Abstract:
:An F(ab')2 fragment of an IgG has been spray-dried on a bench-top machine to examine the presence of insoluble particulates in the redissolved powder product. Preliminary experiments showed that treatment of the F(ab')2 in aqueous solution in a water bath at 65°C for 1 h produced fragmentation and also insoluble particulates, but no alteration in soluble aggregates. On spray drying, there was, however, no fragmentation but rather formation of soluble aggregates and insoluble particulates. There is therefore a strong difference between isothermal heat-induced damage in solution and during spray drying. The insoluble particulates were detected using a particle counter as a number distribution that was converted to a weight distribution. Addition of trehalose to the liquid feed strongly reduced the formation of the insoluble particulates, indicating that these are insoluble aggregates of the protein and not particulate contamination from the spray dryer. Trehalose (100 mM) was required to suppress formation of the insoluble aggregates, whereas 10 mM was sufficient to prevent formation of soluble aggregates. The particle counter and also isoelectric focusing gave consistent detection of the insoluble particles, whereas photon correlation spectroscopy gave inconsistent results. Spray-drying of small volumes of liquid feed on the bench-top scale can be performed without introducing nonproteinaceous insoluble particulates.
journal_name
J Pharm Scijournal_title
Journal of pharmaceutical sciencesauthors
Lassner P,Adler M,Lee Gdoi
10.1002/jps.23891subject
Has Abstractpub_date
2014-04-01 00:00:00pages
1021-31issue
4eissn
0022-3549issn
1520-6017pii
S0022-3549(15)30637-7journal_volume
103pub_type
杂志文章abstract::The degradation of batanopride hydrochloride, an investigational antiemetic drug, was studied in aqueous buffer solutions (pH 2-10; ionic strength, 0.5; 56 degrees C) in an attempt to improve drug stability for parenteral administration. Degradation occurs by two different mechanisms depending on the pH of the solutio...
journal_title:Journal of pharmaceutical sciences
pub_type: 杂志文章
doi:10.1002/jps.2600811109
更新日期:1992-11-01 00:00:00
abstract::Hydroxypropyl cellulose films were prepared by compression molding of three different lots of hydroxypropyl cellulose powder at 149 degrees C, 188 degrees C, and 232 degrees C. Rectangular pieces were cut from these films and viscosity average molecular weight (Mv), degree of orientation, and rate of dissolution were ...
journal_title:Journal of pharmaceutical sciences
pub_type: 杂志文章
doi:10.1002/jps.2600740509
更新日期:1985-05-01 00:00:00
abstract::An approach to analyzing and interpreting kinetic data from stability studies using factorial designs is presented. This may be useful for screening purposes or as an aid in identifying significant effects in complex systems. A typical 2n factorial experiment is discussed, and methods of variance estimation and statis...
journal_title:Journal of pharmaceutical sciences
pub_type: 杂志文章
doi:10.1002/jps.2600720410
更新日期:1983-04-01 00:00:00
abstract::Chloroquine (7-chloro-4-[[4-(diethylamino)-1-methylbutyl]amino]quinoline; CQ) accumulates in the insoluble fraction of rat muscle homogenates with an equilibrium distribution ratio of 7.8 L/kg. This is of a similar magnitude to muscle:plasma ratios observed in vivo. Uptake is approximately linear, even up to concentra...
journal_title:Journal of pharmaceutical sciences
pub_type: 杂志文章
doi:10.1002/jps.2600751109
更新日期:1986-11-01 00:00:00
abstract::Carbamazepine is the first-line anti-epileptic drug for focal seizures and generalized tonic-clonic seizures. Although sustained-release formulations exist, an initial burst of drug release is still present and this results in side effects. Zero-order release formulations reduce fluctuations in serum drug concentratio...
journal_title:Journal of pharmaceutical sciences
pub_type: 杂志文章
doi:10.1016/j.xphs.2016.04.031
更新日期:2016-07-01 00:00:00
abstract::Currently, conjunctivitis is treated by frequent high dose administration of sparfloxacin eye drop solution. However, the eye drops are inconvenient because of low bioavailability, short ocular drug residence time, and need of frequent instillation, which lead to patient noncompliance affecting the routine life style ...
journal_title:Journal of pharmaceutical sciences
pub_type: 杂志文章
doi:10.1016/j.xphs.2020.02.008
更新日期:2020-06-01 00:00:00
abstract::Metronidazole and four derivatives were studied in vitro to investigate the differences in the extent of their binding to plasma proteins. Modification at the terminal portion of the alkyl side chain resulted in wide differences in the extent of binding. Molecular orbital calculations were performed by the CNDO and MI...
journal_title:Journal of pharmaceutical sciences
pub_type: 杂志文章
doi:10.1002/jps.2600641111
更新日期:1975-11-01 00:00:00
abstract::Vehicle effects may be caused by thermodynamic effects and by specific (penetration enhancing) effects. To investigate the effects of various lipophilic vehicles on drug penetration, an in vivo permeability study was conducted with methyl nicotinate as the model drug. The drug was dissolved in the respective vehicles ...
journal_title:Journal of pharmaceutical sciences
pub_type: 临床试验,杂志文章
doi:10.1002/jps.2600840214
更新日期:1995-02-01 00:00:00
abstract::The present study was conducted to investigate the impact of drying method and formulation on the storage stability of IgG1. Formulations of IgG1 with varying levels of sucrose with and without surfactant were dried by different methods, namely freeze drying, spray drying, and foam drying. Dried powders were character...
journal_title:Journal of pharmaceutical sciences
pub_type: 杂志文章
doi:10.1002/jps.20859
更新日期:2007-08-01 00:00:00
abstract::Gas pycnometry is applied to determine the density of solid materials. The analysis of lyophilisates is particularly challenging because of their porous structure. In this study, the density of raw materials and freeze-dried products was determined using different pycnometric methodologies and gases [helium (He), nitr...
journal_title:Journal of pharmaceutical sciences
pub_type: 杂志文章
doi:10.1002/jps.23723
更新日期:2013-11-01 00:00:00
abstract::Recent murine studies found that rifapentine, dosed daily, at least halved tuberculosis treatment times compared with standard rifampicin and isoniazid-containing regimens. However, in humans, an inhalable form of rifapentine may be necessary to considerably shorten treatment duration because of the physiological barr...
journal_title:Journal of pharmaceutical sciences
pub_type: 杂志文章
doi:10.1002/jps.23911
更新日期:2014-05-01 00:00:00
abstract::Postabsorptive factors which can affect systemic drug exposure are assumed to be dependent on the active pharmaceutical ingredient (API), and thus independent of formulation. In contrast, preabsorptive factors, for example, hypochlorhydria, might affect systemic exposure in both an API and a formulation-dependent way....
journal_title:Journal of pharmaceutical sciences
pub_type: 杂志文章
doi:10.1016/j.xphs.2016.10.008
更新日期:2017-02-01 00:00:00
abstract::This in vitro study evaluated the extent of the absorption and metabolism of propranolol in human skin from four sources. Between 10.4 +/- 3.1 and 36.6 +/- 2.6% of the applied dose was absorbed; however, only a small portion (between 4.1 +/- 0.9 and 16.1 +/- 1.3%) of the dose permeated through the skin. Naphthoxyaceti...
journal_title:Journal of pharmaceutical sciences
pub_type: 杂志文章
doi:10.1002/jps.2600820802
更新日期:1993-08-01 00:00:00
abstract::The degradation kinetics of moricizine hydrochloride (1) were examined over a pH range of 0.6 to 6.0 at an ionic strength of 0.3 and 60 degrees C. The disappearance of intact 1 was followed by a stability-indicating HPLC assay. The degradation products, which had approximate solubilities of less than 100 micrograms/mL...
journal_title:Journal of pharmaceutical sciences
pub_type: 杂志文章
doi:10.1002/jps.2600810625
更新日期:1992-06-01 00:00:00
abstract::The development of multiple drug modalities over the past 20 years has dramatically expanded the therapeutic space for intervention in disease processes. Rather than being alternative therapeutic approaches, these modalities tend to be complimentary both in the scope of target space and the biological mechanisms harne...
journal_title:Journal of pharmaceutical sciences
pub_type: 杂志文章
doi:10.1016/j.xphs.2020.09.057
更新日期:2021-01-01 00:00:00
abstract::Preliminary studies indicate that it may be possible to differentiate the effects of a nephrotoxic substance from those of diuretic agents by the measurement of both urine and plasma osmolarity. The nephrotoxic substance, mercuric chloride, decreases urinary osmolality and increases plasma or serum osmolality. The diu...
journal_title:Journal of pharmaceutical sciences
pub_type: 杂志文章
doi:10.1002/jps.2600660411
更新日期:1977-04-01 00:00:00
abstract::Peptidomimetic drugs have favorable bioavailability owing to H(+)/peptide transporter 1 (PEPT1) located in the intestine. Sartans are commonly used and likely coadministered with peptidomimetic drugs in the clinic; however, in vivo interactions between sartans and peptidomimetic drugs have not been systemically unders...
journal_title:Journal of pharmaceutical sciences
pub_type: 杂志文章
doi:10.1002/jps.23805
更新日期:2014-02-01 00:00:00
abstract::The pharmacologically active compound (33% reduction in rabbit intraocular pressure recovery rate assay) 1-ethyl-6-fluoro-1,2,3,4-tetrahydroquinoline (MC4), which showed ocular hypotensive action and had optimum physicochemical properties, was characterized for its ocular absorption and distribution properties to bett...
journal_title:Journal of pharmaceutical sciences
pub_type: 杂志文章
doi:10.1002/jps.22720
更新日期:2011-12-01 00:00:00
abstract::A few 1,2-bis(N-alkylaminomethyl)indolizines, simple indolizinecarboxylic acids, and several 6-alkoxyindolizine-2-carboxylic acids were synthesized and screened as possible oral hypoglycemic agents. The absence of any significant hypoglycemic activity excludes these compounds from the predicted structural lead provide...
journal_title:Journal of pharmaceutical sciences
pub_type: 杂志文章
doi:
更新日期:1975-02-01 00:00:00
abstract::In this study, we explored the bioavailability in dogs and chemical potency of generic ritonavir and lopinavir/ritonavir tablet products manufactured by various pharmaceutical companies. Chemical potency of the products was examined by HPLC quantitation of ritonavir and lopinavir. Using a dog model, we determined poin...
journal_title:Journal of pharmaceutical sciences
pub_type: 杂志文章
doi:10.1002/jps.21712
更新日期:2010-02-01 00:00:00
abstract::Plasma and various organ concentrations of canrenone, canrenoate, and total 3H-activity were measured following single doses of 20 mg of 3H-canrenoate/kg iv to rabbits. Organs studied included heart, lungs, brain, kidneys, liver, adrenal glands, and spleen. Canrenoate was shown to be in rapid equilibrium with canrenon...
journal_title:Journal of pharmaceutical sciences
pub_type: 杂志文章
doi:10.1002/jps.2600660237
更新日期:1977-02-01 00:00:00
abstract::The effect of dimethyl sulfoxide, dimethyl formamide, and dimethyl acetamide on the basal stratum corneum of excised nude mouse skin was investigated. All of these dipolar aprotic solvents caused a swelling of the basal stratum corneum cells and a disruption of the normal keratin pattern. This behavior suggests that d...
journal_title:Journal of pharmaceutical sciences
pub_type: 杂志文章
doi:10.1002/jps.2600770106
更新日期:1988-01-01 00:00:00
abstract::Acetylcarnitine, a naturally occurring compound found in high concentration in heart and skeletal muscle of vertebrates, bears structural resemblance to acetylcholine, and studies have shown that it has slight cholinergic properties. Acetylcarnitine was subjected to conformational analysis by extended Hückel theory (E...
journal_title:Journal of pharmaceutical sciences
pub_type: 杂志文章
doi:10.1002/jps.2600690921
更新日期:1980-09-01 00:00:00
abstract::The synthesis, local anesthetic and antiarrhythmic properties, and CNS toxicity of 14 2-(3-alkylaminoalkylamido)-pyrroles are described. Most of the compounds exhibited local anesthetic activity by the guinea pig wheal test, with seven showing comparable or greater activity than lidocaine. Most compounds also exhibite...
journal_title:Journal of pharmaceutical sciences
pub_type: 杂志文章
doi:10.1002/jps.2600700519
更新日期:1981-05-01 00:00:00
abstract::Bioadhesive polymers that bind to the gastric mucin or epithelial cell surface are useful in drug delivery for the purposes of (a) retaining a dosage from in the GI tract and (b) increasing the intimacy and duration of contact of drug with the absorbing membrane. Polycarbophil has previously been shown to have bioadhe...
journal_title:Journal of pharmaceutical sciences
pub_type: 杂志文章
doi:10.1002/jps.2600740408
更新日期:1985-04-01 00:00:00
abstract::3D cultures of primary human hepatocytes (PHH) are emerging as a more in vivo-like culture system than previously available hepatic models. This work describes the characterisation of drug metabolism in 3D PHH spheroids. Spheroids were formed from three different donors of PHH and the expression and activities of impo...
journal_title:Journal of pharmaceutical sciences
pub_type: 杂志文章
doi:10.1016/j.xphs.2020.10.043
更新日期:2021-01-01 00:00:00
abstract::A GLC-mass spectrometric assay for methylphenidate in biological fluids was developed using the ethyl ester homolog of the drug as the internal standard. The procedure has a lower level of sensitivity of 1.2 ng/ml and is based on GLC-mass spectrometic monitoring of the m/e 180 ion common to the mass spectra of the N-t...
journal_title:Journal of pharmaceutical sciences
pub_type: 杂志文章
doi:10.1002/jps.2600660633
更新日期:1977-06-01 00:00:00
abstract::A single method for the quantitative determinations of three active ingredients, phenylephrine hydrochloride, phenylpropanolamine hydrochloride, and brompheniramine maleate, and one inactive ingredient (sodium benzoate) in a commercial product for colds is reported. The method is based on paired ion high-pressure liqu...
journal_title:Journal of pharmaceutical sciences
pub_type: 杂志文章
doi:10.1002/jps.2600670643
更新日期:1978-06-01 00:00:00
abstract::The inhibitory effect of dioctyl sodium sulfosuccinate of hog pepsin activity was investigated over the pH 1.5-3.0 range. The inhibitory effect was studied using a natural substrate, hemoglobin, and a synthetic substrate, N-acetyl-L-phenylalanyl-L-diiodotyrosine. The mechanistic studies revealed that a substrate-inhib...
journal_title:Journal of pharmaceutical sciences
pub_type: 杂志文章
doi:10.1002/jps.2600650914
更新日期:1976-09-01 00:00:00
abstract::The solvent-free melt electrospinning (MES) method was developed to prepare a drug delivery system with fast release of carvedilol (CAR), a drug with poor water solubility. To the authors knowledge, this is the first report for preparing drug-loaded melt electrospun fibers. Cationic methacrylate copolymer of Eudragit®...
journal_title:Journal of pharmaceutical sciences
pub_type: 杂志文章
doi:10.1002/jps.23374
更新日期:2013-02-01 00:00:00