scholarly journals INFLUENCE OF DOSE AND USP DISSOLUTION APPARATUS IN THE RELEASE PERFORMANCE OF REFERENCE TABLETS: PROPRANOLOL-HCl AND RANITIDINE-HCl CASES

2019 ◽  
pp. 164-170
Author(s):  
JOSE RAUL MEDINA-LOPEZ ◽  
LUIS ANTONIO CEDILLO-DIAZ ◽  
MARCELA HURTADO
Keyword(s):  
In Vitro Dissolution ◽  
Dissolution Time ◽  
Reference Drug ◽  
Cell Method ◽  
Drug Products ◽  
Propranolol Hcl ◽  
Flow Through ◽  
Dissolution Apparatus ◽  
Paddle Apparatus

Objective: Due to quality of generic formulations depends on available information of reference drug products the aim of this work was to perform an in vitro dissolution study of two doses of propranolol-HCl and ranitidine-HCl reference tablets using USP basket or paddle apparatus and flow-through cell method. Methods: Two doses of propranolol-HCl (10-mg and 80-mg) and ranitidine-HCl (150-mg and 300-mg) of Mexican reference products were used. Dissolution profiles of propranolol-HCl were obtained with USP basket apparatus at 100 rpm and 1000 ml of 1% hydrochloric acid. Profiles of ranitidine-HCl were determined with USP paddle apparatus at 50 rpm and 900 ml of distilled water. All formulations were also studied with the flow-through cell method using laminar flow at 16 ml/min. Dissolution profiles were compared by model-independent (f2 similarity factor, mean dissolution time and dissolution efficiency) and model-dependent methods (dissolution data adjusted to some mathematical equations). Time data, derived from these adjustments, as t50%, t63.25%, and t85% were used to compare dissolution profiles. Results: With all approaches used and being high solubility drugs significant differences were found between low and high doses and between USP dissolution apparatuses (*P<0.05). Conclusion: In vitro dissolution performance of two doses of propranolol-HCl and ranitidine-HCl was not expected. Considering the same USP dissolution apparatus, the reference tablets did not allow the simultaneous release of the used doses. The results could be of interest for pharmaceutical laboratories or health authorities that classify some drug products as a reference to be used in dissolution and bioequivalence studies.

scholarly journals DISSOLUTION PERFORMANCE OF MELOXICAM FORMULATIONS UNDER HYDRODYNAMICS OF USP PADDLE APPARATUS AND FLOW-THROUGH CELL METHOD

2019 ◽  
pp. 182-188
Author(s):  
OSE RAUL MEDINA-LOPEZ ◽  
JOSE ANGEL OROZCO-JUAREZ ◽  
MARCELA HURTADO
Keyword(s):  
In Vitro Dissolution ◽  
Dissolution Time ◽  
Weibull Function ◽  
Cell Method ◽  
Drug Products ◽  
Poorly Soluble ◽  
Flow Through ◽  
Dissolution Efficiency ◽  
Paddle Apparatus

Objective: To study the in vitro dissolution performance of four generic formulations of the poorly soluble drug meloxicam and the reference under hydrodynamic environments generated by flow-through cell method and USP paddle apparatus (pharmacopeial test). Methods: Dissolution method was validated according to ICH guidelines. Dissolution profiles were carried out with an automated flow-through cell apparatus (laminar flow at 16 ml/min with 22.6 mm cells) and USP paddle apparatus at 75 rpm. Phosphate buffer pH 7.5 at 37.0±0.5 °C was used as dissolution medium. Spectrophotometric determination of drug at 362 nm was carried out during 30 min. Dissolution profiles were compared with model-dependent and-independent methods. Results: Practically, all generic formulations showed significant differences with the percentage of drug dissolved at 30 min, mean dissolution time and dissolution efficiency, when USP paddle apparatus was used (*P<0.05), while only two generic formulations were different to reference using flow-through cell method. After adjustment to different mathematical equations, Weibull function was the best model to describe meloxicam dissolution performance and significant differences were found with all drug products when USP paddle apparatus was used, while only one formulation was different with flow-through cell method. Conclusion: The study reveals the need to look for better dissolution schemes for meloxicam tablets since USP paddle apparatus may not reflect properly the in vitro dissolution performance of meloxicam generic formulations and reference.

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.

A collaborative study of the in vitro dissolution of acetylsalicylic acid gastro-resistant capsules comparing the flow-through cell method with the USP paddle method

1997 ◽  
Vol 151 (1) ◽  
pp. 81-90 ◽  
Author(s):  
Kirsti Gjellan ◽  
Anna-Britta Magnusson ◽  
Rolf Ahlgren ◽  
Karin Callmer ◽  
Dorte Früs Christensen ◽  
...  
Keyword(s):  
Acetylsalicylic Acid ◽  
Collaborative Study ◽  
In Vitro Dissolution ◽  
Cell Method ◽  
Flow Through

scholarly journals DISSOLUTION BEHAVIOR OF CARBAMAZEPINE SUSPENSIONS USING THE USP DISSOLUTION APPARATUS 2 AND THE FLOW-THROUGH CELL METHOD WITH SIMULATED GI FLUIDS

2017 ◽  
Vol 9 (10) ◽  
pp. 111
Author(s):  
Jose Raul Medina ◽  
Erik Aguilar ◽  
Marcela Hurtado
Keyword(s):  
Laminar Flow ◽  
Simulated Gastric Fluid ◽  
Cell Method ◽  
Drug Products ◽  
Flow Through ◽  
Model Independent ◽  
Dissolution Apparatus ◽  
Usp Apparatus ◽  
Usp Apparatus 2 ◽  
Independent Parameters

Objective: To characterize the dissolution behaviour of carbamazepine generic suspensions using the USP Dissolution Apparatus 2 and the flow-through cell method with simulated gastrointestinal fluids as dissolution media.Methods: Tegretol® suspension and two generic formulations were tested. Dissolution studies were performed using the USP Apparatus 2 (75 rpm and 900 ml of dissolution medium) and the flow-through cell method (laminar flow at 16 ml/min). Simulated gastric fluid (SGF) (with and without pepsin) and simulated intestinal fluid (SIF) (without pancreatin) at 37.0±0.5 °C, was used as dissolution media. The quantity of dissolved carbamazepine was determined at 5 min intervals until reaching 60 min, at 285 nm. Percentage dissolved at 60 min, mean dissolution time, dissolution efficiency values (model-independent parameters), as well as t50% and t63.2% were calculated (model-dependent parameters). Values for all parameters were compared between the reference and generic formulations using one-way analysis of variance (ANOVA) following a Dunnett’s multiple comparison test. Dissolution data were also fitted to different fit models.Results: Since the first sampling time, the reference product had reached 100% of drug dissolved, which was determined using USP Apparatus 2. Nevertheless, significant differences in the three model-independent parameters of generic products were found (*P<0.05). Dissolution data obtained with the paddle apparatus were fitted to different kinetic equations; however, using the flow-through cell method and SIF without pancreatin, the three drug products were fitted to the same kinetic model (Gompertz). With ANOVA-based comparisons and the flow-through cell method, significant differences were found in dissolution data of generic product A versus reference at all sampling times (*P<0.05). The flow-through cell method and SGF with pepsin were the best options to discriminate among dissolution profiles.Conclusion: The flow-through cell method seems to be an adequate dissolution apparatus to characterize in vitrodissolution performance of Class II drugs manufactured as suspensions. For carbamazepine suspensions, SGF and laminar flow at 16 ml/min were the most appropriate conditions to discriminate among generic formulations. Given the physicochemical characteristics of carbamazepine and the environment in which the drug products were tested, these differences could be of clinical relevance. 

Formulation and Evaluation of Bilayer Sustained Release Tablets of Salbutamol and Theophylline

2009 ◽  
Vol 2 (3) ◽  
pp. 638-646
Author(s):  
R. Nagaraju ◽  
Rajesh Kaza
Keyword(s):  
Ethyl Cellulose ◽  
Xanthan Gum ◽  
Dosage Forms ◽  
In Vitro Dissolution ◽  
Dissolution Studies ◽  
Sustained Release Tablets ◽  
Dissolution Apparatus ◽  
Single Dosage

Salbutamol and theophylline are available in conventional dosage forms, administered four times a day, leading to saw tooth kinetics and resulting in ineffective therapy. The combination of these two drugs in a single dosage form will enhance the patient compliance and prolong bronchodilation. Various polymers, such as hydroxy propyl methylcellulose K4M (HPMC- K4M), hydroxy propyl methylcellulose K100M (HPMC- K100M), xanthan gum, ethyl cellulose and hydroxy propyl methylcellulose phthalate (HPMC-P) were studied. HPMC-P and HPMC- K4M were found to be best in controlling the release. In-vitro dissolution studies were carried out for all the bi-layered tablets developed using USP dissolution apparatus type 2 (paddle). It was found that the tablet FB15-FW3 showed 50% release of salbutamol in first hour and the remaining was released for eight hours. However, theophylline was found to be released as per the USP specifications. The IR spectrum was taken for FB15-FW3 formulation and it revealed that there is no disturbance in the principal peaks of pure drugs salbutamol and theophylline. This further confirms the integrity of pure drugs and no incompatibility of them with excipients. Also, formulation of FB15-FW3 has shown required release pattern and complies with all the evaluated parameters and comparable to the marketed formulation.

Formulation and Evaluation of Orodispersible Tablets Containing Taste Masked Mirabegron Resinate

2021 ◽  
pp. 4736-4742
Author(s):  
Sarika S. Malode ◽  
Milind P. Wagh
Keyword(s):  
Overactive Bladder ◽  
Bitter Taste ◽  
In Vitro Release ◽  
In Vitro Dissolution ◽  
Dissolution Time ◽  
Disintegration Time ◽  
Orodispersible Tablets ◽  
Weight Variation

The objective of present work was to develop taste masked orodispersible tablets of mirabegron. Mirabegron is beta 3 adrenoceptor agonist used to treat overactive bladder. Overactive bladder (OAB) is defined as a symptom syndrome showing feeling of urgency to urinate, typically accompanied by frequent daytime and nocturnal urination, in the absence of proven infection or other obvious pathology. Over active bladders are generally common in geriatrics. Moreover, this drug has a very strong bitter taste. Frequent dosing requires frequent water intake, which further aggregates the condition of over active bladder and bitter taste of drug affects patient compliance. Hence a need arises to mask the bitter taste for development of an ODT which does not require consuming water with every dosage. In this work, the bitter taste of mirabegron was masked by forming a complex with an ion exchange resin tulsion 344. The drug resin complexation process was optimized for resin activation, drug: resin ratio, soaking time and stirring time. In –vitro release studies revealed complete drug elution from the complex within 10 minutes in pH 1.2 buffer. The taste-masked complex was then formulated into palatable orodispersible tablets using a direct compression approach by use of superdisintegrants to achieve a rapid disintegration. The tablets were evaluated for weight variation, hardness, friability, drug content, wetting time, In- vivo disintegration time and in-vitro dissolution time.

scholarly journals Dry powder inhalers: An overview of the in vitro dissolution methodologies and their correlation with the biopharmaceutical aspects of the drug products

2018 ◽  
Vol 113 ◽  
pp. 18-28 ◽  
Author(s):  
Sitaram P. Velaga ◽  
Jelena Djuris ◽  
Sandra Cvijic ◽  
Stavroula Rozou ◽  
Paola Russo ◽  
...  
Keyword(s):  
In Vitro Dissolution ◽  
Dry Powder Inhalers ◽  
Dry Powder ◽  
Drug Products

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

TASTE MASKING OF OXYBUTYNIN CHLORIDE USING LIPID EXCIPIENTS AND FORMULATION AS ORODISPERSIBLE TABLETS FOR GERIATRIC POPULATION

INDIAN DRUGS ◽  
2013 ◽  
Vol 50 (10) ◽  
pp. 39-46
Author(s):  
V Prakash ◽  
◽  
L. Keshri ◽  
V. Sharma ◽  
K. Pathak
Keyword(s):  
In Vitro Release ◽  
In Vitro Dissolution ◽  
Taste Masking ◽  
Dissolution Time ◽  
Disintegration Time ◽  
Geriatric Population ◽  
Orodispersible Tablets ◽  
Lipid Excipients

The aim of the present study was to mask the bitter taste of oxybutynin chloride by lipid excipients and to develop its fast disintegrating tablet. For this purpose, a blend of two lipids, glyceryl behenate and glyceryl palmitostearate was utilized for taste masking by solvent evaporation method. The evaporation of solvent was accomplished by freeze drying and taste masked granules were characterized for their micromeritic and rheological properties. The state of dispersion was analyzed by SEM and DSC. Orodispersible tablets were then formulated (F1- F6) using Polyplasdone XL as extragranular superdisintegrant and evaluated for hardness, disintegration time, in vitro dissolution time and in vivo disintegration time. Results indicated that the formulation F6 exhibited minimum in vivo disintegration time of 8 sec with effective taste masking. In vitro release analysis indicated %DE10 and %DE25 of 51.48 and 76.53 respectively. Conclusively, taste masked orodispersible formulation of oxybutynin chloride was developed that could be beneficial for geriatric population.

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