Special Issue "Solid State Chemistry of Drugs"

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A special issue of Pharmaceutics (ISSN 1999-4923).

Deadline for manuscript submissions: closed (15 December 2014)

Special Issue Editors

Guest Editor
Prof. Dr. Stephen R. Byrn

Department of Industrial and Physical Pharmacy, School of Pharmacy and Pharmaceutical Sciences, Purdue University, 575 Stadium Mall Drive, West Lafayette, IN 47906, USA
Website | E-Mail
Phone: 765-714-2808
Interests: solid state chemistry of drugs; stability; polymorphism; formulation; liquid crystals; cocrystals; amorphous materials; nanoparticles
Guest Editor
Dr. David Engers

SSCI, a division of Aptuit, USA
Website | E-Mail
Interests: pharmaceutical material science; solid-state properties of crystalline and non-crystalline solid forms; polymorphism, salt and cocrystal formation of organic compounds; properties modulation of poorly water soluble compounds to improve oral bioavailability, with specific interest in nanocrystalline and amorphous approaches; and product/process transfer and scale-up

Special Issue Information

Submission

Manuscripts should be submitted online at www.mdpi.com by registering and logging in to this website. Once you are registered, click here to go to the submission form. Manuscripts can be submitted until the deadline. Papers will be published continuously (as soon as accepted) and will be listed together on the special issue website. Research articles, review articles as well as communications are invited. For planned papers, a title and short abstract (about 100 words) can be sent to the Editorial Office for announcement on this website.

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Please visit the Instructions for Authors page before submitting a manuscript. The Article Processing Charge (APC) for publication in this open access journal is 500 CHF (Swiss Francs). English correction and/or formatting fees of 250 CHF (Swiss Francs) will be charged in certain cases for those articles accepted for publication that require extensive additional formatting and/or English corrections.

Published Papers (3 papers)

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Research

Open AccessArticle Design of Olanzapine/Lutrol Solid Dispersions of Improved Stability and Performances
Pharmaceutics 2013, 5(4), 570-590; doi:10.3390/pharmaceutics5040570
Received: 3 September 2013 / Revised: 11 October 2013 / Accepted: 14 October 2013 / Published: 25 October 2013
Cited by 3 | PDF Full-text (1484 KB) | HTML Full-text | XML Full-text
Abstract
Eleven solid dispersions containing olanzapine, with carriers of different composition (Lutrol® F68, Lutrol® F127, Gelucire® 44/14), were prepared and examined by thermal (differential scanning calorimetry (DSC); thermomicroscopy (HSM)) and X-ray diffraction (XRD) analysis, both as fresh or aged (one year)
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Eleven solid dispersions containing olanzapine, with carriers of different composition (Lutrol® F68, Lutrol® F127, Gelucire® 44/14), were prepared and examined by thermal (differential scanning calorimetry (DSC); thermomicroscopy (HSM)) and X-ray diffraction (XRD) analysis, both as fresh or aged (one year) samples. Drug and carriers were preliminarily selected in order to avoid problems related to the aging of the formulation, according to the solubility parameters of carriers and drug. These parameters make it possible to predict the low solubility of olanzapine in the carriers (alone or in mixtures). Systems containing only Lutrol (also in the presence of Transcutol®) contain the drug in the form of particles of reduced size and in a crystalline form. Gelucire® 44/14 apparently increases the amount of olanzapine dissolved in the solid carrier, but this is presumed to be a metastable state, probably related to the heterogeneous nature of the carrier that delays crystallization of the drug. The high hydrophilicity of the carriers proves suitable to an accelerated and quick release of the drug regardless of aging. Differences in the release profiles between Lutrol- and Gelucire-containing systems were interpreted in terms of the formation of polymer micelles by the Lutrols when in aqueous solution. Full article
(This article belongs to the Special Issue Solid State Chemistry of Drugs)
Open AccessArticle Terahertz Pulsed Imaging and Magnetic Resonance Imaging as Tools to Probe Formulation Stability
Pharmaceutics 2013, 5(4), 591-608; doi:10.3390/pharmaceutics5040591
Received: 3 August 2013 / Accepted: 21 September 2013 / Published: 25 October 2013
Cited by 3 | PDF Full-text (1687 KB) | HTML Full-text | XML Full-text
Abstract
Dissolution stability over the entire shelf life duration is of critical importance to ensure the quality of solid dosage forms. Changes in the drug release profile during storage may affect the bioavailability of drug products. This study investigated the stability of a commercial
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Dissolution stability over the entire shelf life duration is of critical importance to ensure the quality of solid dosage forms. Changes in the drug release profile during storage may affect the bioavailability of drug products. This study investigated the stability of a commercial tablet (Lescolr XL) when stored under accelerated conditions (40 oC/75% r.h.). Terahertz pulsed imaging (TPI) was used to investigate the structure of the tablet coating before and after the accelerated aging process. The results indicate that the coating was reduced in thickness and exhibited a higher density after being stored under accelerated conditions for four weeks. In situ magnetic resonance imaging (MRI) of the water penetration processes during tablet dissolution in a USP-IV dissolution cell equipped with an in-line UV-vis analyzer was carried out to study local differences in water uptake into the tablet matrix between the stressed and unstressed state. The drug release profiles of the Lescolr XL tablet before and after the accelerated storage stability testing were compared using a “difference” factor ∫1 and a “similarity” factor ∫2. The results reveal that even though the physical properties of the coating layers changed significantly during the stress testing, the coating protected the tablet matrix and the densification of the coating polymer had no adverse effect on the drug release performance. Full article
(This article belongs to the Special Issue Solid State Chemistry of Drugs)
Figures

Open AccessArticle Influence of Sodium Lauryl Sulfate and Tween 80 on Carbamazepine–Nicotinamide Cocrystal Solubility and Dissolution Behaviour
Pharmaceutics 2013, 5(4), 508-524; doi:10.3390/pharmaceutics5040508
Received: 6 August 2013 / Revised: 5 September 2013 / Accepted: 29 September 2013 / Published: 11 October 2013
Cited by 15 | PDF Full-text (804 KB) | HTML Full-text | XML Full-text | Supplementary Files
Abstract
The influence of the surfactants of sodium lauryl sulfate (SLS) and Tween 80 on carbamazepine–nicotinamide (CBZ–NIC) cocrystal solubility and dissolution behaviour has been studied in this work. The solubility of the CBZ–NIC cocrystal was determined by measuring the eutectic concentrations of the drug
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The influence of the surfactants of sodium lauryl sulfate (SLS) and Tween 80 on carbamazepine–nicotinamide (CBZ–NIC) cocrystal solubility and dissolution behaviour has been studied in this work. The solubility of the CBZ–NIC cocrystal was determined by measuring the eutectic concentrations of the drug and the coformer. Evolution of the intrinsic dissolution rate (IDR) of the CBZ–NIC cocrystal was monitored by the UV imaging dissolution system during dissolution. Experimental results indicated that SLS and Tween 80 had little influence upon the solubility of the CBZ–NIC cocrystal but they had totally opposite effects on the IDR of the CBZ–NIC cocrystal during dissolution. SLS significantly increased the IDR of the CBZ–NIC cocrystal while Tween 80 decreased its IDR. Full article
(This article belongs to the Special Issue Solid State Chemistry of Drugs)

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