Quantitative Correlation of Absorption and In Vitro Dissolution Kinetics of Aspirin from Several Dosage Forms

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

Dissolution Technologies ◽

10.14227/dt190112p42 ◽

2012 ◽

Vol 19 (1) ◽

pp. 42-51 ◽

Cited By ~ 4

Author(s):

Sandile M. Khamanga ◽

Roderick B Walker

Keyword(s):

Dissolution Kinetics ◽

Solvent Evaporation ◽

In Vitro Dissolution ◽

Kinetics Of

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

International Journal of Pharmaceutical Sciences and Nanotechnology ◽

10.37285/ijpsn.2009.2.3.7 ◽

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.

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In vitro dissolution absorption system (IDAS2): Use for the prediction of food viscosity effects on drug dissolution and absorption from oral solid dosage forms

European Journal of Pharmaceutical Sciences ◽

10.1016/j.ejps.2019.105164 ◽

2020 ◽

Vol 143 ◽

pp. 105164

Author(s):

Svitlana Silchenko ◽

Nourdine Nessah ◽

Jibin Li ◽

Li-Bin Li ◽

Yuehua Huang ◽

...

Keyword(s):

Dosage Forms ◽

Drug Dissolution ◽

In Vitro Dissolution ◽

Absorption System ◽

Solid Dosage Forms ◽

Solid Dosage ◽

Viscosity Effects

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The differences between the branded and generic medicines using solid dosage forms: In-vitro dissolution testing

Results in Pharma Sciences ◽

10.1016/j.rinphs.2011.12.001 ◽

2012 ◽

Vol 2 ◽

pp. 1-8 ◽

Cited By ~ 16

Author(s):

Mubarak Nasser Al Ameri ◽

Nanda Nayuni ◽

K.G. Anil Kumar ◽

David Perrett ◽

Arthur Tucker ◽

...

Keyword(s):

Dosage Forms ◽

In Vitro Dissolution ◽

Dissolution Testing ◽

Generic Medicines ◽

Solid Dosage Forms ◽

Solid Dosage

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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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Requirements for Additional Strength Biowaivers for Modified Release Solid Oral Dosage Forms in International Pharmaceutical Regulators Programme Participating Regulators and Organisations: Differences and Commonalities

Journal of Pharmacy & Pharmaceutical Sciences ◽

10.18433/jpps32260 ◽

2021 ◽

Vol 24 ◽

pp. 548-562

Author(s):

Matthias Shona Roost ◽

Henrike Potthast ◽

Chantal Walther ◽

Alfredo García-Arieta ◽

Ivana Abalos ◽

...

Keyword(s):

Immediate Release ◽

Dosage Forms ◽

Oral Dosage ◽

In Vitro Dissolution ◽

Quantitative Composition ◽

Modified Release ◽

Solid Oral Dosage Forms ◽

Oral Dosage Forms

This article describes an overview of waivers of in vivo bioequivalence studies for additional strengths in the context of the registration of modified release generic products and is a follow-up to the recent publication for the immediate release solid oral dosage forms. The current paper is based on a survey among the participating members of the Bioequivalence Working Group for Generics (BEWGG) of the International Pharmaceutical Regulators Program (IPRP) regarding this topic. Most jurisdictions consider the extrapolation of bioequivalence results obtained with one (most sensitive) strength of a product series as less straightforward for modified release products than for immediate release products. There is consensus that modified release products should demonstrate bioequivalence not only in the fasted state but also in the fed state, but differences exist regarding the necessity of additional multiple dose studies. Fundamental differences between jurisdictions are revealed regarding requirements on the quantitative composition of different strengths and the differentiation of single and multiple unit dosage forms. Differences in terms of in vitro dissolution requirements are obvious, though these are mostly related to possible additional comparative investigations rather than regarding the need for product-specific methods. As with the requirements for immediate release products, harmonization of the various regulations for modified release products is highly desirable to conduct the appropriate studies from a scientific point of view, thus ensuring therapeutic equivalence.

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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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