Short Disintegration Time Research Articles

Magnesium Stearate Fatty Acid Composition, Lubrication Performance and Tablet Properties

Magnesium stearate (MgSt) is a common tablet lubricant. As variations in MgSt properties are known to influence tablet attributes, the impact of MgSt fatty acid composition, particularly the significance of the stearate and palmitate contents, and its effects on tablet properties warrant further investigation. This study investigated the effect of MgSt with different stearate and palmitate contents but comparable physical properties (e.g. particle size, crystallinity, specific surface area and morphology) on lubrication performance and resulting tablet quality attributes, including mechanical strength, disintegratability and drug release. The influence of MgSt concentration and blending duration on the resulting tablet properties was also examined. Tablets produced using the lower stearate content MgSt had slightly higher tensile strength. The effect of MgSt stearate content was more apparent in the disintegration time and drug release, whereby MgSt of lower stearate content resulted in tablets with longer disintegration time and slower drug release. The lower stearate content also resulted in a lower lubrication performance, leading to a lesser reduction in tablet ejection force. As expected, a longer blending time of the tablet formulation blend with MgSt yielded tablets with reduced tensile strength, shorter disintegration time and slower drug release. Tablets with higher MgSt concentration showed a greater reduction in tensile strength, longer disintegration time and faster drug release. The study findings reinforced observations by other researchers and provided a better understanding of the fatty acid composition effects of MgSt on lubrication performance and the resulting tablet properties.Graphical

Three-Dimensional Printing of PVA Capsular Devices for Applications in Compounding Pharmacy: Effect of Design Parameters on Pharmaceutical Performance.

The creation of products with personalized or innovative features in the pharmaceutical sector by using innovative technologies such as three-dimensional (3D) printing is particularly noteworthy, especially in the realm of compounding pharmacies. In this work, 3D printed capsule devices (CDs) with different wall thicknesses (0.2, 0.3, 0.4, 0.6, and 0.9 mm) and sizes were designed and successfully fabricated varying printing parameters such as extrusion temperature, printing speed, material flow percent, and nozzle diameter. The physicochemical, pharmaceutical, and biopharmaceutical performance of these CDs was evaluated with the aim of achieving an immediate drug release profile comparable to hard gelatin capsules (HGC) for use in magistral compounding. It was observed that the disintegration time of the CDs increased with wall thickness, which correlated with a slower drug release rate. CDs with configurations presenting 0.4 mm wall thickness and sizes comparable to HGC n° 0, 1, and 2 demonstrated satisfactory weight uniformity, short disintegration times, and immediate drug release, indicating their potential as effective devices in future compounding pharmacy applications. In addition, a modified Weibull-type model was proposed that incorporates wall thickness as a new variable in predicting dissolution profiles. This model improves the process of selecting a specific wall thickness to achieve the desired dissolution rate within a specified time frame.

Fabrication, optimization, and evaluation of lyophilized lacidipine-loaded fatty-based nanovesicles as orally fast disintegrating sponge delivery system

Lacidipine (LCD) is a potent antihypertensive agent. Fatty-based nanovesicles (FNVs) were designed to improve LCD low solubility and bioavailability. LCD-FNVs were formulated according to different proportions of cetyl alcohol, cremophor®RH40, and oleic acid adopting Box-Behnken Design. The optimized LCD-FNVs, composed of cetyl alcohol 48.4 mg, cremophor®RH40 120 mg, and oleic acid 40 mg, showed minimum vesicle size (124.8 nm), maximum entrapment efficiency % (91.04 %) and zeta potential (-36.3 mV). The optimized FNVs were then used to formulate the lyophilized orally fast-disintegrating sponge (LY-OFDS). The LY-OFDS had a very short disintegration time (58 sec), remarkably high % drug release (100 % after 15 mins), and increased the drug transbuccal permeation by over 9.5-fold compared to the drug suspension. In-vivo evaluation of antihypertensive activity in rats showed that the LY-OFDS reduced blood pressure immediately after 5 min and reached normal blood pressure 4.5-fold faster than the marketed oral tablets. In the In-vivo pharmacokinetic study in rabbits, the LY-OFDS showed 4.7-fold higher bioavailability compared with the marketed oral tablet. In conclusion, the LY-OFDS loaded with LCD-FNVs is a safe, and non-invasive approach that can deliver LCD effectively to the blood circulation via the buccal mucosa giving superior immediate capabilities of lowering high blood pressure and increasing the drug bioavailability.

Sodium Starch Glycolate (SSG) from Sago Starch (Metroxylon sago) as a Superdisintegrant: Synthesis and Characterization.

The characteristics of sago starch exhibit remarkable resemblances to those of cassava, potato, and maize starches. This review intends to discuss and summarize the synthesis and characterization of sodium starch glycolate (SSG) from sago starch as a superdisintegrant from published journals using keywords in PubMed, Scopus, and ScienceDirect databases by Preferred Reporting Items for Systematic Reviews and Meta-Analyses (PRISMA 2020). There are many methods for synthesizing sodium starch glycolate (SSG). Other methods may include the aqueous, extrusion, organic solvent slurry, and dry methods. Sago starch is a novel form of high-yield starch with significant development potential. After cross-linking, the phosphorus content of sago starch increases by approximately 0.3 mg/g, corresponding to approximately one phosphate ester group per 500 anhydroglucose units. The degree of substitution (DS) of sodium starch glycolate (SSG) from sago ranges from 0.25 to 0.30; in drug formulations, sodium starch glycolate (SSG) from sago ranges from 2% to 8% w/w. Higher levels of sodium starch glycolate (SSG) (2% and 4% w/w) resulted in shorter disintegration times (within 1 min). Sago starch is more swellable and less enzymatically digestible than pea and corn starch. These investigations demonstrate that sago starch is a novel form of high-yield starch with tremendous potential for novel development as superdisintegrant tablets and capsules.

Effect of Powdered Cellulose Nanofiber with Different Particle Sizes on the Physical Properties of Tablets Manufactured via Direct Compression.

Direct compression is a tableting technique that involves a few steps in non-demanding manufacturing conditions. High strength and rapid disintegration of tablet formulations were previously achieved through the addition of cellulose nanofibers (CNFs), which have recently attracted attention as a high-performance biomass material. However, CNF addition results in greater variation in tablet weight and drug content, potentially due to differences in particle size between CNF and other additives. Herein, we used pulverized CNF to evaluate the effect of CNF particle size on the variation in tablet weight and drug content. Tablet formulations consisted of CNF with different particle sizes (approximately 100 µm [CNF100] and 300 µm [CNF300], at 0, 10, 30, or 50%), lactose hydrate, acetaminophen, and magnesium stearate. Ten powder formulations with different particle sizes and CNF concentrations were prepared; thereafter, the tablets were produced using a rotary tableting press with a compression force of 10 kN. The variation in weight and drug content as well as the tensile strength, friability, disintegration time, and drug dissolution of tablets were evaluated. CNF100 addition to the tablets reduced the weight and drug content variation to a greater extent than CNF300 addition. Using CNF300, we produced tablets of sufficient strength and short disintegration time. These properties were also achieved with CNF100 addition. Our findings suggest that adding CNF of small particle size to the tablet formulation can reduce the variation in weight and drug content while maintaining high strength and short disintegration time.

Investigating the Impact of Co-processed Excipients on the Formulation of Bromhexine Hydrochloride Orally Disintegrating Tablets (ODTs)

PurposeOrodispersible tablets (orally disintegrating tablets, ODTs) have been used in pharmacotherapy for over 20 years since they overcome the problems with swallowing solid dosage forms. The successful formula manufactured by direct compression shall ensure acceptable mechanical strength and short disintegration time. Our research aimed to develop ODTs containing bromhexine hydrochloride suitable for registration in accordance with EMA requirements.MethodsWe examined the performance of five multifunctional co-processed excipients, i.e., F-Melt® C, F-Melt® M, Ludiflash®, Pharmaburst® 500 and Prosolv® ODT G2 as well as self-prepared physical blend of directly compressible excipients. We tested powder flow, true density, compaction characteristics and tableting speed sensitivity.ResultsThe manufacturability studies confirmed that all the co-processed excipients are very effective as the ODT formula constituents. We noticed superior properties of both F-Melt’s®, expressed by good mechanical strength of tablets and short disintegration time. Ludiflash® showed excellent performance due to low works of plastic deformation, elastic recovery and ejection. However, the tablets released less than 30% of the drug. Also, the self-prepared blend of excipients was found sufficient for ODT application and successfully transferred to production scale. Outcome of the scale-up trial revealed that the tablets complied with compendial requirements for orodispersible tablets.ConclusionsWe proved that the active ingredient cannot be absorbed in oral cavity and its dissolution profiles in media representing upper part of gastrointestinal tract are similar to marketed immediate release drug product. In our opinion, the developed formula is suitable for registration within the well-established use procedure without necessity of bioequivalence testing.

The effect of polymeric binder type and concentration on flow and dissolution properties of SMEDDS loaded mesoporous silica-based granules

Self-microemulsifying drug delivery systems (SMEDDS) are lipid-based formulations, designed to improve the solubility of poorly-water soluble drugs. Mesoporous silica is frequently used for SMEDDS solidification by various techniques. One of them is wet granulation, which enables achieving both high SMEDDS load and good flow properties. This study investigated the effect of six polymeric binders’ addition to granulation dispersion (GD) (povidone K30, povidone K90, copovidone, Pharmacoat® 603, Pharmacoat® 615 and Methocel™ K100 Premium LV) on characteristics of produced SMEDDS granules, prepared by wet granulation. By incorporation of polymer in GD, it was possible to produce mesoporous silica-based free-flowing granules, with preserved self-microemulsifying properties, responsible for improved in vitro release of carvedilol. The incorporation of higher molecular weight binders resulted in slower in vitro release, while high binder concentration was related to faster drug release. The highest release rate was achieved with povidone K30 at 7.45 % binder concentration, as corresponding granules exhibited complete drug release already in 5 min. Granulation method (manual vs. high-shear) influenced the release rate of carvedilol as it was released slower from SMEDDS granules prepared using the granulator.Finally, SMEDDS tablet formulation was optimized to achieve maximum granule content and adequate tablet hardness. Increased granule content found to negatively influence tablet hardness, as maximum granule content of 25 % was needed to obtain appropriate hardness. Such tablets exhibited short disintegration time, so this final prototype can be considered as orodispersible tablet.

Process Optimization of Sea Buckthorn Fruit Powder Effervescent Tablets by Random Centroid Methodology Combined with Fuzzy Mathematical Sensory Evaluation

Solid beverages of effervescent tablets have good taste and portable features and are favored by consumers, but product quality and nutrition cannot meet the need of increasing nutritional requirements. Sea buckthorn fruit has a special flavor and nutrient-rich characteristics, but the related products of effervescent tablets have not been developed. In this paper, different additive contents (sea buckthorn fruit powder, erythritol, disintegrant, maltodextrin, polyvinylpyrrolidone (PVP)) were optimized using the random centroid method; the obtained effervescent effect sensory evaluation characteristics (appearance, beverage, appearance, taste, solubility) were used to establish a fuzzy mathematic model for sensory evaluation method of process optimizing; and the nutritional components and characteristics of optimized sea buckthorn powder effervescent tablets were compared to the ones of the commercial product. The results show that the optimal process conditions (47.7% sea buckthorn fruit powder, 1.3% erythritol, 1:1 disintegrant ratio, 2% maltodextrin and 2.9% PVP) were obtained according to the highest fuzzy comprehensive sensory score (87.76). Moreover, the optimized one contains a higher content of vitamin C (50.36 mg/100 g), carotenoids (10.18 mg/100 g), total phenols (11.52 GAE/g), and total flavonoids (28.46 mg RE/100 g), as well as a shorter disintegration time (10 s). The results indicate the RCO, combined with fuzzy mathematical sensory evaluation, is preferably suitable for effervescent tablet process optimization, and the quality indicators met the requirements of the effervescent tablet.

Development of canagliflozin nanocrystals sublingual tablets in the presence of sodium caprate permeability enhancer: formulation optimization, characterization, in-vitro, in silico, and in-vivo study

Canagliflozin (CFZ) is a sodium-glucose cotransporter-2 inhibitor (SGLT2) that lowers albuminuria in type-2 diabetic patients, cardiovascular, kidney, and liver disease. CFZ is classified as class IV in the Biopharmaceutical Classification System (BCS) and is characterized by low permeability, solubility, and bioavailability, most likely attributed to hepatic first-pass metabolism. Nanocrystal-based sublingual formulations were developed in the presence of sodium caprate, as a wetting agent, and as a permeability enhancer. This formulation is suitable for children and adults and could enhance solubility, permeability, and avoid enterohepatic circulation due to absorption through the sublingual mucosa. In the present study, formulations containing various surfactants (P237, P338, PVA, and PVP K30) were prepared by the Sono-homo-assisted precipitation ion technique. The optimized formula prepared with PVP-K30 showed the smallest particle size (157 ± 0.32 nm), Zeta-potential (−18 ± 0.01), and morphology by TEM analysis. The optimized formula was subsequently formulated into a sublingual tablet containing Pharma burst-V® with a shorter disintegration time (51s) for the in-vivo study. The selected sublingual tablet improved histological and biochemical markers (blood glucose, liver, and kidney function), AMP-activated protein kinase (AMPK), and protein kinase B (AKT) pathway compared to the market formula, increased CFZ’s antidiabetic potency in diabetic rabbits, boosted bioavailability by five-fold, and produced faster onset of action. These findings suggest successful treatment of diabetes with CFZ nanocrystal-sublingual tablets.

Gelatinized tapioca starch−magnesium aluminum silicate nanocomposites: Physicochemical characterization and evaluation for modified-release tablets

The objectives of this work were to prepare and investigate gelatinized tapioca starch-magnesium aluminum silicate (GTS-MAS) composites for use in modified-release tablets. The dispersions consisting of GTS and MAS with various ratios and %solid content were prepared and dried by spray drying to get the GTS-MAS composites. GTS could molecularly interact with MAS via hydrogen bonding, leading to an enhancement of thixotropic properties in the dispersion and the formation of exfoliated nanocomposites after drying. The GTS-MAS composites presented an elliptical shape with wrinkle shrinkage, powder bulkiness, and poor particle flowability. However, they had better particle flowability and tablet compressibility than the GTS particles. The drug-loaded GTS-MAS tablets provided remarkably higher hardness than the drug-loaded GTS tablets. The shorter disintegration time and the faster drug release of the tablets were found when increasing MAS ratios because the composites with higher MAS ratios displayed higher swelling capacity in both acidic and neutral media. Thus, drug diffusion coupled with swelling/erosion of the gel matrix could retard drug release from tablets. These findings suggested that the GTS-MAS nanocomposites could be employed as a matrix former in tablets intended for modifying drug release.

Oral Dissolving Film of Rivastigmine: Optimization Using Factorial Design

PurposeDue to impairments in memory and judgment, it is difficult for dementia patients to understand why they need medicine. Moreover, they often have swallowing difficulties. In this investigation, an oral dissolving film of rivastigmine tartrate (RT-ODF) was developed, offering a unique and convenient formulation for dementia patients.MethodsRT-ODF was developed using a solvent-casting technique. Sodium alginate and sodium carboxymethyl cellulose were used as film-forming polymers, and glycerol was used as a plasticizer. A full factorial design (32) was employed to estimate the impact of two factors at three levels: polymer concentration (1, 1.5, and 2% w/v) and plasticizer concentration (30, 40, and 50% w/v) on the responses, i.e., the tensile strength (TS), the disintegration time (DT), and the quantity of drug released (Q10 min).ResultsThe optimized formula (A1) that had the highest desirability value (0.923) exhibited the lowest tensile strength (3.67 ± 0.72 MPa), the shortest disintegration time (20 ± 2.0 s), and the highest percentage of drug released after 10 min (97.12 ± 2.01%). It was composed of 1% w/v sodium alginate (ALG-Na) and plasticized with 30% w/v glycerol. The pharmacokinetic study revealed that the RT-ODFs enhanced the drug’s bioavailability by 1.91-fold relative to the reference product (Exelon® capsule).ConclusionOral dissolving films of rivastigmine tartrate could be a promising approach to promote drug bioavailability and convenience for geriatric patients.

Fabrication of Direct Compressible Tablets Containing Chatuphalathika Extract Obtained through Microwave-Assisted Extraction: An Optimization Approach

This research sought to optimize the microwave-assisted extraction of Chatuphalathika as an herbal recipe maximizing the active compounds and the antioxidant activity by the Box–Behnken design. Three factors—microwave power, time, and cycle—were varied. Eight responses—extraction yield, total phenolic content, gallic acid content, corilagin content, chebulagic acid, chebulinic acid, IC50 from DPPH assay, and IC50 from FRAP assay—were monitored. Furthermore, cytotoxicity was evaluated to ensure the safety of the extract. After that, the optimized extract was compressed into tablets. The results showed that the optimal condition of the microwave-assisted extraction gave the simultaneous maximum extraction yield, total phenolic content, and antioxidant activity with a microwave power of 450 W for 30 s and 3 cycles. The extract obtained from the optimal condition exhibited a good safety profile although a concentration of 5 mg/mL was used. The optimized tablets were achieved when a compression force of 1500 psi and magnesium stearate of 1% were applied, and no sodium starch glycolate was added. In conclusion, the optimal green extraction method could be used for the extraction of the Chatuphalathika. Furthermore, the fabrication of Chatuphalathika tablets was successful, as the tablets had low friability with a short disintegration time.

Application of Microwave-Assisted Drying to Shorten Granules Drying Process for the Preparation of Thunbergia laurifolia Lindl. Leaf Tablets

Thunbergia laurifolia Lindl. is a medicinal plant that belongs to the family of Acanthaceae. It possesses several biological and pharmacological activities. According to the Thai National List of Essential Medicines, T. laurifolia leaves are used for the treatment of fever. This work sought to optimize microwave-assisted drying of Thunbergia laurifolia Lindl. leaf granules to shorten the granule drying process by the 32 full factorial design. Power was varied from 300, 450 and 600 W for 5, 10 and 15 min, to minimize moisture content and maximize rosmarinic acid content. Results showed that the optimal microwave-assisted drying condition within the design space and control space was the power of 450 W for 13 min. This condition gave the moisture content of 4.77 ± 0.24 % and rosmarinic acid content of 0.0566 ± 0.0075 %. The HPLC method was validated; it showed good linearity, specificity, precision, and accuracy. Furthermore, the system suitability was achieved. The T. laurifolia leaf granules obtained from the optimal microwave-assisted drying condition were further used to prepare T. laurifolia leaf tablets by the wet granulation method. Three batches of 650 mg tablets containing 250 mg of T. laurifolia leaf powder were prepared using different compression forces: 500, 1,000 and 1,500 psi. The suitable compression force was 1,500 psi; the tablet formulation had suitable hardness (9.88 ± 0.52 kP), low friability (0.20 %), and a short disintegration time (23.17 ± 0.76 s). Rosmarinic acid marker was dissolved from the tablets for approximately 75 % within 4 h when 0.5 % sodium lauryl sulfate aqueous solution was used as dissolution medium. In conclusion, microwave-assisted drying could be applied in preparing T. laurifolia leaf tablets by shortening the granules drying time. HIGHLIGHTS The 32 full factorial design was applied to optimize microwave-assisted drying of Thunbergia laurifolia leaf granules The optimal microwave-assisted drying condition providing the low moisture content with high rosmarinic acid content was the power of 450 W for 13 min The tablets prepared from laurifolia leaf granules had suitable hardness, low friability, short disintegration time, and a high percentage of rosmarinic acid marker dissolved GRAPHICAL ABSTRACT

Embedding of Poorly Water-Soluble Drugs in Orodispersible Films-Comparison of Five Formulation Strategies.

The poor bioavailability of many newly developed active pharmaceutical ingredients (APIs) poses a major challenge in formulation development. To overcome this issue, strategies such as the preparation of amorphous solid dispersions (ASDs), and the application of the APIs in lipid nanocarriers or the wet-milling of the substances into nanoparticles have been introduced. In addition to an efficient formulation strategy, a dosage form that is accepted by all patients is also of great importance. To enable a simple application of the oral dosage form for all patients, orodispersible films (ODFs) are a very promising delivery platform for the APIs because the films directly disintegrate in the mouth. In this study, two poorly water-soluble APIs, fenofibrate and naproxen, were formulated using five different formulation strategies and then embedded in ODFs. It was found that the deliverable amount of API with one ODF highly depends on the formulation strategy as well as the physicochemical properties of the formulated API. The most promising film formulations were ASD-ODFs as well as films with API-loaded lipid nanoemulsions. Both showed a reduction of the dissolution time of the APIs from the ODF compared to an ODF with unformulated API micro particles. In addition, short disintegration times were achieved, although the mechanical film properties were slightly worse compared to the API-free film formulation.

Microcrystalline cellulose promotes superior direct compressed Boesenbergia rotunda (L.) Mansf. extract tablet properties to spray-dried rice starch and spray-dried lactose

This work aimed to select tablet diluent of Boesenbergia rotunda (L.) Mansf. extract tablet. Three tablet diluents, including microcrystalline cellulose (MCC), spray-dried rice starch, and spray-dried lactose were used. MCC exhibited superior performance to the other diluents by providing the hardest tablet, the lowest friability, and the shortest disintegration time. The Box-Behnken design was used to evaluate the effect of hydrophobic excipients when MCC was used as diluent. The optimal formulation was composed of fumed silica 1%, magnesium stearate 1%, and talcum 2%. The tablets had suitable hardness, low friability, and short disintegration time. The marker pinocembrin could be dissolved by 82% within 4 h. Although the marker decreased after three months of stability testing, the antioxidant activity of the formulation remained. In conclusion, MCC was shown to be superior to the other diluents, and the optimal formulation could be used to prepare Boesenbergia rotunda (L.) Mansf. extract tablet as a food supplement.

Design and development of orally disintegrating films: A platform based on hydroxypropyl methylcellulose and guar gum

From a design of experiments (DOE) performed under four independent variables, with the filmogenicity conditions and shortest disintegration time as the answers, a new oral disintegrating film (ODF) based on hydroxypropyl methylcellulose (HPMC) and guar gum (GG) with the essential oil of Plectranthus amboinicus L. (EOPA) was developed. Sixteen formulations were tested for filmogenicity, homogeneity, and viability. The better selected ODF required 230.1 s for complete disintegration. The retention rate of the EOPA was quantified using the nuclear magnetic resonance hydrogen technique (H1 NMR), which identified the presence of 0.14 % carvacrol. The scanning electron microscopy showed a smooth and homogeneous surface with the presence of small white dots. Through the disk diffusion test, the EOPA was able to inhibit the growth of clinical strains of the Candida genus and gram-positive and gram-negative bacterial strains. This work opens new perspectives for the development of antimicrobial ODFS used in clinical practice.

Rapid oral transmucosal delivery of zaleplon–lavender oil utilizing self-nanoemulsifying lyophilized tablets technology: development, optimization and pharmacokinetic evaluation

Based on the administration convenience, transmucosal buccal drug delivery allows special strength points over peroral routes for systemic delivery. It could achieve local or systemic effect and boost drugs’ bioavailability for agents with first pass metabolism. The current study aimed to manufacture and optimize a lavender oil–based nanoemulsion loaded with zaleplon and incorporate it into fast-disintegrating tablets to promote its dissolution and oral bioavailability via oral mucosa. Zaleplon-loaded nanoemulsions were devised with various levels of lavender oil (10% to 25%), the surfactant Sorbeth-20 (35% to 65%), and the co-surfactant HCO-60 (20% to 40%); the extreme vertices mixture statistical design was adopted. The droplet size and drug-loading efficiency were the evaluated. The optimal formulation was transformed into self-nanoemulsified lyophilized tablets (ZP-LV-SNELTs), which were tested for their uniformity of content, friability, and disintegration time with in-vitro release. Finally, the pharmacokinetic parameters of the ZP-LV-SNELTs were determined and compared with those of marketed formulations. The optimal nanoemulsion had a droplet size of 87 nm and drug-loading capacity of 185 mg/mL. ZP-LV-SNELTs exhibited acceptable friability and weight uniformity and a short disintegration time. The in-vitro release of ZP-LV-SNELTs was 17 times faster than that of the marketed tablet. Moreover, the optimal ZP-LV-SNELTs increased the bioavailability of zaleplon in rabbits by 1.6-fold compared with the commercial tablets. Hence, this investigation revealed that ZP-LV-SNELTs delivered zaleplon with enhanced solubility, a fast release, and boosted bioavailability thru oral mucosa which provided a favorable route for drug administration which is suggested to be clinically investigated in future studies

Development of Oro-Dispersible Tablet of Meclizine by Using Different Superdisintegrating Agents

The proposed study is development of oro-dispersible tablet containing meclizine hydrochloride solid dispersion (FMODDs) formulation with using natural superdisintegrant with direct compression. The superdisintegrants and its concentration shall be during the preparation of FMODDs with meclizine hydrochloride by using direct compression via employing different excipients in different ratio including: superdisintegrants {sodium starch glycolate (SSG), Ac-Di-Sol, crosspovidone (CP), Spray dried lactose and microcrystalline cellulose (MCC)} which were used alone and in various combination and mannitol, along with lubricant and glidants. The object of proposed work was preparation of FMODDs with a short disintegration time, sufficient mechanical strength, better patient compliance, and acceptable stability profile by employing different methods of preparation and studying different variables affecting pre and post-compression parameters of formulas of meclizine hydrochloride. The combination of agents have more disintegrating property due to rapid water uptake and dispersion time which lead to rapid release of drug and made the dissolution faster. The results of the release kinetics study showed that all the formulations obeyed first order drug release profile more closely, i.e., the release rate depended upon the initial concentration of drug.
 Keywords: Solid dispersion, Oro-dispersible, Fast disintegration, Direct compressed tablet, Meclizine hydrochloride, Superdisintegranting agents

Quality by design approach for anti-hyperthyroid immediate release tablet of carbimazole

The current study to formulate, evaluate and optimize carbimazole immediate release tablet by using quality by design approach. The look at of optimization formula and experimental design had been done with the aid of using design parameter primarily based totally on Box-Behnken design. Immediate release dosage form for rapid efficacy and inhibit the peroxidase enzymes and act as thyroid inhibitor. Method: Immediate release carbimazole tablets were manufactured by dry granulation using Quality by Design. The optimization of the formulation of tablets is done by examining the profile of the objective quality product. Microcrystalline cellulose, anhydrous lactose and magnesium stearate were all included in experiments designed using the Box-Behnken design. Their concentrations are influenced by the drug disintegration and release factor f2. Result: Optimized batch formulation shows immediate drug release with short disintegration time. In anova models are significant. Conclusion: The utilization of bound together quality by design approach for successful advancement of an IR carbimazole tablet. The effective tablet created with Box-Behnken designs.

Optimization of Microwave-Assisted Granules Drying for Preparation of Tomato Extract Tablets Using Wet Granulation Method

This work aimed to optimize tomato extract granule drying using a microwave to shorten the granule drying process by the 32 full factorial design. The power and time of the microwave were optimized to minimize moisture content and maximize lycopene content. Power was varied from 300 W, 450 W, and 600 W for 10 min, 15 min, and 20 min. Results showed that the optimal condition within the design space and control space was the power of 450 W for 17 min. This condition gave the moisture content of 2.09 ± 0.15% and lycopene content of 0.0798 ± 0.0031%. A low percent error of the prediction was found, indicating that the prediction by a computer program was accurate and reliable. The granules obtained from the optimal condition were further used to prepare tomato extract tablets. Three batches of 650 mg tomato extract tablets were prepared using 1500 psi compression force. All three batches had a hardness of 9.19-10.18 kP, low friability (0.026-0.033%), short disintegration time (1.44-1.70 min), and lycopene content of approximately 0.19%. This work was the first report on optimizing tomato extract granule drying using a microwave-assisted technique according to scientific novelty. In summary, microwave-assisted drying could be applied in preparing tomato extract tablets by shortening the granules drying process.