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Scientia Pharmaceutica is published by MDPI from Volume 84 Issue 3 (2016). Articles in this Issue were published by another publisher in Open Access under a CC-BY (or CC-BY-NC-ND) licence. Articles are hosted by MDPI on mdpi.com as a courtesy and upon agreement with Austrian Pharmaceutical Society (Österreichische Pharmazeutische Gesellschaft, ÖPhG).

Table of Contents

Sci. Pharm., Volume 83, Issue 1 (March 2015) , Pages 1-220

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Open AccessArticle
Linking a Pharmaceutical Chemistry Workshop to Pharmacy Practice
Sci. Pharm. 2015, 83(1), 125-142; https://doi.org/10.3797/scipharm.1410-03
Received: 15 October 2014 / Accepted: 15 December 2014 / Published: 15 December 2014
Viewed by 535 | PDF Full-text (136 KB) | Supplementary Files
Abstract
This paper describes the design and implementation of a workshop to enhance pharmacy students’ appreciation of the importance of chemistry for pharmacy practice. The workshop was designed to form part of the practical work of two modules taught in the second year of [...] Read more.
This paper describes the design and implementation of a workshop to enhance pharmacy students’ appreciation of the importance of chemistry for pharmacy practice. The workshop was designed to form part of the practical work of two modules taught in the second year of the MPharm degree. In this mandatory workshop, second year pharmacy students were required to spot in the dispensary drugs based on their chemical properties like chirality, their origin and chemical structure. The lecturers involved in the workshop showed examples of the application of chemistry in the day to day work of the dispensary (e.g. calculating the dose for a patient in millimoles or how small modifications from a natural product can change its ability to cross the blood-brain-barrier). Feedback from participating students was collected via two survey instruments to examine the impact of the intervention. The survey results showed a clear shift towards a more positive perception by students of the chemistry taught in the MPharm curriculum. Full article
Open AccessArticle
Simultaneous Determination and Pharmacokinetic Study of Losartan, Losartan Carboxylic Acid, Ramipril, Ramiprilat, and Hydrochlorothiazide in Rat Plasma by a Liquid Chromatography/Tandem Mass Spectrometry Method
Sci. Pharm. 2015, 83(1), 107-124; https://doi.org/10.3797/scipharm.1410-15
Received: 21 October 2014 / Accepted: 30 November 2014 / Published: 30 November 2014
Cited by 3 | Viewed by 650 | PDF Full-text (1000 KB) | Supplementary Files
Abstract
The monitoring of the plasmatic concentrations of cardiovascular drugs is crucial for understanding their pharmacokinetics and pharmacodynamics. A simple, sensitive, specific, and high-throughput liquid chromatography/tandem mass spectrometry (LC–MS/MS) method was developed and validated for the simultaneous estimation and pharmacokinetic study of losartan (LOS), [...] Read more.
The monitoring of the plasmatic concentrations of cardiovascular drugs is crucial for understanding their pharmacokinetics and pharmacodynamics. A simple, sensitive, specific, and high-throughput liquid chromatography/tandem mass spectrometry (LC–MS/MS) method was developed and validated for the simultaneous estimation and pharmacokinetic study of losartan (LOS), losartan carboxylic acid (LCA), ramipril (RAM), ramiprilate (RPT), and hydrochloro-thiazide (HCZ) in rat plasma using irbesartan (IBS) and metolazone (MET) as internal standards (ISs). After solid phase extraction (SPE), analytes and ISs were separated on an Agilent Poroshell 120, EC-C18 (50 mm × 4.6 mm, i.d., 2.7 μm) column with a mobile phase consisting of methanol/water (85:15, v/v) containing 5 mmol/L ammonium formate and 0.1% formic acid at a flow rate of 0.4 mL/min. The precursor → product ion transitions for the analytes and ISs were monitored on a triple quadrupole mass spectrometer, operating in the multiple reaction monitoring (MRM) mode and switching the electrospray ionization (ESI) mode during chromatography from positive (to detect LOS, LCA, RAM, RPT, and IBS) to negative (to detect HCZ and MET). The method was validated as per the FDA guidelines and it exhibited sufficient specificity, accuracy, and precision. The method was found to be linear in the range of 3–3000 ng/mL for LOS and LCA, 0.1–200 ng/mL for RAM and RPT, and 1–1500 ng/mL for HCZ. The described method was successfully applied to the preclinical pharmacokinetic study of analytes after oral administration of a mixture of LOS (10 mg/kg), RAM (1 mg/kg), and HCZ (2.5 mg/kg) in rats. Full article
Open AccessArticle
Synthesis and Antifungal Evaluation of Novel N-Alkyl Tetra- and Perhydroquinoline Derivatives
Sci. Pharm. 2015, 83(1), 1-14; https://doi.org/10.3797/scipharm.1409-13
Received: 21 September 2014 / Accepted: 22 November 2014 / Published: 22 November 2014
Cited by 3 | Viewed by 579 | PDF Full-text (171 KB)
Abstract
A series of novel N-alkyl tetra- and perhydroquinoline derivatives and their hydrochlorides were prepared from tetrahydro- or trans-perhydroquinoline by direct alkylation with alkyl halides and subsequent precipitation with HCl gas. The antimicrobial activity of the resulting amines was evaluated in an agar diffusion [...] Read more.
A series of novel N-alkyl tetra- and perhydroquinoline derivatives and their hydrochlorides were prepared from tetrahydro- or trans-perhydroquinoline by direct alkylation with alkyl halides and subsequent precipitation with HCl gas. The antimicrobial activity of the resulting amines was evaluated in an agar diffusion assay. The minimal inhibitory concentrations (MIC) of the active com-pounds were determined by the microdilution method. In contrast to the tetra-hydroquinolines, the perhydro analogues showed significant antifungal activity. In an assay for the detection of target enzymes in ergosterol biosynthesis, N-undecylperhydroquinoline was identified as an inhibitor of Δ8,7-isomerase. Full article
Open AccessArticle
Curcumin Attenuates Oxidative Stress and Activation of Redox-Sensitive Kinases in High Fructose- and High-Fat-Fed Male Wistar Rats
Sci. Pharm. 2015, 83(1), 159-175; https://doi.org/10.3797/scipharm.1408-16
Received: 31 August 2014 / Accepted: 4 November 2014 / Published: 4 November 2014
Cited by 9 | Viewed by 601 | PDF Full-text (448 KB)
Abstract
The present study was carried out to investigate the effects of curcumin on oxidative stress and redox-sensitive kinases in high fructose- and high-fat-fed rats. Sixty rats were randomly divided into six groups with ten animals each. Rats were fed with a standard rodent [...] Read more.
The present study was carried out to investigate the effects of curcumin on oxidative stress and redox-sensitive kinases in high fructose- and high-fat-fed rats. Sixty rats were randomly divided into six groups with ten animals each. Rats were fed with a standard rodent diet, high fructose diet (60%), and high-fat diet (30%). Curcumin was administered to control, high fructose and high fat diet groups for ten weeks. At the end of the study, body weight and blood glucose levels were measured. The antioxidant enzymes GSH (reduced glutathione), GPx (glutathione peroxidase), and catalase activities were estimated in the blood. MDA, TAS, and TOS were estimated in the plasma, liver, and kidney. Curcumin treatment decreased body weight and blood glucose levels in the rats fed with fructose and high-fat diet. Antioxidant enzymes and plasma TAS were significantly improved by curcumin treatment in high fructose-fed rats, whereas in high-fat-fed rats, there was an increase only in the GPx activity. Curcumin significantly attenuated the elevation of plasma MDA and TOS in both diet groups. Hepatic MDA and TOS were found to be decreased upon curcumin supplementation in both diet groups, whereas a decrease in the renal MDA levels was observed only in fructose-treated rats, not in fat-fed rats. Curcumin treatment elevated liver TAS in rats fed only with the fructose-rich diet. Curcumin showed a significant decrease in the oxidative stress index (OSI) in plasma, liver, and kidney tissues in both diet groups. ERK phosphorylation was significantly decreased in both diet groups by curcumin treatment. Similarly, curcumin reduced the phosphorylation of p38 MAPK only in the high fructose-fed rats, not in the high-fat-fed rats. No significant changes were found in JNK phosphorylation in both diet groups. Thus, curcumin may be effective in the management of diet-induced oxidative stress and could be explored as a therapeutic adjuvant against complications associated with obesity and diabetes. Full article
Open AccessArticle
Synthesis and Antioxidant Activity of 7-Thio Derivatives of 6,7-Dihydro-1H-cyclopenta[d]pyrimidine-2,4(3H,5H)-dione
Sci. Pharm. 2015, 83(1), 41-48; https://doi.org/10.3797/scipharm.1406-09
Received: 20 June 2014 / Accepted: 29 October 2014 / Published: 29 October 2014
Viewed by 492 | PDF Full-text (134 KB)
Abstract
New 7-thio derivatives of 6,7-dihydro-1H-cyclopenta[d]pyrimidine-2,4(3H,5H)-dione have been synthesized by the reaction of 3-cyclohexyl-7-thio-6,7-dihydro-1H-cyclopenta[d]pyrimidine-2,4(3H,5H)-dione with alkylhalogenides. The synthesized compounds were tested for antioxidant activity on the model of [...] Read more.
New 7-thio derivatives of 6,7-dihydro-1H-cyclopenta[d]pyrimidine-2,4(3H,5H)-dione have been synthesized by the reaction of 3-cyclohexyl-7-thio-6,7-dihydro-1H-cyclopenta[d]pyrimidine-2,4(3H,5H)-dione with alkylhalogenides. The synthesized compounds were tested for antioxidant activity on the model of Fe2+-dependent oxidation of adrenaline in vitro. It was found that the antiradical activity of 7-thio derivatives of 6,7-dihydro-1H-cyclopenta[d]pyrimidine-2,4(3H,5H)-dione significantly depends on the structure of the substituent which is part of the thioether fragment of the base molecule. Full article
Open AccessArticle
Synthesis, Characterization, and Cytotoxicity of Some New 5-Aminopyrazole and Pyrazolo[1,5-a]pyrimidine Derivatives
Sci. Pharm. 2015, 83(1), 27-39; https://doi.org/10.3797/scipharm.1409-14
Received: 23 September 2014 / Accepted: 24 October 2014 / Published: 24 October 2014
Cited by 18 | Viewed by 608 | PDF Full-text (207 KB)
Abstract
5-Amino-N-aryl-3-[(4-methoxyphenyl)amino]-1H-pyrazole-4-carboxamides 4a–c were synthesized by the reaction of N-(aryl)-2-cyano-3-[(4-methoxyphenyl)-amino]-3-(methylthio)acrylamides 3a–c with hydrazine hydrate in ethanol. The reaction of 5-amino-N-aryl-1H-pyrazoles 4a–c with acetylacetone 5 or 2-(4-methoxybenzylidene)malononitrile 8 yielded the pyrazolo[1,5-a]pyrimidine derivatives 7a–c and [...] Read more.
5-Amino-N-aryl-3-[(4-methoxyphenyl)amino]-1H-pyrazole-4-carboxamides 4a–c were synthesized by the reaction of N-(aryl)-2-cyano-3-[(4-methoxyphenyl)-amino]-3-(methylthio)acrylamides 3a–c with hydrazine hydrate in ethanol. The reaction of 5-amino-N-aryl-1H-pyrazoles 4a–c with acetylacetone 5 or 2-(4-methoxybenzylidene)malononitrile 8 yielded the pyrazolo[1,5-a]pyrimidine derivatives 7a–c and 10a–c, respectively. The structures of the synthesized compounds were established based on elemental analysis and spectral data (IR, MS, 1H-NMR, and 13C-NMR). Representative examples of the new synthesized products were screened for their in vitro cytotoxic activity against Ehrlich Ascites Carcinoma (EAC) cells. Full article
Open AccessArticle
Screening of Panamanian Plants for Cosmetic Properties, and HPLC-Based Identification of Constituents with Antioxidant and UV-B Protecting Activities
Sci. Pharm. 2015, 83(1), 177-190; https://doi.org/10.3797/scipharm.1409-12
Received: 21 September 2014 / Accepted: 15 October 2014 / Published: 15 October 2014
Cited by 6 | Viewed by 627 | PDF Full-text (423 KB) | Supplementary Files
Abstract
A library of 600 taxonomically diverse Panamanian plant extracts was screened for DPPH scavenging and UV-B protective activities, and the methanolic extracts of Mosquitoxylum jamaicense, Combretum cacoucia, and Casearia commersionia were submitted to HPLC-based activity profiling. The compounds located in the [...] Read more.
A library of 600 taxonomically diverse Panamanian plant extracts was screened for DPPH scavenging and UV-B protective activities, and the methanolic extracts of Mosquitoxylum jamaicense, Combretum cacoucia, and Casearia commersionia were submitted to HPLC-based activity profiling. The compounds located in the active time windows were isolated and identified as gallic acid derivatives and flavonoids. Gallic acid methyl ester (3) and digallic acid derivatives (2, 6) showed the highest DPPH scavenging activity (<10 μg/mL), while protocatechuic acid (7) and isoquercitrin (10) exhibited the highest UV-B protective properties. Full article
Open AccessArticle
Identification, Isolation, and Characterization of a New Degradation Impurity in Nafcillin Sodium
Sci. Pharm. 2015, 83(1), 95-106; https://doi.org/10.3797/scipharm.1408-03
Received: 4 August 2014 / Accepted: 15 October 2014 / Published: 15 October 2014
Viewed by 657 | PDF Full-text (252 KB)
Abstract
A new degradant of Nafcillin Sodium was found at a level of 1.8% w/w during the gradient reversed-phase HPLC analysis in stability storage samples. This impurity was identified by LC-MS and was characterized by 1H-NMR, 13C-NMR, LC/MS/MS, elemental analysis, and IR [...] Read more.
A new degradant of Nafcillin Sodium was found at a level of 1.8% w/w during the gradient reversed-phase HPLC analysis in stability storage samples. This impurity was identified by LC-MS and was characterized by 1H-NMR, 13C-NMR, LC/MS/MS, elemental analysis, and IR techniques. Based on the structural elucidation data, this impurity was named as N-[(2S)-2-carboxy-2-{[(2-ethoxy-naphthalen-1-yl)carbonyl]amino}ethylidene]-3-({N-[(2-ethoxynaphthalen-1-yl)-carbonyl]glycyl}sulfanyl)-D-valine. This impurity was prepared by isolation and was co-injected into the HPLC system to confirm the retention time. To the best of our knowledge, this impurity has not been reported elsewhere. The identification and structural elucidation of this degradant impurity has been discussed in detail. Full article
Open AccessArticle
Mitigation of Methimazole-Induced Hepatic Injury by Taurine in Mice
Sci. Pharm. 2015, 83(1), 143-158; https://doi.org/10.3797/scipharm.1408-04
Received: 5 August 2014 / Accepted: 30 September 2014 / Published: 30 September 2014
Cited by 12 | Viewed by 611 | PDF Full-text (412 KB)
Abstract
Methimazole is the most widely prescribed antithyroid medication in humans. However, hepatotoxicity is a deleterious adverse effect associated with methimazole administration. No specific protective agent has been developed against this complication yet. This study was designed to investigate the role of taurine as [...] Read more.
Methimazole is the most widely prescribed antithyroid medication in humans. However, hepatotoxicity is a deleterious adverse effect associated with methimazole administration. No specific protective agent has been developed against this complication yet. This study was designed to investigate the role of taurine as a hepatoprotective agent against methimazole-induced liver injury in mice. Different reactive metabolites were proposed to be responsible for methimazole hepatotoxicity. Hence, methimazole-induced liver injury was investigated in intact and/or enzyme-induced animals in the current investigation. Animals were treated with methimazole (200 mg/kg, by gavage), and hepatic injury induced by this drug was investigated in intact and/or enzyme-induced groups. Markers such as lipid peroxidation, hepatic glutathione content, alanine aminotransferase (ALT) and alkaline phosphatase (ALP) in plasma, and histopathological changes in the liver of animals were monitored after drug administration. Methimazole caused liver injury as revealed by increased plasma ALT. Furthermore, a significant amount of lipid peroxidation was detected in the drug-treated animals, and hepatic glutathione reservoirs were depleted. Methimazole-induced hepatotoxicity was more severe in enzyme-induced mice. The above-mentioned alterations in hepatotoxicity markers were endorsed by significant histopathological changes in the liver. Taurine administration (1 g/kg, i.p.) effectively alleviated methimazole-induced liver injury in both intact and/or enzyme-induced animals. Full article
Open AccessEditorial
Scientia Pharmaceutica, Autorenhinweise 2015
Sci. Pharm. 2015, 83(1), 209-220; https://doi.org/10.3797/scipharm.aut-15-01
Received: 26 September 2014 / Accepted: 26 September 2014 / Published: 26 September 2014
Viewed by 393 | PDF Full-text (134 KB)
Abstract
Die Zeitschrift Scientia Pharmaceutica (www.scipharm.at) erscheint vierteljährlich jeweils am Quartalsende und ist ein Medium zur Publikation von Originalarbeiten, Kurzmit-teilungen und ausgewählten Übersichtsarbeiten aus allen wissenschaftlichen Disziplinen der Pharmazie und angrenzenden Gebieten sowie der pharmazeutischen Praxis. [...] Full article
Open AccessEditorial
In Honour of Em. o. Univ.-Prof. Mag. pharm. Dr. Wolfgang Kubelka on the Occasion of his 80th Birthday
Sci. Pharm. 2015, 83(1), 207; https://doi.org/10.3797/scipharm.ed-15-01
Received: 26 September 2014 / Accepted: 26 September 2014 / Published: 26 September 2014
Viewed by 402 | PDF Full-text (32 KB)
Abstract
Wolfgang Kubelka was born on February 18th, 1935 in Vienna. [...] Full article
Open AccessArticle
Enhancing Skin Permeation of Biphenylacetic Acid (BPA) Using Salt Formation with Organic and Alkali Metal Bases
Sci. Pharm. 2015, 83(1), 191-205; https://doi.org/10.3797/scipharm.1406-19
Received: 30 June 2014 / Accepted: 26 September 2014 / Published: 26 September 2014
Cited by 2 | Viewed by 497 | PDF Full-text (1171 KB)
Abstract
In the present study, a series of organic and alkali metal salts of biphenylacetic acid (BPA) have been prepared and evaluated in vitro for percutaneous drug delivery. The physicochemical properties of BPA salts were determined using solubility measurements, DSC, and IR. The DSC [...] Read more.
In the present study, a series of organic and alkali metal salts of biphenylacetic acid (BPA) have been prepared and evaluated in vitro for percutaneous drug delivery. The physicochemical properties of BPA salts were determined using solubility measurements, DSC, and IR. The DSC thermogram and FTIR spectra confirmed the salt formation with organic and alkali metal bases. Among the series, salts with organic amines (ethanolamine, diethanolamine, triethanol-amine, and diethylamine) had lowered melting points while the alkali metal salt (sodium) had a higher melting point than BPA. The in vitro study showed that salt formation improves the physicochemical properties of BPA, leading to improved permeability through the skin. Amongst all the prepared salts, ethanolamine salt (1b) showed 7.2- and 5.4-fold higher skin permeation than the parent drug at pH 7.4 and 5.0, respectively, using rat skin. Full article
Open AccessArticle
A Stability-Indicating HPLC Method for the Determination of Fingolimod in Pharmaceutical Dosage Forms
Sci. Pharm. 2015, 83(1), 85-93; https://doi.org/10.3797/scipharm.1408-08
Received: 12 August 2014 / Accepted: 23 September 2014 / Published: 23 September 2014
Cited by 1 | Viewed by 856 | PDF Full-text (175 KB)
Abstract
Fingolimod is an immunosuppressive agent which is used for the prophylaxis of organ transplantation rejection or multiple sclerosis treatment. In this study, systematic forced degradation studies on fingolimod bulk powder were performed to develop a stability-indicating HPLC method. Separation of fingolimod and its [...] Read more.
Fingolimod is an immunosuppressive agent which is used for the prophylaxis of organ transplantation rejection or multiple sclerosis treatment. In this study, systematic forced degradation studies on fingolimod bulk powder were performed to develop a stability-indicating HPLC method. Separation of fingolimod and its degradation products was achieved on a Nova-Pak C8 column. The mobile phase was a mixture of potassium dihydrogenphosphate 50 mM (pH 3.0) and acetonitrile (45:55, v/v) at a flow rate of 1 ml/min. The proposed method was linear in the range of 0.125–20 μg mL−1. The within-day and between-day coefficients of variation were in the range of 0.6–1.2%. The developed method was successfully applied for the determination of the fingolimod amount in pharmaceutical dosage forms. Full article
Open AccessArticle
Synthesis and Characterization of Impurities in the Production Process of Lopinavir
Sci. Pharm. 2015, 83(1), 49-63; https://doi.org/10.3797/scipharm.1407-14
Received: 22 July 2014 / Accepted: 22 September 2014 / Published: 22 September 2014
Viewed by 915 | PDF Full-text (167 KB) | Supplementary Files
Abstract
Lopinavir is an antiretroviral drug used for the inhibition of HIV protease. Four related substances of lopinavir were observed during the manufacturing process of lopinavir in the laboratory and they were identified. The present work describes the origin, synthesis, characterization, and control of [...] Read more.
Lopinavir is an antiretroviral drug used for the inhibition of HIV protease. Four related substances of lopinavir were observed during the manufacturing process of lopinavir in the laboratory and they were identified. The present work describes the origin, synthesis, characterization, and control of these related substances. Full article
Open AccessArticle
Design, Synthesis, and Biological Evaluation of New 2-Phenyl-4H-chromen-4-one Derivatives as Selective Cyclooxygenase-2 Inhibitors
Sci. Pharm. 2015, 83(1), 15-26; https://doi.org/10.3797/scipharm.1407-20
Received: 26 July 2014 / Accepted: 15 September 2014 / Published: 15 September 2014
Cited by 4 | Viewed by 509 | PDF Full-text (257 KB)
Abstract
In order to develop new selective COX-2 inhibitors, a new series of 2-phenyl-4H-chromen-4-one derivatives possessing a methylsulfonyl pharmacophore group at the para position of the C-4 phenyl ring were designed, synthesized, and evaluated for cyclooxygenase-2 inhibitory activity. In vitro COX-1/COX-2 isozyme [...] Read more.
In order to develop new selective COX-2 inhibitors, a new series of 2-phenyl-4H-chromen-4-one derivatives possessing a methylsulfonyl pharmacophore group at the para position of the C-4 phenyl ring were designed, synthesized, and evaluated for cyclooxygenase-2 inhibitory activity. In vitro COX-1/COX-2 isozyme inhibition structure-activity studies identified 3-(benzyloxy)-2-[4-(methylsulfonyl)phenyl]-4H-chromen-4-one (5d) as a potent COX-2 inhibitor (IC50 = 0.07 μM) with a high COX-2 selectivity index (SI = 287.1) comparable to the reference drug celecoxib (COX-2 IC50 = 0.06 μM; COX-2 SI = 405). A molecular modeling study where 3-(benzyloxy)-2-[4-(methylsulfonyl)phenyl]-4H-chromen-4-one (5d) was docked into the active site of COX-2 showed that the p-MeSO2 substituent on the C-4 phenyl ring was well-oriented in the vicinity of the COX-2 secondary pocket (Arg513, Val523, and His90) and the carbonyl group of the chromene ring could interact with Ser530. The structure-activity data acquired indicated that the nature and size of the substituent on the C-3 chromene scaffold are important for COX-2 inhibitory activity. Our results also indicated that the chromene moiety constitutes a suitable template to design new COX-2 inhibitors. Full article
Open AccessArticle
Isolation, Identification, and Characterisation of Degradation Products and the Development and Validation of a Stability-Indicating Method for the Estimation of Impurities in the Tolterodine Tartrate Formulation
Sci. Pharm. 2015, 83(1), 65-83; https://doi.org/10.3797/scipharm.1407-18
Received: 24 July 2014 / Accepted: 8 September 2014 / Published: 8 September 2014
Cited by 1 | Viewed by 592 | PDF Full-text (354 KB)
Abstract
A short and sensitive stability-indicating gradient RP-UPLC method was developed for the quantitative determination of process-related impurities and degradation products of tolterodine tartrate in pharmaceutical formulations. The method was developed by using the Waters ACQUITY UPLC™ BEH shield RP18 (2.1 x 100 mm, [...] Read more.
A short and sensitive stability-indicating gradient RP-UPLC method was developed for the quantitative determination of process-related impurities and degradation products of tolterodine tartrate in pharmaceutical formulations. The method was developed by using the Waters ACQUITY UPLC™ BEH shield RP18 (2.1 x 100 mm, 1.7 μm) column with a mobile phase containing a gradient mixture of solvent A and B at a detection wavelength of 210 nm. During the stress study, the degradation products of tolterodine tartrate were well-resolved from tolterodine and its impurities and the mass balances were found to be satisfactory in all the stress conditions, thus proving the stability-indicating capability of the method. The developed method was validated as per ICH guidelines with respect to specificity, linearity, limit of detection and quantifica-tion, accuracy, precision, ruggedness, and robustness. During the stability (40°C/75% RH, 3 months) analysis of the drug product, one unknown impurity was detected by the above stability-indicating method. The unknown impurity was isolated by preparative HPLC and subjected to mass and NMR studies. Based on the spectral data, the unknown impurity was characterised as 2-(3-amino-1-phenylpropyl)-4-methylphenol (des-N,N-diisopropyl tolterodine). Structural elucidation of the impurity by spectral data is discussed in detail. Full article
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