Improved oral absorption of tacrolimus by a solid dispersion with hypromellose and sodium lauryl sulfate

Jung, Hyuck Jun; Ahn, Hye In; Park, Ji Yeon; Ho, Myoung Jin; Lee, Dae Ro; Cho, Ha Ra; Park, Jun Seo; Choi, Yong Seok; Kang, Myung Joo

doi:10.1016/j.ijbiomac.2015.11.063

Cited by 29 publications

(12 citation statements)

References 18 publications

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“…Fasting blood samples were collected in the early morning and analyzed for red blood cells [RBC, sheath flow direct current (DC)] [ 26 ], white blood cells (WBC, flow cytometry method) [ 27 ], serum hemoglobin (Hb, sodium lauryl sulfate-Hb) [ 28 ], hematocrit (Ht, red blood cell pulse height detection method) [ 29 ], blood platelet count (PLT, sheath flow DC) [ 30 ], total protein (TP, biuret method) [ 31 ], serum albumin (bromocresol green) [ 32 ], aspartate aminotransferase (AST), alanine aminotransferase (ALT), and γ-glutamyl transpeptidase (γ-GTP, Japan Society of Clinical Chemistry transferable method) [ 33 ], serum total cholesterol (TC, enzyme method) [ 34 ], triglycerides (TG, enzyme method) [ 34 ], high-density lipoprotein cholesterol (HDL-C, direct method) [ 35 ], low-density lipoprotein cholesterol (LDL-C, enzyme method) [ 34 ], and HbA 1c (latex photometric immunoassay) [ 36 ]. Based on findings from previous studies, inflammation markers [C-reactive protein (CRP, latex turbidimetric immunoassay)] [ 37 ], medications [major and minor tranquilizers, anticonvulsants, and others (i.e., gastrointestinal medications, medications for the common cold, cardiovascular drugs)], and immunoglobulin G (IgG, turbidimetric immunoassay) [ 38 ] were also analyzed.…”

Section: Methodsmentioning

confidence: 99%

Serum albumin levels and their correlates among individuals with motor disorders at five institutions in Japan

et al. 2017

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BACKGROUND/OBJECTIVESThe level of serum albumin is an index of nourishment care and management. However, the distribution and correlates of serum albumin levels among individuals with motor disorders have not been reported until now. Therefore, we examined the distribution and correlates of serum albumin levels among individuals with motor disorders.SUBJECTS/METHODSA cross-sectional study on 249 individuals with motor disabilities (144 men, mean age: 51.4 years; 105 women, mean age: 51.4 years) was conducted at five institutions in Ibaraki Prefecture, Japan in 2008. The results were compared with data from the National Health and Nutrition Survey.RESULTSThe mean serum albumin levels were 4.0 ± 0.4 g/dL for men and 3.8 ± 0.5 g/dL for women. Overall, 17 (11.8%) men and 25 (23.8%) women had hypoalbuminemia (serum albumin level ≤ 3.5 g/dL); these proportions were greater than those among healthy Japanese adults (≤ 1%). Low serum albumin level was related with female sex, older age, low calf circumference, low relative daily energy intake, low hemoglobin (Hb), low blood platelet count, low high-density lipoprotein cholesterol (HDL-C), low HbA1c, and high C-reactive protein (CRP) levels. The strongest correlates, based on standardized betas, were Hb (0.321), CRP (-0.279), and HDL-C (0.279) levels.CONCLUSIONSThese results indicate that the prevalence of hypoalbuminemia is higher in individuals with motor disabilities than in healthy individuals and that inflammation is a strong negative correlate of serum albumin levels. Therefore, inflammation should be examined for the assessment of hypoalbuminemia among institutionalized individuals with motor disabilities.

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Section: Methodsmentioning

confidence: 99%

Serum albumin levels and their correlates among individuals with motor disorders at five institutions in Japan

et al. 2017

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“…The majority of the studies used a large volume of medium (≥250 ml), which can indirectly be translated to the equally large amounts of materials required in practice. Depending on the condition selected (sink or non-sink), weight of samples between 5–1800 mg were reported (72,74,77–79,83–85,87,90,91,95,100,105,106,109–111,114,116,121,126,128,130,135,136,138,149,154,166,170). Interestingly, the use of small-scale or miniaturized in vitro dissolution methods is still limited.…”

Section: Current Status Of Research On Amorphous Formulationsmentioning

confidence: 99%

“…deionized, degassed, distilled, purified), HCl, and phosphate/acetate buffers at pHs ranging from 1.2 to 7.4 (71–74,77–79,81–88,90–92,95,100–107,109–111,113–119,121,126,127,129–133,135–139,149,150,153,154,156,160,161,166,168–177). Among the 88 studies that reported a dissolution assay, only sixteen (~18%) used a biorelevant dissolution medium (BDM) such as simulated gastrointestinal fluids and simulated saliva (77,79,82,97,121,123,130,135,136,145,152,154,160,169,170,176). These disparities in medium used affect the conclusions, which (as with the stability studies) make head-to-head comparison difficult.…”

Section: Current Status Of Research On Amorphous Formulationsmentioning

confidence: 99%

The Need for Restructuring the Disordered Science of Amorphous Drug Formulations

2017

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The alarming numbers of poorly soluble discovery compounds have centered the efforts towards finding strategies to improve the solubility. One of the attractive approaches to enhance solubility is via amorphization despite the stability issue associated with it. Although the number of amorphous-based research reports has increased tremendously after year 2000, little is known on the current research practice in designing amorphous formulation and how it has changed after the concept of solid dispersion was first introduced decades ago. In this review we try to answer the following questions: What model compounds and excipients have been used in amorphous-based research? How were these two components selected and prepared? What methods have been used to assess the performance of amorphous formulation? What methodology have evolved and/or been standardized since amorphous-based formulation was first introduced and to what extent have we embraced on new methods? Is the extent of research mirrored in the number of marketed amorphous drug products? We have summarized the history and evolution of amorphous formulation and discuss the current status of amorphous formulation-related research practice. We also explore the potential uses of old experimental methods and how they can be used in tandem with computational tools in designing amorphous formulation more efficiently than the traditional trial-and-error approach.

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“…This is not surprising as the use of surfactants and surfactants-polymers as carriers has been an emerging trend in the last two decades [26]. When polymers alone cannot achieve high kinetic solubilization, they are augmented with copious amounts of surfactants that can solubilize drugs through micellar solubilization and surfactant-polymer complex formation [22,27,28].…”

Section: Introductionmentioning

confidence: 99%

Spray-Dried Amorphous Solid Dispersions of Griseofulvin in HPC/Soluplus/SDS: Elucidating the Multifaceted Impact of SDS as a Minor Component

et al. 2020

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This study aimed to elucidate the impact of a common anionic surfactant, sodium dodecyl sulfate (SDS), along with hydroxypropyl cellulose (HPC) and Soluplus (Sol) on the release of griseofulvin (GF), a poorly soluble drug, from amorphous solid dispersions (ASDs). Solutions of 2.5% GF and 2.5%–12.5% HPC/Sol with 0.125% SDS/without SDS were prepared in acetone–water and spray-dried. The solid-state characterization of the ASDs suggests that GF–Sol had better miscibility and stronger interactions than GF–HPC and formed XRPD-amorphous GF, whereas HPC-based ASDs, especially the ones with a lower HPC loading, had crystalline GF. The dissolution tests show that without SDS, ASDs provided limited GF supersaturation (max. 250%) due to poor wettability of Sol-based ASDs and extensive GF recrystallization in HPC-based ASDs (max. 50%). Sol-based ASDs with SDS exhibited a dramatic increase in supersaturation (max. 570%), especially at a higher Sol loading, whereas HPC-based ASDs with SDS did not. SDS did not interfere with Sol’s ability to inhibit GF recrystallization, as confirmed by the precipitation from the supersaturated state and PLM imaging. The favorable use of SDS in a ternary ASD was attributed to both the wettability enhancement and its inability to promote GF recrystallization when used as a minor component along with Sol.

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Improved oral absorption of tacrolimus by a solid dispersion with hypromellose and sodium lauryl sulfate

Cited by 29 publications

References 18 publications

Serum albumin levels and their correlates among individuals with motor disorders at five institutions in Japan

Serum albumin levels and their correlates among individuals with motor disorders at five institutions in Japan

The Need for Restructuring the Disordered Science of Amorphous Drug Formulations

Spray-Dried Amorphous Solid Dispersions of Griseofulvin in HPC/Soluplus/SDS: Elucidating the Multifaceted Impact of SDS as a Minor Component

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