Mechanisms of solvent evaporation encapsulation processes: prediction of solvent evaporation rate.

Abstract:

:The mechanism of organic solvent evaporation during microencapsulation and its role during microsphere hardening has been investigated. Evaporation and encapsulation studies were carried out in a jacketed beaker, filled with aqueous hardening solution, which was maintained at constant temperature and constant stirring rate in the turbulent regime. Evaporation of dissolved methylene chloride (MC), ethyl acetate (EA), and acetonitrile (ACN) was examined by the decline in organic solvent concentration in the hardening bath, which was monitored by gas chromatography. The evaporation from the bath followed first-order kinetics under dilute conditions (e.g., MC < 3 mg/mL), yielding an overall permeability coefficient, P. The value of P was theoretically related to the Kolmogorov length-scale of turbulence under conditions that favor liquid-side transport control. According to theory, factors that favored liquid-phase control (as opposed to gas-phase control) were those that favored a high Henry's law constant [i.e., elevated temperature near the normal boiling point (bp) of the organic solvent] and properties of the dissolved organic solvent (i.e., low normal bp and low aqueous solubility). These theoretical hypotheses were confirmed by (1) correlating the experimentally determined P with process variables raised to the appropriate power according to theory, r(2) = 0.95 (i.e., P approximately rotational speed, omega(3/4), impeller diameter, d (5/4), volume of hardening bath, V(-1/4), and the product of kinematic viscosity and diffusion coefficient, nu(-5/12)D (2/3)), and (2) illustrating that at constant temperature, the tendency of the evaporation system to obey liquid-side transport control follows the same order of increasing Henry's law constant (i.e., MC > EA > ACN). To establish the relationship of evaporation with microsphere hardening, the decline in MC concentration was determined in both the continuous and dispersed polymer phases during microencapsulation. By applying a mass balance with respect to MC in the hardening bath, the cumulative hardening profile of the microspheres was accurately predicted from the interpolating functions of the kinetics of MC loss from the bath with and without polymer added. These results have potential use for microsphere formulation, design of encapsulation apparatus, and scale up of microsphere production.

journal_name

J Pharm Sci

authors

Wang J,Schwendeman SP

subject

Has Abstract

pub_date

1999-10-01 00:00:00

pages

1090-9

issue

10

eissn

0022-3549

issn

1520-6017

pii

S0022-3549(15)50889-7

journal_volume

88

pub_type

杂志文章
  • Carrier-mediated transport systems for glucose in mucosal cells of the human oral cavity.

    abstract::The in vitro uptake study was performed using the isolated cells of human oral mucosa, buccal and the dorsum of the tongue, to investigate the mechanisms of glucose uptake. The uptake of D-glucose was much larger in cells of the dorsum of the tongue than in buccal cells and was inhibited more extensively by 2-deoxy-D-...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 临床试验,杂志文章

    doi:10.1021/js980298f

    authors: Oyama Y,Yamano H,Ohkuma A,Ogawara K,Higaki K,Kimura T

    更新日期:1999-08-01 00:00:00

  • Investigation of atypical dissolution behavior of an encapsulated amorphous solid dispersion.

    abstract::Poor dissolution performance is one of the challenges encountered in dosage form design of amorphous solid dispersions (ASDs). This study was aimed to investigate the effect of solid-liquid interactions of an encapsulated ASD on drug release. Drug release profiles of a molecularly interacting amorphous celecoxib solid...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章

    doi:10.1002/jps.22462

    authors: Puri V,Dantuluri AK,Bansal AK

    更新日期:2011-06-01 00:00:00

  • Study of morphology of reactive dissolution interface using fractal geometry.

    abstract::The determination of reactive fractal dimension was carried out using two forms of the Noyes-Whitney equation, -dQ/dt = K(Q/Q0)DR/3 and -dQ/dt = K'RDR-3 using the Richardson plot on the basis of previous data obtained by dissolution of an orthoboric acid powder. The correlation of the results provided by the two ways ...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章

    doi:10.1021/js960059x

    authors: Tromelin A,Gnanou JC,Andrès C,Pourcelot Y,Chaillot B

    更新日期:1996-09-01 00:00:00

  • A site-directed mutagenesis study of drug-binding selectivity in genetic variants of human alpha(1)-acid glycoprotein.

    abstract::Human alpha(1)-acid glycoprotein (AGP), a major carrier of many basic drugs in circulation, consists of at least two genetic variants, namely A and F1*S variant. Interestingly, the variants of AGP have different drug-binding properties. The purpose of this study was to identify the amino acid residues that are respons...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章

    doi:10.1002/jps.21697

    authors: Nishi K,Ueno M,Murakami Y,Fukunaga N,Akuta T,Kadowaki D,Watanabe H,Suenaga A,Maruyama T,Otagiri M

    更新日期:2009-11-01 00:00:00

  • Anticonvulsant activity of some 4-methoxy- and 4-chlorobenzanilides.

    abstract::A series of mono-, di-, and trimethylated derivatives of 4-chloro- and 4-methoxybenzanilide was synthesized and evaluated for anticonvulsant activity. This series was prepared in the course of studies designed to examine the relationship between anticonvulsant effects and benzamide structure. The compounds were tested...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章

    doi:10.1002/jps.2600790308

    authors: Clark CR,McMillian CL

    更新日期:1990-03-01 00:00:00

  • Effect of absorbents on water vapor transmission of free and applied polymer films.

    abstract::The influence of different types of absorbents on moisture transmission through free (cast films) and applied (coated tablets) polymer films was investigated. In free film studies, lubricated granulations were considered to be the absorbent. The compressed tablet was considered to be the absorbent in applied film stud...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章

    doi:10.1002/jps.2600650411

    authors: Amann AH

    更新日期:1976-04-01 00:00:00

  • In vitro adsorption studies of cimetidine.

    abstract::The adsorption of cimetidine on selected pharmaceuticals including kaolin, activated charcoal, talc, and nonsystemic antacids was determined at pH 5.0 and 25 degrees. The Langmuir and Freundlich adsorption isotherms showed that cimetidine adsorption was significant with activated charcoal, kaolin, talc, and magnesium ...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章

    doi:10.1002/jps.2600690329

    authors: Ganjian F,Cutie AJ,Jochsberger T

    更新日期:1980-03-01 00:00:00

  • Pharmacokinetic aspects of biotechnology products.

    abstract::In recent years, biotechnologically derived peptide and protein-based drugs have developed into mainstream therapeutic agents. Peptide and protein drugs now constitute a substantial portion of the compounds under preclinical and clinical development in the global pharmaceutical industry. Pharmacokinetic and exposure/r...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章,评审

    doi:10.1002/jps.20125

    authors: Tang L,Persky AM,Hochhaus G,Meibohm B

    更新日期:2004-09-01 00:00:00

  • Simultaneous determination of methyl, ethyl, propyl, and butyl 4-hydroxybenzoates and 4-hydroxybenzoic acid in liquid antacid formulations by gas chromatography.

    abstract::An isothermal chromatographic (GC) method employing an SE-30 column and flame-ionization detection has been developed for the simultaneous assay of methyl, ethyl, propyl, and butyl 4-hydroxybenzoates and 4-hydroxybenzoic acid in liquid antacid formulations. The method, which uses a silica column chromatographic cleanu...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章

    doi:10.1002/jps.2600730136

    authors: Schieffer GW,Palermo PJ,Pollard-Walker S

    更新日期:1984-01-01 00:00:00

  • Kinetics and mechanism of decomposition of N-chloroamino acids. II: conformationally restricted models.

    abstract::The kinetics of decomposition of the following conformationally restricted N-chloro-alpha-amino acids were studied: 1-amino-1-cyclopentanecarboxylic acid (2), 1-amino-1-cyclohexanecarboxylic acid (4), 2-amino-2-norbornanecarboxylic acid (6), and 2-amino-2-benzonorbornanecarboxylic acid (8). The first-order rate consta...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章

    doi:10.1002/jps.2600791216

    authors: Awad R,Hussain A,Crooks PA

    更新日期:1990-12-01 00:00:00

  • Dissolution rates of corticoid solutions dispersed on silicas.

    abstract::Two nonporous and three porous amorphous silicas were used as dispersion media to convert corticoid solutions into free-flowing powders. The corticoids (prednisone, prednisolone, and hydrocortisone) were dissolved in N,N-dimethylacetamide-polyethylene glycol 400 (7:3 v/v) and their 10% (w/v) solutions were mixed with ...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章

    doi:10.1002/jps.2600730330

    authors: Liao CC,Jarowski CI

    更新日期:1984-03-01 00:00:00

  • Adsorption of pepsin by aluminum hydroxide II: Pepsin inactivation.

    abstract::Pepsin adsorbed on gibbsite or boehmite, non-acid-reactive forms of aluminum hydroxide, had a significantly lower activity than pepsin in solution. IR and desorbed pepsin activity studies showed that the reduced activity of adsorbed pepsin was not due to denaturation of pepsin on adsorption. Steric occlusion of the ac...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章

    doi:10.1002/jps.2600731105

    authors: Sepelyak RJ,Feldkamp JR,Regnier FE,White JL,Hem SL

    更新日期:1984-11-01 00:00:00

  • Pharmacology of malnutrition III: binding of digoxin to normal and kwashiorkor serum.

    abstract::Digoxin binding to normal and kwashiorkor serum was studied and found to be inferior in the latter. Digoxin should be used with care in hypoalbuminemic patients. ...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章

    doi:10.1002/jps.2600650629

    authors: Buchanan N,Van der Walt LA,Strickwold B

    更新日期:1976-06-01 00:00:00

  • Vehicle effects in percutaneous absorption: in vitro study of influence of solvent power and microscopic viscosity of vehicle on benzocaine release from suspension hydrogels.

    abstract::The release through silicone rubber membranes of benzocaine suspended in carbomer hydrogels containing different concentrations of low molecular weight polysols (ethylene glycol, propylene glycol, glycerol, and sorbitol) was studied to establish general principles and procedures for control of the effects on percutane...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章

    doi:10.1002/jps.2600690406

    authors: Di Colo G,Carelli V,Giannaccini B,Serafini MF,Bottari F

    更新日期:1980-04-01 00:00:00

  • Dose-dependent plasma clearance of MK-826, a carbapenem antibiotic, arising from concentration-dependent plasma protein binding in rats and monkeys.

    abstract::After intravenous administration of MK-826, a new carbapenem antibiotic, the compound exhibited nonlinear pharmacokinetics in rats and monkeys. In both species, time-averaged plasma clearance (based on total concentrations) increased about 5-fold over the 10- to 180-mg/kg dose range. MK-826 was extensively plasma prot...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章

    doi:10.1021/js980232k

    authors: Wong BK,Bruhin PJ,Lin JH

    更新日期:1999-02-01 00:00:00

  • Degradation kinetics and isomerization of cefdinir, a new oral cephalosporin, in aqueous solution. 1.

    abstract::Hydrolytic degradation products of cefdinir were studied in acidic (pH 1), neutral (pH 6), and basic (pH 9) solutions. Seven major degradation products were isolated by preparative and/or high-performance liquid chromatography and characterized by UV, IR, 1H-NMR, and mass spectra. To clarify degradation pathways in ea...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章

    doi:10.1021/js950446r

    authors: Okamoto Y,Kiriyama K,Namiki Y,Matsushita J,Fujioka M,Yasuda T

    更新日期:1996-09-01 00:00:00

  • An investigation into the digestion of chitosan (noncrosslinked and crosslinked) by human colonic bacteria.

    abstract::Chitosan salts are being investigated as materials for bacterially triggered colonic drug delivery, via the oral route, based on the assumption that they will be degraded by the enzymes produced by the human colonic bacteria. The actual susceptibility of chitosan to these enzymes is, however, unclear. The digestion of...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章

    doi:10.1002/jps.21271

    authors: McConnell EL,Murdan S,Basit AW

    更新日期:2008-09-01 00:00:00

  • Ocular pharmacokinetics of a novel tetrahydroquinoline analog in rabbit: absorption, disposition, and non-compartmental analysis.

    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

    authors: Pamulapati CR,Schoenwald RD

    更新日期:2011-12-01 00:00:00

  • Isomeric benzoylpyrroleacetic acids: some structural aspects for aldose reductase inhibitory and anti-inflammatory activities.

    abstract::A number of isomeric benzoylpyrroleacetic acids (1-6) were prepared and tested in vitro for rat lenses aldose reductase activity. These pyrrole derivatives are structurally related to the acidic nonsteroidal anti-inflammatory drugs. Therefore, their anti-inflammatory properties were also evaluated in the carrageenan-i...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章

    doi:10.1002/jps.2600840119

    authors: Demopoulos VJ,Rekka E

    更新日期:1995-01-01 00:00:00

  • A method to predict the equilibrium solubility of drugs in solid polymers near room temperature using thermal analysis.

    abstract::A method is presented for determining the equilibrium solubility of a drug in a solid polymer at or near room temperature, which represents a typical storage temperature. The method is based on a thermodynamic model to calculate the Gibbs energy change ΔG(SS) associated with forming a binary drug-polymer solid solutio...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章

    doi:10.1002/jps.23319

    authors: Bellantone RA,Patel P,Sandhu H,Choi DS,Singhal D,Chokshi H,Malick AW,Shah N

    更新日期:2012-12-01 00:00:00

  • Solasodine stability under conditions of saponin hydrolysis.

    abstract::The extent of formation of solasodiene from solasodine upon treatment with hydrochloric acid under various conditions was determined. The diene formed was assayed by using the characteristic extinction at 236 nm. Diene formation was effected by the acid concentration and the boiling point of the solvent used. Optimal ...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章

    doi:10.1002/jps.2600670839

    authors: Segal R,Breuer A,Milo-Goldzweig I

    更新日期:1978-08-01 00:00:00

  • Prediction of Losartan-Active Carboxylic Acid Metabolite Exposure Following Losartan Administration Using Static and Physiologically Based Pharmacokinetic Models.

    abstract::The aim of this study was to evaluate a strategy based on static and dynamic physiologically based pharmacokinetic (PBPK) modeling for the prediction of metabolite and parent drug area under the time-concentration curve ratio (AUCm/AUCp) and their PK profiles in humans using in vitro data when active transport process...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章

    doi:10.1016/j.xphs.2017.03.032

    authors: Nguyen HQ,Lin J,Kimoto E,Callegari E,Tse S,Obach RS

    更新日期:2017-09-01 00:00:00

  • Implications of In-Use Photostability: Proposed Guidance for Photostability Testing and Labeling to Support the Administration of Photosensitive Pharmaceutical Products, Part 3. Oral Drug Products.

    abstract::The ICH Q1B guidance and additional clarifying manuscripts provide the essential information needed to conduct photostability testing for pharmaceutical drug products in the context of manufacturing, packaging, and storage. As the previous 2 papers in this series highlight for drug products administered by injection (...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章,评审

    doi:10.1016/j.xphs.2016.02.035

    authors: Allain L,Baertschi SW,Clapham D,Foti C,Lantaff WM,Reed RA,Templeton AC,Tønnesen HH

    更新日期:2016-05-01 00:00:00

  • Impact of Freeze/Thaw Process on Drug Substance Storage of Therapeutics.

    abstract::The storage of drug substance at subzero temperatures mitigates potential risks associated with liquid storage, such as degradation and shipping stress, making it the best solution for long-term storage. However, slower (generally uncontrolled) rates of freezing and thawing of drug substance in conventional large stor...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章

    doi:10.1016/j.xphs.2017.03.019

    authors: Rayfield WJ,Kandula S,Khan H,Tugcu N

    更新日期:2017-08-01 00:00:00

  • Applications of circular dichroism (CD) for structural analysis of proteins: qualification of near- and far-UV CD for protein higher order structural analysis.

    abstract::Circular dichroism (CD) spectroscopy is routinely used in the biopharmaceutical industry to study the effects of manufacturing, formulation, and storage conditions on protein conformation and stability, and these results are often included in regulatory filings. In this context, the purpose of CD spectroscopy is often...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章

    doi:10.1002/jps.22695

    authors: Li CH,Nguyen X,Narhi L,Chemmalil L,Towers E,Muzammil S,Gabrielson J,Jiang Y

    更新日期:2011-11-01 00:00:00

  • Kinetic analysis of enantiomers of threo-methylphenidate and its metabolite in two healthy subjects after oral administration as determined by a gas chromatographic-mass spectrometric method.

    abstract::A gas chromatographic-mass spectrometric method was developed for the stereoselective quantification of threo-methylphenidate (MPD) and its metabolite, ritalinic acid (RA), in plasma or urine. The plasma concentrations of (+)-MPD after oral administration of two 10-mg conventional tablets containing racemic MPD.HCl or...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章

    doi:10.1002/jps.2600790602

    authors: Aoyama T,Kotaki H,Honda Y,Nakagawa F

    更新日期:1990-06-01 00:00:00

  • Irreversible aggregation of recombinant bovine granulocyte-colony stimulating factor (bG-CSF) and implications for predicting protein shelf life.

    abstract::The kinetics of irreversible aggregation of bovine Granulocyte-Colony Stimulating Factor (bG-CSF) in solution were investigated as a function of temperature (T), concentration, and pH, and analyzed in terms of an Extended Lumry-Eyring model of protein aggregation proceeding via a non-native conformational state. In th...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章

    doi:10.1002/jps.10377

    authors: Roberts CJ,Darrington RT,Whitley MB

    更新日期:2003-05-01 00:00:00

  • Dequaternization of curare bases with sodium thiophenoxide and ethanolamine.

    abstract::To prepare (+)-tubocurine and O,O-dimethyl-(+)-tubocurine, the commonly used dequaternization procedures with sodium theophenoxide and ethanolamine were investigated. The quaternary compounds were (+)-tubocurarine chloride and the chloride and iodide salts of O,O-dimethyl-(+)-chondocurarine. The results obtained with ...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章

    doi:10.1002/jps.2600670904

    authors: Naghaway JA,Soine TO

    更新日期:1978-09-01 00:00:00

  • Degradation kinetics of gonadorelin in aqueous solution.

    abstract::The degradation kinetics of gonadorelin were investigated systematically with reversed-phase high-performance liquid chromatography. The stability-indicating properties of this system were checked with photodiode array detection and by comparison with capillary zone electrophoretic analysis. Influences of gonadorelin ...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章

    doi:10.1021/js9601187

    authors: Hoitink MA,Beijnen JH,Bult A,van der Houwen OA,Nijholt J,Underberg WJ

    更新日期:1996-10-01 00:00:00

  • The biological characteristics and pharmacodynamics of a mycophenolate mofetil nanosuspension ophthalmic delivery system in rabbits.

    abstract::The purpose of this study was to investigate corneal mucoadhesion, pharmacokinetics in lacrimal fluid and aqueous humor, the immune suppression induced by corneal transplantation of mycophenolate mofetil (MMF) nanosuspensions (NS), and the use of a chitosan-modified MMF nanosuspension (C-NS) as an ophthalmic delivery ...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章

    doi:10.1002/jps.22356

    authors: Wu XG,Xin M,Yang LN,Shi WY

    更新日期:2011-04-01 00:00:00