Preparation of inhalable salbutamol sulphate using reactive high gravity controlled precipitation.

Abstract:

:Reactive high gravity controlled precipitation (HGCP) was carried out to produce salbutamol sulphate (SS) particles suitable for inhalation. Aqueous solutions of free salbutamol base and sulphuric acid were mixed intensely inside a HGCP reactor to form the particles. Spray drying was employed to obtain dry powders. Physical properties of the powders were characterised by scanning electron microscopy, X-ray powder diffraction, thermal gravimetric analysis and dynamic water vapour sorption. Aerosol performance of the powders was measured using an Aeroliser connected to a multiple stage liquid impinger operating at 60 L/min. The results showed that the reactive HGCP powder, comprising primary SS sub-micron particles (approximately 100 nm in width and approximately 500 nm in length) packed into loose spherical agglomerates of about 2 microm in diameter, is of the same polymorphic form as the raw crystalline material, has a high specific surface area (24.7 +/- 0.1 m(2)/g), but a low moisture content (0.2%) and low moisture uptake (1.4% at RH 90%). The aerosol performance of the reactive HGCP powder is excellent, showing FPF(loaded) and FPF(emitted) of 76 +/- 5% and 83 +/- 7%, respectively, with low capsule and device retention. In conclusion, reactive HGCP followed by spray drying is suitable to produce stable crystalline powders of salbutamol with enhanced inhalation properties.

journal_name

J Pharm Sci

authors

Hu T,Chiou H,Chan HK,Chen JF,Yun J

doi

10.1002/jps.21026

subject

Has Abstract

pub_date

2008-02-01 00:00:00

pages

944-9

issue

2

eissn

0022-3549

issn

1520-6017

pii

S0022-3549(16)32476-5

journal_volume

97

pub_type

杂志文章
  • Mechanisms and surface chemical prediction of imipramine-induced hemolysis suppressed by modified cyclodextrins.

    abstract::The suppression of imipramine hydrochloride (IMP)- induced hemolysis by native cyclodextrins (alpha-, beta-, and gamma-CDs) and beta-CD derivatives is measured as a function of CD concentration and is quantitatively correlated with the surface tension of the solution determined at 37.0 degrees C. The modified beta-CDs...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章

    doi:10.1002/jps.1059

    authors: Funasaki N,Okuda T,Neya S

    更新日期:2001-08-01 00:00:00

  • Effect of symmetrical tetraalkylammonium salts on cloud point on nonionic surfactants.

    abstract::The salting in and salting out of the nonionic surfactant octoxynol NF by halides of ammonium and the four lowest symmetrical tetraalkylammonium cations were investigated by measuring their effect on the cloud point at various salt concentrations. The chloride anion tended to salt the surfactant out, lowering its clou...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章

    doi:10.1002/jps.2600660208

    authors: Schott H,Han SK

    更新日期:1977-02-01 00:00:00

  • Polymeric systems for amorphous Delta 9-tetrahydrocannabinol produced by a hot-melt method. Part I: chemical and thermal stability during processing.

    abstract::The objective of the present research was to investigate the stability of an amorphous drug, Delta(9)-tetrahydrocannabinol (THC) in polymer-based transmucosal systems. THC was incorporated in polyethylene oxide and hydroxypropylcellulose matrices by a hot-melt fabrication procedure, utilizing various processing aids. ...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章

    doi:10.1002/jps.20667

    authors: Munjal M,Stodghill SP,Elsohly MA,Repka MA

    更新日期:2006-08-01 00:00:00

  • Metabolism of carprofen, a nonsteroid anti-inflammatory agent, in rats, dogs, and humans.

    abstract::The metabolic disposition of 14C-labeled carprofen [(+/-)-6-chloro-alpha-methylcarbazole-2-acetic acid] was investigated in rats, dogs, and humans. Carprofen is eliminated predominantly by biotransformation in these three species. In dogs and rats, the direct conjugation of carprofen to form an ester glucuronide and o...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章

    doi:10.1002/jps.2600691104

    authors: Rubio F,Seawall S,Pocelinko R,DeBarbieri B,Benz W,Berger L,Morgan L,Pao J,Williams TH,Koechlin B

    更新日期:1980-11-01 00:00:00

  • Development of a Novel Amorphous Agomelatine Formulation With Improved Storage Stability and Enhanced Bioavailability.

    abstract::The present work describes the development of a novel formulation of amorphous agomelatine (AGM) that exhibits enhanced in vitro dissolution rate and bioavailability, as well as improved storage stability. AGM was loaded on a mixture of microcrystalline cellulose with a high specific surface area excipient, namely col...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 临床试验,杂志文章,随机对照试验

    doi:10.1016/j.xphs.2017.09.017

    authors: Barmpalexis P,Grypioti A,Vardaka E,Karagianni A,Kachrimanis K

    更新日期:2018-01-01 00:00:00

  • Potency of synthetic luteinizing hormone releasing hormone preparations in rat anterior pituitary cell cultures.

    abstract::Selected synthetic luteinizing hormone releasing hormone preparations were assayed, and their potencies were determined relative to one sample utilizing primary cultures of enzymatically dispersed rat anterior pituitary cells. Preliminary cell culture experiments indicated that luteinizing hormone releasing hormone ha...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章

    doi:10.1002/jps.2600660319

    authors: Dermody WC,Pastushok CA,Sakowski R,Vaitkus JW,Reel JR

    更新日期:1977-03-01 00:00:00

  • Degradation of paclitaxel and related compounds in aqueous solutions I: epimerization.

    abstract::Paclitaxel and other taxanes have complex structures including the presence of numerous hydrolytically sensitive ester groups and a chiral center that readily undergoes epimerization thus making their kinetics complex. The present study attempts to understand the mechanism of epimerization at the 7-position of paclita...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章

    doi:10.1002/jps.21112

    authors: Tian J,Stella VJ

    更新日期:2008-03-01 00:00:00

  • Influence of non-water-soluble placebo pellets of different sizes on the characteristics of orally disintegrating tablets manufactured by freeze-drying.

    abstract::The present study describes the development of an orally disintegrating tablet containing a non-water-soluble drug delivery system. A model system was applied to evaluate the effect of different-sized particles on tablet characteristics. Cellets were incorporated into tablets prepared by freeze-drying from a 100 mg/mL...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章

    doi:10.1002/jps.23517

    authors: Stange U,Führling C,Gieseler H

    更新日期:2013-06-01 00:00:00

  • A Micro-Polyethylene Glycol Precipitation Assay as a Relative Solubility Screening Tool for Monoclonal Antibody Design and Formulation Development.

    abstract::Adequate protein solubility is an important prerequisite for development, manufacture, and administration of biotherapeutic drug candidates, especially for high-concentration protein formulations. A previously established method for determining the relative apparent solubility (thermodynamic activity) of proteins usin...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章

    doi:10.1016/j.xphs.2016.05.021

    authors: Toprani VM,Joshi SB,Kueltzo LA,Schwartz RM,Middaugh CR,Volkin DB

    更新日期:2016-08-01 00:00:00

  • Impurities in a morphine sulfate drug product identified as 5-(hydroxymethyl)-2-furfural, 10-hydroxymorphine and 10-oxomorphine.

    abstract::Stability testing of morphine sulfate formulated with nonpareil sugar seeds (consisting of sucrose and starch) and fumaric acid revealed the formation of the three impurities 5-(hydroxymethyl)-2-furfural, 10-hydroxymorphine and 10-oxomorphine. 5-(Hydroxymethyl)-2-furfural was isolated via semipreparative HPLC utilizin...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章

    doi:10.1002/jps.10330

    authors: Kelly SS,Glynn PM,Madden SJ,Grayson DH

    更新日期:2003-03-01 00:00:00

  • Binding of (+)- and (-)-isomers and racemate of etomoxir to human serum albumin and effect of stearic acid and stanozolol.

    abstract::Binding of (+)- and (-)-isomers and the racemate of sodium 2[6-(4-chlorophenoxy)-hexyl]-oxiran-2-carboxylate dihydrat (etomoxir) to the human serum albumin (HSA) was studied by the gel filtration method. The experimental results are presented graphically using the method of Scatchard. Measurements revealed the followi...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章

    doi:10.1002/jps.2600830408

    authors: Vestemar V,Medic-Saric M,Rendic S

    更新日期:1994-04-01 00:00:00

  • Slow motion picture of protein inactivation during single-droplet drying: a study of inactivation kinetics of L-glutamate dehydrogenase dried in an acoustic levitator.

    abstract::A novel technique is presented to allow measurement of the kinetics of protein inactivation during drying of an acoustically levitated single droplet. Droplets/particles are removed from the acoustic field after various times during drying, and the state of the protein within them is analyzed. The influence of drying ...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章

    doi:10.1002/jps.23129

    authors: Lorenzen E,Lee G

    更新日期:2012-06-01 00:00:00

  • Nonadditive Effects of Repetitive Administration of Lipoplexes in Immunocompetent Mice.

    abstract::Repetitive administration is routinely used to maintain therapeutic drug levels, but previous studies have documented an accelerated blood clearance of some lipid-based delivery systems under these conditions. To assess the effect of repetitive administration, non-PEGylated lipoplexes (+/-0.5) were administered 4 time...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章

    doi:10.1016/j.xphs.2016.11.013

    authors: Betker JL,Anchordoquy TJ

    更新日期:2017-03-01 00:00:00

  • Quantitative structure/property relationship analysis of Caco-2 permeability using a genetic algorithm-based partial least squares method.

    abstract::Caco-2 cell monolayers are widely used systems for predicting human intestinal absorption. This study was carried out to develop a quantitative structure-property relationship (QSPR) model of Caco-2 permeability using a novel genetic algorithm-based partial least squares (GA-PLS) method. The Caco-2 permeability data f...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章

    doi:10.1002/jps.10214

    authors: Yamashita F,Wanchana S,Hashida M

    更新日期:2002-10-01 00:00:00

  • Effect of milling and compression on the solid-state Maillard reaction.

    abstract::The effects of milling and compression on the solid-state Maillard reaction between metoclopramide hydrochloride and lactose were investigated. Anhydrous metoclopramide hydrochloride was milled for various times, and then mixed with amorphous lactose. The mixtures were stored at 105 degrees C and 0% RH. The reactivity...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章

    doi:10.1002/jps.20448

    authors: Qiu Z,Stowell JG,Cao W,Morris KR,Byrn SR,Carvajal MT

    更新日期:2005-11-01 00:00:00

  • Molecular complexes of alprazolam with carboxylic acids, boric acid, boronic acids, and phenols. Evaluation of supramolecular heterosynthons mediated by a triazole ring.

    abstract::A series of molecular complexes, both co-crystals and salts, of a triazole drug-alprazolam-with carboxylic acids, boric acid, boronic acids, and phenols have been analyzed with respect to heterosynthons present in the crystal structures. In all cases, the triazole ring behaves as an efficient hydrogen bond acceptor wi...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章

    doi:10.1002/jps.22117

    authors: Varughese S,Azim Y,Desiraju GR

    更新日期:2010-09-01 00:00:00

  • Determination of serum tulobuterol concentrations by mass fragmentography: comparison with an electron-capture gas chromatographic method.

    abstract::A simple and sensitive method is reported for the quantitative determination of the bronchodilator tulobuterol in human serum. Tulobuterol and an internal standard were extracted from alkalinized serum with ether and then back-extracted into dilute hydrochloric acid. After alkalinization and extraction of the aqueous ...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章

    doi:10.1002/jps.2600720526

    authors: Matsumura K,Kubo O,Sakashita T,Kato H,Watanabe K,Hirobe M

    更新日期:1983-05-01 00:00:00

  • Synthesis of N,N'-bis(3-substituted benzylideneaminopropyl)-piperazines and their anti-inflammatory, antiproteolytic, and anticonvulsant properties.

    abstract::Some N,N'-bis(3-substituted benzylideneaminopropyl) piperazines were synthesized and characterized by their sharp melting points and elemental analyses. These substituted piperazines possessed anti-inflammatory activity, and the protection afforded by these compounds against carrageenan-induced edema ranged from 23 to...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章

    doi:10.1002/jps.2600650323

    authors: Chaturvedi AK,Sastry BV,Chaudhari A,Parmar SS

    更新日期:1976-03-01 00:00:00

  • Application of Online Near Infrared for Process Understanding of Spray-Drying Solution Preparation.

    abstract::Solution preparation is the first unit operation of the manufacturing process for spray-dried solid dispersions. Visual inspection and offline high-performance liquid chromatography analysis are routinely used to assess the solution preparation end point as well as the final solution composition. However, the accuracy...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章

    doi:10.1016/j.xphs.2018.10.022

    authors: Lee YC,Zhou G,Ikeda C,Chouzouri G,Howell L

    更新日期:2019-03-01 00:00:00

  • A new natural angelica polysaccharide based colon-specific drug delivery system.

    abstract::Colon-specific drug delivery systems are clinically necessary to treat colon diseases locally while minimizing systemic side effects. In this study, we extracted angelica polysaccharide from fresh roots of Angelica sinensis Diels and analyzed the monosaccharide components. With succinate as a cross-linker and angelica...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章

    doi:10.1002/jps.21790

    authors: Zhou S,Zhang B,Liu X,Teng Z,Huan M,Yang T,Yang Z,Jia M,Mei Q

    更新日期:2009-12-01 00:00:00

  • Synthesis of 10alpha-methoxy-delta8,9-lysergaldehyde from elymoclavine.

    abstract::A new synthesis is described for 10alpha-methoxy-delta8,9-lysergaldehyde involving the oxidation of elymoclavine with manganese dioxide in methanol. Lysergol and agroclavine provide no reaction under the same conditions. ...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章

    doi:10.1002/jps.2600660937

    authors: Choong TC,Thompson BL,Shough HR

    更新日期:1977-09-01 00:00:00

  • Precursor-dependent indirect pharmacodynamic response model for tolerance and rebound phenomena.

    abstract::A precursor-dependent model of indirect pharmacodynamic response which can describe tolerance and rebound was characterized in terms of the effects of changes in the fundamental properties of the drug on its response profiles. The model extends previous models by considering inhibition or stimulation of production of ...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章

    doi:10.1021/js980171q

    authors: Sharma A,Ebling WF,Jusko WJ

    更新日期:1998-12-01 00:00:00

  • An investigation into the melting behavior of binary mixes and solid dispersions of paracetamol and PEG 4000.

    abstract::The melting behavior of paracetamol and polyethylene glycol (PEG) 4000, both individually and as binary systems, has been studied using differential scanning calorimetry. The appearance of the PEG peaks was shown to be highly dependent on scanning rate, with evidence for the existence of once-folded and extended chain...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章

    doi:10.1021/js970137w

    authors: Lloyd GR,Craig DQ,Smith A

    更新日期:1997-09-01 00:00:00

  • Formulation of Granules for Site-Specific Delivery of an Antimicrobial Essential Oil to the Animal Intestinal Tract.

    abstract::Owing to proliferation of antibiotic-resistant bacteria, the use of antibiotics for livestock growth promotion is banned in many countries and alternatives to in-feed antibiotics are needed. Cinnamon essential oil exhibits strong in vitro antibacterial activity; however, direct addition of essential oils to animal fee...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章

    doi:10.1016/j.xphs.2015.10.001

    authors: Ma YH,Wang Q,Gong J,Wu XY

    更新日期:2016-03-01 00:00:00

  • Stabilizing effect of fructose on aqueous solutions of hydrocortisone.

    abstract::Accelerated stability studies (37 degrees, 47 degrees, and 57 degrees) were conducted on buffered aqueous solutions (pH 7.4, 8.4, and 9.4) of hydrocortisone in the presence of various molar ratios of D-fructose. First-order degradation was observed. Significant improvement in hydrocortisone stability was seen in those...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章

    doi:10.1002/jps.2600720930

    authors: Bansal NP,Holleran EM,Jarowski CI

    更新日期:1983-09-01 00:00:00

  • Hepatobiliary disposition of liposomal amphotericin B in the isolated perfused rat liver.

    abstract::The hepatic distribution, biliary excretion, and mass balance of liposomal amphotericin B (L-AmB) were investigated in recirculated isolated perfused rat liver. The results were compared with those from the conventional AmB formulation, amphotericin B deoxycholate (D-AmB). L-AmB was introduced as a bolus into the perf...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章

    doi:10.1002/jps.20239

    authors: Hong Y,Ramzan I,McLachlan AJ

    更新日期:2005-01-01 00:00:00

  • Development of a CART Model to Predict the Synthesis of Cardiotoxic Daunorubicinol in Heart Tissue Samples From Donors With and Without Down Syndrome.

    abstract::Daunorubicin (DAUN) and doxorubicin (DOX) are used to treat a variety of cancers. The use of DAUN and DOX is hampered by the development of cardiotoxicity. Clinical evidence suggests that patients with leukemia and Down syndrome are at increased risk for anthracycline-related cardiotoxicity. Carbonyl reductases and al...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章

    doi:10.1016/j.xphs.2016.03.013

    authors: Hoefer CC,Blair RH,Blanco JG

    更新日期:2016-06-01 00:00:00

  • Quantitative (13)C Solid-State NMR Spectra by Multiple-Contact Cross-polarization for Drug Delivery: From Active Principles to Excipients and Drug Carriers.

    abstract::In this contribution, we present an analysis of the main parameters influencing the efficiency of the (1)H → (13)C multiple-contact cross-polarization nuclear magnetic resonance (NMR) experiment in the context of solid pharmaceutical materials. Using the optimum experimental conditions, quantitative (13)C NMR spectra ...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章

    doi:10.1016/j.xphs.2016.05.025

    authors: Saïdi F,Taulelle F,Martineau C

    更新日期:2016-08-01 00:00:00

  • Profile of P-glycoprotein distribution in the rat and its possible influence on the salbutamol intestinal absorption process.

    abstract::The intrinsic absorption of salbutamol in different intestinal segments of the rat was measured and related with the corresponding intestinal P-glycoprotein (P-gp) expression levels. The apparent absorption rate constants (k(a), h(-1)) observed in each fraction by means of the "in situ" rat gut absorption method after...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章

    doi:10.1002/jps.20071

    authors: Valenzuela B,Nácher A,Ruiz-Carretero P,Martín-Villodre A,López-Carballo G,Barettino D

    更新日期:2004-06-01 00:00:00

  • Biophysical characterization of insoluble aggregates of a multi-domain protein: an insight into the role of the various domains.

    abstract::Insoluble (visible) aggregates of a homodimer fusion glycoprotein, consisting of the first extracellular domain of a human protein, fused to the hinge, C(H)2, and C(H)3 domains of a human immunoglobulin G(1) (IgG(1)), were observed during early formulation development. The soluble fraction of the fusion protein was co...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章

    doi:10.1002/jps.20423

    authors: Souillac PO

    更新日期:2005-09-01 00:00:00