Dispersible Tablet Formulation Research Articles

Population Pharmacokinetic Modeling of Abacavir/Dolutegravir/Lamivudine to Support a Fixed-Dose Combination in Children with HIV-1.

Once-daily fixed-dose combinations (FDC) containing abacavir (ABC), dolutegravir (DTG), and lamivudine (3TC) have been approved in the US for adults and children with HIV weighing ≥ 6kg. This analysis assessed the ability of previously developed ABC, DTG, and 3TC pediatric population pharmacokinetic (PopPK) models using multiple formulations to describe and predict PK data in young children using dispersible tablet (DT) and tablet formulations of ABC/DTG/3TC FDC in the IMPAACT 2019 study. IMPAACT 2019 was a Phase I/II study assessing the PK, safety, tolerability, and efficacy of ABC/DTG/3TC FDC in children with HIV-1. Intensive and sparse PK samples were collected over 48weeks. Existing drug-specific pediatric PopPK models for ABC (2-compartment), DTG (1-compartment), and 3TC (1-compartment) were applied to the IMPAACT 2019 drug concentration data without re-estimation (external validation) of PopPK parameters. Drug exposures were then simulated across World Health Organization weight bands for children weighing ≥ 6 to < 40kg for each drug and compared with pre-defined exposure target ranges. Goodness-of-fit and visual predictive check plots demonstrated that the previously developed pediatric PopPK models sufficiently described and predicted the data. Thus, new PopPK models describing the IMPAACT 2019 data were unnecessary. Across weight bands, the predicted geometric mean (GM) for ABC AUC0-24 ranged from 14.89 to 18.50μg*h/ml, DTG C24 ranged from 0.74 to 0.95μg/ml, and 3TC AUC0-24 ranged from 10.50 to 13.20μg*h/ml. These exposures were well within the pre-defined target ranges set for each drug. This model-based approach leveraged existing pediatric data and models to confirm dosing of ABC/DTG/3TC FDC formulations in children with HIV-1. This analysis supports ABC/DTG/3TC FDC dosing in children weighing ≥ 6kg.

ReNeu: A pivotal phase 2b trial of mirdametinib in children and adults with neurofibromatosis type 1 (NF1)-associated symptomatic inoperable plexiform neurofibroma (PN).

3016 Background: PN in patients (pts) with NF1 can cause pain, disfigurement, impaired quality of life (QoL), and can undergo malignant transformation. ReNeu (NCT03962543), a multicenter, open-label, Phase 2b study, evaluated efficacy and safety of the highly selective, oral, investigational MEK1/2 inhibitor mirdametinib in adult (≥18 y) and pediatric (2-17 y) pts with inoperable NF1 PN causing significant morbidities. Methods: Mirdametinib was administered as a capsule or dispersible tablet (2 mg/m2 BID, max 4 mg BID) without regard to food in 3 wk on/1 wk off 28-d cycles. The primary endpoint was confirmed objective response rate (ORR; percentage of pts with MRI-assessed ≥20% reduction of target PN volume by blinded independent central review [BICR] within the 24-cycle treatment phase). The minimum clinically relevant ORR (null) was defined as 23% for adults and 20% for pediatrics. Ptscould continue treatment in an optional long-term follow-up (LTFU) phase. Additional key endpoints were duration of response (DoR), time to response (TTR), change from baseline (BL) in target PN volume, pain severity (Numerical Rating Scale-11 [NRS-11]), pain interference (Pain Interference Index [PII]), health-related (HR) QoL (PedsQL), and safety. Results: All114 pts (58 adult, 56 pediatric) received mirdametinib. As of the 20 Sept 2023 data cutoff (DCO), BICR-confirmed ORR during the treatment phase was 41% (95% CI, 29-55; P&lt;.001 vs null) in adults and 52% (95% CI, 38-65; P&lt;.001 vs null) in pediatric pts. Two adult pts and 1 pediatric pt also had a confirmed response in the ongoing LTFU. Median (min, max) target PN volumetric best response from BL was -41% (-90, 13) and -42% (-91, 48) in adult and pediatric pts, respectively. As of the DCO, median treatment duration was 22 mo for each cohort and median DoR was not reached. Median (range) TTR was 7.8 (4-19) mo in adult pts and 7.9 (4-19) mo in pediatric pts. Adult and pediatric pts had statistically significant improvements from BL to cycle 13 in NRS-11, PII, and key PedsQL measures. Most frequent (≥35% pts) treatment-emergent adverse events (TEAEs) were dermatitis acneiform, diarrhea, nausea, and vomiting in adults and diarrhea, dermatitis acneiform, and vomiting in pediatric pts. 16% and 25% of adult and pediatric pts, respectively, had grade ≥3 treatment-related AEs, and 22% and 9%, respectively, discontinued due to TEAEs. Conclusions: In ReNeu, the largest multicenter NF1 PN trial reported to date, mirdametinib demonstrated a statistically significant ORR by BICR, with deep and durable PN volume reductions, significant improvements in pain severity, pain interference, and HRQoL, and a manageable safety profile in both adults and children. Together with a dispersible tablet formulation, these results underscore mirdametinib’s potential to become an important new treatment option for NF1 PN pts across all ages. Clinical trial information: NCT03962543 .

Field testing of user-friendly perennial malaria chemoprevention packaging in Benin, Côte d’Ivoire and Mozambique

BackgroundPerennial malaria chemoprevention (PMC) aims to protect children at risk from severe malaria by the administration of anti-malarial drugs to children of defined ages throughout the year. Sulfadoxine-pyrimethamine (SP) has been widely used for chemoprevention in Africa and a child-friendly dispersible tablet formulation has recently become available.MethodsThis qualitative non-interventional observational study was conducted in Benin, Côte d’Ivoire, and Mozambique between February and June 2022. Prototype blister packs, dispensing boxes and job aids designed to support dispersible SP deployment for PMC were evaluated using focus group discussions (FGD) and semi-structured in-depth individual interviews (IDI) with health authorities, health personnel, community health workers (CHWs) and caregivers. The aim was to evaluate knowledge and perceptions of malaria and chemoprevention, test understanding of the tools and identify gaps in understanding, satisfaction, user-friendliness and acceptability, and assess the potential role of CHWs in PMC implementation. Interviews were transcribed and imported to ATLAS.ti for encoding and categorization. Thematic content analysis used deductive and inductive coding with cross-referencing of findings between countries and participants to enrich data interpretation. Continuous comparison across the IDI and FGD permitted iterative, collaborative development of materials.ResultsOverall, 106 participants completed IDIs and 70 contributed to FGDs. Malaria was widely recognised as the most common disease affecting children, and PMC was viewed as a positive intervention to support child health. The role of CHWs was perceived differently by the target groups, with caregivers appreciating their trusted status in the community, whereas health authorities preferred clinic-based deployment of PMC by health professionals. Empirical testing of the prototype blister packs, dispensing boxes and job aids highlighted the context-specific expectations of respondents, such as familiar situations and equipment, and identified areas of confusion or low acceptance. A key finding was the need for a clear product identity reflecting malaria.ConclusionSimple modifications profoundly affected the perception of PMC and influenced acceptability. Iterative quantitative investigation resulted in PMC-specific materials suited to the local context and socio-cultural norms of the target population with the aim of increasing access to chemoprevention in children most at risk of severe malaria.

Acceptability of levofloxacin dispersible and non-dispersible tablet formulations in children receiving TB preventive treatment.

We evaluated the palatability and acceptability of a 100 mg dispersible and a non-dispersible 250 mg levofloxacin (LVX) tablet formulation in children. Perform was a randomised, open-label, cross-over trial of the relative bioavailability of LVX dispersible vs. crushed non-dispersible tablets in children aged <6 years routinely receiving TB preventive treatment. Children and caregivers completed Likert- and ranking-type measures on the acceptability of both formulations. We used summary, comparative and ranking statistics to characterise formulation acceptability. A total of 25 children were enrolled (median age: 2.6 years, IQR 1.6-4.0). Caregivers reported frequent challenges with preventive therapy in routine care prior to study entry, including taste of tablets (n = 14, 56%), vomiting/spitting out medicines (n = 11, 44%), and children refusing medicines (n = 10, 40%). Caregivers reported that the dispersible formulation was easier for their child to take than the non-dispersible formulation (P = 0.0253). Mean ranks for caregiver's formulation preferences (dispersible tablets: 1.48, SD ±0.71; non-dispersible tablets: 2.12, SD ±0.67; routinely available formulations: 2.40 SD ±0.82) differed significantly (Friedman's F 11.120; P < 0.0038); post-hoc testing showed dispersible tablets were preferred over non-dispersible (P = 0.018) and routinely available LVX formulations (P < 0.001). The dispersible LVX 100 mg tablet formulation was preferred and should be prioritised for integration into routine care.

Compliance and clinical benefit of deferasirox granule and dispersible tablet formulation in pediatric patients with transfusional iron overload: in a randomized, open-label, multicenter, phase II study.

CALYPSO (clinicaltrials gov. Identifier: NCT02435212), a randomized, open-label, multicenter, phase II study evaluated the compliance, clinical benefits, and safety of deferasirox granules and dispersible tablets (DT) in pediatric patients with iron overload. Iron chelation therapy-naive and iron chelation therapy-pretreated patients aged 2 to <18 years with transfusion- dependent anemias were enrolled. Patients were randomized 1:1 to deferasirox granules or DT for 48 weeks, stratified by age group and prior iron chelation therapy. In this study, the co-primary objectives are to evaluate compliance and change from baseline in serum ferritin after 24 weeks for both formulations in iron chelation therapy-naive patients. In total, 224 patients, mostly with β-thalassemia major (63.4%), were randomized to granules (N=112) or DT (N=112). Primary analysis was conducted when 96 iron chelation therapy-naive patients had completed 24 weeks of treatment/discontinued early; least squares mean (LSM) compliance in the deferasirox granules and DT groups, was 86.8% and 84.3% (difference 2.6%; P=0.360) respectively, while least squares mean change from baseline in serum ferritin was +4.8 and -171.5 ng/mL (difference: 176.4 ng/mL; P=0.255). Slight differences were observed in the observer/patient-reported outcome scores between the granule and dispersible-tablet groups and the overall scores indicate good adherence, satisfaction/preference, fewer concerns and good palatability with both deferasirox formulations. Safety analyses (N=221) found that the most frequently observed adverse events (granules and DT) were increased urine protein/creatinine ratio (>0.5 mg/mg; 24.5% and 34.2%), upper respiratory tract infection (28.2% and 29.7%), and pyrexia (26.4% and 23.4%). In iron chelation therapy-naive patients, mean compliance and change from baseline in serum ferritin with both deferasirox formulations were not significantly different. The safety profile was comparable between granule and DT formulations, and was consistent with the general safety profile of deferasirox.

Fexofenadine Hydrochloride Dispersible Tablets: A Taste Masking Strategy using Ion Exchange Resin

The pediatric population is more sensitive to allergies. Fexofenadine hydrochloride (FXD-HCL), a non-sedative antihistaminic drug, was chosen to create taste-masked patient-compliant pediatric dispersible tablets. Due to its bitter taste, fexofenadine hydrochloride is unsuitable for the formulation of dispersible tablets; therefore, Kyron T-134®, cation exchange resin was used to form a taste-masked complex with the drug to overcome its bitterness. The FXD HCL-resin complex was prepared using a kneading method and the complexation was confirmed by differential scanning calorimetry and FTIR studies. The FXD HCL-resin complex was evaluated for flow properties, degree of bitterness, assay and release study. Dispersible tablets were formulated by using a co-processed excipient, Granfiller-D211® containing croscarmellose sodium and crosspovidone, microcrystalline cellulose and mannitol. 22 factorial designs with two replicates optimized the dispersible tablets. The tablets, prepared using the direct compression technique on a single-stroke tablet compression machine, were elegant in appearance. Various pre and post-compression tests were conducted on all formulations. The tablets of hardness 3.5 kg/cm2 showed friability, disintegration time, assay within the compendial limit and showed immediate release of a drug (NLT 60% in 10 min and NLT 80% in 30 minutes) in 0.001 N HCl (pH 3). The DSC thermogram indicated partial amorphization of the FXD HCL. Dispersible tablets of fexofenadine hydrochloride and Granfiller-D®211 at 1:4 proportion was stable for one month at ambient and accelerated storage conditions.

A Review on Orodispersible tablet

The oral route is the most important and recommended route of drug administration. Oral route is the safest and convenient route of drug delivery because of wide range of drugs are administered through this route. Oro dispersible tablets are novel oral drug-delivery system as they have improved patient compliance and have some additional advantages compared to other oral formulation. Oral dispersible tablet are solid unit dosage forms, which disintegrate or dissolves quickly in the mouth within a minute in the presence of saliva without chewing or water. The dosage form containing super disintegrates which impart the quality of quick disintegration in the presence of saliva and also play an important role in the formulation of oral dispersible tablets. The present review is focused on ideal properties, objective, advantages and disadvantages and evaluation parameters.

Pharmacokinetic and Bioequivalence Evaluation of Two Cefprozil Dispersible Tablets in Healthy Chinese Volunteers.

This study aimed to assess the bioequivalence of 2 cefprozil dispersible tablet formulations (250mg) in healthy Chinese volunteers under fasting and fed conditions and to determine the pharmacokinetics of cefprozil. A randomized, single-dose, open-label, 2-formulation, 2-period study was conducted. The elimination period for this study was 7 days. Forty-eight healthy volunteers received 250-mg cefprozil dispersible tablets in each study period under both test and reference conditions. The test and the reference cefprozil were bioequivalent in healthy Chinese volunteers, and there was no significant food effect in individuals receiving either formulation. No serious adverse event was recorded, and no volunteers withdrew from the study.

Children deserve simple, short, safe, and effective treatment for rifampicin-resistant tuberculosis

Children deserve simple, short, safe, and effective treatment for rifampicin-resistant tuberculosis

Patient preference for deferasirox film-coated versus dispersible tablet formulation: a sequential-design phase 2 study in patients with thalassemia.

Iron chelation therapy (ICT) is the mainstay of treatment in patients with thalassemia requiring blood transfusions. This phase 2 JUPITER study evaluated patient preference betweenfilm-coated tablet (FCT) and dispersible tablet (DT) in transfusion-dependent thalassemia (TDT) or non-TDT (NTDT) patients treated with both formulations in a sequential manner. The primary endpoint waspatient-reported preference for FCT over DT, while secondary outcomes included patient reported outcomes (PROs) evaluated by overall preference, and by age, thalassemia transfusion status, and previous ICT status. Out of183 patients screened, 140 and 136 patients completed the treatment periods 1 and 2 of the core study, respectively. At week48, themajority of patients preferred FCT over DT (90.3 vs. 7.5%; difference of percentage: 0.83 [95% confidence interval (CI), 0.75-0.89; P < 0.0001]). FCT scored better on secondary PROs and showed less severe gastrointestinal symptoms than DT, except in the change of modified Satisfaction with Iron Chelation Therapy (mSICT) preference scores, which were similar for both the formulations. Patients with TDT had stable ferritin levels, while it showed adownward trend up to week 48 in patients with NTDT on deferasirox treatment. Overall, 89.9% ofpatients reported ≥ 1 adverse event (AE), of which 20.3% experienced ≥ 1 serious AE. The most common treatment-emergent AEs were proteinuria, pyrexia, urine protein/creatinine ratio increase, diarrhea, upper respiratory tract infections, transaminase increase, and pharyngitis. Overall, this study reinforced the observations from theprevious study by showing a distinct patient preference for FCT over DT formulation and further supported the potential benefits oflife-long compliance with ICT.

Effect of Food on the Pediatric Dispersible Tablet Formulations of TRIUMEQ and DOVATO in Healthy Adult Participants.

This randomized food effect study in healthy adult participants examined dispersible tablet formulations of fixed-dose combinations of dolutegravir/abacavir/lamivudine (TRIUMEQ) and dolutegravir/lamivudine (DOVATO). While adult tablet formulations of these combinations are currently approved for the treatment of human immunodeficiency virus, alternate formulations for children are urgently needed to facilitate appropriate pediatric dosing for patients who may have difficulty swallowing a conventional tablet. This study compared the effect of a high-fat, high-calorie meal on the pharmacokinetics, safety, and tolerability of dispersible tablet (DT) formulations of the two-drug and three-drug regimens, with administration under fasting conditions. Both the two-drug and three-drug dispersible tablet formulations, administered under fasting conditions and following a high-fat, high-calorie meal, were well tolerated in healthy participants. There were no clinically relevant differences in drug exposure for either regimen when administered with a high-fat meal as compared to under fasting conditions. Safety observations were similar for both treatments, either in the fed or fasted state. Both TRIUMEQ DT and DOVATO DT formulations can be administer with or without food.

Evaluation of two different orally disintegrating tablet formulations containing flurbiprofen inclusion complex and its solid dispersion

Purpose: To prepare orally dispersible tablet formulations (ODTs) by increasing the solubility of flurbiprofen (FB), which has low water solubility. &#x0D; Methods: The ODTs were prepared using direct compression method the inclusion complexes and solid dispersions with the highest solubility were further evaluated. Flurbiprofen, polyvinylpyrrolidone (PVP) solid dispersions were blended together by solvent evaporation method, while the inclusion complexes were co-formulated with beta cyclodextrin (β-CD) by kneading at three different ratios. The ODTs were characterized by differential scanning calorimetry (DSC), Fourier transform infra-red spectroscopy (FTIR) and for their micromeritic properties. In addition, the solubility properties of the inclusion complexes and solid dispersions in distilled water were compared with the solubility of flurbiprofen. &#x0D; Results: The highest solubility value of PVP-FB solid dispersions was found at 1:6 (0.501 mg/mL) and for FB β-CD inclusion complex at 1:2 (0.701 mg/mL). Angle of repose ranged from 28.09 – 32.15 (o); Carr’s index from 7.59 to 10.01; and Hausner’s ration from 1.05 – 1.15. DSC and spectral studies indicate that FB did not chemically interact with either PVP or β-CD. &#x0D; Conclusion: Orally dispersible tablets containing flurbiprofen β-CD complex exhibit significantly higher bioavailability than the drug alone due to its increased solubility. &#x0D;

A review on co-processed excipients used in direct compression of tablet dosage form

Co-processed excipients may enhance functionality and reduce drawbacks of traditional excipients for the manufacture of tablets on a commercial scale. The following study aimed to characterize a range of co-processed excipients that may prove suitable for dispersible tablet formulations prepared by direct compression. The dosage form that is used the most is tablets. Their accessibility, simplicity of administration, consistency, and affordability are advantages. Direct compression is the most straightforward method for making tablets, despite the fact that it comes with several challenges, including those connected to the homogeneity and mass variation of the content, disintegration, dissolution, and the radial hardness of the tablets. In today's world, "co-processed excipients," which include frequently processed mixtures of fillers, binders, disintegrants, lubricants, and other excipients, are becoming more popular. Spray drying, fluid bed granulation, wet granulation, melt granulation, dry granulation, and co-crystallization are used to create these mixes. This review article lists technologies, co-processed excipients that are commercially available, and excipients that are typically utilized to make them.

Stable, compounded bedaquiline suspensions to support practical implementation of pediatric dosing in the field.

BACKGROUND: Bedaquiline (BDQ) tablets are indicated as part of a combination regimen for the treatment of multidrug-resistant TB in adults, adolescents and children. A dispersible tablet formulation is now approved but is not currently available in all settings. The aim of this study was to develop stable extemporaneous liquid formulations of BDQ that can be stored at room temperature or 30°C for several weeks, to support pragmatic pediatric dosing in the field and reduce wastage.METHODS: BDQ tablets were suspended in simple syrup and a sugar-free vehicle. Each 20 mg/mL formulation was stored at room temperature or 30°C for 30 days in amber dispensing bottles. Appearance, BDQ potency, pH and microbial counts were determined on Days 0, 15 and 30.RESULTS: The BDQ potency in both formulations remained at 98-101% of the theoretical concentration for 30 days. The appearance, pH and microbial count of sugar-free formulation did not change during the 30-day storage. The simple syrup formulation was stable for 15 days as microbial growth was observed on Day 30.CONCLUSIONS: BDQ may be prepared in syrup or sugar-free suspensions: syrup suspensions can be stored for 15 days at room temperature and 30C, whereas sugar-free suspensions can be stored for 30 days at room temperature and 30C. This information will support practical BDQ dosing for children in the field.

A REVIEW ON: FORMULATION, TECHNOLOGICAL AND BENEFICIAL ASPECTS OF ORAL DISPERSIBLE TABLETS

This review is about oral dispersible tablets a novel approach in drug delivery systems that are now a day’s more focused in formulation world, and laid a new path that, helped the patients to build their compliance level with the therapy, also reduced the cost and ease the administration especially in case of pediatrics and geriatrics. Oral dispersible tablets are advantageous for pediatric, geriatric mentally ill, nausea patients who have difficulty in swallowing conventional tablets and capsules. Using various excipients, evaluation tests marketed formulation and drugs used in the research area. The advantages of mouth dissolving dosage form are increasingly being recognized in both, industry and academia. Their growing importance has been underlined recently when European Pharmacopoeia adopted the term “Oral dispersible Tablet” as tablet that is to be place in the mouth where it disperses rapidly before swallowing. When ODTs are put on tongue they disintegrate instantaneously, releasing the drug which dissolve or disperses in the saliva. Some drugs are absorbed from the mouth, pharynx and esophagus as the saliva passes down in to the stomach. In such cases, bioavailability of a drug is significantly greater than those observed from conventional tablet dosage form.

Extemporaneously compounded liquid formulations of clofazimine.

BACKGROUND: Clofazimine (CFZ) is routinely used worldwide for the treatment of leprosy and TB. However, no liquid or dispersible tablet formulations of CFZ are currently available commercially for patients with challenges ingesting soft gelatin capsules or solid formulations. The aim of this research was to develop stable extemporaneous liquid formulations of CFZ that can be stored at room temperature for several weeks to enable practical dosing in the field. METHODS: Two formulations were prepared in syrup and sugar-free vehicles with CFZ tablets using a simple method that can be used in a routine pharmacy. Suspensions were stored at room temperature and at 30°C for 30 days. Formulation aliquots were tested on Days 0, 15 and 30 for appearance, pH, potency and microbial counts. RESULTS: Appearance remained unchanged during storage. The pH of both formulations was between 4.0 and 6.0. Potency was between 90% and 110% for 30 days in the syrup formulation and for 15 days in the sugar-free formulation. Microbial counts met United States Pharmacopeia 1111 limits for oral aqueous liquids and specific organisms were absent. CONCLUSIONS: A simple field-friendly method was successfully developed for the preparation of CFZ liquid formulations using commonly available ingredients. This will permit practical dosing and titration for children and other patients with swallowing challenges.

Sugar and sugar-free liquid formulations of delamanid for patients with rifampicin-resistant TB.

BACKGROUND: Delamanid (DLM) tablets are recommended for the treatment of rifampicin-resistant TB. However, no liquid or dispersible tablet formulation of DLM is currently commercially available for patients with challenges ingesting these tablets. The aim of this study was to develop stable extemporaneous liquid formulations of DLM that can be stored at room temperature for several weeks.METHODS: DLM tablets were suspended in 1) simple syrup and 2) a specially formulated sugar-free vehicle. These suspensions containing DLM 5 mg/mL were stored in plastic prescription bottles at room temperature or 30°C for 30 days. These suspensions were evaluated for appearance, potency, pH, and microbial counts at Days 0, 15, and 30.RESULTS: The potency of DLM in each formulation remained at 98-104% of the theoretical concentration for 30 days. The appearance, pH, and microbial count did not change for the sugar-free formulation during the 30-day storage period. Microbial growth, however, was observed in the simple syrup formulation on Day 30 but not on Day 15.CONCLUSION: DLM can be formulated in sugar or sugar-free suspensions and stored at room temperature or 30°C for at least 15 and 30 days, respectively.

Implementation and comparison of different taste masking techniques to design and assess dispersible tablet formulations

The objective of this study was to assess the efficacy of several taste-masking techniques and to study the impact of different formulation variables on the physicochemical properties of dispersible tablets containing Ranitidine as a model drug. Ranitidine powder was taste masked using various techniques. Factorial design (24) was applied to design the set of tablet formulations. The four factors implemented were the manufacturing method, filler type, superdisintegrant type and superdisintegrant concentration. Levels selected were direct compression and wet granulation for the manufacturing method, microcrystalline cellulose and mannitol for the diluent type, sodium starch glycolate and croscarmellose sodium for superdisintegrant type, and 2% and 10% for superdisintegrant concentration. Granulation with calcium carbonate (ratio of 1:8) was the taste-masking method of choice to be implemented. The formulated tablets results revealed that the manufacturing method has a significant influence on all the tested physicochemical properties (p-values &lt; 0.05) such as tablet’s weight variation, hardness, friability, and disintegration time. Croscarmellose sodium obtained better results than sodium starch glycolate. Both fillers obtained good properties when implementing direct compression method with croscarmellose sodium concentration of 2%, or wet granulation method with croscarmellose sodium concentration of 10%. Drug release was also increased by increasing concentration of croscarmellose sodium. These findings represent an easy manufacturing procedure with relatively low-cost materials that can be implemented to formulate dispersible tablets of bitter tasting drugs that will enhance patient compliance and lead to faster onset of action.

Formulation and Evaluation of Quinine sulfate Dispersible Tablets with Emphasis on Taste Masking using Cyclodextrin

Dispersible tablets (DTs), also termed quick dissolving, fast melting, fast dissolving, fast disintegrating and rapid dissolving tablets, are uncoated or film-coated tablets intended to be dispersed in water before administration giving a homogeneous dispersion. Conventional quinine tablets have bitter taste when broken or dispersed to allow administration for children. Cyclodextrins (CDs) are cyclic oligosaccharides whose structural feature gives a hydrophobic interior and a hydrophilic exterior are widely used to increase the solubility of poorly soluble drugs. Recent studies showed that CDs masked taste of bitter drugs. The main objective of the present study was to formulate Quinine Sulphate as dispersible tablets via direct compression using different ratios of super-disintegrants. Three formulae were prepared (F1: Crosspovidone 5%, F2: Crosscarmellose 5% and F3: combination of crosspovidone 2.5% + crosscarmellose 2.5%). Further formulation development was done for taste improvement; four formulae were prepared based on the ratio of Quinine: Hydroxy propyl β - Cyclodextrin (HP- βCD) and the method of preparation. The prepared dispersible tablets were then evaluated for various parameters like thickness, hardness, friability, weight variation, assay of content and dispersion time. In vitro drug release profile was also determined. F3 was selected as optimized formula since it showed good dispersion time (58 sec.), acceptable limits of quality control tests and highest percentage of drug released at the end of 10 minutes. Acceptable taste for F3 was achieved when Quinine was complex at the ratio of 1:2 Quinine HP- βCD and the complex dried from water as solvent. More studies using other concentrations and/or complication methods for Cyclodextrin or other approaches are recommended for better taste masking.

Isolation, Characterization of Banana Starch and its Evaluation as a Disintegrating Agent in Dispersible Lornoxicam Tablet

Objective: The present study was designed to isolate, characterize, formulate, and evaluate the disintegration properties of banana starch in dispersible Lornoxicam tablet formulation. Methods: The alkaline extraction method used sodium hydroxide as a lye solution to isolate starch from unripe banana fruit. Starch was subjected to characterization for physicochemical properties, viscosity and flow properties, Fourier-transform infrared spectroscopy (FTIR) scanning electron microscopy (SEM), differential scanning calorimetry (DSC) and X-ray crystallography (XRD) study. Flow properties of starch were determined as per the standard procedure. Tablets were formulated by a wet granulation method using starch as a disintegrant, and the in-vitro release characteristic of the prepared tablets was analyzed. Different concentrations of isolated starch were studied for disintegrating properties compared to corn starch. Results: Studies indicate that starch obtained is qualitatively and quantitatively comparable to corn starch. SEM, FTIR, DSC and XRD data confirmed the polysaccharide nature of the starch. The physicochemical properties of starch passed the prescribed evaluation tests for tablets. These tablets also confirmed the disintegration and dissolution specifications as per Indian Pharmacopoeia. Conclusion: From the above study, it can be concluded that starch obtained from banana shows qualitatively and quantitatively good disintegration characteristics compared to corn starch. These tablets also confirmed a significant degree of dissolution as per the standards. Evaluations also specified that banana starch possesses acceptable disintegrating characteristics compared to corn starch and can be used as a disintegrant in tablet formulation.