THE STUDY ON OPTIMIZATION OF SOLID ORAL FLOATING TABLETS-A REVIEW

THE STUDY ON OPTIMIZATION OF SOLID ORAL FLOATING TABLETS - A REVIEW

Rajesh Pawar ^{* 1} and Swati Jagdale ²

MAEER’s Maharashtra Institute of Pharmacy ¹, MIT Campus, Kothrud, Pune - 411038, Maharashtra, India.

School of Pharmacy ², Dr. Vishwanath Karad MIT World Peace University, MIT Campus, Kothrud, Pune - 411038, Maharashtra, India.

ABSTRACT: The motivation behind composing this review on floating drug delivery systems (FDDS) was to incorporate the ongoing research article with a unique spotlight on the key system of floatation to accomplish gastric maintenance. The ongoing advancements of FDDS, including the physiological and formulation factors influencing gastric maintenance, ways to deal with configuration single-unit, and numerous unit of floating drug delivery systems, and their grouping and formulations perspectives are canvassed in detail. This review has a special focus on the principal mechanism of floatation to achieve gastric retention. Conventional oral dosage forms have short residence times & unpredictable gastric emptying time. The idea of gastric retention comes from the need to localize drugs at a specific region of the gastrointestinal tract (GIT), such as the stomach in the body. Many drugs get absorbed only in the upper intestinal tract, designing such molecules as once-daily formulations are exclusive for these molecules. Thus, gastro retention could help to provide greater availability of new products and consequently improved therapeutic activity and substantial benefits to patients. This article aims at reviewing the floating drug delivery system, including types, approaches for designing the floating dosage form, advantages & disadvantages of FDDS. This drug delivery system is valuable to a few issues experienced during the advancement of a pharmaceutical dosage form.

Floating drug delivery systems, Single-Unit Dosage Forms, Multi-dose, Kinetics

INTRODUCTION: Floating Drug Delivery Systems (FDDS) have a mass thickness lower than gastric liquids and, in this manner, stay light in the stomach for a delayed timeframe without influencing the gastric discharging rate.

While the dosage form float on gastric juice, sedate is discharged gradually at an ideal rate from the dosage form. After the arrival of the drug, the remaining dosage form is exhausted from the stomach. This outcome is an increment in GRT and superior control of changes in plasma tranquilizes focuses. Floating dosage forms can be character-ized into two kinds, non-effervescent dosage form, and effervescent dosage form ^1-5.

Types of Floating Drug Delivery Systems (FDDS): The accompanying methodologies have been utilized for the plan of floating measurement types of single-and various unit systems.

FIG. 1: CLASSIFICATION OF FDDS

Single-Unit Dosage Forms: In the Low-thickness approach, the globular shells having lower thickness than that of gastric liquid can be utilized as a bearer for medicating for its controlled discharge. A light dose structure can likewise be acquired by utilizing a liquid-filled dosage form that floats in the stomach. In covered shells popcorn, price, what's more, polystyrol has been abused as drug bearers. Sugar polymeric materials, for example, methacrylic polymer and cellulose acetic acid derivation phthalate have been utilized to undercoat these shells. These are additionally covered with a drug-polymer blend. The polymer of a decision can be either ethylcellulose or hydroxypropyl cellulose, relying upon the kind of discharge wanted. At long last, the item coasts on the gastric liquid while discharging the drug bit by bit over a drawn-out span ^6-8.

Liquid-filled floating chamber kind of dose structures incorporates the joining of a gas-filled floatation chamber into a microporous part that houses a drug supply. Gaps or openings are available along with the top and base dividers through which the gastrointestinal tract liquid enters to break up the drug. The other two dividers in contact with the liquid are fixed with the goal that the undissolved drug remains in that. The liquid present could be air, under fractional vacuum, or some other appropriate gas, fluid, or strong having a proper explicit gravity and inactive conduct. The gadget is of swallowable size, stays above water inside the stomach for a drawn-out time, and after the total discharge, the shell crumbles give to the digestive system and is dispensed with.

Hydrodynamically adjusted dosage forms (HBS) are intended to drag out the stay of the measurement structure in the gastrointestinal tract and help in upgrading the assimilation. Such dosage forms are most appropriate for drugs having superior solvency in acidic conditions and for the drugs having an explicit site of retention in the upper piece of the small digestive tract. It should remain in the stomach, keep up its auxiliary honesty, furthermore, discharge sedate continually from the dose structure.

The achievement of the HBS case as a extended-release dosage form is best exemplified with chlordiazepoxide hydrochloride ^{9, 10}. HBS of chlordiazepoxide hydrochloride had an equivalent blood level time profile starting at three 10-mg marketed products. Numerous polymers and polymer blends with wet granulation as an assembling system have been investigated to yield floatable tablets.

Different kinds of tablets (bilayered and matrix) have been appeared to have floatable qualities. A portion of the polymers utilized is hydroxypropyl cellulose, hydroxypropyl methylcellulose, crospovidone, sodium carboxymethyl cellulose, and ethyl cellulose. Self-adjusting floatable topsy-turvy arrangement tranquilize conveyance system employs an unbalanced 3-layer network innovation to control sedate discharge.

The 3-layer standard has been improved by an asymmetric configuration drug delivery system in request to regulate the discharge degree and accomplish zero-order discharge energy by at first keeping up a consistent territory at the diffusing front with ensuring disintegration/disintegration toward the finish of the discharge procedure. The system was planned in such a way that it floats to draw out gastric retention time in-vivo, bringing about longer all-out travel time inside the gastrointestinal tract condition with the most extreme absorptive limit and thus more noteworthy bioavailability. This specific trademark would be pertinent to drugs with pH-subordinate solvency, a limited window of assimilation, and are consumed by dynamic vehicles from either the proximal or distal segment of the small digestive tract.  Single-unit formulations are associated with sticking together or being obstructed in the gastrointestinal tract, which may have a potential danger of producing irritation.

Multiple-Unit Dosage Forms: The reason for structuring different unit measurement structures is to build up a dependable plan that has all the benefits of a solitary unit structure and is without any of the abovementioned referenced disservices of single-unit plans. In a quest for this undertaking, numerous various unit floatable measurement structures have been planned. Microspheres have a high stacking limit, and numerous polymers have been utilized, such as egg whites, gelatin, starch, polymethacrylate, polyacrylamide, and poly alkyl cyanoacrylate. Round polymeric microsponges, additionally alluded to as "micro balloons," have been arranged. Microspheres have a trademark inside an empty structure and show brilliant in-vitro flowability. In Carbon dioxide–producing different unit oral formulations, a few gadgets with highlights that broaden, unfurl, or are swelled via carbon dioxide produced in the gadgets after the organization has been depicted in the ongoing patent writing. These measurement structures are avoided from the section of the pyloric sphincter if a distance across of ~12 to 18 mm in their extended state is surpassed ^{11, 12}. Amena. et al., (2019)¹³ prepared and evaluated floating tablets of sitagliptin which is based on the effervescent approach using sodium bicarbonate in which carbon dioxide acted as a releasing agent. Formulator coalesces Sitagliptin, Gum and Guar gum, Microcrystalline cellulose (MCC), sodium bicarbonate, citric acid, Magnesium Stearate polymers in 100 mg, 140 mg, 7 mg, 35 mg, 12 mg, 6 mg, respectively as a best-optimized(S9) formulation its kinetics values mentioned in Table 1. The formulator used a 40% concentration of Guar gum and 35% of sodium bicarbonate as a floating agent to optimize the best formulation of 12 h release time and floating lag time respectively.

TABLE 1: KINETICS VALUE OF S9 FORMULATION

Sharma Aditya et al., (2019) ¹⁴ developed a novel gastro retentive drug delivery system of Tropisetron for active release by using Tropisetron, Carbopol, sodium carbonate, magnesium stearate, citric acid, talc, and lactose in 50mg, 50mg, 20mg, 30 mg, 5 mg, 15 mg, 25 mg respectively as the best formulation blend (F7), sodium bicarbonate and anhydrous citric acid used to directly compress floating tablets. The optimized formulation (F7) exhibited a 63.87% drug release in 12 h emerged as the best formulation based on drug release characteristics and in-vitro drug release study shown in Table 2.

TABLE 2: IN-VITRO DRUG RELEASE STUDY ¹⁴

Tulshi Chakraborty et al., (2019) ¹⁵ prepared and evaluated controlled release floating tablets of Cefixime, polyvinyl alcohol, sodium bicarbonate, citric acid, ethylcellulose, beeswax, carbopol-934, magnesium stearate, talc, in 200 mg, 60 mg, 45 mg, 25 mg 70 mg, 80 mg, 52 mg, 15 mg, 13 mg as an F4 batch controlled release floating tablets of the best choice for which drug released shown in Table 3. Sodium bicarbonate and citric acid are used as floating agents.

TABLE 3: CUMULATIVE % DRUG RELEASE OF TABLETS ¹⁵

Airmen et al., (2019) ¹⁶ formulated an effervescent floating drug delivery system of metformin in which Metformin (500 mg), Grewia mollies (GM) gum (2, 4, 6 8%w/w/), Eudragit RL100 (1%), Sodium bicarbonate (30%), Tartaric acid (5%), Talc (1%) Lactose (QS) is used. Sodium bi-carbonate (30%) and tartaric acid (5%) as gas generating agents. Grewia Molli's gum has been exploited in the formulation of gastro-floating matrix tablets of metformin which may find useful application for drugs that have a narrow absorption window in the upper part of the gastrointestinal tract (GIT). It was noticed that with an increase in the binder concentration of the GM gum, there was a significant increase in the hardness of the tablet. It was observed that an increase in the concentration of GM gum caused a significant increase in the FLT. The indication is that the addition of Eudragit RL100 helped to increase the integrity of the tablet formulation, therefore, showing a buoyancy duration of > 12 h. This study discovered that Grewia Mollis Gum can be used in the formulation of the gastro floating drug delivery system of metformin, and this can be beneficial in the formulation of the controlled release dosage form of metformin.

Chinna eswaraiah et al., (2019) ¹⁷ clarifies the effervescent floating matrix tablet of metronidazole and assesses the impact of fluctuating groupings of hydrophilic polymers on sedate discharge. Drug excipients association was concentrated by Fourier change infrared spectrophotometer. The effer-vescent floating matrix tablets were set up by direct pressure procedure utilizing hydroxypropyl methylcellulose (HPMCK4) and thickener alone and in the mix as discharge retardants. Micro-crystalline cellulose was utilized as diluent.

Sodium bicarbonate was utilized as an effervescent agent. The readied dosage form tablets were assessed for their physicochemical parameters such as weight variety, hardness, friability, content consistency, lightness time, and in-vitro disintegration. Micromeritic properties and post-pressure parameters were assessed, and all the parameters were found inside complying. The drug discharge information we're exposed to various models to assess release kinetics and a mechanism of drug discharge. The tablets formulate with xanthan gum, and a blend of xanthan gum and HPMCK4M have impeded the drug discharge up to 12 h. The discharge component of metronidazole was assessed based on discharge type as per in Peppas model shown in Table 5. The n estimation of the formulations went from 0.46 to 0.89, which demonstrated Case II transport and zero-order discharge. Floating Matrix tablet is a straight-forward, proficient, and economical technique to continue the arrival of metronidazole to annihilate Helicobacter pylori in peptic ulcers.

TABLE 4: CORRELATION COEFFICIENT AND RELEASE KINETICS GRFMT OF METFORMIN (N=3) PREPARED WITH VARYING CONCENTRATION OF GMG ¹⁷

TABLE 5: CORRELATION COEFFICIENTS (R) VALUES OF DRUG RELEASE KINETICS AND MECHANISM OF FLOATING MATRIX TABLETS OF METRONIDAZOLE ¹⁷

Shu Wang et al., (2019) ¹⁸ examined the formulations and assessment of gastric-floating controlled discharge tablets of Ginkgolides. The researcher used a pressure technique joined with a hydrophilic polymer, floating associate agents, and effervescent substance. Details were assessed for in-vitro drug discharge, in-vitro floating capacity and in-vivo gastro-retentive conduct by gamma scintigraphy method extended drug discharge characteristic for 12 h. The discharge practices of the tablets were fitted to the zero-order model in the coupled activity of drug dissemination and matrix disintegration instrument shown in Table 6. In-vivo practices of the tablets were seen at various time interims from the radiographic photos of the healthy volunteers and the maintenance time in the stomach was around 8 h. Results mentioned that gastric-floating tablets of the Ginkgolides had the potential for decent gastric home time and the controlled drug discharge. The optimized formulations showed good instant and total duration floating properties and extended drug release characteristic for 12 h.

TABLE 6: KINETIC RELEASE EQUATIONS OF DIFFERENT MODELS FOR OPTIMIZED FORMULATION ¹⁸

Ranjit Prasad Swain et al., (2019) ¹⁹ explained blend treatment of ezetimibe and atenolol which is profoundly alluring for better administration of dyslipidemia and hypertension. Ezetimibe has poor solvency as a result of lower bioavailability. Atenolol has poor retention in the lower gastrointestinal tract, short half-life. In this way, the present investigation was to create a gastro-bilayer floating matrix tablet in which ezetimibe was consolidated as a prompt layer and atenolol as a supported discharge layer. Solvency of the ezetimibe was improved by a strong scattering method and was described by FTIR, DSC and XRD study. Gastrobilayer floating tablets were set up by direct pressure technique. Hydroxypropyl methyl-cellulose K100 (37.5% w/w) as discharge retardant and croscarmellose sodium (15% w/w) as super disintegrants in the quick layer as upgraded. The all-out floating time of the optimized tablet was 12 h with 9 min of floating lag time. Atenolol discharge was supported through a dissemination system more than 12 h, and more than 95% ezetimibe was discharged within 30 min. It very well may be reasoned that biphasic sedate discharge design was effectively accomplished through the formulations of gastro-floating bilayer tablets right now, reinforced mix treatment for hypertension and dyslipidemia.

TABLE 7: RELEASE KINETICS OF OPTIMIZED FORMULATION ¹⁹

Ali Raza et al., (2017) ²⁰ Completed an examination meant to formulate gastro retentive floating tablets of minocycline hydrochloride with wanted floating properties, wanted drug-discharge rate, its nearby activity in the stomach for treatment of H. Pylori infection and avoidance of a reaction, pseudomembranous colitis. A simplex-mixture blend configuration was utilized to get the trial design. Methocel K100LV, Methocel K15M, and Carbopol 934 were chosen as independent factors. Ten formulations (F1 to F10) were created by direct compression and were assessed for physical parameters, growing index, floating lag time, floating time, and in-vitro drug-discharge rate. Moreover, FTIR spectroscopic investigations were performed to decide the drug-polymer connection. Floating lag time, floating time, total drug discharge at 3 h, 6 h, and 12 h were chosen as needy factors. Kinetic models of drug release for all formulations shown in Table 8 Results indicated that floating lag time and floating time were diminished by the presence of Carbopol 934 in detail while at the same time expanding by Methocel K100LV and Methocel K15M. The presence of Carbopol 934 additionally caused an expansion in the drug-discharge rate, while Methocel K100LV and Methocel K15M contributed to the diminishing discharge rate. Except for F1, the various plans showed floating time>12 h. Based on enhancement criteria, the composition of optimized formulations F10 (Methocel K100LV=7.98 mg and Carbopol 934=82.02 mg) was dictated by the measurable investigation. FTIR spectroscopic investigations demonstrated that no connection was found among polymers and drugs. Compactly, inferred that Carbopol 934 and Methocel 100LV can be utilized to create gastro retentive floating tablets of minocycline hydrochloride with great lightness properties and supported discharge activity.

TABLE 8: KINETIC MODELS OF DRUG RELEASE FOR ALL FORMULATIONS ²⁰

Faria Senjoti et al., (2016) ²¹ taken an effort on oral sustained-release floating tablet detailing of metformin HCl was structured and created. Effervescence and swelling properties were ascribed on the created tablets by sodium bicarbonate and HPMC-PEO polymer mix, individually. Tablet formation was optimized by the response surface methodology (RSM). Seventeen preliminary formulations were broke down as indicated by the Box-Behnken design where polymer substances of HPMC and PEO at 1: 4 proportions, the amount of sodium bicarbonate, and SSG were received as independent variables. Floating lag time in a sec, cumulative percent drug released at 1 h and 12 h were picked as response variables. Tablets from the optimized formulation were additionally put away accelerated stability conditions for 3 months to evaluate their stability profile. RSM could effectively enhance tablet composition with fantastic forecast capacity. In-vitro drug discharge until 12 h, floating lag time, and length of floating were subject to the measure of three chosen independent variables. Optimized tablets stayed floating for more than 24 h with a floating lag time of under 4 min. Given the best fitting strategy, the optimized formulation was found to follow the Korsmeyer-Peppas discharge kinetics. An accelerated stability study uncovered that improved formulations were steady for a quarter of a year with no significant changes in assay, disintegration profile, floating lag time, and other physical properties.

Swati Rawat et al., (2018) ²² Floating Drug Delivery Systems  (FDDS) have a mass thickness lower than gastric liquids and in this way stay light in the stomach for a drawn-out timeframe, without influencing the exhausting gastric rate. While the dosage form is floating on the gastric substance, the drug is discharged gradually at an ideal rate from the dosage form. These floating tablets, for the most part, are arranged for a decrease of lag time and discharge the drug as long as 12 h and may likewise build the bioavailability of the drugs by using the drug to full degree, staying away from the pointless recurrence of dosing.

TABLE 9: SUMMARY OF MATHEMATICAL MODELING OF RELEASE PROFILE OF AN OPTIMIZED FORMULATION ²¹

The examination included formulations of floating tablets utilizing polymers like Hydroxypropyl methylcellulose K15M, PVP K30, Sodium bicarbonate, Xanthan-Gum, Guar-gum, and microcrystalline cellulose as lattice shaping operators. The tablets were straightforwardly compacted utilizing a Lab Press multi-station revolving punching machine. FTIR and DSC-TGA examine adjusted that there was no incongruence between the polymers and the drug. Tablet formulation parameters were inside as compliance. Tablet indicated zero lag time, duration of floating for >12 h. In-vivo X-beam examines delineated that tablets kept on floating in the GIT for 12 h. The in-vitro sedate discharge example of Acyclovir floating tablets was fitted to various dynamic models, which demonstrated the most elevated relapse for zero-order energy with Koresmeyer-Pappas, and the greater part of the formulations followed Non-fickian diffusion.

TABLE 10: IN-VITRO DRUG RELEASE OF FORMULATION ²²

Q li et al., (2019) ²³ projected three-dimensional (3D) expulsions-based printing is a paste-based fast-prototyping process, which is fit for building complex 3D structures. The point of this examination was to investigate the feasibility of 3D expulsion-based printing as a pharmaceutical assembling procedure for the manufacture of gastro-floating tablets. Novel low-thickness cross-section inward structure gastro-floating tablets of dipyridamole were created to drag out the gastric home time to improve the drug-release rate and subsequently improve bioavailability and therapeutic viability. Excipients regularly utilized in the pharmaceutical examination could be productively applied in the room-temperature 3D expulsion-based printing process. The tablets were planned with three sorts of infill percentages and arranged by hydroxypropyl methylcellulose (HPMC K4M) and hydroxypropyl methylcellulose (HPMC E15) as hydrophilic networks and microcrystalline cellulose (MCC PH101) as expulsion forming specialist. In-vitro assessment of the 3D printed gastro-floating tablets was performed by deciding mechanical properties, content consistency, and weight variety. Moreover, re-floating capacity, floating-term time, and drug release conduct were likewise assessed. Disintegration profiles uncovered the connection between infill rate and drug release conduct. The aftereffects of this examination uncovered the capability of 3D expulsion-based printing to create gastro-floating tablets with more than 8 or floating procedures with conventional pharmaceutical excipients and interior grid structure plans. Results of fitting experimental release from dipyridamole floating tablets in-vitro release profiles to shown in Table 11.

TABLE 11: RESULTS OF FITTING EXPERIMENTAL RELEASE, FROM DIPYRIDAMOLE FLOATING TABLETS IN-VITRO RELEASE PROFILES TO (A) ZERO-ORDER, (B) FIRST-ORDER, (C) HIGUCHI AND (D) KORSMEYER PEPPAS KINETIC EQUATIONS ²³

FIG. 2: DRUG RELEASE PROFILES OF THE FORMULATIONS USED IN THE EXPERIMENTS (N=6): (A) COMPARISON OF COMMERCIAL FAST-RELEASE TABLETS AND DOM-FSR TABLETS, (B) THE INFLUENCE OF SHELL NUMBERS, (C) THE INFLUENCE OF INFILL PERCENTAGES, AND (D) COMPARISON OF THE TABLETS WITH OPTIMIZED PARAMETERS, TABLETS USED FOR PHARMACOKINETIC STUDY AND TABLETS USED FOR X-RAY IMAGING ²³

X. Chai et al. (2017) ²⁴ examine the attainability of combined confirmation displaying 3D prints to get ready intragastric floating continued release tablets. Domperidone, an insoluble weak base, was picked as a model drug to explore the capability of FSR in expanding its oral bioavailability and decreasing its regimen frequency. DOM has effectively stacked into hydroxypropyl cellulose fibers utilizing hot-soften expulsion. The fibers were then printed into empty organized tablets by changing the shell numbers and the infill rates. Physical portrayal results showed that most of the DOM step by step transformed into the nebulous structure during the manufacturing procedure.

The streamlined formulation displayed the continued release trademark and had the option to drift for around 10 h in-vitro. Radiographic pictures demonstrated that the BaSO4- labeled tablets were held in the stomach of rabbits for more than 8 h. Moreover, pharmacokinetic studies demonstrated the overall bioavailability of the FSR tablets contrasted and reference marketed tablets was 222.49 ± 62.85%. All the outcomes indicated that FDM-based 3D printing might be a promising method to manufacture hollow tablets with the end goal of intragastric floating drug delivery. Drug release profiles of the formulations used in the experiments are shown in Fig. 1.

Péter Diós et al., (2015) ²⁵ concentrated on planning a local, floating, mucoadhesive drug delivery framework containing metronidazole for Helicobacter pylori destruction. The face-focused focal composite structure was utilized for the assessment and streamlining of in-vitro floating and disintegration examines. Sodium alginate, low-subbed hydroxypropyl cellulose, and sodium bicarbonate focuses were the free factors in the advancement of effervescent floating tablets.

All tablets indicated worthy physicochemical properties. The factual investigation uncovered that tablets with 5.00A% sodium alginate, 38.63% L-HPC B1 and 8.45% sodium bicarbonate substance in-vitro demonstrated promising floating and disintegration properties for additional assessments. Optimized floating tablets communicated astounding floating power. They are in-vitro disintegration examines were contrasted, and two commercially accessible non-floating metronidazole products and afterward microbiologically recognized disintegration, ex-vivo separation power, rheological mucoadhesion studies, and similarity considers were completed.

Model dependent evaluation of dissolution data shown in Table 12 significant likenesses (f1, f2) between in-vitro spectrophotometrically and microbiologically identified disintegrations was found. Studies uncovered noteworthy ex-vivo mucoadhesion of optimized tablets, which were impressively expanded by L-HPC. In-vivo, X-beam CT investigations of optimized tablets indicated 8-h gastro maintenances in rodents represent by an animation arranged by a unique CT procedure.

TABLE 12: MODEL DEPENDENT EVALUATION OF DISSOLUTION DATA ²⁵

Huanbutta et al., (2019) ²⁶ developed three-dimensional printing advancements that are broadly utilized in clinical applications, mirroring the simplicity of customization and personalization. Henceforth, uses of 3D imprinting in pharmaceutical assembling may give assortment and unpredictability of pharmaceutical measurement frames that customary techniques don't. 3D printing can be utilized to deliver individualized drug and measurement structures for future restorative applications. Thus, we built up a pharmaceutical formulation as a floating controlled drug discharge tablet stacked with a metronidazole center utilizing 3D printing. The floating shell or tablet lodging was set up from polyvinyl alcohol. At first, states of tablet floating lodgings were structured and imprinted in the chamber, circle, and cone shapes. Metronidazole tablet centers were then arranged by direct pressure and were gathered into the printed tablet lodging. The researcher analyzed the impacts of states of the floating tablet lodging, shaft sizes for tranquilizing discharge, and air volumes for floating. Tube-shaped floating tablet lodgings floated steadily at the outside of the water. These tablets likewise floated quickly and for more than 4 h, and drug discharge, where over 88% after 8 h. linear regression modeling and drug release kinetics were mentioned in Table 13. Floating tablets with pore sizes of 2.0 mm and air volumes of 132 mm³ gave zero-order tranquilizes discharge in active examinations, with an r2 estimation of 0.9661.

TABLE 13: LINEAR REGRESSION MODELING AND DRUG RELEASE KINETICS OF METRONIDAZOLE-LOADED 3D PRINTED TABLETS ²⁶

Kadivar et al., (2015) ²⁷ Studied Imatinib mesylate, which is an antineoplastic specialist, has high ingestion in the upper piece of the gastrointestinal tract. Traditional imatinib mesylate (Gleevec) tablets produce quick and generally high pinnacle blood levels and require frequent administration to keep the plasma drug level at a powerful range. This may cause symptoms, decreased adequacy, and poor therapeutic administration. Along these lines, floating continued release Imatinib tablets were created to permit the tablets to be released in the upper piece of the GIT and defeat the deficiency of traditional tablets. Technique: Floating continued release Imatinib mesylate tablets were readied utilizing the wet granulation strategy. Tablets were defined utilizing Hydroxypropyl Methylcellulose, with Sodium alginate and Carbomer 934P as release-impeding polymers, sodium bicarbonate as the effervescent specialist, and lactose as a filler. Floating conduct, in-vitro drug release, and growing file examines were directed. Starting and absolute drug release length was contrasted, and a marketed tablet in 0.1 N HCl (pH 1.2) at 37 ± 0.5 °C for 24 h. Tablets were then assessed for different physical parameters, including weight variety, thickness, hardness, friability, and drug content. Subsequently, a half year of physical dependability examination and in-vitro gastro-retentive examinations were directed. Measurable information investigation uncovered that tablets containing a synthesis of 14.67% w/w HPMC K4M, 10.67%, w/w Na alginate, 1.33%, w/w Carbomer 934P, and 9.33%, w/w NaHCO₃ delivered the greatest formulations to create 24-hour supported release tablets with ideal floating conduct and palatable physicochemical attributes. Moreover, the in-vitro release study uncovered that the planned SR tablet had essentially lower C_max and higher T_max contrasted with the ordinary tablet. Therefore, defined SR tablets safeguarded persevering convergence of plasma as long as 24 h. Taking everything into account, to recommend a superior drug delivery framework with a steady, extended-release, bringing about improved retention and fewer reactions, planned CP-HPMC-SA based imatinib mesylate floating supported release tablets can be a promising contender for malignant growth chemotherapy. Release kinetics correlation coefficient (R2) parameter of Imatinib mesylate from the prepared floating sustained-release tablets shown in Table 14.

TABLE 14: RELEASE KINETICS CORRELATION COEFFICIENT (R2) PARAMETER OF IMATINIB MESYLATE FROM THE PREPARED FLOATING SUSTAINED-RELEASE TABLETS ²⁷

J. Fus (2018) ²⁸ examine gastric floating tablets that have the elements of long-haul gastric maintenance supported release and improving bioavailability however, the floating time and continued release is generally not fulfilled. Authors planned a novel gastric floating framework by joining compacted tablets with 3D printed gadgets, wherein a riboflavin tablet was contained into a gadget, named tablet-in-gadget (TiD) frameworks. Marketed poly fibers were utilized for 3D printing of the body and top of the gadget. Four sorts of TiD frameworks were readied, including non-net, halfway symmetric two-fold net, single-net, and unusual twofold net. They were structured and indicated great floating capacity, albeit just the last two TiD frameworks were chosen because of the ideal drug release. Compacted riboflavin tablets were set up with fast drug release; however, the release was profoundly impeded by the gadgets because of the obstruction impact and the slurry development. The single-net and twofold net TiD frameworks accomplished the combined release of 41% and 62% at 72 h, separately. The long haul (>72 h) gastric floating capacity of TiD frameworks was additionally exhibited on the hare models by the CT examination. TiD frameworks are suitable for oral organization dependent on their fulfilled floating capacity and controlled release, the release of riboflavin from the compressed tablets shown in Fig. 3.

FIG. 3: RELEASE OF RIBOFLAVIN FROM THE COMPRESSED TABLETS ²⁸

Huanbutta et al., (2000) ²⁹ examine to create a floating drug delivery framework by sublimation of ammonium carbonate. The core tablets contain a model drug, hydrochlorothiazide, and different levels of AMC. The tablets were then covered with various measures of the polyacrylate polymers.

The coated tablets were kept at encompassing temperature (25 °C) or relieved at 70 °C for 12 h before further examination. The floating and drug release practices of the tablets were acted in simulated gastric liquid USP without pepsin at 37 °C. The outcomes indicated that a high measure of AMC prompted the floating of the tablets. The coated tablets containing 40 and a half AMC drifted longer than 8 h with an opportunity to-buoyancy of around 3 min. The sublimation of AMC from the center tablets diminished the thickness of the framework, causing the floating of the tablets. The tablets covered with Eudragit® RL100 floating at a quicker rate than those of Eudragit. Indeed, even the covering level of polymer didn't impact an opportunity to-buoy and floating time of covered tablets containing a similar measure of AMC; the drug release from the tablets covered with higher covering levels of polymer demonstrated more slow drug release. The outcomes proposed that the sublimation method utilizing AMC is promising for the improvement of the floating drug delivery framework. Drug release profiles of floating tablets are shown in Fig. 3.

FIG. 4: DRUG RELEASE PROFILES OF FLOATING TABLETS ²⁶

CONCLUSION: Drug ingestion in the gastrointestinal tract is a profoundly variable technique, and dragging out gastric maintenance of the measurement structure expands the ideal opportunity for sedate retention. FDDS vows to be a potential methodology for gastric maintenance. Even though there are several challenges to be worked out to accomplish delayed gastric maintenance, countless organizations are centering toward commercializing this strategy.

ACKNOWLEDGEMENT: Authors are profusely thankful to the Principal, Department of Pharmaceutics, MAEER’s Maharashtra Institute of Pharmacy, Kothrud, Pune for their valuable suggestions and guidance.

CONFLICTS OF INTEREST: We declare that no conflicts of interest

REFERENCES:

1. Patel G and Siddaiah M: Formulation and evaluation of effervescent tablets, a review. Journal of Drug Delivery and Therapeutics 2018; 8(6): 296-03.
2. Dallas RT, Sharma S and Sharma M: Formulation and evaluation of gastroretentive floating tablets of lafutidine, Journal of Drug Delivery and Thera 2018; 8(5): 393-399
3. Soni H, Ghulaxe C, Upadhyay S and Pillai S: Development and in-vitro evaluation of an oral floating tablet of metronidazole. Journal of Drug Delivery and Therapeutics 2018; 8(2): 83-86.
4. Agrawal P and Banjare AT: Formulation and evaluation of directly compressed floating tablets of candesartan cilexetil for gastro retentive drug delivery. Research Journal of Pharmacy and Tech 2018; 11(7): 2804-08.
5. Sharma A, Gupta AK, Gupta MK and Sharma VA: Review: formulation and characterization of fast dissolving tablet of carvedilol. Journal of Drug Delivery and Therapeutics 2019; 9(3): 749-52.
6. Teżyk M, Milanowski B, Ernst A and Lulek J: Recent progress in continuous and semi-continuous processing of solid oral dosage forms: a review. Drug Development, and Industrial Pharmacy 2016; 42(8): 1195-14.
7. Aleksovski A, Dreu R, Gašperlin M and Planinšek O: Mini-tablets: a contemporary system for oral drug delivery in targeted patient groups. Expert Opinion on Drug Delivery 2015; 12(1): 65-84.
8. Gullapalli RP and Mazzitelli CL: Gelatin and non-gelatin capsule dosage forms. Journal of Pharmaceutical Sciences 2017; 106(6): 1453-65.
9. Park BJ, Choi HJ, Moon SJ, Kim SJ, Bajracharya R, Min JY and Han HK: Pharmaceutical applications of 3D printing technology: current understanding and future perspectives. Journal of Pharmaceutical Investigation 2019; 49: 575-85.
10. Gioumouxouzis CI, Baklavaridis A, Katsamenis OL, Markopoulou CK, Bouropoulos N, Tzetzes D and Fatouros DA: 3D printed bilayer oral solid dosage form combining metformin for prolonged and glimepiride for immediate drug delivery. European Journal of Pharmaceutics and Biopharmaceutics 2018; 120: 40-52.
11. Niharika MG, Krishnamoorthy K and Akkala M: Overview on floating drug delivery system. International Journal of Applied Pharmaceutics 2018; 10(6): 65-71.
12. Vo A, Feng QX, Morott JT, Pimparade MB, Tiwari RV, Zhang F and Repka M: A novel floating controlled release drug delivery system prepared by hot-melt extrusion. Euro Journal of Pharma and Biopharma 2016; 98: 108-21.
13. Begum RU: Formulation development and in-vitro evaluation of sitagliptin floating tablets. Development and Delivery 2019; 2(1): 25-30.
14. Aditya S, Vishkha C, Tahir N, Neelesh M, Namrata R and Vyas I: Formulation and evaluation of floating tablet of tropisetron Sharma. Journal of Drug Delivery and Therapeutics 2019; 9(2): 44-46.
15. Chakraborty TN and Saini VR: Formulation and evaluation of controlled release floating tablets of cefixime using hydrophilic polymers. International Research Journal of Pharmacy 2019; 10(1):171-75.
16. Collins O and Uwumagbe MU: Formulation and evaluation of effervescent floating matrix tablets of a biguanide using grewia mollis gum. Asian journal applied sciences 2019; 12 (2): 91-98.
17. Eswaraiah C: Design and in-vitro characterization of floating tablets of metronidazole. Asian Journal of Pharmaceutical and Clinical Research 2019; 12(3): 539-44.
18. Wang S, Wen H; Li P, Cui M, Sun W, Wang H, Liu H, Li S, Pan W and Yang X: Formulation and evaluation of gastric-floating controlled-release tablets of ginkgolides. Journal of Drug Delivery Science and Technology 2019; 51 (1): 7-17.
19. Swain RP, Pendela S and Panda S: Formulation and evaluation of gastro-bilayer floating tablets of simvastatin as immediate release layer and atenolol as sustained release layer. Indian Journal of Pharmaceutical Sciences 2016; 78(4): 458-68.
20. Raza A, Bukhari NI, Karim S, Hafiz MA and Hayat U: Floating tablets of minocycline hydrochloride: formulation, in-vitro evaluation and optimization. Future Journal of Pharmaceutical Sciences 2017; 10(3): 161.
21. Senjoti FG, Mahmood S, Jaffri JM and Mandal UK: Design and in-vitro evaluation of sustained release floating tablets of metformin HCl based on effervescence and swelling. Iranian Journal of Pharmaceutical Research 2016; 15(1): 53-70.
22. Rawat S, Sangali S and Gupta A: Formulation and evaluation of floating matrix tablets of acyclovir using 3² factorial design. Research Journal of Pharmaceutical Dosage Forms and Technology 2018; 10(1): 01-09.
23. Li Q, Guan X, Cui M, Zhu Z, Chen K, Wen H, Jia D, Hou J, Xu W and Yang X: Preparation and investigation of novel gastro-floating tablets with 3D extrusion-based printing. International Journal of Pharmaceutics 2018; 15: 325-32.
24. Chai X, Chai H, Wang X, Yang J, Li J, Zhao Y, Cai W, Tao T and Xiang X: Fused deposition modeling (FDM) 3D printed tablets for intragastric floating delivery of domperidone. Scientific Reports 2017; 7(1): 2829.
25. Diós P, Nagy S, Pál S, Pernecker T, Kocsis B, Budán F, Horváth I, Szigeti K, Bölcskei K and Máthé D: Preformulation studies and optimization of sodium alginate based floating drug delivery system for eradication of helicobacter pylori. European Journal of Pharmaceutics and Biopharmaceutics 2015; 96: 196-06.
26. Huanbutta K and Sangnim T: Design and development of zero-order drug release gastroretentive floating tablets fabricated by 3d printing technology. Journal of Drug Delivery Science and Technology 2019; 12: 77.
27. Kadivar A, Kamalidehghan B, Javar HA, Davoudi ET, Zaharuddin ND, Sabeti B, Chung LY and Noordin MI: Formulation and in-vitro, in-vivo Evaluation of Effervescent Floating Sustained-Release Imatinib Mesylate Tablet. PLOS One 2015; 2; 10(6): 1-23.
28. Fu J, Yin H, Yu X, Xie C, Jiang H, Jin Y and Sheng F: Combination of 3D Printing Technologies and Compressed Tablets for Preparation of Riboflavin Floating Tablet-in-Device (TiD) Systems. International Journal of Pharmaceutics 2018; 549(1-2): 370-79.
29. Huanbutta K, Limmatvapirat S, Sungthongjeen S and Sriamornsak P: Novel Strategy to Fabricate Floating Drug Delivery System Based on Sublimation Technique. The American Associ of Pharma Scientists 2016; 17(3): 693-9
    

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    How to cite this article:

    Pawar R and Jagdale S: The study on optimization of solid oral floating tablets-a review. Int J Pharm Sci & Res 2021; 12(3): 1399-11. doi: 10.13040/IJPSR.0975-8232.12(3).1399-11.

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