In Vitro Dissolution Kinetics of Captopril from Microspheres Manufactured by Solvent Evaporation

A biowaiver means that in vivo bioavailability and/or bioequivalence studies may be waived (not considered necessary for product approval). Instead of conducting expensive and time consuming in vivo studies, a dissolution test could be adopted as the surrogate basis for the decision as to whether the two pharmaceutical products are equivalent. The biowaiver approach based on BCS is intended to replace bioequivalence in vivo studies. The aim of the study was to study dissolution kinetics of amlodipine tablets in order to assess their equivalence under conditions in vitro according to the biowaiver. The study of dissolution kinetics of drugs in the form of amlodipine tablets has been carried out in accordance with the requirements of the “biowaiver” procedure, the recommendations of the SPhU and the WHO requirements in order to assess the possibility of replacing the pharmacokinetic studies in vivo by tests in vitro. The possibility to use the recommendations of the "biowaiver" procedure for the registration of generics amlodipine tablets has been found. The studies conducted have shown that amlodipine can be referred to class І of the biopharmaceutical classification system, i.e. substances with a high biopharmaceutical solubility and a high penetration rate. It will allow conducting comparative studies in vitro to confirm the equivalence of drugs. The evaluated amlodipine drugs fulfill biowaiver criteria for drugs containing BCS Class I active pharmaceutical ingredients. Both drugs are “rapidly dissolving,” both meet the criteria of dissolution profile similarity, f2 (i.e., the dissolution profile of the test product is similar to that of the reference product in pH 1.2, 4.5, and 6.8 buffers using the paddle method at 75 rpm), and both are considered to be in vitro equivalent without in vivo evaluation. The proposed chromatographic methods are simple, rapid and accurate for the determination of amlodipine in pharmaceutical dosage forms and can be used for routine quality control of drugs and in vitro dissolution study.

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Development and Validation of an Eco-friendly HPLC-UV-DAD Method for the Determination of Allopurinol in Pharmaceuticals with Application to In vitro Dissolution Studies

Biointerface Research in Applied Chemistry ◽

10.33263/briac115.1308913101 ◽

2021 ◽

Vol 11 (5) ◽

pp. 13089-13101

Keyword(s):

Factorial Design ◽

Matrix Effects ◽

Dissolution Kinetics ◽

In Vitro Dissolution ◽

Dissolution Test ◽

Dissolution Studies ◽

Dissolution Tests ◽

Development And Validation

In this study, a sustainable HPLC-UV-DAD method was developed and validated for the determination of allopurinol in tablets and optimization of the dissolution test using factorial design. The separation of the analyte from the sample matrix was achieved in 3.01 minutes in a C8 column (4.6 mm X 150 mm X 5 μm), using mobile phase 0.1 mol L-1 HCl (25%) + ethanol (50%) + ultrapure water (25%) by UV detection at 249 nm. The method presented satisfactory analytical parameters of validation (specificity, selectivity, linearity, stability, precision, accuracy, and robustness), showing no matrix effects. The dissolution test was optimized by complete factorial design 23 and, the optimal conditions were: HCl 0.001 mol L-1, apparatus II (paddle) and 75 rpm. The analytical procedures and dissolution tests were applied to allopurinol tablets marketed in Bahia, Brazil, to evaluate the dissolution studies. The pharmaceuticals had similar dissolution profiles and first-order dissolution kinetics. This new and sustainable HPLC-UV-DAD method is friendly to the environment and can be used for the routine pharmaceutical analysis of allopurinol in fixed dosage forms.

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Physicochemical Characterization and In Vitro Dissolution Test of Quercetin-Succinic Acid Co-crystals Prepared Using Solvent Evaporation

Turkish Journal of Pharmaceutical Sciences ◽

10.4274/tjps.16362 ◽

2017 ◽

pp. 280-284 ◽

Cited By ~ 2

Author(s):

Dwi SETYAWAN ◽

Indah Pudji OKTAVIA ◽

Rizka FARIZKA ◽

Retno SARI

Keyword(s):

Succinic Acid ◽

Physicochemical Characterization ◽

Solvent Evaporation ◽

In Vitro Dissolution ◽

Dissolution Test

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Assessment of in Vitro Comparative Dissolution Kinetics of Moxonidine Products as a Factor Potentially Determining Effectiveness of Antihypertensive Treatment

Rational Pharmacotherapy in Cardiology ◽

10.20996/1819-6446-2018-14-6-951-957 ◽

2019 ◽

Vol 14 (6) ◽

pp. 951-957

Author(s):

G. V. Ramenskaya ◽

I. E. Shokhin ◽

N. I. Gaponova ◽

V. R. Abdrakhmanov

Keyword(s):

Generic Drugs ◽

Dissolution Kinetics ◽

Acetate Buffer Solution ◽

Medicinal Products ◽

Buffer Solution ◽

Reference Drug ◽

Similarity Factor ◽

Kinetics Of ◽

Comparative Dissolution

Aim. Investigation of comparative dissolution kinetics of generic medicinal products containing moxonidine versus reference drug. Material and methods. Objects of the research were film-coated tablets containing moxonidine (INN) in a dose 0.4 mg: a reference drug Physiotens® and 4 generic drugs. In vitro dissolution test of moxonidine from the study drugs was performed using comparative dissolution kinetics test (CDKT). The CDKT was performed in the media with the following pH: 1.2 (1:9 mixture of 0.1 M hydrochloric acid and water), 4.5 (acetate buffer solution, prepared as per State Pharmacopoeia, XIII), and 6.8 (phosphate buffer solution, prepared as per State Pharmacopoeia, XIII). The sampling for dissolved moxonidine was performed 5, 10, 15, 20, and 30 min after the test was started. An high performance liquid chromatography method with ultraviolet detection at 220 nm was used to assay. Results. Within 15 min more that 85% of moxonidine dissolved from the reference drug and all study drugs at pH 1.2; dissolution profiles were similar without calculation of similarity factor f2. Similarly, at pH 4.5 dissolution profiles of study drugs #2 and #3 were similar to that of the reference drug, and the similarity factor f2 was not calculated. However, in case of study drugs #1 and #4 significant differences were observed at a single time point (15 min), which suggests that their dissolution profiles are non-similar to that of the reference drug. Similarity factors f2 were calculated 17.52 and 35.30, respectively (less than 50). At pH 6.8 similarity factors f2 for all study generic drugs were also less than 50 (23.8, 49.8, 38.6, and 35.9), so their dissolution curves were non-similar to that of reference drug. Conclusion. In our study we observed difference in release in vitro of medicinal products containing moxonidines: none of the study drugs was fully similar to the reference drug in all media. The differences observed at pH 6.8 were noteworthy, where the samples had or faster kinetics (study drugs #2 and #3), or slower dissolution kinetics (test drugs #1 and #4). Observed differences in moxonidine release rate may impact absorption of active pharmaceutical ingredient into the blood following drug administration.

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Dissolution kinetics of glass fibres in saline solution: in vitro persistence of a sparingly soluble aluminium-rich leached layer

Journal of Materials Science ◽

10.1007/bf00356707 ◽

1995 ◽

Vol 30 (22) ◽

pp. 5691-5699 ◽

Cited By ~ 5

Author(s):

P. Baillif ◽

B. Chouikhi ◽

L. Barbanson ◽

J. C. Touray

Keyword(s):

Saline Solution ◽

Dissolution Kinetics ◽

Glass Fibres ◽

Kinetics Of

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Improvement in vitro Dissolution Rate of Quercetin Using Cocrystallization of Quercetin-Malonic Acid

Indonesian Journal of Chemistry ◽

10.22146/ijc.28511 ◽

2018 ◽

Vol 18 (3) ◽

pp. 531 ◽

Cited By ~ 2

Author(s):

Dwi Setyawan ◽

Sukma Adhi Permata ◽

Ahmad Zainul ◽

Maria Lucia Ardhani Dwi Lestari

Keyword(s):

Dissolution Rate ◽

Malonic Acid ◽

Fourier Transforms ◽

Solvent Evaporation ◽

Physical Mixture ◽

Original Position ◽

In Vitro Dissolution ◽

Solvent Evaporation Method ◽

Evaporation Method

The aim of the study was to improve the in-vitro dissolution rate of quercetin (Qu) using cocrystallization of quercetin. Cocrystals of quercetin (Co Qu) were produced with malonic acid (Ma) as coformer at ratio 1:2 using solvent evaporation method. Cocrystals quercetin-malonic acid (Co Qu-Ma) was characterized using Differential Thermal Analysis (DTA), Powder X-Ray Diffraction (PXRD), Scanning Electron Microscope (SEM), and Fourier Transforms Infrared Spectrophotometer (FTIR) and in-vitro dissolution study. A new endothermic peak at 277.9 °C was shown from the thermogram. Diffractogram of Co Qu-Ma showed a new diffraction peak at 2θ 9.81, 12.99, and 19.80°. Microphotograph showed that Qu and Ma exhibited a columnar-shaped and a pebble-shaped crystal, respectively, and FTIR wavenumber of O-H functional group of quercetin was shifted from its original position at 3411 to 3428 cm-1 in the physical mixture (pm) of Qu-Ma and 3418 cm-1 in Co Qu-Ma, respectively. The physicochemical characterizations using DTA, PXRD, SEM and FTIR indicated that Co Qu-Ma were successfully obtained through solvent evaporation method. The in-vitro dissolution rate of Co Qu-Ma was 95.30% at 60 min. Cocrystals effectively increased dissolution rate and dissolution efficiency in comparison to the pure quercetin and physical mixture of quercetin-malonic acid.

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Formulation, Characterization and Solubility Enhancement of Manidipine Solid Dispersions

International Journal of Pharmaceutical Sciences and Nanotechnology ◽

10.37285/ijpsn.2019.12.2.3 ◽

2019 ◽

Vol 12 (2) ◽

pp. 4453-4460

Author(s):

Laxmi Raj A ◽

Y. Shravan Kumar

Keyword(s):

Solid Dispersion ◽

Drug Carrier ◽

Solid Dispersions ◽

Solvent Evaporation ◽

In Vitro Dissolution ◽

X Ray Diffraction ◽

Amorphous Form ◽

X Ray ◽

Solvent Evaporation Process

The study was aimed to formulate solid dispersions of Manidipine by using different novel carriers like Labrafac PG, Kolliwax RH 40, Soluplus, Kolliwax GMS II, Kolliphor EL and SLS in drug carrier ratio by using solvent evaporation method. The formulations were characterized for physical appearance, solubility and in vitro dissolution studies. The optimized formulation was characterized and Formulation SD13 was found to be optimized one based on the solubility, dissolution and other parameters using Kolliwax GMS II and SLS. The drug release of the optimized formulation was found to be 99.41±5.38% within 90 min. Powder X-ray diffraction studies performed on solid dispersion showed that Manidipine existed in the amorphous form within the solid dispersion formulation fabricated using the solvent evaporation process. Additionally, scanning electron microscopy studies suggested the conversion of crystalline Manidipine to an amorphous form. Therefore, the solid dispersions using Kolliwax GMS II as hydrophilic carrier in the combination of SLS can be successfully used for improvement of solubility and dissolution of Manidipine.

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ENHANCEMENT OF SOLUBILITY AND DISSOLUTION OF IBUPROFEN BY SOLID DISPERSION TECHNIQUE AND FORMULATION OF SUSTAINED RELEASE TABLETS CONTAINING THE OPTIMISED BATCH OF SOLID DISPERSION

International Journal of Current Pharmaceutical Research ◽

10.22159/ijcpr.2017v9i5.22134 ◽

2017 ◽

pp. 37-44

Author(s):

ABHIK KAR ◽

ABDUL BAQUEE AHMED

Keyword(s):

Sustained Release ◽

Solid Dispersion ◽

Solid Dispersions ◽

Solvent Evaporation ◽

Poloxamer 407 ◽

In Vitro Dissolution ◽

Solvent Evaporation Method ◽

Evaporation Method ◽

Sustained Release Tablets

Objective: The present study was aimed to enhance the solubility of poorly water soluble drug Ibuprofen using solid dispersion technique and to develop sustained release tablets containing solid dispersion granules of the optimized batch. Ibuprofen is a non-steroidal anti-inflammatory drug (NSAID) with analgesic, antipyretic, andÂ anti-inflammatory propertiesMethods: Solid dispersions of Ibuprofen were prepared by using PEG 20000 and Poloxamer 407 in different weight ratios by fusion and solvent evaporation method. Drug-carrier physical mixtures were also prepared. Solid dispersions were characterized by saturation solubility, drug content, in vitro dissolution, FTIR and DSC analysis. Solid dispersion formulation, SDF9 (PEG 20000 and Poloxamer 407, 1:3:3) prepared by solvent evaporation method was considered as the optimized batch. Sustained release tablets containing the solid dispersion granules of the optimized batch were prepared by direct compression method using HPMC K100M at three concentrations (10%, 14%, 18% w/w). The prepared formulations were evaluated for hardness, thickness, weight variation, friability, in vitro dissolution studies and release kinetics modelling.Results: Solid dispersion formulation, SDF9showed 95.09% drug release in 60 min and considered as the optimized batch. Tablet formulation, FT3 (HPMC K100M 18% w/w) showed 96% drug release for 12 h.Conclusion: Solid dispersions of ibuprofen using a combination of PEG 20000 and poloxamer 407 by solvent evaporation method may result in higher aqueous solubility of the drug. Also sustained release tablets containing solid dispersion granules of ibuprofen, using HPMC K100M may be a promising approach to extend the release rate of the drug from the solid dispersion for 12 h.

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