Applications of USP apparatus 3 in assessing the in vitro release of solid oral dosage forms

Abstract

USP Apparatus 3 (reciprocating cylinder) is a very versatile device for the in vitro assessment of release characteristics of solid oral dosage forms, because it enables the product to be subjected to different dissolution media and agitation speeds in a single run. In this paper, a brief history and a description of this system are presented, along with its applications in the development of immediate and modified release products and in the simulation of fasted and fed states using biorelevant media. Furthermore, a comparison is made with the basket and paddle apparatus, especially highlighting the superior hydrodynamics of USP apparatus 3, since the results are not sensitive to factors such as the presence of sample collection probes or air bubbles in the dissolution medium.Uniterms: Solid dosage forms/in vitro release. Solid dosage forms/dissolution. Apparatus 3/use/evaluation of solid dosage forms. Reciprocating cylinders.USP aparato 3 (cilindros recíprocos) é um equipamento bastante versátil para a avaliação das características de liberação in vitro de formas farmacêuticas sólidas orais, pois permite que o produto seja submetido a diferentes meios de dissolução e condições de agitação, em um único ensaio. Neste trabalho, são apresentados um breve histórico e a descrição desse sistema, suas aplicações no desenvolvimento de produtos de liberação imediata e modificada, assim como sua utilização na simulação dos estados não alimentado e alimentado com o emprego de meios biorrelevantes. Além disso, uma comparação é estabelecida com o cesto e a pá, com destaque para a hidrodinâmica superior do USP aparato 3, que faz com que os resultados não sejam influenciados por fatores como o uso de sondas de coleta de amostras ou presença de bolhas de ar no meio de dissolução.Unitermos: Formas farmacêuticas sólidas/liberação in vitro. Formas farmacêuticas sólidas/dissolução. USP Aparato 3/uso/avaliação de formas farmacêuticas sólidas. Cilindros recíprocos.

Development of a Dissolution Method for Gliclazide Modified-Release Tablets Using USP Apparatus 3 with <i>in Vitro–in Vivo</i> Correlation

“…USP apparatus 2 can present some disadvantages depending on the agitation rate and pharmaceutical formulation, such as the coning phenomenon, 35) which was observed in this study. This phenomenon is characterized by a cone-shaped formation at the bottom of the dissolution vessel composed of visible particulates of the pharmaceutical under study caused by the weak agitation capacity of the system.…”

“…Previous reports on the use of the USP1 for the evaluation of pharmaceutical formulations containing hydrophilic matrices, such as the GLZ MR tablets studied here, indicated that hydration and swelling of the dosage matrix form can clog the retaining basket, which could disrupt the hydrodynamics of dissolution and, thereby, reduce the total percentage of dissolved drug. 34,35) Due to the greater dissolution of GLZ in a USP2 and the dependence of the drug release rate on media composition, 5) dissolution profiles were determined in the USP2 for three different media maintaining the other variables (Fig. 3B).…”

“…These particles do not dissolve appropriately and may reduce the total percentage of the dosage form dissolution. 34,35) Therefore, it was of interest to evaluate other dissolution apparatus for GLZ MR tablets, such as apparatus 3, which was specifically designed for MR dosage forms. Although USP1 and USP2 did not demonstrate the ideal hydrodynamic conditions to reflect in vivo conditions, their use in the evaluation of the different dissolution media was important to our study.…”

“…11,35) The use of different dissolution media and pH steps are generally more discriminative and better able to mimic in vivo conditions. 34,35) Our focus shifted to employing the USP3 and the effect of the immersion rate on the IVIVC, presented in Fig. 6A, which indicated a high correlation coefficient (R 2 >0.95) for each of the three rates.…”

Determination of absorption curves, dissolution profiles and establishment of <i>in vitro-in vivo</i> correlation by <i>in silico</i> methods using GastroPlus^TM and DDDPlus^TM

“…Dissolution kinetics were carried out with four ketoprofen matrix tablet formulations (FM1, FM2, FM3 and FM4) containing 200 mg of the drug and hypromellose (Methocel ® K4M or Methocel ® K100M) at the following ratios: FM1 (10% Methocel ® K4M), FM2 (10% Methocel ® K100M), FM3 (20% Methocel ® K4M) and FM4 (20% Methocel ® K100M), as previously reported by Pezzini;Ferraz (2009) Dissolution kinetic models (Zero-order, Higuchi and Korsmeyer-Peppas) were applied to dissolution profiles using the add-in program DDSolver for Microsoft Excel (ZHANG et al, 2010;ZUO et al, 2014). For comparative purposes, the same dissolution kinetic models were applied to the dissolution profile of the reference product Profenid ® Retard 200 mg tablets (Ref) obtained from previous work (ÇOMOĞLU et al, 2007), considering dissolution using USP Apparatus 2 with 900 mL of phosphate buffer pH 7.4, at 50 rpm and 37 ± 0.5 °C.…”