Polymorphism: an evaluation of the potential risk to the quality of drug products from the Farmácia Popular Rede Própria

Santos, Olimpia Maria Martins; Reis, Maria Esther Dias; Jacon, Jennifer Tavares; Lino, Mônica Esselin de Sousa; Simões, Juliana Savioli

doi:10.1590/s1984-82502011000100002

Cited by 42 publications

(20 citation statements)

References 192 publications

(82 reference statements)

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“…Anhydrous forms of drugs, for example, have a higher thermodynamic activity compared to the corresponding hydrates, and, consequently, increased solubility and dissolution rate. Different polymorphic forms can arise from the conditions employed in the synthesis and purification of the drug, depending, for example, on the type of solvent used and the reaction temperature [24,27,28].…”

Section: Factors Affecting Drug Bioavailability: Related To the Drugmentioning

confidence: 99%

Challenges to improve the biopharmaceutical properties of poorly water-soluble drugs and the application of the solid dispersion technology

et al. 2018

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The oral solid dosage forms are extremely relevant to drug therapy and responsible for much of the pharmaceutical industry turnover worldwide. However, the development of medicines in solid form involves significant challenges, including obtaining formulations with appropriate bioavailability for low aqueous solubility drugs (classes II and IV of the Biopharmaceutics Classification System). One of the most effective strategies to overcome poor dissolution rate and low absorption of drugs is the solid dispersion technique, however, although it has been the focus of much research in recent decades, there are relatively few commercially available products based on such technology. This is mainly due to problems related to production scale-up and physicochemical instability and creates opportunities for new studies to explore the full potential of the technology. This review presents an overall approach to the factors affecting the dissolution rate and oral bioavailability of BCS-classes II and IV drugs and a brief review of the state-of-the-art of solid dispersion technology.

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Section: Factors Affecting Drug Bioavailability: Related To the Drugmentioning

confidence: 99%

Challenges to improve the biopharmaceutical properties of poorly water-soluble drugs and the application of the solid dispersion technology

et al. 2018

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“…Therefore, they can have impact on solubility and dissolution rate of the drug. The strategy involves drug-coformer combinations that have the potential of forming energetically and structurally robust interactions [3][4][5][6][7][8]. Pharmaceutical cocrystals often rely on hydrogen-bonded assemblies between an API and coformer with well-defined stoichiometries.…”

Section: Introductionmentioning

confidence: 99%

Cocrystallization Acyclovir-Succinic Acid Using Solvent Evaporation Methods

Winantari

Setyawan

Siswodihardjo

et al. 2017

Asian J Pharm Clin Res

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Objective: The aim of this research is to prepare and characterize cocrystals of acyclovir through cocrystallization of acyclovir-succinic acid (AS) to improve the physical properties of the drug.Methods: AS cocrystals were prepared using solvent evaporation method. The cocrystals were characterized by polarization microscope, scanning electron microscopy (SEM), differential scanning calorimetry, powder X-ray diffraction (PXRD), and Fourier transform infrared spectroscopy.Results: Physical characterization using polarization microscope and SEM showed the AS cocrystals have unique crystal habit and morphology. Phase diagram at a molar ratio of 50:50% (acyclovir:succinic acid) showed a decrease in the melting temperature, i.e., 176.23°C in comparison with the melting point of the constituent materials (acyclovir 253.53°C and succinic acid 187.29°C). The PXRD pattern of AS cocrystals (ethanol) exhibited new diffraction peaks at 2θ=5.91°; 9.16°; and 13.40°. Besides, cocrystals of AS (glacial acetic acid) indicated new peaks at 2θ=5.98°; 9.19°; and 13.43°. Furthermore, there was a shift in the N-H, O-H, and C=O. Conclusion:Cocrystallization of AS acid in ethanol and glacial acetic acid were successfully formed using solvent evaporation methods.

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“…Polymorphism is a frequently encountered problem faced by industry during the production of commercial pharmaceutical formulations that can alter physicochemical properties of resulting end-products (3). Many reviews are available in the literature describing the types of polymorphs and their significance in pharmaceutical industry (4)(5)(6). Due to the importance of polymorphism, it is essential to pay great heed during drug product development and regulatory review.…”

Section: Introductionmentioning

confidence: 99%

Near-Infrared Spectroscopy: Effective Tool for Screening of Polymorphs in Pharmaceuticals

Chadha

Haneef

2015

Applied Spectroscopy Reviews

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Near-infrared (NIR) spectroscopy has emerged as an important technique for the screening and characterization of polymorphs in pharmaceuticals. Polymorphism, the ability of a substance to exist in two or more crystalline phases having different physicochemical and biopharmaceutical parameters, has attracted pharmaceutical scientists due to the patentability of new forms. Transformation of the solid phase due to polymorphic changes during manufacturing and storage may lead to formulation hurdles. Vibrational spectroscopy, particularly NIR spectroscopy, is a widely used technique for polymorphs screening in drug development processes and has emerged as a process analytical technology tool. In this review, a brief overview of NIR spectroscopy, chemometric tools, and polymorphs screening of pharmaceuticals using NIR spectroscopy is presented. Recent developments in NIR spectroscopy instrumentation are also discussed.

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Polymorphism: an evaluation of the potential risk to the quality of drug products from the Farmácia Popular Rede Própria

Cited by 42 publications

References 192 publications

Challenges to improve the biopharmaceutical properties of poorly water-soluble drugs and the application of the solid dispersion technology

Challenges to improve the biopharmaceutical properties of poorly water-soluble drugs and the application of the solid dispersion technology

Cocrystallization Acyclovir-Succinic Acid Using Solvent Evaporation Methods

Near-Infrared Spectroscopy: Effective Tool for Screening of Polymorphs in Pharmaceuticals

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