scholarly journals COMPARATIVE DISSOLUTION STUDIES OF WARFARIN SODIUM TABLETS: INFLUENCE OF AGITATION RATE, DISSOLUTION MEDIUM, AND USP APPARATUS

2021 ◽  
pp. 117-123
Author(s):  
JOSE RAUL MEDINA LOPEZ ◽  
LUIS DANIEL MAZON ROMAN ◽  
JUAN MANUEL CONTRERAS JIMENEZ ◽  
JUAN CARLOS RUIZ-SEGURA
Keyword(s):  
In Vitro Release ◽  
Agitation Rate ◽  
Dissolution Medium ◽  
Dissolution Studies ◽  
Warfarin Sodium ◽  
Flow Through ◽  
Vitro Release ◽  
Comparative Dissolution ◽  
Paddle Apparatus

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

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

2020 ◽  
Vol 579 ◽  
pp. 119130 ◽  
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

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

2017 ◽  
Vol 9 (4) ◽  
pp. 54 ◽  
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. 

An Investigation of the Release Properties of a Cationic Drug From a Hydrophobic Polyanhydride Matrix as a Function of Dissolution Medium

1998 ◽  
Vol 550 ◽  
Author(s):  
E. J. Ginsburg ◽  
T. D. Stultz ◽  
D. A. Stephens ◽  
D. Robinson ◽  
Y. Tian ◽  
...  
Keyword(s):  
Drug Delivery ◽  
Drug Delivery System ◽  
Anion Exchange ◽  
Polymer Chain ◽  
Delivery System ◽  
In Vitro Release ◽  
Dissolution Medium ◽  
Poorly Soluble ◽  
Vitro Release

AbstractThe dissolution of a drug delivery system consisting of gentamicin sulfate in a hydrophobic polyanhydride matrix has been examined. The in vitro release of gentamicin is a function of the composition of the dissolution medium, with slower release in pH 7.4 buffer than in unbuffered water. This is consistent with an anion exchange taking place under conditions in which carboxylate polymer chain-ends form a poorly soluble salt with gentamicin, and sulfate is released into solution. Results of additional experiments probing this model are digeussed.

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

2013 ◽  
Vol 20 (1) ◽  
pp. 27-34 ◽  
Author(s):  
Laila H. Emara ◽  
Aya R. Abdou ◽  
Ahmed A. El-Ashmawy ◽  
Rania M. Badr ◽  
Nesrin F. Taha ◽  
...  
Keyword(s):  
In Vitro Release ◽  
Specific Design ◽  
Floating Tablets ◽  
Flow Through ◽  
Vitro Release

Formulation and Evaluation of Oral Controlled Release Clarithromycin Matrix Tablets using Hydrophilic Polymer

2013 ◽  
Vol 6 (4) ◽  
pp. 2255-2259
Author(s):  
Suriyaprakash T N K ◽  
S. Lakshmana Prabu ◽  
Arumugarajan A ◽  
Sumathi A
Keyword(s):  
Phosphate Buffer ◽  
In Vitro Release ◽  
Release Profile ◽  
Matrix Tablets ◽  
Lauryl Sulfate ◽  
Dissolution Medium ◽  
Release Studies ◽  
The Matrix ◽  
Vitro Release

The objective of the present study was to develop clarithromycin tablets from polymeric hydrophilic matrices using methocel and characterization for its physic-chemical properties and in vitro release studies to optimize its release profile with the standard marketed product. Matrix tablets were prepared by wet granulation method using PVP and ethyl cellulose as binding agents. The matrix tablets were evaluated for its thickness, hardness, friability, weight variation, drug content and in vitro release studies. The drug delivery was analyzed using the paddle method in phosphate buffer pH 6.0 (dissolution medium I) and phosphate buffer pH 6.8 containing 0.5% sodium lauryl sulfate (dissolution medium II) and compared with USP dissolution limits. The dissolution release profile of formulation F9 was comparable with the market formulation and the difference factor and similarity factor f1 and f2 was found to be 2.44 and 83.18 in dissolution medium I; 1.44 and 89.71 in dissolution medium II. Stability studies were carried out as per ICH guidelines and tested for its physicochemical properties and in vitro studies. The study shows that the matrix method can be employed for preparing clarithromycin sustained release formulation using combination of hydrophilic polymers like Methocels and sodium carboxy methyl cellulose.

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

2017 ◽  
Vol 9 (4) ◽  
pp. 90 ◽  
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. 

scholarly journals In vitro release studies of furosemide reference tablets: influence of agitation rate, USP apparatus and dissolution media

ADMET & DMPK ◽  
2020 ◽  
Author(s):  
Raúl Medina-López ◽  
Sergio Guillén-Moedano ◽  
Marcela Hurtado
Keyword(s):  
Laminar Flow ◽  
Phosphate Buffer ◽  
In Vitro Release ◽  
Dosage Forms ◽  
Drug Dissolution ◽  
Agitation Rate ◽  
Usp Apparatus 4 ◽  
Usp Apparatus ◽  
Vitro Release

<p class="ADMETabstracttext">Furosemide is a diuretic drug widely used in chronic renal failure. The drug has low solubility and permeability, which cause clinical problems. Studying the in vitro release performance elucidates the rate and extent of drug dissolved from dosage forms under different conditions. Furosemide reference tablets were tested using USP Apparatuses 1 and 2 as well as the flow-through cell method (USP Apparatus 4), a dissolution apparatus that simulates the human gastrointestinal tract better than the other methods. Dissolution profiles were created with USP Apparatuses 1 and 2 at 25, 50, and 75 rpm and 900 mL of 0.1 M hydrochloric acid, acetate buffer (pH 4.5), and phosphate buffer (pH 6.8). USP Apparatus 4 with a laminar flow of 16 mL/min and 22.6 mm cells was used. Drug dissolution was quantified at 274 nm for 60 min. Mean dissolution time, dissolution efficiency, time to 50 % dissolution, and time to 80 % dissolution data were used to compare dissolution profiles. Additionally, zero-order, first-order, Higuchi, Hixson-Crowell, Makoid-Banakar, and Weibull models were used to adjust furosemide dissolution data. Between USP Apparatus 1 and 2, significant differences were observed in almost all parameters at 50 and 75 rpm (p &lt; 0.05). A similar dissolution profile (f<sub>2</sub> &gt; 50) with a pharmacopoeial dissolution method (USP Apparatus 2 at 50 rpm and 900 mL of phosphate buffer pH 5.8) and USP Apparatus 4 (laminar flow of 16 mL/min, 22.6 mm cells, and pH 6.8) was observed. The Weibull function was the best mathematical model to describe the in vitro release performance of furosemide in the three USP dissolution apparatuses. These results could be used to manufacture better furosemide dosage forms and decrease the negative clinical impact of current furosemide formulations.</p>

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

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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