Toxicological Effects of Copaiba Oil (Copaifera spp.) and Its Active Components.

Vegetable oils are among the most important traditional resources of Amazonia. Oleoresins are a type of oil that have interesting characteristics and highly bioactive properties with pharmacological potential. Oleoresins produced in the trunks of Copaifera (Fabaceae) spp. trees, known as copaiba oils, are made up of terpenes from the sesquiterpene (volatile) and diterpene (resinous) classes, but in amounts that vary between species and depending on several factors, such as soil type. Despite being used for medicinal purposes, via topical and oral application, the toxic effects of copaiba oils and their constituents are little known. The current paper reviews the toxicological studies, both in vitro and in vivo, described in the literature for copaiba oils, as well as the cytotoxic characteristics (against microorganisms and tumor cells) in in silico, in vitro and in vivo models for the sesquiterpenes and diterpenes that make up these oils.

University Pharmacy: from the foundation to the Pandemic times of Covid-19

Abstract The University Pharmacy Program (FU), from the Federal University of Rio de Janeiro (UFRJ), was created based on the need to offer a curricular internship to students of the Undergraduate Course at the Faculty of Pharmacy. Currently, it is responsible for the care of about 200 patients/day, offering vacancies for curricular internships for students in the Pharmacy course, it has become a reference in the manipulation of many drugs neglected by the pharmaceutical industry and provides access to medicines for low-income users playing an important social function. Research is one of the pillars of FU-UFRJ and several master and doctoral students use the FU research laboratory in the development of dissertations and theses. As of 2002, the Pharmaceutical Care extension projects started to guarantee a rational and safe pharmacotherapy for the medicine users. From its beginning in 1982 until the current quarantine due to the COVID-19 pandemic, FU-UFRJ has been adapting to the new reality and continued to provide patient care services, maintaining its teaching, research, and extension activities. The FU plays a relevant social role in guaranteeing the low-income population access to special and neglected medicines, and to pharmaceutical and education services in health promotion.

Development and characterization of photoprotective nanoemulsions containing Babassu (Orbignya phalerata Mart. ) lipophilic extract

Abstract Oil-in-water photoprotective nanoemulsions (NEs) were developed using Babassu (BBS) lipophilic extract, nonionic surfactants, and low concentrations of organic sunscreens by ultrasonic processing. BBS extract was chosen due to its suitable physicochemical properties (acidity index, peroxide index, refraction index, and relative density) and predominance of saturated fatty acids, identified by gas chromatography-mass spectrometry (GC-MS), which promote biological activities and high oxidative stability. NEs were characterized by mean droplet size, morphology, polydispersity index (PdI), pH, and organoleptic properties, and the physical stability of the NEs was evaluated for 120 days at room temperature. The sun protection factor (SPF) was determined, and the photostability and in vitro cytotoxicity assays were performed for NEs. All NEs remained stable for 120 days, with a droplet size <150 nm and a monomodal distribution profile. The pH values were compatible with the skin's pH. NE3 showed a spherical morphology, with a mean droplet size of 125.15 ± 0.16 nm and PdI of 0.145 ± 0.032. NE3 containing BBS extract and sunscreens presented an SPF of 35.5 ± 3.0, was photostable after 6 h of radiation and was non-cytotoxic to fibroblast cells. Thus, NE3 could be considered a promising formulation for developing synergic plant-extract sunscreen photoprotective products for the market

Development and clinical application of hydrogel formulations containing papain and urea for wound healing

Abstract Hydrogels are used for wound treatment, as they may contain one or more active components and protect the wound bed. Papain is one of the active substances that have been used with this purpose, alongside urea. In this paper, carboxypolymethylene hydrogels containing papain (2% and 10% concentrations) and urea (5% concentration) were produced. Physical-chemical stability was performed at 0, 7, 15 and 30 days at 2-8ºC, 25ºC and 40ºC, as well as the rheological aspects and proteolytic activity of papain by gel electrophoresis. Clinical efficacy of the formulations in patients with lower limb ulcers was also evaluated in a prospective, single-center, randomized, double-blind and comparative clinical trial. The results showed 7-day stability for the formulations under 25ºC, in addition to approximately 100% and 15% of protein activity for 10% and 2% papain hydrogel, respectively. The rheological profile was non-Newtonian for the 10% papain hydrogel tested. There were no significant differences regarding the mean time for healing of the lesions, although 10% papain presented a better approach to be used in all types of tissue present in the wound bed.

In vitro approaches to antioxidant screening for the development of a sunscreen formulation

Abstract The incorporation of antioxidants into sunscreens may provide additional skin photoprotection against the harmful photobiological effects of ultraviolet radiation. The present study evaluated the applicability of a screening approach to the assessment of the antioxidant and photoprotective properties of vitamin C, vitamin E, and coenzyme Q10 and then determined the performance of the most effective antioxidant in a sunscreen formulation. Antioxidant activity was assessed by the 2,2-diphenyl-1-picrylhydrazyl (DPPH) assay, 2,2`-azino-bis (3-ethylbenzothiazoline-6-sulfonic acid) (ABTS) assay, and oxygen radical absorbance capacity (ORAC) assay, and the photoprotective potential was investigated by the yeast photoprotection assay. The antioxidant with the best effect was incorporated into sunscreen formulations which were evaluated for 120 days regarding their in vitro photoprotective parameters. Vitamin C showed high antioxidant capacity as well as a photoprotective potential against simulated solar irradiation applied for times longer than 1 h. Although the Sun Protection Factor, UVA/UVB ratio and critical wavelength did not differed significantly (p<0.05) between the formulation blank and the formulations containing 0.5% or 1% vitamin C, formulations with vitamin C kept their photostability for 6 months. Consequently, the proposed screening approach seems to be promising for the development of an antisolar photostable formulation containing vitamin C as an antioxidant.

Development, physicochemical evaluation, and in vivo permeation studies of topical formulations containing 0.1% tacrolimus

Abstract The objective of this paper was to develop and evaluate two semi-solid pharmaceutical forms containing 0.1% tacrolimus: cream (CRT01) and gel (GLT01). For the evaluation of physicochemical stability, at times 0, 30, 60 and 90 days, at 23°C and at 40°C, High Performance Liquid Chromatography coupled with a Diode Array Detector (HPLC-DAD) was employed. This method was developed and validated for tacrolimus quantification. The occlusivity test and skin permeation assay were also performed, using an animal model (Wistar rats), and the CRT01 and GLT01 were compared to the 0.1% tacrolimus ointment (PFU01) obtained from the University Pharmacy, Federal University of Rio de Janeiro, Brazil. CRT01 and GLT01 presented a homogeneous aspect and consistency adequate for topical products, along with sensory characteristics above PFU01. They also presented adequate physicochemical stability for 90 days and a lower occlusive effect than PFU01 (p<0.05). CRT01 showed greater affinity for the skin when compared to PFU01 and GLT01, with low systemic absorption. The CRT01 semi-solid formulation was considered the most adequate one to treat patients with atopic dermatitis or other dermatologic inflammatory diseases, promoting rational use of tacrolimus

Captopril oral solution for pediatric use: formulation, stability study and palatability assessment in vivo

Abstract he aim of this work was to develop an oral solution of captopril at 5 mg/mL preservative-free. Two formulations were prepared, one containing sweetener (formulation 1) and the other without this excipient (formulation 2). The results found of validation parameters from analytical method performed by HPLC for captopril were, linearity 0.9998, the limit of detection 15.71 µg/mL, the limit of quantification 47.60 µg/mL, repeatability 1.05%, intermediate precision 2.42%, accuracy intraday 101,53%, accuracy inter-day 99.85%. Moreover, the results found for captopril disulfide were, linearity 0.9999, limit of detection 0.65 µg/mL, limit of quantification 1.96 µg/mL, repeatability 2.28%, intermediate precision 1.51%, accuracy intraday 101.36%, accuracy inter-day 100.29%. The appearance of formulations was clear and colorless, pH measures were 3.12 and 3.04, dosage of captopril and captopril disulfide were 99.45% and 99.82%, 0.24% and 0.12% for formulation 1 and formulation 2, respectively. The stability study demonstrated that the concentration of captopril and captopril disulfide in the formulations was > 90% and below 3%, respectively. The in vivo palatability study in animals and humans showed that Formulation 1 containing the sweetener had better acceptance. Thus, the sweetener was able to improve the unpleasant taste of the formulation

Medication Errors in Compounding Pharmacy / Erros de Medicação em Farmácia de Manipulação

Abstract The traditional role of compounding pharmacies is to make drugs prescribed by physicians for patients with needs that cannot be met by commercially available drugs. Medication errors have attracted attention of health authorities since they compromise the patient's assistance, enhance morbidity rates and increase the healthcare costs. This study analyzed medication errors that occurred in a compounding pharmacy school in order to identify types and periodicity and to outline strategies in the service delivery process to mitigate such errors. This is a retrospective descriptive study carried out from March to June of 2018 and based on the analysis of occurrences recorded by the service sector of a magistral pharmacy school in Rio de Janeiro. The errors were classified according to the stage in the pharmaceutical assistance process and reached 124 records, with an average of 1.03 occurrence/day. The main causes were prescription errors (95 occurrences or 76.60%), administering (12 occurrences or 9.68%), labeling (7 occurrences or 5.65%), dispensing (7 occurrences or 5.65%) and handling (3 occurrences or 2.42%). The errors in the prescription stage, the most frequent ones, were potential but intercepted and cleared before they resulted in a harmful outcome. This study identified medication errors in a magistral pharmacy. The errors were potential but intercepted and resolved before they resulted in a harmful outcome. The results points to the need for systematic surveillance of adverse events in a more active way and for standardizing the procedures throughout the process, from assessing the medical prescription to guiding the patient for proper administration and storage. (AU)

Resumo O papel tradicional das farmácias de manipulação é manipular medicamentos prescritos por médicos para pacientes com necessidades que não podem ser atendidas pelos medicamentos disponíveis no mercado. Os erros de medicação são eventos que vêm recebendo grande destaque entre autoridades sanitárias por contribuírem com o aumento das taxas de morbidade e dos custos do sistema de saúde, comprometendo a qualidade da assistência prestada ao paciente. as it involves legal and ethical aspects of impact on professional practice. Errors in the administration of medications point out the responsibility of the nursing category. An adequate performance of this role enables the prevention of real errors. The purpose of this study was to analyze nursing responsibilities in the administration of medications through a bibliographical research in the Medline and Lilacs data bases (1997/1999O presente estudo teve por objetivo analisar os principais erros de medicação observados em uma Farmácia Escola magistral localizada no sudeste do Brasil. Foi desenvolvido um estudo descritivo retrospectivo no período de março a junho de 2018, baseado na análise das ocorrências de erros de medicação registradas no período. Os erros foram classificados de acordo com as etapas da assistência farmacêutica. Um total de 124 registros foram verificados no período, com média diária de 1,03 ocorrências/dia. As principais causas destes registros foram em 95 (76,60%) devido a erros de prescrição, 3 (2,42%) referentes à erros de manipulação dos medicamentos, 7 (5,65%) erros de rotulagem, 7 (5,65%) erros de dispensação, e 12 (9,68%) referentes à erros de administração do medicamento pelo paciente. Os erros de maior frequência foram relacionados à escrituração da prescrição. Os erros verificados eram potenciais e foram interceptados e resolvidos antes que resultassem em um desfecho danoso. Os resultados indicaram a necessidade de avançar para uma vigilância sistemática de eventos adversos de forma mais ativa e padronização das condutas relacionadas aos processos desde a avaliação da qualidade da prescrição até a orientação para administração e guarda adequada do medicamento pelo paciente. (AU)

Preparation of extemporaneous oral liquid in the hospital pharmacy

At the hospital, the pharmacist is constantly challenged to prepare extemporaneous solutions from tablets, capsules or drug powder for patients unable to swallow, such as pediatric, elderly and patients that use nasoenteric and nasogastric tubes. The preparation of extemporaneous solutions from capsules, tablets and drug powder requires stability studies analysis. This article is a bibliographic review of preparation of extemporaneous oral liquid from solid oral dosage forms used in clinical practice. The selected articles contain all the information regarding manipulation techniques, pharmaceutical excipients, packaging, storage conditions and results of stability studies above 90% performed by HPLC analysis. In addition, a situational analysis of the strategies for the preparation of the extemporaneous solution was described to help the manipulator in the decision. The preparation of extemporaneous solution from solid oral dosage forms is based on information from official compendium or scientific literature, to ensure safe and effective manipulated medicine.

Development and characterization of photoprotective formulations containing keratin particles

This work deals with development and evaluation of MFQ protective formulation, which contains two organic filters, namely: octyl-p-methoxycinnamate (OMC) and benzophenone-3 (BP-3); a photostabilizing agent called ethylhexylmethoxycrylene (EHMCR) and keratin particles. The MFQ formulation was evaluated in order to measure its pH, spin-spin lattice relaxation time (T2H), occlusivity factor, formulation efficacy, photostability and skin permeation, as well as keratin particle properties. Keratin particle size increased when incorporated to formulation, however, it did not affect pH. The MFQ formulation was found to be photostable and photoprotective, as evidenced by sunlight photostability test, sun protection factor (SPF), UVA/UVB ratio and critical wavelength. Interaction between keratin particles and active substances (OMC, BP-3 and EHMCR) was evidenced by T2H measurements. Evidences suggest that keratin reduces the permeation of both UV filters employed along this study, therefore, it can be stated that keratin has a promising potential for use in sunscreen formulations.

Multifunctional photoprotection: corrective makeup for cutaneous dyschromias

The aim of this study was to develop and evaluate a corrective and photoprotective makeup for patients with dyschromias. An emulsion was prepared and pigment mixtures were incorporated in the formulation, producing five shades of corrective makeup: BEIGE (I, II, III), BRONZE and TAN. The sun protection factor (SPF) and UVA/UVB ratio of the corrective makeup were determined using spectrophotometry with a Labsphere® analyser. The spreadability, occlusivity, stability, and photostability of the photoprotective formulations were also evaluated. For all formulations there was no statistical difference among them (p > 0.05) in terms of spreadability, occlusivity and SPF. They were considered to be photostable under solar radiation, with variations in SPF value and UVA/UVB ratio lower than 20%. The corrective makeup presented average-to-high UVB photoprotection and broad spectrum photoprotection. After 90 days, pH, density and SPF values showed no significant differences among formulations (p>0.05). All corrective makeup presented separation of the pigments, however, they returned to a homogeneous aspect and to the original color shade after shaking. The corrective makeup presented a fine texture, little brightness, and a homogeneous, dry-to-the-touch aspect. This work may benefit patients with dyschromias, improving their quality of life, besides promoting photoprotection and covering the skin blemishes

Development and validation of an analytical method using High Performance Liquid Chromatography (HPLC) to determine ethyl butylacetylaminopropionate in topical repellent formulations

ABSTRACT Diseases caused by insects are frequent in poor countries, leading to epidemic scenarios in urban areas; e.g., Dengue, Zika and Chikungunya. For this reason, the development of a safe and efficient topical formulation is essential. Ethyl butylacetylaminopropionate (EB) is a mosquito repellent developed by Merck, which is used in products for adults, children and especially babies, due to its low allergenic potential. The aim of this work was to validate an analytical methodology to quantify EB in a new poloxamer-based formulation by high-performance liquid chromatography (HPLC). The quantification methodology was performed at 40 ºC using a Kromasil reverse-phase column (C18), with the dimensions of 250 x 4.6 mm. The mobile phase was acetonitrile:water (1:1) at a 1.0 mL/min flow-rate. The detector wavelength was set at 218 nm to detect EB. The methodology was considered validated since the results indicated linearity (R2>0.99), specificity, selectivity, precision and accuracy (active recovery between 98% and 102%). It also presented limits of detection and quantification of 0.255 µg/mL and 0.849 µg/mL, respectively. The present study demonstrated the EB vehiculated in poloxamer gel is promising as a new insect repellent formulation, since it could be quantified and quality control evaluated.

Promotion of cutaneous penetration of nifedipine for nanoemulsion

ABSTRACT This article reports the development and characterization of a nanoemulsion (NE) able to improve the cutaneous penetration of nifedipine. NE with nifedipine was development and characterized, presenting droplet size of 20 nm with low polydispersity index (IP<0.1), spherical shape without aggregation, pH compatible with typical skin levels and stability evaluated by seven months. In the permeation studies, a classical formulation based in an oil/water cream containing nifedipine was used for comparison with NE. Nanoemulsion promoted and improved the retention of nifedipine in the epidermis and dermis in relation to classical formulation. This promoting effect is related to the nanometric size of the droplets of the NE (20 nm), which give him a large superficial area, favoring the contact of the nanocarrier with the skin surface. The NE was efficient in promoting accumulation of nifedipine in the dermis, which is the site of vasodilation action. NE was not irritating according to the primary dermal irritation tests. NE is a promising release system to promote cutaneous penetration of nifedipine and can be used in the future in clinical trials to promote healing of lesions caused by peripheral vascular diseases.

Development, characterization and evaluation of the dissolution profile of sulfasalazine suspensions / Desenvolvimento, caracterização e avaliação do perfil de dissolução de suspensões sulfasalazina

This paper reports the development, characterization and in vitrodissolution behavior of sulfasalazine suspensions for treatment of chronic intestinal inflammatory diseases. Three formulations were developed, from powdered sulfasalazine obtained from different suppliers. The sulfasalazine was characterized regarding concentration, Fourier Transform Infrared Spectroscopy (FTIR), Differential Scanning Calorimetry (DSC), X-Ray Diffraction (XRD), particle size distribution, polydispersion and solubility. The suspensions were developed and characterized regarding pH, viscosity, density, particle size, sedimentation volume, concentration and dissolution. The pH values were slightly acidic. The method of preparing the suspensions reduced the particle sizes and made the size distribution more homogeneous. The dissolution studies showed that the sulfasalazine suspensions had low solubility in acidic media, but dissolve quickly, reaching levels of 85%, in neutral media or media containing 0.5% of surfactants such as polysorbate 80. Besides this, the sulfasalazine suspensions were classified as having immediate dissolution because they reached dissolution levels near 100% in 20 minutes...

O trabalho reporta o desenvolvimento, caracterização e estudo in vitro de dissolução de suspensões de sulfassalazina para uso em doenças inflamatórias crônicas intestinais. Desenvolveram-se três formulações baseadas em fornecedores diferentes de pó de sulfassalazina. A sulfassalazina foi caracterizada quanto a Teor, Infravermelho por Transformada de Fourier (FTIR), Calorimetria Diferencial de Varredura (DSC), Difração de Raios-X (XRD), distribuição de tamanho das partículas, índice de polidispersão e solubilidade. A suspensão foi desenvolvida e caracterizada quanto a pH, viscosidade, densidade, tamanho de partícula, volume de sedimentação, teor e estudo de dissolução. Os valores de pH determinados foram levemente ácidos. O método de preparo das suspensões reduziu o tamanho das partículas e tornou a distribuição de tamanho mais homogênea. Os estudos de dissolução mostraram que a suspensão de sulfassalazina tem problemas de solubilidade em meios de caráter ácido, entretanto, sofre dissolução rápida acima de 85% em meios neutros ou contendo 0,5% de tensoativos como Polissobato 80. Além disso, as suspensões de sulfassalazina foram classificadas como formulações de dissolução imediata porque a partir de 20 minutos sofrem dissolução em torno de 100%...

Development of methodologies for dimethylaminoethanol glycolate assay in association with sunscreens in dermocosmetic formulation

DMAE glycolate (DG) and sunscreens have been used associated in anti-aging dermocosmetic formulations. Despite extensive use of these substances, methods for quantification of DG as raw material and in cosmetic formulations, especially when associated, are not described in the literature. RP-HPLC and non-aqueous titration methods, with determination potentiometric end-point (PT), were developed and validated for rapid assay of DG as raw material and in a topic emulsion in association with sunscreens. Both methods are simple, selective, linear, accurate and precise. The PT method was chosen for stability study of DG in the formulation developed. The proposed formulation presented good stability performance as regards aspect, pH, apparent viscosity, and SPF, with less than 5% of DG degradation compared to initial conditions.

Glicolato de DMAE (DG) e protetores solares têm sido utilizados associados em formulações dermocosméticas antiidade. Apesar da ampla utilização dessas substâncias, métodos de quantificação para DG matéria-prima e em formulações cosméticas, especialmente quando associados, não estão descritos na literatura. Neste trabalho foram desenvolvidas e validadas metodologias por CLAE-FR e titulação em meio não-aquoso, com determinação do ponto final por potenciométrica (TP), para a rápida análise de DG matéria-prima e em emulsão tópica em associação com fotoprotetores. Ambos os métodos são simples, seletivos, lineares, exatos e precisos. O método TP foi escolhido para o estudo da estabilidade do DG na formulação desenvolvida. A formulação proposta apresentou um bom desempenho no que se refere a estabilidade, aspecto, pH, viscosidade aparente e SPF, com menos de 5% degradação do DG comparado as condições iniciais.