scholarly journals Developing methods to compare tablet formulations of atorvastatin

2012 ◽  
Vol 48 (4) ◽  
pp. 801-810 ◽  
Author(s):  
Marcelo Antonio de Oliveira ◽  
Caroline Dutra Lacerda ◽  
André Fazôlo Bonella
Keyword(s):  
Rotation Speed ◽  
Pharmaceutical Formulations ◽  
Generic Product ◽  
Dissolution Test ◽  
Dissolution Medium ◽  
Differential Dissolution ◽  
Tablet Formulations ◽  
Biopharmaceutical Classification System ◽  
Paddle Apparatus ◽  
The Ideal

Atorvastatin (ATV) is an antilipemic drug of great interest to the pharmaceutical industry. ATV does not appear in the monographs of Brazilian pharmacopoeia, and analytical methodologies for its determination have been validated. The chromatographic conditions used included: RP-18 column-octadecylsilane (250 x 4.6 mm, 5 mm), detection at 238 nm, mobile phase containing 0.1% phosphoric acid and acetonitrile (35:65% v/v), flow at 1.5 mL min-1, oven temperature at 30ºC, and injection volume of 10 mL. ATV is classified as a class II product, according to the biopharmaceutical classification system. As such, a dissolution test was proposed to evaluate pharmaceutical formulations on the market today, under the following conditions: water as a dissolution medium, 1000 mL as a volume, paddle apparatus at a rotation speed of 50 rpm, 80% (Q) in 15 minutes with UV spectrophotometer readings at 238 nm. In the pattern condition proposed as the ideal dissolution test, which appropriately differentiates amongst formulations, the generic product was not considered pharmaceutically equivalent; however, in other less differential dissolution methods, which also fall within appropriate legal parameters, this product could come to be regarded as generic.

scholarly journals Design of Experiments for the Establishment of the Dissolution Test Conditions of Rupatadine Fumarate 10 mg tablets

2019 ◽  
Vol 9 (1-s) ◽  
pp. 331-336 ◽  
Author(s):  
Castillo Henríquez Luis ◽  
Madrigal Redondo German ◽  
Vargas Zúñiga Rolando ◽  
Carazo Berrocal Gustavo
Keyword(s):  
Design Of Experiments ◽  
Statistical Model ◽  
Rotation Speed ◽  
Dissolution Test ◽  
Dissolution Medium ◽  
Independent Variables ◽  
Test Conditions ◽  
Pharmaceutical Technology ◽  
Dependent Variables ◽  
Pharmaceutical Form

Design of Experiments (DoE) is a statistical model that aims to determine if the factors under study affect the response, and if so, it determines the conditions under which this variable of interest can be optimized. In terms of pharmaceutical technology, independent variables are usually factors of the formulation, while dependent variables are properties of the product or parameters that indicate the performance of the process. Precisely, the dissolution test is a tool of interest for the developers of medicines since it allows them to evaluate the performance of a formulation designed in a solid pharmaceutical form, such as tablets. The present investigation used the design of experiments to establish and optimize the conditions of the dissolution test of a 10 mg Rupatadine fumarate tablets formulation, resulting in the use of HCl 0,1 N (pH 1) dissolution medium and a rotation speed of 100 rpm for the apparatus II USP, which allow the analysis of the product in a reproducible and reliable way. Keywords: Analysis of variances, Design of experiments, Dissolution test, Factorial design, Rupatadine Fumarate, Tablets, Test conditions.

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

scholarly journals DEVELOPMENT OF ANALYTICAL METHOD AND ITS VALIDATION FOR SILDENAFIL CITRATE BY UV-SPECTROPHOTOMETRY

2020 ◽  
Vol 11 (12) ◽  
pp. 41-45
Author(s):  
Deepali Tomar ◽  
Peeyush Kaushik ◽  
Ashish S Mishra ◽  
Lalan Kumar Sah
Keyword(s):  
Analytical Method ◽  
Limit Of Detection ◽  
Pharmaceutical Formulations ◽  
Sildenafil Citrate ◽  
Uv Spectrophotometry ◽  
Calibration Curves ◽  
Coefficient Corrélation ◽  
The Stability ◽  
Versus Concentration ◽  
The Ideal

bulk drugs and the drug formulations and its validation. Method: The ideal conditions were established for the investigation or analysis of the drug. Results: The λmax of 293.2nmwas found for the Sildenafil citrate. Within, 8 to 60μg/ml concentration range the method complied with Beer's Law and show exceptional sensitivity with linearity. Moreover, 1.012 and 3.036 were observed limit of detection and quantification, respectively. When the absorbance versus concentration graph was plotted on the calibration curves a linear relationship was observed with the coefficient correlation of 0.99. The observed regression coefficient (Y) of the calibration curves was found to be 0.0131x- 0.0191. The method was precise and accurate with the experiential value of 2.0325± 0.044. The stability of the test solution was up to 48 hours. Conclusion: The proposed analytical method is simple, economical and experimentally less time-consuming. Therefore, it will be appropriate for Sildenafil citrate analysis of pharmaceutical formulations in bulk.

scholarly journals Stability-indicating HPLC-PDA assay for simultaneous determination of paracetamol, thiamine and pyridoxal phosphate in tablet formulations

2019 ◽  
Vol 69 (2) ◽  
pp. 249-259 ◽  
Author(s):  
Amir Ali ◽  
Muhammad Makshoof Athar ◽  
Mahmood Ahmed ◽  
Kashif Nadeem ◽  
Ghulam Murtaza ◽  
...  
Keyword(s):  
Simultaneous Determination ◽  
Pyridoxal Phosphate ◽  
Degradation Products ◽  
Ammonium Phosphate ◽  
Pharmaceutical Formulations ◽  
Hplc Method ◽  
Complete Separation ◽  
Coefficient Of Determination ◽  
Tablet Formulations

Abstract With the increased number of multi-drug formulations, there is a need to develop new methods for simultaneous determinations of drugs. A precise, accurate and reliable liquid chromatographic method was developed for simultaneous determination of paracetamol, thiamine, and pyridoxal phosphate in pharmaceutical formulations. Separation of analytes was carried out with an Agilent Poroshell C18 column. A mixture of ammonium phosphate buffer (pH = 3.0), acetonitrile and methanol in the ratio of 86:7:7 (V/V/V) was used as the mobile phase pumped at a flow rate of 1.8 mL min−1. Detection of all three components, impurities and degradation products was performed at the selected wavelength of 270 nm. The developed method was validated in terms of linearity, specificity, precision, accuracy, LOD and LOQ as per ICH guidelines. Linearity of the developed method was found in the range 17.5–30 µg mL−1 for thiamine, 35–60 µg mL−1 for pyridoxal phosphate and 87.5–150 µg mL−1 for paracetamol. The coefficient of determination was ≥ 0.9981 for all three analytes. The proposed HPLC method was found to be simple and reliable for the routine simultaneous analysis of paracetamol, thiamine and pyridoxal phosphate in tablet formulations. Complete separation of analytes in the presence of degradation products indicated selectivity of the method.

scholarly journals Solid Dispersion of Resveratrol Supported on Magnesium Dihydroxide (RESV@MDH) Microparticles  Improves Oral Bioavailability

2018 ◽  
Author(s):  
Roberto Spogli ◽  
Maria Bastianini ◽  
Francesco Ragonese ◽  
Rossana Giulietta Iannitti ◽  
Lorenzo Monarca ◽  
...  
Keyword(s):  
Solid Dispersion ◽  
Dissolution Test ◽  
Solubility In Water ◽  
Granulometric Analysis ◽  
Size Type ◽  
Type 3 ◽  
Low Solubility ◽  
Biopharmaceutical Classification System

Resveratrol, because of its low solubility in water and its high membrane permeability, is collocated in the second class of the biopharmaceutical classification system, with limited bioavailability due to its dissolution rate. Solid dispersion of resveratrol supported on magnesium dihydroxide (RESV@MDH) was evaluated to improve solubility and increase bioavailability of resveratrol. Fluorimetric microscopy and granulometric analysis display three types of microparticles with similar size: type 1 that emitted preferably fluorescence at 463 nm (&lambda;ecc 358 nm), type 2 that emitted preferably fluorescence at 605 nm (&lambda;ecc 550 nm) andtype 3 that are non-fluorescent. Micronized pure resveratrol display only microparticles type 1 whereas type 3 are associated to pure magnesium dihydroxide. Dissolution test in simulated gastric environment resveratrol derived from RESV@MDH in comparison to resveratrol alone displayed better solubility. According to the biopharmaceutical classification, an increase of 3 fold of resveratrol bioavailabilitywas observed after oral administration of 50 mg/Kg of resveratrol of RESV@MDH in rabbits. We hypothesize that type 2 microparticles represent magnesium dihydroxide microparticles with a resveratrol shell and that they are responsible for the improved resveratrol solubility and bioavailability of RESV@MDH.

scholarly journals The effect of dissolution medium, rotation speed and compaction pressure on the intrinsic dissolution rate of amlodipine besylate, using the rotating disk method

2014 ◽  
Vol 50 (3) ◽  
pp. 513-520 ◽  
Author(s):  
Leandro Giorgetti ◽  
Michele Georges Issa ◽  
Humberto Gomes Ferraz
Keyword(s):  
Dissolution Rate ◽  
Rotation Speed ◽  
Compaction Pressure ◽  
Rotating Disk ◽  
Fractional Factorial ◽  
Amlodipine Besylate ◽  
Dissolution Medium ◽  
Intrinsic Dissolution ◽  
Intrinsic Dissolution Rate ◽  
Disk Method

The aim of this study was to evaluate the effect of dissolution medium, rotation speed and compaction pressure on the intrinsic dissolution rate (IDR) of the antihypertensive drug amlodipine besylate, using the rotating disk method. Accordingly, a fractional factorial design (33-1) was used, employing dissolution media (water, phosphate buffer pH 6.8 and HCl 0.1 M), rotation speed (50, 75 and 100 rpm), and compaction pressure (1000, 1500 and 2000 psi) as independent variables. The assays were randomized and statistically compared using the Statistica(r) 11 software program. Significance testing (ANOVA) indicated that the dissolution medium had a considerable impact on the IDR of amlodipine besylate. Analysis of the linear and quadratic components of the variables led to the proposition of a mathematical model that describes the IDR as a function of the parameters studied. Conversely, the levels of compaction pressure and rotation speed employed during experimental planning were less relevant, especially when the assay was conducted in the HCl 0.1 M medium.

scholarly journals Method Development and Validation for Determination of Voglibose in Tablet Formulation Using LC-MS/MS

2011 ◽  
Vol 8 (4) ◽  
pp. 1770-1783
Author(s):  
Mithlesh Rajput ◽  
Meenakshi Dahiya ◽  
Premlata Kumari ◽  
Kamini Kalra ◽  
Manjeet Aggarwal ◽  
...  
Keyword(s):  
Method Development ◽  
Limit Of Detection ◽  
Pharmaceutical Formulations ◽  
Limit Of Quantitation ◽  
Positive Mode ◽  
Method Development And Validation ◽  
Treatment Of Diabetes ◽  
Tablet Formulations ◽  
Development And Validation

Voglibose is a potent α glucosidase inhibitor, used for the treatment of diabetes mellitus. For quantitative determination of voglibose in pharmaceutical formulations of low doses, simple, sensitive, accurate and precise LC-MS/MS method using electrospray ionization in positive mode was developed and validated. The method was found linear in the concentration range of 25.0-1200 ηg/mL with a correlation coefficient of 0.9998. The limit of detection (LOD) of the method was found to be 1.5 ηg/mL and limit of quantitation (LOQ) was achieved at 3.0 ηg/mL. The recoveries of voglibose from spiked samples at different concentration levels were found in the range of 98-102%. The proposed method was found suitable for quantitation of voglibose and for the determination of uniformity of content of the dosage units of the tablet formulations.

scholarly journals Comparative studies of the kinetics of dissolution of medicines on the basis of clopidogrel

2021 ◽  
pp. 26-34
Author(s):  
O. P. Baula ◽  
O. O. Saliy ◽  
V. I. Bessаrabov ◽  
A. М. Gerasimchuk
Keyword(s):  
Comparative Studies ◽  
Generic Drugs ◽  
Dissolution Kinetics ◽  
Dissolution Test ◽  
Generic Medicines ◽  
Dissolution Medium ◽  
Clopidogrel Bisulfate ◽  
Kinetics Of Dissolution ◽  
Kinetics Of

Generic medicines occupy dominant positions both in the pharmaceutical market of Ukraine and in industrial production by domestic pharmaceutical enterprises. The use of generic drugs in medical practice is of significant medical and social importance for expanding the accessibility of the general population to essential drugs. In Ukraine, more than twenty generic medicines based on clopidogrel, both foreign and domestic, are registered. All generic drugs containing clopidogrel bisulfate must comply with pharmaceutical bisulfate must comply with pharmaceutical equivalence, the kinetics of release of the active pharmaceutical ingredient using the Dissolution test in vitro, and pharmacokinetic parameters in vivo. The aim of the work was to carry out comparative studies of the dissolution kinetics of four samples of generic drugs based on clopidogrel with the dissolution kinetics of the original drug Plavix®, to evaluate the similarity factor of dissolution profiles and to determine the effect of biopharmaceutical factors on the equivalence of generics. Comparative studies of the kinetics of dissolution were carried out by the in vitro method according to the «Dissolution» test using a device with a blade with a rotation speed of 50 rpm, a dissolution medium with a pH value of 2.0 in a volume of 900 ml at a temperature of 37 ± 1 °C. The determination of the quantitative content of clopidogrel, which passed into the dissolution medium, was carried out by the method of adsorption spectrophotometry in the ultraviolet region at a wavelength of about 240 ± 2 nm. Based on the data obtained, the dissolution profiles of the original drug Plavix® and the studied samples of generic drugs were constructed, the similarity of which was assessed by the value of the similarity factor. According to the research results, it was found that one sample of the generic drug proved its equivalence by the in vitro method to Plavix®, and three other samples of generics had differences in dissolution kinetics in comparison with the original drug. Biopharmaceutical factors were analyzed that could affect the dissolution kinetics of the studied generic drugs, from which the physicochemical characteristics of clopidogrel bisulfate, the qualitative and quantitative composition of excipients and the features of the technological process were determined. Thus, on the basis of the comparative studies of the dissolution kinetics of drugs based on clopidogrel, generics were found that did not correspond to the in vitro equivalence according to the Dissolution test to the original drug, which could be due to the influence of a combination of biopharmaceutical factors.

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