Reformulation of a new vancomycin analog: An example of the importance of buffer species and strength.

Abstract:

:The purpose of this research was to use our previously validated dynamic injection apparatus as a rapid method for screening pH-adjusted formulations of a new vancomycin analog, Van-An, for their potential to precipitate upon dilution. In 1 vial, Van-An was reconstituted according to the manufacturer's instructions. In a separate vial, the Van-An formulation's existing phosphate buffer species was supplemented with acetate buffer, which has a pKa in the desired range: between the pH values of the formulation (pH 3.9) and blood (pH 7.4). The formulations were injected using the dynamic injection apparatus into a flowing stream of isotonic Sorensen's phosphate buffer at rates of 0.25, 0.5, 1, and 2 mL/min. The peaks obtained with the spectrophotometer were reproducible for each injection rate/formulation combination. For the phosphate-buffered formulation, the least amount of precipitation was obtained at the 0.25 mL/min injection rate. Acetate buffer was able to substantially reduce such precipitation, even at the highest injection rate. The opacity peaks for the formulation with the acetate addition were significantly smaller (P<.05) than those obtained for the unaltered formulation at all 4 injection rates. The results suggest that acetate is a better buffer species than phosphate for the pH range defined. Furthermore, we present evidence to support a generally applicable approach to screening new formulations of drug products that may be clinically useful for reducing the incidence of phlebitis in humans.

journal_name

AAPS PharmSciTech

journal_title

AAPS PharmSciTech

authors

Johnson JL,Yalkowsky SH

doi

10.1208/pt070105

subject

Has Abstract

pub_date

2006-03-01 00:00:00

pages

E33-E37

issue

1

issn

1530-9932

pii

10.1208/pt070105

journal_volume

7

pub_type

杂志文章
  • Impact of physicochemical environment on the super disintegrant functionality of cross-linked carboxymethyl sodium starch: insight on formulation precautions.

    abstract::The aim of this work is to improve the understanding of the physicochemical mechanisms involved in the functionality of cross-linked carboxymethyl sodium starch (CCSS) as a tablet super disintegrant (SD). The behavior and properties of this SD (medium uptake, disintegration times, particle size, and rheology) was inve...

    journal_title:AAPS PharmSciTech

    pub_type: 杂志文章

    doi:10.1208/s12249-014-0121-z

    authors: Delalonde M,Fitouri R,Ruiz E,Bataille B,Sharkawi T

    更新日期:2015-04-01 00:00:00

  • Preparation and characterization of a novel co-processed excipient of chitin and crystalline mannitol.

    abstract::A co-processed excipient was prepared from commercially available crystalline mannitol and α-chitin using direct compression as well as spray, wet, and dry granulation. The effect of the ratio of the two components, percentage of lubricant and particle size, on the properties of the prepared co-processed excipient has...

    journal_title:AAPS PharmSciTech

    pub_type: 杂志文章

    doi:10.1208/s12249-010-9523-8

    authors: Daraghmeh N,Rashid I,Al Omari MM,Leharne SA,Chowdhry BZ,Badwan A

    更新日期:2010-12-01 00:00:00

  • Self-associated submicron IgG1 particles for pulmonary delivery: effects of non-ionic surfactants on size, shape, stability, and aerosol performance.

    abstract::The ability to produce submicron particles of monoclonal antibodies of different sizes and shapes would enhance their application to pulmonary delivery. Although non-ionic surfactants are widely used as stabilizers in protein formulations, we hypothesized that non-ionic surfactants will affect the shape and size of su...

    journal_title:AAPS PharmSciTech

    pub_type: 杂志文章

    doi:10.1208/s12249-012-9913-1

    authors: Srinivasan AR,Shoyele SA

    更新日期:2013-03-01 00:00:00

  • Sustained Release of Poorly Water-Soluble Drug from Hydrophilic Polymeric Film Sandwiched Between Hydrophobic Layers.

    abstract::This proof-of-concept study explores the feasibility of using a drug-loaded hydrophilic polymeric layer sandwiched between two hydrophobic layers for improving film drug load while achieving sustained release of poorly water-soluble drug. Such films having total thickness in range ~ 146-250 μm were prepared by slurry-...

    journal_title:AAPS PharmSciTech

    pub_type: 杂志文章

    doi:10.1208/s12249-018-1089-x

    authors: Kevadiya BD,Zhang L,Davé RN

    更新日期:2018-08-01 00:00:00

  • Thermal Magnetic Field Activated Propolis Release From Liquid Crystalline System Based on Magnetic Nanoparticles.

    abstract::Intra-periodontal pocket drug delivery systems, such as liquid crystalline systems, are widely utilized improving the drug release control and the therapy. Propolis is used in the treatment of periodontal diseases, reducing the inflammatory and infectious conditions. Iron oxide magnetic nanoparticles (MNPs) can improv...

    journal_title:AAPS PharmSciTech

    pub_type: 杂志文章

    doi:10.1208/s12249-018-1163-4

    authors: de Alcântara Sica de Toledo L,Rosseto HC,Dos Santos RS,Spizzo F,Del Bianco L,Montanha MC,Esposito E,Kimura E,Bonfim-Mendonça PS,Svidzinski TIE,Cortesi R,Bruschi ML

    更新日期:2018-10-01 00:00:00

  • Formulation Screening and Freeze-Drying Process Optimization of Ginkgolide B Lyophilized Powder for Injection.

    abstract::The purpose of this study was to prepare ginkgolide B (GB) lyophilized powder for injection with excellent appearance and stable quality through a formulation screening and by optimizing the freeze-drying process. Cremophor EL as a solubilizer, PEG 400 as a latent solvent, and mannitol as an excipient were mixed to in...

    journal_title:AAPS PharmSciTech

    pub_type: 杂志文章

    doi:10.1208/s12249-017-0858-2

    authors: Liu D,Galvanin F,Yu Y

    更新日期:2018-02-01 00:00:00

  • Self-microemulsifying Drug Delivery System for Improved Oral Delivery of Limonene: Preparation, Characterization, in vitro and in vivo Evaluation.

    abstract::The current investigation aimed at formulating self-microemulsifying drug delivery system (SMEDDS) to ameliorate oral bioavailability of a hydrophobic functional ingredient, limonene. Solubility test, compatibility test, and pseudo-ternary phase diagrams (PTPD) were adopted to screen the optimal compositions of limone...

    journal_title:AAPS PharmSciTech

    pub_type: 杂志文章

    doi:10.1208/s12249-019-1361-8

    authors: Zhu Y,Xu W,Zhang J,Liao Y,Firempong CK,Adu-Frimpong M,Deng W,Zhang H,Yu J,Xu X

    更新日期:2019-03-26 00:00:00

  • Novel Application of Hot Melt Extrusion for the Manufacturing of Vaginal Films Containing Microbicide Candidate Dapivirine.

    abstract::Polymeric films are safe and effective and can be used for vaginal administration of microbicide drug candidates. Dapivirine (DPV), an investigational and clinically advanced antiretroviral drug, was selected as a model compound for this study. We have previously developed and clinically tested a quick-dissolving DPV ...

    journal_title:AAPS PharmSciTech

    pub_type: 杂志文章

    doi:10.1208/s12249-019-1442-8

    authors: Regev G,Patel SK,Moncla BJ,Twist J,Devlin B,Rohan LC

    更新日期:2019-06-26 00:00:00

  • Tunable Properties of Poly-DL-Lactide-Monomethoxypolyethylene Glycol Porous Microparticles for Sustained Release of Polyethylenimine-DNA Polyplexes.

    abstract::Direct pulmonary delivery is a promising step in developing effective gene therapies for respiratory disease. Gene therapies can be used to treat the root cause of diseases, rather than just the symptoms. However, developing effective therapies that do not cause toxicity and that successfully reach the target site at ...

    journal_title:AAPS PharmSciTech

    pub_type: 杂志文章

    doi:10.1208/s12249-018-1215-9

    authors: Terry TL,Givens BE,Rodgers VGJ,Salem AK

    更新日期:2019-01-02 00:00:00

  • Characterization and in vitro drug release studies of a natural polysaccharide Terminalia catappa gum (Badam gum).

    abstract::The main objective of the present study is the physicochemical characterization of naturally available Terminalia catappa gum (Badam gum [BG]) as a novel pharmaceutical excipient and its suitability in the development of gastroretentive floating drug delivery systems (GRFDDS) to retard the drug for 12 h when the dosag...

    journal_title:AAPS PharmSciTech

    pub_type: 杂志文章

    doi:10.1208/s12249-012-9873-5

    authors: Meka VS,Nali SR,Songa AS,Kolapalli VR

    更新日期:2012-12-01 00:00:00

  • Correction for irrelevant absorption in multicomponent spectrophotometric assay of riboflavin, formylmethylflavin, and degradation products: kinetic applications.

    abstract::In the spectrophotometric assay of multicomponent systems involved in drug degradation studies, some minor or unknown degradation products may be present. These products may interfere in the assay and thus invalidate the results due to their absorption in the range of analytical wavelengths. This interference may be e...

    journal_title:AAPS PharmSciTech

    pub_type: 杂志文章

    doi:10.1208/s12249-013-9998-1

    authors: Ahmad I,Qadeer K,Iqbal K,Ahmed S,Sheraz MA,Ali SA,Mirza T,Hafeez A

    更新日期:2013-09-01 00:00:00

  • Intestinal Targeting of Ganciclovir Release Employing a Novel HEC-PAA Blended Lyomatrix.

    abstract::A hydroxyethylcellulose-poly(acrylic acid) (HEC-PAA) lyomatrix was developed for ganciclovir (GCV) intestine targeting to overcome its undesirable degradation in the stomach. GCV was encapsulated within the HEC-PAA lyomatrix prepared by lyophilization. Conventional tablets were also prepared with identical GCV concent...

    journal_title:AAPS PharmSciTech

    pub_type: 杂志文章

    doi:10.1208/s12249-015-0442-6

    authors: Mabrouk M,Mulla JA,Kumar P,Chejara DR,Badhe RV,Choonara YE,du Toit LC,Pillay V

    更新日期:2016-10-01 00:00:00

  • The influence of modified pluronic F127 copolymers with higher phase transition temperature on arsenic trioxide-releasing properties and toxicity in a subcutaneous model of rats.

    abstract::Pluronic F127 (PF-127) shows thermoreversible property, which is of the utmost interest in optimizing drug formulation and delivery. However, its hitherto unresolved drawback of a low phase transition temperature (T (tr)) has limited its application in injectable drug delivery systems. We have ...

    journal_title:AAPS PharmSciTech

    pub_type: 杂志文章

    doi:10.1208/s12249-012-9756-9

    authors: Ma Y,Zhang C,Chen X,Jiang H,Pan S,Easteal AJ,Sun X

    更新日期:2012-06-01 00:00:00

  • Acoustic-resonance spectrometry as a process analytical technology for rapid and accurate tablet identification.

    abstract::This research was performed to test the hypothesis that acoustic-resonance spectrometry (ARS) is able to rapidly and accurately differentiate tablets of similar size and shape. The US Food and Drug Administration frequently orders recalls of tablets because of labeling problems (eg, the wrong tablet appears in a bottl...

    journal_title:AAPS PharmSciTech

    pub_type: 杂志文章

    doi:10.1208/pt070125

    authors: Medendorp J,Lodder RA

    更新日期:2006-03-01 00:00:00

  • Anti-Helicobacter pylori effect of mucoadhesive nanoparticles bearing amoxicillin in experimental gerbils model.

    abstract::The purpose of the present study was to design mucoadhesive gliadin nanoparticles (GNP) containing amoxicillin and to evaluate their effectiveness in eradicating Helicobacter pylori. GNP-bearing amoxicillin (AGNP) was prepared by desolvation method. The effect of process variables such as gliadin concentration and ini...

    journal_title:AAPS PharmSciTech

    pub_type: 杂志文章

    doi:10.1208/pt050232

    authors: Umamaheshwari RB,Ramteke S,Jain NK

    更新日期:2004-04-07 00:00:00

  • Quercetin in lyotropic liquid crystalline formulations: physical, chemical and functional stability.

    abstract::The purpose of this study was to develop a lyotropic liquid crystalline formulation using the emulsifier vitamin E TPGS and evaluate its behavior after incorporation of a flavonoid, quercetin. The physical (macro and microscopic), chemical (determination of quercetin content by the HPLC method) and functional (determi...

    journal_title:AAPS PharmSciTech

    pub_type: 杂志文章

    doi:10.1208/s12249-008-9091-3

    authors: Vicentini FT,Casagrande R,Verri WA Jr,Georgetti SR,Bentley MV,Fonseca MJ

    更新日期:2008-01-01 00:00:00

  • Evaluation of a new wireless Temperature Remote Interrogation System (TEMPRIS) to measure product temperature during freeze drying.

    abstract::The purpose of this research was to evaluate a new wireless and battery-free sensor technology for invasive product temperature measurement during freeze-drying. Product temperature is the most critical process parameter in a freeze-drying process, in particular during primary drying. The product temperature over time...

    journal_title:AAPS PharmSciTech

    pub_type: 杂志文章

    doi:10.1208/s12249-008-9099-8

    authors: Schneid S,Gieseler H

    更新日期:2008-01-01 00:00:00

  • Studies on formulation development of mucoadhesive sustained release itraconazole tablet using response surface methodology.

    abstract::The purpose of this research was to prepare and evaluate sustained release mucoadhesive tablets of Itraconazole. It is practically insoluble in aqueous fluids hence its solid dispersion with Eudragit E100 was prepared by spray drying. This was formulated in matrix of hydrophilic mucoadhesive polymers Carbopol 934P (CP...

    journal_title:AAPS PharmSciTech

    pub_type: 杂志文章

    doi:10.1208/s12249-008-9119-8

    authors: Madgulkar A,Kadam S,Pokharkar V

    更新日期:2008-01-01 00:00:00

  • Behavior of freezable bound water in the bacterial cellulose produced by Acetobacter xylinum: an approach using thermoporosimetry.

    abstract::The aim of the study is to examine thermal behavior of water within reticulated structure of bacterial cellulose (BC) films by sub-ambient differential scanning calorimetry (DSC). BC films with different carbon source, either manitol (BC (a)) or glycerol (BC (b)), were produced by Acetobacter xylinum using Hestrin and...

    journal_title:AAPS PharmSciTech

    pub_type: 杂志文章

    doi:10.1208/s12249-008-9104-2

    authors: Kaewnopparat S,Sansernluk K,Faroongsarng D

    更新日期:2008-01-01 00:00:00

  • Development and Evaluation of Astaxanthin as Nanostructure Lipid Carriers in Topical Delivery.

    abstract::The study is designed to formulate, optimize, and evaluate astaxanthin (ASTA)-loaded nanostructured lipid carrier (NLC) with an aim to improve its stability, water solubility, skin permeability and retention and reduce drug-related side effects. ASTA was extracted from Haematococcus pluvialis. ASTA-NLC was formulated ...

    journal_title:AAPS PharmSciTech

    pub_type: 杂志文章

    doi:10.1208/s12249-020-01822-w

    authors: Geng Q,Zhao Y,Wang L,Xu L,Chen X,Han J

    更新日期:2020-11-11 00:00:00

  • Effect of Different Nail Penetration Enhancers in Solid Lipid Nanoparticles Containing Terbinafine Hydrochloride for Treatment of Onychomycosis.

    abstract::Onychomycosis is considered a stubborn nail fungal infection that does not respond to conventional topical antifungal treatments. This study aimed to develop and characterize novel solid lipid nanoparticles (SLNs) formulae containing terbinafine HCl (TFH) and loaded with different nail penetration enhancers (nPEs). Th...

    journal_title:AAPS PharmSciTech

    pub_type: 杂志文章

    doi:10.1208/s12249-020-01893-9

    authors: Abobakr FE,Fayez SM,Elwazzan VS,Sakran W

    更新日期:2021-01-06 00:00:00

  • Terminalia gum as a directly compressible excipient for controlled drug delivery.

    abstract::The exudates from the incised trunk of Terminalia randii has been evaluated as controlled release excipient in comparison with xanthan gum and hydroxypropylmethylcellulose (HPMC) using carvedilol (water insoluble) and theophylline (water soluble) as model drugs. Matrix tablets were prepared by direct compression and t...

    journal_title:AAPS PharmSciTech

    pub_type: 杂志文章

    doi:10.1208/s12249-011-9712-0

    authors: Bamiro OA,Odeku OA,Sinha VR,Kumar R

    更新日期:2012-03-01 00:00:00

  • Release characteristics of quetiapine fumarate extended release tablets under biorelevant stress test conditions.

    abstract::The aim of the present work was the investigation of robustness and reliability of drug release from 50 to 400 mg quetiapine extended release HPMC matrix tablets towards mechanical stresses of biorelevant intensity. The tests were performed under standard conditions (USP apparatus II) as well as under simulated gastro...

    journal_title:AAPS PharmSciTech

    pub_type: 杂志文章

    doi:10.1208/s12249-013-0050-2

    authors: Garbacz G,Kandzi A,Koziolek M,Mazgalski J,Weitschies W

    更新日期:2014-02-01 00:00:00

  • Nanoparticles in Colorectal Cancer Therapy: Latest In Vivo Assays, Clinical Trials, and Patents.

    abstract::Colorectal cancer (CRC) is the third most common cancer worldwide. Its poor response to current treatment options in advanced stages and the need for efficient diagnosis in early stages call for the development of new therapeutic and diagnostic strategies. Some of them are based on the use of nanometric materials as c...

    journal_title:AAPS PharmSciTech

    pub_type: 杂志文章,评审

    doi:10.1208/s12249-020-01731-y

    authors: Cabeza L,Perazzoli G,Mesas C,Jiménez-Luna C,Prados J,Rama AR,Melguizo C

    更新日期:2020-06-26 00:00:00

  • Design of a Time-Controlled Pulsatile Release System for Propranolol Using the Dry-Coated Method: In Vitro and In Vivo Evaluation.

    abstract::The objective of this study was to design a time-controlled pulsatile release (TCPR) system containing propranolol (PNH) as an active pharmaceutical ingredient. Here, the developed dosage forms were coated with hydroxypropyl-methylcellulose (HPMC) and other excipients as barrier layer using dry-coated technology. The ...

    journal_title:AAPS PharmSciTech

    pub_type: 杂志文章

    doi:10.1208/s12249-017-0746-9

    authors: Chen K,Wang Y,Gai X,Wang H,Li Y,Wen H,Pan W,Yang X

    更新日期:2017-10-01 00:00:00

  • Polymorph transformation in paracetamol monitored by in-line NIR spectroscopy during a cooling crystallization process.

    abstract::The reliable in-line monitoring of pharmaceutical processes has been regarded as a key tool toward the full implementation of process analytical technology. In this study, near-infrared (NIR) spectroscopy was examined for use as an in-line monitoring method of the paracetamol cooling crystallization process. The drug ...

    journal_title:AAPS PharmSciTech

    pub_type: 杂志文章

    doi:10.1208/s12249-011-9642-x

    authors: Wang IC,Lee MJ,Seo DY,Lee HE,Choi Y,Kim WS,Kim CS,Jeong MY,Choi GJ

    更新日期:2011-06-01 00:00:00

  • In vitro dissolution of generic immediate-release solid oral dosage forms containing BCS class I drugs: comparative assessment of metronidazole, zidovudine, and amoxicillin versus relevant comparator pharmaceutical products in South Africa and India.

    abstract::Biowaivers are recommended for immediate-release solid oral dosage forms using dissolution testing as a surrogate for in vivo bioequivalence studies. Several guidance are currently available (the World Health Organization (WHO), the US FDA, and the EMEA) where the conditions are described. In this study, definitions, ...

    journal_title:AAPS PharmSciTech

    pub_type: 杂志文章

    doi:10.1208/s12249-014-0135-6

    authors: Reddy NH,Patnala S,Löbenberg R,Kanfer I

    更新日期:2014-10-01 00:00:00

  • Preparation and physicochemical characterization of dioctyl sodium sulfosuccinate (aerosol OT) microemulsion for oral drug delivery.

    abstract::The performance of dioctyl sodium sulfosuccinate (aerosol OT) in the development of a pharmaceutically acceptable, stable, self-emulsifying water continuous microemulsion with high dilution efficiency was assessed. A pseudoternary microemulsion system was constructed using aerosol OT/medium-chain triglycerides with ol...

    journal_title:AAPS PharmSciTech

    pub_type: 杂志文章

    doi:10.1208/pt040111

    authors: El-Laithy HM

    更新日期:2003-01-01 00:00:00

  • Trans-ungual Delivery of AR-12, a Novel Antifungal Drug.

    abstract::AR-12 is a novel small molecule with broad spectrum antifungal activity. Recently, AR-12 was found to be highly active against Trichophyton rubrum, one of the predominantly responsible organisms that cause onychomycosis. The primary objective of this project was to investigate the ability of AR-12 to penetrate into an...

    journal_title:AAPS PharmSciTech

    pub_type: 杂志文章

    doi:10.1208/s12249-017-0752-y

    authors: Kushwaha AS,Sharma P,Shivakumar HN,Rappleye C,Zukiwski A,Proniuk S,Murthy SN

    更新日期:2017-10-01 00:00:00

  • Pulmonary and Regional Deposition of Nebulized and Dry Powder Aerosols in Ferrets.

    abstract::The utilization of ferrets as a non-clinical model for disease is rapidly increasing within drug development. Many of these models include respiratory diseases that involve targeted drug delivery via nose-only inhalation. While the deposition patterns within other non-clinical models (mice, rats, canines, and non-huma...

    journal_title:AAPS PharmSciTech

    pub_type: 杂志文章

    doi:10.1208/s12249-019-1382-3

    authors: Kuehl PJ,Chand R,McDonald JD,Hava DL,DeHaan WH

    更新日期:2019-07-01 00:00:00