DEFAR - Departamento de Farmácia

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Autor: search.filters.author.Souza, Jacqueline deTem arquivos: Sim

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Agora exibindo 1 - 10 de 29
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    Dissolution test for oral suspension : an overview about use and importance.
    (2022) Soares, Thaís dos Santos Paulino; Souza, Jacqueline de; Rosa, Lorena de Sousa; Marinho, Flávia Dias Marques
    This work aims to ascertain the comprehensiveness of dissolution tests for oral suspensions registered in Brazil and the USA. After consulting literature since 1994, a paucity of information about dissolution methods for suspensions was detected. It makes it difficult to establish the most appropriate test parameters. In January, 2019, there were 46 drugs registered in Anvisa (Brazil) as oral suspension, being 47 reference, 173 generic and 114 interchangeable similar (IS) medicines; while in the USA, 90 drugs were registered as oral suspension by FDA, 235 Abreviatted New Drug Application and 111 New Drug Application medicines. Out of 46 and 90, only six and 15 drugs as oral suspension had a pharmacopeial dissolution test, corresponding to 70 (20.9%) and 82 (23.7%) products in Brazil and the USA, respectively. Dissolution studies were found for 17 drugs as oral suspension in the non-compendial literature. Dissolution test conditions were established to few marketable oral suspension drugs, most of which are BCS class II or IV. Thus, investing in dissolution studies could subsidize the registration of these products by regulators, especially for generic and IS drugs, by comparing dissolution profiles, and predicting their in vivo behavior to avoid exposure of healthy individuals to clinical research.
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    Chemical analysis of Eruca sativa ethanolic extract and its effects on hyperuricaemia.
    (2022) Teixeira, Arthur Ferrari; Souza, Jacqueline de; Dophine, Douglas Daniel; Souza Filho, José Dias de; Guimarães, Dênia Antunes Saúde
    In vivo assays and chemical analyses were performed on the ethanolic extract from leaves of Eruca sativa. UHPLC-ESI-QTOF analysis confirmed the presence of glucosinolates and flavonol glucosides. The major flavonoid of the ethanolic extract, kaempferol-3,40 -di-O-β-glucoside, was isolated, a HPLC-DAD method developed and validated to quantify its content in the extract. In vivo experiments were carried out on Wistar rats with hyperuricaemia induced by potassium oxonate and uric acid. A hypouricaemic effect was observed in hyperuricaemic Wistar rats treated with ethanolic extract at dose of 125 mg/kg and kaempferol-3,40 -di-O-β-glucoside at dose of 10 mg/kg. The main anti-hyperuricaemic mechanism observed in the extract was uricosuric. Kaempferol-3,40 -di-O-β- glucoside was identified as an important component responsible for the total activity of the ethanolic extract and was considered as a good chemical and biological marker of the ethanolic extract of E. sativa. The obtained results indicated the potential of E. sativa in the treatment of hyperuricaemia and its comorbidities.
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    Effects of experimental conditions on solubility measurements for BCS classification in order to improve the biowaiver guidelines.
    (2021) Monteiro, Patrícia Fernanda; Barcellos, Neila Marcia Silva; Caldeira, Tamires Guedes; Reis, Adriana Cotta Cardoso; Ribeiro, Amanda Santos; Souza, Jacqueline de
    Among the methods described for determining the solubility, shake-flask is suitable to evaluate the equilibrium solubility according to the BCS. Nevertheless, experimental conditions related to the shake-flask method are not well described. Evaluating the effects of experimental conditions on solubility measurements by shake-flask method is important and contributes in biowaiver decision. For this work, propranolol hydrochloride and nimesulide were used as model compound of high and low solubility, respectively. Equilibrium solubility was evaluated at 37 oC, 100 rpm during 48 hours in buffer media. Effects of the rotation speed, temperature, substance in excess and aliquot withdrawn were evaluated. Small variations of temperature caused significant differences in the solubility and then this parameter must be controlled. Excess of raw material influenced the results of the nimesulide, then, little excess is recommended. Rotation speed did not cause differences in the equilibrium solubilities, but at 150 rpm the equilibrium was reached faster. Aliquot did not present significant differences, but excessive withdrawn should be avoided. Therefore, the evaluation of equilibrium solubility using shake-flask method must be performed in physiological pH conditions, 37 ± 1 oC, substance in excess 10% above saturation, 50, 100 or 150 rpm and aliquot withdrawn not more than 10% of the media volume.
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    Novel insights to enhance therapeutics with acyclovir in the management of herpes simplex encephalitis.
    (2021) Assis, Maria Silvia Gurgel; Pedrosa, Taciane Cristina Fernandes; Moraes, Fernanda Segurasse de; Caldeira, Tamires Guedes; Pereira, Gislaine Ribeiro; Souza, Jacqueline de; Ruela, Andre Luís Morais
    Acyclovir is an antiviral drug poorly absorbed in the gastrointestinal tract due to its hydrophilicity, with low oral bioavailability (~20%). Although acyclovir is prescribed in the management of herpes simplex encephalitis (HSE), the disease has a poor prognosis, particularly if the treatment is delayed, reaching mortality rates of 70% if left untreated. Thus, high acyclovir doses are administered by intravenous (IV) infusion, usually at a dosage of 10 mg kg1 8-hourly in adults with normal renal function. However, the mortality related to HSE treated with acyclovir remains high (~20%) and permanent sequelae are commonly reported after 1 year (~50%). This review analyzed clinical trials following IV acyclovir administration. Novel insights aiming to improve drug bioavailability were reviewed, including acyclovir or its prodrugs, leading to the systemic distribution of the drug or drug targeting. Much research effort has been made to improve antiviral therapy, searching for delivery systems increasing acyclovir bioavailability by non-invasive pathways, such as oral and nasal pathways, or parenterally administered nanotechnology-based systems leading to drug targeting. Nanocarriers administered by non-invasive pathways represent feasible alternatives to treat HSE, even though not be industrially manufactured yet.
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    Stability and degradation kinetics of an ethanolic extract and tincture of aerial parts from lychnophora passerina (Brazilian arnica).
    (2021) Ugoline, Bruno César de Albuquerque; Souza, Jacqueline de; Caldeira, Tamires Guedes; Guimarães, Dênia Antunes Saúde
    Previous studies have demonstrated the anti-infammatory and antihyperuricemic activities of dried ethanolic extract of the aerial parts of Lychnophora passerina (Mart ex DC.) Gardner, Asteraceae, and then the potential to become a pharmaceutical product. However, many of the constituents present in these medicines can be degraded, raising serious concerns about the stability of products. Considering the impact on the quality of herbal medicines, this study evalu- ated the stability of a dried ethanolic extract and tincture of the aerial parts of L. passerina. For the accelerated stability study, the dried ethanolic extract and tincture were stored at 40±2 °C for 6 months. For the long-term stability study, the dried ethanolic extract was stored at 30±2 °C for 12 months. The organoleptic properties and goyazensolide content were analyzed. The pH, relative density, and dry residue were evaluated for the tincture. In addition, forced degradation and stability studies at room temperature (25±2 °C) were carried out. In glass bottles that were hermetically sealed and protected from light, the dried ethanolic extract remained stable for 3 months when stored at 30±2 °C and for 12 months at 25±2 °C. The tinctures remained stable for 6 months when stored at 25±2 °C. In addition, the dried ethanolic extract and tincture showed zero-order degradation kinetics. The dried ethanolic extract and tincture of L. passerina had greater stability when compared to preparations of other species of Lychnophora. Thus, this species could be directed for phar- maceutical preparations aimed at use by the population.
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    Eremantholide C from aerial parts of Lychnophora trichocarpha, as drug candidate : fraction absorbed prediction in humans and BCS permeability class determination.
    (2021) Caldeira, Tamires Guedes; Guimarães, Dênia Antunes Saúde; González Álvarez, Isabel; Bermejo, Marival; Souza, Jacqueline de
    Background Lychnophora trichocarpha (Spreng.) Spreng. ex Sch.Bip has been used in folk medicine to treat pain, inflammation, rheumatism and bruises. Eremantholide C, a sesquiterpene lactone, is one of the substances responsible for the anti-inflammatory and anti-hyperuricemic effects of L. trichocarpha. Objectives Considering the potential to become a drug for the treatment of inflammation and gouty arthritis, this study evaluated the permeability of eremantholide C using in situ intestinal perfusion in rats. From the permeability data, it was possible to predict the fraction absorbed of eremantholide C in humans and elucidate its oral absorption process. Methods In situ intestinal perfusion studies were performed in the complete small intestine of rats using different concentrations of eremantholide C: 960 μg/ml, 96 μg/ml and 9.6 μg/ml (with and without sodium azide), in order to verify the lack of dependence on the measured permeability as a function of the substance concentration in the perfusion solutions. Results Eremantholide C showed Peff values, in rats, greater than 5 × 10−5 cm/s and fraction absorbed predicted for humans greater than 85%. These results indicated the high permeability for eremantholide C. Moreover, its permeation process occurs only by passive route, because there were no statistically significant differences between the Peff values for eremantholide C. Conclusion The high permeability, in addition to the low solubility, indicated that eremantholide C is a biologically active substance BCS class II. The pharmacological activities, low toxicity and biopharmaceutics parameters demonstrate that eremantholide C has the necessary requirements for the development of a drug product, to be administered orally, with action on inflammation, hyperuricemia and gout.
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    Gliclazide : biopharmaceutics characteristics to discuss the biowaiver of immediate and extended release tablets.
    (2020) Mapa, Bruna de Carvalho; Araújo, Lorena Ulhôa; Barcellos, Neila Marcia Silva; Caldeira, Tamires Guedes; Souza, Jacqueline de
    The lists of essential medicines of the World Health Organization (WHO) and Brazil include gliclazide as an alternative to the oral antidiabetic drug of first choice, metformin, in the treatment of type 2 diabetes mellitus because of its pharmacokinetic profile and few side effects. Thus, it is also considered by WHO and the International Pharmaceutical Federation (FIP) as a drug candidate to biowaiver, which is the evaluation of how favorable the biopharmaceutics characteristics are in order to obtain waiver from the relative bioavailability/bioequivalence (RB/BE) studies to register new medicines. This paper presents a review about the solubility, permeability and dissolution of gliclazide. A critical analysis of the information allowed to identify gliclazide as a Biopharmaceutics Classification System (BCS) Class II drug. Therefore, new drugs in immediate release dosage forms will not be eligible for biowaiver. Regarding the extended release dosage forms, besides the limited solubility, no information on the comparative dissolution profile was found, which would be necessary to analyze a possible biowaiver for a smaller dosage. It can be concluded that the registration of new medicines containing gliclazide must undergo RB/BE studies, since there is not enough evidence to recommend the replacement and waiver of such studies for immediate and extended release formulations.
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    A sustainable UPLC-UV method for quantification of donepezil hydrochloride in biorelevant media applied to dissolution profile comparison.
    (2020) Campos, Débora Priscila de; Barcellos, Neila Marcia Silva; Marinho, Flávia Dias Marques; Barbosa, Guilherme Xavier; Lana, Victoria Luiza Vieira Vidigal; Souza, Jacqueline de
    Donepezil hydrochloride is one of the most prescribed anti-Alzheimer’s drugs, despite being available for more than two decades, chromatographic methods for the quantification of the drug in biorelevant media that mimics pH physiological conditions in vivo (pH 1.2, 4.5, and 6.8) are not available in the literature. These media are used in the dissolution test, an important tool, for registration and quality control of medicines. Considering the need for methods with this purpose, this work aimed to develop and validate a sustainable UPLC-UV method for quantification of donepezil hydrochloride in tablets, specifically on assay and dissolution profile, with reduced environmental impacts. The proposed method has a run time of 2 min and requires for each run, only 0.8 mL of solvents, providing excellent green analysis. The method proved to be selective, linear, precise, accurate, robust in the range of 2–14 mg/mL. Three products (reference, similar, and generic) were analyzed and showed very rapid dissolution. The average content varied from 100.2 ± 0.6% to 109.5 ± 2.1%. Using dissolution efficiency (DE), the drug release profiles were com pared in different biorelevant media.
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    Equilibrium solubility study to determine fexofenadine hydrochloride BCS class and challenges in establishing conditions for dissolution profiles applied to suspension.
    (2020) Rosa, Lorena de Sousa; Marinho, Flávia Dias Marques; Braga, Silmara Leôncio; Souza, Jacqueline de
    The aim of this work was to perform solubility studies for fexofenadine hydrochloride and establish dissolution conditions for this drug in oral suspension dosage form. The solubility study was executed through the shake-flask method, below 37 ºC±1 ºC, at 100 rpm stirring for 12 h in three buffer solutions: hydrochloric acid pH 2.0, acetate pH 4.5 and phosphate pH 6.8. The dissolution test was developed in vessels containing 900 mL of the same buffer, employing the paddle apparatus in speed of 25 and 50 rpm, below 37 ºC±0.5 ºC. The drug was classified as low solubility according to the Biopharmaceutics Classification System, since the dose/solubility ratio was higher than 250 mL in all media tested (326.55 mL in buffer pH 2.0; 2,456.33 mL in buffer pH 4.5 and 1,021.16 mL in buffer pH 6.8). The dissolution test showed that a release of 85% in 30 min could be established. The rotation speed of 25 rpm, media volume of 900 mL and insertion of the samples through weighted syringes are adequate. The buffered media pH 2.0 could be chosen as dissolution media.
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    The evaluation of valsartan biopharmaceutics properties.
    (2020) Castro, Lara Maria Lopes de; Souza, Jacqueline de; Caldeira, Tamires Guedes; Mapa, Bruna de Carvalho; Soares, Anna Flávia Matos; Gomes, Bruna Pegorelli; Croce, Carolina Carvalho Della; Barcellos, Neila Marcia Silva
    Background: Solubility, intestinal permeability and dissolution are the main factors that govern the rate and extent of drugs absorption and are directly related to bioavailability. Biopharmaceutics Classification System (BCS) is an important tool that uses in vitro results for comparison with bioavailability in vivo (biowaiver). Valsartan is widely used in the treatment of hypertension and shows different BCS classification in the literature (BCS class II or III). Objective: This work proposes the study of valsartan biopharmaceutics properties and its BCS classification. Method: High performance liquid chromatography (HPLC) method was developed and validated to quantify the drug in buffers pH 1.2, 4.5 and 6.8. Valsartan solubility was determined in these three different media using shake flask method and intrinsic dissolution rate. Evaluation of dissolution profile from coated tablets was conducted. Results: The low solubility (pH 1.2 and 4.5) and high solubility (pH 6.8) was observed for both solubility methods. Permeability data reported from literature showed that valsartan is a low permeability drug. Valsartan presented rapid release profile only in pH 6.8. Conclusion: We defined that valsartan is a class IV drug, in disagreement with what has been published so far. It is important to emphasize that the conditions considered here are the indicated to define the biopharmaceutics classification by regulatory agencies.