http://sedici.unlp.edu.ar:80/handle/10915/20167 2026-05-17T09:03:20Z 2026-05-17T09:03:20Z Tietbohl, Luis A. C. Lima, Barbara G. Fernandes, Caio P. Santos, Marcelo G. Silva, Fabiana E. B. da Denardin, Elton L. G. Bachinski, Róber Alves, Gutemberg G. Silva Filho, Moacélio V. Rocha, Leandro http://sedici.unlp.edu.ar:80/handle/10915/20211 2019-07-06T20:03:01Z 2012-01-01T00:00:00Z

Comunicacion Latin American Journal of Pharmacy; vol. 31, no. 4 Myrciaria floribunda (H.West ex Willd.) O.Berg, Myrtaceae, popularly known as “camboim amarelo”, was collected in Restinga de Jurubatiba (RJ, Brazil). Leaves, stems and flowers were individually submitted to hydrodistillation, affording the respective essential oils. Monoterpenes were the main group of essential oils from leaves (53.9 %) and flowers (55.4 %). Sesquiterpenes were more representative in stems (72.2 %). 1,8-cineole was the major constituent in the essential oil from leaves (38.4 %) and flowers (22.8 %). The major constituent from stems was (2E,6E)-farnesyl acetate (19.9 %). To our knowledge, these are the first contributions for essential oils from stems and flowers of M. floribunda. It was also performed the acetylcholinesterase inhibitory bioassay of the essential oil from stems, flowers and leaves of M. floribunda. Flowers and leaves oils had an IC50 of 1583 and 681 μg/mL, respectively, being both low to mild values.

2012-01-01T00:00:00Z Myrciaria floribunda (H.West ex Willd.) O.Berg, Myrtaceae, popularly known as “camboim amarelo”, was collected in Restinga de Jurubatiba (RJ, Brazil). Leaves, stems and flowers were individually submitted to hydrodistillation, affording the respective essential oils. Monoterpenes were the main group of essential oils from leaves (53.9 %) and flowers (55.4 %). Sesquiterpenes were more representative in stems (72.2 %). 1,8-cineole was the major constituent in the essential oil from leaves (38.4 %) and flowers (22.8 %). The major constituent from stems was (2E,6E)-farnesyl acetate (19.9 %). To our knowledge, these are the first contributions for essential oils from stems and flowers of M. floribunda. It was also performed the acetylcholinesterase inhibitory bioassay of the essential oil from stems, flowers and leaves of M. floribunda. Flowers and leaves oils had an IC50 of 1583 and 681 μg/mL, respectively, being both low to mild values. Eghrary, Shadi H. Zarghami, Reza Jouyban, Abolghasem http://sedici.unlp.edu.ar:80/handle/10915/20210 2019-07-06T20:02:48Z 2012-01-01T00:00:00Z

Comunicacion Latin American Journal of Pharmacy; vol. 31, no. 4 The solubilities of losartan potassium in eight solvents; 1,4-dioxane, acetonitrile, propylene glycol, N-methyl-2-pyrrolidone, 1-butanol, 1-hexanol, 1-heptanol, and 1-octanol, were measured at temperatures ranging from 293.2 to 318.2 K at atmospheric pressure using shake-flask method of Higuchi and Connors. N-methyl-2-pyrrolidone dissolved the highest amount of losartan potassium and 1,4-dioxane possessed the lowest solubilization power among the investigated solvents. The generated data was used to calculate the thermodynamic parameters of the system using the modified van’t Hoff equation and the Gibbs free energy data was correlated using Abraham solvation parameters.

2012-01-01T00:00:00Z The solubilities of losartan potassium in eight solvents; 1,4-dioxane, acetonitrile, propylene glycol, N-methyl-2-pyrrolidone, 1-butanol, 1-hexanol, 1-heptanol, and 1-octanol, were measured at temperatures ranging from 293.2 to 318.2 K at atmospheric pressure using shake-flask method of Higuchi and Connors. N-methyl-2-pyrrolidone dissolved the highest amount of losartan potassium and 1,4-dioxane possessed the lowest solubilization power among the investigated solvents. The generated data was used to calculate the thermodynamic parameters of the system using the modified van’t Hoff equation and the Gibbs free energy data was correlated using Abraham solvation parameters. Xing, Jin Che, Wen http://sedici.unlp.edu.ar:80/handle/10915/20209 2019-07-06T20:02:54Z 2012-01-01T00:00:00Z

Comunicacion Latin American Journal of Pharmacy; vol. 31, no. 4 Drug-drug interaction (DDI) is a challenging problem for treatment of HIV-infected patients. Zidovudine (AZT), prescribed under the names Retrovir and Retrovis, is the first U.S. government-approved antiretroviral drug used for the successful treatment of HIV/AIDS infectiousness. Given that ginseng is frequently utilized in combination with AZT and AZT is mainly eliminated by UDP-glucuronosyltransferase 2B7, the aim of present study is to investigate the inhibition of UGT2B7-catalyzed AZT glucuronidation by 20(S)-protopanaxatriol type (Ppt) which is the main ginsenoside absorbed into the plasma. The results showed that ppt competitively inhibited UGT2B7-catalyzed AZT glucuronidation, and the inhibition kinetic parameter (Ki ) was determined to be 24.7 μM. Using the maximum plasma concentration of ppt (Cmax ), the alteration of area under the curve (AUC) of AZT was 6 %. All these results provide important information for understanding ginseng-AZT interaction. However, considering the complication of herbs and individuals, the in vitro-in vivo extrapolation (IV-IVE) results should be explained with more caution.

2012-01-01T00:00:00Z Drug-drug interaction (DDI) is a challenging problem for treatment of HIV-infected patients. Zidovudine (AZT), prescribed under the names Retrovir and Retrovis, is the first U.S. government-approved antiretroviral drug used for the successful treatment of HIV/AIDS infectiousness. Given that ginseng is frequently utilized in combination with AZT and AZT is mainly eliminated by UDP-glucuronosyltransferase 2B7, the aim of present study is to investigate the inhibition of UGT2B7-catalyzed AZT glucuronidation by 20(S)-protopanaxatriol type (Ppt) which is the main ginsenoside absorbed into the plasma. The results showed that ppt competitively inhibited UGT2B7-catalyzed AZT glucuronidation, and the inhibition kinetic parameter (Ki ) was determined to be 24.7 μM. Using the maximum plasma concentration of ppt (Cmax ), the alteration of area under the curve (AUC) of AZT was 6 %. All these results provide important information for understanding ginseng-AZT interaction. However, considering the complication of herbs and individuals, the in vitro-in vivo extrapolation (IV-IVE) results should be explained with more caution. Yu, Jian Wang, Chuan-Qiang Fang, Long-Hao Li, Meng Wang, Xiangyang Dai, Lu-Lu Gao, Ya-Jie http://sedici.unlp.edu.ar:80/handle/10915/20208 2019-07-06T20:02:45Z 2012-01-01T00:00:00Z

Comunicacion Latin American Journal of Pharmacy; vol. 31, no. 4 Tacrolimus (Brand name: Prograf), a kind of immunosuppressants, has been reported to induce drug-drug interaction with many clinical drugs. Tacrolimus-mycophenolic acid (MPA) interaction has been widely and frequently reported. Intestinal UDP-glucuronosyltransferase (UGT) 1A8-mediated metabolism plays a key role in the elimination of MPA, and alteration of the activity of UGT1A8 resulting from gene polymorphisms could significantly influence the catalyzing activity of MPA glucuronidation. The aim of the present study is to investigate the inhibitory potential of tacrolimus towards UGT1A8, which was speculated to be a potential cause for tacrolimus-MPA interaction. The recombinant UGT1A8 was used as enzyme source, and a nonspecific substrate 4-methylumbelliferone (4-MU) was utilized as substrate. The results showed that 100 μM of tacrolimus inhibited UGT1A8-mediated 4-MU glucuronidation activity by 82.3%. Further inhibition kinetic investigation showed that the inhibition of UGT1A8 by tacrolimus was best fit to competitive inhibition type, and the inhibition kinetic parameter (Ki) was determined to be 6.1 μM. All these results indicated that tacrolimus could exhibit strong inhibition towards UGT1A8, which should be paid more attention when explaining clinical tacrolimus-MPA interaction.

2012-01-01T00:00:00Z Tacrolimus (Brand name: Prograf), a kind of immunosuppressants, has been reported to induce drug-drug interaction with many clinical drugs. Tacrolimus-mycophenolic acid (MPA) interaction has been widely and frequently reported. Intestinal UDP-glucuronosyltransferase (UGT) 1A8-mediated metabolism plays a key role in the elimination of MPA, and alteration of the activity of UGT1A8 resulting from gene polymorphisms could significantly influence the catalyzing activity of MPA glucuronidation. The aim of the present study is to investigate the inhibitory potential of tacrolimus towards UGT1A8, which was speculated to be a potential cause for tacrolimus-MPA interaction. The recombinant UGT1A8 was used as enzyme source, and a nonspecific substrate 4-methylumbelliferone (4-MU) was utilized as substrate. The results showed that 100 μM of tacrolimus inhibited UGT1A8-mediated 4-MU glucuronidation activity by 82.3%. Further inhibition kinetic investigation showed that the inhibition of UGT1A8 by tacrolimus was best fit to competitive inhibition type, and the inhibition kinetic parameter (Ki) was determined to be 6.1 μM. All these results indicated that tacrolimus could exhibit strong inhibition towards UGT1A8, which should be paid more attention when explaining clinical tacrolimus-MPA interaction. Souza, Gustavo D. de Fernandes, Lucianno E. Rodrigues, Mônica A. Silva, Priscila P. Pereira-Maia, Elene C. Guerra, Wendell http://sedici.unlp.edu.ar:80/handle/10915/20207 2019-07-06T20:02:44Z 2012-01-01T00:00:00Z

Comunicacion Latin American Journal of Pharmacy; vol. 31, no. 4 New complexes of platinum and palladium were isolated with 2,4-dinitrophenylhydrazine (2,4-DNPH). These complexes were characterized and the results shown that the ligand is coordinated to platinum or palladium by the basic nitrogen of NH2 group and have the general structure cis-[M(2,4- DNPH)2Cl2 ].H2O where M = Pt or Pd. The thermal stability of the complexes was followed in the temperature range 25-850 ºC. The antitumor activity of the synthesized compounds has been studied and the compound cis-[Pt(2,4-DNPH)2Cl2 ], was found to display cytotoxicity (IC50 = 4.6 μmol/L) against K562 tumoral cell line. This work is the first to describe the cytotoxic activity of complexes containing 2,4-dinitrophenylhydrazine

2012-01-01T00:00:00Z New complexes of platinum and palladium were isolated with 2,4-dinitrophenylhydrazine (2,4-DNPH). These complexes were characterized and the results shown that the ligand is coordinated to platinum or palladium by the basic nitrogen of NH2 group and have the general structure cis-[M(2,4- DNPH)2Cl2 ].H2O where M = Pt or Pd. The thermal stability of the complexes was followed in the temperature range 25-850 ºC. The antitumor activity of the synthesized compounds has been studied and the compound cis-[Pt(2,4-DNPH)2Cl2 ], was found to display cytotoxicity (IC50 = 4.6 μmol/L) against K562 tumoral cell line. This work is the first to describe the cytotoxic activity of complexes containing 2,4-dinitrophenylhydrazine Qiu, Xiangjun Li, Wanshu Li, Junwei Wang, Mengmeng Wang, Jia Chen, Lianguo Sun, Wei Zhang, Likang Wen, Congcong Ge, Renshan Hu, Guoxin http://sedici.unlp.edu.ar:80/handle/10915/20206 2019-07-06T20:02:40Z 2012-01-01T00:00:00Z

Comunicacion Latin American Journal of Pharmacy; vol. 31, no. 4 11β-hydroxysteroid dehydrogenase (11β-HSD) plays an important part in mediating glucocorticoid action, catalyzing the interconversion of corticosterone (B) and dehydrocorticosterone (A) in rodents. The aim of our study is to investigate the effects of (+)-gossypol (G+) on 11β-HSD. Adult ICR mice were given B and B + (G+) by intraperitoneal injection. The activity of 11β-HSD was evaluated by measuring the ratio of A and B, meanwhile the effects of (+)-gossypol on the conversion rate of B to A was determined with HPLC. Serum A/B levels of the B+(G+) group decreased by 2.42, 7.32, 17.85, 31.39, and 40.02 % compared to the B group at each measured time interval. A/B levels at 1 h for the B + (G+) group decreased by 43.78, 21.29 and 34.47% in liver, kidney and adrenal glands, respectively, in comparison to the B group. However, (+)-gossypol had no effect on brain and testis. (+)-Gossypol was an inhibitor of 11β-HSD.

2012-01-01T00:00:00Z 11β-hydroxysteroid dehydrogenase (11β-HSD) plays an important part in mediating glucocorticoid action, catalyzing the interconversion of corticosterone (B) and dehydrocorticosterone (A) in rodents. The aim of our study is to investigate the effects of (+)-gossypol (G+) on 11β-HSD. Adult ICR mice were given B and B + (G+) by intraperitoneal injection. The activity of 11β-HSD was evaluated by measuring the ratio of A and B, meanwhile the effects of (+)-gossypol on the conversion rate of B to A was determined with HPLC. Serum A/B levels of the B+(G+) group decreased by 2.42, 7.32, 17.85, 31.39, and 40.02 % compared to the B group at each measured time interval. A/B levels at 1 h for the B + (G+) group decreased by 43.78, 21.29 and 34.47% in liver, kidney and adrenal glands, respectively, in comparison to the B group. However, (+)-gossypol had no effect on brain and testis. (+)-Gossypol was an inhibitor of 11β-HSD. Sun, Yingqian Wan, Shuxin Zhou, Lijun http://sedici.unlp.edu.ar:80/handle/10915/20190 2019-07-06T20:03:18Z 2012-01-01T00:00:00Z

Articulo Latin American Journal of Pharmacy; vol. 31, no. 4 Chitosan microparticles (Cs-MPs) for the dissolution and oral bioavailability improvement of curcumin (Cur) were prepared with sodium tripolyphosphate (TPP) by ionotropic gelation method. Response surface methodology (RSM) based on a three-factor, three-level Box-Behnken Design (BBD), was used to optimize the preparative conditions of Cs-MPs. The Cs-MPs were characterized for particle size distribution, morphology, X-ray diffractometry, Fourier transform infrared spectroscopy, dissolution profiles, and oral absorption. The optimum conditions were found to be: 1 % of acetic acid concentration, 0.83 of Cs/Cur ratio, 0.15 % of TPP concentration. Loading capacity, encapsulation efficiency and yield of the optimized Cs-MPs were 62.92, 95.41, and 66.20 %, respectively with 83.60 % cumulative release and 18.45 % burst release. Solid-state characterization techniques revealed the decreased crystallinity nature of Cur in Cs-MPs. Cs-MPs provided an improved pharmacokinetic parameter (Cmax = 782.84 ng/mL, tmax = 3.15 h) in rats as compared with pure drug (Cmax = 86.39 ng/mL, tmax = 1.05 h).

2012-01-01T00:00:00Z Chitosan microparticles (Cs-MPs) for the dissolution and oral bioavailability improvement of curcumin (Cur) were prepared with sodium tripolyphosphate (TPP) by ionotropic gelation method. Response surface methodology (RSM) based on a three-factor, three-level Box-Behnken Design (BBD), was used to optimize the preparative conditions of Cs-MPs. The Cs-MPs were characterized for particle size distribution, morphology, X-ray diffractometry, Fourier transform infrared spectroscopy, dissolution profiles, and oral absorption. The optimum conditions were found to be: 1 % of acetic acid concentration, 0.83 of Cs/Cur ratio, 0.15 % of TPP concentration. Loading capacity, encapsulation efficiency and yield of the optimized Cs-MPs were 62.92, 95.41, and 66.20 %, respectively with 83.60 % cumulative release and 18.45 % burst release. Solid-state characterization techniques revealed the decreased crystallinity nature of Cur in Cs-MPs. Cs-MPs provided an improved pharmacokinetic parameter (Cmax = 782.84 ng/mL, tmax = 3.15 h) in rats as compared with pure drug (Cmax = 86.39 ng/mL, tmax = 1.05 h). Lourenço, Felipe R. Pinto, Terezinha J. A. http://sedici.unlp.edu.ar:80/handle/10915/20189 2019-07-06T20:02:53Z 2012-01-01T00:00:00Z

Articulo Latin American Journal of Pharmacy; vol. 31, no. 4 Pharmaceutical equivalence is an important step towards the confirmation of similarity and interchangeability among pharmaceutical products, particularly regarding those that will not be tested for bioequivalence. The aim of this paper is to compare traditional difference testing to two one-side equivalence tests in the assessment of pharmaceutical equivalence, by means of equivalence studies between similar, generic and reference products of acyclovir cream, atropine sulfate injection, meropenem for injection, and metronidazole injection. All tests were performed in accordance with the Brazilian Pharmacopeia or the United States Pharmacopeia. All four possible combinations of results arise in these comparisons of difference testing and equivalence testing. Most of the former did not show significant difference, whereas the latter presented similarity. We concluded that equivalence testing is more appropriate than difference testing, what can make it a useful tool to assess pharmaceutical equivalence in products that will not be tested for bioequivalence.

2012-01-01T00:00:00Z Pharmaceutical equivalence is an important step towards the confirmation of similarity and interchangeability among pharmaceutical products, particularly regarding those that will not be tested for bioequivalence. The aim of this paper is to compare traditional difference testing to two one-side equivalence tests in the assessment of pharmaceutical equivalence, by means of equivalence studies between similar, generic and reference products of acyclovir cream, atropine sulfate injection, meropenem for injection, and metronidazole injection. All tests were performed in accordance with the Brazilian Pharmacopeia or the United States Pharmacopeia. All four possible combinations of results arise in these comparisons of difference testing and equivalence testing. Most of the former did not show significant difference, whereas the latter presented similarity. We concluded that equivalence testing is more appropriate than difference testing, what can make it a useful tool to assess pharmaceutical equivalence in products that will not be tested for bioequivalence. Liu, Bo Wu, Rong Zhang, Wei Zhang, Feng Zhou, Huamei Wang, Lulu Xiao, Xiaoqiu Zhang, Xia Wu, Xiaoling http://sedici.unlp.edu.ar:80/handle/10915/20188 2019-07-06T20:03:16Z 2012-01-01T00:00:00Z

Articulo Latin American Journal of Pharmacy; vol. 31, no. 4 The aim of this research was to evaluate the effect of the angiotensin converting enzyme (ACE) inhibitor fosinopril on liver fibrosis in rats with high fat diet (HFD) induced nonalcoholic steatohepatitis (NASH). We found that treatment with fosinopril improved liver fibrosis. Moreover, treatment with fosinopril decreased serum Angiotensin (Ang) II, leptin, transforming growth factor β1 and hyaluronic acid concentrations, increased serum ACE2, Ang-(1-7), and adiponectin concentrations in rats fed with HFD. In the liver, fosinopril led to decreased leptin, α-smooth muscle actin, and collagen I expression, increased ACE2 and adiponectin expression. In conclusion, Fosinopril improves liver fibrosis by upregulating ACE2/Ang-(1-7) axis activation in rats with HFD-induced NASH. Furthermore, fosinopril might regulate the progression of liver fibrosis through the downregulation of leptin and the upregulation of adiponectin.

2012-01-01T00:00:00Z The aim of this research was to evaluate the effect of the angiotensin converting enzyme (ACE) inhibitor fosinopril on liver fibrosis in rats with high fat diet (HFD) induced nonalcoholic steatohepatitis (NASH). We found that treatment with fosinopril improved liver fibrosis. Moreover, treatment with fosinopril decreased serum Angiotensin (Ang) II, leptin, transforming growth factor β1 and hyaluronic acid concentrations, increased serum ACE2, Ang-(1-7), and adiponectin concentrations in rats fed with HFD. In the liver, fosinopril led to decreased leptin, α-smooth muscle actin, and collagen I expression, increased ACE2 and adiponectin expression. In conclusion, Fosinopril improves liver fibrosis by upregulating ACE2/Ang-(1-7) axis activation in rats with HFD-induced NASH. Furthermore, fosinopril might regulate the progression of liver fibrosis through the downregulation of leptin and the upregulation of adiponectin. Cardillo, Alejandra B. Rodríguez Talou, Julián Giulietti, Ana María http://sedici.unlp.edu.ar:80/handle/10915/20187 2019-07-06T20:03:30Z 2012-01-01T00:00:00Z

Articulo Latin American Journal of Pharmacy; vol. 31, no. 4 Hyoscyamine, 6β-hydroxyhyoscyamine and scopolamine are anticholinergic agents that belong to the tropane alkaloids, a pharmacological important group of secondary metabolites. Hyoscyamine and scopolamine were historically used in medicine. Additionally, potential medical applications for 6β- hydroxyhyoscyamine were described in the last years. Previous works carried out in our lab allowed us the construction of a Saccharomyces cerevisiae strain harboring the Hyoscyamine-6β-hydroxylase (H6H) enzyme which is responsible of the conversion of hyoscyamine into 6β-hydroxyhyoscyamine and scopolamine. Several factors influenced and complicated the optimization of the hyoscyamine bioconversion process. The aim of this work was to evaluate the analytical factors that critically affect the performance of the alkaloid extraction and the detection and quantification method of the alkaloids implied in the biocatalytical process. The mechanical breakdown of yeast cells by continuous agitation at 4 °C in 2 mL tubes was the method of choice for an efficient recovery of the functional H6H enzyme. In addition, the different pH assayed for the alkaloid extraction caused significant variations in the recovery of the alkaloids, specifically impacting on scopolamine recovery which decreased a 35 % after the increase of the pH of the extraction. The development of robust and sensitive analytical methods was requisite for the correct monitoring and quantification of the alkaloids produced in order to evaluate the technological and economic feasibility of this process.

2012-01-01T00:00:00Z Hyoscyamine, 6β-hydroxyhyoscyamine and scopolamine are anticholinergic agents that belong to the tropane alkaloids, a pharmacological important group of secondary metabolites. Hyoscyamine and scopolamine were historically used in medicine. Additionally, potential medical applications for 6β- hydroxyhyoscyamine were described in the last years. Previous works carried out in our lab allowed us the construction of a Saccharomyces cerevisiae strain harboring the Hyoscyamine-6β-hydroxylase (H6H) enzyme which is responsible of the conversion of hyoscyamine into 6β-hydroxyhyoscyamine and scopolamine. Several factors influenced and complicated the optimization of the hyoscyamine bioconversion process. The aim of this work was to evaluate the analytical factors that critically affect the performance of the alkaloid extraction and the detection and quantification method of the alkaloids implied in the biocatalytical process. The mechanical breakdown of yeast cells by continuous agitation at 4 °C in 2 mL tubes was the method of choice for an efficient recovery of the functional H6H enzyme. In addition, the different pH assayed for the alkaloid extraction caused significant variations in the recovery of the alkaloids, specifically impacting on scopolamine recovery which decreased a 35 % after the increase of the pH of the extraction. The development of robust and sensitive analytical methods was requisite for the correct monitoring and quantification of the alkaloids produced in order to evaluate the technological and economic feasibility of this process. Gontijo, Mônica F. Ribeiro, Andréia Q. Klein, Carlos H. Rozenfeld, Suely Acurcio, Francisco de A. http://sedici.unlp.edu.ar:80/handle/10915/20185 2019-07-06T20:03:28Z 2012-01-01T00:00:00Z

Articulo Latin American Journal of Pharmacy; vol. 31, no. 4 Age-related transformations make the elderly more susceptible to medicine adverse events, and knowledge of factors associated with drug use are essential to develop national strategies of prescription. To estimate the prevalence of use of antihypertensive and hypoglycemic agents and investigate the factors associated with their consumption. Household survey among 667 elderly living in Belo Horizonte/MG, interviewed regarding socio-demographic indicator of health conditions and medication use. Univariate and multivariate analysis were performed. Among respondents, 62 % used antihypertensive and 12 % hypoglycemic drugs. Consumption of antihypertensive drugs was associated with a higher number of medical appointments, diabetes and hypertension, more cases of morbidity and use ≥ five active substances. Hypoglycemic drugs consumption was associated with male, older age, higher number of medical appointments, the occurrence of diabetes and hypertension. Considering determinants associated with medication use could help develop strategies for the safe medicine use.

2012-01-01T00:00:00Z Age-related transformations make the elderly more susceptible to medicine adverse events, and knowledge of factors associated with drug use are essential to develop national strategies of prescription. To estimate the prevalence of use of antihypertensive and hypoglycemic agents and investigate the factors associated with their consumption. Household survey among 667 elderly living in Belo Horizonte/MG, interviewed regarding socio-demographic indicator of health conditions and medication use. Univariate and multivariate analysis were performed. Among respondents, 62 % used antihypertensive and 12 % hypoglycemic drugs. Consumption of antihypertensive drugs was associated with a higher number of medical appointments, diabetes and hypertension, more cases of morbidity and use ≥ five active substances. Hypoglycemic drugs consumption was associated with male, older age, higher number of medical appointments, the occurrence of diabetes and hypertension. Considering determinants associated with medication use could help develop strategies for the safe medicine use. Solliman, Mukhtar A Hassali, Mohamed A. Al-Haddad, Mahmoud Sadi Sulaiman, Syed Azhar Syed Atif, Muhammad Saleem, Fahad http://sedici.unlp.edu.ar:80/handle/10915/20184 2019-07-06T20:03:12Z 2012-01-01T00:00:00Z

Articulo Latin American Journal of Pharmacy; vol. 31, no. 4 A retrospective study conducted in North East of Libya to evaluate treatment outcome of smear positive pulmonary tuberculosis (PTB) patients and factors associated with unsuccessful outcome and treatment default has been developed. Three hundred and twenty seven patients were notified in Kuwaifia chest hospital, Benghazi and Shahat chest hospital, Shahat, during 2007-2008. Using the World Health Organization criteria, treatment completion and cure rate was 1.2 % and 57.5 %, respectively. Treatment failure occurred in 7(2.1 %) cases. Ninety (27.5 %) patients defaulted treatment, 11 (3.4 %) died and 26 (8 %) transferred out. Over all, successful and unsuccessful treatment outcome was 58.7 % and 41.3 %, respectively. Libyan nationality was the only predictor of successful treatment outcome while Libyan nationality and diabetes mellitus had negative association with treatment default. Improving clinical and laboratory infrastructure in peripheral areas, educating defaulters about benefits of completing therapy and stratifying foreigners as high risk groups could improve success rate. Measures should be taken to improve professional commitment and expertise of health care professionals.

2012-01-01T00:00:00Z A retrospective study conducted in North East of Libya to evaluate treatment outcome of smear positive pulmonary tuberculosis (PTB) patients and factors associated with unsuccessful outcome and treatment default has been developed. Three hundred and twenty seven patients were notified in Kuwaifia chest hospital, Benghazi and Shahat chest hospital, Shahat, during 2007-2008. Using the World Health Organization criteria, treatment completion and cure rate was 1.2 % and 57.5 %, respectively. Treatment failure occurred in 7(2.1 %) cases. Ninety (27.5 %) patients defaulted treatment, 11 (3.4 %) died and 26 (8 %) transferred out. Over all, successful and unsuccessful treatment outcome was 58.7 % and 41.3 %, respectively. Libyan nationality was the only predictor of successful treatment outcome while Libyan nationality and diabetes mellitus had negative association with treatment default. Improving clinical and laboratory infrastructure in peripheral areas, educating defaulters about benefits of completing therapy and stratifying foreigners as high risk groups could improve success rate. Measures should be taken to improve professional commitment and expertise of health care professionals. Manivannan, E. Moorthy, N.S.H.N. http://sedici.unlp.edu.ar:80/handle/10915/20183 2019-07-06T20:03:25Z 2012-01-01T00:00:00Z

Articulo Latin American Journal of Pharmacy; vol. 31, no. 4 Classical Hansch type quantitative structure-activity relationship (QSAR) has been performed on a set of structurally modified celecoxib analogues for their inhibitory potency and selectivity towards cyclooxygenase isozymes using classical physicochemical and structural parameters. Statistically significant regression models were developed for cyclooxygenase-1 (COX-1), cyclooxygenase-2 (COX-2) inhibitory potency as well as selectivity index. The results of our QSAR study suggest the importance of the molecular size, shape and electronic character of the aromatic ring substituents. Further our investigation provides important structural and physicochemical features for designing potent and selective COX-2 inhibitors within the congener series of compounds.

2012-01-01T00:00:00Z Classical Hansch type quantitative structure-activity relationship (QSAR) has been performed on a set of structurally modified celecoxib analogues for their inhibitory potency and selectivity towards cyclooxygenase isozymes using classical physicochemical and structural parameters. Statistically significant regression models were developed for cyclooxygenase-1 (COX-1), cyclooxygenase-2 (COX-2) inhibitory potency as well as selectivity index. The results of our QSAR study suggest the importance of the molecular size, shape and electronic character of the aromatic ring substituents. Further our investigation provides important structural and physicochemical features for designing potent and selective COX-2 inhibitors within the congener series of compounds. Chen, Qiaoyun Liu, Yang Luo, Y.H. Luo, M. Luo, L.Y. http://sedici.unlp.edu.ar:80/handle/10915/20182 2019-07-06T20:03:10Z 2012-01-01T00:00:00Z

Articulo Latin American Journal of Pharmacy; vol. 31, no. 4 The aim of the present study was to establish a method for the determination of folic acid and related substances content in dispersible tablets. Method: A Shim-pack VP-ODS C18 reversed phase column (4.6 mm × 250 mm) was used. The mobile phase consisted of methanol-phosphate buffer (20:80) with a pH of 6.3.The flow rate was 1.0 mL/min, and the detection wavelength was 277nm and the column temperature was 30 °C. Results: The calibration curve was linear in the range of 5~150 μg/mL (r = 0.9998) for folic acid. The minimal detection limit was 99.08 %, n = 9 and the related substances were well separated. This method resulted to be convenient, accurate, selective and reliable, and can be applied for the quality control of folic acid.

2012-01-01T00:00:00Z The aim of the present study was to establish a method for the determination of folic acid and related substances content in dispersible tablets. Method: A Shim-pack VP-ODS C18 reversed phase column (4.6 mm × 250 mm) was used. The mobile phase consisted of methanol-phosphate buffer (20:80) with a pH of 6.3.The flow rate was 1.0 mL/min, and the detection wavelength was 277nm and the column temperature was 30 °C. Results: The calibration curve was linear in the range of 5~150 μg/mL (r = 0.9998) for folic acid. The minimal detection limit was 99.08 %, n = 9 and the related substances were well separated. This method resulted to be convenient, accurate, selective and reliable, and can be applied for the quality control of folic acid. Shahba, Ahmad A. Alanazi, Fars K. Mohsin, Kazi Abdel-Hamid, Magdi http://sedici.unlp.edu.ar:80/handle/10915/20181 2019-07-06T20:02:39Z 2012-01-01T00:00:00Z

Articulo Latin American Journal of Pharmacy; vol. 31, no. 4 The current study was designed to evaluate the chemical and physical stability of cinnarizine within self-emulsifying drug delivery systems. According to International Conference of Harmonization guidelines, the selected formulations were enrolled into both accelerated and long-term stability studies up to 6 and 12 months, respectively. The chemical stability of the formulations was assessed periodically based on the intact cinnarizine level. The physical stability was evaluated based on the physical appearance and color change pattern of the formulations. The accelerated stability study revealed significant cinnarizine degradation in all the tested formulations at 3 and 6 months. All the tested formulations experienced sharp discoloration within 6 months of storage. On the other hand, the long-term stability study showed no significant cinnarizine degradation or color change within the formulations containing 100 % saturated medium chain glycerides (as oil component). While, the formulations containing 50 % unsaturated long chain fatty acids showed considerable drug degradation as well as significant discoloration. Accordingly, The formulations containing 100 % saturated medium chain glycerides provide excellent chemical and physical stability pattern and have the potential to provide a stable dosage form of cinnarizine.

2012-01-01T00:00:00Z The current study was designed to evaluate the chemical and physical stability of cinnarizine within self-emulsifying drug delivery systems. According to International Conference of Harmonization guidelines, the selected formulations were enrolled into both accelerated and long-term stability studies up to 6 and 12 months, respectively. The chemical stability of the formulations was assessed periodically based on the intact cinnarizine level. The physical stability was evaluated based on the physical appearance and color change pattern of the formulations. The accelerated stability study revealed significant cinnarizine degradation in all the tested formulations at 3 and 6 months. All the tested formulations experienced sharp discoloration within 6 months of storage. On the other hand, the long-term stability study showed no significant cinnarizine degradation or color change within the formulations containing 100 % saturated medium chain glycerides (as oil component). While, the formulations containing 50 % unsaturated long chain fatty acids showed considerable drug degradation as well as significant discoloration. Accordingly, The formulations containing 100 % saturated medium chain glycerides provide excellent chemical and physical stability pattern and have the potential to provide a stable dosage form of cinnarizine. Döll-Boscardini, Patrícia M. Almeida, Martinha A. Nakashima, Tomoe Paula, Josiane de F. Padilha de Kanunfre, Carla C. Farago, Paulo V. http://sedici.unlp.edu.ar:80/handle/10915/20179 2019-07-06T20:03:20Z 2012-01-01T00:00:00Z

Articulo Latin American Journal of Pharmacy; vol. 31, no. 4 Few studies are concerned about the essential oil extracted from leaves of Eucalyptus benthamii Maiden et Cambage that shows high content of α-pinene. The goal of this paper was to investigate the in vitro effect of the essential oil of E. benthamii and α-pinene on lipopolysaccharide (LPS)-induced nitric oxide (NO) production in mouse peritoneal macrophages. Macrophages were harvested by washing with phosphate buffered saline and cultured with 10 μg/mL LPS. Three concentrations (5, 10, and 20 μg/mL) of the essential oil of E. benthamii and α-pinene were investigated. Nitrite levels were measured based on the Griess reaction, an indirect assay for NO production. The essential oil of E. benthamii significantly suppressed NO production in murine peritoneal macrophages at 10 and 20 μg/mL. In contrast, α-pinene did not inhibit NO production.

2012-01-01T00:00:00Z Few studies are concerned about the essential oil extracted from leaves of Eucalyptus benthamii Maiden et Cambage that shows high content of α-pinene. The goal of this paper was to investigate the in vitro effect of the essential oil of E. benthamii and α-pinene on lipopolysaccharide (LPS)-induced nitric oxide (NO) production in mouse peritoneal macrophages. Macrophages were harvested by washing with phosphate buffered saline and cultured with 10 μg/mL LPS. Three concentrations (5, 10, and 20 μg/mL) of the essential oil of E. benthamii and α-pinene were investigated. Nitrite levels were measured based on the Griess reaction, an indirect assay for NO production. The essential oil of E. benthamii significantly suppressed NO production in murine peritoneal macrophages at 10 and 20 μg/mL. In contrast, α-pinene did not inhibit NO production. Malkoc, Ismail Cetin, Nihal Altuner, Durdu Hacimuftuoglu, Ahmet Gursan, Nesrin Bakan, Ebubekir Akcay, Fatih Suleyman, Halis http://sedici.unlp.edu.ar:80/handle/10915/20178 2019-07-06T20:03:22Z 2012-01-01T00:00:00Z

Articulo Latin American Journal of Pharmacy; vol. 31, no. 4 The adverse biochemical and structural effects of antihypertensive drugs over a long period (clonidine, methyldopa, rilmenidine, amlodipine, ramipril) on hepatic tissue has been examined in this study. The results are considered to be beneficial for the identification of indications and contraindications in hypertensive patients. Severe bile duct proliferation, portal inflammation, interface hepatitis, focal necrosis and hepatocyte degeneration were demonstrated in the clonidine and amlodipine groups, which had higher oxidant parameters, aspartate aminotransferase, alanine amino transferase and lactate dehydrogenase activity and a higher amount of 8-OH Gua. In the group receiving rilmenidine, all the histopathological findings were the same as those in the clonidine and amlodipine groups, except for bile duct proliferation and interface hepatitis. On histopathological examination of the cell anatomy, it was shown that methyldopa and ramipril caused mild liver damage. While clonidine and amlodipine gave rise to severe liver damage, rilmenidine caused moderate damage, and methyldopa and ramipril led to mild loss of liver function.

2012-01-01T00:00:00Z The adverse biochemical and structural effects of antihypertensive drugs over a long period (clonidine, methyldopa, rilmenidine, amlodipine, ramipril) on hepatic tissue has been examined in this study. The results are considered to be beneficial for the identification of indications and contraindications in hypertensive patients. Severe bile duct proliferation, portal inflammation, interface hepatitis, focal necrosis and hepatocyte degeneration were demonstrated in the clonidine and amlodipine groups, which had higher oxidant parameters, aspartate aminotransferase, alanine amino transferase and lactate dehydrogenase activity and a higher amount of 8-OH Gua. In the group receiving rilmenidine, all the histopathological findings were the same as those in the clonidine and amlodipine groups, except for bile duct proliferation and interface hepatitis. On histopathological examination of the cell anatomy, it was shown that methyldopa and ramipril caused mild liver damage. While clonidine and amlodipine gave rise to severe liver damage, rilmenidine caused moderate damage, and methyldopa and ramipril led to mild loss of liver function. Chen, Xiaole Xu, Tao Wang, Zhe Pan, Peipei Luo, Shunbing Lin, Dan Hu, Guoxin Pan, Jianchun http://sedici.unlp.edu.ar:80/handle/10915/20174 2019-07-06T20:02:34Z 2012-01-01T00:00:00Z

Articulo Latin American Journal of Pharmacy; vol. 31, no. 4 A sensitive and selective liquid chromatography–mass spectrometry (LC–MS) method for determination of midazolam and its metabolite 1’-hydroxymidazolam in rat plasma was developed and validated. After addition of carbamazepine as internal standard (IS), protein precipitation by acetonitrile was used as sample preparation. The chromatographic separation was performed on a Zorbax SB-C18 column (150 × 2.1 mm, 5 μm), using acetonitrile-0.1 % formic acid as the mobile phase with gradient elution, delivered at a flow-rate of 0.4 mL/min. Electrospray ionization (ESI) source was applied and operated in positive ion mode, and selected ion monitoring (SIM) mode used to quantify midazolam and its metabolite 1’- hydroxymidazolam. Calibration curves were linear in the concentration ranges of 5-2000 ng/mL for midazolam and 10-2000 ng/mL for 1’-hydroxymidazolam, with a lower limit of quantification (LLOQ) of 5 ng/mL for midazolam and 10 ng/mL for 1’-hydroxymidazolam, respectively. Intra- and inter-day precision were less than 13 % and the accuracy ranged from -10.7 to 9.5 %. This developed method was successfully used for determination of midazolam and its metabolite 1’-hydroxymidazolam in rat plasma for pharmacokinetic study.

2012-01-01T00:00:00Z A sensitive and selective liquid chromatography–mass spectrometry (LC–MS) method for determination of midazolam and its metabolite 1’-hydroxymidazolam in rat plasma was developed and validated. After addition of carbamazepine as internal standard (IS), protein precipitation by acetonitrile was used as sample preparation. The chromatographic separation was performed on a Zorbax SB-C18 column (150 × 2.1 mm, 5 μm), using acetonitrile-0.1 % formic acid as the mobile phase with gradient elution, delivered at a flow-rate of 0.4 mL/min. Electrospray ionization (ESI) source was applied and operated in positive ion mode, and selected ion monitoring (SIM) mode used to quantify midazolam and its metabolite 1’- hydroxymidazolam. Calibration curves were linear in the concentration ranges of 5-2000 ng/mL for midazolam and 10-2000 ng/mL for 1’-hydroxymidazolam, with a lower limit of quantification (LLOQ) of 5 ng/mL for midazolam and 10 ng/mL for 1’-hydroxymidazolam, respectively. Intra- and inter-day precision were less than 13 % and the accuracy ranged from -10.7 to 9.5 %. This developed method was successfully used for determination of midazolam and its metabolite 1’-hydroxymidazolam in rat plasma for pharmacokinetic study. Duarte, Márcia do Rocio Dranka, Elize R. K. Yano, Mami http://sedici.unlp.edu.ar:80/handle/10915/20173 2019-07-06T20:02:50Z 2012-01-01T00:00:00Z

Articulo Latin American Journal of Pharmacy; vol. 31, no. 4 The genus Ormosia (Fabaceae-Faboideae) is common in the neotropics and includes different species used in folk medicine for various purposes. Ormosia arborea is a tree popularly known as “olho-decabra” and used for its contraceptive effects in Brazilian rural communities. As it lacks data about this medicinal plant, this work has carried out anatomical studies on the leaf of this potential vegetal drug. Fully-expanded leaves were fixed and prepared according to light and scanning electron microscopic techniques. Microchemical tests were also carried out. The leaf has paracytic stomata confined to the abaxial side. The cuticle is smooth and there are bicellular non-glandular trichomes predominantly on the abaxial surface. The mesophyll is dorsiventral and traversed by minor collateral vascular bundles with sclerenchymatic and crystalliferous bundle sheaths which may attain the epidermis. The midrib is concaveconvex in transection and has one major collateral vascular bundle in circular arrangement and one or two minor ones, each of which encircled by a sclerenchymatic bundle sheath. The petiole is circular in transection and possesses a ring of numerous collateral vascular bundles enclosed in a conspicuous sclerenchymatic sheath. Some cells bearing phenolic compounds and prismatic crystals of calcium oxalate are also present in the leaf.

2012-01-01T00:00:00Z The genus Ormosia (Fabaceae-Faboideae) is common in the neotropics and includes different species used in folk medicine for various purposes. Ormosia arborea is a tree popularly known as “olho-decabra” and used for its contraceptive effects in Brazilian rural communities. As it lacks data about this medicinal plant, this work has carried out anatomical studies on the leaf of this potential vegetal drug. Fully-expanded leaves were fixed and prepared according to light and scanning electron microscopic techniques. Microchemical tests were also carried out. The leaf has paracytic stomata confined to the abaxial side. The cuticle is smooth and there are bicellular non-glandular trichomes predominantly on the abaxial surface. The mesophyll is dorsiventral and traversed by minor collateral vascular bundles with sclerenchymatic and crystalliferous bundle sheaths which may attain the epidermis. The midrib is concaveconvex in transection and has one major collateral vascular bundle in circular arrangement and one or two minor ones, each of which encircled by a sclerenchymatic bundle sheath. The petiole is circular in transection and possesses a ring of numerous collateral vascular bundles enclosed in a conspicuous sclerenchymatic sheath. Some cells bearing phenolic compounds and prismatic crystals of calcium oxalate are also present in the leaf. Rao, Ganji Srinivas Karimian, Hamed Razavi, Mahboubeh Kumar, Nanjundan Prem Khajuria, Deepak Kumar Srinivas, Pradeep Sahebrao, Devkar Satish http://sedici.unlp.edu.ar:80/handle/10915/20172 2019-07-06T20:02:59Z 2012-01-01T00:00:00Z

Articulo Latin American Journal of Pharmacy; vol. 31, no. 4 The present study was undertaken to evaluate the possible antinociceptive effect of Terminalia bellirica fruit aqueous extract in animal models of diabetic neuropathic pain. Diabetes was induced by streptozotocin (50 mg/kg i.p.). T. bellirica (70 mg/kg), fluoxetine (14.5 mg/kg), imipramine (10.5 mg/kg) and quercetin (10 mg/kg) were administered orally for 21 consecutive days, starting after 4th week in streptozotocin induced diabetic rats. Hot plate test, tail immersion test and formalin test were used to assess the antinociceptive activity. For assessment of the role of opioid receptors in antinociception of T. bellirica, naloxone (2 mg/kg, i.p.) as opioid receptor antagonist was injected prior to its administration. Thiobarbituric acid reactive species (TBARS), catalase and superoxide dismutase were also estimated to evaluate oxidative stress. Diabetes induced axonal degeneration was assessed histopathologically. T. bellirica attenuated hyperalgesia in streptozotocin induced diabetic rats. Furthermore, T. bellirica significantly decreased TBARS and restored the activity of SOD and catalase towards normal. Histopathological examination of sciatic nerve also confirms the protective nature of T. bellirica. Antinociceptive activity of T. bellirica was reversed by prior administration of naloxone, and. was comparable with standard treatments like fluoxetine, imipramine and quercetin. The antidepressant and anti-oxidant activity of T. bellirica may be responsible for its antinociceptive action in diabetic neuropathy.

2012-01-01T00:00:00Z The present study was undertaken to evaluate the possible antinociceptive effect of Terminalia bellirica fruit aqueous extract in animal models of diabetic neuropathic pain. Diabetes was induced by streptozotocin (50 mg/kg i.p.). T. bellirica (70 mg/kg), fluoxetine (14.5 mg/kg), imipramine (10.5 mg/kg) and quercetin (10 mg/kg) were administered orally for 21 consecutive days, starting after 4th week in streptozotocin induced diabetic rats. Hot plate test, tail immersion test and formalin test were used to assess the antinociceptive activity. For assessment of the role of opioid receptors in antinociception of T. bellirica, naloxone (2 mg/kg, i.p.) as opioid receptor antagonist was injected prior to its administration. Thiobarbituric acid reactive species (TBARS), catalase and superoxide dismutase were also estimated to evaluate oxidative stress. Diabetes induced axonal degeneration was assessed histopathologically. T. bellirica attenuated hyperalgesia in streptozotocin induced diabetic rats. Furthermore, T. bellirica significantly decreased TBARS and restored the activity of SOD and catalase towards normal. Histopathological examination of sciatic nerve also confirms the protective nature of T. bellirica. Antinociceptive activity of T. bellirica was reversed by prior administration of naloxone, and. was comparable with standard treatments like fluoxetine, imipramine and quercetin. The antidepressant and anti-oxidant activity of T. bellirica may be responsible for its antinociceptive action in diabetic neuropathy.