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Bol. latinoam. Caribe plantas med. aromát ; 21(3): 389-403, mayo 2022. ilus, tab
Article in English | LILACS | ID: biblio-1397080


This study evaluated the specific interactions between drug and polymers in amorphous spray dried dispersions (SDDs). Four Biopharmaceutics Classification System (BCS) II class drugs were evaluated. Binary and ternary SDDs were manufactured with conventional polymers and arabinogalactan. Specific interaction parameters between drug and polymer were determined using theoretical calculations and DSC data. Analytical methods were used to evaluate solid and solution state interactions. Maximum amorphous content for each formulation was calculated using DSC. Flory-Huggins Specific Interaction Parameters were calculated. Negative specific parameters were associated with solid-state interactions and improved capacity of drug in the amorphous state. Ternary SDDs containing drug, polymer, and arabinogalactan displayed similar hydrogen bonding as was observed with binary SDDs. Solution-state interactions observed in binary systems may be used in tertiary systems to improve the amorphous drug capacity and improved dissolution compared to the binary. The resultant tertiary systems are an improvement over binary drug polymer systems.

Este estudio evaluó las interacciones específicas entre el fármaco y los polímeros en dispersiones amorfas secadas por pulverización (SDD). Se evaluaron cuatro fármacos de clase II del Sistema de Clasificación Biofarmacéutica (BCS). Los SDD binarios y ternarios se fabricaron con polímeros convencionales y arabinogalactano. Los parámetros de interacción específicos entre el fármaco y el polímero se determinaron utilizando cálculos teóricos y datos de DSC. Se utilizaron métodos analíticos para evaluar las interacciones del estado sólido y de la solución. El contenido amorfo máximo para cada formulación se calculó usando DSC. Se calcularon los parámetros de interacción específicos de Flory-Huggins. Los parámetros específicos negativos se asociaron con interacciones en estado sólido y una capacidad mejorada del fármaco en el estado amorfo. Los SDD ternarios que contienen fármaco, polímero y arabinogalactano mostraron enlaces de hidrógeno similares a los observados con los SDD binarios. Las interacciones de estado de solución observadas en sistemas binarios pueden usarse en sistemas terciarios para mejorar la capacidad del fármaco amorfo y mejorar la disolución en comparación con el binario. Los sistemas terciarios resultantes son una mejora con respecto a los sistemas de polímeros de fármacos binarios.

Polymers/chemistry , Solubility , Pharmaceutical Preparations/chemistry , Biological Availability , Temperature , X-Ray Diffraction , Microscopy, Electron, Scanning , Spectroscopy, Fourier Transform Infrared , Proton Magnetic Resonance Spectroscopy
Rev. bras. cir. cardiovasc ; 37(1): 65-73, Jan.-Feb. 2022. tab, graf
Article in English | LILACS-Express | LILACS | ID: biblio-1365536


Abstract Introduction: In this study, Anzer propolis, which can only be obtained from the Eastern Black Sea region in Turkey, is studied for its effect on spinal cord ischemia/reperfusion injury. Methods: A total of 12 healthy male New Zealand White rabbits with an average weight of 3.0 to 3.5 kg were separated into two blind and randomized groups: the ischemia/reperfusion group (n=6) and the treatment group (n=6). Each rabbit in the treatment group was given a dose of 100 mg/kg of ethanol-dissolved Anzer propolis orally 1 hour before surgery. Blood samples were examined at the 0th hour and postoperatively at the 24th and 48th hours. Tissue samples were taken at the 48th hour during the sacrification. Results: There was a statistically significant difference between the two groups in terms of postoperative Tarlov scoring (P=0.012). There was a difference between the two groups in terms of the blood levels of interleukin-6 (IL-6) and tumor necrosis factor-alpha (TNF-α) at the 48th hour, myeloperoxidase (MPO) at the 24th and 48th hours, ischemia-modified albumin (IMA) at the 24th hour, and intercellular adhesion molecule-1 (ICAM-1) and total oxidant status (TOS) at the 48th hour (P<0.005). There was also a difference between the two groups in terms of apoptotic index data obtained with the terminal deoxynucleotidyl transferase (TdT)‐mediated dUTP nick‐end labelling (TUNEL) method in the histopathological examination (P=0.001). In the transmission electron microscopic (TEM) analysis, while ischemia/reperfusion group generally had axon-myelin separation, axoplasmic dissolution and myelin separation, the propolis treatment group had normal myelin sequencing. Discussion: In our study, after biochemical, histopathological, ultrastructural and neurological functional examination, it was demonstrated that Anzer propolis has sufficient neuroprotective effect on spinal cord ischemia/reperfusion injury in rabbits.

J. res. dent ; 10(1): 9-13, jan.-feb2022.
Article in English | LILACS, BBO | ID: biblio-1378178


Aim To evaluate physicochemical properties and semi-quantitative elemental analysis of AH Plus Jet with samples from the beginning, middle and final portions of the automix syringe system. Methodology Three experimental groups based on the source of the material used (beginning, middle and final portion) were established for each of the evaluated properties. Setting time, flow and radiopacity were evaluate following ANSI/ADA n. 57 specification. Set specimens was used in the semi-quantitative elemental analysis in an energy-dispersive X ray spectroscopy and scanning-electron microscopy (EDS/SEM). Statistical analysis was performed using one-way ANOVA followed by Tukey test (P<0.05). Results Flow, setting time, solubility and EDS/SEM tests showed no significant differences among the three portions of the automix syringe (P>0.05). Radiopacity test showed significant differences in the beginning of the syringe comparing to the middle and final portions (P<0.05). EDS/SEM analysis identified the presence of C, O, Al, Ca, Zr and W. The element Al, however, was found only in the final portion of the syringe. Conclusions The results of AH Plus Jet suggested an adequate ratio of the components, without segregation between organic and inorganic components, since the results of setting time, flow, solubility and EDS/SEM analysis presented similar values regardless of the portion of the syringe from where the sealer was taken.

Humans , Root Canal Filling Materials , Solubility , Chemical Phenomena
Braz. J. Pharm. Sci. (Online) ; 58: e191123, 2022. tab, graf
Article in English | LILACS | ID: biblio-1394050


Chemotherapy induced nausea and vomiting (CINV) and post-operative nausea and vomiting (PONV) is a problem, often occurs in patient. Inspite of high bioavailability, the demerits such as: hepatic first pass metabolism and invasive nature of oral and parenteral dosage forms can be avoided with anti-emetic therapy of transdermal device. The major objective of the present study is to modify the hydrochloride (HCl) form of Ondansetron (OND) to the base form followed by improvement of solubility and permeability of OND by employing solid dispersion (SD) loaded patches. Preformulation study, as observed, begins with an approach to enthuse solubility of OND by SD technique choosing different carriers. The choice of carriers was rationalized by phase solubility study. Several combinations of transdermal films were prepared with pure drug, carriers and SDs with plasticizer Ka values of OND-HPßCD binary system were found lower (54.43 to 187.57 M-1) than that of OND-PVP K-30 binary system (1156.77 to 12203.6 M-1). The drug content of SDs and patches were found satisfactory. Better permeation rate (236.48±3.66 µg/3.935 cm2) with promising flux enhancement (8.30 fold) was found with DBP loaded SD patch (P6*). Hence, enhancement of solubility and permeability of P6* ensures that it can successfully enhance the bioavailability

Plasticizers/adverse effects , Solubility , Ondansetron/antagonists & inhibitors , Patients/classification , Vomiting , Pharmaceutical Preparations/analysis , Postoperative Nausea and Vomiting , Dosage Forms , Drug Therapy/instrumentation , Methods , Motion Pictures/classification
Braz. dent. sci ; 25(2): 1-8, 2022. tab, ilus
Article in English | LILACS, BBO | ID: biblio-1370587


Objective: Resin-modified glass ionomer (RMGI) cements are among the commonly used restorative materials in low stress-bearing areas and also for temporary restorations. The competition between acid-base reactions and light polymerization reactions in delayed curing of RMGIs can affect their physical and mechanical properties, as well as their degree of conversion. Since solubility, color stability, and opacity are among the main physical properties affecting the durability and clinical service of RMGI restorations, this study aimed to assess the effect of delayed curing on solubility, color stability, and opacity of Fuji II LC RMGI. Material and Methods: This in vitro, experimental study evaluated 80 Fuji II LC RMGI specimens (10 specimens per each in 4 groups) in terms of solubility, color stability, and opacity at 6 months later. Specimens were cured immediately or were cured with 1, 5 and 10 min delay. Results: Maximum solubility and minimum change in opacity and color stability at 6 months were noted in the group with delayed curing by 10 min. A significant difference was noted in the solubility of specimens cured after 10 min and 1 min. Significant differences were also noted in the opacity and color stability of specimens cured after 10 min and all other groups (P < 0.05). Conclusion: Delayed curing by 1 min decreased the solubility of RMGI specimens compared with immediate curing or curing after 5 min. Although this difference did not reach statistical significance. Color stability and changes in opacity are mainly influenced by the acid-base reactions rather than polymerization reactions.(AU)

Objetivo: Cimentos de ionômero de vidro modificado por resina (CIVMR) estão entre os materiais restauradores mais comumente utilizados em áreas de baixa tensão e também para restaurações temporárias. A competição entre reações ácido-base e reações provenientes da fotopolimerização tardia dos CIVRMs podem afetar suas propriedades físicas e mecânicas, bem como seu grau de conversão. Uma vez que a solubilidade, estabilidade de cor e opacidade estão entre as principais propriedades físicas que afetam a durabilidade e o tempo de serviço clinico de restaurações de CIVMR, este estudo teve como objetivo avaliar o efeito da fotopolimerizaçao tardia na solubilidade, estabilidade de cor e opacidade do CIVMR Fuji II LC. Material e Métodos: Este estudo experimental in vitro avaliou 80 espécimes de CIVMR Fuji II LC (4 grupos com 10 espécimes cada) em termos de solubilidade, estabilidade de cor e opacidade apos 6 meses. As amostras foram fotopolimerizadas imediatamente ou com 1, 5 e 10 min de atraso. Resultados: Máxima solubilidade e mínima alteração na opacidade e estabilidade da cor em 6 meses foram observadas no grupo com fotopolimerização tardia em 10 min. Uma diferença significativa foi observada na solubilidade das amostras fotopolimerizadas após 10 min e 1 min. Diferenças significativas também foram observadas na opacidade e estabilidade de cor das amostras fotopolimerizadas após 10 min e em todos os outros grupos (P <0,05). Conclusão: A fotopolimerizaçao tardia em 1 min diminuiu a solubilidade das amostras CIVMR em comparação com a fotopolimerizaçao imediata ou após 5 min. Embora essa diferença não tenha alcançado significância estatística. A estabilidade da cor e as mudanças na opacidade são influenciadas principalmente por reações ácido-base, em vez de reações causadas pela polimerização(AU)

Solubility , Color , Glass Ionomer Cements
Braz. J. Pharm. Sci. (Online) ; 58: e20013, 2022. tab, graf
Article in English | LILACS | ID: biblio-1394062


The aim of the present study is to improve the solubility and antimicrobial activity of 3-(3-(2-chlorophenyl)prop-2-enoyl)-4-hydroxycoumarin by formulating its inclusion complexes with 2-hydroxypropyl-ß-cyclodextrin in solution and in solid state. The phase solubility study was used to investigate the interactions between 3-(3-(2-chlorophenyl)prop-2-enoyl)-4-hydroxycoumarin and 2-hydroxypropyl-ß-cyclodextrin and to estimate the molar ratio between them. The structural characterization of binary systems (prepared by physical mixing, kneading and solvent evaporation methods) was analysed using the FTIR-ATM spectroscopy. The antimicrobial activity of 3-(3-(2-chlorophenyl)prop-2-enoyl)-4-hydroxycoumarin and inclusion complexes prepared by solvent evaporation method was tested by the diffusion and dilution methods on various strains of microorganisms. The results of phase solubility studies showed that 3-(3-(2-chlorophenyl)prop-2-enoyl)-4-hydroxycoumarin formed the inclusion complexes with 2-hydroxypropyl-ß-cyclodextrin of AP type. The solubility of 3-(3-(2-chlorophenyl)prop-2-enoyl)-4-hydroxycoumarin was increased 64.05-fold with 50% w/w of 2-hydroxypropyl-ß-cyclodextrin at 37 oC. The inclusion complexes in solid state, prepared by the solvent evaporation method, showed higher solubility in purified water and in phosphate buffer solutions in comparison with 3-(3-(2-chlorophenyl)prop-2-enoyl)-4-hydroxycoumarin alone. The inclusion complexes prepared by solvent evaporation method showed higher activity on Bacillus subtilis and Staphylococcus aureus compared to uncomplexed 3-(3-(2-chlorophenyl)prop-2-enoyl)-4-hydroxycoumarin due to improved aqueous solubility, thus increasing the amount of available 3-(3-(2-chlorophenyl)prop-2-enoyl)-4-hydroxycoumarin that crosses the bacterial membrane.

Solubility , Cyclodextrins/agonists , Anti-Infective Agents , Spectrum Analysis/instrumentation , Staphylococcus aureus/classification , Bacillus subtilis/classification , Spectroscopy, Fourier Transform Infrared , Dilution
Ciênc. rural (Online) ; 52(1): e20200723, 2022. tab, graf
Article in English | LILACS-Express | LILACS, VETINDEX | ID: biblio-1286034


ABSTRACT: The effect of methods to remove protein content on the properties of glucosamine hydrochloride from the shells of white leg shrimp (Litopenaeus vannamei) and black tiger shrimp (Penaeus monodon) was investigated. Chitin from shrimp shells was obtained by demineralization in 6% HCl for 12h, deproteinization by two different methods (first group soaked in 8% NaOH for 36h and second group treated in Alcalase enzyme at the concentration of 0.2% for 36h). Two group samples were converted to glucosamine hydrochloride by soaking in 36.76% HCl solution for 5h at 85 °C. The results of fourier transform infrared spectroscopy (FTIR), solubility and recovery yield analysis showed that deproteinization methods did not significantly affect the properties of glucosamine hydrochloride. However, glucosamine hydrochloride from white leg shrimp shells contained higher recovery yield and solubility than black tiger shrimp shells.

RESUMO: Investigou-se o efeito de métodos para remover o conteúdo de proteínas nas propriedades do cloridrato de glucosamina das conchas de camarão de pernas brancas (Litopenaeus vannamei) e camarão de tigre preto (Penaeus monodon). A quitina das cascas de camarão foi obtida por desmineralização em HCl a 6% por 12 h, desproteinização por dois métodos diferentes (primeiro grupo embebido em NaOH a 8% por 36 h e segundo grupo tratado na enzima Alcalase na concentração de 0,2% por 36 h). Duas amostras de grupo foram convertidas em cloridrato de glucosamina por imersão em solução de 12M HCl por 5 h a 85 °C. Os resultados das análises de FTIR, solubilidade e rendimento de recuperação mostraram que os métodos de desproteinização não afetaram significativamente as propriedades do cloridrato de glucosamina. No entanto, o cloridrato de glucosamina de cascas de camarão de pernas brancas continha maior rendimento e solubilidade de recuperação do que as cascas de camarão tigre preto.

Chinese Journal of Biotechnology ; (12): 749-759, 2022.
Article in Chinese | WPRIM | ID: wpr-927741


Genistein and its monoglucoside derivatives play important roles in food and pharmaceuticals fields, whereas their applications are limited by the low water solubility. Glycosylation is regarded as one of the effective approaches to improve water solubility. In this paper, the glycosylation of sophoricoside (genistein monoglucoside) was investigated using a cyclodextrin glucosyltransferase from Penibacillus macerans (PmCGTase). Saturation mutagenesis of D182 from PmCGTase was carried out. Compared with the wild-type (WT), the variant D182C showed a 13.42% higher conversion ratio. Moreover, the main products sophoricoside monoglucoside, sophoricoside diglucoside, and sophoricoside triglucoside of the variant D182C increased by 39.35%, 56.05% and 64.81% compared with that of the WT, respectively. Enzymatic characterization showed that the enzyme activities (cyclization, hydrolysis, disproportionation) of the variant D182C were higher than that of the WT, and the optimal pH and temperature of the variant D182C were 6 and 40℃, respectively. Kinetics analysis showed the variant D182C has a lower Km value and a higher kcat/Km value than that of the WT, indicating the variant D182C has enhanced affinity to substrate. Structure modeling and docking analysis demonstrated that the improved glycosylation efficiency of the variant D182C may be attributed to the increased interactions between residues and substrate.

Cyclodextrins , Genistein , Glucosyltransferases/metabolism , Glycosylation , Kinetics
Acta Pharmaceutica Sinica ; (12): 331-342, 2022.
Article in Chinese | WPRIM | ID: wpr-922912


Ionic liquids (ILs) are liquid mixtures formed by anions and cations in a certain stoichiometric ratio under certain conditions. They are widely used in various fields because of their simple preparation process, low volatility, high stability, high conductivity and non-flammability. Here, we firstly introduce their formation principles, classification, and physical and chemical properties in detail. Then, we summarize their functions in pharmaceutical preparations, such as improving the solubility of insoluble drugs, enhancing the stability of drugs, and promoting the permeability of drugs, as well as their role as active pharmaceutical ingredients (API) to fabricate new drug delivery systems of API-ILs. Finally, we reviewed the applications of ILs in different administration routes, including oral, transdermal, mucosal, and injection routes, and meanwhile offer perspectives for the further use of ILs.

São Paulo; s.n; s.n; 2022. 70 p. tab, graf.
Thesis in English | LILACS | ID: biblio-1392313


The purpose of this work was to elaborate a diagnosis of the dissolution test in Africa in comparison with Brazil, evaluating the dissolution profile of low solubility drugs such as albendazole, ibuprofen, furosemide, glibenclamide, hydrochlorothiazide and carvedilol to ascertain their quality. The dissolution profiles were evaluated by utilizing the United States Pharmacopeia (USP). The glibenclamide medicine was evaluated according to the Food and Drug Administration (FDA), while a dissolution method was developed for the carvedilol medicine. A filter selection test for all the drugs showed that cannula is suitable for all, except for carvedilol, which is centrifuged. The various brands of Nigerian and Brazilian medicines tested showed some statistical differences. The suitable conditions that allowed the dissolution of carvedilol to be determined were the USP type II apparatus at 75 rpm containing 900 mL of acetate buffer, pH 4.5. The results of the dissolution test showed that out of the 17 different brands of Brazilian medicines and 17 different products from Nigeria, 94.12% and 58.82% passed respectively

O objetivo deste trabalho foi elaborar um diagnóstico do teste de dissolução na África em comparação ao Brasil, avaliando o perfil de dissolução de medicamentos de baixa solubilidade como albendazol, ibuprofeno, furosemida, glibenclamida, hidroclorotiazida e carvedilol para verificar sua qualidade.Os perfis de dissolução foram avaliados utilizando a Farmacopeia dos Estados Unidos (USP). O medicamento glibenclamida foi avaliado de acordo com a Food and Drug Administration (FDA), enquanto um método de dissolução foi desenvolvido para o medicamento carvedilol.Um teste de seleção de filtro para todos os medicamentos mostrou que a cânula é adequada para todos, exceto para o carvedilol, que é centrifugado. As diversas marcas de medicamentos Nigerianos e Brasileiros testadas apresentaram algumas diferenças estatísticas. As condições adequadas que permitiram a determinação da dissolução do carvedilol foram o aparelho USP tipo II a 75 rpm contendo 900 mL de tampão acetato, pH 4,5. Os resultados do teste de dissolução mostraram que das 17 diferentes marcas de medicamentos brasileiros e 17 diferentes produtos da Nigéria, 94,12% e 58,82% foram aprovados, respectivamente

Solubility , Brazil/ethnology , Pharmaceutical Preparations/analysis , Africa/ethnology , Dissolution , United States Food and Drug Administration , Albendazole/pharmacology , Ibuprofen , Carvedilol/pharmacology , Furosemide/pharmacology , Methods , Acetates/adverse effects
Article in Chinese | WPRIM | ID: wpr-920659


@#Water content determination is an important aspect of quality research in the whole process of pharmaceutical development, production, storage and use.Therefore, it is significant to develop an accurate and robust method for the determination of water content in the quality control of pharmaceuticals.In this article, the selection and strategy for the study of water determination methods are explained on the basis of general water determination principles and application examples in Chinese and foreign pharmacopoeias, together with the analysis of sample structure, solubility and water content.This article aims to provide basis for the development of moisture testing methods and formulation of proper quality standards for pharmaceuticals.

Dent. press endod ; 11(2)maio-ago.2021. Ilus
Article in English | LILACS | ID: biblio-1377855


Introdução: A solubilidade é uma propriedade relaciona- da à dissociação dos constituintes do material, pela ação do contato com o líquido circundante. Introdução: O objetivo do presente estudo foi avaliar o efeito da hidratação durante a varredura com microtomografia (micro-TC) sobre a alteração volumétrica do MTA HP. Métodos: foram utilizados 20 dentes incisivos superiores de acrílico com cavidade retrógrada. O cimento MTA HP foi inserido na cavidade com um condensador Paiva. As amostras foram inspecionadas visualmente com uma lupa de 5x, para garantir que não permanecessem espaços vazios ou lacunas. Os espécimes foram divididos em dois grupos (n=10). Os dentes foram escaneados logo após o manuseio do MTA. Para o grupo com imersão em água, Eppendorf hidratado foi mantido com 1mL de água durante a varredura; no outro grupo, os dentes foram escaneados sem água. Nos dois grupos, os dentes foram imersos em água durante sete dias. Em seguida, os dentes foram escaneados novamente em micro-TC usando os mesmos parâmetros e condições de cada grupo. Foi realizada a reconstrução das imagens pelo software Nrecon e o volume de solubilidade, determinado pelo software CTan, analisando-se a variação volumétrica. Resultados: O grupo de corpos de prova escaneados imersos na água apresentou maior variação volumétrica, com diferenças estatisticamente significativas em relação ao grupo escaneado sem imersão. O escaneamento do corpo de prova imerso em água favorece uma maior perda volumétrica do material. Conclusão: Os estudos para avaliar a variação volumétrica de cimentos de silicato de cálcio devem ser feitos com imersão em água.

Introduction: Solubility is a property related to the dissocia- tion of the constituents of the material by the action of contact with the surrounding liquid, for this reason, the aim of this study was to evaluate the effect of the hydration during the scanning in the microtomography on the volumetric alteration of the MTA HP. Methods: Twenty acrylic teeth upper incisor with retrograde cavity were utilized. The MTA HP cement was inserted into the cavity using a Paiva condensor. The specimens were visually inspected with a 5x magnifying glass to ensure they did not remain void or gaps. The specimens were divided into 2 groups (n=10). The teeth were scanned shortly after handling the MTA. For the group with water immersion, hydrated Eppendorf was kept with 1mL the water during the scanning and the other group, the teeth were scanning without water. In the two groups the teeth were immersed into water during 7 days. Next the teeth were newly scanned in the Micro-CT using the same parameters and conditions of each group. Reconstruction of images by the Nrecon software and the solubility volume determined by the CTan, analyzing the volumetric change. Results: The group of specimens scanned immersed into the water presented higher volumetric change with statistically significant differences in relation the group scanned without immersion. The scanning of the specimen immersed in water favors the greater volumetric loss of the material. Conclusion: Studies to evaluate volumetric change of calcium silicate cements should be made immersed in wate

Pemetrexed , Immersion , Minerals , Solubility , Methods
Acta Pharmaceutica Sinica B ; (6): 2914-2923, 2021.
Article in English | WPRIM | ID: wpr-888894


Cyclodextrin metal-organic framework (CD-MOF) as a highly porous supramolecular carrier could be one of the solutions to the insolubility of isosteviol (STV). The solubility of STV was lower than 20.00 ng/mL at pH 1.0 and pH 4.5, whilst its solubility increased to 20,074.30 ng/mL at pH 6.8 and 129.58 ng/mL in water with a significant pH-dependence. The

Acta Pharmaceutica Sinica B ; (6): 2585-2604, 2021.
Article in English | WPRIM | ID: wpr-888873


Invasive fungal infections (IFIs) represent a growing public concern for clinicians to manage in many medical settings, with substantial associated morbidities and mortalities. Among many current therapeutic options for the treatment of IFIs, amphotericin B (AmB) is the most frequently used drug. AmB is considered as a first-line drug in the clinic that has strong antifungal activity and less resistance. In this review, we summarized the most promising research efforts on nanocarriers for AmB delivery and highlighted their efficacy and safety for treating IFIs. We have also discussed the mechanism of actions of AmB, rationale for treating IFIs, and recent advances in formulating AmB for clinical use. Finally, this review discusses some practical considerations and provides recommendations for future studies in applying AmB for combating IFIs.

Article in Chinese | WPRIM | ID: wpr-888177


In this study, we studied the solubility and permeability of matrine, oxymatrine, sophoridine, and oxysophocarpine, four alkaloids in the Mongolian herbal medicine Sophorae Flavescentis Radix, and evaluated the absorption mechanism with the Caco-2 cell model, so as to provide a basis for the new drug development and efficacy evaluation of Sophorae Flavescentis Radix. The results showed that all the four alkaloids had high solubility and high permeability and can be well absorbed, belonging to the class-I drugs of Biopharmaceutical Classification System(BCS). The absorption(AP→BL) and excretion(BL→AP) of matrine and oxymatrine were not affected by the concentration while the absorption depended on P-gp protein. The absorption(AP→BL) and excretion(BL→AP) of sophoridine and oxysophocarpine were positively related to the concentration and time, and the absorption process was independent from P-gp protein. The results provide scientific reference and an experimental basis for the development of Mongolian medical prescriptions containing Sophorae Flavescentis Radix.

Alkaloids , Biological Products , Caco-2 Cells , Drugs, Chinese Herbal , Herbal Medicine , Humans , Sophora
Acta Pharmaceutica Sinica ; (12): 2282-2288, 2021.
Article in Chinese | WPRIM | ID: wpr-887048


The object of this study is to preparate the berberine hydrochloride (BBH) resin compound with taste masking effect. We took the BBH as the model drug and Amberlite IRP69 as the drug carriers, uncovered the curve of solubility of BBH in different cosolvent with a certain range of temperature, and then used it to calculate the parameters during the preparation of the complex such as adding quantity of BBH and the reaction temperature. Afterwards, the characteristic and in vitro release experiments were studied to verify the formation and predict the in vivo release behavior of the complex. The results showed that in the condition of using 60% ethanol as a cosolvent and stirring at 50 ℃ for 1 h, the drug loading and drug availability of the complex are at about 35% and 64%, respectively, and has a better taste-masking effect. In this study, a method was provided for preparing a taste-masking preparation of BBH.

Acta Pharmaceutica Sinica ; (12): 1902-1910, 2021.
Article in Chinese | WPRIM | ID: wpr-887017


Nanocrystal drugs have many advantages, such as no carrier materials, easy industrialization, diversified dosage forms, and can significantly improve the solubility and bioavailability of insoluble drugs, so many drugs have been on the market. The traditional nanocrystal preparation technology has the problems of low preparation efficiency and process limitation of the smallest achievable particle size. With the progress of pharmaceutical preparation technology, the preparation technology of nanocrystal drugs is constantly improving, and new preparation technologies are constantly emerging. The emergence of new technologies has greatly shortened the process time and makes it possible to prepare nanocrystal drugs with smaller particle diameters. In this paper, the preparation technologies of nanocrystal drugs, especially the new preparation technologies such as high gravity controlled precipitation, microfluidic reaction technology and various combination technologies, are reviewed from three aspects: "Top-down" technology, "Bottom-up" technology and combination technology. This article also prospects the development of new preparation technologies, hoping to provide reference for the related research of nano-preparations.

São Paulo; s.n; s.n; 2021. 176 p. tab, graf.
Thesis in Portuguese | LILACS | ID: biblio-1396454


A baixa solubilidade aquosa dos insumos farmacêuticos ativos (IFA) é um grande desafio no desenvolvimento de formulações farmacêuticas, pois pode resultar em biodisponibilidade insuficiente e variável. Diversas estratégias de modificação do estado sólido dos compostos ativos, têm sido propostas para incrementar a solubilidade de fármacos pouco solúveis em água. Dentre as estratégias abordadas a ispersão sólida (DS) é uma das formas mais promissoras de aumentar a solubilidade, dissolução e a biodisponibilidade de IFAs com baixa solubilidade aquosa. O efavirenz (EFV) é um inibidor não nucleosídeo da transcriptase reversa (NNRTI) e um dos componentes da terapia antirretroviral de alta atividade (HAART), sendo parte da primeira linha de tratamento de infecções do vírus HIV tipo 1. O antirretroviral está classificado como pertencente à classe II do SCB, e exibe baixa solubilidade aquosa (solubilidade menor que 10 µg/mL) e alta permeabilidade com absorção dependente da taxa de dissolução, resultando em biodisponibilidade oral baixa e variável. A administração de fármacos pouco solúveis na forma de DS é um método atraente para aumentar a biodisponibilidade in vivo. Neste estudo, um método de triagem rápida por evaporação de solvente foi empregado para preparar DS de EFV, variando-se proporções em misturas compostas pelos carreadores, polivinilpirrolidona K-28/32 (PVP K-28/32), copovidona (CoPVP), hidroxipropilmetilcelulose ftalato (HPMCP-50, HPMCP-55 e HPMCP-55s), poloxâmero 188 (P188) e poloxâmero 407 (P407). A solubilidade das DS foi avaliada por meio do método do equilíbrio (shake-flask), onde selecionou-se os polímeros P188 e P407 que conduziram a uma elevada capacidade de saturação em meio aquoso, superior a 1.000 vezes ao fármaco puro. As propriedades físico-químicas e do estado sólido das amostras foram avaliadas por meio de calorimetria exploratória diferencial (DSC); termogravimetria (TG); espectroscopia do infravermelho com transformada de Fourier (FTIR), difratometria de raios X pelo método do pó (DRXP) e ensaios de dissolução com emprego do aparato IV USP. Os resultados de DRXP demonstraram que os carreadores P188 e P407 foram capazes de estabilizar o EFV na forma amorfa nas DS, fato esse evidenciado pela ausência de picos característicos do antirretroviral

he low aqueous solubility of the active pharmaceutical ingredient (API) is a major challenge in the development of pharmaceutical formulations as it may result in insufficient and variable bioavailability. Several strategies for modifying the solid-state of the active compounds have been proposed to increase solubility of drugs that are poorly soluble in water. Among the strategies approaches, solid dispersion (SD) is one of the most promising ways to increase solubility, dissolution and bioavailability of APIs with low aqueous solubility. Efavirenz (EFV) is a non-nucleoside reverse transcriptase inhibitor (NNRTI) and one of the components of highly active antiretroviral therapy (HAART), being part of the first line of treatment of type 1 HIV virus infections. The antiretroviral is classified as belonging to BCS class II, and exhibits low aqueous solubility (solubility less than 10 µg / mL) and high permeability with dissolution ratedependent absorption, resulting in low and variable oral bioavailability. Drug delivery of poorly aqueous soluble drugs in form SD is an appealing method to increase in vivo bioavailability. In this study, a fast screening method of solvent evaporation method was used to prepare EFV SD, varying the proportions in mixtures composed by the carriers polyvinylpyrrolidone K-28/32 (PVP K-28/32), copovidone (CoPVP), hydroxypropylmethylcellulose phthalate (HPMCP-50, HPMCP-55 e HPMCP-55s), poloxamer 188 (P188) e poloxamer 407 (P407). The solubility of the samples was evaluated by the method of equilibrium (shake-flask), wherein the polymers P188 and P407 were selected due to the capacity to promote high saturation in aqueous medium, 1,000 times superior to the pure drug. The physicochemical and solid-state properties of the samples were evaluated by differential scanning calorimetry (DSC); thermogravimetry (TG); Fourier transform infrared spectroscopy (FTIR), X-ray powder diffraction (XRPD) and dissolution assays using the IV USP apparatus. The results of XRPD demonstrated that the carriers P188 and P407 were able to stabilize the EFV in amorphous form in the SD, a fact evidenced by the absence of characteristic peaks of the antiretroviral

Pharmaceutical Preparations/administration & dosage , Pharmaceutical Raw Material , Dissolution , Spectrum Analysis/instrumentation , Calorimetry, Differential Scanning/methods , RNA-Directed DNA Polymerase/adverse effects , Spectroscopy, Fourier Transform Infrared , Poloxamer/analogs & derivatives , Antiretroviral Therapy, Highly Active/instrumentation , Hypromellose Derivatives/metabolism , Fourier Analysis
Braz. J. Pharm. Sci. (Online) ; 57: e18910, 2021. tab, graf
Article in English | LILACS | ID: biblio-1345454


Chemotherapy induced nausea and vomiting (CINV) is an issue, which usually occurs in cancer patient. Despite high bioavailability of oral and intravenous administration, these have some drawbacks. The oral route causes hepatic first pass metabolism and intravenous route is invasive in nature. Hence, antiemetic drug by means of transdermal route is necessary to administer in such cases. The aim of the present investigation is to develop suitable Transdermal Therapeutic System (TTS) with an objective to enhance solubility and skin permeability properties of metoclopramide base. Preformulation study begins with an approach to enhance solubility of 40 metoclopramide base by solid dispersion technique. transdermal films were prepared with 41 the solid dispersion as well as with pure drug. Phase solubility study at various temperatures reveals binding constants (Ka, 95-350 M-1 for PVP K30; 56-81 M-1 for HPßCD). Spontaneity of solubilization was justified by AL type linear profiles. The films showed satisfactory diffusion (%), permeation rate and flux after 8 h study. The transdermal patches as prepared were analyzed under FTIR, DSC and SEM. Both solubility and permeability rate in this investigation have been enhanced. So, it can be affirmed that this route would effectively enhance bioavailability

Solubility , Metoclopramide/antagonists & inhibitors , Patients/classification , Pharmaceutical Preparations/administration & dosage , Biological Availability , Spectroscopy, Fourier Transform Infrared , Diffusion/drug effects , Drug Therapy , Administration, Intravenous/instrumentation , Motion Pictures , Neoplasms/pathology