Abstract:
:Bupivacaine lipid microparticles were prepared and evaluated as a parenteral sustained-release dosage form for postoperative pain management. Bupivacaine free base was incorporated into a molten tristearin matrix and lipid micro-particles were subsequently formed from this molten mixture by a spray-congealing process. A 3% injectable bupivacaine lipid microparticle suspension was prepared by dispersing 30% bupivacaine lipid microparticles in an aqueous medium containing carboxymethylcellulose (CMC), mannitol, and Tween 80. Upon room temperature storage, the fluid suspension gradually changed into a nonflowing semisolid (gelation) as a result of crystal growth of bupivacaine. However, suspensions prepared with bupivacaine lipid microparticles that were previously annealed at an elevated temperature remained fluid upon long-term storage. Differential scanning calorimetry (DSC), x-ray powder diffraction (XRPD), and isoperibol solution calorimetry were used to investigate the changes in the solid-state properties of tristearin and bupivacaine in the lipid microparticles before and after the heat treatment. The DSC and XRPD results indicate that after 24 hours of heating at 40 degrees C, tristearin was completely converted from the unstable alpha form to the stable beta form. Using the isoperibol solution calorimetric method, bupivacaine was found to transform into a more stable form after the lipid microparticles were heated at 60 degrees C for 24 hours. The generation of the unstable solid forms of tristearin and bupivacaine was attributed to the resolidification of both components from the molten mixture during the spray-congealing process.
journal_name
Pharm Dev Technoljournal_title
Pharmaceutical development and technologyauthors
Li LC,Zhu L,Song JF,Deng JS,Bandopadhyay R,Wurster DEdoi
10.1081/pdt-54475subject
Has Abstractpub_date
2005-01-01 00:00:00pages
309-18issue
2eissn
1083-7450issn
1097-9867journal_volume
10pub_type
杂志文章abstract::Nucleic acids therapeutic efficiency is generally limited by their low stability and intracellular bioavailability, and by the toxicity of the carriers used to deliver them to the target sites. Aminated poly(glycerol methacrylate) polymers are biodegradable and pH-sensitive polymers that have been used previously to d...
journal_title:Pharmaceutical development and technology
pub_type: 杂志文章
doi:10.1080/10837450.2017.1312443
更新日期:2018-04-01 00:00:00
abstract::Aluminum hydroxide adjuvant was pretreated with six concentrations of potassium dihydrogen phosphate to produce a series of adjuvants with various degrees of phosphate substitution for surface hydroxyl. The adsorption of three phosphorylated proteins (alpha casein, dephosphorylated alpha casein, and ovalbumin) by the ...
journal_title:Pharmaceutical development and technology
pub_type: 杂志文章
doi:10.1081/pdt-120017526
更新日期:2003-01-01 00:00:00
abstract::In pediatrics, it is crucial to ameliorate the unpleasant taste of oral pharmaceutical formulations in order to facilitate patient compliance. Scientists' attempt to develop modern products for children is included among the new trends in pharmaceutical technology. Designing the preparation procedures and selecting th...
journal_title:Pharmaceutical development and technology
pub_type: 杂志文章
doi:10.1080/10837450.2019.1609499
更新日期:2020-01-01 00:00:00
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::The purpose of this study was to improve the sensitivity and accuracy of quantitative analysis of polymorphic mixtures. Various techniques such as hand grinding and mixing (in mortar and pestle), air jet milling and ball milling for micronization of particle and mixing were used to prepare binary mixtures. Using these...
journal_title:Pharmaceutical development and technology
pub_type: 杂志文章
doi:10.3109/10837450903286511
更新日期:2010-09-01 00:00:00
abstract::A carbopol 934P-based drug delivery system (AmDDS) was developed to achieve the dual-controlled delivery of Nonoxynol-9 (N-9), a spermicidal agent, and EDTA, a potentiator of spermicidal activity. This gel-type system made intimate contact with vaginal mucosa and maintained an effective drug concentration within the v...
journal_title:Pharmaceutical development and technology
pub_type: 杂志文章
doi:10.3109/10837459609029888
更新日期:1996-07-01 00:00:00
abstract::We have proposed a theory indicating the correlation between the dissolution rate and the heat of solution of drug substances. The initial dissolution rates of the drug substances containing amorphous were predicted accurately from their heats of solution. In this report, the possibility for the theory to estimate the...
journal_title:Pharmaceutical development and technology
pub_type: 杂志文章
doi:10.1081/pdt-120002234
更新日期:2002-01-01 00:00:00
abstract::The objective of the study was to develop a mathematical model for predicting the disintegration time of fast disintegrating tablets (FDTs) by estimating the powder characteristics of powder blend prior to compression. A combination of chitosan-alginate complex and glycine in the ratio of 50:50 was used for preparing ...
journal_title:Pharmaceutical development and technology
pub_type: 杂志文章
doi:10.3109/10837450903479996
更新日期:2011-02-01 00:00:00
abstract::Controlled release of a marker drug, 4,4'-bis(2-sulfostyryl) biphenyl (DSBP) from genipin crosslinked gelatin thin films, with application to drug delivery by transdermal patches is studied in this paper. A simple method for fabrication of nano-thin films, using basic lab equipment is introduced. This method consists ...
journal_title:Pharmaceutical development and technology
pub_type: 杂志文章
doi:10.1080/10837450802309679
更新日期:2008-01-01 00:00:00
abstract::Oily liquid drugs are not convenient for oral administration. We developed a powder containing clofibrate (CF), a model of an oily drug, using aminoalkyl methacrylate copolymer (EPO) or methacrylic acid copolymer (L100). CF or a mixture of CF and soybean oil was emulsified with EPO or L100 aqueous solution. Using a hi...
journal_title:Pharmaceutical development and technology
pub_type: 杂志文章
doi:10.3109/10837450.2015.1086370
更新日期:2016-12-01 00:00:00
abstract::The purpose of this work was to investigate the effect that changes in design and process variables had on the movement of particles around a fluidized bed coating apparatus. To measure the mean and variance of the particle cycle time distribution (CTD), the number of passages taken by a magnetic tracer particle throu...
journal_title:Pharmaceutical development and technology
pub_type: 杂志文章
doi:10.1081/pdt-100100546
更新日期:2000-01-01 00:00:00
abstract::Pulmonary delivery of peptides remains an important, noninvasive route of administration that is attractive because it offers high bioavailability and patient compliance. Optimization of particle characteristics for deposition in the deep regions of the lung after inhalation and retention of peptide stability are key ...
journal_title:Pharmaceutical development and technology
pub_type: 杂志文章
doi:10.3109/10837450.2015.1125924
更新日期:2017-09-01 00:00:00
abstract::Pharmaceutical aerosols have the potential to prevent pulmonary infectious diseases. Liposomal amphotericin B (LAMB, Ambisome, Astellas Pharma US, Deerfield, IL, USA) is approved as an intravenous infusion for empiric treatment of presumed fungal infections in neutropenic, febrile patients, as well as patients infecte...
journal_title:Pharmaceutical development and technology
pub_type: 杂志文章
doi:10.3109/10837450.2011.591803
更新日期:2011-11-01 00:00:00
abstract::In this study, we developed a one-step method to prepare ibuprofen fast- and sustained-release complex preparation. It was based on a double jets electrospinning process. Ibuprofen, a poorly water-soluble drug, was electrospun into fibers with polyvinyl pyrrolidone and hydroxypropyl methyl cellulose by two jets, respe...
journal_title:Pharmaceutical development and technology
pub_type: 杂志文章
doi:10.1080/10837450.2020.1728773
更新日期:2020-07-01 00:00:00
abstract::An osmotic-controlled pulsatile delivery technology was developed for targeted drug delivery. This novel system consists of a tablet core surrounded by an osmotic coating that has been mechanically compromised in strategic locations to facilitate reliable drug release at a given time point after administration. The ta...
journal_title:Pharmaceutical development and technology
pub_type: 杂志文章
doi:10.1080/10837450902838692
更新日期:2009-01-01 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 biopharmaceutical assessment of new drug candidates based on their chemical structure is important in drug discovery and development. The scope of this study is to focus on lipophilic drugs and to clarify the role of their chemical predictors on oral bioavailability in humans. First their chemical properties were ...
journal_title:Pharmaceutical development and technology
pub_type: 杂志文章
doi:10.1080/10837450802626296
更新日期:2009-01-01 00:00:00
abstract::The aim of this study was to investigate intravitreal injection of silk fibroin nanoparticles (SFNs) encapsulating bio-macromolecules, achieving enhanced drug bioavailability, and extended retention in retina. SFNs were prepared with regenerated silk fibroin using desolvation method with fluorescein isothiocyanate lab...
journal_title:Pharmaceutical development and technology
pub_type: 杂志文章
doi:10.1080/10837450.2018.1545236
更新日期:2019-06-01 00:00:00
abstract::Mefenamic acid (MA), a poorly water-soluble drug, was used as a model substance to investigate granules and tablet characteristics to be optimized for the loading volume of MA (0-74.1% v/v) in the formulation including lactose monohydrate/maize starch (7/3) as excipients. The compactibility of granules increased with ...
journal_title:Pharmaceutical development and technology
pub_type: 杂志文章
doi:10.1080/10837450701702941
更新日期:2008-01-01 00:00:00
abstract::The purpose of this work was to prepare and characterize Angiopep-2 functionalized ginsenoside-Rg3 loaded nanoparticles (ANG-Rg3-NP) and evaluate the therapeutic effect on C6 glioma cells. Nanoparticles were prepared by the emulsion solvent evaporation method. Angiopep-2 was functionalized to nanoparticles via a malei...
journal_title:Pharmaceutical development and technology
pub_type: 杂志文章
doi:10.1080/10837450.2018.1551901
更新日期:2020-03-01 00:00:00
abstract::In recent years, drug delivery systems such as liposomes and microparticles have been used in clinic for the treatment of different diseases and from a regulatory point of view, a parenterally applied drug and drug delivery systems must be sterile and pyrogen free. Radiation sterilization is a method recognized by pha...
journal_title:Pharmaceutical development and technology
pub_type: 杂志文章
doi:10.3109/10837450.2016.1163393
更新日期:2017-09-01 00:00:00
abstract::Vardenafil hydrochloride (VAR) is an erectile dysfunction treating drug. VAR has a short elimination half-life (4-5 h) and suffers low oral bioavailability (15%). This work aimed to explore the dual potential of VAR-dendrimer complexes as drug release modulators and oral bioavailability enhancers. VAR-dendrimer comple...
journal_title:Pharmaceutical development and technology
pub_type: 杂志文章
doi:10.1080/10837450.2018.1472611
更新日期:2019-03-01 00:00:00
abstract::The objective of this paper was to evaluate the mucoadhesive and sustained-release properties of the water-soluble gum obtained from Hakea gibbosa (hakea), for the formulation of buccal tablets. Flatfaced tablets containing hakea were formulated using chlorpheniramine maleate (CPM) as a model drug. Two types of tablet...
journal_title:Pharmaceutical development and technology
pub_type: 杂志文章
doi:10.1081/pdt-100101370
更新日期:1999-08-01 00:00:00
abstract::The objective of this study was to investigate the effect of the physiological parameters (pH, buffer capacity, and ionic strength) of the gastrointestinal (GI) fluid on the dissolution behavior of the class II weakly acidic (BCS class IIa) drug valsartan. A series of in vitro dissolution studies was carried out on Di...
journal_title:Pharmaceutical development and technology
pub_type: 杂志文章
doi:10.1080/10837450.2018.1536996
更新日期:2018-12-01 00:00:00
abstract::In the current study, the influence of chitosan on the dissolution rate and bioavailability of acyclovir has been illustrated through the preparation of co-crystals by simple solvent change method. Chitosan was precipitated on acyclovir crystals using sodium citrate as the salting out agent. The pure drug and the prep...
journal_title:Pharmaceutical development and technology
pub_type: 杂志文章
doi:10.3109/10837450.2011.595798
更新日期:2013-07-01 00:00:00
abstract::This study reports on the impact of cyclodextrin addition on the phase behavior of microemulsion systems. Three distinct oil-in-water microemulsions were formulated and subjected to increasing concentrations of various cyclodextrins. The prepared formulations underwent visual, textural and microscopic characterization...
journal_title:Pharmaceutical development and technology
pub_type: 杂志文章
doi:10.1080/10837450.2017.1371191
更新日期:2018-02-01 00:00:00
abstract::In this study, we designed a polymersome system for the controlled release of methotrexate (MTX) as an anticancer drug with the objective of improving the loading efficiency of the drug in polymersomes as well as achievement of an efficient control on the release rate of drug from nanocarriers. We synthesized mono met...
journal_title:Pharmaceutical development and technology
pub_type: 杂志文章
doi:10.1080/10837450.2018.1425433
更新日期:2019-01-01 00:00:00
abstract::The aim of the present investigation was to develop and study topical gel delivery of curcumin for its anti-inflammatory effects. Carbopol 934P (CRB) and hydroxypropylcellulose (HPC) were used for the preparation of gels. The penetration enhancing effect of menthol (0-12.5% w/w) on the percutaneous flux of curcumin th...
journal_title:Pharmaceutical development and technology
pub_type: 杂志文章
doi:10.1080/10837450802409438
更新日期:2009-01-01 00:00:00
abstract::Submicron colloidal suspensions of poly(epsilon-caprolactone) (PCL) were prepared by the solvent displacement method, using either the conventional form or a new recirculation device. In the latter case, a process that allows the recirculation of the aqueous phase into a device, providing a continuous flow, is propose...
journal_title:Pharmaceutical development and technology
pub_type: 杂志文章
doi:10.1080/10837450600940824
更新日期:2006-01-01 00:00:00
abstract::A novel analytical procedure has been developed for quantitative determination of levodopa and carbidopa in aqueous binary solutions acidified by HCl and without any other sample pretreatment. The method is based partially on least squares treatment of data obtained by attenuated total reflectance Fourier transform in...
journal_title:Pharmaceutical development and technology
pub_type: 杂志文章
doi:10.1080/10837450701481249
更新日期:2007-01-01 00:00:00