight variation, hardness, thickness, friability, drug content uniformity, Surface pH, in-vitro studies like drug release. Formulation (F4) containing HPMC K4M in the ratio of (1:1) showed maximum drug release of 99.54% in 8 hrs. The drug content of shown highest of 99.61 %, Surface pH was found to be 6.05. All the evaluation parameters given the positive results and comply with the standards. The results indicate that the mucoadhesive buccal tablets of Omeprazole may be good choice to bypass the extensive hepatic first pass metabolism with an improvement in the bioavailability of Omeprazole through buccal mucosa.

In vivo Evaluation for the Anticoagulant Activity of Dipyridamole Matrix Tablets

Dipyridamole (DYP) is potent drug that prevents the thromboembolic risk. It has been clinically used for chronic treatment of angina pectoris treatment and during the valve replacement. heart valve replacement and long-term angina pectoris treatment and is well absorbed in the stomach with BCS class II drug and low oral bioavailability. The present research investigation was focused on the formulation of matrix tablets of Dipyridamole cocrystals and the evaluation of In vivo anticoagulant activity. The results of the study showed that the formulated matrix tablets of dipyridamole cocrystals showed improved efficacy in comparison with the plain drug by enhancing the pre-compression parameters such as bulk density, tap density, Carr's index, angle of repose and Hausner's ratio and post-compression parameters like thickness and weight variation, hardness and friability, In vitro dissolution parameters. The improved efficacy was confirmed by improvement in the pharmacodynamic parameters such as cutaneous bleeding time and clotting time indicative of enhanced bioavailability of dipyridamole. Thus, it can be concluded that the dipyridamole matrix tablets prove to be more effective in producing the anticoagulant effect in clinical practice as compared to the plain drug resulting in more patient compliance.

Formulation development and evaluation of controlled release matrix tablets of glibenclamide

The present study aimed to formulate and evaluate the controlled-release matrix tablets of Glibenclamide which is an antidiabetic drug that belongs to the second-generation oral hypoglycemics. Matrix tablets were prepared by three different polymers as sustained-release agents, using Glibenclamide as a model drug. Three polymers were selected for this study- HPMC K 15, HPMC K 100, and EC in different drug: polymer ratios. The drug was identified by FTIR spectroscopic method. The pre-compression and post-compression parameters of all formulations were found to be within acceptable limits. The release rate of Glibenclamide from matrix tablets was studied using the USP Dissolution Testing Apparatus type-I (Basket method). The formulation F6 which contained EC 50mg showed a maximum release of 99.28% in 24 hrs and revealed that EC was more effective in sustaining the drug release therefore formulation F6 was selected as the optimized formulation. The in-vitro release data of optimized formulation was fit into various kinetic models, among the different model's data of in-vitro release of best fit into Zero order kinetic model. The formulation best fit the Higuchi model and showed that drug release from the prepared matrix tablets occurs via a diffusion process.

Formulation and in vitro evaluation of compression coated mebeverine HCl tablets for colon targeting

The aim of the study was to develop colon targeted compression coated Mebeverine HCl (MEB) tablets using pH dependent, swellable and rupturable polymers for effective treatment of irritable bowel syndrome (IBS). The MEB loaded core tablets were prepared by direct compression method using CCM and CP as super disintegrating agents at different concentrations and evaluated for pre compression and post compression parameters. The optimized core tablets were further used to fabricate compression coated tablets using different ratios of Eudragit L100, Eudragit S100 as pH- dependent polymers, Keltone and Ethocel as swellable and rupturable polymers by modified compression method. Drug compatibility with excipients was checked by FTIR studies and results indicate no interaction. The precompression and post compression studies were within acceptable limits. In vitro dissolution studies were done for compression coated tablets to find out the lag phase, burst drug release and retard drug release The findings of this study concludes that the lag time of compression coated tablet can be modulated by combining with EL 100, ES 100, Keltone and Ethocel in different weight ratio. These designed tablet system was found to be satisfactory in terms of release of the drug after the predetermined lag time, thus the system can be target to release in the colon proximity. The compression coating technique can be successfully applied for MEB for colon targeting to treat IBS.

Formulation and Evaluation of Gastro-retentive Drug Delivery System of Novel Famotidine Phospholipid Complex

Famotidine is an H2 receptor antagonist belonging to the BCS Class II, characterized by low solubility and limited oral bioavailability. The current study encompasses the formulation of novel famotidine phospholipid complex (FHC) with the aid of design of experiments (Central Composite Design) using solvent evaporation technique to overcome the disadvantages of Famotidine. To further enhance the physicochemical properties of FHC, it was incorporated into gastro-retentive floating tablets (GRDDS) using direct compression technique with sodium bicarbonate as a gas generating agent and its properties were compared to famotidine floating tablets. The pre-compression parameters, namely bulk density, tapped density, Hausner’s ratio, Carr’s compressibility index and angle of repose were evaluated. The flow properties of FHC granules were found to be better than the plain famotidine granules. The postcompression parameters, namely thickness, hardness, friability, weight variation, drug content and swelling index showed better results for FHC as compared to famotidine floating tablets. In-vitro buoyancy study indicated that the floating lag time for FHC tablets (110 ± 0.021 seconds) was higher than famotidine tablets (36 ± 0.033 seconds) owing to the higher molecular weight of phosphatidylcholine. But the total floating time for FHC tablets was found to be more than 18 hours and for famotidine tablets it was ~12 hours, indicating the improved residence time and buoyancy. The in-vitro dissolution study depicted that the cumulative release for FHC tablets (99.84 ± 0.058%) was enhanced 1.07 fold than Famotidine tablets (92.73 ± 0.028%) and 1.6 fold than marketed tablet, Famocid (62.24 ± 0.023%). When kinetic modeling was performed, famotidine tablet followed zero order kinetics, whereas FHC tablet followed Higuchi model indicating a modified and sustained release pattern. The statistical analysis for %cumulative release performed using ANOVA and Dunnett’s test showed the p-value to be below 0.05 (0.0043) indicating that the analysis model was significant. An accelerated stability study was performed for a period of 6 months at 25 ± 2°C; 60 ± 5% RH. FHC tablets showed a better stability profile than famotidine tablets. In conclusion, FHC gastro-retentive floating tablets showed improved flow properties, post compression properties, better drug content, improved in-vitro buoyancy and enhanced cumulative release and stability profile.

DESIGN, FORMULATION, AND IN-VITRO EVALUATION OF IMMEDIATE RELEASE TABLET OF ETORICOXIB USING QUALITY BY DESIGN (QbD) APPROACH

Introduction: The current research aimed to formulate and evaluate the immediate-release tablet of etoricoxib. Etoricoxib belongs to BCS class II drugs; hence the solubility was enhanced using different techniques, thus achieving the dissolution of the drug. The formulation with maximum solubility enhancement was selected as the final formulation for the preparation of immediate-release tablets. Material and Methods: These tablets were prepared using the wet granulation technique. Sodium starch glycolate was used as a super disintegrant, microcrystalline cellulose was used as a binder, and sodium bicarbonate was used as effervescent material for the preparation of an immediate-release tablet. Different trial batches were prepared and the formulations were optimized using design expert software. The optimized formulation was prepared and evaluated for different post-compression parameters. Results and Discussion: The disintegration time was found to be 2 minutes 16 seconds and the percent cumulative drug release was found to be 90.30%. The pharmacokinetic behavior of the drug was studied and first-order kinetics was found to be the best fit model for immediate-release tablets. The accelerated stability study for the immediate-release tablet was carried out at 40℃ ±75% RH and different parameters were evaluated and were found within specified limits. Conclusion: Thus immediate release tablets of etoricoxib were found to be a promising candidate for the treatment of acute pain or arthritis.