Biowaiver Monographs for Immediate-Release Solid Oral Dosage Forms: Folic Acid

Hofsäss, Martin A.; Souza, Jacqueline de; Silva-Barcellos, Neila Márcia; Bellavinha, Karime Rezende; Abrahamsson, Bertil; Cristofoletti, Rodrigo; Groot, D.W.; Parr, Alan; Langguth, Peter; Polli, James E.; Shah, Vinod P.; Tajiri, Tomokazu; Mehta, Mehul; Dressman, Jennifer B.

doi:10.1016/j.xphs.2017.08.007

Cited by 20 publications

(12 citation statements)

References 49 publications

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“…At the pH of ATPS studied in this work (PEG–Na 3 Citrate: pH 8.25 [bottom], 8.45 [top], PEG–Na 2 Tartrate: pH 7.75 [bottom], 7.70 [top]) the water‐soluble vitamins under consideration are negatively charged (VB2 − , VB3 acid− , VB9 2− , VB9 3− ) or neutral (VB3 amide , VB12). The p K a values necessary for the calculation of vitamin species distributions in each ATPS phase have been used as reported in the literature 39‐47 (Table 1). The mean charge number q mean of all vitamin species present in aqueous solution over different pHs is shown in Figure 1.…”

Section: Introductionmentioning

confidence: 99%

Partitioning of water‐soluble vitamins in biodegradable aqueous two‐phase systems: Electrolyte perturbed‐chain statistical associating fluid theory predictions and experimental validation

et al. 2020

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Partition coefficients (K) of vitamins (riboflavin, nicotinic acid, nicotinamide, folic acid, cyanocobalamin) in aqueous two‐phase systems (ATPS) composed by polyethylene glycol (PEG 4000, PEG 6000) and organic salt (sodium citrate and sodium tartrate) at T = 298.15 K and p = 1 bar have been studied. Data on liquid–liquid equilibria of the ATPS considered in this study have been taken from the literature (PEG‐Na3Citrate) or measured in this work (PEG‐Na2Tartrate) for PEG 4000 and PEG 6000 at T = 298.15 K and p = 1 bar. The experimental K values were validated by electrolyte perturbed‐chain‐statistical associating fluid theory predictions. The neutral cyanocobalamin has the highest K values among all studied vitamins at any ATPS studied in this work. This finding contrasted with expectations based on literature data which let assume that charged species have typically the highest K values in the considered ATPS. Thus, besides the typically strong charge–charge interactions especially specific forces (e.g., hydrogen bonding) explains the strong PEG‐cyanocobalamin interaction resulting in the high K values.

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Section: Introductionmentioning

confidence: 99%

Partitioning of water‐soluble vitamins in biodegradable aqueous two‐phase systems: Electrolyte perturbed‐chain statistical associating fluid theory predictions and experimental validation

et al. 2020

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“…The development of pharmaceutical forms begins with the preformulation process, which establishes the physical and chemical, pharmaceutical and technological, pharmacological and toxicological features of substances [ 1 ]. As an active pharmaceutical ingredient, miconazole nitrate (MN) is a broad spectrum antifungal agent which has already been studied in the form of mucoadhesive tablets, polymeric matrices (chitosan, gelatine, gum arabic, alginate, carbopol or acrylic resins), microgels, nano-lipid gels or nano-vesicles formulated to treat oral or vaginal candidiasis [ 2 , 3 , 4 , 5 , 6 , 7 ].…”

Section: Introductionmentioning

confidence: 99%

Development of Dermal Films Containing Miconazole Nitrate

et al. 2018

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This study aims to develop new antifungal dermal films based on their mechanical properties (elongation, adhesion, behaviour towards vapour moisture) and the in vitro availability of miconazole nitrate, used as a pharmaceutical active ingredient in various concentrations. The three polymeric films prepared were translucent or shiny, with the surface of 63.585 cm2, 0.20–0.30 mm thickness, and content of miconazole nitrate of 3.931 or 15.726 mg·cm2. The mechanical resistance and elongation tests demonstrated that the two films based on hydroxyethyl cellulose (HEC) polymer were more elastic than the one prepared with hydroxypropyl methylcellulose (HPMC). The vapour water absorption and vapour water loss capacity of the films revealed that the HPMC film did not dry very well in the process of preparation by the evaporation of the solvent technique, unlike the HEC films that jellified more evenly in water and had higher drying capacity at 40 °C. The in vitro availability of miconazole nitrate from dermal films was evaluated using the Franz diffusion cell method, through a synthetic membrane (Ø 25 mm × 0.45 µm) and acceptor media with pH 7.4 (phosphate buffer and sodium lauryl sulphate 0.045%), resulting a release rate of up to 70%.

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“…The highly hydrophilic FA is less likely to pass the intestinal membrane by passive transport, thus having lower HIA percentages, unlike the more lipophilic thiopurines. A number of studies, however, determined the absorption of FA to be relatively high, ranging from 75 to 90 % (35). It can be concluded that the platforms predict HIA according to lipophilicity, but do not take the vital role of various transporters present in the human intestines into account.…”

Section: Comparison Of Experimental and Predicted Datamentioning

confidence: 99%

Miniaturized shake-flask HPLC method for determination of distribution coefficient of drugs used in inflammatory bowel diseases

et al. 2019

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A new method for determination of distribution coefficient of drugs azathioprine, 6-mercaptopurine and 6-thioguanine and nutrient folic acid used in the treatment of inflammatory bowel disease based on a miniaturized shake-flask and HPLC/DAD was developed. Special attention was made to the most commonly reported problems in the measurement of distribution coefficients using a shake-flask method such as mixing technique, speed and time, the temperature of experiment, type of buffer and its pH as well as n-octanol/buffer phase ratio. The concentration of compounds in the buffer is determined by HPLC directly from shake flasks or conventional 2-mL vials. The developed method was fully validated according to ICH guidelines. Furthermore, experimental data were successfully compared with lipophilicity and human intestinal absorption calculated by the use of four different theoretical approaches. The method shows potential for high-throughput measurements of a large number of compounds.

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Biowaiver Monographs for Immediate-Release Solid Oral Dosage Forms: Folic Acid

Cited by 20 publications

References 49 publications

Partitioning of water‐soluble vitamins in biodegradable aqueous two‐phase systems: Electrolyte perturbed‐chain statistical associating fluid theory predictions and experimental validation

Partitioning of water‐soluble vitamins in biodegradable aqueous two‐phase systems: Electrolyte perturbed‐chain statistical associating fluid theory predictions and experimental validation

Development of Dermal Films Containing Miconazole Nitrate

Miniaturized shake-flask HPLC method for determination of distribution coefficient of drugs used in inflammatory bowel diseases

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