In Vitro Release Evaluation of Gastroretentive Amoxicillin Floating Tablets Employing a Specific Design of the Flow-Through Cell

Objective: The aim of this study was to carry out comparative dissolution studies with warfarin sodium reference tablets under the hydrodynamic environments generated by the USP basket and paddle apparatus and flow-through cell using different agitation rates and dissolution media. Methods: Dissolution profiles were obtained with the USP basket and paddle apparatus at 50, 75, and 100 rpm and 900 ml of water as dissolution medium. After this, dissolution profiles of warfarin sodium were obtained with the USP paddle apparatus and flow-through cell method using 0.1 N hydrochloric acid, acetate buffer pH 4.5, phosphate buffer pH 6.8, and water. Spectrophotometric determination at 308 nm was carried out during 30 min. Dissolution profiles were compared with model-independent and model-dependent approaches. Results: Significant differences were found with mean dissolution time and dissolution efficiency at 50 and 75 rpm (*P<0.05). Makoid-Banakar was the best-fit model used to describe the in vitro release performance of warfarin sodium with 50-100 rpm and the USP basket and paddle apparatuses. Significant differences in all calculated parameters were found (*P<0.05) excepting percent dissolved at 30 min with 0.1 N hydrochloric acid and phosphate buffer pH 6.8. Conclusion: More research is necessary to identify the in vitro release performance of poorly soluble drugs under available USP apparatuses considering factors as agitation rate and kind of dissolution media. The knowledge of the in vitro release performance of reference drug products is important for the design of better generic formulations

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Flow-through cell-based in vitro release method for triamcinolone acetonide poly (lactic-co-glycolic) acid microspheres

International Journal of Pharmaceutics ◽

10.1016/j.ijpharm.2020.119130 ◽

2020 ◽

Vol 579 ◽

pp. 119130 ◽

Cited By ~ 3

Author(s):

Namita P. Tipnis ◽

Jie Shen ◽

Derek Jackson ◽

Daniel Leblanc ◽

Diane J. Burgess

Keyword(s):

Triamcinolone Acetonide ◽

Glycolic Acid ◽

In Vitro Release ◽

Flow Through ◽

Release Method ◽

Vitro Release

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IN VITRO RELEASE STUDIES OF CARBAMAZEPINE TABLETS AND BENZOYL METRONIDAZOLE SUSPENSIONS USING THE FLOW-THROUGH CELL APPARATUS AND SIMULATED GASTROINTESTINAL FLUIDS

International Journal of Applied Pharmaceutics ◽

10.22159/ijap.2017v9i4.18929 ◽

2017 ◽

Vol 9 (4) ◽

pp. 54 ◽

Cited By ~ 3

Author(s):

Jose Raul Medina ◽

Jonathan Hernandez ◽

Marcela Hurtado

Keyword(s):

In Vitro Release ◽

Gastric Fluid ◽

Simulated Gastric Fluid ◽

Dissolution Time ◽

Intestinal Fluid ◽

Simulated Intestinal Fluid ◽

Release Studies ◽

Flow Through ◽

Vitro Release

Objective: To characterize the in vitro release of carbamazepine tablets and benzoyl metronidazole suspensions using the flow-through cell apparatus and simulated gastrointestinal fluids.Methods: Tegretol® tablets, Flagyl® suspension, and generic formulations of each were tested. Release studies were performed using an automated flow-through cell apparatus. Simulated gastric fluid (with and without pepsin) and simulated intestinal fluid (without pancreatin) at 16 ml/min and fasted state simulated intestinal fluid at 8 ml/min, all at 37.0±0.5 °C, were used as dissolution media. The quantity of dissolved carbamazepine and benzoyl metronidazole was determined at 5-min intervals until 60 min at 285 and 278 nm, respectively. Percentage dissolved at 60 min, mean dissolution time, dissolution efficiency values, and t10%, t25%, t50% and t63.2% were calculated. Mean values for all parameters were compared between the reference and generic formulations using Studentʼs t-test. Dissolution data were fitted to different kinetic models.Results: Simulated gastric fluid without pepsin showed no discriminative capability for carbamazepine tablets. Significant differences were observed between the reference and generic formulations for almost all parameters (*P<0.05). In some cases, the logistic model best described the in vitro release of both drugs.Conclusion: Using an apparatus and media that best simulates the gastrointestinal environment, we identified differences in the rate and extent of dissolution of both drugs that could help to optimise the design of interchangeable formulations. Based on the physicochemical characteristics of carbamazepine and benzoyl metronidazole and the conditions in which the formulations were tested, these differences could be of clinical relevance.

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IN VITRO RELEASE MODELING OF ASPIRIN FLOATING TABLETS USING DDSOLVER

INDONESIAN JOURNAL OF PHARMACY ◽

10.14499/indonesianjpharm26iss2pp94 ◽

2015 ◽

Vol 26 (2) ◽

pp. 94 ◽

Cited By ~ 2

Author(s):

Agus Siswanto ◽

Achmad Fudholi ◽

Akhmad Kharis Nugroho ◽

Sudibyo Martono

Keyword(s):

In Vitro Release ◽

Floating Tablets ◽

Vitro Release

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Development and Evaluation of Floating Tablets of Lamivudine

Research Journal of Pharmacy and Technology ◽

10.52711/0974-360x.2021.00456 ◽

2021 ◽

pp. 2593-2597

Author(s):

Chinmaya Keshari Sahoo ◽

Amiyakanta Mishra ◽

Amaresh Prusty ◽

S. Ram Mohan Rao ◽

Jimidi Bhaskar

Keyword(s):

Drug Release ◽

Release Kinetics ◽

In Vitro Release ◽

Stability Study ◽

Compression Method ◽

Short Term ◽

In Vitro Drug Release ◽

Floating Tablets ◽

Vitro Release

The present study was undertaken to develop floating tablets of lamivudine. The tablets were prepared by direct compression method. The prepared tablets were evaluated for pre compression parameters, post compression parameters, in vitro drug release study and in vitro buoyancy study. Among the prepared formulations F4 batch show 90.98% drug release in 12 h. The in vitro release kinetics were analyzed for different batches by different pharmacokinetic models such as zero order, first order, Higuchi, and Korsmeyer Peppas. The result of optimized formulation releases drug up to 12 h in a controlled manner and follows Higuchi kinetics. Short term stability study at 40±2ºC/75±5% RH for three months on the best formulation was performed showing no significant changes in thickness, hardness, friability, drug content and in vitro drug release.

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Formulation and Evaluation of Gastroretentive Floating Tablets of Quetiapine Fumarate

Journal of Drug Delivery and Therapeutics ◽

10.22270/jddt.v11i3-s.4833 ◽

2021 ◽

Vol 11 (3-S) ◽

pp. 65-73

Author(s):

Keyur S. Patel ◽

Akshar N. Rao ◽

Deepa R. Patel ◽

Dhaval M. Patel ◽

Advaita B. Patel

Keyword(s):

Drug Release ◽

Sodium Bicarbonate ◽

Factorial Design ◽

Release Kinetics ◽

In Vitro Release ◽

Lag Time ◽

Quetiapine Fumarate ◽

Floating Tablets ◽

Vitro Release

The objective of the present study was to develop gastroretentive floating tablets of quetiapine fumarate. The gastroretentive floating tablets of quetiapine fumarate were formulated using natrosol 250 HHX as a sustained release polymer and sodium bicarbonate as a gas forming agents. A 32 factorial design was employed to study the influence of concentration of natrosol HHX 250 (X1) and concentration of sodium bicarbonate (X2) on the dependent variables % drug release at 1h (Y1), % drug release at 8 h (Y2) and floating lag time (Y3). The optimized formulation (O1) showed floating lag time 49 ± 3 sec and % drug release 99.54± 0.81 at 12 h. The in vitro release of F1-F9 batches were found in between 99.95 ± 1.18 % to 86.32 ±1.71 % at 12 h. Floating lag time of F1-F9 batches were found to be 25± 2 sec to 178 ± 3 sec. FTIR studies shown that there was no interaction between quetiapine fumarate and excipients. From the factorial design batches it was found that floating lag time was decreased with increasing the amount of sodium bicarbonate and decreasing the amount of natrosol 250 HHX. Here % release of drug was decreased with increase the extent of natrosol 250 HHX. The in-vitro release kinetics revealed Korsmeyer-Peppas model is followed and drug release is by anomalous diffusion. Keywords: Quetiapine fumarate, Natrosol 250 HHX, Sodium bicarbonate, Gastroretentive floating tablets

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Gastro retentive Drug Delivery of Cyclobenzaprine Hydrochloride

Gastroenterology Pancreatology and Hepatobilary Disorders ◽

10.31579/2641-5194/006 ◽

2018 ◽

Vol 2 (1) ◽

pp. 01-03

Author(s):

Swathi chilukala

Keyword(s):

Drug Delivery ◽

Controlled Release ◽

In Vitro Release ◽

Wet Granulation ◽

Floating Tablets ◽

Compression Properties ◽

Weight Variation ◽

Vitro Release ◽

Gastro Retentive

Drugs that are easily absorbed from the GI tract and have a short half-life are eliminated quickly from the blood circulation, require frequent dosing. To avoid this problem, the oral controlled release formulations are being developed. Gastro-retentive dosage forms have the potential from use as controlled release systems. The purpose of this research is to develop the gastro retentive drug delivery system of centrally acting alpha adrenergic agonist cyclobenzaprine Hydrochloride (cyclobenzaprine HCl). It is well absorbed from the upper part of the GIT, due to short gastric residence time the bioavailability is low and hence it is need to develop a dosage form that releases the drug in stomach using gastro retentive system. Different formulations of cyclobenzaprine HCl gastro-retentive floating tablets were prepared by wet granulation method using various concentrations of HPMC K4M / HPMC K100M and combination of Psyllium husk and HPMC K100M as matrix forming agent. Sodium bicarbonate and citric acid were used as a gas generating agent that helps in maintaining the buoyancy. The prepared cyclobenzaprine HCl gastro-retentive floating granules were subjected to pre-compression properties to comply with pharmacopoeial limits and the prepared gastro-retentive floating tablets were characterized for weight variation, hardness, thickness and friability drug content, swelling studies. The floating lag time of all formulation is good and the Total floating time of all the formulations was >12 hours. The tablets were evaluated for in vitro release characteristics for 12hrs in 0.1N HCl at 37 oC and from this in vitro release studies the formulations F-5, F-9 and F-15 exhibited good controlled release profile of about 96.0%, 94.5% and 95.0% when compared with other formulations while floating on the dissolution medium.

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COMPARISON OF THE USP APPARATUS 2 AND 4 FOR TESTING THE IN VITRO RELEASE PERFORMANCE OF IBUPROFEN GENERIC SUSPENSIONS

International Journal of Applied Pharmaceutics ◽

10.22159/ijap.2017v9i4.19926 ◽

2017 ◽

Vol 9 (4) ◽

pp. 90 ◽

Cited By ~ 1

Author(s):

Jose Raul Medina ◽

Mariel Cortes ◽

Erik Romo

Keyword(s):

In Vitro Release ◽

Generic Product ◽

Dissolution Profile ◽

Drug Products ◽

Flow Through ◽

Usp Apparatus 4 ◽

Usp Apparatus ◽

Usp Apparatus 2 ◽

Vitro Release

Objective: The aim of this study was the comparison of the in vitro release performance of ibuprofen generic suspensions and reference, based on the hydrodynamic environment generated by the flow-through cell method (USP Apparatus 4). Results were compared with those obtained by the use of the USP Apparatus 2.Methods: The Advil® suspension (2 g/100 ml) and two generic formulations with the same dose were tested. Dissolution studies were carried out using a USP Apparatus 4 Sotax CE6 with 22.6 mm cells, laminar flow at 16 ml/min, and pH 7.2 phosphate buffer at 37.0±0.5 °C as dissolution medium. Ibuprofen was quantified spectrophotometrically at 222 nm. The in vitro release of the three drug products were studied using the USP Apparatus 2. The dissolution profiles of generic products were compared with the reference by model-independent, model-dependent, and analysis of variance (ANOVA)-based comparisons.Results: The dissolution profile of the generic product A was similar to the dissolution profile of reference, only with the use of the USP Apparatus 4. The f2 similarity factor was>50 and no significant differences were found with dissolution efficiency data (*P>0.05). Similar results were found with the comparison of t50% and t63.2% values. Similar dissolution profiles between generic product A and reference were also found with ANOVA-based comparisons.Conclusion: The flow-through cell method was adequate for study the in vitro release of ibuprofen suspensions. It is necessary to evaluate the in vivoperformance of the drug products used in order to estimate the predictability of the proposed methodology.

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IN VITRO RELEASE PERFORMANCE OF METFORMIN HYDROCHLORIDE FORMULATIONS USING THE FLOW-THROUGH CELL METHOD

International Journal of Applied Pharmaceutics ◽

10.22159/ijap.2020v12i6.39230 ◽

2020 ◽

pp. 76-82

Author(s):

JOSE RAUL MEDINA-LÓPEZ ◽

FRIDA IRIANA MEDINA-MORALES ◽

RAFAEL ALONSO GALVEZ LOMELIN ◽

JUAN CARLOS RUIZ SEGURA ◽

MARCELA HURTADO

Keyword(s):

Drug Product ◽

In Vitro Release ◽

Dissolution Time ◽

Metformin Hydrochloride ◽

Reference Drug ◽

Cell Method ◽

Post Marketing ◽

Flow Through ◽

Vitro Release

Objective: The objective of this work was to evaluate the in vitro release performance of metformin hydrochloride formulations (500-mg tablets) using the hydrodynamic environment of the flow-through cell method. Results were compared with those generated by the official dissolution test (USP basket apparatus). Methods: The reference drug product and three generic formulations were tested with phosphate buffer pH 6.8 as dissolution medium. Dissolution profiles were carried out with an automated flow-through cell apparatus using laminar flow at 16 ml/min. Drug was quantified at 233 nm during 45 min. Dissolution profiles were compared with the calculation of f2 similarity factor, mean dissolution time, dissolution efficiency, t50% and t63.2%. Dissolution data were adjusted to several mathematical models such as Makoid-Banakar, Peppas-Sahlin, Weibull and Logistic. Results: With the flow-through cell method and at 45 min less than 60% of metformin hydrochloride dissolved was found, while with the USP basket apparatus, less than 75% of the drug was found. Some generic formulations showed f2>50 with both USP apparatuses, but statistical comparisons of parameters indicated significant differences between their dissolution profiles and reference. Due to variability obtained no dissolution profiles were compared by model-dependent approach. Conclusion: To demonstrate safe interchangeability between metformin hydrochloride generic formulations and reference bioequivalence studies should be performed. It is important post-marketing monitoring of the commercial formulations because health regulatory agencies of each country must ensure drug products with quality, safety, and efficacy at the lowest possible cost.

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FORMULATION AND CHARACTERIZATION OF CLARITHROMYCIN FLOATING TABLETS BY USING VARIOUS POLYMERS

International Journal of Advanced Research ◽

10.21474/ijar01/13609 ◽

2021 ◽

Vol 9 (10) ◽

pp. 766-776

Author(s):

Nitija Prakash Kawade ◽

◽

Vaibhav V. Changediya ◽

Keyword(s):

Drug Release ◽

Ethyl Cellulose ◽

In Vitro Release ◽

Angle Of Repose ◽

Compression Technique ◽

Duration Of Action ◽

Floating Tablets ◽

Gastric Residence Time ◽

Vitro Release

The present study outlines a systematic approach for designing and development of Clarithromycin floating tablets to enhance the bioavailability and therapeutic efficacy of the drug. Floating tablets of Clarithromycin have shown sustained release there by proper duration of action at a particular site and are designed to prolong the gastric residence time after oral administration. Different formulations were formulated by using direct compression technique. A floating drug delivery system (FDDS) was developed by using sodium bicarbonate as gas-forming agent and Chitosan, HPMC K4M and Ethyl cellulose as polymers. The preformulation parameters like Organoleptic properties, angle of repose, bulk density, tapped density, Hausners ratio, carrs index and compressibility index of pure drug was evaluated and complied with the pharmacopoeial specifications. FTIR studies showed there was no interaction between drug and polymer. The prepared tablets were evaluated in terms of their physical characteristics, post compression parameters in vitro release and buoyancy lag time the results of the in vitro release studies showed that the optimized formulation (C7) could sustain drug release for 12 hrs by using Ethyl cellulose in the concentration of 50 mg. The in vitro drug release followed Kors Mayer peppas release. Results revealed that the floating formulation of the Clarithromycin is the best formulation to obtain better therapeutic effect and Ethyl cellulose at a concentration of 50mg up to some extent it increases the Bioavailability of the drug to retain the dosage form on the desired site for effective period of the time.

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