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Bayesian Methods for In Vitro Dissolution Drug Testing and Similarity Comparisons
Published in Emmanuel Lesaffre, Gianluca Baio, Bruno Boulanger, Bayesian Methods in Pharmaceutical Research, 2020
Key product development and pivotal clinical lots of IR products are usually tested at 3 to 6 time points (e.g. 15, 20, 25, 30, 45, and 60 minutes). However, Kielt et al. (2016) illustrate technology permitting continuous dissolution monitoring. Dissolution testing over time provides a dissolution profile (plot of observed % dissolution over time) for each unit tested. A wide variety of linear and nonlinear mathematical models have been fitted to dissolution profiles. Zhang et al. (2010) provide a comprehensive description of such models. An empirical model we have found useful in our work, and which we illustrate here, is the Weibull drug dissolution model. The 3-parameter Weibull drug dissolution model is obtained by adding a scale parameter M (described below) to the cumulative 2-parameter Weibull distribution function (the complement of which is the Weibull survival function which is useful in reliability analysis). This model expresses % dissolution, w, as a function of dissolution time, t, conditional on parameters M, T and b. Namely,
Use of Nanocarriers to Enhance Artemisinin Activity
Published in Tariq Aftab, M. Naeem, M. Masroor, A. Khan, Artemisia annua, 2017
The relative bioavailability in comparison with an intramuscular injection of a suspension in oil is estimated to be about 32% (Navaratnam et al., 2000). A study carried out by Ashton et al. (1998) showed high interindividual variability in plasma concentrations after both oral and rectal administration. The low bioavailability after oral intake can be due to (1) low transepithelial transport across the intestinal mucosa or (2) to the poor dissolution characteristics of artemisinin in the intestinal fluids. In any case, due to the facility of administration and improved patient compliance, artemisinin solid oral dosage forms, such as tablets and capsules, represented the most widely used formulations against malaria in China, Vietnam, and Thailand. However, no data have been reported on their comparability. During the development of a new oral dosage form, the pharmaceutical or in vitro bioavailability is generally measured for the investigation of drug bioavailability. It is evaluated by dissolution testing, considered to be sensitive, reliable, and rational for predicting in vivo drug bioavailability behavior, and is now one of the most important quality control tests performed on drugs and drug products.
Hard Shell Capsules in Clinical Trials
Published in Larry L. Augsburger, Stephen W. Hoag, Pharmaceutical Dosage Forms, 2017
Moji Christianah Adeyeye, Amusa Adebayo
The regulatory requirement for biowaivers stemmed from the BCS classification as stated earlier. Examples of useful FDA documents that can serve as a guide include Guidance for Industry: Dissolution Testing of Immediate Release Solid Oral Dosage Forms [138] and Bioavailability and Bioequivalence Studies for Orally Administered Drug Products—General Considerations [139]. The purpose of the former guidance is to act as supplement to the SUPAC-IR guidance for industry: Immediate Release Solid Oral Dosage Forms: Scale-up and Post-Approval Changes: Chemistry, Manufacturing and Controls, In Vitro Dissolution Testing, and In Vivo Bioequivalence Documentation with specific emphasis on comparative dissolution profiles. Because of the dependence of absorption on the release of the drug substance from the drug product and the dissolution or solubilization of the drug under physiological conditions, in vitro dissolution becomes an essential data for assessment of lot-to-lot quality of duct immediate-release solid dosage forms such as hard shell capsules. The data would also serve in the development of new formulations. The BCS can serve, for example, in setting in vitro dissolution specification and predicting the likelihood of achieving in vitro–in vivo correlation. The dissolution testing conditions and the basis for biowaivers are contained in the reference.
In-silico, in-vitro and ex-vivo evidence of combining silymarin phytopharmaceutical with piperine, and fulvic acid for enhancing its solubility and permeability
Published in Pharmaceutical Development and Technology, 2023
Tanya Ralli, Zoya Saifi, Amita Kumari, Vidhu Aeri, Kanchan Kohli
Dissolution testing is one of an appropriate way to test the in-vitro performance of a dosage form as well as comparing it with the reference standard (Dressman and Krämer 2005). The current section deals with studying the application of Quality by Design (QbD) assisted Design of experiment (DOE) in deciding the concentration of the BA enhancers and developing a dissolution method for the prepared formulation (Dickinson et al. 2008; Abend et al. 2019). The factors which have been taken into consideration are a) pH, b) dissolution volume, and c) concentration of bioenhancers used (in this case PIP and FA). 4 different pH conditions (DW, pH 1.2, pH 4.5, pH 6.8), 2 dissolution volume (500 and 900 ml) and 5 concentrations of bioenhancers were employed. Thus, we have applied multi-level factorial design for this purpose. Therefore, 40 experiments were performed for taking PIP and 40 experiments for taking FA with SM. Since, it was not feasible to perform such a large number of dissolution studies, thus we have mimicked the in-vitro dissolution studies in the mechanical shaker taking 10 ml of dissolution medium for 1 h at 100 rpm. After 1 h, samples were withdrawn and their concentration was estimated using UV-visible spectrophotometer.
Methylprednisolone 100 mg tablet formulation with pea protein: experimental approaches over intestinal permeability and cytotoxicity
Published in Drug Development and Industrial Pharmacy, 2023
Erhan Koc, Fatih Ciftci, Hilal Calik, Seval Korkmaz, Rabia Cakir Koc
Dissolution testing is an important quality control measure used to ensure that tablets meet these requirements and that patients receive the expected therapeutic benefits from their medicines. The dissolution test assesses how quickly and to what extent a pharmaceutical dosage form, such as a tablet or capsule, forms a solution. For a drug to be bioavailable and therapeutically effective, it must dissolve. Dissolution rate is critical in determining the therapeutic efficacy, bioequivalence and bioavailability of active pharmaceutical ingredients in the early stages of drug development. The purpose of these tests is to assess the race and extent of dissolution of the API in gastrointestinal fluids, which is an important element in predicting its absorption and distribution in the body. As a result, dissolution testing is an important technique in the development of new drugs and generic versions of established drugs [30].
Integrated approaches to testing and assessment for grouping nanomaterials following dermal exposure
Published in Nanotoxicology, 2022
Luisana Di Cristo, Gemma Janer, Susan Dekkers, Matthew Boyles, Anna Giusti, Johannes G. Keller, Wendel Wohlleben, Hedwig Braakhuis, Lan Ma-Hock, Agnes G. Oomen, Andrea Haase, Vicki Stone, Fiona Murphy, Helinor J. Johnston, Stefania Sabella
As described previously, dissolution can differ between physiological media. Indeed, we investigated the possibility of predicting dissolution of NFs in artificial sweat based on dissolution data generated in neutral pH simulated LSF and low pH PSF in a dynamic set-up. This could allow extensive dissolution testing to be minimized in the future as existing data may be used as a surrogate for estimating dissolution in different biological media. Available studies suggested strong pH dependency, where ZnO NFs dissolve quicker in acidic PSF fluid than SiO2 NFs, whereas SiO2 NFs dissolved faster in basic LSF fluids (Table SI6) (Wohlleben et al. 2019; Keller et al. 2020; Keller et al. 2021). As summarized in Table SI6, the results in ISO 105-04 simulant sweat for both ZnO and SiO2 NFs showed remarkably quicker dissolution than in LSF (pH 7.4) and PSF (pH 4.5). As metal ions are likely to be sequestrated by histidine and indeed a higher dissolution rate was observed for ZnO and SiO2, NFs in sweat simulant as compared to lung fluids, it is assumed that the outcome of dissolution studies in water or using physiological fluids other than sweat would generally be conservative (keeping the threshold at <1 h), but acceptable. Once more data becomes available on the comparative dissolution of NFs in sweat versus other commonly available physiological media, more guidance could be provided on the most relevant media to select.