Excipient selection can significantly affect solid-state phase transformation in formulation during wet granulation.

Abstract:

:Phase transformations in formulations can lead to instability in physicochemical, biopharmaceutical, and processing properties of products. The influences of formulation design on the optimal dosage forms should be specified. The aim here was to investigate whether excipients with different water sorption behavior affect hydrate formation of nitrofurantoin in wet masses. Nitrofurantoin anhydrate was used as a hydrate-forming model drug, and 4 excipients with different water-absorbing potential (amorphous low-substituted hydroxypropylcellulose, modified maize starch, partially amorphous silicified microcrystalline cellulose, and crystalline alpha-lactose monohydrate) were granulated with varying amounts of purified water. Off-line evaluation of wet masses containing nitrofurantoin anhydrate and excipient (1:1) was performed using an X-ray powder diffractometer (XRPD) and near-infrared spectroscopy, and drying phase was evaluated by variable temperature XRPD. Only amorphous excipient in the formulation retarded hydrate formation of an active pharmaceutical ingredient (API) at high water contents. Hygroscopic partially crystalline excipient hindered hydrate formation of API at low water contents. Crystalline excipient was unable to control hydrate formation of API. The character of excipient affects the stability of formulation. Thus, correct selection of excipients for the formulation can control processing-induced phase transitions and improve the storage stability of the final dosage form.

journal_name

AAPS PharmSciTech

journal_title

AAPS PharmSciTech

authors

Airaksinen S,Karjalainen M,Kivikero N,Westermarck S,Shevchenko A,Rantanen J,Yliruusi J

doi

10.1208/pt060241

keywords:

subject

Has Abstract

pub_date

2005-10-06 00:00:00

pages

E311-22

issue

2

issn

1530-9932

journal_volume

6

pub_type

杂志文章
  • Fabrication of modified transport fluconazole transdermal spray containing ethyl cellulose and Eudragit RS100 as film formers.

    abstract::The present investigation was undertaken to fabricate modified transport fluconazole transdermal spray using ethyl cellulose and Eudragit RS100 as film-forming polymers. Eudragit RS100 (X(1)) and ethyl cellulose (X(2)) were selected as independent variables in 3(2) full factorial design, whereas drug transport in firs...

    journal_title:AAPS PharmSciTech

    pub_type: 杂志文章

    doi:10.1208/s12249-009-9256-8

    authors: Gohel MC,Nagori SA

    更新日期:2009-01-01 00:00:00

  • Design and Evaluation of Hydrophilic Matrix System for pH-Independent Sustained Release of Weakly Acidic Poorly Soluble Drug.

    abstract::The aim of this research was to design and evaluate a hydrophilic matrix system for sustained release of glipizide, a weakly acidic poor soluble drug. A combination of inclusion complexation and microenvironmental pH modification techniques was utilized to improve the dissolution and pH-independent release of glipizid...

    journal_title:AAPS PharmSciTech

    pub_type: 杂志文章

    doi:10.1208/s12249-018-1008-1

    authors: Huang J,Lin H,Peng B,Huang Q,Shuai F,Xie Y

    更新日期:2018-07-01 00:00:00

  • Development of Methotrexate and Minocycline Loaded Nanoparticles for the Effective Treatment of Rheumatoid Arthritis.

    abstract::Rheumatoid arthritis is an autoimmune disease that leads to cartilage destruction, synovial joint inflammation, and bacterial joint/bone infections. In the present work, methotrexate and minocycline-loaded nanoparticles (MMNPs) were developed with an aim to provide relief from inflammation and disease progression/join...

    journal_title:AAPS PharmSciTech

    pub_type: 杂志文章

    doi:10.1208/s12249-019-1581-y

    authors: Janakiraman K,Krishnaswami V,Sethuraman V,Natesan S,Rajendran V,Kandasamy R

    更新日期:2019-12-23 00:00:00

  • Formulation study and evaluation of matrix and three-layer tablet sustained drug delivery systems based on Carbopols with isosorbite mononitrate.

    abstract::The purpose of this research was to develop and evaluate different preparations of sustained delivery systems, using Carbopols as carriers, in the form of matrices and three-layer tablets with isosorbite mononitrate. Matrix tablets were prepared by direct compression whereas three-layer tablets were prepared by compre...

    journal_title:AAPS PharmSciTech

    pub_type: 杂志文章

    doi:10.1208/s12249-008-9084-2

    authors: Efentakis M,Peponaki C

    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

  • Pharmaceutical and pharmacokinetic evaluation of a novel fast dissolving film formulation of flupentixol dihydrochloride.

    abstract::The objective of the present study was to develop fast dissolving oral film of the antipsychotic drug, flupentixol dihydrochloride, to enhance its bioavailability, optimize its therapeutic effect when used to treat depression with anxiety, and increase the convenience and compliance by the mentally ill, developmentall...

    journal_title:AAPS PharmSciTech

    pub_type: 杂志文章,随机对照试验

    doi:10.1208/s12249-014-0186-8

    authors: Abdelbary A,Bendas ER,Ramadan AA,Mostafa DA

    更新日期:2014-12-01 00:00:00

  • Zolendronic Acid-Conjugated PLGA Ultrasmall Nanoparticle Loaded with Methotrexate as a Supercarrier for Bone-Targeted Drug Delivery.

    abstract::Drug delivery to deep-seated tissues such as bone has been a major complication till date. This preferential drug delivery is further important in targeting anti-tumour agents to bone metastasis owing to its complexity. The present study involves the formulation of PLGA nanoparticles and conjugation with zolendronic a...

    journal_title:AAPS PharmSciTech

    pub_type: 杂志文章

    doi:10.1208/s12249-016-0691-z

    authors: Raichur V,Vemula KD,Bhadri N,Razdan R

    更新日期:2017-08-01 00:00:00

  • Synthesis of a semi-interpenetrating polymer network as a bioactive curcumin film.

    abstract::This study focused on the synthesis and characterization of a natural polymeric system employing the interpenetrating polymer network (IPN) comprising curcumin as a bioactive. Biopolymers and actives such as chitosan, hypromellose, citric acid, genipin, and curcumin were used to develop an effective, biodegradable, an...

    journal_title:AAPS PharmSciTech

    pub_type: 杂志文章

    doi:10.1208/s12249-014-0170-3

    authors: Mayet N,Kumar P,Choonara YE,Tomar LK,Tyagi C,du Toit LC,Pillay V

    更新日期:2014-12-01 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

  • Influence of pH modifiers and HPMC viscosity grades on nicotine-magnesium aluminum silicate complex-loaded buccal matrix tablets.

    abstract::Hydroxypropyl methylcellulose (HPMC) tablets containing nicotine-magnesium aluminum silicate (NCT-MAS) complex particles and pH modifiers, namely, sodium chloride, citric acid, and magnesium hydroxide, were prepared using the direct compression method. The effects of HPMC viscosity grades and pH modifiers on NCT relea...

    journal_title:AAPS PharmSciTech

    pub_type: 杂志文章

    doi:10.1208/s12249-012-9790-7

    authors: Pongjanyakul T,Kanjanabat S

    更新日期:2012-06-01 00:00:00

  • Formulation of a novel tianeptine sodium orodispersible film.

    abstract::The present investigation was undertaken with the objective of formulating orodispersible film(s) of the antidepressant drug tianeptine sodium to enhance the convenience and compliance by the elderly and pediatric patients. The novel film former, lycoat NG73 (granular hydroxypropyl starch), along with different film-f...

    journal_title:AAPS PharmSciTech

    pub_type: 杂志文章

    doi:10.1208/s12249-010-9464-2

    authors: El-Setouhy DA,Abd El-Malak NS

    更新日期:2010-09-01 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

  • Preparation of Ergosterol-Loaded Nanostructured Lipid Carriers for Enhancing Oral Bioavailability and Antidiabetic Nephropathy Effects.

    abstract::In our previously studies, we confirmed that ergosterol could ameliorate diabetic nephropathy by suppressing the proliferation of mesangial cells and the accumulation of extracellular matrix (ECM). However, the therapeutic application of ergosterol may be confined due to poor aqueous solubility and low oral bioavailab...

    journal_title:AAPS PharmSciTech

    pub_type: 杂志文章

    doi:10.1208/s12249-019-1597-3

    authors: Dong Z,Iqbal S,Zhao Z

    更新日期:2020-01-13 00:00:00

  • Thermally Induced Denaturing Energetics of Human Blood Plasma Albumin by Differential Scanning Calorimetry (DSC) as an Indicator for Breast Cancer Diagnosis in Female Patients.

    abstract::Cancerous invasion yields unusual metabolisms providing a significant amount of peptide albuminomes that modulate albumin stability via binding. The study aimed at the investigation of the thermal stability of human plasma albumin with breast cancer of various stages by means of differential scanning calorimetry (DSC)...

    journal_title:AAPS PharmSciTech

    pub_type: 杂志文章

    doi:10.1208/s12249-019-1356-5

    authors: Faroongsarng D,Sunpaweravong S,Raksawong A

    更新日期:2019-03-18 00:00:00

  • The Influence of Simulated Fasted Gastrointestinal pH Profiles on Diclofenac Sodium Dissolution in a Glass-Bead Flow-Through System.

    abstract::High inter- and intra-individual variability in the pH of fluids in the human gastrointestinal (GI) tract has been described in the literature. The aim of this study was to assess the influence of physiological variability in fasted pH profiles of media along the GI tract on diclofenac sodium (DF-Na) dissolution from ...

    journal_title:AAPS PharmSciTech

    pub_type: 杂志文章

    doi:10.1208/s12249-018-1140-y

    authors: Felicijan T,Pišlar M,Vene K,Bogataj M

    更新日期:2018-10-01 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

  • Preparation of gelatin microbeads with a narrow size distribution using microchannel emulsification.

    abstract::The purpose of this study was to prepare monodisperse gelatin microcapsules containing an active agent using microchannel (MC) emulsification, a novel technique for preparing water-in-oil (W/O) and oil-in-water (O/W) emulsions. As the first step in applying MC emulsification to the preparation of monodisperse gelatin ...

    journal_title:AAPS PharmSciTech

    pub_type: 杂志文章

    doi:10.1208/pt030325

    authors: Iwamoto S,Nakagawa K,Sugiura S,Nakajima M

    更新日期:2002-01-01 00:00:00

  • Advanced technologies for oral controlled release: cyclodextrins for oral controlled release.

    abstract::Cyclodextrins (CDs) are used in oral pharmaceutical formulations, by means of inclusion complexes formation, with the following advantages for the drugs: (1) solubility, dissolution rate, stability, and bioavailability enhancement; (2) to modify the drug release site and/or time profile; and (3) to reduce or prevent g...

    journal_title:AAPS PharmSciTech

    pub_type: 杂志文章,评审

    doi:10.1208/s12249-011-9690-2

    authors: Salústio PJ,Pontes P,Conduto C,Sanches I,Carvalho C,Arrais J,Marques HM

    更新日期:2011-12-01 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

  • Biopharmaceutics classification system-based biowaivers for generic oncology drug products: case studies.

    abstract::Establishing bioequivalence (BE) of drugs indicated to treat cancer poses special challenges. For ethical reasons, often, the studies need to be conducted in cancer patients rather than in healthy volunteers, especially when the drug is cytotoxic. The Biopharmaceutics Classification System (BCS) introduced by Amidon (...

    journal_title:AAPS PharmSciTech

    pub_type: 杂志文章,评审

    doi:10.1208/s12249-014-0195-7

    authors: Tampal N,Mandula H,Zhang H,Li BV,Nguyen H,Conner DP

    更新日期:2015-02-01 00:00:00

  • New insights into the pelletization mechanism by extrusion/spheronization.

    abstract::Pellet manufacturing by extrusion/spheronization is quite common in the pharmaceutical field because the obtained product is characterized by a high sphericity as well as a narrow particle size distribution. The established mechanisms only consider deformation of the initially fractured particles but do not account fo...

    journal_title:AAPS PharmSciTech

    pub_type: 杂志文章

    doi:10.1208/s12249-010-9532-7

    authors: Koester M,Thommes M

    更新日期:2010-12-01 00:00:00

  • GM-144, a novel lipophilic vaginal contraceptive gel-microemulsion.

    abstract::In a systematic effort to develop a dual-function intravaginal spermicide as well as a drug delivery vehicle against sexually transmitted pathogens, a submicron particle size (30-80 nm), lipophilic and spermicidal gel-microemulsion (viz GM-144) containing the pharmaceutical excipients propylene glycol, Captex 300, Cre...

    journal_title:AAPS PharmSciTech

    pub_type: 杂志文章

    doi:10.1208/pt020205

    authors: D'Cruz OJ,Yiv SH,Uckun FM

    更新日期:2001-04-09 00:00:00

  • In vitro permeability enhancement in intestinal epithelial cells (Caco-2) monolayer of water soluble quaternary ammonium chitosan derivatives.

    abstract::The aim of this study was to investigate the effects of a type of hydrophobic moiety, extent of N-substitution (ES), and degree of quaternization (DQ) of chitosan (CS) on the transepithelial electrical resistance and permeability of Caco-2 cells monolayer, using fluorescein isothiocyanate dextran 4,400 (FD-4) as the m...

    journal_title:AAPS PharmSciTech

    pub_type: 杂志文章

    doi:10.1208/s12249-010-9399-7

    authors: Kowapradit J,Opanasopit P,Ngawhirunpat T,Apirakaramwong A,Rojanarata T,Ruktanonchai U,Sajomsang W

    更新日期:2010-06-01 00:00:00

  • To Evaluate the Effect of Solvents and Different Relative Humidity Conditions on Thermal and Rheological Properties of Microcrystalline Cellulose 101 Using METHOCEL™ E15LV as a Binder.

    abstract::The solvent used for preparing the binder solution in wet granulation can affect the granulation end point and also impact the thermal, rheological, and flow properties of the granules. The present study investigates the effect of solvents and percentage relative humidity (RH) on the granules of microcrystalline cellu...

    journal_title:AAPS PharmSciTech

    pub_type: 杂志文章

    doi:10.1208/s12249-015-0424-8

    authors: Jagia M,Trivedi M,Dave RH

    更新日期:2016-08-01 00:00:00

  • Pulmonary Administration of Microparticulate Antisense Oligonucleotide (ASO) for the Treatment of Lung Inflammation.

    abstract::Targeted delivery to the lung for controlling lung inflammation is an area that we have explored in this study. The purpose was to use microparticles containing an antisense oligonucleotide (ASO) to NF-κB to inhibit the production of proinflammatory cytokines. Microparticles were prepared using the B-290 Buchi Spray D...

    journal_title:AAPS PharmSciTech

    pub_type: 杂志文章

    doi:10.1208/s12249-018-1002-7

    authors: Ubale RV,Shastri PN,Oettinger C,D'Souza MJ

    更新日期:2018-05-01 00:00:00

  • Synthesis, Formulation, and Characterization of Doxorubicin-Loaded Laponite/Oligomeric Hyaluronic Acid-Aminophenylboronic Acid Nanohybrids and Cytological Evaluation against MCF-7 Breast Cancer Cells.

    abstract::As a synthetic clay material, laponite RDS (LR) was investigated as an effective drug carrier as a result of the special nanodisk structure together with the negative-charged surface to achieve enhanced cellular uptake and targeted delivery. In this research work, the synthesized oligomeric hyaluronic acid-aminophenyl...

    journal_title:AAPS PharmSciTech

    pub_type: 杂志文章

    doi:10.1208/s12249-019-1533-6

    authors: Yang Y,Li J,Chen F,Qiao S,Li Y,Pan W

    更新日期:2019-11-20 00:00:00

  • 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. I...

    journal_title:AAPS PharmSciTech

    pub_type: 杂志文章

    doi:10.1208/pt070105

    authors: Johnson JL,Yalkowsky SH

    更新日期:2006-03-01 00:00:00

  • Effect of degree of esterification of pectin and calcium amount on drug release from pectin-based matrix tablets.

    abstract::The aim of this work was to assess the effect of 2 formulation variables, the pectin type (with different degrees of esterification [DEs]) and the amount of calcium, on drug release from pectin-based matrix tablets. Pectin matrix tablets were prepared by blending indomethacin (a model drug), pectin powder, and various...

    journal_title:AAPS PharmSciTech

    pub_type: 杂志文章

    doi:10.1208/pt050109

    authors: Sungthongjeen S,Sriamornsak P,Pitaksuteepong T,Somsiri A,Puttipipatkhachorn S

    更新日期:2004-02-12 00:00:00

  • Influence of Polyvinyl Alcohol (PVA) on PVA-Poly-N-hydroxyethyl-aspartamide (PVA-PHEA) Microcrystalline Solid Dispersion Films.

    abstract::This study was conducted to formulate buccal films consisting of polyvinyl alcohol (PVA) and poly-N-hydroxyethyl-aspartamide (PHEA), to improve the dissolution of the drug through the oral mucosa. Ibuprofen sodium salt was used as a model drug, and the buccal film was expected to enhance its dissolution rate. Two diff...

    journal_title:AAPS PharmSciTech

    pub_type: 杂志文章

    doi:10.1208/s12249-020-01811-z

    authors: Al-Sahaf Z,Raimi-Abraham B,Licciardi M,de Mohac LM

    更新日期:2020-10-02 00:00:00

  • Enhancing and sustaining AMG 009 dissolution from a matrix tablet via microenvironmental pH modulation and supersaturation.

    abstract::The objective of this study was to investigate the combined effect of pH modifiers and nucleation inhibitors on enhancing and sustaining the dissolution of AMG 009 tablet via supersaturation. Several bases and polymers were added as pH modifiers and nucleation inhibitors, respectively, to evaluate their impact on the ...

    journal_title:AAPS PharmSciTech

    pub_type: 杂志文章

    doi:10.1208/s12249-011-9679-x

    authors: Bi M,Kyad A,Kiang YH,Alvarez-Nunez F,Alvarez F

    更新日期:2011-12-01 00:00:00