Conventional Tablet Formulation Research Articles

Unleashing the Potential of β -cyclodextrin Inclusion Complexes in Bitter Taste Abatement: Development, Optimization and Evaluation of Taste Masked Anti-emetic Chewing Gum of Promethazine Hydrochloride.

Motion sickness also known as kinetosis is a condition in which there exists a disagreement between visually perceived movement and the vestibular system's sense of movement. Nausea, vomiting, dizziness, fatigue, and headache are the most common symptoms of motion sickness. This study mainly focuses on the taste masking of Promethazine Hydrochloride (PMZ) by inclusion complexation method, its formulation development in the chewing gum form by using directly compressible gum base HIG® and its quality and performance testing. Different molar ratios (1:1, 1:2, 1:3 and 1:4) of PMZ-cyclodextrin complexes were prepared by using β-Cyclodextrin(β-CD) as a taste masking agent. These complexes were evaluated for FTIR, DSC, % Entrapment Efficiency, % drug yield, and taste evaluation by E-Tongue. The optimized ratio was further evaluated by sophisticated analytical techniques such as Scanning Electron Microscopy (SEM) and X-Ray Diffraction (XRD). A central composite design (CCD) (3 ^2) was utilized to examine the effects of independent variables (amount of gum-X1 and amount of plasticizer-X2) on dependent variables (%CDRY1 and hardness Y2). The prepared gums were evaluated for drug content, organoleptic properties, in-vitro dissolution testing by fabricated disintegration apparatus, texture analysis, etc. The optimization statistics showed that on decreasing the amount of gum, in- vitro drug release increases and hardness decreases. The optimized batch MCG-2 of Promethazine MCG showed 92.34 ± 0.92% of drug release, whereas for marketed formulation (Phenergan®-25mg) drug release value was 86.19 ± 1.88%. Results provided evidence that PMZ MCGs could be a better alternative to conventional tablet formulations with improved drug release, palatability and texture.

Formulation Development of Medicated Chewing Gum by Direct Compression utilizing the SeDeM Diagram Expert System

The main objective of this study was to prepare and characterize the MCG of Ondan HCl which helps to improve the effectivity of the drug and to investigate the applicability of the SeDeM system for the formulation of MCG. The Ondan HCl was formulated into directly compressed MCG utilizing the SeDeM Diagram Expert System. The MCG was optimized using 32 factorial design. Performance evaluation was carried out by evaluating different parameters. Statistical analysis showed that micromeritic properties were improved after inclusion of appropriate excipient in optimum amount. In-vitro drug release study showed 90.01% drug release whereas ex vivo buccal permeation study exhibited significant drug permeation within 15 min indicating its potential for increasing bioavailability. It was concluded that various characteristics of powder material at pre formulation level can be successfully predicted by SeDeM diagram expert system. The developed medicated chewing gum is more effective than mouth dissolving and conventional tablet formulation.
 Keywords: Ondansetron HCl; Medicated chewing gum; direct compression; SeDeM diagram expert system.

Evaluating the pharmacokinetic parameters of a single dose of oral disintegrating tablets in elderly patients with hypertension and hyperlipidemia

Cardiovascular diseases (CVDs) are the leading cause of death worldwide, particularly in underprivileged areas such as Pakistan. Hypertension and hyperlipidemia are major risk factors for CVDs and often require medication for effective management. This study aimed to develop and validate a high-performance liquid chromatography (HPLC) method to assess the bioavailability of orally disintegrating tablets (ODTs) of atenolol and atorvastatin in elderly volunteers with high blood pressure and cholesterol levels by comparing the pharmacokinetic parameters of these ODTs with those of conventional tablet formulations. The study was conducted in Sargodha, Punjab Province, Pakistan, by recruiting 30 male and female elderly volunteers aged 45-65 years and weighing 60-90 kilograms. Each participant was administered a single dose of atenolol (25 mg), atorvastatin (10 mg), or an ODT containing both drugs. Blood samples were collected at specific intervals up to 48 hours postadministration. The concentrations of atenolol, atorvastatin, and the ODTs were measured using HPLC, and various pharmacokinetic parameters, including the area under the curve (AUC), maximum plasma concentration (Cmax), and elimination half-life (t½), were analyzed. The maximum concentration (Cmax) of 10 mg atorvastatin occurred at 4 hours (9.50 ng/mL), while for 25 mg atenolol, it peaked at 4 hours (150.00 ng/mL). The ODTs showed comparable pharmacokinetic profiles, with the Cmax values for atorvastatin and atenolol at 4 hours being 4.00 ng/mL and 165.00 ng/mL, respectively. The elimination half-life (t½) for the ODTs was 4.62 hours for atorvastatin and 4.95 hours for atenolol. The pharmacokinetic analysis indicated that the AUC and Cmax of the ODTs met the bioequivalence criteria, demonstrating absorption and elimination properties similar to those of conventional tablet formulations. The study concluded that the pharmacokinetic parameters of the ODT formulations atenolol and atorvastatin are comparable to those of conventional tablets. ODTs offer a viable and effective alternative for delivering these medications, particularly for patients who have difficulty swallowing pills, thereby potentially improving patient compliance.

Application of biorelevant in vitro assays for the assessment and optimization of ASD-based formulations for pediatric patients

Amorphous solid dispersions (ASD) have been a successful formulation strategy to overcome the poor aqueous solubility of many novel drugs, but the development of pediatric formulations presents a special challenge due to variable gastrointestinal conditions in children. It was the aim of this work to design and apply a staged biopharmaceutical test protocol for the in vitro assessment of ASD-based pediatric formulations. Ritonavir was used as a model drug with poor aqueous solubility. Based on the commercial ASD powder formulation, a mini-tablet and a conventional tablet formulation were prepared. Drug release from the three formulations was studied in different biorelevant in vitro assays (i.e. MicroDiss, two-stage, transfer model, tiny-TIM) to consider different aspects of human GI physiology. Data from the two-stage and transfer model tests indicated that by controlled disintegration and dissolution excessive primary precipitation can be prevented. However, this advantage of the mini-tablet and tablet formulation did not translate into better performance in tiny-TIM. Here, the in vitro bioaccessibility was comparable for all three formulations. In the future, the staged biopharmaceutical action plan established herein will support the development of ASD-based pediatric formulations by improving the mechanistic understanding so that formulations are developed for which drug release is robust against variable physiological conditions.

BOX-BEHNKEN DESIGN FOR OPTIMIZATION OF FORMULATION VARIABLES FOR CONTROLLED RELEASE GASTRORETENTIVE TABLET OF VERAPAMIL HYDROCHLORIDE

Objective: To develop a Verapamil hydrochloride controlled release gastro-retentive (CRGR) tablet for once-daily dosing using the response surface Box-Behnken Design (BBD) approach for the improvement of bioavailability and reduction in dosing frequency to overcome the issues related to the conventional tablet formulation. Methods: For the optimization, 33Box-Behnken design was used. The independent variables were selected, the amount of Compritol 888 ATO (A), HPMC K15M (B), and Sodium bicarbonate (C). The dependent variables were Cumulative % drug release in 1.5 h (Q1.5), 8 h (Q8), 24 H (Q24) and floating lag time (FLT). Flow properties of pre-compressed powder, physical characteristics, drug content, floating lag time, total floating time and in vitro dissolution study of all formulation were assessed. In vitro dissolution study of optimized formulation that was prepared experimentally was performed and compared with predicted data obtained from the software. Drug release kinetics of the optimized formulation was also assessed to know the mechanism of drug release from the CRGR tablets. Results: Responses of experimental runs were found as Q1.5: 12.78-33.62 (%), Q8: 43.03-64 (%), Q24: 78.77 to 103.57 (%) and floating lag time as 3.01 min to 5.08 min. The predicted optimized formula with the highest desirability value of 0.963 containing amount 126.030 mg, 160.00 mg and 80.955 mg of Compritol 888 ATO, HPMC K15M and Sodium biarbonate respectively was prepared and evaluated. The experimental values from optimized formulation were obtained as Q1.5: 23.397%, Q8; 57.744%, Q24: 97.150% and FLT: 3.12 min. Predicted and experimental results were found comparable for all the responses. The release data from the optimized formulation were best fitted in the Higuchi (r2 = 0.999) and the Korsmeyer-Peppas ((r2 = 0.998, n=0.54) model. The in vitro drug release studies indicated that the Verapamil hydrochloride gastroretentive tablet releases the drug in controlled manner for 24 h. Conclusion: This study found that using Box-Behnken Design with the response and variable relation, it is possible to achieve an optimum formulation with desirable characteristics. This study also established the suitability of Compritol 888 ATO-HPMC K15M combination with Sodium bicarbonate to increase the gastric residence time tablet formulation had once-daily dosing of the Verapamil Hcl with improved bioavailability for effective management of hypertension.

Optimization and validation of stability indicating RP-HPLC method for the quantification of gefitinib in bulk drug and nanoformulations: An application towards in vitro and ex vivo performance evaluation

Gefitinib (GFB) is an epidermal growth factor receptor (EGFR) tyrosine kinase inhibitor used primarily to treat non-small cell lung cancer (NSCLC), but it also works by lowering AKT and MAPK phosphorylation, which makes it effective against the breast cancer cells. A high-performance liquid chromatography (HPLC) method was developed for detecting gefitinib by C18 analytical column with mobile phase containing acetonitrile and 1 % w/v ammonium acetate in water with ratio of 60:40. Box-Behnken design was used to optimize the chromatographic conditions, and method was validated for accuracy, precision, linearity, robustness, ruggedness, limit of detection, and limit of quantification. The developed method was found to be useful in estimating gefitinib in conventional marketed tablet dosage forms and nanoformulations such as SLNs and liposomes. With a calibration curve, linearity was attained in the drug concentration range of 8–56 µg/mL (r2 = 0.9996), and sensitivity was found to be 1.3 and 3.9 µg/mLas LOD and LOQ, respectively. All the validation criteria for the method were within the acceptable limits. The drug content in the conventional tablet formulation was found to be 99.99 %. The HPLC analysis indicated that gefitinib was highly soluble in Precirol ATO5 as solid lipid and tween 80 as surfactant. Drug entrapment efficiency was found to be 83.1 % and 80.5 % for SLNs and liposomes respectively. In vitro release data revealed that 30 % of drug was released from plain suspension and more than 77 % released from both nanoformulations after 24 h at pH 7.4 respectively. By applying kinetic fit, data was most appropriately fitted into first order as compared to other. The apparent permeability of gefitinib from plain suspension, SLNs and Liposomes was found to be 3.98 × 10−4 cm/min, 1.35 × 10−4 cm/min and 1.79 × 10−4 cm/min.

FORMULATION AND EVALUATION OF MEDICATED CHEWING GUM OF EGCG (EPIGALLOCATECHIN GALLATE) ENRICHED EXTRACT OF CAMELLIA SINENSIS (GREEN TEA) FOR PERIODONTAL DISEASE

The aim of this study was the formulation and evaluation of medicated chewing gum of EGCG (epigallocatechin gallate) enriched extract of camellia sinensis. The extraction of marketed lipton green tea was done by infusion method and antibacterial activities of extract were done against P. gingivalis and S. mutan by well diffusion method. Chewing gum was prepared by softening of gum bases and then mixing with other formulation ingredients and optimization of the formulation by screening of different excipients. Performance evaluation was carried out by evaluating hardness, fracturability, adhesiveness, elasticity, cohesiveness, stringiness, chewiness, gumminess, in vivo drug release study. Precentage yield of extract in first step and second step were found to be 9.43, 11.65 respectively by infusion method. The EGCG obtained with second step of two step method was found significantly greater. In antibacterial activities, the glucan synthesis by the bacterial S. mutan glucosyl transferase was strongly inhibited by (-)-epigallocatechin gallate (EGCG) at concentrations of 50-200ug/ml, the main components of the green tea polyphenols and completely inhibited the growth and adherence of P. gingivalis onto the buccal epithelial cells. Optimized formulations MCG-6 showed hardness, adhesiveness, elasticity, gumminess, chewiness, resilience and cohesiveness values are similar to that of the reference (Nicogum). In vitro drug released of optimized formulation was found to be 77% within 15 min. The developed formulation of medicated chewing gum can be a better alternative to mouth dissolving and conventional tablet formulation. It may be proved as a promising approach to improve the bioavailability as well as to improve patient compliance.

Combining Liquisolid and Co-grinding Techniques to Enhance the Dissolution Rate of Celecoxib

PurposeThe classic liquisolid technique is used to enhance the dissolution rate of poorly water-soluble drugs, but in some cases, it is impossible to reach the desired dissolution rate using this technique alone. Therefore, a novel approach using a combination of ball milling and liquisolid technology was investigated to improve the dissolution rate for celecoxib.MethodsFirst, celecoxib was dispersed in a liquid vehicle (PEG 200), then ground in a ball mill for 3 h. Other excipients, including PVP, microcrystalline cellulose as the carrier powder, and silica as the coating material, were added to the mortar. Dissolution testing was carried out in simulated intestinal fluid (SIF) and simulated gastric fluid (SGF) media. The effects of aging on the hardness and dissolution profile were also studied. X-ray diffraction (XRD) and differential scanning calorimetry (DSC) was used to identify changes in the crystallinity or complex formation.ResultsThe novel formulations showed a higher dissolution rate than the conventional tablet or classic liquisolid formulations. Aging did not affect the hardness and dissolution profiles of the liquisolid compacts. The DSC and XRD results suggested that the enhanced dissolution rate is not caused by the formation of any complexes and reduction in crystallinity degree may contribute to the dissolution enhancement. The enhanced dissolution rate is attributed to the elevated specific surface area of the drug in the liquisolid state.ConclusionThe results showed that liquisolid technology combined with ball milling is an efficient tool for enhancing the dissolution of poorly water-soluble drugs.

In Vitro Evaluation of Dalbergia sissoo and Acacia modesta gum as Pharmaceutical Binders for Drug Delivery System

The present study aimed to compare the crude, modified and hydrolyzed gums of Dalbergia sissoo and Acacia modesta as a biodegradable binder for drug delivery system using acetaminophen as a model drug. The physiochemical properties such as pH, fluorescence analysis and swelling index were determined. The gums were hydrolyzed and modified. Acetaminophen tablets were prepared using wet granulation technique and the gum solutions were used as a binder. Hydroxypropyl methylcellulose was used as a synthetic binder. Different properties of granules and tablets were evaluated. Results showed that both gums were acidic in nature, while D. sissoo and A. modesta showed light brown and creamy color in fluorescence analysis. The swelling ratio was the highest in water followed by 0.1N HCl and least in phosphate buffer. The prepared tablets showed faster and slower dissolution profiles in the same dissolution system. The crude gums have the highest dissolution rate, and this rate was decreased in the case of modified and hydrolyzed gums samples. The crude gums showing slower release can be useful in sustained-release tablets, while the modified gums having faster release rate are helpful in conventional tablet formulation. Taken together, the selected gums could be a good model for evaluation as a binder or hydrophilic polymer in tablet formulation.

Efficacy of the Orally Disintegrating Strip Sildenafil for the Treatment of Erectile Dysfunction: A Prospective, Randomized Trial.

IntroductionPhosphodiesterase 5 inhibitors are the predominant treatment option for erectile dysfunction.AimThis study evaluates the efficacy and safety of sildenafil orally disintegrating strips for the treatment of erectile dysfunction.MethodsOne hundred twenty erectile dysfunction patients were enrolled in a prospective, randomized, controlled crossover study and allocated into 2 groups of 60 participants. Patients were either treated with sildenafil strips or tablets for 8 weeks after which they crossed over into the alternate treatment formulation for another 8 weeks following a 4-week wash-out period. Each participant was assessed 8 times throughout the study period and their formulation preference registered at the end of the study.Main outcomes and measuresChanges in the abridged International Index of Erectile Function (IIEF-5) score and Erection Hardness Score (EHS) resulting from sildenafil orally disintegrating strip or tablet treatments were the primary end points, with differences in onset of action, duration of action, and incidence of adverse events between the 2 formulations included as secondary end points.ResultsBoth sildenafil formulations were effective in treating patients with erectile dysfunction. There was significant improvement of erectile function in term of IIEF-5 score and EHS from both formulations. The number and type of adverse events were also comparable. Likewise, there were no statistically significant differences between the earliest onset of action times and longest duration of action times. However, the results showed a 7.1-minute earlier onset of action time for orally disintegrating strips that may be considered as clinically meaningful by some patients.ConclusionSildenafil orally disintegrating strips are a safe and effective alternative to the conventional tablet formulation for the treatment of erectile dysfunction. Sangkum P, Sirisopana K, Matang W, et al. Efficacy of the Orally Disintegrating Strip Sildenafil for the Treatment of Erectile Dysfunction: A Prospective, Randomized Trial. Sex Med 2021;9:100453.

Development of an Age-Appropriate Mini Orally Disintegrating Carvedilol Tablet with Paediatric Biopharmaceutical Considerations.

Owing to considerable differences observed in anatomy and physiology between paediatric subsets, it has been well established that children respond to drugs differently compared to adults. Furthermore, from a formulation perspective, there is a distinct challenge to develop a dosage form that is capable of safely, accurately, and reliably delivering the dose across the whole paediatric population. Orally disintegrating mini-tablets (ODMT) have widely been considered as an age-appropriate formulation option that possess the ability for adequate dose flexibility, avoids swallowing difficulties, and exhibits superior stability due to its solid state. Within this study, two strengths (0.5 mg and 2 mg) of carvedilol ODMT formulations were developed using an excipient composition and load that is appropriate for paediatric use. The formulations demonstrated adequate mechanical strength (>20 N) and fast disintegration times (<30 s). Dissolution profiles observed were robust and comparable to the marketed conventional tablet formulation across various parts of the gastrointestinal (GI) tract in both the fed and fasted state, signifying appropriate efficacy, quality, and performance. As such, the formulations developed in this study show potential to address the need of an ‘age-appropriate’ formulation of carvedilol, as highlighted by the European Medicines Agency (EMA) Inventory of the Needs for Paediatric Medicine.

Rimegepant: First Approval.

The orally disintegrating tablet (ODT) formulation of rimegepant (NURTEC ODT®) is a small molecule, highly-selective, calcitonin gene-related peptide antagonist that was developed by Biohaven Pharmaceutical Holding Company Ltd as an acute treatment for migraine. A conventional tablet formulation of the drug is being investigated for the acute treatment (under FDA review in the USA) and prevention of migraine and the treatment of refractory trigeminal neuralgia. In February 2020, rimegepant ODT received its first global approval in the USA for the acute treatment of migraine (± aura) in adults. This article summarizes the milestones in the development of rimegepant leading to its first global approval for acute treatment of migraine (± aura) in adults.

Taste masking of enalapril maleate by microencapsulation in Eudragit EPO® microparticles.

Microencapsulation is one of the most commonly used taste masking techniques. It can be accomplished by various methods, including coacervation, solvent evaporation, extrusion and spray-drying. Enalapril maleate, a bitter-tasting ACE-inhibitor, is available worldwide in conventional tablet formulations and as oral solution in the USA. The purpose of this study was to develop enalapril-loaded microparticles using spray-drying and to test their taste masking potential. Eudragit EPO® was used as a taste masking polymer for the preparation of a drugpolymer suspension. The suspension was then spray-dried under the following conditions: inlet temperature 65 °C, outlet temperature 30 °C, aspiration 100% and pump rate 10%. The drug-to-polymer ratio was varied and seven different microparticle models were developed. The yield of spray-dried particles ranged from of 51.3 to 85.4%, drug loading varied from 7.75 to 24.69% and encapsulation efficiency ranged from 58.5 to 95.7%. The particle size varied between 5.00 μm and 17.47 μm and the moisture content varied between 7.1% and 10.3%. In vitro taste assessment revealed minimal or no ENA release in artificial saliva. In vivo studies (with experimental animals and healthy volunteers) were used to evaluate the taste masking potential of spray-dried microparticles of enalapril maleate and Eudragit EPO®.

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.

FORMULATION AND EVALUATION OF CHLOROTHALIDONE LOADED MOUTH DISSOLVING FILM-A BIOAVAILABILITY ENHANCEMENT APPROACH USING MULTILEVEL CATEGORIC DESIGN

Objective: The intension of the present study includes fabrication and optimization of mouth dissolving film loaded with Chlorothalidone by solvent evaporation techniques using two components and their three levels as multilevel Categoric design.&#x0D; Methods: Major problem associated with the development of film loaded with BCS class II drug is to increase its solubility. Here the Chlorothalidone solubility achieved by co-solvents, such as methanol. After dissolving the drug in co-solvent, this drug solution is poured into an aqueous dispersion of Hydroxypropyl Methylcellulose E5 (HPMC E5) and Polyethylene glycol 400 (PEG 400). The two independent variables selected are factor A (concentration of HPMC E5) and factor B (concentration of PEG 400) was selected on the basis of preliminary trials. The percentage drug release (R1), Disintegration time in sec (R2) and folding endurance (R3) were selected as dependent variables. Here HPMC E5 used as a film former, PEG 400 as plasticizer, mannitol as bulking agent, Sodium starch glycolate as a disintegrating agent, tween 80 as the surfactant, tartaric acid as saliva stimulating agent, sodium saccharin as a sweetener and orange flavour etc. These fabricated films were evaluated for physicochemical properties, disintegration time and In vitro drug release study.&#x0D; Results: The formulation F6 has more favorable responses as per multilevel categoric design is % drug release about 98.95 %, average disintegration time about 24.33 second and folding endurance is 117. Thus formulation F6 was preferred as an optimized formulation.&#x0D; Conclusion: The present formulation delivers medicament accurately with good therapeutic efficiency by oral administration, this mouth dissolving films having a rapid onset of action than conventional tablet formulations.

Formulation Optimization and Evaluation of Immediate Release Tablet of Telmisartan

Telmisartan is an angiotensin-II receptor antagonist used in the treatment of hypertension. The goal of this research work was to develop the formulation as immediate release tablet of telmisartan by using the superdisintegrants by design of experiments. The FTIR study revealed that there was no interaction between drug and polymer and combination can be safely prepared. Tablets were prepared by using direct compression method. Tablets were evaluated for hardness, thickness, weight variation, disintegration time, drug content, friability and in vitro drug release. All the physical parameters were in acceptable limit of pharmacopoeial specification. A Central Composite Design (CCD) was selected to optimize the formulation B6 which showed the in-vitro drug release 97.16% at 30 min. The two factors croscarmellose sodium and microcrystalline cellulose were varied as required by the experimental design. A composition was selected as optimized formulation (N1), which was compared with the conventional tablet (10% MCC) formulation, while difference (F1) factor and similarity (F2) factor found to be 6.96 and 60.5 respectively. The optimized formulation (N1) was showed in-vitro drug release of 97.74% at the end of 30 minutes, while disintegration time of the tablet was showed 19 sec comparison to other formulations. Further the drug release of immediate release tablets was compared with the drug release profile of conventional tablet which was prepared by using 10% micro crystalline cellulose (MCC) as disintegrating agent.

Enhanced Systemic Exposure and Efficacy of Diltiazem from Novel Microemulsion Formulation: Characterization, In vitro Release, In vivo Pharmacokinetic and Efficacy Evaluation

: Purpose: Diltiazem, a calcium ion cellular influx inhibitor is known for its limited and variable bioavailability. This study is intended to explore the benefits of microemulsion formulation as oral drug delivery system for immediate release to improve the bioavailability and efficacy of Diltiazem. Methods: Oil in water microemulsion was prepared using the simple water titration method. The optimized formulation was evaluated for physicochemical parameters like viscosity, pH, conductivity and accelerated stability studies. In vitro release, in vivo pharmacokinetics and in vivo efficacy of the optimized diltiazem microemulsion was investigated. Results: The optimized diltiazem microemulsion consisted of 60% water, 5% Almond oil, 35% mixture of surfactant (Tween 80) and cosurfactant (Polyethyne glycol 400) (1:8). The existence of microemulsion region was investigated using pseudoternary phase diagrams. The average particle size by dynamic light scattering technique was found to be 13.8 nm with polydispersity index of 0.474. The optimized microemulsion was found to be thermodynamically stable with in vitro release of 91.82% compared with that of suspension at 55.2%. The peak exposure of diltiazem was 1.23 fold higher and the extent of exposure was found to be 1.24 to 1.29 fold greater for microemulsion compared to the reference tablet formulation when tested in rabbits. The novel formulation was found to have greater efficacy compared to conventional tablet formulation in reducing systolic blood pressure in rats. Conclusion: The diltiazem microemulsion greatly improves the pharmacokinetic parameters and thus improves therapeutic efficacy of diltiazem and could be a potential alternative oral dosage form in therapeutic management of hypertension.Key words: Bioavailability, Diltiazem Efficacy, Micro emulsion, Pharmacokinetics, Release kinetics.

FAST DISSOLVING TABLETS: A REVIEW

Fast dissolving tablets emerge as one of the popular and widely accepted dosage forms, especially for pediatric patients because of incomplete development of the muscular and nervous system and a case of geriatric patients suffering from Parkinson’s disorder or hand tremors. Few solid dosage forms like capsules and tablets are present days facing the problems like difficulty in swallowing (dysphagia), resulting in many incidences of non-compliance and making the therapy ineffective. Oral dosage form and oral route are the most preferred route of administration for various drugs have limitations like first-pass metabolism, psychiatric patients, bedridden and uncooperative patients. FDTs are disintegrating or dissolve quickly in the saliva without a need of water. Fast dissolving tablets are designed to dissolve in saliva remarkably faster, within a few seconds (less than 60 seconds), and those are real fast-dissolving tablets. FDTs formulations contain super disintegrants to enhance the disintegration rate of a tablet in the buccal cavity. FDTs have advantages such as easy portability and manufacturing, accurate dosing, good chemical and physical stability and an ideal alternative for geriatric and pediatric patients. FDTs have disintegrated quickly, absorb faster so, in vitro drug release time improve and this property of drugs (dosage form) enhanced bioavailability. FDT formulations have the advantage of both conventional tablet formulation and liquid dosage form. There are several technologies that are conventional or patented based on spray drying, cotton candy process, sublimation, melt granulation, direct compression freezes drying/lyophilization, phase transition process, mass extrusion, etc. have been developed for manufacturing of FDTs. In this review contain brief information about FDTs including definition, advantages, needs or requirements of FDTs, salient features of FDTs, limitations, challenges to developing FDT, marketed formulations of fast dissolving tablets, etc.

Novel Co-processed Spray Dried Super Disintegrants Designing of Fast Dissolving Tablets Using

In the present study, novel co-processed superdisintegrants were developed by spray drying method using microcrystalline cellulose and mannitol in different ratios (1:1, 1:2 and 1:3) for use in the fast dissolving tablet formulations. The developed excipients were evaluated for angle of repose, Carr’s index and Hausner’s ratio in comparison with physical mixture of superdisintegrants. The angle of repose of the developed excipients was found to be &lt; 30o, Carr’s index in the range of 9-15 % and Hausner’s ratio in the range of 1.12-1.16. Fast dissolving tablets of glibenclamide were prepared using the above co-processed superdisintegrants and evaluated for pre-compression and post-compression parameters. Based on in vitro dispersion time (approximately 22.23 sec), promising formulation MCM3 was tested for in vitro drug release pattern in pH 6.8 phosphate buffer and stability (at 400C/75 % RH for 3 months), drug excipients interaction (IR spectroscopy) were studied. Among the designed formulations, the formulation (MCM3) containing 8 % w/w of co-processed superdisintegrant (1:3 mixture of microcrystalline cellulose and mannitol) emerged as the overall best formulation (t50% 1.6 min) based on drug release characteristics in pH 6.8 phosphate buffer compared to commercial conventional tablet formulation (t50% 6 min). Stability studies on promising formulation indicated that there were no significant changes in drug content and in vitro dispersion time (p&lt;0.05).Dhaka Univ. J. Pharm. Sci. 15(2): 167-172, 2016 (December)

Review: ODT’s drug containing Spironolactone

Orally disintegrating tablets (ODTs) have emerged as one of the popular and widely accepted dosage forms, especially for the pediatric and geriatric patients. To obviate the problem of dysphagia and to improve patient compliance, ODTs have gained considerable attention as preferred alternatives to conventional tablet and capsule formulations In the present study, an attempt has been made to prepare orally disintegrating tablet of the drug Spironolactone using superdisintegrants crosspovidone, crosscarmellose sodium and sodium starch glycolate by direct compression technique. Various scientific techniques including freeze drying, moulding, spray drying, sublimation, direct compression, cotton candy process, mass extrusion, melt granulation etc. have been employed for the development of ODTs. The prepared tablets were evaluated for pre and post compression parameters i.e. angle of repose, car’s index, hausner’s ratio, hardness, friability, wetting time, weight variation, in vitro disintegration and in vitro dissolution study.