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

Sci. Pharm., Volume 79, Issue 1 (March 2011) – 16 articles , Pages 1-224

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188 KiB  
Editorial
Scientia Pharmaceutica, Autorenhinweise 2011
by Scientia Pharmaceutica Editorial Office
Sci. Pharm. 2011, 79(1), 213-224; https://doi.org/10.3797/scipharm.aut-11-01 - 12 Feb 2011
Viewed by 1003
164 KiB  
Short Communication
Phenolics from Rhagadiolus stellatus (Asteraceae, Cichorieae)
by Romana KRIMPLSTÄTTER, Benjamin MA, Renate SPITALER, Ernst ELLMERER and Christian ZIDORN
Sci. Pharm. 2011, 79(1), 175-180; https://doi.org/10.3797/scipharm.1011-12 - 7 Feb 2011
Cited by 5 | Viewed by 1228
Abstract
Rhagadiolus stellatus Gaertn., a Mediterranean member of the Cichorieae tribe of the Asteraceae family used as a food plant, was analyzed for its spectrum of phenolic compounds. Kaempferol 3-O-β-glucoside 1, kaempferol 3-O-β- rutinoside (nicotiflorin) 2, quercetin 3-O-β-glucoside [...] Read more.
Rhagadiolus stellatus Gaertn., a Mediterranean member of the Cichorieae tribe of the Asteraceae family used as a food plant, was analyzed for its spectrum of phenolic compounds. Kaempferol 3-O-β-glucoside 1, kaempferol 3-O-β- rutinoside (nicotiflorin) 2, quercetin 3-O-β-glucoside 3, and luteolin 4 were isolated from the n-butanol layer of a methanolic extract of whole plants of Rh. stellatus of Spanish origin by repeated Sephadex LH-20 column chromatography. Structures were determined based on NMR and MS data as well as by comparison with literature data. Additionally, chlorogenic acid 5 and 3,5-dicaffeoylquinic acid 6 were detected by HPLC/DAD and HPLC/MS. Chemosystematic implications of the presented findings are discussed in comparison with other members of the Cichorieae tribe. Full article
192 KiB  
Article
Antitrypanosomal and Cytotoxic Activities of 22-Hydroxyclerosterol, a New Sterol from Allexis cauliflora (Violaceae)
by Yves Oscar D. NGANSO, Igor Eric W. NGANTCHOU, Ernestine NKWENOUA, Barthelemy NYASSE, Colette DENIER, Véronique HANNERT and Bernd SCHNEIDER
Sci. Pharm. 2011, 79(1), 137-144; https://doi.org/10.3797/scipharm.1012-10 - 7 Feb 2011
Cited by 9 | Viewed by 1600
Abstract
In the search for new antiparasitic natural compounds from the medicinal plants from Cameroon, the new 22-hydroxyclerosterol, established as such on the basis of detailed chemical and spectroscopic analysis, was isolated from the hexane extract of the stem bark of Allexis cauliflora together [...] Read more.
In the search for new antiparasitic natural compounds from the medicinal plants from Cameroon, the new 22-hydroxyclerosterol, established as such on the basis of detailed chemical and spectroscopic analysis, was isolated from the hexane extract of the stem bark of Allexis cauliflora together with the known clerosterol. 22-Hydroxyclerosterol inhibited the growth of Trypanosoma brucei brucei cells with an ED50 value of 1.56 μM. The compound was also established as an uncompetitive inhibitor of the glycolytic enzyme PGI of T. brucei (Ki’= 3 ± 1 μM), an uncompetitive inhibitor of mammalian rabbit muscles’ enzyme PyK (Ki’= 26 ± 3 μM) and a mixed inhibitor of PyK of Leishmania mexicana (Ki’= 65 ± 10 μM; Ki= 24 ± 5 μM). Full article
199 KiB  
Article
Stability Indicating LC-Method for Estimation of Paracetamol and Lornoxicam in Combined Dosage Form
by Dimal A. SHAH, Neel J. PATEL, Sunil L. BALDANIA, Usman K. CHHALOTIYA and Kashyap K. BHATT
Sci. Pharm. 2011, 79(1), 113-122; https://doi.org/10.3797/scipharm.1012-03 - 20 Jan 2011
Cited by 12 | Viewed by 1706
Abstract
A simple, specific and stability indicating reversed phase high performance liquid chromatographic method was developed for the simultaneous determination of paracetamol and lornoxicam in tablet dosage form. A Brownlee C-18, 5 μm column having 250×4.6 mm i.d. in isocratic mode, with mobile phase [...] Read more.
A simple, specific and stability indicating reversed phase high performance liquid chromatographic method was developed for the simultaneous determination of paracetamol and lornoxicam in tablet dosage form. A Brownlee C-18, 5 μm column having 250×4.6 mm i.d. in isocratic mode, with mobile phase containing 0.05 M potassium dihydrogen phosphate:methanol (40:60, v/v) was used. The flow rate was 1.0 ml/min and effluents were monitored at 266 nm. The retention times of paracetamol and lornoxicam were 2.7 min and 5.1 min, respectively. The linearity for paracetamol and lornoxicam were in the range of 5–200 μg/ml and 0.08–20 μg/ml, respectively. Paracetamol and lornoxicam stock solutions were subjected to acid and alkali hydrolysis, chemical oxidation and dry heat degradation. The proposed method was validated and successfully applied to the estimation of paracetamol and lornoxicam in combined tablet dosage form. Full article
333 KiB  
Article
Development and Validation of a Stability Indicating RP-UPLC Method for Determination of Quetiapine in Pharmaceutical Dosage Form
by Rakshit Kanubhai TRIVEDI and Mukesh C. PATEL
Sci. Pharm. 2011, 79(1), 97-112; https://doi.org/10.3797/scipharm.1009-12 - 16 Jan 2011
Cited by 21 | Viewed by 2000
Abstract
The present work reports a stability indicating reversed phase ultra performance liquid chromatography (RP-UPLC) method for the quantitative determination of quetiapine in pharmaceutical dosage form. The chromatographic separation is performed on an Agilent Eclipse Plus C18, RRHD 1.8 μm (50 mm x 2.1 [...] Read more.
The present work reports a stability indicating reversed phase ultra performance liquid chromatography (RP-UPLC) method for the quantitative determination of quetiapine in pharmaceutical dosage form. The chromatographic separation is performed on an Agilent Eclipse Plus C18, RRHD 1.8 μm (50 mm x 2.1 mm) column using gradient elution. The optimized mobile phase consists of 0.1 % aqueous triethylamine (pH 7.2) as a solvent-A and 80:20 v/v mixture of acetonitrile and methanol as solvent-B. The eluted compounds are monitored at 252 nm wavelength using a UV detector. The developed method separates quetiapine from its five impurities/degradation products within a run time of 5 min. Stability indicating capability of the developed method is established by analyzing forced degradation samples in which the spectral purity of quetiapine is ascertained along with the separation of degradation products from analyte peak. The developed RP-UPLC method is validated as per International Conference on Harmonization (ICH) guidelines with respect to system suitability, specificity, precision, accuracy, linearity, robustness and filter compatibility. Full article
240 KiB  
Article
Optimization of Forced Degradation Using Experimental Design and Development of a Stability-Indicating Liquid Chromatographic Assay Method for Rebamipide in Bulk and Tablet Dosage Form
by Sandeep SONAWANE and Paraag GIDE
Sci. Pharm. 2011, 79(1), 85-96; https://doi.org/10.3797/scipharm.1011-06 - 10 Jan 2011
Cited by 13 | Viewed by 2943
Abstract
A novel stability-indicating RP-HPLC assay method was developed and validated for quantitative determination of rebamipide in bulk and tablet dosage form. Rebamipide (drug and drug product) solutions were exposed to acid and alkali hydrolysis, thermal stress, oxidation by hydrogen peroxide and photodegradation. Experimental [...] Read more.
A novel stability-indicating RP-HPLC assay method was developed and validated for quantitative determination of rebamipide in bulk and tablet dosage form. Rebamipide (drug and drug product) solutions were exposed to acid and alkali hydrolysis, thermal stress, oxidation by hydrogen peroxide and photodegradation. Experimental design has been used during forced degradation to determine significant factors responsible for degradation and to obtain optimal degradation conditions. In addition, acid and alkali hydrolysis was performed using a microwave oven. The chromatographic method employed the HiQ sil C-18HS (250 × 4.6 mm; 5 μm) column with mobile phase consisting of 0.02 M potassium phosphate (pH adjusted to 6.8) and methanol (40:60, v/v) and the detection was performed at 230 nm. The procedure was validated for specificity, linearity, accuracy, precision and robustness. There was no interference observed of excipients and degradation products in the determination of the active pharmaceutical ingredient. The method showed good accuracy and precision (intra and inter day) and the response was linear in a range from 0.5 to 5 μg mL−1. The method was found to be simple and fast with less trial and error experimentation by making use of experimental design. Also, it proved that microwave energy can be used to expedite hydrolysis of rebamipide. Full article
358 KiB  
Article
Rapid Simultaneous Determination of Telmisartan, Amlodipine Besylate and Hydrochlorothiazide in a Combined Poly Pill Dosage Form by Stability-Indicating Ultra Performance Liquid Chromatography
by Santaji NALWADE, Vangala RANGA REDDY, Dantu DURGA RAO and Inabathina KOTESWARA RAO
Sci. Pharm. 2011, 79(1), 69-84; https://doi.org/10.3797/scipharm.1006-10 - 4 Jan 2011
Cited by 44 | Viewed by 2855
Abstract
A simple, precise and rapid stability-indicating ultra-performance liquid chromatography (UPLC) method is developed for the simultaneous quantitative determination of Telmisartan, Amlodipine besylate and Hydrochlorothiazide from their innovative poly pill combination drug product in the presence of degradation products. It involves a 100 mm [...] Read more.
A simple, precise and rapid stability-indicating ultra-performance liquid chromatography (UPLC) method is developed for the simultaneous quantitative determination of Telmisartan, Amlodipine besylate and Hydrochlorothiazide from their innovative poly pill combination drug product in the presence of degradation products. It involves a 100 mm x 2.1 mm, 1.7 μm C-18 column. The separation is achieved on a simple gradient method. The mobile phase A contains a mixture of sodium perchlorate buffer pH 3.2 (0.053M): acetonitrile in the ratio 90:10, v/v, and mobile B contains a mixture of sodium perchlorate buffer pH 3.2 (0.053M): acetonitrile in the ratio 20:80, v/v. The flow rate is 0.6 mL min−1 and the column temperature is maintained at 55°C.The gradient program (T/%B) is set as 0/5, 1.2/5, 1.6/40, 4/40, 4.1/5 and 4.5/5. The detector wavelength is 271 nm for Hydrochlorothiazide and Telmisartan and 237 nm for Amlodipine. The retention times of Telmisartan, Amlodipine, and Hydrochlorothiazide are 3.6 minutes, 3.2 minutes and 0.9 minutes; respectively. The total runtime for the separation of the three active compounds and their degradation products is 4.5 minutes. The described method is validated with respect to system suitability, specificity, linearity, precision and accuracy. The precision of the assay method is evaluated by carrying out six independent assays of T, A and H (0.032 mg mL−1 of T, 0.004 mg mL−1 of A, 0.01 mg mL−1 of H). The accuracy of the method is evaluated in triplicate at three concentration levels, i.e. 50%, 100% and 150% of target test concentration (0.64 mg mL−1 of T, 0.08 mg mL−1 of A, 0.2 mg mL−1 of H). The described method is linear over the range, 16 to 48 μg mL−1 for T, 2 to 6 μg mL−1A and 5 to 15 μg mL−1 for H. The method is fast and suitable for high-throughput analysis allowing the analysis of about 250 samples per working day. Full article
450 KiB  
Review
Phytoestrogen Biological Actions on Mammalian Reproductive System and Cancer Growth
by E ZHAO and Qing MU
Sci. Pharm. 2011, 79(1), 1-20; https://doi.org/10.3797/scipharm.1007-15 - 31 Dec 2010
Cited by 67 | Viewed by 2993
Abstract
Phytoestrogens are a family of diverse polyphenolic compounds derived from nature plant that structurally or functionally mimic circulating estrogen in the mammalian reproductive system. They induce estrogenic and anti-estrogenic effects in the brain-pituitary-gonad axis (a principal endocrine system involving in reproductive regulation) and [...] Read more.
Phytoestrogens are a family of diverse polyphenolic compounds derived from nature plant that structurally or functionally mimic circulating estrogen in the mammalian reproductive system. They induce estrogenic and anti-estrogenic effects in the brain-pituitary-gonad axis (a principal endocrine system involving in reproductive regulation) and peripheral reproductive organs. The dichotomy of phytoestrogen-mediated actions elucidates that they play the biological activities via complex mechanisms and belong to various chemical classes. In comparison with their unobvious physiological functions in normal reproductive tissues, there are increasing investigations showing that phytoestrogen induces significant inhibitory effects on the growth of breast and ovarian cancers through different signaling pathways. This review summarized the results of the previous studies regarding principal signaling transductions for mediating the growth of the ovarian and breast cancers. Phytoestrogen potentially modulates the signaling molecules via: (1) blocking the nuclear and membrane estrogen receptors (ER), (2) interfering with the growth factor receptor, (3) inhibiting the G protein-coupled receptor in ER-deficient cells, (4) activating apoptosis and nullifying anti-apoptotic signals. Full article
190 KiB  
Article
The Gramine Route to Pyrido[4,3-b]indol-3-ones – Identification of a New Cytotoxic Lead
by Uwe WOLLEIN and Franz BRACHER
Sci. Pharm. 2011, 79(1), 59-68; https://doi.org/10.3797/scipharm.1011-11 - 18 Dec 2010
Cited by 8 | Viewed by 1308
Abstract
A novel approach to 3-oxo-γ-carbolines was worked out starting from methyl indol-2-ylacetate via a gramine derivative. After quaternization, ammonia and 4-methoxybenzylamine could be inserted giving appropriate 3-oxo-γ-carbolines. Condensation with 2-chlorobenzaldehyde under microwave irradiation gave a 4-(2-chlorobenzyl)-3-oxo-γ-carboline. N-methylation lead to a product with [...] Read more.
A novel approach to 3-oxo-γ-carbolines was worked out starting from methyl indol-2-ylacetate via a gramine derivative. After quaternization, ammonia and 4-methoxybenzylamine could be inserted giving appropriate 3-oxo-γ-carbolines. Condensation with 2-chlorobenzaldehyde under microwave irradiation gave a 4-(2-chlorobenzyl)-3-oxo-γ-carboline. N-methylation lead to a product with very promising antifungal and cytotoxic activities. Full article
188 KiB  
Article
New Substituted Isocoumarins and Dihydroisocoumarins and their Cytotoxic Activities
by Veronika Hampl, Isolde Wetzel, Franz Bracher and Jürgen KRAUSS
Sci. Pharm. 2011, 79(1), 21-30; https://doi.org/10.3797/scipharm.1011-10 - 18 Dec 2010
Cited by 10 | Viewed by 1488
Abstract
New isocoumarins were prepared in an efficient way from 2-iodobenzoic acid derivatives and hept-1-yne in a Sonogashira reaction, followed by spontaneous cyclization. Catalytic hydrogenation gave the corresponding dihydroisocoumarins. A 4-chloroisocoumarin was prepared on an alternative pathway. Some of the new compounds showed moderate [...] Read more.
New isocoumarins were prepared in an efficient way from 2-iodobenzoic acid derivatives and hept-1-yne in a Sonogashira reaction, followed by spontaneous cyclization. Catalytic hydrogenation gave the corresponding dihydroisocoumarins. A 4-chloroisocoumarin was prepared on an alternative pathway. Some of the new compounds showed moderate cytotoxic activities against a human leukemia cell line (HL 60). Full article
272 KiB  
Article
Preparation of Mucoadhesive Oral Patches Containing Tetracycline Hydrochloride and Carvacrol for Treatment of Local Mouth Bacterial Infections and Candidiasis
by Rana M. OBAIDAT, Ammar BADER, Wafa AL-RAJAB, Ghassan ABU SHEIKHA and Aiman A. OBAIDAT
Sci. Pharm. 2011, 79(1), 197-212; https://doi.org/10.3797/scipharm.1004-18 - 14 Dec 2010
Cited by 40 | Viewed by 2336
Abstract
The specific aim of this work was to prepare mucoadhesive patches containing tetracycline hydrochloride and carvacrol in an attempt to develop a novel oral drug delivery system for the treatment of mouth infections. The bilayered patches were prepared using ethyl cellulose as a [...] Read more.
The specific aim of this work was to prepare mucoadhesive patches containing tetracycline hydrochloride and carvacrol in an attempt to develop a novel oral drug delivery system for the treatment of mouth infections. The bilayered patches were prepared using ethyl cellulose as a backing layer and carbopol 934 as a matrix mucoadhesive layer. Patches were prepared with different loading amounts of tetracycline hydrochloride and carvacrol. The antimicrobial activity was assessed for the prepared patches using the disc-diffusion method against the yeast Candida albicans and five bacterial strains, including Pseudomonas aeruginosa, Escherichia coli, Bacillus cereus, Staphylococcus aureus, and Bacillus bronchispti. In this work, we highlighted the possibility of occurrence of a synergistic action between carvacrol and tetracycline. The best formulation was selected based on microbiological tests, drug release, ex-vivo mucoadhesive performance, and swelling index. Physical characteristics of the selected formulations were determined. These included pH, patch thickness, weight uniformity, content uniformity, folding endurance, and patch stability. Full article
542 KiB  
Article
Optimization, Characterisation and Pharmacokinetic Studies of Mucoadhesive Oral Multiple Unit Systems of Ornidazole
by Govind S. ASANE, Yamsani Madhusudan RAO, Jaykrishna H. BHATT and Karimunnisa S. SHAIKH
Sci. Pharm. 2011, 79(1), 181-196; https://doi.org/10.3797/scipharm.1003-03 - 2 Dec 2010
Cited by 7 | Viewed by 1410
Abstract
The objective of the present study was to investigate the applicability of matrix type mucoadhesive oral multiple unit systems (MUS) for sustaining the release of ornidazole in the gastrointestinal tract (GIT).The MUS were prepared by ionotropic gelation method using chitosan and hydroxypropyl methyl [...] Read more.
The objective of the present study was to investigate the applicability of matrix type mucoadhesive oral multiple unit systems (MUS) for sustaining the release of ornidazole in the gastrointestinal tract (GIT).The MUS were prepared by ionotropic gelation method using chitosan and hydroxypropyl methyl cellulose K4M (HPMC K4M) according to 32 factorial designs and were evaluated in vitro and in vivo. The particle size length ranged from 0.78 to 1.30 mm and breadth from 0.76 to 1.30 mm, respectively. The entrapment efficiency was in range of 80 to 96%. The rapid wash-off test was observed faster at intestinal pH 6.8 as compared to acidic pH 1.2. The fluoroscopic study revealed the retention of MUS in GIT for more than 5 hours. The pharmacokinetic parameters Cmax, Tmax, mean residence time (MRT) and area under curve (AUC) of developed MUS were found to be improved significantly (p<0.05) when compared with marketed immediate release tablets each containing 500 mg of drug. This study demonstrates that the MUS could be a good alternative to immediate release tablets to deliver ornidazole and expected to be less irritant to gastric and intestinal mucosa. Full article
6201 KiB  
Article
Anatomy of Subterranean Organs of Medicinally Used Cardueae and Related Species and its Value for Discrimination
by Elisabeth FRITZ and Johannes SAUKEL
Sci. Pharm. 2011, 79(1), 157-174; https://doi.org/10.3797/scipharm.1010-05 - 2 Dec 2010
Cited by 9 | Viewed by 1481
Abstract
Numerous species of the Asteraceae, the composites, are famous for their use in both traditional and conventional medicine. Reliable anatomical descriptions of these plants and of possible adulterations provide a basis for fast identification and cheap purity controls of respective medicinal drugs by [...] Read more.
Numerous species of the Asteraceae, the composites, are famous for their use in both traditional and conventional medicine. Reliable anatomical descriptions of these plants and of possible adulterations provide a basis for fast identification and cheap purity controls of respective medicinal drugs by means of light microscopy. Nevertheless, detailed comparative studies on root and rhizome anatomy of valuable as well as related inconsiderable composite plants are largely missing yet. The presented study aims to narrow this gap by performing anatomical analyses of roots and rhizomes of 16 species belonging to the tribe Cardueae, of formerly and currently used drugs as well as their near relatives as potential adulterations (Carlina acaulis L., Carlina vulgaris L., Arctium lappa L., Arctium tomentosum Mill., Carduus defloratus L., Carduus personata (L.) Jacq, Cirsium arvense (L.) Scop., Cirsium vulgare (Savi) Ten., Cirsium erisithales (Jacq.) Scop., Onopordum acanthium L., Silybum marianum (L.) Gaertn., Rhaponticum scariosum Lam., Centaurea jacea L., Centaurea scabiosa L., Centaurea cyanus L., Cnicus benedictus L.). A detailed verbal and graphical survey of the analysed anatomical features is provided. Several characters were finally extracted which allow for discrimination of the examined species and may be effectively used for drug quality controls. Full article
289 KiB  
Article
Chemometric QSAR Modeling and In Silico Design of Antioxidant NO Donor Phenols
by Indrani MITRA, Achintya SAHA and Kunal ROY
Sci. Pharm. 2011, 79(1), 31-58; https://doi.org/10.3797/scipharm.1011-02 - 2 Dec 2010
Cited by 29 | Viewed by 1457
Abstract
An acceleration of free radical formation within human system exacerbates the incidence of several life-threatening diseases. The systemic antioxidants often fall short for neutralizing the free radicals thereby demanding external antioxidant supplementation. Therein arises the need for development of new antioxidants with improved [...] Read more.
An acceleration of free radical formation within human system exacerbates the incidence of several life-threatening diseases. The systemic antioxidants often fall short for neutralizing the free radicals thereby demanding external antioxidant supplementation. Therein arises the need for development of new antioxidants with improved potency. In order to search for efficient antioxidant molecules, the present work deals with quantitative structure-activity relationship (QSAR) studies of a series of antioxidants belonging to the class of phenolic derivatives bearing NO donor groups. In this study, several QSAR models with appreciable statistical significance have been reported. Models were built using various chemometric tools and validated both internally and externally. These models chiefly infer that presence of substituted aromatic carbons, long chain branched substituents, an oxadiazole-N-oxide ring with an electronegative atom containing group substituted at the 5 position and high degree of methyl substitutions of the parent moiety are conducive to the antioxidant activity profile of these molecules. The novelty of this work is not only that the structural attributes of NO donor phenolic compounds required for potent antioxidant activity have been explored in this study, but new compounds with possible antioxidant activity have also been designed and their antioxidant activity has been predicted in silico. Full article
575 KiB  
Article
Preparation of Herbal Tea as Infusion or by Maceration at Room Temperature Using Mistletoe Tea as an Example
by Sebastian JÄGER, Markus BEFFERT, Katharina HOPPE, Dominik NADBEREZNY, Bruno FRANK and Armin SCHEFFLER
Sci. Pharm. 2011, 79(1), 145-156; https://doi.org/10.3797/scipharm.1006-06 - 30 Nov 2010
Cited by 23 | Viewed by 3412
Abstract
Herbal tea can be prepared by infusion or maceration at room temperature resulting in different compositions of extractable constituents, which possibly influences the mode of action or safety profile. Knowledge on this topic is limited. The aim of this study was to investigate [...] Read more.
Herbal tea can be prepared by infusion or maceration at room temperature resulting in different compositions of extractable constituents, which possibly influences the mode of action or safety profile. Knowledge on this topic is limited. The aim of this study was to investigate the substantial differences between infusion and maceration as recommended preparation methods for the preparation of herbal mistletoe tea, a traditional remedy against cardiovascular diseases. No active substances are known but analytical marker substances such as proteins, triterpenoids, phenylpropane derivatives and flavonoids can be quantified within the herb and the different herbal tea preparations. Whereas phenylpropane derivatives were completely extracted by infusion and maceration, neither method dissolved viscotoxins. 43% of mistletoe lectins were extracted by maceration, whereas by infusion they are inactivated by thermal degradation. By contrast, oleanolic acid and betulinic acid are present in higher concentrations in infusates compared with macerates, but even infusion extracted less than 2%. Infusion extracted 43% of flavonoid-like substances and maceration only 31%. In conclusion this study determines some differences between both extraction methods on the profile of solved substances. The relevance of it should be determined in studies dealing with the efficacy of herbal mistletoe tea. Full article
228 KiB  
Article
Formulation and Bioequivalence of Two Valsartan Tablets After a Single Oral Administration
by Abdel Naser ZAID, Rita CORTESI, Aiman QADDOMI and Saed KHAMMASH
Sci. Pharm. 2011, 79(1), 123-136; https://doi.org/10.3797/scipharm.1009-01 - 20 Nov 2010
Cited by 17 | Viewed by 2901
Abstract
The aim of this study is to assess the quality of Valzan® tablet (160 mg, valsartan immediate release test formulation) by comparing its pharmacokinetic parameters with Diovan® tablet (160 mg, valsartan reference formulation). Valzan® tablets were prepared according to a [...] Read more.
The aim of this study is to assess the quality of Valzan® tablet (160 mg, valsartan immediate release test formulation) by comparing its pharmacokinetic parameters with Diovan® tablet (160 mg, valsartan reference formulation). Valzan® tablets were prepared according to a dry granulation method (roll compaction). To assess the bioequivalence of Valzan® tablets a randomized, two-way, crossover, bioequivalence study was performed in 24 healthy male volunteers. The selected volunteers were divided into two groups of 12 subjects. One group was treated with the reference formulation (Diovan®) and the other one with the generic Valzan®, with a cross-over after the drug washout period of 14 days. Blood samples were collected at fixed time intervals and valsartan concentrations were determined by a validated HPLC assay method. The pharmacokinetic parameters AUC0–48, AUC0–∞, Cmax, Tmax, Ke and T1/2 were determined for both the tablets and were compared statistically to evaluate the bioequivalence between the two brands of valsartan, using the statistical model recommended by the FDA. The analysis of variance (ANOVA) did not show any significant difference between the two formulations and 90% confidence intervals (CI) fell within the acceptable range for bioequivalence. Based on this statistical evaluation it was concluded that the test tablets (Valzan®) is well formulated, since it exhibits pharmacokinetic profile comparable to the reference brand Diovan®. Full article
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