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@#In order to mask the bitterness of azithromycin (AZI) and individually regulate the drug release rate to reduce gastrointestinal irritation, immediate-release AZI-AmberliteTM IRP64/HPC and delayed-release AZI-AmberliteTM IRP69/RS100 were prepared by modifying with hydroxypropyl cellulose (HPC) and Eudragit RS100, respectively, and further combined to achieve controlled release.The drug loading and drug utilization rate of AZI-ion exchange resin complexes were measured; the structure of AZI-ion exchange resin complexes was characterized by differential scanning calorimetry and X-ray diffraction; and the wetting humidity, odor masking effects, in vitro dissolution and release behaviors were determined.The results showed that the formation of AZI-ion exchange resin complexes changed the original crystallization state of the drug, that the 2.5% HPC-modified AZI-AmberliteTM IRP64/HPC and the 0.5% RS100-modified AZI-AmberliteTM IRP69/RS100 demonstrated good taste masking effect, and that their combination in the drug content ratio of 13∶67 achieved the expected drug release behavior, i.e.rapid release of AZI in the first 10 min and smooth release in the later 6 h.These results indicated that the AZI-ion exchange resin complexes prepared by surface modification and their composites could mask the bitterness of AZI and realize the flexible adjustment of drug release rate, which lays the foundation for the research and development of new AZI preparations.
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With the implementation of the two-child policy and the growing demand for child health, pediatric medication has been arousing widespread social concern. To develop the drugs suitable for children, including new compounds, new specifications and new dosage forms, is urgently required for pharmaceutical researchers. In this review, several technical bottlenecks for pediatric oral liquid preparations, as well as the novel strategies involved in drug nanocrystals, self-microemulsion, ion exchange resin and Pickering emulsion were discussed, which may be benefit to play a theoretical guiding role in the research and development of children's oral liquid formulation.
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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.
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OBJECTIVE： To establish the separation and purification technology of sanguinarine from the extract of Macleaya cordata with ion exchang resin. METHODS： The content of sanguinarine from the extract of M. cordata was determined by HPLC， with Cosmosil C18-R-Ⅱ column （250 mm×4.6 mm，5 μm）， mobile phase of acetonitrile-0.2％ acetic acid solution （25 ∶ 75，V/V）， the flow rate of 1 mL/min， detection wavelength of 270 nm， column temperature of 30 ℃， and sample size of 20 μL. Static adsorption and desorption tests were carried out to compare the adsorption and desorption properties of 8 ion exchange resins for sanguinarine. The optimum concentration of sample solution， pH value and volume of sample were investigated by optimum ion exchange resin. APPS 10D liquid phase preparation system was used to investigate the dynamic elution conditions and obtain M. cordata refined extract solution. The refined purified product of M. cordata was obtained by desalination， elution on a reversed-phase （RP） C18 column and drying. The purity of the purified product was analyzed by HPLC. The structure of the purified product was confirmed by HPLC， UV spectrophotometry， MS and NMR. RESULTS： CM-FF resin was screened for the separation and purification of sanguinarine from M. cordata extract. It was eluted with 20 mmol/L ammonium acetate solution 100 mL containing 20％ methanol and 0.25 mol/L sodium chloride. The optimal dynamic absorption condition included that the concentration of sample was 6.0 mg/mL at pH 5.0，and the loading amount was 25 mL； after desalination and refinement， for the eluted refined extract， the purified product with 97％ purity （purified yield of 71％） was obtained， and its structure was confirmed to be sanguinarine. CONCLUSIONS： The optimal separation and purification technology by ion exchange resin is green， safe， efficient and easy to operate， which can be used for the separation and purification of sanguinarine from M. cordata extract and is suitable for industrial production.
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OBJECTIVE: To prepare and characterize paroxetine resinate, and evaluate the in vitro drug release rate and taste-masking effect. METHODS: A full factorial design was first conceived and applied to screen some process and formulation parameters (reaction temperature, stirring speed, drug concentration in solution and the ratio of resin to drug) on the key responses of resinationprocess, such as drug utilization ratio, drug loading and complexation constant. The paroxetine resinate was then characterized and evaluated by scanning electronic microscope (SEM), differential scanning calorimetry (DSC), in vitro drug release test and panel test of taste-masking. RESULTS: The resin/drug ratio and reaction temperature were identified as the most important factors on paroxetine resinate preparation.The drug-resin complex was successfully formed via ion exchange mechanism rather than physical absorption with complete in vitro drug release (>96%) in acidic or salt solution and good taste-masking effect. CONCLUSION: Paroxetine resinate with good performance can be prepared via optimization of process and formulation parameters, which will facilitate the development of generic paroxetine suspension.
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Objective: To establish a simple and effective extraction method for the preparation of total saponins of Panax japonicas (TSPJ). Methods: Combination of macroporous adsorption and ion exchange resin chromatography was adopted in the present study. For quality evaluation, chikusetsusaponin IVa was used as reference, and vanillin-perchloric acid was applied as chromogenic reagent to determine total saponin content at 545 nm. Results: X-5 macrophous resin offered better adsorption and desorption capacities for TSPJ than other macrophous resins. The optimum purification process was confirmed as follows: The sample solution concentration was 0.2 mg/L; The sample volume was 10 g/g, and eluting with 5 mL of 70% aqueous ethanol solutions on 1 g wet macrophous resin column. Followed this step, decoloring of TSPJ was studied and the decoloring capacity of two different types of ion exchange resins was evaluated. The result showed that 732-type cation exchange resin was the better resin for decolorization of the TSPJ. The total saponin products with higher purity and quality were obtained, with the mass fraction more than 85.0%, and the transfer rate of TSPJ was more than 70.0%. Conclusion: The results show that the total saponins can be separated and purified effectively from P. japonicus. The preparation method is simple, effective, and efficient for large-scale preparation of TSPJ.
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AIM@#To prepare high-purity ginseng total saponins from a water decoction of Chinese ginseng root.@*METHOD@#Total saponins were efficiently purified by dynamic anion-cation exchange following the removal of hydrophilic impurities by macroporous resin D101. For quality control, ultrahigh-performance liquid chromatography with a charged aerosol detector (CAD) was applied to quantify marker components. The total saponin content was estimated by a colorimetric method using a vanillin-vitriol system and CAD response.@*RESULTS@#D201, which consisted of a cross-linked polystyrene matrix and -N(+)(CH3)3 functional groups, was the best of the four anion exchange resins tested. However, no significant difference in cation exchange ability was observed between D001 (strong acid) and D113 (weak acid), although they have different functional groups and matrices. After purification in combination with D101, D201, and D113, the estimated contents of total saponins were 107% and 90% according to the colorimetric method and CAD response, respectively. The total amount of representative ginsenosides Re, Rd, Rg1, and compound K was approximately 22% based on ultrahigh-performance liquid chromatography-CAD quantitative analysis.@*CONCLUSION@#These findings suggest that an ion exchange resin, combined with macroporous adsorption resin separation, is a promising and feasible purification procedure for neutral natural polar components.
Subject(s)
Adsorption , Chromatography, Ion Exchange , Methods , Drugs, Chinese Herbal , Chemistry , Ion Exchange Resins , Chemistry , Panax , Chemistry , Plant Roots , Chemistry , Porosity , Saponins , ChemistryABSTRACT
Objective: To research the adsortpion and separation function of ion-exchange resin on 5-hydroxytryptophan (5-HTP) in extract from the seeds of Griffonia simplicifolia and to screen the ion-exchange resin with high selective adsorption. Methods: The static adsorptive properties of eight different types of ion-exchange resins were evaluated using adsorptive content, desorption rate, adsorption rate, and adsorption temperature as indexes in order to optimize the resin. And the effects of different pH values, injection rates, injection concentration, eluent concentration, and elution rates on adsorptive properties of resins were investigated. Results: The 001 × 7 cation exchange resin showed the best comprehensive adsorption property. The loading solution concentration was 10.8 mg/mL, the pH value was 3.5, the flow rate of loading solution was 4.0 mL/min, and 3BV 7.0% ammonia water solution in 3.0 mL/min velocity was used to elute. In this process, the product was obtained with the 5-HTP purity of greater than 99.0% and the ash content of less than 1.0%, product average yield was 7.95% and the product quality could meet the market demand. Conclusion: The 001 × 7 cation exchange resin shows a better comprehensive adsorption property. It could be used to isolate and purify the 5-HTP for scale production.
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Nonsteroidal anti-inflammatory drugs (NSAIDs) are the most widely used of all analgesic agents in the world. In arthritis, NSAIDs are considered to be the major option in therapy but off-late the incidence of gastric side effects have been cause for concern. Diclofenac-colestyramine is an improved formulation of diclofenac which utilizes the ion-exchange resin drug delivery technology. The review of literature and pharmacokinetics of diclofenac-colestyramine reveals a unique quick-slow effect for both acute as well as chronic pain. The faster onset of action, the sustained-release effect, lower gastric side effects add on to the superior potency of diclofenac to provide effective pain relief in arthritis and postoperative pain/outcomes. Twice-daily dosing helps improve the patient compliance - a very important factor in treatment of chronic diseases like arthritis.
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Bitter taste of ofloxacin, a broad spectrum bactericidal agent, is masked and orally disintegrating tablets were formulated. The bitter taste is masked by forming complex between drug and weak cation exchange resins, Tulsion 335 and Indion 204. Effect of pH and drug:resin ratio on the drug loading was studied. Maximum drug loading was observed at pH 6. Ratio of 1:2 of drug:resin masked almost complete bitterness of ofloxacin. Formation of complexes was confirmed by IR spectroscopy. Physical characterization of taste masked complexes was carried out. Present work envisages the taste masking of ofloxacin and development of orally disintegrating tablets. The effect of pH and resin quantities on drug loading were studied to find the optimum conditions of drug loading for complete taste masking. Effect of superdisintegrants like sodium starch glycolate, croscarmellose sodium and polyplasdone XL at varying level on physical parameters of compressed tablets was also assessed. The formulations containing 5 % w/w polyplasdone XL showed about 90 % of drug release within 5 minutes. No significant differences were observed in the physical parameters of resinates as well as tablets prepared from Tulsion 335 and Indion 204.
O gosto amargo de ofloxacina, agente bactericida de largo espectro, é mascarado e formularam-se comprimidos dispersíveis. O sabor amargo é mascarado pela formação de complexo entre o fármaco e resinas de troca catiônica fraca, Tulsion 335 e Indion 204. Efeito do pH e da proporção fármaco: resina sobre a carga de fármaco foi estudada. Carga de fármaco máxima foi observada em pH 6. Proporção 1:2 do fármaco: resina mascarou quase completamente o gosto amargo de ofloxacina. A formação de complexos foi confirmada por espectroscopia no IV. Caracterização física dos complexos de sabor mascarado foi realizada. O presente trabalho preconiza o mascaramento do gosto de ofloxacina e desenvolvimento decomprimidos por via oral, se desintegrando. O efeito do pH e da resina quantidades de carga de fármaco foram estudadas paraencontrar as condições óptimas de carga de fármaco para dissimulação do saborcompleto. Efeito da superdisintegrants como amido glicolato de sódio, croscarmelose sódica e Polyplasdone XL em diferentes níveis de parâmetros físicos de comprimidos também avaliados foi avaliada. As formulações contendo 5 %w/w Polyplasdone XL mostraram cerca de 90% de libertação do fármaco no prazo de 5 minutos. Não foram observadas diferenças significativas nos parâmetros físicos de resinatosbem como comprimidos preparados a partir de Tulsion 335 e Indion 204.
Subject(s)
Tablets/pharmacokinetics , Ofloxacin/analysis , Ion Exchange Resins/pharmacokinetics , Hepatocyte Growth Factor/classificationABSTRACT
In the present work, the effect of bed expansion on BSA adsorption on Amberlite IRA 410 ion-exchange resin was studied. The hydrodynamic behavior of an expanded bed adsorption column on effects of the biomolecules and salt addition and temperature were studied to optimize the conditions for BSA recovery on ion-exchange resin. Residence time distribution showed that HEPT, axial dispersion and the Pecletl number increased with temperature and bed height, bed voidage and linear velocity. The binding capacity of the resin increased with bed height. The Amberlite IRA 410 ion-exchange showed an affinity for BSA with a recovery yield of 78.36 percent of total protein.
No presente trabalho foi estudado o efeito da expansão do leito sobre a adsorção de BSA na resina de troca iônica Amberlite IRA 410. O comportamento hidrodinâmico de uma coluna de adsorção em leito expandido sob efeito da adição de biomoléculas, sal e variação da temperatura também foi estudado para obter as condições ótimas de recuperação da BSA sob a resina de troca iônica. A distribuição do tempo de residência mostrou que a HEPT, a dispersão axial e o número de Pecletl aumentaram com a temperatura, altura do leito, porosidade do leito e velocidade linear. A capacidade de ligação da resina aumentou com a expansão do leito. A resina de troca iônica Amberlite IRA 410 mostrou ter afinidade pela BSA, com uma recuperação de 78,36 por cento da proteína total.
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Amyloglucosidase enzyme was produced by Aspergillus niger NRRL 3122 from solid-state fermentation, using deffated rice bran as substrate. The effects of process parameters (pH, temperature) in the equilibrium partition coefficient for the system amyloglucosidase - resin DEAE-cellulose were investigated, aiming at obtaining the optimum conditions for a subsequent purification process. The highest partition coefficients were obtained using 0.025M Tris-HCl buffer, pH 8.0 and 25ºC. The conditions that supplied the highest partition coefficient were specified, the isotherm that better described the amyloglucosidase process of adsorption obtained. It was observed that the adsorption could be well described by Langmuir equation and the values of Qm and Kd estimated at 133.0 U mL-1 and 15.4 U mL-1, respectively. From the adjustment of the kinetic curves using the fourth-order Runge-Kutta algorithm, the adsorption (k1) and desorption (k2) constants were obtained through optimization by the least square procedure, and the values calculated were 2.4x10-3 mL U-1 min-1 for k1 and 0.037 min-1 for k2 .
A enzima amiloglicosidase foi produzida por Aspergillus niger NRRL 3122 através de fermentação em estado sólido, tendo como substrato farelo de arroz desengordurado. Os efeitos dos parâmetros de processo (pH e temperatura) no coeficiente de partição no equilíbrio, para o sistema amiloglicosidase - resina DEAE-celulose foram investigados, com o objetivo de se obter as melhores condições para um posterior processo de purificação. Os maiores coeficientes de partição foram obtidos usando tampão Tris-HCl 0,025M pH 8,0 e 25°C. Determinadas as condições que forneceram o maior coeficiente de partição obteve-se a isoterma que melhor descrevia o processo de adsorção de amiloglicosidase. Foi verificado que adsorção pode ser bem descrita pela equação de Langmuir e os valores de Qm e Kd foram estimados em 133,0 U mL-1 e 15,4 U mL-1 respectivamente. A partir do ajuste das curvas cinéticas utilizando o método de Runge-Kutta de quarta ordem, obteve-se as constantes de adsorção (k1) e dessorção (k2) através da otimização pelo método dos mínimos quadrados, os valores encontrados foram 2,4x10-3 mL U-1 min-1 para k1 e 0,037 min-1 para k2.
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Zwittermicin A was purified by ion exchange resin and HPLC from supernatants of Bacillus thuringiensis.subsp.kurstaki strain D1-23 cultivation.2.89mg pure Zwittermicin A was acquired,proved by HPLC-MS.Results show that the optimized wash concentration of NH_ 4 H_ 2 PO_ 4 is 5mmol/L at first step.Next step CH_ 3 COONH_ 4 concentration is 30 mmol/L,the gradient pH is 8.0～9.5.Totally 93% Zwittermicin A can be reserved with ion exchange resin.The temperature and pH stability experiments show the half life of Zwittermicin A is 48.22 minutes in 100℃,and it is more stable in lower pH in pH 2.0～12.0.