Development of Dissolution Tests on the Basis of Gastrointestinal Physiology

Klein, Sandra; Wunderlich, Martin; Stippler, Erika; Dressman, Jennifer B.

doi:10.1201/9780849359170.ch7

Cited by 13 publications

(20 citation statements)

References 8 publications

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“…A range of biorelevant dissolution test media and experimental methodologies have been developed that have application in drug release studies from lipid-based oral formulations. 27,28 However, an in vitro dispersion test in aqueous media can estimate how much drug will be in solution before absorption and thus may predict the fate of the drug in vivo.…”

Section: Dynamic Dispersion and Drug Precipitation Studiesmentioning

confidence: 99%

Development of self-nanoemulsifying drug delivery systems for the enhancement of solubility and oral bioavailability of fenofibrate, a poorly water-soluble drug

Kazi¹,

Alamri²,

Ahmad³

et al. 2016

IJN

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Background Self-nanoemulsifying drug delivery systems (SNEDDS) have become a popular formulation option as nanocarriers for poorly water-soluble drugs. The objective of this study was to investigate the factor that can influence the design of successful lipid formulation classification system (LFCS) Type III SNEDDS formulation and improve the oral bioavailability (BA) of fenofibrate. Materials and methods LFCS Type III SNEDDS were designed using various oils, water-soluble surfactants, and/or cosolvents (in considering the polarity of the lipids) for the model anticholesterol drug, fenofibrate. The developed SNEDDS were assessed visually and by measurement of the droplet size. Equilibrium solubility of fenofibrate in the SNEDDS was conducted to find out the maximum drug loading. Dynamic dispersion studies were carried out (1/100 dilution) in water to investigate how much drug stays in solution after aqueous dispersion of the formulation. The BA of SNEDDS formulation was evaluated in the rat. Results The results from the characterization and solubility studies showed that formulations containing mixed glycerides were highly efficient SNEDDS as they had higher solubility of the drug and produced nanosized droplets. The dispersion studies confirmed that SNEDDS (containing polar mixed glycerides) can retain >98% drug in solution for >24 hours in aqueous media. The in vivo pharmacokinetics parameters of SNEDDS formulation in comparison with pure drug showed significant increase in C max and AUC 0– t , ~78% and 67%, respectively. The oral BA of fenofibrate from SNEDDS in rats was ~1.7-fold enhanced as compared with the BA from pure drug. Conclusion Fenofibrate-loaded LFCS Type III SNEDDS formulations could be a potential oral pharmaceutical product for administering the poorly water-soluble drug, fenofibrate, with an enhanced oral BA.

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Section: Dynamic Dispersion and Drug Precipitation Studiesmentioning

confidence: 99%

Development of self-nanoemulsifying drug delivery systems for the enhancement of solubility and oral bioavailability of fenofibrate, a poorly water-soluble drug

Kazi¹,

Alamri²,

Ahmad³

et al. 2016

IJN

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“…These methodologies involve mostly weak acids or bases (Klein et al, 2005). When modified-release products are tested in apparatus 3, it is possible to simulate the different environments to which the dosage forms are subject when they pass through the GI tract (Figure 2).…”

Section: Applications For Modified-release Solid Oral Dosage Formsmentioning

confidence: 99%

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

Pezzini

Issa

Duque

et al. 2015

Braz. J. Pharm. Sci.

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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.

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“…Residence times were chosen to represent typical GI transit of solid dosage forms. The pH and the bile salt (sodium taurocholate) concentration were adjusted to mimic physiological conditions and the active reabsorption of bile salts from the ileum as described by Klein et al (11) and shown in Table 2.…”

Section: Experiments With Usp Apparatusmentioning

confidence: 99%

“…After cooling to room temperature, the volume was adjusted to 2 L with blank FaSSIF. To simulate the upper ileum, 1.55 g of sodium taurocholate was used to constitute halved bile salts (11).…”

Section: Fasted State Simulated Intestinal Fluid (Fassif)mentioning

confidence: 99%

Modeling and Comparison of Dissolution Profiles of Diltiazem Modified-Release Formulations

Samaha¹,

Shehayeb

Kyriacos

2009

Dissolution Technol.

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Generic drugs offer a cost-effective alternative to brand-name products. However, the main concern with modified-release formulations is the substitution of one product for another. Accordingly, the first objective of this study was to assess the interchangeability of the available diltiazem extended-release (ER) products on the basis of their in vitro dissolution characteristics using USP Apparatus 2 and 3. The second objective was to compare dissolution profiles in simulated fasted and fed states and determine whether there is a change in the mechanism of drug release. Dissolution profiles characterized using Apparatus 2 or 3 under fasted conditions were similar. However, Apparatus 3 testing provided a more discriminating and comprehensive evaluation of the drug release performance of ER products. Testing using Apparatus 3 in the fed state highlighted some difference in dissolution profiles, suggesting a food effect on drug release. This implies that, depending on the targeted concentration, a patient should be instructed whether to take the medication in fasted or fed state. The study therefore shows the necessity of testing the products in both fasted and fed states to determine their similarity and therapeutic interchangeability. Apparatus 3 testing was also more accurate in determining the release mechanism than the Apparatus 2 method. No change in the mechanism of drug release between fasted and fed state was observed.

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Development of Dissolution Tests on the Basis of Gastrointestinal Physiology

Cited by 13 publications

References 8 publications

Development of self-nanoemulsifying drug delivery systems for the enhancement of solubility and oral bioavailability of fenofibrate, a poorly water-soluble drug

Development of self-nanoemulsifying drug delivery systems for the enhancement of solubility and oral bioavailability of fenofibrate, a poorly water-soluble drug

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

Modeling and Comparison of Dissolution Profiles of Diltiazem Modified-Release Formulations

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