Floating Lag Time Research Articles

Controlled Release Bilayer Floating Effervescent and Noneffervescent Tablets Containing Levofloxacin and Famotidine

The present study is aimed at designing bilayer-floating tablets to improve the drug concentration in the stomach for enhanced therapeutic efficacy. The tablets are comprised of an upper layer of levofloxacin (466.5 mg) and a lower layer of famotidine (133.5 mg). Five formulations (F1-F5) were developed by using hydroxypropyl methylcellulose grades (K4M, K15M, and K100M) along with Carbopol 934. In the case of the effervescent system (F1-F3), sodium bicarbonate was added to impart buoyancy to the tablets; while in the case of noneffervescent formulations (F4 & F5), guar gum and xanthan gum were incorporated to induce flotation and swelling and retard the release of a drug. The precompression characteristics of tablets depict the suitability of all formulation powder for direct compression. The ATR-FTIR analyses have shown that the components of both effervescent and noneffervescent tablets are compatible with each other. The total weight of each tablet was 600 mg, with a weight variation of about ≤10 mg. Both the layers were smooth and flat with a thickness ranging from 3.16±0.04 to 3.54±0.01 mm. The diameters of prepared floating tablets were about 15 mm, optimum for oral administration. After adjusting the tablet’s hardness to 6-7 kg/cm2, its friability was found to be <0.35 percent. The mean drug content of the formulations was above 90%. The floating lag time of all formulations (F2-F5) was below 25 seconds, except F1 which took almost 50 seconds to start floating on the surface of gastric content due to its higher density. The total floating time of effervescent (F1-F3) and noneffervescent formulations was in the range of 15-25 hours, thereby providing sufficient time to complete drug release and absorption in the gastric area. The total floating time of noneffervescent formulations was higher (p≤0.05) than effervescent formulations due to efficient wettability and swelling characteristics. The release of drugs from both layers of noneffervescent tablets was significantly controlled when compared to the effervescent system, and an anomalous non-Fickian diffusion was found for the drug release. The stability study of the optimized formulation proved the integrity and stability of the developed formulation. Thus, developed formulations are deemed suitable for controlled codelivery of active pharmaceutical ingredients for the effective treatment of H. pylori.

Quality by design approach for the formulation of bilayer tablets of domperidone and itopride in gastro esophageal reflux disease

In the current work, a bilayer tablet of itopride gastroretentive and domperidone immediate release formulation was developed showing the synergistic effect of gastric motility in gastroesophageal reflux disease, through antidopaminergic and antiacetylcholine stearic activities. A bilayer tablet of domperidone and itopride was optimized using quality by design and its product performance was analyzed. Itopride was designed to be gastroretentive and remains in the stomach for a longer period, providing sustained release. The domperidone layer was optimized by an empirical hit and trial method, while the itopride layer was optimized using the Box Behnken experimental design. Three independent variables were considered as hydroxypropyl methyl cellulose K 100 M, xanthum gum, and Carbomer 974 with dependent variables like floating lag time, swellable index, and percentage drug release at 24 hours. Quality target product profile and critical quality attributes were studied which helps in an effective way to develop bilayer tablets. The excipients were chosen based on the time taken by medicaments to be released and the quantity was optimized according to Handbook of Pharmaceutical Excipient. From the optimization processes, DF5 and IH2 were selected as optimized composition for the formulation of domperidone and itopride layer of bilayer tablet respectively. The bilayer tablets were formulated in 16 × 8.26 mm oblong plain biconcave die and punch. The in-vitro drug release of domperidone was 99.39% in 30 minutes and itopride was 27.50%, 53.45%, and 93.65% at 4, 16, and 24 hours respectively.

In-vitro Evaluation and Optimization of Sacubitril and Valsartan Floating Tablet using Natural Polymer

Oral systems have become gradually extensive for human consumption because of their numerous advantages, such as formulation efficiency, cost-effectiveness, and patient safety compliance. These systems offer a versatile platform for controlled drug release, allowing precise targeting of absorption site in the gastrointestinal tract. Accomplishing ideal therapeutic results for certain medications often requires precise control of drug release at specific locations within the gastrointestinal tract. In this study, our goal was to create a floating drug delivery system for two vital cardiovascular medications, sacubitril and valsartan. Our specific objectives were to extend floating time, prolong stomach residency, and reduce floating lag time. The strategy involved harnessing the synergistic potential of natural polymers in optimal proportions to enhance drug activity. Following the principles of quality by design (QbD), we systematically explored various formulation factors to optimize the drug delivery system. Analysis of tablet characteristics revealed significant variations in key parameters, such as swelling index, floating lag time (FLT), total floating time (TFT), and drug content for both sacubitril and valsartan. The enhanced formulation (F12) stood out with a remarkable swelling index of 93.4%, a floating lag time of 6.7 seconds, and an impressive total floating time of 12 hours. Furthermore, high drug content percentages were achieved, with sacubitril at 98.70% and valsartan at 94.65%. The successful development and optimization of the floating tablet formulation carry substantial clinical implications. The extended gastric retention, controlled drug release, and high drug content of the optimized formulation suggest enhanced bioavailability and therapeutic efficacy for both sacubitril and valsartan. The prolonged total floating time offers convenience to patients, potentially improving medication adherence in managing cardiovascular diseases. In conclusion, this study highlights the formulation and optimization of floating tablets as a noteworthy advancement in drug delivery technology, promising improved therapeutic outcomes and enhanced patient convenience.

The Development of Alternative Dosage Form for Creatine Monohydrate: A Floating Tablet

Creatine monohydrate has been developed as a neuroprotective agent and can penetrate in vitro model of the blood-brain barrier. However, its delivery is hampered by its limited capacity of creatine transporter. The floating system is known to increase the residence time of drugs in the stomach; thus, the active substances can be absorbed more optimally. Therefore, this study is aimed to develop creatine monohydrate floating tablets by optimizing the proportion of HPMC K100M and NaHCO2 and evaluating the quality of floating tablets. The formula was designed Simplex Lattice Design method. Tablets were prepared by the wet granulation method and evaluated for granule and tablet parameters. The results showed that HPMC K100M significantly increased flow time, absorption rate, hardness, floating time, swelling index; decreased index tap, fragility, and floating lag time. Meanwhile, an increase in NaHCO2 significantly affects an increase in floating lag time. The optimum formula obtained was 18.87% HPMC K100M and 21.12% NaHCO2. Verification of the optimum formula showed that tablet parameters were not significantly different from the predicted formula. The studies suggest that this prototype can be developed to increase creatine residence time in the stomach.

Shellac‐based drug delivery system with controlled drug‐release and tunable intragastric floating‐retention properties

AbstractIntragastric floating‐retention drug delivery system (IFRDDS) could effectively prolong drug‐releasing time, achieving a good clinical efficacy of encapsulated drug. In this research, the green amphiphilic resin, shellac was adopted to fabricate a continuous network as the matrix of IFRRDS by their self‐assembly behavior triggered by H+. Meanwhile, the NaHCO3 and hydroxypropyl methyl cellulose (HPMC) acted as a forming agent and a precipitating agent to control the floating behavior, respectively, which could create a porous structure for lowering the true density of the tablet and continuously absorb water to enhance the density of tablet, respectively. Interestingly, the synergistic effect of NaHCO3 and HPMC was beneficial to the initiation of the floating of the complex tablet. By regulating tablet's constitution, we could tune the floating lag time, floating time, and drug‐release behavior of the tablet. For example, the drug‐releasing curve of the shellac‐based tablet containing 3 wt% HPMC and 10 wt% NaHCO3 presented a typical linear model, which was an ideal linear drug‐releasing system, and could float in 3 min and last for 16 h. Therefore, we successfully employed a facile strategy to fabricate a biobased IFRRDS with controlled drug‐release and tunable intragastric floating‐retention properties, which has great potential for the advanced medical industry.

Development and Evaluation of Ranitidine Floating Tablet for Ulcer Healing and Soothing

In this current work floating tablets of ranitidine and aloe vera was prepared. The objective behind the work was to develop a formulation of H2 antagonist in collaboration with aloe vera to produce an ulcer soothing and ulcer protective effect. Ranitidine is a histamine H2-receptor antagonist. It is widely prescribed in active duodenal ulcers, gastric ulcers, Zollinger-Ellison syndrome, gastroesophageal reflux disease, and erosive esophagitis. The effective treatment of erosive esophagitis requires administration of 150 mg of Ranitidine, four times a day. A conventional dose of 150 mg can inhibit gastric acid whereas aloe vera will produce ulcer soothing affect and laxative effect too. In- vitro buoyancy studies were performed for all the ten formulations as per the method described by Rosa et al. The randomly selected tablets from each formulation were kept in a 100ml beaker containing simulated gastric fluid, pH 1.2 as per USP. The time taken for the tablet to rise to the surface and float was taken as floating lag time (FLT).

Formulation and Evaluation of Azithromycin Dihydrate Based In situ Gel as Floating Drug Delivery System

Floating Drug Delivery Systems have been used to overcome some of the problems like low oral absorption of drugs with narrow absorption window as it has an advantage of sustained release of drugs over a prolonged period of time. In-situ gels are the novel approach in the context of floating drug delivery systems. The aim of this present study was to develop an oral stomach specific floating in-situ gel of Azithromycin dihydrate. In-situ gelling system was prepared by dissolving different concentrations of polymers like sodium alginate, xanthan gum in the de-ionized water already prepared with sodium citrate at 60°C to 90°C. After the heating with continuous stirring the formulation was cooled below the temperature of 40°C with the addition of certain amount of drug and calcium carbonate which acts as gas generating agent. All the formulations showed pH in the range of 6.1 to 6.7, drug content was found to be in the range of 97.29% to 99.27%. Floating lag time was less than 1 minute for all the formulations and the duration of floatation was more than 24 hours for the combination of polymers. Appearance and measurement of water uptake by the gel was also good. Stability studies were also done and was found to be at normal phase at different temperatures and at interval of times. Although, F9 showed the maximum properties of an in-situ gel with increased gastric retention time with low slowly release of the drug. Drug release was found to be decreasing as the concentration of polymer increases. However, it was concluded that the in-situ gelling system of Azithromycin dihydrate could be prepared in various concentrations of different polymers and the combination of polymers to increase the patient compliance and reduction in the frequency of dosing of the drug with the increased gastric residence time for the drug in the stomach.

Formulation and Evaluation of Nifedipine Bilayer Floating Tablets

In the present investigation concern, the formulation and evaluation of bilayer floating tablet of Nifedipine which after an oral administration increase gastric residence time, to increase the bioavailability. Nifedipine is the Calcium channel blocker of the dihydropyridine type which used in angina pectoris and hypertension. It has a half-life of 2-4hours and bioavailability of 45-56%. It is advantageous to formulate bilayer floating tablet of Nifedipine helps to increase bioavailability, reduce dosing frequency, and reach maximum plasma concentration rapidly. Bilayer floating tablets comprised of two layers, immediate and sustain release layers. The immediate release layer is comprised of super disintegrating agent Karaya gum, and sustain release layer comprised of low density release retardant polymers like HPMC K4M and Guar gum; and sodium bicarbonate and citric acid gas generating agents. The prepared powder mixtures were subjected to FT-IR for all interaction. The tablets were prepared by direct compression. First, the powder blends of sustained release layer was pre-compressed and then powder blends of immediate release layer was added. Hardness, friability, drug content, floating lag time, total floating time, swelling index and in-vitro drug release were evaluated. In the present study, it was found that formulation F4 containing HPMC K4M and Guar gum in the ratio of 2:1 showed maximum drug release. The release data were adjusted to various mathematical models such as Higuchi, 1st order and zero order to evaluate the kinetics and mechanisms of the drug release and it was best suited for the Higuchi model. There were no notable changes in stability studies.

EFFECT OF VARIOUS SUSTAINED RELEASE POLYMERS ON FLOATING TABLETS OF CARVEDILOL PHOSPHATE-A COMPARATIVE STUDY

Objective: This study aimed to develop floating tablets of Carvedilol phosphate containing various excipients such as HPMC K100M, Carbopol, Polyox WSR, HPMC K4M, and sodium bicarbonate to generate gas. Additionally, the impact of DCP, spray dried lactose, and HPβCD on drug release was investigated. Methods: A total of eighteen formulations were prepared using the direct compression method and evaluated for hardness, drug content, friability, floating lag time, floatation time and drug release properties. Results: FTIR analysis confirmed that there were no chemical interactions between Carvedilol phosphate and the excipients used in the formulation of the floating tablets. Most of the Carvedilol phosphate floating tablets, except for F9 and F10, did not disintegrate in water, alkaline fluids (pH 7.4), or acidic aqueous solutions (pH 1.2). These tablets exhibited satisfactory quality attributes in terms of hardness, drug content, and friability, making them suitable for sustained release. The floating lag time of the tablets ranged from 25 seconds to 34 min, while the floating duration varied from 2 to 24 h. The drug release from the tablets was gradual and sustained over 12 h, depending on the composition of the tablets. Polyox WSR (F9 and F10) resulted in a rapid drug release, whereas an increase in the polymer concentration led to a decrease in the rate of drug release across all formulations. Conclusion: The study reveals that the use of hydrophilic polymers enhanced the drug release, whereas hydrophobic polymers decreased the drug release. As such, formulations, F11, F15, and F16, which gave 100% drug release within 12 h are finalized as the optimized formulations of Carvedilol phosphate floating tablet.

Development and assessment of gastro retentive floating tablets of celiprolol using natural polymers

Gastro retentive floating tablets are a promising drug delivery system for improving the bioavailability and therapeutic efficacy of orally administered drugs, particularly those with a narrow absorption window in the gastrointestinal tract. In this study, we aimed to develop and evaluate gastro retentive floating tablets of Celiprolol using natural polymers. The tablets were formulated by incorporating a combination of natural polymers, including hydroxypropyl methylcellulose (HPMC) and sodium alginate, to achieve buoyancy and sustained drug release. Various formulation parameters, such as polymer concentration, drug-to-polymer ratio, and effervescent agents, were optimized to attain desired tablet characteristics. The prepared tablets were evaluated for their physical characteristics, floating behavior, drug release profile, and drug stability. The optimized formulation demonstrated excellent floating properties, with a floating lag time of less than 60 seconds and a floating duration of more than 12 hours. In vitro drug release studies revealed sustained release of Celiprolol from the tablets over a period of 12 hours. The drug release kinetics followed the Higuchi model, suggesting diffusion as the predominant mechanism. Stability studies indicated that the floating tablets maintained their physical and drug release characteristics over a period of six months under accelerated storage conditions. Overall, the developed gastro retentive floating tablets of Celiprolol using natural polymers showed promising characteristics in terms of floating behavior, sustained drug release, and stability. This formulation has the potential to improve the therapeutic outcomes of Celiprolol by enhancing its bioavailability and ensuring prolonged drug exposure in the gastrointestinal tract. Further in vivo studies are warranted to validate the efficacy and pharmacokinetic profile of these tablets for potential clinical applications in the treatment of hypertension and other cardiovascular condition.

Preparation and In Vitro Evaluation of Levofloxacin-Loaded Floating Tables Using Various Rate-Controlling Agents.

Floating tablets are a new approach to extending the time a drug is in the stomach to improve therapy outcomes. Floating tablets were formulated with the drug, the polymers hydroxypropyl methylcellulose (HPMC), carboxymethyl cellulose (CMC), and starch, fillers, and lubricants. The tablets were prepared using the direction compression method. The tablets' physical quality control tests were found to be within acceptable limits. The tablets extended drug release up to 12 h and were uniform in their drug contents. The swelling index of the tablets ranged from 60 ± 0.11 to 66 ± 0.14%, and the tablets were less dense than water. The floating lag time (10 ± 0.23 to 16 ± 0.09 s) and total floating time (>12 h) showed good floating behaviors. The kinetic modeling showed that the drug was released from the tablets by pseudo-diffusion, swelling, erosion, or anomalous non-Fickian diffusion. F6 (starch and CMC) showed higher n values (0.994 ± 0.04), exhibiting pseudo-zero-order drug release kinetics compared to those of other tablets. The dissolution data of the test and reference tables were not similar (P > 0.05). In terms of antimicrobial activity, the zones of inhibition of the test F6 tablet powders (5.3 ± 0.08 mm) and the reference tablet powders (5.9 ± 0.13 mm) were found to be significantly similar (P > 0.05). The study concluded that these floating tablets can improve the gastric residence time and therapeutic outcomes.

Formulation and Evaluation of Gastroretentive In Situ Gelling System of Ketoprofen

Abstract A revolutionary concept for achieving long-term medication release is the gastroretentive in situ gelling system. The goal of this research was to formulate and test a gastroretentive in situ gel for ketoprofen delivery to targeted site to increase the residence and delivery time. Ketoprofen gastroretentive in situ gels were synthesized using a cation-driven gelation approach using various combinations and concentrations of polymers such as gellan gum, sodium alginate, and hydroxypropyl methylcellulose (HPMC) K100M. Visual appearance, pH, viscosity, in vitro gelation, in vitro buoyancy, drug content, density measurement, gel strength measurement, water uptake, and in vitro drug release were all evaluated. The total floating time was more than 12 h, with a floating lag time of less than 2 min. The formulations showed pH ranging from 6.89 to 7.61 and drug content ranging from 82.01% to 95.53%. For 11 h, the percent cumulative drug release of formulations F5 and F14, which contained a greater concentration of polymer sodium alginate (1.5%) and a combination of gellan gum and HPMC K100M (0.175% and 0.2%), was 84.10% and 85.49%, respectively. In vitro dissolution experiments and stability investigations both revealed no significant changes in drug content. The findings revealed that the formulated in situ gels aided in extending gastric residence duration, allowing the drug to be released in the stomach.

In situ gastric floating gel of atazanavir sulphate for sustained release: formulation, optimization and evaluation.

Aim: Atazanavir sulphate belongs to BCS class II drug, its oral bioavailability is limited due to its rapid first-pass metabolism and P-gp efflux. Materials & methods: The insitu floating gel using the complexed drug was prepared by ion gelation method and optimized the formulation as per 32 full factorial design. Results: Floating lag time of optimized formulation was found to be 18sand percentage drug release of 94.18±0.18 % at the end of 16h. The concentration of gelling polymer affects drug release and a floating lag time and vice versa. Conclusion: Insitu floating gel of atazanavir sulphate was found promising to sustain drug release due to an increased gastric residence time, which leads to enhanced potential therapy.

Formulation and In-Vitro Evaluation of Amlodipine Besylate Floating Tablets Using Different Polymers

Gastric-retentive amlodipine besylate effervescent tablets have been developed using a variety of hydrophilic polymers. Formulations were developed using different grades of different concentrations of polymer. H. HPMC K4M, HPMC K15M, HPMC K100 and xanthan gum were used as polymeric substances. The formulated mixtures have been subjected to various pre-formulation studies and flow properties, and all formulations show that the powder mixtures have good flow properties. Among all formulations, drug release was delayed for the desired period, H. 12 hours, for the HPMC K100 formulation as a polymer. The dissolution data showed that formulations made with HPMC K100M and xanthan gum as the polymer sustained drug release for the desired period. H. 12 hours at a concentration of 150 mg. On the other hand, in formulations containing HPMC K4M, HPMC K15M as polymer failed to produce the desired drug release. Therefore, the floating drug delivery system of amlodipine using the appropriate amount of appropriate polymer can increase the activity of the drug by prolonging the gastric residence time or decreasing the floating lag time. Keywords: Gastric-retentive, amlodipine besylate, effervescent tablets, HPMC K4M

DEVELOPMENT AND EVALUATION OF GASTRIC FLOATING TABLETS OF RIBOFLAVIN USING BOX-BEHNKEN DESIGN

Objective: To develop and evaluate gastric floating tablets of riboflavin that was thermally fused using an experimental design method. Methods: Gastric floating tablets were developed using the Box-Behnken design. The effect of sintering on various tablet properties is assessed. The prepared floating tablets were tested for characteristics like usual tablet quality control tests with special emphasis on buoyancy studies and in vitro drug release studies. Results: The drug-excipient incompatibility studies indicated no interactions between riboflavin and carnauba wax. Sintering the powder at 1200, °C partially decreased its crystallinity and improved drug release for up to 16 h. The tablets demonstrated good flow properties, acceptable hardness, low friability, and uniformity in thickness and diameter. Statistical models successfully optimized the formulation to achieve desired characteristics and practical compressibility. The optimal amounts of the variables, according to Design Expert® 12 software, were 59.19 mg of carnauba wax, 14.63% w/w of sodium bicarbonate, a sintering temperature of 74.68 °C, and a sintering exposure time of 1.99 h. Conclusion: In vitro dissolution studies were conducted on the optimized formulation to verify the model's predictions. The experimental results closely matched the predictions. The optimized formulations showed a floating lag time of 104 seconds and a floating duration of 12.3 h. The obtained T90 was found to be 11.3 h which followed zero order kinetics with a non-Fickian diffusion mechanism.

EVALUASI SIFAT FISIK TABLET FLOATING FUROSEMIDE DENGAN MATRIKS CARBOPOL

Furosemide is a sulfonamide-derived diuretic drug which is an alternative treatment for heart failure. Furosemide was made into slow-release tablets to improve the criteria for poor furosemide and maximize its absorption in the stomach. The purpose of this study was to determine whether floating furosemide tablets with a concentration of 23% carbopol matrix could meet the requirements for evaluating the physical properties of tablets compared theoretically with the literatur. The research design used was pre-experimental. In this study, the results of the weight uniformity test showed that there were no deviations from column A and column B, tablet hardness test with an average of 5.4 kg, tablet friability test with a % friability value of 0.08%, floating lag time test with an average time of 184 seconds, and the floating duration time test is with an average time of 8 hours. From the research data, it can be concluded that the floating furosemide tablet with a carbopol matrix concentration of 23% fulfills all evaluations of the physical properties of the tablet

Controlled release of MT-1207 using a novel gastroretentive bilayer system comprised of hydrophilic and hydrophobic polymers

In the present study, novel gastroretentive bilayer tablets were developed that are promising for the once-a-day oral delivery of the drug candidate MT-1207. The gastroretentive layer consisted of a combination of hydrophilic and hydrophobic polymers, namely polyethylene oxide and Kollidon® SR. A factorial experiment was conducted, and the results revealed a non-effervescent gastroretentive layer that, unlike most gastroretentive layers reported in the literature, was easy to prepare, and provided immediate tablet buoyancy (mean floating lag time of 1.5 s) that lasted over 24 h in fasted state simulated gastric fluid (FaSSGF) pH 1.6, irrespective of the drug layer, thereby allowing a 24-hour sustained release of MT-1207 from the drug layer of the tablets. Furthermore, during in vitro buoyancy testing of the optimised bilayer tablets in media of different pH values (1.0, 3.0, 6.0), the significant difference (one-way ANOVA, p < 0.001) between the respective total floating times indicated that stomach pH effects on tablet buoyancy are important to be considered during the development of non-effervescent gastroretentive formulations and the choice of dosing regimen. To the best of our knowledge, this has not been reported before, and it should probably be factored in when designing dosing regimens. Finally, a pharmacokinetic study in Beagle dogs indicated a successful in vivo 24-hour sustained release of MT-1207 from the optimised gastroretentive bilayer tablet formulations with the drug plasma concentration remaining above the estimated minimum effective concentration of 1 ng/mL at the 24-hour timepoint and also demonstrated the gastroretentive capabilities of the hydrophilic and hydrophobic polymer combination. The optimised formulations will be forwarded to clinical development.

Effect of modification of formulation variables on physical characterization of superporouse hydrogel

Superporouse hydrogel (SPH) is widely used and investigated as a gastro retentive drug delivery system to extend drug residence time in the stomach&#x0D; &#x0D; However, their mechanical strength represents a problem because they need to withstand the peristaltic movement of the stomach. Properties of SPH are widely affected by the materials used for their synthesis. The aim of the research is to study the effect of changing the foaming agent and foam stabilizer amount on physical properties, in particular mechanical strength, and drug release from SPH. Trifluoperazine HCl will be used as model drug in the study.&#x0D; SPH formulations was prepared using fixed amount of acrylamide (AM) and polyvinyl alcohol (PVA) as monomers, polyethylene glycol diacrylate (PEGDA) as cross-linker, TRFP as model drug and variable amount of sodium bicarbonate (NaHCO3) as foaming agent, and tween 20 as foam stabilizer. Ammonium persulphate (APS) / tetramethyl ethylenediamine (TEMED) system was used as polymerization initiator. The effect of changing foaming agent and foam stabilizer on mechanical strength, buoyancy, porosity, density, drug release, drug content, swelling ratio, and swelling time was investigated.&#x0D; Modifying both factors affected all the physical properties and drug release profile. When tween 20 was increased the mechanical strength, density and floating lag time was increased with a reduction in porosity and drug release. While increasing NaHCO3 reduced mechanical strength, density and floating lag time with increased porosity and faster drug release was observed. Optimum physical properties were observed in formula 2 which had 230 µl of Tween 20 (v/v) and 50 mg of NaHCO3 in which the mechanical strength was 579±0.4, floating lag time 14 min and 80% of the drug was released within 12 hr.&#x0D; As a conclusion SPH with improved mechanical strength, physical properties and drug release pattern can be achieved by changing foam stabilizer and foaming agent amount in the formulations.

Formulation and Characterization of a New Gastrointestinal Drug Delivery System of Cinnarizine Hydrochloride

The goal of this study was to create and test an in vitro floating drug delivery system employing polymers such as sodium carboxymethyl cellulose (CMC Sodium), Xanthan gum (XG), and sodium alginate (SA), using cinnarizine hydrochloride (CNZ) as the model drug. The efficacy of the model drug was proven during the pre-formulation research. 18 distinct formulations were developed using a direct compression (effervescent) technique (F1-F18). As a gas generator, sodium bicarbonate was employed. Physical properties such as weight variation, hardness, friability, floating lag time, and total floating duration were assessed in all of the formulations. Four mathematical models were used to predict the drug release Kinetics: zero order, first order, Higuchi, and Korsmeyer Peppas. F1, F2, F3, F6, and F7 were known to be the optimum formulations. They all include the same amount of sodium bicarbonate (40 mg) and ethyl cellulose (40 mg), but different quantities of CMC Sodium, XG, and SA (150mg, 120mg, 90mg, 150mg and 120mg of CMC Sodium:30mg, 60mg, 90mg, 0mg, 0mg of XA &amp; 0mg, 0mg, 0mg, 30mg and 60mg of SA respectively). In 0.1N HCl, all of the optimized batches had a release rate of 92 % to 99.8% in 12 hours and showed adequate swelling for up to 10 hours. Polymers such as CMC sodium, XG, and SA, in conjunction with sodium bicarbonate as a gas producing agent, may be employed to formulate sustained release floating tablets containing CNZ, according to the findings.

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

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