Insight into the solubility and dissolution behavior of piroxicam anhydrate and monohydrate forms

Paaver, Urve; Lust, Andres; Mirza, Sabiruddin; Rantanen, Jukka; Veski, Peep; Heinämäki, Jyrki; Kogermann, Karin

doi:10.1016/j.ijpharm.2012.04.042

Cited by 36 publications

(37 citation statements)

References 38 publications

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“…) to manufacture printable dosage forms. PRX is known to have a slow dissolution rate and poor aqueous solubility . The drug was printed on edible paper substrates using two printing methods: (1) inkjet printing and (2) flexography.…”

Section: Introductionmentioning

confidence: 99%

A Step Toward Development of Printable Dosage Forms for Poorly Soluble Drugs

Raijada

Genina

Fors

et al. 2013

Journal of Pharmaceutical Sciences

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Section: Introductionmentioning

confidence: 99%

A Step Toward Development of Printable Dosage Forms for Poorly Soluble Drugs

Raijada

Genina

Fors

et al. 2013

Journal of Pharmaceutical Sciences

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“…12,16 A recent paper particularly emphasized the effect of sodium dodecyl sulfate on solvent-mediated phase changes of piroxicam. 8 In this study, 1% SDS (w/w) in a slurry inhibited conversion of PRXAH to PRXMH. However, more data of such excipient effects are needed for practical formulation development and to ultimately gain better mechanistic understanding.…”

Section: ■ Introductionmentioning

confidence: 56%

Influence of Excipients on Solvent-Mediated Hydrate Formation of Piroxicam Studied by Dynamic Imaging and Fractal Analysis

Kirchmeyer

Wyttenbach

Alsenz

et al. 2015

Crystal Growth & Design

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Hydrate formation of pharmaceutical compounds can affect critical drug properties such as solubility and dissolution. There is, early in development, a need for a deeper understanding of how excipients influence hydrate formation mechanistically. The influence of excipients and of biorelevant medium on the kinetics of hydrate formation of piroxicam was studied with the aim of describing the kinetic changes of both the bulk suspension and the drug compact surface. Kinetic experiments were based on a miniaturized method using X-ray diffraction for solid-state analysis and ultra-high pressure liquid chromatography for drug concentration determination in bulk solution. Surface changes on drug compacts were monitored by dynamic image analysis of microscopic pictures and subsequent determination of a fractal dimension using box counting. Surface analysis correlated well with bulk monitoring of the piroxicam hydrate formation. Individual excipients exhibited highly specific effects on the kinetics of hydrate formation, but at equilibrium, the finally obtained fractal dimensions reached the same value of 1.85. The cluster structure of hydrate particles and therefore the recrystallization process were hardly affected by excipients; in contrast, excipients strongly affected the kinetics of hydrate formation, which is of pharmaceutical relevance.

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“…The concentration of PRX in the dissolution medium (900 mL) was measured at 354 nm by using a UV-VIS spectrophotometer (Ultrospec III, Biochrom Ltd., UK). Since PRX has two pKa values (pKa 1.86 and 5.46) and the different forms of the molecules have different solubility and dissolution in the release media, it was important to perform in vitro dissolution tests in more than one pH [27, 28]. Sink-conditions were maintained at all time in the in vitro dissolution tests.…”

Section: Methodsmentioning

confidence: 99%

Soluplus Graft Copolymer: Potential Novel Carrier Polymer in Electrospinning of Nanofibrous Drug Delivery Systems for Wound Therapy

Paaver

Tamm

Laidmäe

et al. 2014

BioMed Research International

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Electrospinning is an effective method in preparing polymeric nanofibrous drug delivery systems (DDSs) for topical wound healing and skin burn therapy applications. The aim of the present study was to investigate a new synthetic graft copolymer (Soluplus) as a hydrophilic carrier polymer in electrospinning of nanofibrous DDSs. Soluplus (polyvinyl caprolactam-polyvinyl acetate-polyethylene glycol graft copolymer (PCL-PVAc-PEG)) was applied in the nonwoven nanomats loaded with piroxicam (PRX) as a poorly water-soluble drug. Raman spectroscopy, X-ray powder diffraction, differential scanning calorimetry, and scanning electron microscopy (SEM) were used in the physical characterization of nanofibrous DDSs. According to the SEM results, the drug-loaded PCL-PVAc-PEG nanofibers were circular in cross-section with an average diameter ranging from 500 nm up to 2 µm. Electrospinning stabilized the amorphous state of PRX. In addition, consistent and sustained-release profile was achieved with the present nanofibrous DDSs at the physiologically relevant temperature and pH applicable in wound healing therapy. In conclusion, electrospinning can be used to prepare nanofibrous DDSs of PCL-PVAc-PEG graft copolymer (Soluplus) and to stabilize the amorphous state of a poorly water-soluble PRX. The use of this synthetic graft copolymer can open new options to formulate nanofibrous DDSs for wound healing.

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Insight into the solubility and dissolution behavior of piroxicam anhydrate and monohydrate forms

Cited by 36 publications

References 38 publications

A Step Toward Development of Printable Dosage Forms for Poorly Soluble Drugs

A Step Toward Development of Printable Dosage Forms for Poorly Soluble Drugs

Influence of Excipients on Solvent-Mediated Hydrate Formation of Piroxicam Studied by Dynamic Imaging and Fractal Analysis

Soluplus Graft Copolymer: Potential Novel Carrier Polymer in Electrospinning of Nanofibrous Drug Delivery Systems for Wound Therapy

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