Abstract:
:Spironolactone is a drug derived from sterols that exhibits an incomplete oral absorption due to its low water solubility and slow dissolution rate. In this study, formulations of spironolactone with four disintegrants named as croscarmellose sodium, crospovidone, sodium starch glycolate and microcrystalline cellulose II (MCCII) were conducted. The effect of those disintegrants on the tensile strength, disintegration time and dissolution rate of spironolactone-based compacts was evaluated using a factorial design with three categorical factors (filler, lubricant, and disintegrant). The swelling values, water uptake and water sorption studies of these disintegrants all suggested that MCCII compacts disintegrate by a wicking mechanism similar to that of crospovidone, whereas a swelling mechanism was dominant for sodium starch glycolate and croscarmellose sodium. The disintegration time of MCCII and sodium starch glycolate remained unchanged with magnesium stearate. However, this lubricant delayed the disintegration time of crospovidone and croscarmellose sodium. MCCII presented the fastest disintegration time independent of the medium and lubricant employed. The water sorption ratio and swelling values determined sodium starch glycolate followed by croscarmellose sodium as the largest swelling materials, whereas crospovidone and MCCII where the least swelling disintegrants. The swelling property of sodium starch glycolate and croscarmellose sodium was strongly affected by the medium pH. The disintegration time of spironolactone compacts was faster when starch was used as a filler due to the formation of soft compacts. In this case, the type of filler employed rather than the disintegrant had a major effect on the disintegration and dissolution times of spironolactone.
journal_name
AAPS PharmSciTechjournal_title
AAPS PharmSciTechauthors
Rojas J,Guisao S,Ruge Vdoi
10.1208/s12249-012-9835-ysubject
Has Abstractpub_date
2012-12-01 00:00:00pages
1054-62issue
4issn
1530-9932journal_volume
13pub_type
杂志文章abstract::The aims of the current study were to develop and evaluate clindamycin palmitate hydrochloride (CPH) 3D-printed tablets (printlets) manufactured by selective laser sintering (SLS). Optimization of the formulation was performed by studying the effect of formulation and process factors on critical quality attributes of ...
journal_title:AAPS PharmSciTech
pub_type: 杂志文章
doi:10.1208/s12249-020-01775-0
更新日期:2020-08-13 00:00:00
abstract::The aim of this study was to investigate the effects of a type of hydrophobic moiety, extent of N-substitution (ES), and degree of quaternization (DQ) of chitosan (CS) on the transepithelial electrical resistance and permeability of Caco-2 cells monolayer, using fluorescein isothiocyanate dextran 4,400 (FD-4) as the m...
journal_title:AAPS PharmSciTech
pub_type: 杂志文章
doi:10.1208/s12249-010-9399-7
更新日期:2010-06-01 00:00:00
abstract::Hard capsules are made from gelatin, an organic polymer obtained through the hydrolysis of collagen present in animal tissues. Gelatin can be degraded by microorganisms and some strategies can be used to control contaminating micro-organisms. Gamma irradiation is considered as an effective sterilization method; howeve...
journal_title:AAPS PharmSciTech
pub_type: 杂志文章
doi:10.1208/s12249-019-1394-z
更新日期:2019-05-20 00:00:00
abstract::A novel polymer-drug conjugate, polyethylene glycol-N-(acetyl)-glucosamine-doxorubicin (PEG-NAG-DOX) was evaluated in this study for its in vivo potential for treatment of tumours demonstrating improved efficacy and reduced toxicity. The proposed polymer-drug conjugate comprised of polyethylene glycol-maleimide (mPEG-...
journal_title:AAPS PharmSciTech
pub_type: 杂志文章
doi:10.1208/s12249-017-0787-0
更新日期:2017-11-01 00:00:00
abstract::Colorectal cancer is a global concern, and its treatment is fraught with non-selective effects including adverse side effects requiring hospital visits and palliative care. A relatively safe drug formulated in a bioavailability enhancing and targeting delivery platform will be of significance. Metformin-loaded solid l...
journal_title:AAPS PharmSciTech
pub_type: 杂志文章
doi:10.1208/s12249-016-0505-3
更新日期:2017-02-01 00:00:00
abstract::A simple but novel mixed surfactant system was designed to fabricate a self-nanoemulsifying drug delivery system (SNEDDS) based on hydrophilic-lipophilic balance (HLB) value. The impacts of HLB and molecular structure of surfactants on the formation of SNEDDS were investigated. After screening various oils and surfact...
journal_title:AAPS PharmSciTech
pub_type: 杂志文章
doi:10.1208/s12249-014-0078-y
更新日期:2014-04-01 00:00:00
abstract::The purpose of this research was to evaluate a new wireless and battery-free sensor technology for invasive product temperature measurement during freeze-drying. Product temperature is the most critical process parameter in a freeze-drying process, in particular during primary drying. The product temperature over time...
journal_title:AAPS PharmSciTech
pub_type: 杂志文章
doi:10.1208/s12249-008-9099-8
更新日期:2008-01-01 00:00:00
abstract::Present investigation deals with formulation and evaluation of tamoxifen (TMX)-loaded liquid crystalline nanoparticles (TMX-LCNPs) for improving oral bioavailability and safety of the existing treatment. Hexagonal Glyceryl monooleate-based TMX-LCNPs (GLCNPs) and Phytantriol-based TMX-LCNPs (PLCNPs) were prepared by di...
journal_title:AAPS PharmSciTech
pub_type: 杂志文章
doi:10.1208/s12249-017-0851-9
更新日期:2018-01-01 00:00:00
abstract::Solid dispersion is one of the most effective ways to improve the dissolution of insoluble drugs. When the carrier can highly disperse the drug, it will increase the wettability of the drug and reduce the surface tension, thus improving the solubility, dissolution, and bioavailability. However, amorphous solid dispers...
journal_title:AAPS PharmSciTech
pub_type: 杂志文章
doi:10.1208/s12249-020-01802-0
更新日期:2020-09-25 00:00:00
abstract::A folic acid-conjugated paclitaxel (PTX)-doxorubicin (DOX)-loaded nanostructured lipid carrier(s) (FA-PTX-DOX NLCs) were prepared by using emulsion-evaporation method and extensively characterized for particle size, polydispersity index, zeta potential, and % entrapment efficiency which were found to be 196 ± 2.5 nm, ...
journal_title:AAPS PharmSciTech
pub_type: 杂志文章
doi:10.1208/s12249-018-1185-y
更新日期:2018-11-01 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::Multidrug resistance is the major problem in cancer treatment nowadays. Compounds from plants are the new targets to solve this problem. Quercetin (QCT), quercetrin (QTR), and rutin (RUT) are potential anticancer flavonoids but their poor water solubility leads to less efficacy. In this study, the polymeric micelles o...
journal_title:AAPS PharmSciTech
pub_type: 杂志文章
doi:10.1208/s12249-020-01657-5
更新日期:2020-04-26 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::High inter- and intra-individual variability in the pH of fluids in the human gastrointestinal (GI) tract has been described in the literature. The aim of this study was to assess the influence of physiological variability in fasted pH profiles of media along the GI tract on diclofenac sodium (DF-Na) dissolution from ...
journal_title:AAPS PharmSciTech
pub_type: 杂志文章
doi:10.1208/s12249-018-1140-y
更新日期:2018-10-01 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::The effect of storage condition (% RH) on flufenamic acid:nicotinamide (FFA:NIC) cocrystal compressibility, compactibility, and tabletability profiles was not observed after visual evaluation or linear regression analysis. However, multivariate statistical analysis showed that storage condition had a significant effec...
journal_title:AAPS PharmSciTech
pub_type: 杂志文章
doi:10.1208/s12249-020-01712-1
更新日期:2020-07-07 00:00:00
abstract::The purpose of this study was to prepare ginkgolide B (GB) lyophilized powder for injection with excellent appearance and stable quality through a formulation screening and by optimizing the freeze-drying process. Cremophor EL as a solubilizer, PEG 400 as a latent solvent, and mannitol as an excipient were mixed to in...
journal_title:AAPS PharmSciTech
pub_type: 杂志文章
doi:10.1208/s12249-017-0858-2
更新日期:2018-02-01 00:00:00
abstract::The objective of the present study is to investigate the confounding effects, if any, of beta-cyclodextrins (βCDs) on corneal permeability coefficients obtained from in vitro transmembrane diffusion studies. Transcorneal permeability studies were carried out with 2-hydroxypropyl-beta-cyclodextrin (HPβCD) and randomly ...
journal_title:AAPS PharmSciTech
pub_type: 杂志文章
doi:10.1208/s12249-015-0315-z
更新日期:2015-10-01 00:00:00
abstract::The classically used nontargeted chemotherapeutic approach to pancreatic cancer has a dual drawback of suboptimal drug delivery at the target site and the systemic side effects produced by the unfettered exposure of the drug to healthy tissue. This study has the objective of developing novel poly(2-ethyl-2-oxazoline) ...
journal_title:AAPS PharmSciTech
pub_type: 杂志文章
doi:10.1208/s12249-020-01745-6
更新日期:2020-08-10 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::Amylin is a pancreatic hormone that plays important roles in overall metabolism and in glucose homeostasis. The therapeutic restoration of postprandial and basal amylin levels is highly desirable for patients with diabetes who need to avoid glucose excursions. Protein conjugation with polyethylene glycol (PEG) has lon...
journal_title:AAPS PharmSciTech
pub_type: 杂志文章
doi:10.1208/s12249-013-9987-4
更新日期:2013-09-01 00:00:00
abstract::Vemurafenib is a poorly soluble, low permeability drug that has a demonstrated need for a solubility-enhanced formulation. However, conventional approaches for amorphous solid dispersion production are challenging due to the physiochemical properties of the compound. A suitable and novel method for creating an amorpho...
journal_title:AAPS PharmSciTech
pub_type: 杂志文章
doi:10.1208/s12249-018-0988-1
更新日期:2018-07-01 00:00:00
abstract::A new, simple, inexpensive, and rapid 96-well plate UV spectrophotometric method was developed and validated for the quantification of compound 48/80 (C48/80) associated with particles. C48/80 was quantified at 570 nm after reaction with acetaldehyde and sodium nitroprusside in an alkaline solution (pH 9.6). The metho...
journal_title:AAPS PharmSciTech
pub_type: 杂志文章
doi:10.1208/s12249-013-9950-4
更新日期:2013-06-01 00:00:00
abstract::The purpose of this research was to use inline real-time near-infrared (NIR) to measure the moisture content of granules manufactured using a commercial production scale continuous twin-screw granulator fluid-bed dryer milling process. A central composite response surface statistical design was used to study the effec...
journal_title:AAPS PharmSciTech
pub_type: 杂志文章
doi:10.1208/s12249-011-9669-z
更新日期:2011-12-01 00:00:00
abstract::The exudates from the incised trunk of Terminalia randii has been evaluated as controlled release excipient in comparison with xanthan gum and hydroxypropylmethylcellulose (HPMC) using carvedilol (water insoluble) and theophylline (water soluble) as model drugs. Matrix tablets were prepared by direct compression and t...
journal_title:AAPS PharmSciTech
pub_type: 杂志文章
doi:10.1208/s12249-011-9712-0
更新日期:2012-03-01 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::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 corr...
journal_title:AAPS PharmSciTech
pub_type: 杂志文章
doi:10.1208/s12249-019-1544-3
更新日期:2019-10-24 00:00:00
abstract::This work examines the influence of various process parameters (like sodium alginate concentration, calcium chloride concentration, and hardening time) on papain entrapped in ionotropically cross-linked alginate beads for stability improvement and site-specific delivery to the small intestine using neural network mode...
journal_title:AAPS PharmSciTech
pub_type: 杂志文章
doi:10.1208/pt060231
更新日期:2005-09-30 00:00:00
abstract::Our aim was to investigate the cellular uptake, in vitro cytotoxicity and bioavailability of ginsenoside-modified nanostructured lipid carrier loaded with curcumin (G-NLC). The formulation was prepared by melt emulsification technique, in which water was added to the melted lipids and homogenized to give a uniform sus...
journal_title:AAPS PharmSciTech
pub_type: 杂志文章
doi:10.1208/s12249-019-1295-1
更新日期:2019-01-23 00:00:00
abstract::In our previously studies, we confirmed that ergosterol could ameliorate diabetic nephropathy by suppressing the proliferation of mesangial cells and the accumulation of extracellular matrix (ECM). However, the therapeutic application of ergosterol may be confined due to poor aqueous solubility and low oral bioavailab...
journal_title:AAPS PharmSciTech
pub_type: 杂志文章
doi:10.1208/s12249-019-1597-3
更新日期:2020-01-13 00:00:00