Influence of solid phase and formulation processing on stability of Abbott-232 tablet formulations.

Abstract:

:Abbott-232 is a chemically stable, highly water soluble non-hygroscopic compound selected for development as a potent uroselective alpha(1A) agonist. An anhydrate, a monohydrate, and an amorphous phase were isolated. The anhydrate was chosen for formulation development based on solid-state characterization. Excipients for immediate release (IR) tablet formulations were selected according to compatibility studies. However, the prototype IR tablets designed for clinical trials were found to be chemically unstable. Thus, process-induced phase transformation was investigated as the likely cause of the observed instability. Since the drug loading in the formulations was low (1%), model granulations containing 30% drug were evaluated to test this hypothesis. Investigation using a variety of analytical techniques indicated that the observed degradation was, indeed, a result of a solution-mediated phase transformation from anhydrate to amorphous Abbott-232 during wet granulation. A new direct compression formulation was, therefore, developed to prevent the solution-mediated process induced phase transition. Since the drug loading was low, a polarized light microscope (PLM) method was used to evaluate the solid phase in the new formulation. PLM confirmed that the original anhydrate form remained unchanged in tablets manufactured by the dry process. Stability studies confirmed that both IR and extended release (ER) tablets of Abbott-232 were successfully developed for clinical trials using direct compression.

journal_name

J Pharm Sci

authors

Wardrop J,Law D,Qiu Y,Engh K,Faitsch L,Ling C

doi

10.1002/jps.20679

subject

Has Abstract

pub_date

2006-11-01 00:00:00

pages

2380-92

issue

11

eissn

0022-3549

issn

1520-6017

pii

S0022-3549(16)32121-9

journal_volume

95

pub_type

杂志文章
  • Polyanhydride microsphere formulation by solvent extraction.

    abstract::A novel process based on solvent extraction was developed to produce drug-loaded polyanhydride microspheres for controlled-release applications. The technique consists of adding a chloroform solution of polyanhydride and drug into a stirred silicone oil phase containing suspended droplets of surfactant. No chemical re...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章

    doi:10.1002/jps.2600770811

    authors: Bindschaedler C,Leong K,Mathiowitz E,Langer R

    更新日期:1988-08-01 00:00:00

  • Simple procedure for determining octanol--aqueous partition, distribution, and ionization coefficients by reversed-phase high-pressure liquid chromatography.

    abstract::The described simple, accurate, and precise reversed-phase high-pressure liquid chromatographic procedure is in excellent agreement with 1-octanol shake-flask partition or distribution coefficients over a 3.5 log range. A chemically bonded octadecylsilane support is persilated and coated with 1-octanol. With 1-octanol...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章

    doi:10.1002/jps.2600671008

    authors: Unger SH,Cook JR,Hollenberg JS

    更新日期:1978-10-01 00:00:00

  • Assay of adinazolam in plasma by liquid chromatography.

    abstract::A procedure for the quantitative determination of adinazolam in plasma was developed. The drug, an N-demethylated metabolite, and an internal standard were extracted from basified plasma into ethyl acetate. After evaporation, the residue was dissolved in toluene which was washed with sodium hydroxide. The toluene was ...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章

    doi:10.1002/jps.2600730840

    authors: Peng GW

    更新日期:1984-08-01 00:00:00

  • Plasma binding of benzodiazepines in humans.

    abstract::Plasma binding of chlordiazepoxide, diazepam, loraxepam, and oxazepam was determined by equilibrium dialysis in 20 male, healthy volunteers, 25-86 years old. A wide range of binding was observed, with the free fraction varying twofold for lorazepam, fourfold for chlordiazepoxide and diazepam, and over 20-fold for oxa...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章

    doi:10.1002/jps.2600681034

    authors: Johnson RF,Schenker S,Roberts RK,Desmond PV,Wilkinson GR

    更新日期:1979-10-01 00:00:00

  • Evaluation of Systemic and Mucosal Immune Responses Induced by a Nasal Powder Delivery System in Conjunction with an OVA Antigen in Cynomolgus Monkeys.

    abstract::An immune response for a nasal ovalbumin (OVA) powder formulation with an applied nasal delivery platform technology, consisting of a powdery nasal carrier and a device, was evaluated in monkeys with similar upper respiratory tracts and immune systems to those of humans, in order to assess the applicability to a vacci...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章

    doi:10.1016/j.xphs.2020.11.023

    authors: Torikai Y,Sasaki Y,Sasaki K,Kyuno A,Haruta S,Tanimoto A

    更新日期:2020-12-03 00:00:00

  • Polymorphism and solvatomorphism 2007.

    abstract::Papers and patents that deal with polymorphism (crystal systems for which a substance can exist in structures characterized by different unit cells, but where each of the forms has exactly the same elemental composition) and solvatomorphism (systems where the crystal structures of the substance are defined by differen...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章,评审

    doi:10.1002/jps.21518

    authors: Brittain HG

    更新日期:2009-05-01 00:00:00

  • The influence of hepatic transport on the distribution volumes and mean residence time of drug in the body and the accuracy of estimating these parameters by the traditional pharmacokinetic calculations.

    abstract::The influence of hepatic uptake and efflux, which includes passive diffusion and transporter-mediated component, on drug distribution volumes [steady-state volume of distribution (V(ss)) and terminal volume of distribution (V(β))], mean residence time (MRT), clearance, and terminal half-life is considered using a simp...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章

    doi:10.1002/jps.22696

    authors: Berezhkovskiy LM

    更新日期:2011-11-01 00:00:00

  • Utilization of Zwitterion-based solutions to dissect the relative effects of solution pH and ionic strength on the aggregation behavior and conformational stability of a fusion protein.

    abstract::Solution pH and ionic strength (I) have complex effects on protein stability. We developed an experimental approach based on exploitation of the zwitterionic characteristic of amino acid molecules to probe the relative contribution from each. A variety of types of amino acid solutions were adopted to investigate the e...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章

    doi:10.1002/jps.24118

    authors: Zhou R,Nashine V,Palm T,Gandhi R,Adams M

    更新日期:2014-10-01 00:00:00

  • Shear-induced degradation of plasmid DNA.

    abstract::The majority of gene therapy clinical trials use plasmid DNA that is susceptible to shear-induced degradation. Many processing steps in the extraction, purification, and preparation of plasmid-based therapeutics can impart significant shear stress that can fracture the phosphodiester backbone of polynucleotides, and r...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章,评审

    doi:10.1002/jps.10140

    authors: Lengsfeld CS,Anchordoquy TJ

    更新日期:2002-07-01 00:00:00

  • Preparation of spherically agglomerated crystals of aminophylline.

    abstract::The spherically agglomerated crystals of aminophylline (theophylline-ethylenediamine complex) can be compounded directly into pharmaceutical formulations without further processing, e.g., granulation. Such crystals were prepared by mixing theophylline and ethylenediamine in a partially miscible solvent system, i.e., o...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章

    doi:10.1002/jps.2600731021

    authors: Kawashima Y,Aoki S,Takenaka H,Miyake Y

    更新日期:1984-10-01 00:00:00

  • The Disintegration Process in Microcrystalline Cellulose Based Tablets, Part 1: Influence of Temperature, Porosity and Superdisintegrants.

    abstract::Disintegration performance was measured by analysing both water ingress and tablet swelling of pure microcrystalline cellulose (MCC) and in mixture with croscarmellose sodium using terahertz pulsed imaging (TPI). Tablets made from pure MCC with porosities of 10% and 15% showed similar swelling and transport kinetics: ...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章

    doi:10.1002/jps.24544

    authors: Yassin S,Goodwin DJ,Anderson A,Sibik J,Ian Wilson D,Gladden LF,Axel Zeitler J

    更新日期:2015-10-01 00:00:00

  • Facile synthesis of glycol metabolites of phenethylamine drugs.

    abstract::High yields of potential glycol metabolites of p-synephrine, epinephrine, octopamine, and normacromerine can be obtained from the readily available monosubstituted and disubstituted acetophenones. The general procedure involves alpha-bromination followed by displacement with acetate ion and reduction with lithium alum...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章

    doi:10.1002/jps.2600750621

    authors: Holshouser MH,Kolb M

    更新日期:1986-06-01 00:00:00

  • Determination of benzalkonium chloride by reversed-phase high-pressure liquid chromatography.

    abstract::A new, specific, and useful approach for the analysis of benzalkonium chloride is presented. Reversed-phase high-pressure liquid chromatography is used to determine benzalkonium chloride in an ophthalmic system at the presevative level of 0.004%. Since the method separates each homolog, it can be extended to determine...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章

    doi:10.1002/jps.2600691006

    authors: Meyer RC

    更新日期:1980-10-01 00:00:00

  • Impact of formulation and methods of pulmonary delivery on absorption of parathyroid hormone (1-34) from rat lungs.

    abstract::The aim of this work was to optimize the absorption of parathyroid hormone 1-34 (PTH) from the lungs by determining factors favoring its transport from the air spaces into the bloodstream. We simultaneously conducted pharmacokinetic and regional lung deposition studies in vivo in the rat following intratracheal admini...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章

    doi:10.1002/jps.20053

    authors: Codrons V,Vanderbist F,Ucakar B,Préat V,Vanbever R

    更新日期:2004-05-01 00:00:00

  • Separation, identification, and quantitation of anthralin and its decomposition products.

    abstract::Anthralin and its decomposition products were separated by both column chromatographic and TLC techniques. Two decomposition products were characterized by TLC, melting-point data, and UV and IR spectroscopy. Pure anthralin and its decomposition products also were determined quantitatively. ...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章

    doi:10.1002/jps.2600680340

    authors: Elsabbagh HM,Whitworth CW,Schramm LC

    更新日期:1979-03-01 00:00:00

  • Development and optimization of self-nanoemulsifying drug delivery system with enhanced bioavailability by Box-Behnken design and desirability function.

    abstract::The aim of our study was to characterize and optimize a self-nanoemulsifying drug delivery system (SNEDDS) formulation by a three-factor, three-level Box-Behnken design (BBD) combined with a desirability function. The independent factors were the amounts of Capryol PGMC (X(1)), Tween 20 (X(2)), and Transcutol HP (X(3)...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章

    doi:10.1002/jps.23333

    authors: Marasini N,Yan YD,Poudel BK,Choi HG,Yong CS,Kim JO

    更新日期:2012-12-01 00:00:00

  • Determination of propylene carbonate in pharmaceutical formulations using liquid chromatography.

    abstract::A stability-indicating reversed-phase high-performance liquid chromatographic method using a refractive index detector is described for the determination of propylene carbonate in pharmaceutical formulations. Good precision and accuracy of the method was demonstrated using an aqueous formulation. This method is also a...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章

    doi:10.1002/jps.2600740626

    authors: Cheng H,Gadde RR

    更新日期:1985-06-01 00:00:00

  • No clinically relevant pharmacokinetic and safety interactions of ambrisentan in combination with tadalafil in healthy volunteers.

    abstract::Ambrisentan is a nonsulfonamide, ET(A)-selective endothelin receptor antagonist (ERA) approved for the treatment of pulmonary arterial hypertension (PAH), and tadalafil is a phosphodiesterase type 5 (PDE-5) inhibitor under investigation for treatment of PAH. Due to the potential combination use, the pharmacokinetic (P...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章,随机对照试验

    doi:10.1002/jps.21789

    authors: Spence R,Mandagere A,Harrison B,Dufton C,Boinpally R

    更新日期:2009-12-01 00:00:00

  • Michaelis-Menten metabolite formation kinetics: equations relating area under the curve and metabolite recovery to the administered dose.

    abstract::A computational approach which concomitantly determines the capacity-limited rate constants of parent drug elimination and metabolite formation is presented. The approach applies both the presently derived total excretory recovery versus dose relationships of the metabolite and the AUC versus dose relationships of the...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章

    doi:10.1002/jps.2600791012

    authors: Chow AT,Jusko WJ

    更新日期:1990-10-01 00:00:00

  • Use of parenteral dipeptides to increase serum tyrosine levels and to enhance catecholamine-mediated neurotransmission.

    abstract::The use of intravascular tyrosine (TYR) to enhance catecholamine release in hemorrhagic shock and other cardiovascular diseases, or as a constituent of nutrient mixtures used for total parenteral nutrition, is limited by the unusually poor solubility of the amino acid in water. We have thus examined the ability of var...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章

    doi:10.1002/jps.2600790807

    authors: Maher TJ,Kiritsy PJ,Moya-Huff FA,Casacci F,De Marchi F,Wurtman RJ

    更新日期:1990-08-01 00:00:00

  • High Sensitivity Detection of a Solubility Limiting Surface Transformation of Drug Particles by DNP SENS.

    abstract::We investigate the presence of a surface species for the active pharmaceutical ingredient (API) AZD9496 with dynamic nuclear polarization surface enhanced nuclear spectroscopy (DNP SENS). We show that using DNP we can elucidate the presence of an amorphous form of the API at the surface of crystalline particles of the...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章

    doi:10.1016/j.xphs.2020.12.037

    authors: Viger-Gravel J,Pinon AC,Björgvinsdóttir S,Skantze U,Svensk Ankarberg A,Von Corswant C,Schantz S,Emsley L

    更新日期:2021-01-05 00:00:00

  • Pharmacokinetics of nitroglycerin in rats.

    abstract::The plasma nitroglycerin levels obtained after intracardial (0.7 mg/kg), oral (7 mg/kg), and topical (7--14 mg/kg) doses of nitroglycerin in rats are reported. Nitroglycerin followed essentially one-compartment kinetics after intracardial administration, showing a mean half-life of about 4 min and a mean apparent volu...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章

    doi:10.1002/jps.2600670446

    authors: Yap PS,Fung HL

    更新日期:1978-04-01 00:00:00

  • Quantitative flash-methylation analysis of phenobarbital.

    abstract::In phenobarbital measurement by GLC with the flash-methylation technique, using trimethylanilinium hydroxide as a methylating reagent, a small amount of water decomposed phenobarbital and interfered with the quantitative analysis. Thus, both the sample and the methylating reagent must be sufficiently dehydrated to att...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章

    doi:10.1002/jps.2600680938

    authors: Kurata K,Takeuchi M,Yoshida K

    更新日期:1979-09-01 00:00:00

  • STRITERFIT, a least-squares pharmacokinetic curve-fitting package using a programmable calculator.

    abstract::A program is described that permits iterative least-squares nonlinear regression fitting of polyexponential curves using the Hewlett Packard HP 41 CV programmable calculator. The program enables the analysis of pharmacokinetic drug level profiles with a high degree of precision. Up to 15 data pairs can be used, and in...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章

    doi:10.1002/jps.2600740510

    authors: Thornhill DP,Schwerzel E

    更新日期:1985-05-01 00:00:00

  • Stress Temperature Studies in Small Scale Hastelloy® Drug Substance Containers Lead to Increased Extent of and Increased Variability in Antibody-Drug Conjugate and Monoclonal Antibody Aggregation: Evidence for Novel Oxidation-Induced Crosslinking in Monoc

    abstract::Health authorities require that suitable stability of the drug substance be shown in relevant materials of construction. ICH Q1A(R2) explicitly states that "stability studies should be conducted on drug substance packaged in a container closure system that is the same as or simulates the packaging proposed for storage...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章

    doi:10.1016/j.xphs.2020.09.052

    authors: Klair N,Kim MT,Lee A,Xiao NJ,Patel AR

    更新日期:2020-10-07 00:00:00

  • Development of a Rational Design Space for Optimizing Mixing Conditions for Formation of Adhesive Mixtures for Dry-Powder Inhaler Formulations.

    abstract::The purpose of the present study was to develop guidance toward rational choice of blenders and processing conditions to make robust and high performing adhesive mixtures for dry-powder inhalers and to develop quantitative experimental approaches for optimizing the process. Mixing behavior of carrier (LH100) and Astra...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章

    doi:10.1016/j.xphs.2016.07.012

    authors: Sarkar S,Minatovicz B,Thalberg K,Chaudhuri B

    更新日期:2017-01-01 00:00:00

  • Pharmacokinetics of the anticancer agent sulofenur in mice, rats, monkeys, and dogs.

    abstract::The absorption and pharmacokinetics of sulofenur [N-(indan-5-sulfonyl)-N'-(4-chlorophenyl)urea, LY186641] and its major metabolites were examined in mice, rats, monkeys, and dogs. The compound is a diarylsulfonylurea currently being evaluated as an oncolytic agent in phase I and II trials. In all species, sulofenur wa...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章

    doi:10.1002/jps.2600820703

    authors: Ehlhardt WJ,Sullivan HR,Wood PG,Woodland JM,Hamilton M,Hamilton C,Cornpropst D,Grindey GB,Worzalla JF,Bewley JR

    更新日期:1993-07-01 00:00:00

  • Characterization of the Partition Rate of Ibuprofen Across the Water-Octanol Interface and the Influence of Common Pharmaceutical Excipients.

    abstract::This work reports the measurement of the partition rate of a model drug, ibuprofen (IBU), from aqueous solutions into octanol in the absence and presence of common pharmaceutical excipients including glucose, lactose, maltoheptaose, hydroxypropyl methylcellulose, polyvinylpyrrolidone, polyvinylpyrrolidone-vinyl acetat...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章

    doi:10.1016/j.xphs.2018.11.026

    authors: Xu H,Wang W,Shi Y,Gao P

    更新日期:2019-01-01 00:00:00

  • Linear drug release from laminated hydroxypropyl cellulose-polyvinyl acetate films.

    abstract::Release of drug from a single-layer film containing dispersed drug follows a diffusion-controlled matrix model, where the quantity released per unit area is proportional to the square root of time. The kinetics may be made linear with time (zero order) by laminating a second film without drug to the releasing side of ...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章

    doi:10.1002/jps.2600640806

    authors: Borodkin S,Tucker FE

    更新日期:1975-08-01 00:00:00

  • Developability index: a rapid in silico tool for the screening of antibody aggregation propensity.

    abstract::Determining the aggregation propensity of protein-based biotherapeutics is an important step in the drug development process. Typically, a great deal of data collected over a large period of time is needed to estimate the aggregation propensity of biotherapeutics. Thus, candidates cannot be screened early on for aggre...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章

    doi:10.1002/jps.22758

    authors: Lauer TM,Agrawal NJ,Chennamsetty N,Egodage K,Helk B,Trout BL

    更新日期:2012-01-01 00:00:00