Solid-state characterization of fluconazole.

Abstract:

:Two polymorphs and three solvates of fluconazole were isolated and characterized by x-ray powder diffractometry, IR spectroscopy, differential scanning calorimetry (DSC), thermogravimetry, and their dissolution rates. The different forms were prepared by crystallization of the original powder in different solvents at different cooling rates. X-ray diffraction patterns of the five solid modifications exhibited substantial differences in both the intensity and position of the peaks. FTIR spectra of the five different solid-state modifications also exhibited differences in the peaks' positions and intensities. DSC thermogram of anhydrate form I showed a single melting point at 139.2 degrees C. Anhydrate form II showed two endothermic peaks at 136.5 and 139.2 degrees C and one exothermic peak in between. The DSC thermogram of acetone 1/4 solvate exhibited two endothermic peaks at 75.5 and 139.2 degrees C. Benzene 1/7 solvate exhibited two endothermic peaks at 131.5 and 138.8 degrees C. Hydrate E exhibited two endothermic peaks at 102.7 and 139.2 degrees C. The DSC thermogram of anhydrate form II showed that this form is sensitive to the application of a mechanical force. The solubility study showed that anhydrate form II and acetone 1/4 solvate have higher solubilities than anhydrate form I while benzene 1/7 solvate and monohydrate have lower solubilities than anhydrate form I. The intrinsic dissolution study confirmed these results.

journal_name

Pharm Dev Technol

authors

Alkhamis KA,Obaidat AA,Nuseirat AF

doi

10.1081/pdt-120015052

subject

Has Abstract

pub_date

2002-11-01 00:00:00

pages

491-503

issue

4

eissn

1083-7450

issn

1097-9867

journal_volume

7

pub_type

杂志文章
  • A method for the preparation of sustained release-coated Metoprolol Succinate pellet-containing tablets.

    abstract::The purpose of this study was to develop a method to prepare Metoprolol Succinate (MS) sustained release pellets and compress them into pellet-containing tablets without losing sustained release property. The drug layered pellets were coated with Eudragit NE 30D to obtain a sustained release (SR) property. The mechani...

    journal_title:Pharmaceutical development and technology

    pub_type: 杂志文章

    doi:10.3109/10837450.2015.1081612

    authors: Yang Z,Yu J,Yang T,Xing H,Zhang J,Xian L,Ding P,Wang D

    更新日期:2016-12-01 00:00:00

  • Characterization of nano oxaliplatin prepared by novel Fat Employing Supercritical Nano System, the FESNS®.

    abstract:BACKGROUND:Oxaliplatin has long been used for the treatment of colorectal cancer via intra-venous infusion. In order to improve patient compliance, a solid dosage form for oral administration of oxaliplatin was prepared as nano-sized particles. METHOD:Nano oxaliplatin was prepared employing Fat Employing Supercritical...

    journal_title:Pharmaceutical development and technology

    pub_type: 杂志文章

    doi:10.3109/10837450.2010.531735

    authors: Lee SJ,Kim YH,Lee SH,Hahn M

    更新日期:2012-03-01 00:00:00

  • Effect of sample preparation method on quantification of polymorphs using PXRD.

    abstract::The purpose of this study was to improve the sensitivity and accuracy of quantitative analysis of polymorphic mixtures. Various techniques such as hand grinding and mixing (in mortar and pestle), air jet milling and ball milling for micronization of particle and mixing were used to prepare binary mixtures. Using these...

    journal_title:Pharmaceutical development and technology

    pub_type: 杂志文章

    doi:10.3109/10837450903286511

    authors: Alam S,Patel S,Bansal AK

    更新日期:2010-09-01 00:00:00

  • The absorption of (99m)Tc-alendronate given by rectal route in rabbits.

    abstract::Alendronate sodium (ALD) is a bisphosphonate medication used in the treatment and prevention of osteoporosis. Absorption of ALD as oral formulation is very poor (0.5%-1%). Its bioavailability can decrease with food effect. It has some gastrointestinal adverse effects such as gastritis, gastric ulcer, and esophagitis. ...

    journal_title:Pharmaceutical development and technology

    pub_type: 杂志文章

    doi:10.1080/10837450801949509

    authors: Asikoğlu M,Ozguney I,Ozcan I,Orumlu O,Guneri T,Koseoğlu K,Ozkilic H

    更新日期:2008-01-01 00:00:00

  • The preparation of rapidly disintegrating tablets in the mouth.

    abstract::Elderly people, children and patients sometimes have difficulties swallowing tablets. To solve this problem, a novel method of preparing tablets that disintegrate rapidly in the mouth was developed. A tablet with high porosity is required for rapid disintegration, but such a tablet is generally fragile. To make a tabl...

    journal_title:Pharmaceutical development and technology

    pub_type: 杂志文章

    doi:10.1081/pdt-120000287

    authors: Sugimoto M,Matsubara K,Koida Y,Kobayashi M

    更新日期:2001-11-01 00:00:00

  • Estimation of initial dissolution rate of drug substance by thermal analysis: application for carbamazepine hydrate.

    abstract::We have proposed a theory indicating the correlation between the dissolution rate and the heat of solution of drug substances. The initial dissolution rates of the drug substances containing amorphous were predicted accurately from their heats of solution. In this report, the possibility for the theory to estimate the...

    journal_title:Pharmaceutical development and technology

    pub_type: 杂志文章

    doi:10.1081/pdt-120002234

    authors: Yoshihashi Y,Yonemochi E,Terada K

    更新日期:2002-01-01 00:00:00

  • Investigation of propellant-free aqueous foams as pharmaceutical carrier systems.

    abstract::Due to their light consistency and good spreadability, aqueous foams are considered as convenient and highly accepted drug carrier systems that are of great importance in the field of topical drug delivery. The production of a stable, easy to dose, preferably environmentally harmless foam formulation is challenging. T...

    journal_title:Pharmaceutical development and technology

    pub_type: 杂志文章

    doi:10.1080/10837450.2020.1863426

    authors: Farkas D,Kállai-Szabó N,Sárádi-Kesztyűs Á,Lengyel M,Magramane S,Kiss É,Antal I

    更新日期:2020-12-27 00:00:00

  • Preparation and in vitro characterization of diltiazem hydrochloride loaded alginate microspheres.

    abstract::The main objective of the present study was to improve bioavailability of diltiazem hydrochloride and decrease the frequency of dosage form administration by increasing the encapsulation efficiency of the drug, residence time of the dosage form at the site of absorption and sustained release of the drug from the deliv...

    journal_title:Pharmaceutical development and technology

    pub_type: 杂志文章

    doi:10.1080/10837450802626304

    authors: Sultana Y,Mall S,Maurya DP,Kumar D,Das M

    更新日期:2009-01-01 00:00:00

  • Isolation technology for research and development applications: from concept to production.

    abstract::A prototype parenteral manufacturing facility based on isolation technology was designed, constructed, and commissioned at Warner-Lambert Co., Morris Plains, NJ, with emphasis on its application to research and development (R&D) settings. The facility contains closed isolators for holding, transferring, and manufactur...

    journal_title:Pharmaceutical development and technology

    pub_type: 杂志文章

    doi:10.1081/pdt-100102034

    authors: Krishna AK,Lodhi SA,Harris MR

    更新日期:2000-01-01 00:00:00

  • Formulation strategy of nitrofurantoin: co-crystal or solid dispersion?

    abstract::Poor solubility and bioavailability of drugs are often affected by its microscopic structural properties. Nitrofurantoin (NF), a Biopharmaceutics Classification System class II item, has a low water solubility with low plasma concentrations. To improve its therapeutic efficacy, formulation strategy of solid dispersion...

    journal_title:Pharmaceutical development and technology

    pub_type: 杂志文章

    doi:10.1080/10837450.2019.1689401

    authors: Teoh XY,Bt Mahyuddin FN,Ahmad W,Chan SY

    更新日期:2020-02-01 00:00:00

  • Conjugates of TAT and folate with DOX-loaded chitosan micelles offer effective intracellular delivery ability.

    abstract::The key for better antitumor efficacy is to improve the specificity of antitumor drugs for tumor cells and diminish their cytotoxicity to normal tissues. Targeted nanoparticles as antitumor drug delivery system can resolve this problem. In this study, we prepared folate and TAT (arginine-rich cell-penetrating peptide)...

    journal_title:Pharmaceutical development and technology

    pub_type: 杂志文章

    doi:10.1080/10837450.2018.1469147

    authors: Zhang S,Liu Y,Gan Y,Qiu N,Gu Y,Zhu H

    更新日期:2019-02-01 00:00:00

  • Evaluation of PLGA microsphere size effect on myotoxicity using the isolated rodent skeletal muscle model.

    abstract::The present work investigated the magnitude of microsphere-induced acute myotoxicity and determined whether this myotoxicity is related to microsphere size and/or reconstitution solvent. Using a high molecular weight poly(dl-lactide-co-glycolide) copolymer, the myotoxicity of two different size microsphere formulation...

    journal_title:Pharmaceutical development and technology

    pub_type: 杂志文章

    doi:10.3109/10837459609022596

    authors: Brazeau GA,Sciame M,al-Suwayeh SA,Fattal E

    更新日期:1996-10-01 00:00:00

  • Polyamidoamine (PAMAM) dendrimers as potential release modulators and oral bioavailability enhancers of vardenafil hydrochloride.

    abstract::Vardenafil hydrochloride (VAR) is an erectile dysfunction treating drug. VAR has a short elimination half-life (4-5 h) and suffers low oral bioavailability (15%). This work aimed to explore the dual potential of VAR-dendrimer complexes as drug release modulators and oral bioavailability enhancers. VAR-dendrimer comple...

    journal_title:Pharmaceutical development and technology

    pub_type: 杂志文章

    doi:10.1080/10837450.2018.1472611

    authors: Tawfik MA,Tadros MI,Mohamed MI

    更新日期:2019-03-01 00:00:00

  • Preparation and characterization of letrozole-loaded poly(d,l-lactide) nanoparticles for drug delivery in breast cancer therapy.

    abstract::Letrozole (LTZ), an aromatase inhibitor used for the treatment of hormonally-positive breast cancer in postmenopausal women, has poor water solubility, rapid metabolism, and a range of side effects. In this study, polymer-based nanoparticles (NPs) incorporating the drug have been designed and characterized, aimed to c...

    journal_title:Pharmaceutical development and technology

    pub_type: 杂志文章

    doi:10.1080/10837450.2018.1455698

    authors: Alemrayat B,Elhissi A,Younes HM

    更新日期:2019-02-01 00:00:00

  • A quality by design approach using artificial intelligence techniques to control the critical quality attributes of ramipril tablets manufactured by wet granulation.

    abstract::Quality by design (QbD) is an essential part of the modern approach to pharmaceutical quality. This study was conducted in the framework of a QbD project involving ramipril tablets. Preliminary work included identification of the critical quality attributes (CQAs) and critical process parameters (CPPs) based on the qu...

    journal_title:Pharmaceutical development and technology

    pub_type: 杂志文章

    doi:10.3109/10837450.2012.705294

    authors: Aksu B,Paradkar A,de Matas M,Özer Ö,Güneri T,York P

    更新日期:2013-02-01 00:00:00

  • Release kinetics of a controlled-release multiparticulate dosage form prepared using a hot-melt fluid bed coating method.

    abstract::Dissolution profiles of various multiparticulate controlled-release dosage forms prepared by applying lipophilic materials using a hot-melt coating technique were analyzed to determine release kinetics. The dosage forms were prepared using a novel solid dispersion hot-melt fluid bed coating method. Various lipophilic ...

    journal_title:Pharmaceutical development and technology

    pub_type: 杂志文章

    doi:10.1080/10837459908984231

    authors: Griffin EN,Niebergall PJ

    更新日期:1999-01-01 00:00:00

  • Use of poloxamer polymers to stabilize recombinant human growth hormone against various processing stresses.

    abstract::Several processing and shipping stresses were investigated for their effect on the physical stability of recombinant human growth hormone (rhGH). These included exposure to air/water interfaces, adsorption to hydrophobic surfaces, freeze-thaw cycles, and temperature. The interfacially and thermally denatured hormone w...

    journal_title:Pharmaceutical development and technology

    pub_type: 杂志文章

    doi:10.3109/10837459709022619

    authors: Katakam M,Banga AK

    更新日期:1997-05-01 00:00:00

  • Formulation development and systematic optimization of stabilized ziprasidone hydrochloride capsules devoid of any food effect.

    abstract:CONTEXT AND OBJECTIVE:The objective of the study was to develop a stable capsule formulation of ziprasidone hydrochloride which can be administered without regards to food intake. MATERIALS AND METHODS:The unstable anhydrous form of ziprasidone hydrochloride was stabilized employing hot-melt extrusion and further opti...

    journal_title:Pharmaceutical development and technology

    pub_type: 杂志文章

    doi:10.3109/10837450.2015.1055764

    authors: Banerjee S,Shankar KR,Prasad Y R

    更新日期:2016-11-01 00:00:00

  • Effect of storage conditions on the recrystallization of drugs in solid dispersions with crospovidone.

    abstract::The physical stability of amorphous solid dispersions (SDs) is influenced by their storage conditions. The goal of this work was to investigate the factors affecting the recrystallization of drugs in SDs after storage under conditions of high temperature and high humidity. SDs of three drugs (dipyridamole, nifedipine ...

    journal_title:Pharmaceutical development and technology

    pub_type: 杂志文章

    doi:10.3109/10837450.2013.795168

    authors: Shibata Y,Fujii M,Suzuki A,Koizumi N,Kanada K,Yamada M,Watanabe Y

    更新日期:2014-06-01 00:00:00

  • Development and in vivo evaluation of baicalin-loaded W/O nanoemulsion for lymphatic absorption.

    abstract::Background: Lymphatic formations that effectively eradicate the virus in the lymphatic system will be therapeutically advantagous in hepatitis B virus (HBV) infection. Lipid-based formulation is often used to deliver drug via the lymphatic system. Baicalin nanoemulsion may be a promising drug delivery system for impro...

    journal_title:Pharmaceutical development and technology

    pub_type: 杂志文章

    doi:10.1080/10837450.2019.1646757

    authors: Xu Q,Zhou A,Wu H,Bi Y

    更新日期:2019-11-01 00:00:00

  • The development and in vitro evaluation of herbal pellets coated with Eudragit FS 30.

    abstract::The objective of this study was to prepare pellets of thyme (Thymus vulgaris L.), stinging nettle (Urtica dioica L.) and sage (Salvia officinalis L.) dry extracts by extrusion-spheronization technique to improve technological properties and investigate dissolution profiles of pellets covered different levels of pH-sen...

    journal_title:Pharmaceutical development and technology

    pub_type: 杂志文章

    doi:10.3109/10837450.2014.920355

    authors: Kaledaite R,Bernatoniene J,Dvořáčková K,Gajdziok J,Muselík J,Pečiūra R,Masteikova R

    更新日期:2015-11-01 00:00:00

  • The impact of crystallinity on Brequinar sodium hygroscopicity.

    abstract::The hygroscopicity of Brequinar sodium, an organ transplant immunosuppressant, at 75% relative humidity highly depends on the crystal form or crystallinity of the drug substance. Hygroscopicity and ease of water uptake of three lots of Brequinar sodium were investigated. Those lots contained different impurities at le...

    journal_title:Pharmaceutical development and technology

    pub_type: 杂志文章

    doi:10.3109/10837459609031417

    authors: Wu LS,Pang J,Hussain MA

    更新日期:1996-04-01 00:00:00

  • Preparation of a reproducible long-acting formulation of risperidone-loaded PLGA microspheres using microfluidic method.

    abstract::The aim of the present study is to prepare risperidone-loaded poly lactic-co-glycolic acid (PLGA) microspheres within microfluidic system and to achieve a formulation with uniform size and monotonic and reproducible release profile. In comparison to batch method, T-junction and serpentine chips were utilized and optim...

    journal_title:Pharmaceutical development and technology

    pub_type: 杂志文章

    doi:10.1080/10837450.2016.1221426

    authors: Jafarifar E,Hajialyani M,Akbari M,Rahimi M,Shokoohinia Y,Fattahi A

    更新日期:2017-09-01 00:00:00

  • Dual drug nanocrystals loaded microparticles for fixed dose combination of simvastatin and ezetimibe.

    abstract::Dual drug nanocrystals loaded nano embedded microparticles (DNEMs) were prepared for fixed dose combination of simvastatin (SIM) and ezetimibe (EZE) using NanoCrySP technology. The purpose was to generate nanonized SIM and EZE dispersed in matrix of single crystallization inducing excipient and investigate their in vi...

    journal_title:Pharmaceutical development and technology

    pub_type: 杂志文章

    doi:10.1080/10837450.2019.1669181

    authors: Nandi S,Kaur A,Bansal AK

    更新日期:2020-01-01 00:00:00

  • Controlled delivery of the antiprotozoal agent (tinidazole) from intravaginal polymer matrices for treatment of the sexually transmitted infection, trichomoniasis.

    abstract::Microporous polymeric matrices prepared from poly(ɛ-caprolactone) [PCL] were evaluated for controlled vaginal delivery of the antiprotozoal agent (tinidazole) in the treatment of the sexually transmitted infection, trichomoniasis. The matrices were produced by rapidly cooling co-solutions of PCL and tinidazole in acet...

    journal_title:Pharmaceutical development and technology

    pub_type: 杂志文章

    doi:10.1080/10837450.2018.1481430

    authors: Fernando HV,Chan LL,Dang N,Santhanes D,Banneheke H,Nalliah S,Coombes AGA

    更新日期:2019-03-01 00:00:00

  • A new method for evaluating the dissolution of orodispersible films.

    abstract::The aim of this research was to develop and assess a new dissolution apparatus for orodispersible films (ODFs). The new apparatus was based on a flow-through cell design which requires only a limited amount of dissolution medium and can automatically collect samples in short-time intervals. Compared with the dissoluti...

    journal_title:Pharmaceutical development and technology

    pub_type: 杂志文章

    doi:10.3109/10837450.2014.882936

    authors: Xia Y,Chen F,Zhang H,Luo C

    更新日期:2015-05-01 00:00:00

  • Preparation of celecoxib tablet by hot melt extrusion technology and application of process analysis technology to discriminate solubilization effect.

    abstract::The aim of this study was to prepare various types of solid dispersions (SDs) by the hot-melt extrusion technique. Next, process analytical technology (PAT) such as Fourier transform-infrared (FT-IR) and Raman and near infrared (NIR) spectroscopy were applied to determine the solubilization effect. The SDs and its tab...

    journal_title:Pharmaceutical development and technology

    pub_type: 杂志文章

    doi:10.1080/10837450.2020.1723023

    authors: Hwang I,Renuka V,Lee JH,Weon KY,Kang CY,Lee BJ,Park JB

    更新日期:2020-06-01 00:00:00

  • Poly(glycerol methacrylate)-based degradable nanoparticles for delivery of small interfering RNA.

    abstract::Nucleic acids therapeutic efficiency is generally limited by their low stability and intracellular bioavailability, and by the toxicity of the carriers used to deliver them to the target sites. Aminated poly(glycerol methacrylate) polymers are biodegradable and pH-sensitive polymers that have been used previously to d...

    journal_title:Pharmaceutical development and technology

    pub_type: 杂志文章

    doi:10.1080/10837450.2017.1312443

    authors: Morsi NG,Ali SM,Elsonbaty SS,Afifi AA,Hamad MA,Gao H,Elsabahy M

    更新日期:2018-04-01 00:00:00

  • Correlation of the thermal stability of phospholipid-based emulsions and the microviscosity measurements using fluorescence polarization.

    abstract::The fluorescence polarization technique was used to measure the microviscosity of a series of phospholipid-based emulsions. Fourteen different oil-in-water emulsions containing 20% medium chain length triglycerides, various concentrations and types of phospholipids, and 2.2% glycerin were prepared by microfluidization...

    journal_title:Pharmaceutical development and technology

    pub_type: 杂志文章

    doi:10.1081/pdt-120030251

    authors: Zhang X,Kirsch LE

    更新日期:2004-01-01 00:00:00

  • Formulation and physicochemical characterization of chitosan/acyclovir co-crystals.

    abstract::In the current study, the influence of chitosan on the dissolution rate and bioavailability of acyclovir has been illustrated through the preparation of co-crystals by simple solvent change method. Chitosan was precipitated on acyclovir crystals using sodium citrate as the salting out agent. The pure drug and the prep...

    journal_title:Pharmaceutical development and technology

    pub_type: 杂志文章

    doi:10.3109/10837450.2011.595798

    authors: Allam AN,Naggar VF,El Gamal SS

    更新日期:2013-07-01 00:00:00