Abstract:
:Dual drug nanocrystals loaded nano embedded microparticles (DNEMs) were prepared for fixed dose combination of simvastatin (SIM) and ezetimibe (EZE) using NanoCrySP technology. The purpose was to generate nanonized SIM and EZE dispersed in matrix of single crystallization inducing excipient and investigate their in vitro performance. DNEM were prepared using mannitol (MAN) as crystallization inducer (active pharmaceutical ingredients (APIs)/MAN = 3:7 w/w) using spray drying. TPGS (0.1% w/v) was used as surfactant for stabilization of nanocrystals. Crystallinity of DNEM was confirmed by solid-state characterization using DSC and PXRD. Particle size analysis was carried out using Zetasizer® and the Scherrer equation as primary techniques and SEM and TEM as orthogonal techniques. Size of both SIM and EZE in DNEM was close to 600 nm. In vitro performance was assessed using USP apparatus II in 0.025% SLS containing sodium phosphate buffer. Powder dissolution of DNEM increased 1.45 times for SIM and 1.65 times for EZE as compared to their physical mixture in discriminatory medium. MAN did not plasticize SIM or EZE by virtue of its immiscibility with the two drugs. However, MAN helped in inducing crystallization via heterogeneous nucleation. The generated DNEM were stable in terms of assay, polymorphic form and dissolution for 90 days of accelerated storage at 40 °C/75% RH.
journal_name
Pharm Dev Technoljournal_title
Pharmaceutical development and technologyauthors
Nandi S,Kaur A,Bansal AKdoi
10.1080/10837450.2019.1669181subject
Has Abstractpub_date
2020-01-01 00:00:00pages
40-53issue
1eissn
1083-7450issn
1097-9867journal_volume
25pub_type
杂志文章abstract::Fixed dose combination (FDC) products are common in the treatment of hypertension, diabetes, human immunodeficiency virus, and tuberculosis. They make it possible to combine two or more drug molecules with different modes of pharmacological actions in a single dosing unit and optimize the treatment. From a patient per...
journal_title:Pharmaceutical development and technology
pub_type: 杂志文章,评审
doi:10.3109/10837450.2012.660699
更新日期:2013-11-01 00:00:00
abstract::In the present study, Simvastatin was incorporated in emulsion of soybean oil and propylene glycol monocaprylate as oily phase and Tween 80 and Cremophor EL as surfactants and also their mixtures. Dry adsorbed emulsions were prepared by using colloidal silicon dioxide in varying proportions to adsorb the liquid emulsi...
journal_title:Pharmaceutical development and technology
pub_type: 杂志文章
doi:10.1080/10837450701557246
更新日期:2007-01-01 00:00:00
abstract:CONTEXT:Bioadhesiviness of polyacrylic acid polymers make them promising hydrogels to design topical drug delivery systems, allowing a close contact with biological substrate as well as an enhanced local concentration gradient, both factors that may improve the biological performance of the drugs. AIM:Texture and bioa...
journal_title:Pharmaceutical development and technology
pub_type: 杂志文章
doi:10.3109/10837450.2014.882941
更新日期:2015-06-01 00:00:00
abstract::The purpose of this paper is to reject or to confirm the hypothesis that the influence of the water addition rate on the size and size distribution of pellets is caused by insufficient spreading of the added water at higher water addition rates. To overcome insufficient spreading of the added water, the agitation in t...
journal_title:Pharmaceutical development and technology
pub_type: 杂志文章
doi:10.3109/10837459609031431
更新日期:1996-12-01 00:00:00
abstract::Starches obtained from four different Dioscorea species namely White (D. rotundata), Bitter (D. dumetorum), Chinese (D. oppositifolia) and Water yam (D. alata), were modified by acid hydrolysis and the physicochemical, material and tablet formation properties of the starches were investigated with the aim of determini...
journal_title:Pharmaceutical development and technology
pub_type: 杂志文章
doi:10.1080/10837450802572367
更新日期:2009-01-01 00:00:00
abstract::The purpose of this study was to assess the usefulness of waxy corn (maize) starch as a cofiller and diluent in pellets produced by aqueous extrusion-spheronization. Waxy corn starch was combined with microcrystalline cellulose (MCC) in the range of 20-50% of the entire composition. Pellets containing ordinary corn st...
journal_title:Pharmaceutical development and technology
pub_type: 杂志文章
doi:10.1081/pdt-100100521
更新日期:2000-01-01 00:00:00
abstract::There is as yet no commercialized preparation for oral administration of flecainide acetate (FA) to children. In such cases, manipulation of commercial tablets is the usual practice in pharmacy services of hospitals and compounding pharmacies, to provide a suitable dosage form for this vulnerable pediatric population ...
journal_title:Pharmaceutical development and technology
pub_type: 杂志文章
doi:10.1080/10837450.2016.1238484
更新日期:2018-12-01 00:00:00
abstract::This study examines the influence of off-bottom clearance on size and size distribution of pellets produced during melt pelletization at different postmelt impeller speeds and binder concentrations using lactose and polyethylene glycol. Melt pelletization of lactose powder 450 M in an 8-liter highshear mixer, the floo...
journal_title:Pharmaceutical development and technology
pub_type: 杂志文章
doi:10.1080/10837459908984221
更新日期:1999-01-01 00:00:00
abstract::The main purpose of this work was to develop a supersaturatable self-microemulsifying drug delivery system (S-SMEDDS) of carbamazepine (CBZ). S-SMEDDS of CBZ was prepared and drug precipitation behavior, dissolution rate in vitro and particle size distribution were evaluated. The relative bioavailability of S-SMEDDS f...
journal_title:Pharmaceutical development and technology
pub_type: 杂志文章
doi:10.3109/10837451003774419
更新日期:2011-08-01 00:00:00
abstract::The aim of this work is to evaluate the feasibility of hydrophilic silica aerogels as drug carriers and to investigate the influence of the aerogels properties on the release rate of poorly water-soluble drugs. Hydrophilic silica aerogels of different densities were loaded with two model drugs, ketoprofen and griseofu...
journal_title:Pharmaceutical development and technology
pub_type: 杂志文章
doi:10.1081/pdt-200035804
更新日期:2004-11-01 00:00:00
abstract::In this study, chlorhexidine-loaded poly(ε-caprolactone) nanospheres (CHX-NS) were prepared and successfully coated on the urinary catheters. Properties of CHX-NS were evaluated including drug loading content and the nanosphere size. Effects of different lyoprotectants for long-term storage of CHX-NS were also investi...
journal_title:Pharmaceutical development and technology
pub_type: 杂志文章
doi:10.1080/10837450.2018.1502317
更新日期:2019-04-01 00:00:00
abstract::The unstirred aqueous boundary layer (ABL) thickness was determined for modified Franz diffusion cells using three test compounds--parathion, 4-hexylresorcinol, and 2,4-dinitrochlorobenzene (DNCB). Steady-state fluxes through one, two, and three dialysis membranes in series were achieved in donor-saturated, infinite-d...
journal_title:Pharmaceutical development and technology
pub_type: 杂志文章
doi:10.3109/10837450.2011.572895
更新日期:2012-11-01 00:00:00
abstract::In the current study, we demonstrate a structured approach to downstream process development for spray dried amorphous solid dispersions. Direct compression is generally not suitable due to typically poor flow of spray dried powders in tablets. Roller compaction (RC) is therefore the method of choice to enable spray d...
journal_title:Pharmaceutical development and technology
pub_type: 杂志文章
doi:10.1080/10837450.2020.1863985
更新日期:2021-01-04 00:00:00
abstract::The purpose of this study was to investigate the effect of the composition of a binary powder mixture on the bonding index, the brittle fracture index, and the strain index, as defined by Hiestand. The studies involved tensile strength and dynamic indentation hardness determinations of square compacts, the solid fract...
journal_title:Pharmaceutical development and technology
pub_type: 杂志文章
doi:10.3109/10837459709022630
更新日期:1997-11-01 00:00:00
abstract::A colchicine release system utilizing biodegradable poly(phosphazenes) was investigated in vitro for intra-articular administration. Polymer degradation and drug release studies were performed on colchicine-loaded poly(phosphazenes) containing either imidazolyl (I-PPHOS) or ethyl glycinato (EG-PPHOS) side chain substi...
journal_title:Pharmaceutical development and technology
pub_type: 杂志文章
doi:10.3109/10837459809028479
更新日期:1998-02-01 00:00:00
abstract::Effects of various factors, such as light intensity, polarizability of n-alcohol solvents, addition of colorants, and viscosity of solutions on the kinetics of the photoisomerization of therapeutically effective E-isomer of sorivudine to its less effective Z-isomer were studied. Solutions of known concentrations of E-...
journal_title:Pharmaceutical development and technology
pub_type: 杂志文章
doi:10.1081/pdt-100000047
更新日期:2001-01-01 00:00:00
abstract::The aim of this work is development of a nontoxic, long-term stable solid lipid nanoparticles (SLN) formulation for the loading of Nimesulide (NiM) by a 22 factorial design. The optimized formulation was composed of 10 wt% of glyceryl behenate and 2.5 wt% of poloxamer 188. Immediately after production, Z-Ave of NiM-SL...
journal_title:Pharmaceutical development and technology
pub_type: 杂志文章
doi:10.1080/10837450.2018.1549075
更新日期:2019-06-01 00:00:00
abstract::The present study reports the solid-state properties of Fluvastatin sodium salt crystallized from different solvents for comparison with crystalline forms of the commercially available raw material and United States Pharmacopeia (USP) reference standard. Fluvastatin (FLV) samples were characterized by several techniqu...
journal_title:Pharmaceutical development and technology
pub_type: 杂志文章
doi:10.3109/10837450.2012.727000
更新日期:2013-03-01 00:00:00
abstract::Two types of casein hydrolysates, casein A (mean peptide length 3.3) and casein B (mean peptide length 17.4) were prepared by the enzymatic hydrolysis of casein, and their effects on in vitro dissolution rates and oral bioavailability of drugs were evaluated. The in vitro dissolution behavior of the kneaded mixture of...
journal_title:Pharmaceutical development and technology
pub_type: 杂志文章
doi:10.3109/10837459809028499
更新日期:1998-05-01 00:00:00
abstract::The taste of oral dosage forms is an important argument regarding patient's compliance and acceptability. For this reason, it is often necessary to mask an undesirable and unpleasant taste of an active pharmaceutical ingredient. The purpose of this study was to mask the taste of naproxen sodium by a new fluid-bed coat...
journal_title:Pharmaceutical development and technology
pub_type: 杂志文章
doi:10.3109/10837450.2012.757784
更新日期:2014-03-01 00:00:00
abstract::The present study was aimed to optimize capsulated unfolding type gastroretentive bilayer film constituting immediate release (IR) layer of amlodipine besylate and sustained release (SR) layer of atorvastatin calcium. A three-factor, three-level Box-Behnken-design was used to optimize bilayer film with dual-release ch...
journal_title:Pharmaceutical development and technology
pub_type: 杂志文章
doi:10.1080/10837450.2019.1705486
更新日期:2020-04-01 00:00:00
abstract:INTRODUCTION:Theoretical models of the freeze-drying process are potentially useful to guide the design of a freeze-drying process as well as to obtain information not readily accessible by direct experimentation, such as moisture distribution and glass transition temperature, Tg, within a vial during processing. Previ...
journal_title:Pharmaceutical development and technology
pub_type: 杂志文章
doi:10.1081/pdt-35869
更新日期:2005-01-01 00:00:00
abstract::This study investigates the physicochemical properties of glycyl-histidyl-lysine-copper (GHK-Cu) to support the development of a formulation for effective topical delivery. The solubility and distribution coefficients (log D) were investigated using conventional methods and GHK concentrations were quantified with a va...
journal_title:Pharmaceutical development and technology
pub_type: 杂志文章
doi:10.3109/10837450.2014.979944
更新日期:2016-03-01 00:00:00
abstract::Owing to its limited aqueous solubility, Phytomenadione (vitamin K) undergoes a low bioavailability (50%) with a large inter-individual variability after oral administration. Therefore, the aim of this work was to incorporate vitamin K into nanostructure lipid carrier systems to improve its aqueous solubility and bioa...
journal_title:Pharmaceutical development and technology
pub_type: 杂志文章
doi:10.1080/10837450.2017.1312440
更新日期:2018-04-01 00:00:00
abstract::Novel fast-disintegrating multi-unit tablets (FDMUTs) were prepared to modify the release of lornoxicam (a potent non-steroidal anti-inflammatory drug with a short half-life) as well as to combine the advantages of multi-unit systems with the cost-effectiveness of compressed tablets. The proposed FDMUTs consisted of s...
journal_title:Pharmaceutical development and technology
pub_type: 杂志文章
doi:10.3109/10837451003692595
更新日期:2011-08-01 00:00:00
abstract::The aim of the present work was the development of vaginal sponge-like dressings based on chitosan ascorbate (CS) and on hyaluronic acid sodium salt/lysine acetate (HAS) combination. Sponge-like dressings were prepared by freeze-drying and characterized for mechanical resistance and mucoadhesion. CS dressings show hig...
journal_title:Pharmaceutical development and technology
pub_type: 杂志文章
doi:10.3109/10837450.2010.531736
更新日期:2012-03-01 00:00:00
abstract::The objective of the present investigation was to enhance skin permeation of diclofenac using water-in-oil microemulsion and to elucidate its skin permeation mechanism. The w/o microemulsion formulations were selected based on constructed pseudoternary phase diagrams depending on water solubilization capacity and ther...
journal_title:Pharmaceutical development and technology
pub_type: 杂志文章
doi:10.3109/10837450.2013.788658
更新日期:2014-05-01 00:00:00
abstract::The dry coating process was evaluated in terms of storage stability investigating drug release and agglomeration tendency of the different coated oral dosage forms; hydroxypropyl methylcellulose acetate succinate (HPMCAS) was used with triethylcitrate (TEC) as plasticizer and acetylated monoglyceride (Myvacet) as wett...
journal_title:Pharmaceutical development and technology
pub_type: 杂志文章
doi:10.3109/10837450902882336
更新日期:2009-01-01 00:00:00
abstract::A prototype parenteral manufacturing facility based on isolation technology was designed, constructed, and commissioned at Warner-Lambert Co., Morris Plains, NJ, with emphasis on its application to research and development (R&D) settings. The facility contains closed isolators for holding, transferring, and manufactur...
journal_title:Pharmaceutical development and technology
pub_type: 杂志文章
doi:10.1081/pdt-100102034
更新日期:2000-01-01 00:00:00
abstract::New microspheres containing hydrophilic core and hydrophobic coating as a controlled-release system with no toxic reagents were proposed. Water in oil in water (W/O/W) emulsion and solvent evaporation methods were used to make chitosan/ cellulose acetate (CCA) microspheres sized 200 - 400 microm. Ranitidine hydrochlor...
journal_title:Pharmaceutical development and technology
pub_type: 杂志文章
doi:10.1081/pdt-54421
更新日期:2005-01-01 00:00:00