Special Issue "The Solid State Characterization of Pharmaceuticals and The Development of Dosage Forms"

A special issue of Materials (ISSN 1996-1944). This special issue belongs to the section "Biomaterials".

Deadline for manuscript submissions: 1 May 2020.

Special Issue Editors

Prof. Dr. Fábio Seigi Murakami
Website
Guest Editor
Universidade Federal do Parana, Department of Pharmacy, Curitiba, Brazil
Interests: solid-state characterization, thermal analysis, compatibility studies, new materials for film coating
Prof. Dr. Paulo Renato De Oliveira
Website
Guest Editor
Universidade Estadual do Centro Oeste, Post Graduation Program in Pharmaceutical Sciences, Guarapuava, Brazil
Interests: solid-state characterization, drug-excipient compatibility, solid dispersions, co-crystals, dissolution studies

Special Issue Information

Dear Colleagues,

The characterization of solid-state properties at an early stage, using appropriate analytical methodologies, is a prerequisite in the development of solid dosage forms both from scientific and regulatory points of view. In the pre-formulation studies of new solid dosage forms, it is essential to have readily available knowledge of the physicochemical properties of the active component and excipients. Also, new technologies are emerging for the improvement of dissoltution/solubility characteristics, mainly for BCS class II drugs, and the resulting product needs to be well characterized.

The major purpose of this Special Issue is to provide new research involving relevant topics related to the physicochemical characterization of pharmaceutical solids and the development of new dosage forms. This Special Issue will consider the following:

  • Solid-state characterization;
  • Pharmaceutical materials selection and characterization;
  • Thermal analysis applied in drug development;
  • Pharmaceutical formulation development;
  • Pharmaceutical dosage forms;
  • New materials for coating of solid forms;
  • Novel drug delivery technologies.

All researchers working in the field are cordially invited to contribute original research papers, communications, or reviews to this Special Issue of Materials.

Prof. Dr. Fábio Seigi Murakami
Prof. Dr. Paulo Renato de Oliveira
Guest Editors

Manuscript Submission Information

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. All papers will be peer-reviewed. Accepted papers will be published continuously in the journal (as soon as accepted) and will be listed together on the special issue website. Research articles, review articles as well as short 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.

Submitted manuscripts should not have been published previously, nor be under consideration for publication elsewhere (except conference proceedings papers). All manuscripts are thoroughly refereed through a single-blind peer-review process. A guide for authors and other relevant information for submission of manuscripts is available on the Instructions for Authors page. Materials is an international peer-reviewed open access semimonthly journal published by MDPI.

Please visit the Instructions for Authors page before submitting a manuscript. The Article Processing Charge (APC) for publication in this open access journal is 2000 CHF (Swiss Francs). Submitted papers should be well formatted and use good English. Authors may use MDPI's English editing service prior to publication or during author revisions.

Keywords

  • solid-state characterization
  • drug-excipient compatibility
  • solid dispersions
  • co-crystals
  • dissolution studies
  • dosage forms

Published Papers (3 papers)

Order results
Result details
Select all
Export citation of selected articles as:

Research

Open AccessArticle
Solid-State Characterization and Compatibility Studies of Penciclovir, Lysine Hydrochloride, and Pharmaceutical Excipients
Materials 2019, 12(19), 3154; https://doi.org/10.3390/ma12193154 - 27 Sep 2019
Cited by 2
Abstract
The physical and chemical characterization of the solid-state properties of drugs and excipients is fundamental for planning new formulations and developing new strategies for the treatment of diseases. Techniques such as differential scanning calorimetry, thermogravimetry, X-ray powder diffraction, Fourier transform infrared spectroscopy, and [...] Read more.
The physical and chemical characterization of the solid-state properties of drugs and excipients is fundamental for planning new formulations and developing new strategies for the treatment of diseases. Techniques such as differential scanning calorimetry, thermogravimetry, X-ray powder diffraction, Fourier transform infrared spectroscopy, and scanning electron microscopy are among the most commonly used techniques for these purposes. Penciclovir and lysine are individually used to treat the herpes virus. As such, the development of a formulation containing both drugs may have therapeutic potential. Solid-state characterization showed that both penciclovir and lysine were crystalline materials with melting points at 278.27 °C and 260.91 °C, respectively. Compatibility studies of penciclovir and lysine indicated a possible interaction between these substances, as evidenced by a single melting point at 253.10 °C. The compatibility of several excipients, including ethylenediaminetetraacetic acid, cetostearyl alcohol, sodium lauryl sulphate, di-tert-butyl methyl phenol, liquid petrolatum, methylparaben, nonionic wax, paraffin, propylene glycol, and propylparaben, was evaluated in ternary (penciclovir-lysine-excipient) mixtures (1:1:1, w/w/w) to determine the optimal formulation. The developed formulation was stable under accelerated and ambient conditions, which demonstrated that the interaction between penciclovir and lysine was suitable for the development of a formulation containing both drugs. Full article
Show Figures

Graphical abstract

Open AccessArticle
Solid-State Characterization of Different Crystalline Forms of Sitagliptin
Materials 2019, 12(15), 2351; https://doi.org/10.3390/ma12152351 - 24 Jul 2019
Abstract
Sitagliptin is an inhibitor of the enzyme dipeptidyl peptidase-4, used for the treatment of type 2 diabetes mellitus. The crystal structure of active pharmaceutical solids determines their physical and chemical properties. The polymorphism, solvates and hydrates can influence the free energy, thermodynamic parameters, [...] Read more.
Sitagliptin is an inhibitor of the enzyme dipeptidyl peptidase-4, used for the treatment of type 2 diabetes mellitus. The crystal structure of active pharmaceutical solids determines their physical and chemical properties. The polymorphism, solvates and hydrates can influence the free energy, thermodynamic parameters, solubility, solid-state stability, processability and dissolution rate, besides directly affecting the bioavailability. Thus, the physicochemical characterization of an active pharmaceutical ingredient is required to guarantee the rational development of new dosage forms. In this context, we describe herein the solid-state characterization of three crystalline forms of sitagliptin: sitagliptin phosphate monohydrate, sitagliptin phosphate anhydrous and sitagliptin base form. The investigation was carried out using differential scanning calorimetry (DSC), thermogravimetry (TG)/derivative thermogravimetry (DTG), spectroscopic techniques, X-ray powder diffraction (XRPD) and morphological analysis by scanning electron microscopy. The thermal analysis revealed that during the dehydration of sitagliptin phosphate monohydrate (Tpeak = 134.43 °C, ΔH = −1.15 J g−1) there is a characteristic crystalline transition event, which alters the physicochemical parameters of the drug, such as the melting point and solubility. The crystalline behavior of sitagliptin base form differs from that of sitagliptin phosphate monohydrate and sitagliptin phosphate anhydrous, mainly with regard to the lower temperature of the fusion event. The melting point (Tpeak) values obtained were 120.29 °C for sitagliptin base form, 206.37 °C for sitagliptin phosphate monohydrate and 214.92 °C for sitagliptin phosphate anhydrous. In relation to the thermal stability, sitagliptin phosphate monohydrate and sitagliptin phosphate anhydrous showed a slight difference; however, both are more thermostable than the base molecule. Therefore, through this study it was possible to establish the most suitable crystalline form of sitagliptin for the development of a safe, effective and appropriate pharmaceutical dosage form. Full article
Show Figures

Graphical abstract

Open AccessArticle
Preparation, Characterization, and Stability Evaluation of Taste-Masking Lacosamide Microparticles
Materials 2019, 12(6), 1000; https://doi.org/10.3390/ma12061000 - 26 Mar 2019
Cited by 1
Abstract
Lacosamide (LCM) is a third-generation antiepileptic drug. Selective action of the drug on voltage-gated sodium channels reduces side effects. Oral administration of LCM shows good pharmacokinetic profile. However, the bitter taste of LCM is a barrier to the development of oral formulations. In [...] Read more.
Lacosamide (LCM) is a third-generation antiepileptic drug. Selective action of the drug on voltage-gated sodium channels reduces side effects. Oral administration of LCM shows good pharmacokinetic profile. However, the bitter taste of LCM is a barrier to the development of oral formulations. In this study, we aimed to prepare encapsulated LCM microparticles (MPs) for masking its bitter taste. Encapsulated LCM MPs were prepared with Eudragit® E100 (E100), a pH-dependent polymer, by spray drying. Three formulations comprising different ratios of LCM and E100 (3:1, 1:1, and 1:3) were prepared. Physicochemical tests showed that LCM was in an amorphous state in the prepared formulations, and they were not miscible. LCM-E100 (1:3) had a rough surface due to surface enrichment of LCM. Increased E100 ratio in LCM-E100 MPs resulted in better taste-making effectiveness: LCM-E100 (1:1) and LCM-E100 (1:3) showed good taste-masking effectiveness, while LCM-E100 (3:1) could not mask the bitter taste of LCM. Dissolution results of the prepared formulations showed good correlation with taste-masking effectiveness. Nevertheless, high E100 ratio reduced the stability of the prepared formulations. Especially the difference in initial dissolution profile observed for LCM-E100 (1:3) indicated rapid reduction in taste-masking effectiveness and surface recrystallization. Therefore, LCM-E100 formulation in the ratio of 1:1 was selected as the best formulation with good taste-masking effectiveness and stability. Full article
Show Figures

Figure 1

Back to TopTop