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The Solid State Characterization of Pharmaceuticals and the Development of Dosage Forms

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

Deadline for manuscript submissions: closed (31 December 2020) | Viewed by 13810

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Prof. Dr. Fábio Seigi Murakami

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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

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Department of Pharmacy, Universidade Estadual do Centro Oeste (Unicentro), Campus CEDETEG, Alameda Élio Antonio Dalla Vechhia, 838 – Vila Carli, Guarapuava 85040-167, PR, Brazil
Interests: solid-state characterization; drug-excipient compatibility; solid dispersions; co-crystals; dissolution studies
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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

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Keywords

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

Published Papers (3 papers)

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14 pages, 3400 KiB

Open AccessArticle

Solid-State Characterization and Compatibility Studies of Penciclovir, Lysine Hydrochloride, and Pharmaceutical Excipients

by Rafaela Z. C. Meira, Isabela F. B. Biscaia, Camila Nogueira, Fabio S. Murakami, Larissa S. Bernardi and Paulo R. Oliveira

Materials 2019, 12(19), 3154; https://doi.org/10.3390/ma12193154 - 27 Sep 2019

Cited by 10 | Viewed by 3300

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 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

(This article belongs to the Special Issue The Solid State Characterization of Pharmaceuticals and the Development of Dosage Forms)

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16 pages, 3724 KiB

Open AccessArticle

Solid-State Characterization of Different Crystalline Forms of Sitagliptin

by Nayana C. F. Stofella, Andressa Veiga, Laiane J. Oliveira, Elisa F. Montin, Itamar F. Andreazza, Marco A. S. Carvalho Filho, Larissa S. Bernardi, Paulo R. Oliveira and Fábio S. Murakami

Materials 2019, 12(15), 2351; https://doi.org/10.3390/ma12152351 - 24 Jul 2019

Cited by 23 | Viewed by 6028

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, 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

(This article belongs to the Special Issue The Solid State Characterization of Pharmaceuticals and the Development of Dosage Forms)

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14 pages, 20183 KiB

Open AccessArticle

Preparation, Characterization, and Stability Evaluation of Taste-Masking Lacosamide Microparticles

by Chang-Soo Han, Seungsu Kim, Dong-Won Oh, Jeong Yeol Yoon, Eun-Seok Park, Yun-Seok Rhee, Ju-Young Kim, Dae Hwan Shin, Dong-Wook Kim and Chun-Woong Park

Materials 2019, 12(6), 1000; https://doi.org/10.3390/ma12061000 - 26 Mar 2019

Cited by 8 | Viewed by 3647

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 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

(This article belongs to the Special Issue The Solid State Characterization of Pharmaceuticals and the Development of Dosage Forms)

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