http://sedici.unlp.edu.ar:80/handle/10915/244 2026-06-13T03:21:11Z 2026-06-13T03:21:11Z Zhang, Boli Zhou, Shuiping Ma, Xiaohui Wang, Xiangyang Li, Wei Chu, Yang Zhu, Yonghong http://sedici.unlp.edu.ar:80/handle/10915/8448 2019-07-06T04:02:34Z 2012-01-01T00:00:00Z

Comunicacion Latin American Journal of Pharmacy; vol. 31, no. 1 The objective of this study was to compare the pharmacokinetic characteristics of ascaridole following oral administration of pure ascaridole and Jinghuaweikang (JHWK) capsule. Besides, additional rats were given pure ascaridole via intravenous administration for the bioavailability study. The concentration of ascaridole in rat plasma was determined by a GC/MS method. Following oral administration of pure ascaridole and JHWK capsule, the maximum mean concentration in rat plasma (Cmax, 2701.4 ± 1282.6 ng/mL and 3008.0 ± 273.5 ng/mL) were achieved at 0.25 ± 0.09 h and 0.47 ± 0.22 h (Tmax), and the absolute bioavailabilities were approximately 20.8 and 26.9 %, respectively. The results indicated that other ingredients in JHWK capsule might facilitate and prolong the absorption procedure of ascaridole, and thus enhance its bioavailability in rats. The present study provided the necessary information for the further investigation of Chenopodium ambrosioides L. and its preparation.

2012-01-01T00:00:00Z The objective of this study was to compare the pharmacokinetic characteristics of ascaridole following oral administration of pure ascaridole and Jinghuaweikang (JHWK) capsule. Besides, additional rats were given pure ascaridole via intravenous administration for the bioavailability study. The concentration of ascaridole in rat plasma was determined by a GC/MS method. Following oral administration of pure ascaridole and JHWK capsule, the maximum mean concentration in rat plasma (Cmax, 2701.4 ± 1282.6 ng/mL and 3008.0 ± 273.5 ng/mL) were achieved at 0.25 ± 0.09 h and 0.47 ± 0.22 h (Tmax), and the absolute bioavailabilities were approximately 20.8 and 26.9 %, respectively. The results indicated that other ingredients in JHWK capsule might facilitate and prolong the absorption procedure of ascaridole, and thus enhance its bioavailability in rats. The present study provided the necessary information for the further investigation of Chenopodium ambrosioides L. and its preparation. Zhang, Meiling Wang, Xuebao Wang, Zhiyi Deng, Mingjie Xu, Zhisheng Zheng, Yuancai Zhang, Yuan Huang, Xueli http://sedici.unlp.edu.ar:80/handle/10915/8447 2019-07-05T20:03:57Z 2012-01-01T00:00:00Z

Comunicacion Latin American Journal of Pharmacy; vol. 31, no. 1 A sensitive and selective liquid chromatography-mass spectrometry (LC–MS) method for determination of esomeprazole in rabbit plasma was developed and validated. After addition of midazolam as internal standard (IS), protein precipitation by acetonitrile was used as sample preparation, and chromatography involved Agilent SB-C18 column (2.1 x 150 mm, 5.0 μm) using 0.1 % formic acid in water and acetonitrile as a mobile phase with gradient elution. Detection involved positive ion mode electrospray ionization (ESI), and selective ion monitoring (SIM) mode was used for quantification of target fragment ions m/z 198 for esomeprazole and m/z 326 for midazolam (internal standard, IS). The assay was linear over the range of 10–2000 ng/mL for esomeprazole, with a lower limit of quantitation (LLOQ) of 10 ng/mL for esomeprazole. Intra- and inter-day precisions were less than 14 % and the accuracies were in the range of 89.2-112.6 % for esomeprazole. This developed method was successfully applied for the determination of esomeprazole in rabbit plasma for pharmacokinetic study.

2012-01-01T00:00:00Z A sensitive and selective liquid chromatography-mass spectrometry (LC–MS) method for determination of esomeprazole in rabbit plasma was developed and validated. After addition of midazolam as internal standard (IS), protein precipitation by acetonitrile was used as sample preparation, and chromatography involved Agilent SB-C18 column (2.1 x 150 mm, 5.0 μm) using 0.1 % formic acid in water and acetonitrile as a mobile phase with gradient elution. Detection involved positive ion mode electrospray ionization (ESI), and selective ion monitoring (SIM) mode was used for quantification of target fragment ions m/z 198 for esomeprazole and m/z 326 for midazolam (internal standard, IS). The assay was linear over the range of 10–2000 ng/mL for esomeprazole, with a lower limit of quantitation (LLOQ) of 10 ng/mL for esomeprazole. Intra- and inter-day precisions were less than 14 % and the accuracies were in the range of 89.2-112.6 % for esomeprazole. This developed method was successfully applied for the determination of esomeprazole in rabbit plasma for pharmacokinetic study. Hu, Lufeng Chen, Xiaole Chen, Chan Wang, Jinjin Wang, Zhibin Wang, Zhiyi http://sedici.unlp.edu.ar:80/handle/10915/8446 2019-07-05T20:03:52Z 2012-01-01T00:00:00Z

Comunicacion Latin American Journal of Pharmacy; vol. 31, no. 1 A sensitive and simple liquid chromatography/electrospray mass spectrometry (LC-ESI-MS) method for determination of torsemide in rabbit plasma using one-step protein precipitation was developed and validated. After addition of midazolam as internal standard (IS), protein precipitation by acetonitrile was used in sample preparation. Chromatographically separation was achieved on an SB-C18 (2.1 mm×150 mm, 5 μm) column with acetonitrile-0.1 % formic acid as the mobile phase with gradient elution. Electrospray ionization (ESI) source was applied and operated in positive ion mode; selected ion monitoring (SIM) mode was used to quantification using target fragment ions m/z 349 for torsemide and m/z 326 for the IS. Calibration plots were linear over the range of 5-1000 ng/mL for torsemide in rabbit plasma. Lower limit of quantification (LLOQ) for torsemide was 5 ng/mL. Mean recovery of torsemide from plasma was in the range of 82.7-88.2 %. CV of intra-day and inter-day precision were both less than 15 %. This method is simple and sensitive enough to be used in pharmacokinetic research for determination of torsemide in rabbit plasma.

2012-01-01T00:00:00Z A sensitive and simple liquid chromatography/electrospray mass spectrometry (LC-ESI-MS) method for determination of torsemide in rabbit plasma using one-step protein precipitation was developed and validated. After addition of midazolam as internal standard (IS), protein precipitation by acetonitrile was used in sample preparation. Chromatographically separation was achieved on an SB-C18 (2.1 mm×150 mm, 5 μm) column with acetonitrile-0.1 % formic acid as the mobile phase with gradient elution. Electrospray ionization (ESI) source was applied and operated in positive ion mode; selected ion monitoring (SIM) mode was used to quantification using target fragment ions m/z 349 for torsemide and m/z 326 for the IS. Calibration plots were linear over the range of 5-1000 ng/mL for torsemide in rabbit plasma. Lower limit of quantification (LLOQ) for torsemide was 5 ng/mL. Mean recovery of torsemide from plasma was in the range of 82.7-88.2 %. CV of intra-day and inter-day precision were both less than 15 %. This method is simple and sensitive enough to be used in pharmacokinetic research for determination of torsemide in rabbit plasma. Oliveira, Thompson L. Lianza, Maria C. S. Fernandes, Héllisson B. Oliveira Filho, Abrahão Alves de Fernandes, Heloísa M. B. http://sedici.unlp.edu.ar:80/handle/10915/8445 2019-07-05T20:03:50Z 2012-01-01T00:00:00Z

Comunicacion Latin American Journal of Pharmacy; vol. 31, no. 1 Infections with intestinal parasites represent a worsening public health, given the large number of individuals affected and various organic changes that can be caused. The objective was to conduct a survey of individuals affected by these parasites assisted by the Clinical Laboratory of the HULW from January 2010 to January 2011, as well as characterizing data intrinsic to individuals. Data were obtained through a statistical analysis of 7844 reports of fecal examinations. Among the results was shown that 32.5 % of samples were parasitized, Ascaris lumbricoides being the most frequent in these reports, accounting for 36 %. Female patients were the most affected, comprising 62 % of positive cases. It was detected the existence of multiple parasitism in 30.7 %. Therefore, the high frequency of intestinal parasites detected is a reality that needs to be minimized in the population assisted by the HULW’s Clinical Laboratory.

2012-01-01T00:00:00Z Infections with intestinal parasites represent a worsening public health, given the large number of individuals affected and various organic changes that can be caused. The objective was to conduct a survey of individuals affected by these parasites assisted by the Clinical Laboratory of the HULW from January 2010 to January 2011, as well as characterizing data intrinsic to individuals. Data were obtained through a statistical analysis of 7844 reports of fecal examinations. Among the results was shown that 32.5 % of samples were parasitized, Ascaris lumbricoides being the most frequent in these reports, accounting for 36 %. Female patients were the most affected, comprising 62 % of positive cases. It was detected the existence of multiple parasitism in 30.7 %. Therefore, the high frequency of intestinal parasites detected is a reality that needs to be minimized in the population assisted by the HULW’s Clinical Laboratory. Vargas Villarreal, Javier Cortes Gutiérrez, Elva I. Garza González, Jesús N. Rivera Silva, Gerardo Mata Cárdenas, Benito D. González Salazar, Francisco http://sedici.unlp.edu.ar:80/handle/10915/8444 2019-07-05T20:03:49Z 2012-01-01T00:00:00Z

Comunicacion Latin American Journal of Pharmacy; vol. 31, no. 1 Trichomoniasis is the most common, curable sexually transmitted disease in the world. The first line treatment of trichomoniasis is metronidazole. Recently, the resistance of T. vaginalis to metronidazole and imidazoles has been shown to increase. Ivermectin is a synthetic machrolid drug with activity versus endo and ectoparasitic organisms. In this assay, was tested the effects of ivermectin on T. vaginalis trophozoites. Ivermectin have anti-parasitic activity upon trichomonas trophozoites. However, the IC50 of ivermectin against T. vaginalis was high compared with metronidazole.

2012-01-01T00:00:00Z Trichomoniasis is the most common, curable sexually transmitted disease in the world. The first line treatment of trichomoniasis is metronidazole. Recently, the resistance of T. vaginalis to metronidazole and imidazoles has been shown to increase. Ivermectin is a synthetic machrolid drug with activity versus endo and ectoparasitic organisms. In this assay, was tested the effects of ivermectin on T. vaginalis trophozoites. Ivermectin have anti-parasitic activity upon trichomonas trophozoites. However, the IC50 of ivermectin against T. vaginalis was high compared with metronidazole. Rocha, Leandro Silva Filho, Moacélio V. Santos, Marcelo G. Botas, Gisele da S. Cruz, Rodrigo A.S. Fernandes, Caio P. Tietbohl, Luis A. C. Lima, Barbara G. http://sedici.unlp.edu.ar:80/handle/10915/8443 2019-07-05T20:03:45Z 2012-01-01T00:00:00Z

Comunicacion Latin American Journal of Pharmacy; vol. 31, no. 1 The chemical composition of the essential oils from leaves and stems of Eugenia sulcata Spring ex Mart., obtained by hydrodistillation, was analyzed by GC-MS and quantified by CG-FID. In all, 37 components were identified and sesquiterpenes represented the largest fraction of both oils, in the leaves (58.2 %) and stems (85.3 %). The major constituent found in the essential oil from leaves and stems of E. sulcata was β-caryophyllene, corresponding to 24.6 % and 18.8 %, respectively. The substances α- cubebene (1.1 %), β-copaene (0.5 %), cis-muurola-3,5-diene (0.6 %), cis-muurola-4(14),5-diene (1.3 %), γ- himachalene (2.0 %), epizonarene (0.8 %), trans-calamenene (4.4 %) and trans-cadina-1,4-diene (3.4 %) were identified for the first time as chemical constituents of essential oil from leaves of E. sulcata. To our knowledge, this was the first phytochemical contribution to the essential oil from stems of E. sulcata. It was also performed the acetylcholinesterase inhibitory bioassay of the essential oil from leaves of E. sulcata, which was considered active and exhibited an IC50 value of 4.66 ± 0.48 μg.mL^-1.

2012-01-01T00:00:00Z The chemical composition of the essential oils from leaves and stems of Eugenia sulcata Spring ex Mart., obtained by hydrodistillation, was analyzed by GC-MS and quantified by CG-FID. In all, 37 components were identified and sesquiterpenes represented the largest fraction of both oils, in the leaves (58.2 %) and stems (85.3 %). The major constituent found in the essential oil from leaves and stems of E. sulcata was β-caryophyllene, corresponding to 24.6 % and 18.8 %, respectively. The substances α- cubebene (1.1 %), β-copaene (0.5 %), cis-muurola-3,5-diene (0.6 %), cis-muurola-4(14),5-diene (1.3 %), γ- himachalene (2.0 %), epizonarene (0.8 %), trans-calamenene (4.4 %) and trans-cadina-1,4-diene (3.4 %) were identified for the first time as chemical constituents of essential oil from leaves of E. sulcata. To our knowledge, this was the first phytochemical contribution to the essential oil from stems of E. sulcata. It was also performed the acetylcholinesterase inhibitory bioassay of the essential oil from leaves of E. sulcata, which was considered active and exhibited an IC50 value of 4.66 ± 0.48 μg.mL^-1. Xing, Biao Zhang, Guofeng Li, Meng Hu, Weixing Gu, Peiyuan Wei, Dong Xu, Jing Ma, Banyou Gu, Bing Chen, Gong Li, Junyang http://sedici.unlp.edu.ar:80/handle/10915/8442 2019-07-05T20:03:42Z 2012-01-01T00:00:00Z

Comunicacion Latin American Journal of Pharmacy; vol. 31, no. 1 Glioblastoma is one of the most malignant brain tumors. Current treatments for glioblastoma usually make poor responses, and novel treatment strategies are extremely imperative. Cytochalasin E was reported to inhibit angiogenesis and tumor growth in some studies, but its effects on gliomas are still unknown. In this study, we found cytochalasin E inhibits U87 human glioblastoma cell growth in a very low concentration range of 10^-8 to 10^-6 M in a time and concentration dependent manner, and the IC50 were 1.17 ± 0.32 × 10^-7 M for 48 h treatment, 6.65 ± 1.12 × 10^-8 M for 72 h and 3.78 ± 1.30 × 10^-8 M for 96 h. We also found cytochalasin E induces cell-cycle G2/M phase arrest (72 h-treatment of 10^-6 M cytochalasin E caused 56.2 ± 6.1 % cells arrest in G2/M phase) and cell apoptosis (96 h-treatment of 10^-6 M cytochalasin E induced 24.1 ± 4.2 % cells apoptosis). Thus, cytochalasin E is proposed as a potential agent for glioblastoma chemotherapy.

2012-01-01T00:00:00Z Glioblastoma is one of the most malignant brain tumors. Current treatments for glioblastoma usually make poor responses, and novel treatment strategies are extremely imperative. Cytochalasin E was reported to inhibit angiogenesis and tumor growth in some studies, but its effects on gliomas are still unknown. In this study, we found cytochalasin E inhibits U87 human glioblastoma cell growth in a very low concentration range of 10^-8 to 10^-6 M in a time and concentration dependent manner, and the IC50 were 1.17 ± 0.32 × 10^-7 M for 48 h treatment, 6.65 ± 1.12 × 10^-8 M for 72 h and 3.78 ± 1.30 × 10^-8 M for 96 h. We also found cytochalasin E induces cell-cycle G2/M phase arrest (72 h-treatment of 10^-6 M cytochalasin E caused 56.2 ± 6.1 % cells arrest in G2/M phase) and cell apoptosis (96 h-treatment of 10^-6 M cytochalasin E induced 24.1 ± 4.2 % cells apoptosis). Thus, cytochalasin E is proposed as a potential agent for glioblastoma chemotherapy. Pandit, Jayant K. Sharma, Suresh D. Nagarwal, Ramesh C. Verma, Anurag http://sedici.unlp.edu.ar:80/handle/10915/8441 2019-07-05T20:03:41Z 2012-01-01T00:00:00Z

Articulo Latin American Journal of Pharmacy; vol. 31, no. 1 The objective of the present investigation was to evaluate the potential of gellan gum- low molecular weight chitosan (GG-LMCH) polyelectrolyte complex (PEC) in the form of beads as prolonged release stomach specific floating drug delivery system. PEC beads were prepared in one step, without using any chemical crosslinker, by dropwise addition of GG to a solution of LMCH in acetic acid. Buoyancy to the beads was attributed to the use of CaCO₃ . The % buoyancy, encapsulation efficiency and drug release from PEC beads were compared with Ca⁺⁺ crosslinked GG floating beads prepared under same conditions using rifabutin as model drug. Our finding showed that the PEC beads remained buoyant for up to 8 h and showed significantly better (p < 0.05) control over drug release compared to Ca⁺⁺ crosslinked GG beads and, therefore, possess great potential for the stomach specific sustained delivery of drugs like rifabutin for the treatment of Helicobacter pylori infection.

2012-01-01T00:00:00Z The objective of the present investigation was to evaluate the potential of gellan gum- low molecular weight chitosan (GG-LMCH) polyelectrolyte complex (PEC) in the form of beads as prolonged release stomach specific floating drug delivery system. PEC beads were prepared in one step, without using any chemical crosslinker, by dropwise addition of GG to a solution of LMCH in acetic acid. Buoyancy to the beads was attributed to the use of CaCO₃ . The % buoyancy, encapsulation efficiency and drug release from PEC beads were compared with Ca⁺⁺ crosslinked GG floating beads prepared under same conditions using rifabutin as model drug. Our finding showed that the PEC beads remained buoyant for up to 8 h and showed significantly better (p < 0.05) control over drug release compared to Ca⁺⁺ crosslinked GG beads and, therefore, possess great potential for the stomach specific sustained delivery of drugs like rifabutin for the treatment of Helicobacter pylori infection. Simões, Cláudia Maria Oliveira Reginatto, Flávio Henrique Calvete, Eunice Blum Silva, Carlos H. Carvalho, Annelise http://sedici.unlp.edu.ar:80/handle/10915/8440 2019-07-05T20:03:37Z 2012-01-01T00:00:00Z

Articulo Latin American Journal of Pharmacy; vol. 31, no. 1 Five strawberry (Fragaria x ananassa) cultivars harvested in Passo Fundo (State of Rio Grande do Sul, Brazil) were quantified for their total flavonoids (TF) and total anthocyanins contents (TA) and the extracts were evaluated for their in vitro antiherpes (anti-HSV-1, KOS strain) activity. The cultivars Camarosa and Aromas presented the highest TF (149.1 and 129.4 mg RE/100g FF), respectively; and TA (92.8 and 84.4 mg CGE/100 g FF), respectively. On the other hand, Camino Real cultivar showed the lowest TF (69.9 mg RE/100 g FF) and TA (46.2 mg CGE/100 g FF). With regard to the antiherpes activity, Camarosa and Aromas cultivars also displayed the highest activity detected (IC50 = 1.68 mg/mL and 1.80 mg/mL, respectively) and Camino Real the lowest (IC50 = 2.69 mg/mL). A relationship between the presence of flavonoids and anthocyanins and the detected anti-HSV-1 activity might be suggested for the strawberry cultivars studied.

2012-01-01T00:00:00Z Five strawberry (Fragaria x ananassa) cultivars harvested in Passo Fundo (State of Rio Grande do Sul, Brazil) were quantified for their total flavonoids (TF) and total anthocyanins contents (TA) and the extracts were evaluated for their in vitro antiherpes (anti-HSV-1, KOS strain) activity. The cultivars Camarosa and Aromas presented the highest TF (149.1 and 129.4 mg RE/100g FF), respectively; and TA (92.8 and 84.4 mg CGE/100 g FF), respectively. On the other hand, Camino Real cultivar showed the lowest TF (69.9 mg RE/100 g FF) and TA (46.2 mg CGE/100 g FF). With regard to the antiherpes activity, Camarosa and Aromas cultivars also displayed the highest activity detected (IC50 = 1.68 mg/mL and 1.80 mg/mL, respectively) and Camino Real the lowest (IC50 = 2.69 mg/mL). A relationship between the presence of flavonoids and anthocyanins and the detected anti-HSV-1 activity might be suggested for the strawberry cultivars studied. Wang, Yuefei Liu, Haitao Qi, Aidi Chai, Xin Olaleye, Olajide Peng, Siwei Zhu, Lin http://sedici.unlp.edu.ar:80/handle/10915/8439 2019-07-05T20:03:35Z 2012-01-01T00:00:00Z

Articulo Latin American Journal of Pharmacy; vol. 31, no. 1 "JiangYaBiFeng" (JYBF) tablet for treatment of hypertension in China is a composite prescription of Chinese and western medicines. By using ultra high performance liquid chromatography coupled with mass spectrometry (UPLC-MS), twenty-five compounds were simultaneously identified or tentatively characterized based on their retention times and MS spectra. Nine target compounds, hydrochlorothiazide (HC), rutin, genistin, sophoricoside, baicalin, wogonoside, genistein, baicalein and wogonin, were further quantified by ultra high performance liquid chromatography with diode-array detector (UPLC-DAD). Chromatographic separation was successfully performed on a C₁₈ column with gradient elution of 0.1 % formic acid aqueous solution and acetonitrile at the flow rate of 0.4 mL/min in 15 min at 52 °C. Different wavelengths were used to determine corresponding compounds to ensure the best resolution. According to the methodological validation, including linearity, precision, accuracy and stability, this method was proved to be rapid, comprehensive, sensitive and feasible in the quality assessment of JYBF tablet.

2012-01-01T00:00:00Z "JiangYaBiFeng" (JYBF) tablet for treatment of hypertension in China is a composite prescription of Chinese and western medicines. By using ultra high performance liquid chromatography coupled with mass spectrometry (UPLC-MS), twenty-five compounds were simultaneously identified or tentatively characterized based on their retention times and MS spectra. Nine target compounds, hydrochlorothiazide (HC), rutin, genistin, sophoricoside, baicalin, wogonoside, genistein, baicalein and wogonin, were further quantified by ultra high performance liquid chromatography with diode-array detector (UPLC-DAD). Chromatographic separation was successfully performed on a C₁₈ column with gradient elution of 0.1 % formic acid aqueous solution and acetonitrile at the flow rate of 0.4 mL/min in 15 min at 52 °C. Different wavelengths were used to determine corresponding compounds to ensure the best resolution. According to the methodological validation, including linearity, precision, accuracy and stability, this method was proved to be rapid, comprehensive, sensitive and feasible in the quality assessment of JYBF tablet. Silva, Camilla V.N.S. Santos, Noemia P. S. Santos Magalhães, Nereide S. Lira, Mariane C. B. Honda, Neli Kika Ferraz, Milena S. http://sedici.unlp.edu.ar:80/handle/10915/8438 2019-07-05T20:03:33Z 2012-01-01T00:00:00Z

Articulo Latin American Journal of Pharmacy; vol. 31, no. 1 Diffractaic acid (DA) presents several biological activities. The goal of this study was to develop and validate a UV spectrophotometric method for determining diffractaic acid in inclusion complexes with hydroxypropyl-β-cyclodextrin. Validation parameters were determined according to international guidelines for standardization. The linearity range of analytical curve was from 1 to 5 μg/mL and the regression equation: CDA = (Area - 0.0053)/0.1541 (r2 = 0.99998; n = 3). The intermediate precision indicated that the difference between the means was statistically insignificant (p < 0.05). Accuracy revealed a mean recovery percentage of diffractaic acid in inclusion complexes of 100.1 %. The method was robust and the formulation excipients did not interfere on diffractaic acid quantification. Limits of detection and quantification of diffractaic acid were 0.03 and 0.08 μg/mL, respectively. The proposed method proved to be accurate, precise and reproducible, thus being able to quantify diffractaic acid in raw material and inclusion complexes.

2012-01-01T00:00:00Z Diffractaic acid (DA) presents several biological activities. The goal of this study was to develop and validate a UV spectrophotometric method for determining diffractaic acid in inclusion complexes with hydroxypropyl-β-cyclodextrin. Validation parameters were determined according to international guidelines for standardization. The linearity range of analytical curve was from 1 to 5 μg/mL and the regression equation: CDA = (Area - 0.0053)/0.1541 (r2 = 0.99998; n = 3). The intermediate precision indicated that the difference between the means was statistically insignificant (p < 0.05). Accuracy revealed a mean recovery percentage of diffractaic acid in inclusion complexes of 100.1 %. The method was robust and the formulation excipients did not interfere on diffractaic acid quantification. Limits of detection and quantification of diffractaic acid were 0.03 and 0.08 μg/mL, respectively. The proposed method proved to be accurate, precise and reproducible, thus being able to quantify diffractaic acid in raw material and inclusion complexes. Bi, Kaishun Yan, Baoqing Huo, Yanshuang Chen, Xaohui Sun, Linxin Zhang, Huifen http://sedici.unlp.edu.ar:80/handle/10915/8437 2019-07-05T20:03:30Z 2012-01-01T00:00:00Z

Articulo Latin American Journal of Pharmacy; vol. 31, no. 1 A LC-MS method was developed and validated for simultaneous determination of 6, 7-di-hydroxyligustilide and gastrodin in rat plasma, and which was subsequently applied in the pharmacokinetic analysis of an administration of a Chinese herbal extract containing Chuanxiong Rhizoma and Gastrodia Elata Rhizome, i.e. TianShu capsule against migraine. The analytes were separated on a Kromasil C18 column with a gradient elution program and detected without interference in the selected ion monitoring mode with positive electrospray ionization. The linear range was 0.010-10.0 μg/mL for 6,7-di-hydroxyligustilide and 0.025-25.0 μg/mL for gastrodin with the limit of quantitation of 0.01 and 0.025 μg/mL, respectively. The intra-day and inter-day precisions for the entire validation were less than14.7 % of RSD. The pharmacokinetic parameters indicated that 6, 7-di-hydroxyligustilide and gastrodin are absorbed rapidly and reached a maximum concentration within one hour, which was consistent with the clinical requirements for the rapid relieving the symptoms of migraine.

2012-01-01T00:00:00Z A LC-MS method was developed and validated for simultaneous determination of 6, 7-di-hydroxyligustilide and gastrodin in rat plasma, and which was subsequently applied in the pharmacokinetic analysis of an administration of a Chinese herbal extract containing Chuanxiong Rhizoma and Gastrodia Elata Rhizome, i.e. TianShu capsule against migraine. The analytes were separated on a Kromasil C18 column with a gradient elution program and detected without interference in the selected ion monitoring mode with positive electrospray ionization. The linear range was 0.010-10.0 μg/mL for 6,7-di-hydroxyligustilide and 0.025-25.0 μg/mL for gastrodin with the limit of quantitation of 0.01 and 0.025 μg/mL, respectively. The intra-day and inter-day precisions for the entire validation were less than14.7 % of RSD. The pharmacokinetic parameters indicated that 6, 7-di-hydroxyligustilide and gastrodin are absorbed rapidly and reached a maximum concentration within one hour, which was consistent with the clinical requirements for the rapid relieving the symptoms of migraine. Conceição, Edmilson C. da Paula, José R. de Bara, María Teresa. F. Freitas, Osvaldo de Martins, Frederico S. Oliveira, Ezequiane M. S. Couto, Renê O. http://sedici.unlp.edu.ar:80/handle/10915/8436 2019-07-05T20:03:25Z 2012-01-01T00:00:00Z

Articulo Latin American Journal of Pharmacy; vol. 31, no. 1 The effects of drying air inlet temperature (IT) and concentration of Aerosil® 200 (C<SUB>A</SUB>) on several properties of spray-dried Apeiba tibourbou extracts were investigated following a 3<SUP>2</SUP> full factorial design. Powder recovery varied from 9.83 to 46.95% and dried products showed moisture contents below 7%. Although the spray-dried products lost some of their polyphenols, they still present excellent antioxidant activity, opening perspectives for its use to medicinal purpose. C<SUB>A</SUB> exerted a key role on the properties of spray-dried extracts, while IT did not present a significative influence. Aerosil® 200 proved to be an interesting alternative as an excipient for the drying of the herbal extract, even at intermediate concentrations such as 15%. The best combination of conditions to use for obtaining dry A. tibourbou extracts with adequate physicochemical and functional properties involves an IT of 100 ºC and a C<SUB>A</SUB> of 15%.

2012-01-01T00:00:00Z The effects of drying air inlet temperature (IT) and concentration of Aerosil® 200 (C<SUB>A</SUB>) on several properties of spray-dried Apeiba tibourbou extracts were investigated following a 3<SUP>2</SUP> full factorial design. Powder recovery varied from 9.83 to 46.95% and dried products showed moisture contents below 7%. Although the spray-dried products lost some of their polyphenols, they still present excellent antioxidant activity, opening perspectives for its use to medicinal purpose. C<SUB>A</SUB> exerted a key role on the properties of spray-dried extracts, while IT did not present a significative influence. Aerosil® 200 proved to be an interesting alternative as an excipient for the drying of the herbal extract, even at intermediate concentrations such as 15%. The best combination of conditions to use for obtaining dry A. tibourbou extracts with adequate physicochemical and functional properties involves an IT of 100 ºC and a C<SUB>A</SUB> of 15%. Santos Magalhães, Nereide S. Maciel, Maria A. M. Lira, Mariane C. B. Morais, Waldenice A. Lapenda, Taciana L.S. http://sedici.unlp.edu.ar:80/handle/10915/8435 2019-07-05T20:03:23Z 2012-01-01T00:00:00Z

Articulo Latin American Journal of Pharmacy; vol. 31, no. 1 Trans-dehydrocrotonin (t-DCTN) is a 19-nor-clerodan diterpen with several important pharmacological properties, including hypoglycemic and antitumor activity. However the low water solubility and hepatotoxicity of t-DCTN limit its use in therapeutic applications. Drug inclusion complexes with cyclodextrins (CDs) can modify physicochemical properties of parent drugs, such as improving their aqueous solubility and reducing their toxicity. A UV method was therefore validated for determining t-DCTN in HP-β-CD inclusion complexes with a view to future applications in research and therapy. The regression equation of the analytical curve (1–20 μg/mL) was [t-DCTN] = absorbance + 0.00147/0.04214. The precision of the method was satisfactory, producing values of relative standard deviation less than 2 % for all samples analyzed. The accuracy was between 99.6 and 100.02 %. The content of t-DCTN in tDCTN:HP-β-CD was 99.8 %. The UV validated method developed is straightforward and suitable for use in the routine analysis of t-DCTN complexed with hydroxypropyl-β-cyclodextrin.

2012-01-01T00:00:00Z Trans-dehydrocrotonin (t-DCTN) is a 19-nor-clerodan diterpen with several important pharmacological properties, including hypoglycemic and antitumor activity. However the low water solubility and hepatotoxicity of t-DCTN limit its use in therapeutic applications. Drug inclusion complexes with cyclodextrins (CDs) can modify physicochemical properties of parent drugs, such as improving their aqueous solubility and reducing their toxicity. A UV method was therefore validated for determining t-DCTN in HP-β-CD inclusion complexes with a view to future applications in research and therapy. The regression equation of the analytical curve (1–20 μg/mL) was [t-DCTN] = absorbance + 0.00147/0.04214. The precision of the method was satisfactory, producing values of relative standard deviation less than 2 % for all samples analyzed. The accuracy was between 99.6 and 100.02 %. The content of t-DCTN in tDCTN:HP-β-CD was 99.8 %. The UV validated method developed is straightforward and suitable for use in the routine analysis of t-DCTN complexed with hydroxypropyl-β-cyclodextrin. Wagner, Vilegas Severi, Juliana A. Wessjohann, Ludger A. Schneider, Alex http://sedici.unlp.edu.ar:80/handle/10915/8434 2019-07-05T20:03:22Z 2012-01-01T00:00:00Z

Articulo Latin American Journal of Pharmacy; vol. 31, no. 1 Comparative HPLC-UV and LC-MS/MS studies of impurity profiles of a reference sample (Xenical®, F. Hoffmann-La Roche Ltd., Switzerland) vs. generic (Lipiblock®, EMS-Sigma Pharma, a generic drug) were carried out with ethanol extracts of commercial samples. The generic formulation contained higher levels of common impurities as well as a considerable number of impurities not found in the reference product. The detected impurity profile of Lipiblock® revealed that it most likely is based on fermentation. Since the effect of the impurities is unknown, at this point fully synthetic Xenical® appears to offer a better safety margin than Lipiblock® which, however, compares quite well to other generic formulations.

2012-01-01T00:00:00Z Comparative HPLC-UV and LC-MS/MS studies of impurity profiles of a reference sample (Xenical®, F. Hoffmann-La Roche Ltd., Switzerland) vs. generic (Lipiblock®, EMS-Sigma Pharma, a generic drug) were carried out with ethanol extracts of commercial samples. The generic formulation contained higher levels of common impurities as well as a considerable number of impurities not found in the reference product. The detected impurity profile of Lipiblock® revealed that it most likely is based on fermentation. Since the effect of the impurities is unknown, at this point fully synthetic Xenical® appears to offer a better safety margin than Lipiblock® which, however, compares quite well to other generic formulations. Younus Pasha, Mohammed Bhat, Sudeendra R. Hani, Umme http://sedici.unlp.edu.ar:80/handle/10915/8433 2019-07-05T20:03:19Z 2012-01-01T00:00:00Z

Articulo Latin American Journal of Pharmacy; vol. 31, no. 1 The purpose of this work was to design and evaluate a novel vaginal delivery system for the local treatment of vaginal candidiasis. Bioadhesive vaginal films of metronidazole that could be retained in the vagina for prolonged period for more effective treatment against vaginal candidiasis were formulated by solvent casting technique using bioadhesive polymers such as chitosan, HPC and sodium CMC. Glycerine and propylene glycol were used as plasticizer. The films were characterized for various physical, mechanical, and aesthetic properties. Bioadhesive strength and in vitro release studies suggested that the prolonged release bioadhesive vaginal film formulation of metronidazole is useful and effective dosage form for treating vaginal candidiasis. It may be concluded from present study that MTZ bioadhesive vaginal film can be used as a novel delivery system for local therapy of vaginal candidiasis.

2012-01-01T00:00:00Z The purpose of this work was to design and evaluate a novel vaginal delivery system for the local treatment of vaginal candidiasis. Bioadhesive vaginal films of metronidazole that could be retained in the vagina for prolonged period for more effective treatment against vaginal candidiasis were formulated by solvent casting technique using bioadhesive polymers such as chitosan, HPC and sodium CMC. Glycerine and propylene glycol were used as plasticizer. The films were characterized for various physical, mechanical, and aesthetic properties. Bioadhesive strength and in vitro release studies suggested that the prolonged release bioadhesive vaginal film formulation of metronidazole is useful and effective dosage form for treating vaginal candidiasis. It may be concluded from present study that MTZ bioadhesive vaginal film can be used as a novel delivery system for local therapy of vaginal candidiasis. Hussain, Izhar Azhar, Saira Murtaza, Ghulam Ullah, Majeed http://sedici.unlp.edu.ar:80/handle/10915/8432 2019-07-05T20:03:17Z 2012-01-01T00:00:00Z

Articulo Latin American Journal of Pharmacy; p. 78-83 The present study was undertaken to investigate the effect of nature of polymers like HPMC, carbopol-934P and their content levels on the release profiles of water soluble drug, diclofenac potassium. For this purpose, different tablets were prepared by wet granulation technique using HPMC-K15, carbopol-934P and blends of HPMC with carbopol-934P. Release kinetics was evaluated using USP apparatus II at 50 rpm in phosphate buffer pH 6.8 for 12 h. HPMC showed less release retardant effect compared to carbopol-934P at same concentration, while blends of these polymers gave an intermediate release profile, i.e. decreasing the quantity of carbopol-934P while increasing the amount of HPMC, increased the release of drug from matrix tablets. The release retarding capacity of two used polymers is as follows: Carbopol- 934P > HPMC-K15. Formulations containing HPMC exhibited first order release, while all other formulations showed zero order pattern. Present study showed that drug release retardant effect of carbopol was higher as compared to HPMC. It also confirmed that release rate of drug is mainly controlled by drugpolymer ratios.

2012-01-01T00:00:00Z The present study was undertaken to investigate the effect of nature of polymers like HPMC, carbopol-934P and their content levels on the release profiles of water soluble drug, diclofenac potassium. For this purpose, different tablets were prepared by wet granulation technique using HPMC-K15, carbopol-934P and blends of HPMC with carbopol-934P. Release kinetics was evaluated using USP apparatus II at 50 rpm in phosphate buffer pH 6.8 for 12 h. HPMC showed less release retardant effect compared to carbopol-934P at same concentration, while blends of these polymers gave an intermediate release profile, i.e. decreasing the quantity of carbopol-934P while increasing the amount of HPMC, increased the release of drug from matrix tablets. The release retarding capacity of two used polymers is as follows: Carbopol- 934P > HPMC-K15. Formulations containing HPMC exhibited first order release, while all other formulations showed zero order pattern. Present study showed that drug release retardant effect of carbopol was higher as compared to HPMC. It also confirmed that release rate of drug is mainly controlled by drugpolymer ratios. Tan, Yvonne T.F. Abdulameer, Shaymaa A. Peh, Kok K. Darwis, Yusrida Sahib, Mohanad N. http://sedici.unlp.edu.ar:80/handle/10915/8431 2019-07-05T20:03:15Z 2012-01-01T00:00:00Z

Articulo Latin American Journal of Pharmacy; vol. 31, no. 1 The aim of this study was to investigate the potential of a polyethylene glycol-phosphatidylethanolamine conjugate (PEG₂₀₀₀ -DSPE) to solubilize budesonide (BUD) for pulmonary delivery. The BUD-strictly stabilized phospholipid nanomicelles (SSMs) were prepared using the coprecipitation and reconstitution method and the physicochemical characteristics and pharmacodynamic duration of the BUD-SSMs were determined. The solubility of BUD was highly improved by at least 52 times its intrinsic solubility. The hydrodynamic particle size and zeta potential were 14.31 ± 1.40 nm and -46.61 ± 2.94 mV, respectively. The in vitro release of BUD from SSMs was completed within 6 days. Aerosolization of rehydrated BUD-SSMs with different nebulizers showed superior and significant aerodynamic characterizations compared to Pulmicort Respules® (PR). An in vivo study showed a significant reduction in the inflammatory cell counts of bronchoalveolar lavage fluid compared to PR. As a result, this study suggested that PEG₂₀₀₀ -DSPE is a promising candidate as a budesonide carrier for pulmonary delivery.

2012-01-01T00:00:00Z The aim of this study was to investigate the potential of a polyethylene glycol-phosphatidylethanolamine conjugate (PEG₂₀₀₀ -DSPE) to solubilize budesonide (BUD) for pulmonary delivery. The BUD-strictly stabilized phospholipid nanomicelles (SSMs) were prepared using the coprecipitation and reconstitution method and the physicochemical characteristics and pharmacodynamic duration of the BUD-SSMs were determined. The solubility of BUD was highly improved by at least 52 times its intrinsic solubility. The hydrodynamic particle size and zeta potential were 14.31 ± 1.40 nm and -46.61 ± 2.94 mV, respectively. The in vitro release of BUD from SSMs was completed within 6 days. Aerosolization of rehydrated BUD-SSMs with different nebulizers showed superior and significant aerodynamic characterizations compared to Pulmicort Respules® (PR). An in vivo study showed a significant reduction in the inflammatory cell counts of bronchoalveolar lavage fluid compared to PR. As a result, this study suggested that PEG₂₀₀₀ -DSPE is a promising candidate as a budesonide carrier for pulmonary delivery. Consolini, Alicia Elvira Spegazzini, Etile Dolores Debenedetti, Silvia Laura Rosella, María Adelaida Colareda, Germán Andrés Ramos, Pablo http://sedici.unlp.edu.ar:80/handle/10915/8430 2026-06-12T16:00:59Z 2012-01-01T00:00:00Z

Articulo Latin American Journal of Pharmacy; vol. 31, no. 1 The pseudobulbs of Catasetum macroglossum (Orchidaceae) are popularly used as topical anti-inflammatory and antirheumatic in the forests and medium lands of Ecuador, but they were never studied. We evaluated whether the decoction of C. macroglossum has antiinflammatory effect and which is its phytochemical profile. The effect of 30 and 90 mg lyophilized/kg via i.p. was studied on the carrageenaninduced edema in the paw rat, in comparison with saline and indomethacin. The paw edema was inhibited in about 60 to 80 % after 1 to 3 h of carrageenan injection. The phytochemical profile was done by chemical tests to evaluate the presence of reducing sugars and flavonoids, and TLC of the aqueous extract and the hydrolyzed one. There were detected reductive substances after the acidic hydrolysis, and two spots with the features and Rf of the standard glucose and mannose. Some peaks in the HPLC-DAD chromatogram showed absorption at 225 and 280 nm in agreement with dihydro derivatives of phenantrene and stilbene in traces amount. The antiinflammatory kinetic of C. macroglossum suggests inhibition on prostaglandins. This work validates the popular use of C. macroglossum, which could be due to the presence of a glucomannan and traces of phenantrene and stilbene, as in other species of Catasetum.

2012-01-01T00:00:00Z The pseudobulbs of Catasetum macroglossum (Orchidaceae) are popularly used as topical anti-inflammatory and antirheumatic in the forests and medium lands of Ecuador, but they were never studied. We evaluated whether the decoction of C. macroglossum has antiinflammatory effect and which is its phytochemical profile. The effect of 30 and 90 mg lyophilized/kg via i.p. was studied on the carrageenaninduced edema in the paw rat, in comparison with saline and indomethacin. The paw edema was inhibited in about 60 to 80 % after 1 to 3 h of carrageenan injection. The phytochemical profile was done by chemical tests to evaluate the presence of reducing sugars and flavonoids, and TLC of the aqueous extract and the hydrolyzed one. There were detected reductive substances after the acidic hydrolysis, and two spots with the features and Rf of the standard glucose and mannose. Some peaks in the HPLC-DAD chromatogram showed absorption at 225 and 280 nm in agreement with dihydro derivatives of phenantrene and stilbene in traces amount. The antiinflammatory kinetic of C. macroglossum suggests inhibition on prostaglandins. This work validates the popular use of C. macroglossum, which could be due to the presence of a glucomannan and traces of phenantrene and stilbene, as in other species of Catasetum. Ramos Ligonio, Ángel López Monteon, Aracely Carrera Huerta, Francisco García Gálvez, Ana M. Márquez López , Elizabeth Sánchez Pavón, Esmeralda http://sedici.unlp.edu.ar:80/handle/10915/8429 2019-07-05T04:04:38Z 2012-01-01T00:00:00Z

Articulo Latin American Journal of Pharmacy; vol. 31, no. 1 Chagas' disease, caused by the protozoan parasite Trypanosoma cruzi, affects 9-12 million of people in Latin America and it is an important cause of heart disease. Although transmission has been reduced, an effective therapy for the infected population is lacking. New isomers nitroimidazole derivatives [4(5)-bromo-1-phenacyl-5(4)-nitroimidazoles] were developed and their antichagasic properties were studied. Five compounds (with different substituents in their aromatic ring) displayed remarkable in vitro activities against T. cruzi. The results demonstrated that 4(5)-bromo-1-(4-methoxiphenacyl)-2-methyl-5(4)- nitroimidazole, 4(5)-bromo-1-(4-chlorophenacyl)-2-methyl-5(4)-nitroimidazole, and 4(5)-bromo-1-(4- cianophenacyl)-2-methyl-5(4)-nitroimidazole have IC50 values of of 3.95, 2.3, and 1.15 μg/mL, respectively, and show acceptable values of cytotoxicity, at concentrations below 5 μg/mL. Our results indicate that mixtures of isomers are a potent inhibitor of T. cruzi growth. The present evidence shows very promising results of new isomers, which emerge as strong candidates for further tests as anti-T. cruzi agents.

2012-01-01T00:00:00Z Chagas' disease, caused by the protozoan parasite Trypanosoma cruzi, affects 9-12 million of people in Latin America and it is an important cause of heart disease. Although transmission has been reduced, an effective therapy for the infected population is lacking. New isomers nitroimidazole derivatives [4(5)-bromo-1-phenacyl-5(4)-nitroimidazoles] were developed and their antichagasic properties were studied. Five compounds (with different substituents in their aromatic ring) displayed remarkable in vitro activities against T. cruzi. The results demonstrated that 4(5)-bromo-1-(4-methoxiphenacyl)-2-methyl-5(4)- nitroimidazole, 4(5)-bromo-1-(4-chlorophenacyl)-2-methyl-5(4)-nitroimidazole, and 4(5)-bromo-1-(4- cianophenacyl)-2-methyl-5(4)-nitroimidazole have IC50 values of of 3.95, 2.3, and 1.15 μg/mL, respectively, and show acceptable values of cytotoxicity, at concentrations below 5 μg/mL. Our results indicate that mixtures of isomers are a potent inhibitor of T. cruzi growth. The present evidence shows very promising results of new isomers, which emerge as strong candidates for further tests as anti-T. cruzi agents.