D. Csupor, K. Boros, B. Danko, K. Veres, K. Szendrei, J. Hohmann
{"title":"Rapid identification of sibutramine in dietary supplements using a stepwise approach.","authors":"D. Csupor, K. Boros, B. Danko, K. Veres, K. Szendrei, J. Hohmann","doi":"10.1691/PH.2013.2069","DOIUrl":"https://doi.org/10.1691/PH.2013.2069","url":null,"abstract":"Adulteration of botanical food supplements with undeclared synthetic drugs is a common problem. One of the most affected product groups are the slimming agents. There are no analytical protocols for the detection of synthetic adulterants from these products. The present study aimed at the development of a multistep analytical method for the quick and reliable determination of sibutramine, one of the most common adulterants among botanical food supplements. The extract of a sibutramine-containing slimming formula was analysed by colour tests, TLC, HPLC-DAD, MS and NMR. The multistep method proposed by the authors allows the quick identification of sibutramine in counterfeit samples in laboratories with different instrumentation.","PeriodicalId":86039,"journal":{"name":"Die Pharmazie. Beihefte","volume":"66 1","pages":"15-8"},"PeriodicalIF":0.0,"publicationDate":"2013-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"73736571","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
S. S. Olmez, I. Vural, S. Sahin, A. Ertuğrul, Y. Capan
{"title":"Formulation and evaluation of clozapine orally disintegrating tablets prepared by direct compression.","authors":"S. S. Olmez, I. Vural, S. Sahin, A. Ertuğrul, Y. Capan","doi":"10.1691/PH.2013.2098","DOIUrl":"https://doi.org/10.1691/PH.2013.2098","url":null,"abstract":"In this study, clozapine orally disintegrating tablets (ODTs) were prepared by direct compression method. Disintegration time, resistance to crushing of tablets, porosity, friability, dissolution tests were performed and dissolution profiles of ODTs were investigated. Morphological and interaction studies were also performed. Friability values were found to be less than 1%. All tablet formulations disintegrated within 1 min and fulfilled the 3 min disintegration time required for ODTs given in the European Pharmacopoeia. More than 85% of the labeled amount of clozapine was dissolved in 15 min from the ODTs. No interaction or changes were found between active substance and excipients. As a result of the studies, ODT formulations developed in this study can be suggested as promising formulations, which assist development and manufacturing a generic product of clozapine.","PeriodicalId":86039,"journal":{"name":"Die Pharmazie. Beihefte","volume":"24 1","pages":"110-6"},"PeriodicalIF":0.0,"publicationDate":"2013-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"81460252","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
T. Zheng, C. Su, J. Zhao, X. -. Zhang, T. Y. Zhang, L. R. Zhang, Q. Kan, S. Zhang
{"title":"Effects of CYP3A5 and CYP2D6 genetic polymorphism on the pharmacokinetics of diltiazem and its metabolites in Chinese subjects.","authors":"T. Zheng, C. Su, J. Zhao, X. -. Zhang, T. Y. Zhang, L. R. Zhang, Q. Kan, S. Zhang","doi":"10.4172/0975-0851.S1.013","DOIUrl":"https://doi.org/10.4172/0975-0851.S1.013","url":null,"abstract":"PURPOSE To assess the possibility of using CYP2D6 10 +/- CYP3A5*3 as biomarkers to predict the pharmacokinetics of diltiazem and its two metabolites among healthy Chinese subjects. METHODS 41 healthy Chinese were genotyped for CYP3A5 3 and CYP2D6 10, and then received a single oral dose of diltiazem hydrochloride capsules (300 mg). Multiple blood samples were collected over 48 h, and the plasma concentrations of diltiazem, N-desmethyl diltiazem and desacetyl diltiazem were determined by HPLC-MS/MS. The relationships between the genotypes and pharmacokinetics were investigated. RESULTS The pharmacokinetics of diltiazem, N-desmethyl diltiazem were not significantly affected by both CYP3A5 3 and CYP2D6*10 alleles. However, the systemic exposure of the pharmacologyically active metabolites, desacetyl diltiazem, was 2-fold higher in CYP2D6 10/10 genotype carriers than in 1/10 or 1/1 ones (AUC(o-inf) of CYP2D6 1/1, 1/10 and 10/10 are 398.2 +/- 162.9, 371,0 69.2 and 726.2 +/- 468.1 respectively, p <0.05). CONCLUSIONS Two of the most frequent alleles, CYP3A5 3 and CYP2D6 10, among Chinese do not have major impacts on the disposition of diltiazem and N-desmethyl diltiazem. However, the desacetyl diltiazem showed 2-fold accumulation in individuals with CYP2D6 10/10 genotype. Despite this, the effect of genotype of CYP2D6 on clinical outcome of diltiazem treatment is expected to be limited.","PeriodicalId":86039,"journal":{"name":"Die Pharmazie. Beihefte","volume":"9 7 1","pages":"257-60"},"PeriodicalIF":0.0,"publicationDate":"2013-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"80634309","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
T. Araki, M. Takaai, A. Miyazaki, S. Ohshima, T. Shibamiya, T. Nakamura, K. Yamamoto
{"title":"Clinical efficacy of two forms of intravenous iron--saccharated ferric oxide and cideferron--for iron deficiency anemia.","authors":"T. Araki, M. Takaai, A. Miyazaki, S. Ohshima, T. Shibamiya, T. Nakamura, K. Yamamoto","doi":"10.1691/PH.2012.2588","DOIUrl":"https://doi.org/10.1691/PH.2012.2588","url":null,"abstract":"Over 90% of iron deficiency anemia cases are due to iron deficiency associated with depletion of stored iron or inadequate intake. Parenteral iron supplementation is an important part of the management of anemia, and some kinds of intravenous iron are used. However, few studies have evaluated the clinical efficacy of these drugs. The purpose of this study was to compare and assess the clinical efficacy of two types of intravenous iron injection, saccharated ferric oxide (SFO) and cideferron (CF). Medical records were obtained for 91 unrelated Japanese anemia patients treated with SFO (n = 37) or CF (n = 54) from May 2005 to May 2010 at Gunma University Hospital. Patients treated with blood transfusion, erythropoietin or oral iron were excluded. Hemoglobin (Hb) values measured on day 0, 7 and 14 were used to assess the efficacy of intravenous irons. A significant increase was observed in the mean Hb value by day 14 of administration in both the CF group and SFO group, and the mean Hb increase due to administration of CF for 7 days was comparable to that of SFO for 14 days. Age and sex did not affect improvement of Hb value. CF is fast acting and highly effective compared with SFO for the treatment of iron deficiency anemia. The use of CF may shorten a therapeutic period for iron deficiency anemia, and CF may be feasible for reducing the hospitalization period.","PeriodicalId":86039,"journal":{"name":"Die Pharmazie. Beihefte","volume":"9 1","pages":"1030-2"},"PeriodicalIF":0.0,"publicationDate":"2012-12-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"80655069","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
{"title":"A novel reversed-phase LC method for quantitative detection of azithromycin in bulk drug and tablet formulations in various aqueous media.","authors":"R. Odendaal, W. Liebenberg, M. Aucamp","doi":"10.1691/PH.2012.2041","DOIUrl":"https://doi.org/10.1691/PH.2012.2041","url":null,"abstract":"A novel reversed-phase HPLC method with UV-detection for separation, identification and quantification of azithromycin (AZH) was developed. The method was validated for the purpose of quantifying AZH in stability, dissolution and solubility studies. The method was validated at two optimum wavelengths where linear regression at both 205 and 210 nm, resulted in correlation coefficients of r2 = 0.9999. This HPLC method proved to be superior to other published methods due to the specificity, resulting in less peak interference and tailing. The pH of the mobile phase, as well as the ratio of buffer to organic component included in the mobile phase, proved to be critical factors in the improved detection of AZH.","PeriodicalId":86039,"journal":{"name":"Die Pharmazie. Beihefte","volume":"19 1","pages":"984-6"},"PeriodicalIF":0.0,"publicationDate":"2012-12-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"80895198","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
{"title":"Interference by bovine serum albumin in PED6 based phospholipase A2 screening assays.","authors":"L. Pohjala, N. Sairio, P. Vuorela","doi":"10.1691/PH.2012.2584","DOIUrl":"https://doi.org/10.1691/PH.2012.2584","url":null,"abstract":"","PeriodicalId":86039,"journal":{"name":"Die Pharmazie. Beihefte","volume":"49 1","pages":"954-5"},"PeriodicalIF":0.0,"publicationDate":"2012-11-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"74653026","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
{"title":"Synthesis, characterization, drug-loading capacity and safety of novel pH-independent amphiphilic amino acid copolymer micelles.","authors":"Jihui Tang, Jing Yao, Jingbo Shi, Qingping Xiao, Jianping Zhou, Feihu Chen","doi":"10.1691/PH.2012.1152","DOIUrl":"https://doi.org/10.1691/PH.2012.1152","url":null,"abstract":"A novel block copolymer containing two polymeric components, poly(L-aspartic acid)-b-poly (L-phenylalanine) (PAA-PPA), was synthesized and its potential for the preparation of copolymer micelles with a poorly water-soluble drug was investigated in this study. The chemical structure and physical properties of PAA-PPA were characterized by FTIR, 1H NMR and TG. The degree of polymerization of PAA-PPA was calculated by analyzing the relative area of N-CH signal and C-CH3 of 1H NMR spectra. The critical micelle concentration (CMC) of the PAA-PPA achieved a minimum of 11.1 mg/L. Studies on the drug-free PAA-PPA solutions showed PAA-PPA aggregation into micellar type in the sub-150 nm size range. Furthermore, the size of the PAA-PPA micelles was found to be pH-independent between the pH range of 4.0 and 8.0, which could be favorable to avoid the limitation of the size change at the specified pH value seeking drug stability. 4-amino-2-trifluoromethyl-phenyl retinate (ATPR) was studied as a poorly water-soluble model drug. The drug-loading and entrapment efficiency of the ATPR-loaded PAA-PPA micelles were 30.9 wt% and 87.9 %, respectively. The high drug-loading and entrapment efficiency were due to the synergistic effect of the micellar encapsulation and the binding interaction between drug and PAA-PPA. The ATPR-loaded PAA-PPA micelles showed a narrow size distribution, low zeta potential, high drug-loading capacity and good stable. The PAA-PPA was safer than Tween-80 and Cremophor EL (CrmEL) as an injectable pharmaceutical adjuvant for ATPR as indicated by the hemolysis and cytotoxicity studies. The novel amphiphilic amino acid copolymer can be considered as a prospective injectable delivery system for ATPR in terms of the pH-independent, greater drug-loading capacity and safety.","PeriodicalId":86039,"journal":{"name":"Die Pharmazie. Beihefte","volume":"46 1","pages":"756-64"},"PeriodicalIF":0.0,"publicationDate":"2012-09-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"91251042","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Zheng-gen Liao, Nan Zhang, Guowei Zhao, Jing Zhang, Xinli Liang, S. Zhong, G. Wang, Xu-long Chen
{"title":"Multivariate analysis approach for correlations between material properties and tablet tensile strength of microcrystalline cellulose.","authors":"Zheng-gen Liao, Nan Zhang, Guowei Zhao, Jing Zhang, Xinli Liang, S. Zhong, G. Wang, Xu-long Chen","doi":"10.1691/PH.2012.1158","DOIUrl":"https://doi.org/10.1691/PH.2012.1158","url":null,"abstract":"In this study we applied statistical multivariate analysis techniques to establish correlations between material properties and tablet tensile strength (TS) of microcrystalline cellulose (MCC) with different types and manufacturers. There were sixteen MCC samples included in this analysis described by 22 material parameters. For data analysis, principal component analysis (PCA) was used to model and evaluate the various relationships between the material properties and TS. Furthermore, partial least squares regression (PLS) analysis was performed to quantify the relationships between the material properties and TS and to predict the most influential MCC parameters contributing to the compactibility. The results showed that the moisture content, hygroscopicity and crystallinity did not exhibit significant impact on TS. The turgidity, maximum water uptake, degree of polymerization and molecular weight presented a strong positive influence on TS, while the density property, bulk and tap density, exhibited an obvious negative impact. The present work demonstrated that multivariate data analysis techniques (PCA and PLS) are useful for interpreting complex relations between 22 material properties and the tabletting properties of MCC. Furthermore, the method can be used for material classification.","PeriodicalId":86039,"journal":{"name":"Die Pharmazie. Beihefte","volume":"29 1","pages":"774-80"},"PeriodicalIF":0.0,"publicationDate":"2012-09-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"89174461","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Y. Shimizu, K. Isoda, E. Tezuka, T. Yufu, Y. Nagai, I. Ishida, M. Tezuka
{"title":"Influence of 50-nm polystyrene particles in inducing cytotoxicity in mice co-injected with carbon tetrachloride, cisplatin, or paraquat.","authors":"Y. Shimizu, K. Isoda, E. Tezuka, T. Yufu, Y. Nagai, I. Ishida, M. Tezuka","doi":"10.1016/J.TOXLET.2013.05.596","DOIUrl":"https://doi.org/10.1016/J.TOXLET.2013.05.596","url":null,"abstract":"","PeriodicalId":86039,"journal":{"name":"Die Pharmazie. Beihefte","volume":"7 1","pages":"712-4"},"PeriodicalIF":0.0,"publicationDate":"2012-08-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"83053643","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
L. Nardo, S. Kristensen, H. Tønnesen, A. Høgset, M. Lilletvedt
{"title":"Solubilization of the photosensitizers TPCS(2a) and TPPS(2a) in aqueous media evaluated by time-resolved fluorescence analysis.","authors":"L. Nardo, S. Kristensen, H. Tønnesen, A. Høgset, M. Lilletvedt","doi":"10.1691/PH.2012.1791","DOIUrl":"https://doi.org/10.1691/PH.2012.1791","url":null,"abstract":"The pH-dependent aggregation of the novel photosensitizer TPCS(2a) is investigated at low concentration (c = 10(-6) M) in aqueous media by means of time-correlated single-photon counting, and compared to that of the chemically related photosensitizer TPPS(2a). The efficacy of selected solubilizers, i.e., various nonionic Pluronic block copolymers and the nonionic surfactant Tween 80, in inhibiting aggregation of the two photosensitizers is evaluated, which is important for the further formulation of TPCS(2a).","PeriodicalId":86039,"journal":{"name":"Die Pharmazie. Beihefte","volume":"72 1","pages":"598-600"},"PeriodicalIF":0.0,"publicationDate":"2012-07-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"84036940","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}