Abstract:
:Combined dissolution and permeation systems are designed to simultaneously assess the dissolution of a pharmaceutical dosage form and the permeation of dissolved drugs therefrom. However, there were still some limitations on predicting the possible absorption rate-limiting steps and improving the in vitro-in vivo correlation (IVIVC) of a complete dosage form. In this study, the modified biorelevant media with some solubilizers and pH modifiers were integrated into the drug dissolution/absorption simulating system (DDASS). Indapamide, a poorly soluble compound (pKa = 8.8), was selected to validate the applicability of the modified biorelevant media. The elution and permeation dynamics of indapamide were investigated by using appropriate solubilizing agents in the DDASS. The absorption behaviors were analyzed after oral administration of indapamide in beagle dogs. The absorption rate-limiting steps and IVIVCs were predicted from the dissolution-permeation-absorption dynamic parameters. As a result, the absorption fraction of indapamide in the FaSSIFmod of DDASS was estimated to be approximately 100%, in accordance with its high permeability. The ratios of permeation rate to elution rate were 2.55 and 3.34 for the immediate- and sustained-release tablets of indapamide, respectively, suggesting a dissolution rate-limiting absorption for indapamine. In addition, point-to-point correlations were established between in vitro elution and in vivo absorption by the nonlinear and linear regression analysis ways (r > 0.85). The findings indicate that DDASS is a promising technique to develop improved IVIVCs of a complete dosage form, and the FaSSIFmod is suitable to predict the possible absorption rate-limiting steps of poorly soluble drugs in DDASS.
journal_name
AAPS PharmSciTechjournal_title
AAPS PharmSciTechauthors
Li Z,He X,Tian S,Feng G,Huang C,Xun M,Wu Z,Wang Ydoi
10.1208/s12249-019-1544-3subject
Has Abstractpub_date
2019-10-24 00:00:00pages
321issue
8issn
1530-9932pii
10.1208/s12249-019-1544-3journal_volume
20pub_type
杂志文章abstract::The purpose of this research was to use our previously validated dynamic injection apparatus as a rapid method for screening pH-adjusted formulations of a new vancomycin analog, Van-An, for their potential to precipitate upon dilution. In 1 vial, Van-An was reconstituted according to the manufacturer's instructions. I...
journal_title:AAPS PharmSciTech
pub_type: 杂志文章
doi:10.1208/pt070105
更新日期:2006-03-01 00:00:00
abstract::The potential value of succinylated soy protein (SPS) as a wall material for the encapsulation of ibuprofen (IBU), a model hydrophobic drug, by spray-drying was investigated. A succinylation rate of 93% was obtained for soy protein isolate, with a molar ratio of 1/1.5 (NH2/succinic anhydride). The solubility profile a...
journal_title:AAPS PharmSciTech
pub_type: 杂志文章
doi:10.1208/s12249-018-1250-6
更新日期:2019-01-11 00:00:00
abstract::The present investigation concerns with the development and optimization of an in situ forming formulation using 3(3) full factorial design experimentation. Metformin, an antidiabetic drug with upper part of gastrointestinal tract as absorption window was used as a model drug. The formulations were designed with an ob...
journal_title:AAPS PharmSciTech
pub_type: 杂志文章
doi:10.1208/s12249-009-9285-3
更新日期:2009-01-01 00:00:00
abstract::Bottles and carboys are used for frozen storage and transport of biopharmaceutical formulations under a wide range of conditions. The quality of freezing and thawing in these systems has been questioned due to the formation of heterogeneous ice structures and deformation of containers. This work shows that during free...
journal_title:AAPS PharmSciTech
pub_type: 杂志文章
doi:10.1208/s12249-020-01794-x
更新日期:2020-09-01 00:00:00
abstract::The purpose of this research was to develop and evaluate buccal mucoadhesive controlled release tablets of lercanidipine hydrochloride using polyethylene oxide and different viscosity grades of hydroxypropyl methylcellulose individually and in combination. Effect of polymer type, proportion and combination was studied...
journal_title:AAPS PharmSciTech
pub_type: 杂志文章
doi:10.1208/s12249-007-9031-7
更新日期:2008-01-01 00:00:00
abstract::The objective of the present study is to investigate the effect of hydrocarbon chain length in 1,2-alkanediols on percutaneous absorption of metronidazole (MTZ). Twelve formulations (1,2-propanediol, 1,2-butanediol, 1,2-pentanediol, 1,2-hexanediol in 4% concentration, 1,2-hexanediol, and 1,2-heptanediol in 1% concentr...
journal_title:AAPS PharmSciTech
pub_type: 杂志文章
doi:10.1208/s12249-013-0066-7
更新日期:2014-04-01 00:00:00
abstract::The purpose of this research was to improve the solubility and therefore dissolution and bioavailability of triamterene, a poorly water soluble diuretic, by complexation with beta-cyclodextrin. Triamterene has been reported to show low bioavailability after oral administration, with wide intersubject variation. This s...
journal_title:AAPS PharmSciTech
pub_type: 杂志文章
doi:10.1208/pt050119
更新日期:2004-03-29 00:00:00
abstract::The main principles of green chemistry and engineering were extended to pharmaceutical formulations to prepare eco-friendly surfactant-free dry emulsion tablets (SFDETs) devoid of solvents or synthetic surfactants. Surfactant-free emulsions were stabilized by in situ cyclodextrins/sweet almond oil inclusion complexes ...
journal_title:AAPS PharmSciTech
pub_type: 杂志文章
doi:10.1208/s12249-019-1450-8
更新日期:2019-07-18 00:00:00
abstract::A co-processed excipient was prepared from commercially available crystalline mannitol and α-chitin using direct compression as well as spray, wet, and dry granulation. The effect of the ratio of the two components, percentage of lubricant and particle size, on the properties of the prepared co-processed excipient has...
journal_title:AAPS PharmSciTech
pub_type: 杂志文章
doi:10.1208/s12249-010-9523-8
更新日期:2010-12-01 00:00:00
abstract::The purpose of this research was to evaluate in vitro transnasal sustained-release ability of sorbitan monostearate (SMS) organogels in isopropyl myristate (IM). Organogels were prepared containing SMS (2.5%-20%) and water (5%-25%) in IM and analyzed microscopically for phase behavior. The effect of Tween surfactants ...
journal_title:AAPS PharmSciTech
pub_type: 杂志文章
doi:10.1208/pt050463
更新日期:2004-09-13 00:00:00
abstract::The aim of this study was to identify trends in deficiencies raised during the EU evaluation of the quality part of dossiers for marketing authorisation applications of biosimilar medicinal products. All adopted day 120 list of questions on the quality module of 22 marketing authorisation applications for biosimilars ...
journal_title:AAPS PharmSciTech
pub_type: 杂志文章
doi:10.1208/s12249-017-0892-0
更新日期:2018-02-01 00:00:00
abstract::The present work embarks upon increasing the dissolution rate and the bioavailability of model anti-diabetic drug, gliquidone, a sulfonylurea class drug used for treating diabetes mellitus type 2. The gliquidone nanoparticles were prepared by using anti-solvent precipitation technique in which, gliquidone solution in ...
journal_title:AAPS PharmSciTech
pub_type: 杂志文章
doi:10.1208/s12249-019-1577-7
更新日期:2019-12-26 00:00:00
abstract::The purpose of this research was to develop and evaluate different preparations of sustained delivery systems, using Carbopols as carriers, in the form of matrices and three-layer tablets with isosorbite mononitrate. Matrix tablets were prepared by direct compression whereas three-layer tablets were prepared by compre...
journal_title:AAPS PharmSciTech
pub_type: 杂志文章
doi:10.1208/s12249-008-9084-2
更新日期:2008-01-01 00:00:00
abstract::Pharmaceutical excipients contain reactive groups and impurities due to manufacturing processes that can cause decomposition of active drug compounds. The aim of this investigation was to determine if commercially available oral disintegrating tablet (ODT) platforms induce active pharmaceutical ingredient (API) degrad...
journal_title:AAPS PharmSciTech
pub_type: 杂志文章
doi:10.1208/s12249-013-0015-5
更新日期:2013-12-01 00:00:00
abstract::The current study aimed to develop a prolonged-release pramipexole (PPX) transdermal patch for the treatment of Parkinson's disease. Permeation parameters of PPX were investigated using human cadaver skin. Pramipexole patches were prepared using DURO-TAK® pressure-sensitive-adhesive (PSA) and evaluated for drug stabil...
journal_title:AAPS PharmSciTech
pub_type: 杂志文章
doi:10.1208/s12249-016-0555-6
更新日期:2017-04-01 00:00:00
abstract::This work presents a new user-friendly lyophilization simulation and process optimization tool, freely available under the name LyoPRONTO. This tool comprises freezing and primary drying calculators, a design-space generator, and a primary drying optimizer. The freezing calculator performs 0D lumped capacitance modeli...
journal_title:AAPS PharmSciTech
pub_type: 杂志文章
doi:10.1208/s12249-019-1532-7
更新日期:2019-10-31 00:00:00
abstract::The topical application of all-trans retinoic acid (ATRA) is an effective treatment for several skin disorders, including photo-aging. Unfortunately, ATRA is susceptible to light, heat, and oxidizing agents. Thus, this study aimed to investigate the ability of polymeric micelles prepared from polyethylene glycol conju...
journal_title:AAPS PharmSciTech
pub_type: 杂志文章
doi:10.1208/s12249-011-9749-0
更新日期:2012-03-01 00:00:00
abstract::A near-infrared (NIR) spectroscopic method to determine content uniformity of a large, thick tablet using an approach that could facilitate future validations has been developed. A CT ibuprofen 800-mg tablet weighs about 1150 mg and is about 18.6 mm wide and 7.6 mm thick. The FT NIR spectrometer was optimized for tran...
journal_title:AAPS PharmSciTech
pub_type: 杂志文章
doi:10.1208/pt020311
更新日期:2001-07-12 00:00:00
abstract::As a synthetic clay material, laponite RDS (LR) was investigated as an effective drug carrier as a result of the special nanodisk structure together with the negative-charged surface to achieve enhanced cellular uptake and targeted delivery. In this research work, the synthesized oligomeric hyaluronic acid-aminophenyl...
journal_title:AAPS PharmSciTech
pub_type: 杂志文章
doi:10.1208/s12249-019-1533-6
更新日期:2019-11-20 00:00:00
abstract::This study examined the mechanical (hardness, compressibility, adhesiveness, and cohesiveness) and rheological (zero-rate viscosity and thixotropy) properties of polyethylene glycol (PEG) gels that contain different ratios of Carbopol 934P (CP) and polyvinylpyrrolidone K90 (PVP). Mechanical properties were examined us...
journal_title:AAPS PharmSciTech
pub_type: 杂志文章
doi:10.1208/pt010324
更新日期:2000-08-17 00:00:00
abstract::The second author's name was incorrectly published as "Niha F. Younes". The correct name is "Nihal Farid Younes" as shown above in the list of authors. ...
journal_title:AAPS PharmSciTech
pub_type: 已发布勘误
doi:10.1208/s12249-019-1321-3
更新日期:2019-02-25 00:00:00
abstract::Successful pellet production has been reported in literature with cross-linked poly(vinylpyrrolidone), Polyplasdone® XL-10 and INF-10. In the present study, a quality by experimental design approach was used to assess several formulation and process parameter effects on the characteristics of Polyplasdone® XL-10 pelle...
journal_title:AAPS PharmSciTech
pub_type: 杂志文章
doi:10.1208/s12249-015-0345-6
更新日期:2016-04-01 00:00:00
abstract::The objective of the current study was to develop an amorphous solid dispersion for a high melting point compound, griseofulvin (GRF), with an enhanced solubility and a controlled release pattern utilizing hot melt extrusion (HME) technology. Hypromellose acetate succinate (HPMCAS, Shin-Etsu AQOAT®, medium particle si...
journal_title:AAPS PharmSciTech
pub_type: 杂志文章
doi:10.1208/s12249-017-0846-6
更新日期:2018-01-01 00:00:00
abstract::The use of amorphous solid dispersions to improve the bioavailability of active ingredients from the BCS II and IV classifications continues to gain interest in the pharmaceutical industry. Over the last decade, methods for generating amorphous solid dispersions have been well established in commercially available pro...
journal_title:AAPS PharmSciTech
pub_type: 杂志文章,评审
doi:10.1208/s12249-017-0861-7
更新日期:2018-07-01 00:00:00
abstract::The paper introduces evaluation methodologies and associated statistical approaches for process validation lifecycle Stage 3A. The assessment tools proposed can be applied to newly developed and launched small molecule as well as bio-pharma products, where substantial process and product knowledge has been gathered. T...
journal_title:AAPS PharmSciTech
pub_type: 杂志文章,评审
doi:10.1208/s12249-016-0641-9
更新日期:2017-07-01 00:00:00
abstract::The primary objective of this study was to evaluate the effect of drug loading on the release of leuprolide acetate from an injectable polymeric implant, formed in situ, and efficacy of the released drug in suppressing serum testosterone levels in dogs for at least 90 days. An additional objective was to compare the o...
journal_title:AAPS PharmSciTech
pub_type: 杂志文章
doi:10.1208/pt010101
更新日期:2000-02-28 00:00:00
abstract::The effects of solvent [acetonitrile, methanol, and acetonitrile/water mixture (20:80, v/v)], buffer concentration (phosphate buffer, pH 7.5), ionic strength and commonly employed adjuvants on the photodegradation of betamethasone-17 valerate in cream and gel formulations have been studied on exposure to UV light (300...
journal_title:AAPS PharmSciTech
pub_type: 杂志文章
doi:10.1208/s12249-012-9902-4
更新日期:2013-03-01 00:00:00
abstract::To enhance the stability of coenzyme Q10 (CoQ10), Kolliphor® HS 15 (HS15) was employed as a carrier to build up a stable CoQ10-loaded micelle delivery system. The impact of micellar compositions, the preparation condition, and the preparation method on size characteristics, the solubilization efficiency, and micellar ...
journal_title:AAPS PharmSciTech
pub_type: 杂志文章
doi:10.1208/s12249-015-0399-5
更新日期:2016-06-01 00:00:00
abstract::Individualized medicines for pediatrics are a useful alternative if there is no correct dosage marketed for this segment (easy to swallow, adequate volume and content, correct composition for pediatrics, good organoleptic properties, etc.). Its validation process must ensure quality testing: its content uniformity, ph...
journal_title:AAPS PharmSciTech
pub_type: 杂志文章
doi:10.1208/s12249-019-1432-x
更新日期:2019-06-03 00:00:00
abstract::The ability to produce submicron particles of monoclonal antibodies of different sizes and shapes would enhance their application to pulmonary delivery. Although non-ionic surfactants are widely used as stabilizers in protein formulations, we hypothesized that non-ionic surfactants will affect the shape and size of su...
journal_title:AAPS PharmSciTech
pub_type: 杂志文章
doi:10.1208/s12249-012-9913-1
更新日期:2013-03-01 00:00:00