Influence of the solid form of siramesine hydrochloride on its behavior in aqueous environments.

Abstract:

PURPOSE:To study the influence of solid form on the behavior of the salt siramesine hydrochloride in aqueous environments. METHODS:The solubilities and dissolution rates of siramesine hydrochloride anhydrate and monohydrate were determined at pH 3.4 and 6.4, and precipitates were examined by X-ray powder diffraction. The mechanism of anhydrate-hydrate conversion was investigated by optical microscopy, and wet massing of the anhydrate was carried out using water and 60% (v/v) ethanol separately as granulation liquids. The wet masses were analyzed using Raman microscopy. RESULTS:At pH 3.4 the anhydrate and monohydrate salts exhibited similar dissolution profiles. At pH 6.4 both the anhydrate and monohydrate salts formed supersaturated solutions of high apparent solubility. From the anhydrate solution, precipitation of the free base occurred, while the solution of the monohydrate salt remained in the supersaturated state. This resulted in a superior dissolution profile of the monohydrate salt. Microscopy and wet massing experiments showed that the anhydrate-hydrate conversion of siramesine hydrochloride was solution-mediated and dissolution-controlled. CONCLUSION:During development of a formulation based on the anhydrate salt, the risk of processing-induced transformation to the monohydrate form as well as precipitation of the free base should be considered.

journal_name

Pharm Res

journal_title

Pharmaceutical research

authors

Zimmermann A,Tian F,Lopez de Diego H,Ringkjøbing Elema M,Rantanen J,Müllertz A,Hovgaard L

doi

10.1007/s11095-008-9783-0

subject

Has Abstract

pub_date

2009-04-01 00:00:00

pages

846-54

issue

4

eissn

0724-8741

issn

1573-904X

journal_volume

26

pub_type

杂志文章
  • Evaluation of Intranasal Vaccine Delivery Using Anatomical Replicas of Infant Nasal Airways.

    abstract:PURPOSE:Nasal delivery is a favorable route for vaccination against most respiratory infections, as antigen deposited in the nasal turbinate and Waldeyer's ring areas induce mucosal and systemic immune responses. However, little is known about the nasal distribution of the vaccines, specifically for infants. METHODS:A...

    journal_title:Pharmaceutical research

    pub_type: 杂志文章

    doi:10.1007/s11095-020-02976-9

    authors: Wilkins JV Jr,Golshahi L,Rahman N,Li L

    更新日期:2021-01-15 00:00:00

  • Pharmacokinetic significance of renal OAT3 (SLC22A8) for anionic drug elimination in patients with mesangial proliferative glomerulonephritis.

    abstract:PURPOSE:Our previous studies showed that the mRNA level of human organic anion transporter (hOAT) 3 in the kidney was correlated with the rate of elimination of an anionic antibiotic cefazolin. However, the correlation coefficient was not so high. In the present study, therefore, we enrolled more patients to examine wh...

    journal_title:Pharmaceutical research

    pub_type: 杂志文章

    doi:10.1007/s11095-005-8383-5

    authors: Sakurai Y,Motohashi H,Ogasawara K,Terada T,Masuda S,Katsura T,Mori N,Matsuura M,Doi T,Fukatsu A,Inui K

    更新日期:2005-12-01 00:00:00

  • Comparative study of the skin penetration of protein transduction domains and a conjugated peptide.

    abstract:PURPOSE:We examined the ability of a protein transduction domain (PTD), YARA, to penetrate in the skin and carry a conjugated peptide, P20. The results with YARA were compared to those of a well-known PTD (TAT) and a control, nontransducing peptide (YKAc). The combined action of PTDs and lipid penetration enhancers was...

    journal_title:Pharmaceutical research

    pub_type: 杂志文章

    doi:10.1007/s11095-005-2591-x

    authors: Lopes LB,Brophy CM,Furnish E,Flynn CR,Sparks O,Komalavilas P,Joshi L,Panitch A,Bentley MV

    更新日期:2005-05-01 00:00:00

  • Protein inhalation powders: spray drying vs spray freeze drying.

    abstract:PURPOSE:To develop a new technique, spray freeze drying, for preparing protein aerosol powders. Also, to compare the spray freeze-dried powders with spray-dried powders in terms of physical properties and aerosol performance. METHODS:Protein powders were characterized using particle size analysis, thermogravimetric an...

    journal_title:Pharmaceutical research

    pub_type: 杂志文章

    doi:10.1023/a:1018828425184

    authors: Maa YF,Nguyen PA,Sweeney T,Shire SJ,Hsu CC

    更新日期:1999-02-01 00:00:00

  • Characterization of asparagine deamidation and aspartate isomerization in recombinant human interleukin-11.

    abstract:UNLABELLED:PURPOSE; The aim of this study was to investigate asparagine (Asn) deamidation and aspartate (Asp) isomerization and to measure the content of isoaspartate (isoAsp) in recombinant human interleukin-11 (rhIL-11). METHODS:The rhIL-11 control and heat stressed samples were characterized with trypsin and endopr...

    journal_title:Pharmaceutical research

    pub_type: 杂志文章

    doi:10.1023/a:1019814713428

    authors: Zhang W,Czupryn JM,Boyle PT Jr,Amari J

    更新日期:2002-08-01 00:00:00

  • Immobilization of active urokinase on albumin microspheres: use of a chemical dehydrant and process monitoring.

    abstract::A method of immobilizing urokinase on albumin microspheres has been developed. Laser scattering, which was used to follow particle size from the initial emulsification stage to the final aqueous resuspension of the microsphere stage, showed that particle coalescence and crosslinking were critical parameters in manufac...

    journal_title:Pharmaceutical research

    pub_type: 杂志文章

    doi:10.1023/a:1015855622459

    authors: Bhargava K,Ando HY

    更新日期:1992-06-01 00:00:00

  • Effect of Relative Humidity on Bipolar Electrostatic Charge Profiles of dry Powder Aerosols.

    abstract:PURPOSE:This work investigated the effect of relative humidity (RH) on bipolar electrostatic charge profiles of dry powder inhaler aerosols using the Bipolar Charge Analyzer (BOLAR). METHODS:Two commercial products, Pulmicort® (400 μg, budesonide) and Bricanyl® (500 μg, terbutaline sulfate) Turbuhaler®, were used as m...

    journal_title:Pharmaceutical research

    pub_type: 杂志文章

    doi:10.1007/s11095-017-2178-3

    authors: Yu J,Wong J,Ukkonen A,Kannosto J,Chan HK

    更新日期:2017-08-01 00:00:00

  • In vitro- in vivo correlation's dissolution limits setting.

    abstract:PURPOSE:In vitro in vivo correlation (IVIVC) is a biopharmaceutical tool recommended for use in formulation development. When validated, IVIVC can be used to set dissolution limits and, based on the dissolution limits, as a surrogate for an in vivo study. The purpose of this paper is to study the various methods used t...

    journal_title:Pharmaceutical research

    pub_type: 杂志文章

    doi:10.1007/s11095-014-1349-8

    authors: Roudier B,Davit BM,Beyssac E,Cardot JM

    更新日期:2014-09-01 00:00:00

  • The effect of engineered mannitol-lactose mixture on dry powder inhaler performance.

    abstract:PURPOSE:To co-crystallise mannitol and lactose with a view to obtaining crystals with more favourable morphological features than either lactose or mannitol alone, suitable for use as carriers in formulations for dry powder inhalers (DPIs) using simultaneous engineering of lactose-mannitol mixtures. METHODS:Mannitol a...

    journal_title:Pharmaceutical research

    pub_type: 杂志文章

    doi:10.1007/s11095-012-0743-3

    authors: Kaialy W,Larhrib H,Martin GP,Nokhodchi A

    更新日期:2012-08-01 00:00:00

  • Scale of health: indices of safety and efficacy in the evolving environment of large biological datasets.

    abstract::The interdependent relationship between pharmacology and toxicology is fundamental to the concepts of efficacy and safety of both drugs and xenobiotics. The traditional concept of establishing efficacious and tolerated doses to define a 'therapeutic window' appears simplistic in the context of an exponentially increas...

    journal_title:Pharmaceutical research

    pub_type: 杂志文章,评审

    doi:10.1007/s11095-014-1415-2

    authors: Sayes CM,Staats H,Hickey AJ

    更新日期:2014-09-01 00:00:00

  • Molecular modeling study of diltiazem mimics at L-type calcium channels.

    abstract:PURPOSE:A theoretical study was performed to generate a pharmacophore model for chemically diverse structures that specifically interact with the diltiazem binding site of L-type calcium channels. METHODS:Via molecular mechanics and quantum chemical methods solvation energies, logP values, conformational and electroni...

    journal_title:Pharmaceutical research

    pub_type: 杂志文章

    doi:10.1023/a:1015037800903

    authors: Schleifer KJ,Tot E

    更新日期:1999-10-01 00:00:00

  • Identification of human UDP-glucuronosyltransferase responsible for the glucuronidation of niflumic acid in human liver.

    abstract:PURPOSE:To assess the uridine diphosphate (UDP)-glucuronosyltransferase (UGT) isozymes involved in the glucuronidation of niflumic acid in human liver. METHODS:The glucuronidation activity of niflumic acid was determined in liver microsomes and recombinant UGT isozymes by incubation of niflumic acid with UDP-glucuroni...

    journal_title:Pharmaceutical research

    pub_type: 杂志文章

    doi:10.1007/s11095-006-0250-5

    authors: Mano Y,Usui T,Kamimura H

    更新日期:2006-07-01 00:00:00

  • Oral absorption enhancement of cromolyn sodium through noncovalent complexation.

    abstract:PURPOSE:To determine the effect of Sodium N-[8-(2-hydroxybenzoyl)amino]caprylate (SNAC) on the permeation of cromolyn across Caco-2 cell monolayers and explore the molecular basis for the enhanced absorption. METHODS:Transport studies of cromolyn across Caco-2 cell monolayers were conducted in the presence of various ...

    journal_title:Pharmaceutical research

    pub_type: 杂志文章

    doi:10.1007/s11095-004-7671-9

    authors: Ding X,Rath P,Angelo R,Stringfellow T,Flanders E,Dinh S,Gomez-Orellana I,Robinson JR

    更新日期:2004-12-01 00:00:00

  • A model for targeting colon carcinoma cells using single-chain variable fragments anchored on virus-like particles via glycosyl phosphatidylinositol anchor.

    abstract:PURPOSE:VLPs displaying tumor targeting single-chain variable fragments (VLP-rscFvs) which targets tumor-associated glycoprotein-72 (TAG-72) marker protein have a potential for immunotherapy against colon carcinoma tumors. In this study, scFvs anchored on VLPs using glycosylphosphatidylinositol (GPI) were prepared to t...

    journal_title:Pharmaceutical research

    pub_type: 杂志文章

    doi:10.1007/s11095-014-1316-4

    authors: Deo VK,Yui M,Alam J,Yamazaki M,Kato T,Park EY

    更新日期:2014-08-01 00:00:00

  • SB-239063, a potent and selective inhibitor of p38 map kinase: preclinical pharmacokinetics and species-specific reversible isomerization.

    abstract:PURPOSE:A series of studies was conducted to evaluate the preclinical pharmacokinetics of SB-239063 (trans-1-(4-hydroxycyclohexyl)-4-(4-fluorophenyl)-5-[(2-methoxy)pyrimidin-4-yl] imidazole), a potent and selective p38 MAP kinase inhibitor. METHODS:SB-239063 was administered both i.v. and p.o. in the rat, dog, cynomol...

    journal_title:Pharmaceutical research

    pub_type: 杂志文章

    doi:10.1023/a:1013002414678

    authors: Ward KW,Proksch JW,Azzarano LM,Salyers KL,McSurdy-Freed JE,Molnar TM,Levy MA,Smith BR

    更新日期:2001-09-01 00:00:00

  • Effects of solute characteristics and concentration on a lyotropic liquid crystal: solute-induced phase change.

    abstract::We investigated the effects of increased concentrations of the solutes, salicylic acid, benzoic acid, and o-, m-, and p-methoxy benzoic acids, on the anisotropic properties of a liquid crystal solvent. The lamellar liquid crystal was composed of 37% polyoxyethylene (20) isohexadecyl ether in aqueous buffer of pH 1. Ph...

    journal_title:Pharmaceutical research

    pub_type: 杂志文章

    doi:10.1023/a:1018920118631

    authors: Ibrahim HG,Sallam ES,Takieddin M,Habboub M

    更新日期:1993-05-01 00:00:00

  • A study on structural and diffusion properties of porcine stratum corneum based on very small angle neutron scattering data.

    abstract:PURPOSE:Generation of valuable information about the biphasic geometrical configuration of porcine stratum corneum from Very Small Angle Neutron Scattering (VSANS) data and investigation of its effect on the corresponding effective diffusivity. METHODS:Spectra of porcine stratum corneum are mathematically transformed ...

    journal_title:Pharmaceutical research

    pub_type: 杂志文章

    doi:10.1023/a:1026453628800

    authors: Charalambopoulou GC,Karamertzanis P,Kikkinides ES,Stubos AK,Kanellopoulos NK,Papaioannou AT

    更新日期:2000-09-01 00:00:00

  • Multi-compartmental nanoparticles-in-emulsion formulation for macrophage-specific anti-inflammatory gene delivery.

    abstract:PURPOSE:To develop a safe and effective non-viral vector for gene delivery and transfection in macrophages for potential anti-inflammatory therapy. METHODS:Solid nanoparticles-in-emulsion (NiE) multi-compartmental delivery system was designed using plasmid DNA-encapsulated type B gelatin nanoparticles suspended in the...

    journal_title:Pharmaceutical research

    pub_type: 杂志文章

    doi:10.1007/s11095-012-0677-9

    authors: Attarwala H,Amiji M

    更新日期:2012-06-01 00:00:00

  • Effect of some penetration enhancers on epithelial membrane lipid domains: evidence from fluorescence spectroscopy studies.

    abstract::The effect of the penetration enhancers Azone, oleic acid, 1-dodecanol, dodecyl N,N-dimethylaminoacetate (DDAA), and dodecyl N,N-dimethylaminoisopropionate (DDAIP) on epithelial membrane lipids was examined using human buccal cell membranes as a model for epithelial lipid bilayer. Buccal epithelial cells (BEC) were la...

    journal_title:Pharmaceutical research

    pub_type: 杂志文章

    doi:10.1023/a:1018919811227

    authors: Turunen TM,Urtti A,Paronen P,Audus KL,Rytting JH

    更新日期:1994-02-01 00:00:00

  • A spectroscopic investigation of losartan polymorphs.

    abstract::Losartan, an antihypertensive agent in clinical development, was found to exist in two enantiotropic polymorphic forms, a low-temperature stable form (Form I) and a high-temperature stable form (Form II), the temperatures at which they are stable being related to the transition temperature. X-ray powder diffraction pa...

    journal_title:Pharmaceutical research

    pub_type: 杂志文章

    doi:10.1023/a:1018973530443

    authors: Raghavan K,Dwivedi A,Campbell GC Jr,Johnston E,Levorse D,McCauley J,Hussain M

    更新日期:1993-06-01 00:00:00

  • Characterization of the mechanism of zidovudine uptake by rat conditionally immortalized syncytiotrophoblast cell line TR-TBT.

    abstract:PURPOSE:To characterize the uptake mechanism of zidovudine (AZT), a nucleoside reverse transcriptase inhibitor, in syncytiotrophoblast cells using the TR-TBT 18d-1 cell line previously established by our group. MATERIALS AND METHODS:The effects of several transporter inhibitors on the initial and steady-state apical u...

    journal_title:Pharmaceutical research

    pub_type: 杂志文章

    doi:10.1007/s11095-008-9564-9

    authors: Sai Y,Nishimura T,Shimpo S,Chishu T,Sato K,Kose N,Terasaki T,Mukai C,Kitagaki S,Miyakoshi N,Kang YS,Nakashima E

    更新日期:2008-07-01 00:00:00

  • Iontophoretic delivery of 5-aminolevulinic acid (ALA): effect of pH.

    abstract:PURPOSE:To examine the iontophoretic delivery of ALA as a function of pH and to determine the principal mechanisms responsible for its electrotransport. METHODS:Anodal iontophoretic transport of ALA was measured as a function of its concentration and pH of the donor solution. Experiments were performed in vitro using ...

    journal_title:Pharmaceutical research

    pub_type: 杂志文章

    doi:10.1023/a:1011050829531

    authors: Lopez RF,Bentley MV,Delgado-Charro MB,Guy RH

    更新日期:2001-03-01 00:00:00

  • Relative reactivity of dihydropyridine derivatives to electrogenerated superoxide ion in DMSO solutions: a voltammetric approach.

    abstract:PURPOSE:To evaluate the reaction of a large series of pharmacologically significant 1,4-dihydropyridine (1,4-DHP) compounds with superoxide (O2.-) in dimethylsulfoxide using differential pulse voltammetry and controlled potential electrolysis. METHODS:Differential pulse voltammetry was used to track the consumption of...

    journal_title:Pharmaceutical research

    pub_type: 杂志文章

    doi:10.1023/a:1022291624933

    authors: Oriz ME,Núñez-Vergara LJ,Squella JA

    更新日期:2003-02-01 00:00:00

  • Alterations in neuronal transport but not blood-brain barrier transport are observed during gamma-hydroxybutyrate (GHB) sedative/hypnotic tolerance.

    abstract:PURPOSE:To investigate if gamma-Hydroxybutyrate (GHB) tolerance is mediated by alterations in GHB systemic pharmacokinetics, transport (blood brain barrier (BBB) and neuronal) or membrane fluidity. MATERIALS AND METHODS:GHB tolerance in rats was attained by repeated GHB administration (5.31 mmol/kg, s.c., QD for 5 day...

    journal_title:Pharmaceutical research

    pub_type: 杂志文章

    doi:10.1007/s11095-006-9066-6

    authors: Bhattacharya I,Raybon JJ,Boje KM

    更新日期:2006-09-01 00:00:00

  • In vitro/in vivo correlation for 14C-methylated lysozyme release from poly(ether-ester) microspheres.

    abstract:PURPOSE:The purpose of this study was to obtain an in vitro/in vivo correlation for the sustained release of a protein from poly(ethylene glycol) terephthalate (PEGT)/poly(butylene terephthalate) (PBT) microspheres. METHODS:Radiolabeled lysozyme was encapsulated in PEGT/PBT microspheres via a water-in-oil-in-water emu...

    journal_title:Pharmaceutical research

    pub_type: 杂志文章

    doi:10.1023/B:PHAM.0000019303.12086.d1

    authors: van Dijkhuizen-Radersma R,Wright SJ,Taylor LM,John BA,de Groot K,Bezemer JM

    更新日期:2004-03-01 00:00:00

  • Colonic absorption of insulin-like growth factor I in vitro.

    abstract::Colonic absorption of recombinant human insulin-like growth factor I (rhIGF-I) was measured in vitro using both rat and minipig colon. The permeability coefficients were 8.03 +/- 1.03 and 4.75 +/- 0.43 x 10(-8) cm sec-1 in the rat and minipig, respectively. The steady-state flux in rat colon was linearly related to th...

    journal_title:Pharmaceutical research

    pub_type: 杂志文章

    doi:10.1023/a:1018999106684

    authors: Quadros E,Landzert NM,LeRoy S,Gasparini F,Worosila G

    更新日期:1994-02-01 00:00:00

  • Metabolism of azetirelin, a new thyrotropin-releasing hormone (TRH) analogue, by intestinal microorganisms.

    abstract:PURPOSE:We evaluated the effect of luminal bacterial metabolism on intestinal absorption of azetirelin in rats. In vitro characteristics of bacterial metabolism of azetirelin were also investigated with the goal of overcoming the low stability of the peptidic drug against luminal microorganisms. METHODS:Plasma azetire...

    journal_title:Pharmaceutical research

    pub_type: 杂志文章

    doi:10.1023/a:1012141025938

    authors: Sasaki I,Tamura T,Shibakawa T,Fujita T,Murakami M,Yamamoto A,Muranishi S

    更新日期:1997-08-01 00:00:00

  • Saquinavir Loaded Acetalated Dextran Microconfetti - a Long Acting Protease Inhibitor Injectable.

    abstract:PURPOSE:Since the adoption of highly active antiretroviral therapy, HIV disease progression has slowed across the world; however, patients are often required to take multiple medications daily of poorly bioavailable drugs via the oral route, leading to gastrointestinal irritation. Recently, long acting antiretroviral i...

    journal_title:Pharmaceutical research

    pub_type: 杂志文章

    doi:10.1007/s11095-016-1936-y

    authors: Collier MA,Gallovic MD,Bachelder EM,Sykes CD,Kashuba A,Ainslie KM

    更新日期:2016-08-01 00:00:00

  • Antigene, ribozyme and aptamer nucleic acid drugs: progress and prospects.

    abstract::Nucleic acids are increasingly being considered for therapeutic uses, either to interfere with the function of specific nucleic acids or to bind specific proteins. Three types of nucleic acid drugs are discussed in this review: aptamers, compounds which bind specific proteins; triplex forming (antigene) compounds; whi...

    journal_title:Pharmaceutical research

    pub_type: 杂志文章,评审

    doi:10.1023/a:1016281324761

    authors: Stull RA,Szoka FC Jr

    更新日期:1995-04-01 00:00:00

  • The effect of immunosuppression by total-body irradiation on the pharmacodynamics of centrally active drugs in rats.

    abstract::The aim of this investigation was to assess whether immunosuppression induced by total-body irradiation (TBI) affects the pharmacodynamics of centrally acting drugs. Female Sabra rats were exposed to a single dose of gamma irradiation (5.3 Gy). Four days later, when both the cellular and the humoral immune responses w...

    journal_title:Pharmaceutical research

    pub_type: 杂志文章

    doi:10.1023/a:1018928329824

    authors: Hoffman A,Alfon J,Habib G,Pinto E,Gorodetsky R

    更新日期:1994-05-01 00:00:00