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Sci. Pharm.
Volume 78
Issue 4
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Sci. Pharm., Volume 78, Issue 4 (December 2010) – 17 articles , Pages 745-998

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7 pages, 206 KiB  
Article
Synthesis and Antimicrobial Activity of Long-Chain 3,4-Epoxy-2-alkanones
by William F. WOOD
Department of Chemistry, Humboldt State University, 1 Harpst St., Arcata, California, 95521, U.S.A.
Sci. Pharm. 2010, 78(4), 745-752; https://doi.org/10.3797/scipharm.1009-02 - 9 Oct 2010
Viewed by 1620
Abstract
3,4-Epoxy-2-dodecanone, a major component in the preorbital gland of the African grey duiker (Sylvicapra grimmia), showed antimicrobial activity in preliminary tests. The C11 to C17 homologues of this compound were prepared and their activity against several pathogenic dermal bacteria [...] Read more.
3,4-Epoxy-2-dodecanone, a major component in the preorbital gland of the African grey duiker (Sylvicapra grimmia), showed antimicrobial activity in preliminary tests. The C11 to C17 homologues of this compound were prepared and their activity against several pathogenic dermal bacteria and fungi was tested. 3,4-Epoxy-2-dodecanone and 3,4-epoxy-2-tridecanone inhibited the growth of Trichophyton mentagrophytes at 25 μg/mL. Moderate inhibition of the growth of the bacteria Propionibacterium acnes and the lipophilic yeast, Pityrosporum ovale, was seen for several of the homologues. Full article
13 pages, 300 KiB  
Article
New 4-Thiazolidinones of Nicotinic Acid with 2-Amino-6-methylbenzothiazole and their Biological Activity
by Navin B. PATEL * and Faiyazalam M. SHAIKH
Department of Chemistry, Veer Narmad South Gujarat University, Surat 395007, Gujarat, India
Sci. Pharm. 2010, 78(4), 753-766; https://doi.org/10.3797/scipharm.1009-15 - 24 Oct 2010
Cited by 46 | Viewed by 2122
Abstract
The title compounds 6a–j, 2-[(6-methyl-1,3-benzothiazol-2-yl)amino]-N- [2-(substituted phenyl/furan-2-yl)-4-oxo-1,3-thiazolidin-3-yl]nicotinamides, were prepared from 2-chloropyridine-3-carboxylic acid (1) and 2-amino-6-methylbenzothiazole (2) by known methods. All the compounds have been established by IR, 1H NMR, 13C NMR and elemental analyses. [...] Read more.
The title compounds 6a–j, 2-[(6-methyl-1,3-benzothiazol-2-yl)amino]-N- [2-(substituted phenyl/furan-2-yl)-4-oxo-1,3-thiazolidin-3-yl]nicotinamides, were prepared from 2-chloropyridine-3-carboxylic acid (1) and 2-amino-6-methylbenzothiazole (2) by known methods. All the compounds have been established by IR, 1H NMR, 13C NMR and elemental analyses. The in vitro antimicrobial screening of the compounds were carried out against two Gram positive (S. aureus, S. pyogenes), two Gram negative (E. coli, P. aeruginosa) bacteria and three fungal species (C. albicans, A. niger, A. clavatus) using the broth microdilution method. Some of the compounds are comparable with standard drugs. Full article
23 pages, 453 KiB  
Article
Synthesis, Photochemical and Photoinduced Antibacterial Activity Studies of meso-Tetra(pyren-1-yl)porphyrin and its Ni, Cu and Zn Complexes
by Tamara ZOLTAN 1,*, Franklin VARGAS 1, Carlos RIVAS 1, Verónica LÓPEZ 1, Jhackelym PEREZ 1 and Antonio BIASUTTO 2
1 Laboratorio de Fotoquímica, Centro de Química, Instituto Venezolano de Insvestigaciones Científicas, I.V.I.C., Apartado 21827, Caracas 1020-A, Venezuela
2 Universidad de Carabobo, Facultad Experimental de Ciencia y Tecnología, Escuela de Química, Valencia, Edo. Carabobo, Venezuela
Sci. Pharm. 2010, 78(4), 767-790; https://doi.org/10.3797/scipharm.1003-13 - 7 Aug 2010
Cited by 28 | Viewed by 2010
Abstract
The synthesis of the meso-tetra(pyren-1-yl)porphyrin (1) was successfully accomplished by means of the pyrrole condensation with pyrene-1-carbaldehyde in acidic media. Its metallization was carried out in an almost quantitative yield to obtain the corresponding complexes of Ni(II) (2), [...] Read more.
The synthesis of the meso-tetra(pyren-1-yl)porphyrin (1) was successfully accomplished by means of the pyrrole condensation with pyrene-1-carbaldehyde in acidic media. Its metallization was carried out in an almost quantitative yield to obtain the corresponding complexes of Ni(II) (2), Cu(II) (3) and Zn (4). Their photophysical properties such as fluorescence quantum yield and energy transfer to oxygen for an efficient generation of singlet oxygen were determined. Their photophysical and photochemical properties were compared with those of other similar porphyrin derivatives such as tetraphenylporphyrin and tetranaphthylporphyrin. Photochemical studies on their effectiveness as photosensitizer were carried out by means of the photoinduced oxidation of aromatic alcohols like α-naphthol to naphthoquinone. The antibacterial photoactivity assay for compounds 1–4 was testeted against Escherichia coli (ATCC 8739) and its proliferation and viability were measured by chemiluminescence. An efficient inactivation of E. coli was observed. This was more efficient for compounds 2 and 3, following the direct relationship to high generation of singlet oxygen by these compounds. Full article
30 pages, 394 KiB  
Article
Models for Antitubercular Activity of 5'-O-[(N-Acyl)sulfamoyl]adenosines
by Rakesh K. GOYAL 1, Harish DUREJA 2, Gajendra SINGH 1 and Anil Kumar MADAN 1,*
1 Faculty of Pharmaceutical Sciences, Pt. B.D. Sharma University of Health Sciences, Rohtak,124 001, India
2 Faculty of Pharmaceutical Sciences, M. D. University, Rohtak, 124 001, India
Sci. Pharm. 2010, 78(4), 791-820; https://doi.org/10.3797/scipharm.1006-03 - 13 Aug 2010
Cited by 9 | Viewed by 1384
Abstract
The relationship between topological indices and antitubercular activity of 5'-O- [(N-Acyl)sulfamoyl]adenosines has been investigated. A data set consisting of 31 analogues of 5'-O-[(N-Acyl)sulfamoyl]adenosines was selected for the present study. The values of numerous topostructural and [...] Read more.
The relationship between topological indices and antitubercular activity of 5'-O- [(N-Acyl)sulfamoyl]adenosines has been investigated. A data set consisting of 31 analogues of 5'-O-[(N-Acyl)sulfamoyl]adenosines was selected for the present study. The values of numerous topostructural and topochemical indices for each of 31 differently substituted analogues of the data set were computed using an in-house computer program. Resulting data was analyzed and suitable models were developed through decision tree, random forest and moving average analysis (MAA). The goodness of the models was assessed by calculating overall accuracy of prediction, sensitivity, specificity and Mathews correlation coefficient. Pendentic eccentricity index – a novel highly discriminating, non-correlating pendenticity based topochemical descriptor – was also conceptualized and successfully utilized for the development of a model for antitubercular activity of 5'-O-[(N-Acyl)sulfamoyl]adenosines. The proposed index exhibited not only high sensitivity towards both the presence as well as relative position(s) of pendent/heteroatom(s) but also led to significant reduction in degeneracy. Random forest correctly classified the analogues into active and inactive with an accuracy of 67.74%. A decision tree was also employed for determining the importance of molecular descriptors. The decision tree learned the information from the input data with an accuracy of 100% and correctly predicted the cross-validated (10 fold) data with accuracy up to 77.4%. Statistical significance of proposed models was also investigated using intercorrelation analysis. Accuracy of prediction of proposed MAA models ranged from 90.4 to 91.6%. Full article
14 pages, 281 KiB  
Article
Simultaneous Quantitative Determination of Metoprolol, Atorvastatin and Ramipril in Capsules by a Validated Stability-Indicating RP-UPLC Method
by Raja Kumar SESHADRI 1,*, Makarand Madhukar DESAI 1, Thummala Veera RAGHAVARAJU 1, Deepa KRISHNAN 1, Dama Venugopala RAO 1 and Ivon Elisha CHAKRAVARTHY 2
1 Analytical Research and Development, Integrated Product Development, Dr. Reddy’s Laboratories Ltd., Bachupally, Hyderabad-500 072, India
2 Department of Chemistry, Rayalaseema University, Kurnool-518002, A.P., India
Sci. Pharm. 2010, 78(4), 821-834; https://doi.org/10.3797/scipharm.1004-14 - 24 Aug 2010
Cited by 33 | Viewed by 3005
Abstract
A simple ultra performance liquid chromatographic (UPLC) method has been developed for the simultaneous estimation of Metoprolol (MT), Atorvastatin (AT) and Ramipril (RM) from capsule dosage form. The method was developed using Zorbax® XDB-C18 (4.6 mm x 50 mm, 1.8 μm) column with [...] Read more.
A simple ultra performance liquid chromatographic (UPLC) method has been developed for the simultaneous estimation of Metoprolol (MT), Atorvastatin (AT) and Ramipril (RM) from capsule dosage form. The method was developed using Zorbax® XDB-C18 (4.6 mm x 50 mm, 1.8 μm) column with a mobile phase consisting of 0.06% ortho phosphoric acid in Milli Q® water having an ion pair reagent, 0.0045 M Sodium lauryl sulphate as buffer, at ratio of buffer: Acetonitrile (50:50 v/v), at 55°C column temperature with a flow rate of 1.0 ml/min. Detection was carried out with ultra-violet detection at 210 nm for RM, MT and AT respectively. The retention times were about 1.3, 2.1 and 2.6 min for MT, AT and RM respectively, the method was validated for linearity, accuracy, precision, specificity, robustness and ruggedness. The % mean recoveries are 101.9, 102.1 and 101.4 for MT, AT and RM respectively. The method was found to be rugged and robust and can be successfully used to determine the three drugs and its combinations. Full article
12 pages, 319 KiB  
Article
Determination of Residual Epichlorohydrin in Sevelamer Hydrochloride by Static Headspace Gas Chromatography with Flame Ionization Detection
by Kaliaperumal KARTHIKEYAN 1,2,*, Govindasamy T. ARULARASU 1, Perumalsamy DEVARAJ 1 and Karnam Chandrasekara PILLAI 2
1 Analytical Development, Shasun Research Center, 27, Vandalur Kelambakkam Road, Keelakottaiyur, Chennai 600048, India
2 Department of Physical Chemistry, University of Madras, Guindy Campus, Chennai 600025, India
Sci. Pharm. 2010, 78(4), 835-846; https://doi.org/10.3797/scipharm.1007-20 - 26 Sep 2010
Cited by 7 | Viewed by 2932
Abstract
A sensitive static headspace gas chromatographic method was developed and validated for the determination of residual epichlorohydrin (ECH) in sevelamer hydrochloride (SVH) drug substance. This method utilized a Phenomenex Zebron ZB-WAX GC column, helium as carrier gas with flame ionization detection. The critical [...] Read more.
A sensitive static headspace gas chromatographic method was developed and validated for the determination of residual epichlorohydrin (ECH) in sevelamer hydrochloride (SVH) drug substance. This method utilized a Phenomenex Zebron ZB-WAX GC column, helium as carrier gas with flame ionization detection. The critical experimental parameters, such as, headspace vial incubation time and incubation temperature were studied and optimized. The method was validated as per United States Pharmacopoeia (USP) and International Conference on Harmonization (ICH) guidelines in terms of detection limit (DL), quantitation limit (QL), linearity, precision, accuracy, specificity and robustness. A linear range from 0.30 to 10 μg/mL was obtained with the coefficient of determination (r2) 0.999. The DL and QL of ECH were 0.09 μg/mL and 0.30 μg/mL, respectively. The recovery obtained for ECH was between 91.7 and 96.6%. Also, the specificity of the method was proved through gas chromatography mass spectrometry (GC-MS). This method was applied successfully to determine the content of residual ECH in SVH bulk drug. Full article
10 pages, 222 KiB  
Article
Sensitive and Rapid HPLC Method for Determination of Memantine in Human Plasma Using OPA Derivatization and Fluorescence Detection: Application to Pharmacokinetic Studies
by Afshin ZARGHI 1,*, Alireza SHAFAATI 1, Seyed Mohsen FOROUTAN 2, Arash KHODDAM 3 and Babak MADADIAN 3
1 Department of Pharmaceutical Chemistry, School of Pharmacy, Shahid Beheshti University of Medical Sciences, Tehran, Iran
2 Department of Pharmaceutics, School of Pharmacy, Shahid Beheshti University of Medical Sciences, Tehran, Iran
3 Noor Research and Educational Institute, Tehran, Iran
Sci. Pharm. 2010, 78(4), 847-856; https://doi.org/10.3797/scipharm.1008-17 - 5 Oct 2010
Cited by 26 | Viewed by 2998
Abstract
A rapid, sensitive and reproducible HPLC method was developed and validated for the analysis of memantine in human plasma after derivatization with o-phthaldialdehyde (OPA) and fluorescence detection. Amantadine was used as internal standard. The derivatized memantine and amantadine were eluted in less [...] Read more.
A rapid, sensitive and reproducible HPLC method was developed and validated for the analysis of memantine in human plasma after derivatization with o-phthaldialdehyde (OPA) and fluorescence detection. Amantadine was used as internal standard. The derivatized memantine and amantadine were eluted in less than 10 min with no interference from endogenous plasma peaks. The analysis was carried out on a monolithic silica column (Chromolith Performance RP-18e, 100×4.6 mm). The mobile phase was composed of a mixture of acetonitrile and 0.025 M phosphate buffer (50:50, v/v, pH=4.6) with a flow rate of 2.5 mLmin−1. The excitation and emission wavelengths were set at 335 nm and 440 nm respectively. The assay enables the measurement of memantine for therapeutic drug monitoring with a lower quantification limit of 2 ngmL−1. The method involves simple extraction procedure and analytical recovery was 82.8± 0.9%. The calibration curve was linear over the concentration range 2–80 ngmL−1. The coefficients of variation for inter-day and intra-day assay were found to be less than 8%. The method was successfully applied to pharmacokinetic studies in humans. Full article
12 pages, 226 KiB  
Article
Development and Validation of a Stability-Indicating RP-HPLC Method for Duloxetine Hydrochloride in its Bulk and Tablet Dosage Form
by Usmangani K. CHHALOTIYA *, Kashyap K. BHATT, Dimal A. SHAH and Sunil L. BALDANIA
Indukaka Ipcowala College of Pharmacy, Beyond GIDC Phase IV, Vithal Udyognagar, New Vallabh Vidyanagar-388121, Anand, Gujarat, India
Sci. Pharm. 2010, 78(4), 857-868; https://doi.org/10.3797/scipharm.1009-11 - 25 Oct 2010
Cited by 29 | Viewed by 2408
Abstract
The objective of the present work was to develop a stability-indicating RP-HPLC method for duloxetine hydrochloride (DUL) in the presence of its degradation products generated from forced decomposition studies. The drug substance was found to be susceptible to stress conditions of acid hydrolysis. [...] Read more.
The objective of the present work was to develop a stability-indicating RP-HPLC method for duloxetine hydrochloride (DUL) in the presence of its degradation products generated from forced decomposition studies. The drug substance was found to be susceptible to stress conditions of acid hydrolysis. The drug was found to be stable to dry heat, photodegradation, oxidation and basic condition attempted. Successful separation of the drug from the degradation products formed under acidic stress conditions was achieved on a Hypersil C-18 column (250 mm X 4.6 mm id, 5μm particle size) using acetonitrile: 0.01 M potassium dihydrogen phosphate buffer (pH 5.4 adjusted with orthophosphoric acid) (50:50, v/v) as the mobile phase at a flow rate of 1.0 ml/min. Quantification was achieved with photodiode array detection at 229 nm over the concentration range 1–25 μg/ml with range of recovery 99.8–101.3 % for DUL by the RP-HPLC method. Statistical analysis proved the method to be repeatable, specific, and accurate for estimation of DUL. It can be used as a stabilityindicating method due to its effective separation of the drug from its degradation products. Full article
12 pages, 375 KiB  
Article
Interaction of Bioactive Coomassie Brilliant Blue G with Protein: Insights from Spectroscopic Methods
by Umesha KATRAHALLI, Shankara Sharanappa KALANUR and Jaladappagari SEETHARAMAPPA *
Department of Chemistry, Karnatak University, Dharwad 580 003, India
Sci. Pharm. 2010, 78(4), 869-880; https://doi.org/10.3797/scipharm.1008-15 - 6 Nov 2010
Cited by 32 | Viewed by 2782
Abstract
The binding of coomassie brilliant blue G (CBB) to bovine serum albumin (BSA) was investigated under simulative physiological conditions employing different optical spectroscopic techniques viz., fluorescence emission, UV–visible absorption and FTIR. Fluorescence quenching data obtained at different temperatures suggested the presence of [...] Read more.
The binding of coomassie brilliant blue G (CBB) to bovine serum albumin (BSA) was investigated under simulative physiological conditions employing different optical spectroscopic techniques viz., fluorescence emission, UV–visible absorption and FTIR. Fluorescence quenching data obtained at different temperatures suggested the presence of dynamic type of quenching mechanism. The binding constant of CBB-BSA and the number of binding sites (n) for CBB in BSA were calculated and found to be 4.20 x 104 M−1 and 0.96 respectively, at 302 K. The value of n close to unity indicated that the protein has a single class of binding sites for CBB. The thermodynamic parameters revealed that the hydrophobic forces played a major role in the interaction of CBB to BSA. The distance between the CBB and protein was calculated using the theory of Föster’s Resonance Energy Transfer (FRET). The conformational change in the secondary structure of BSA upon interaction with dye was investigated by synchronous fluorescence and FTIR techniques. Competitive binding studies were also carried out to know the location of binding of CBB on BSA. Full article
16 pages, 903 KiB  
Article
Protective Effect of L-Carnitine and Coenzyme Q10 on CCl4-Induced Liver Injury in Rats
by Sanaa Ahmed ALI 1,*, Lilla FADDAH 2, Ateff ABDEL-BAKY 3 and Asmaa BAYOUMI 3
1 National Research Centre, El-Behooth St. 12622 Dokki, Giza, Cairo, Egypt
2 King Saud University, KSA, 11495 Ryad, Zip code 22480, Saudi Arabia
3 El-Minia University, Faculty of Pharmacy, Salah Salem St. 61519, Egypt
Sci. Pharm. 2010, 78(4), 881-896; https://doi.org/10.3797/scipharm.1006-02 - 23 Aug 2010
Cited by 52 | Viewed by 2357
Abstract
This study provides an information about the mechanisms of liver injury induced by CCl4, and determines the influence of administration of L-carnitine or/and CoQ10 as prophylactic agents against CCl4 deteriorative effect. The study was carried out on 80 adult male albino rats divided [...] Read more.
This study provides an information about the mechanisms of liver injury induced by CCl4, and determines the influence of administration of L-carnitine or/and CoQ10 as prophylactic agents against CCl4 deteriorative effect. The study was carried out on 80 adult male albino rats divided into eight groups, 10 animals each, as follows: four normal groups (control, treated with L-carnitine, treated with CoQ10, and treated with a combination of Lcarnitine and CoQ10) and four liver injury groups treated with CCl4 (control, treated with L-carnitine, treated with CoQ10, and treated with a combination of L-carnitine and CoQ10). Liver injury was induced by s.c. injection of a single dose of CCl4 (1 ml/kg). L-carnitine (50 mg/kg/day) was given i.p. for four successive days 24 hours before CCl4 injection, and CoQ10 (200 mg/kg) was given as a single i.p. dose 24 hours before CCl4 injection. Animals were sacrificed 24 hours after CCl4 injection, blood samples were withdrawn and liver tissue samples were homogenized. The levels of the following parameters were determined: hepatic reduced glutathione, serum ALT and AST, hepatic lipid peroxides, hepatic vitamin C, hepatic and serum total protein, serum albumin, serum sialic acid, serum nitrite, and serum and hepatic total LDH activities and LDH isoenzymes. The obtained data revealed that CCl4 injection produced a significant decrease in reduced glutathione content, vitamin C, total protein and albumin levels. However, there was a significant increase in serum ALT and AST activities, lipid peroxides, sialic acid, nitric oxide, serum and hepatic total LDH activities. On the other hand, groups treated with L-carnitine or/and CoQ10 prior to CCl4 injection showed an improvement in most parameters when compared with cirrhotic control group. It has been concluded that L-carnitine and coenzyme Q10 have a pronounced prophylactic effect against liver damage induced by halogenated alkanes such as carbon tetrachloride. Full article
11 pages, 241 KiB  
Article
Polyphenols from Ginkgo biloba
by Fadi QA’DAN 1,*, Adolf NAHRSTEDT 2, Mathias SCHMIDT 3 and Kenza MANSOOR 4
1 Faculty of Pharmacy, Petra University, Airport Street, P O Box 961343 Amman, Jordan
2 Institut fuer pharmazeutische Biologie und Phytochemie, Hittorfstrasse 56, D-48149 Muenster, Germany
3 HerbResearch, Wartbergweg 15, D-86874 Mattsies, Germany
4 School of Pharmacy, Al-Ahliyya Amman University: Amman-19328, Jordan
Sci. Pharm. 2010, 78(4), 897-908; https://doi.org/10.3797/scipharm.1003-19 - 28 Oct 2010
Cited by 23 | Viewed by 1863
Abstract
By Sephadex LH-20 gel chromatography of an extract from Gingko biloba leaves, polymeric proanthocyanidins were eluted after the fractions of flavonol glycosides and biflavone glycosides. A purified proanthocyanidin polymer accounted for 86.6% of the total proanthocyanidins, and for 37.7% of the total antioxidant [...] Read more.
By Sephadex LH-20 gel chromatography of an extract from Gingko biloba leaves, polymeric proanthocyanidins were eluted after the fractions of flavonol glycosides and biflavone glycosides. A purified proanthocyanidin polymer accounted for 86.6% of the total proanthocyanidins, and for 37.7% of the total antioxidant activity of this leaf extract. For structure elucidation, the polymer was submitted to acidic depolymerization in the presence of phloroglucinol. The structures of the resulting flavan-3-ols and phloroglucinol adducts were determined on the basis of 1D-and reverse 2D-NMR (HSQC, HMBC) spectra of their peracetylated derivatives, MALDI-TOF-MS and CD-spectroscopy. The observations resulting from the degradation with phloroglucinol were confirmed by 13C-NMR spectroscopy of the polymer. The mean molecular weight of the polymeric fraction was estimated to be 9–10 flavan-3-ol-units. Full article
17 pages, 1406 KiB  
Article
Development and Evaluation of Cefadroxil Drug Loaded Biopolymeric Films Based on Chitosan-Furfural Schiff Base
by Ritu B. DIXIT 1,*, Rahul A. UPLANA 1, Vishnu A. PATEL 2, Bharat C. DIXIT 3 and Tarosh S. PATEL 3
1 Ashok & Rita Patel Institute of Integrated Study & Research in Biotechnology and Allied Sciences, New Vallabh Vidyanagar-388121, India
2 Department of Pharmaceutics, A. R. College of Pharmacy, Vallabh Vidyanagar-388120, India
3 Department of Chemistry, V. P. & R. P. T. P. Science College, Vallabh Vidyanagar-388120, India
Sci. Pharm. 2010, 78(4), 909-926; https://doi.org/10.3797/scipharm.0912-20 - 26 Sep 2010
Cited by 6 | Viewed by 1780
Abstract
Cefadroxil drug loaded biopolymeric films of chitosan-furfural schiff base were prepared by reacting chitosan with furfural in presence of acetic acid and perchloric acid respectively for the external use. Prepared films were evaluated for their strength, swelling index, thickness, drug content, uniformity, tensile [...] Read more.
Cefadroxil drug loaded biopolymeric films of chitosan-furfural schiff base were prepared by reacting chitosan with furfural in presence of acetic acid and perchloric acid respectively for the external use. Prepared films were evaluated for their strength, swelling index, thickness, drug content, uniformity, tensile strength, percent elongation, FTIR spectral analysis and SEM. The results of in vitro diffusion studies revealed that the films exhibited enhanced drug diffusion as compared to the films prepared using untreated chitosan. The films also demonstrated good to moderate antibacterial activities against selective gram positive and gram negative bacteria. Full article
13 pages, 250 KiB  
Article
Floating Matrix Dosage Form for Propranolol Hydrochloride Based on Gas Formation Technique: Development and In Vitro Evaluation
by Kiran CHATURVEDI 1,*, S. UMADEVI 1 and Subhash VAGHANI 2
1 P. E. S. College of Pharmacy, Bangalore, India
2 Smt. R. B. Patel Mahila Pharmacy College, Atkot, Gujarat, India
Sci. Pharm. 2010, 78(4), 927-940; https://doi.org/10.3797/scipharm.0909-02 - 26 Sep 2010
Cited by 40 | Viewed by 2170
Abstract
Gastroretentive tablets of propranolol hydrochloride were developed by direct compression method using citric acid and sodium bicarbonate as the effervescent base. Hydroxypropyl methylcellulose; HPMC K15M was used to prepare the floating tablets to retard the drug release for 12h in stomach. Na-carboxymethyl cellulose [...] Read more.
Gastroretentive tablets of propranolol hydrochloride were developed by direct compression method using citric acid and sodium bicarbonate as the effervescent base. Hydroxypropyl methylcellulose; HPMC K15M was used to prepare the floating tablets to retard the drug release for 12h in stomach. Na-carboxymethyl cellulose (NaCMC) or carbopol 934P was added to alter the drug release profile or the dimensional stability of the formulation. Dicalcium phosphate (DCP) was used as filler. Formulations were evaluated for floating lag time, duration of floating, dimensional stability, drug content and in vitro drug release profile. The formulations were found to have floating lag time less than 1min. It was found that the dimensional stability of the formulations increase with increasing concentration of the swelling agent. The release mechanism of propranolol hydrochloride from floating tablets was evaluated on the basis of Peppas and Higuchi model. The ‘n’ value of the formulations ranged from 0.5201 to 0.7367 (0.5<n<1.0) which indicated anomalous (non-Fickian) transport mechanism. Formulation containing 27.5% HPMC K15M, 29% DCP, 3.75% citric acid and 18.75% sodium bicarbonate seemed most desirable. FTIR, DSC and XRPD studies indicated the absence of any significant chemical interaction within dug and excipients. Stability study of optimized formulation revealed no significant change and found to be stable. Full article
17 pages, 564 KiB  
Article
Sodium Alginate Based Mucoadhesive System for Gatifloxacin and Its In Vitro Antibacterial Activity
by Karthikeyan KESAVAN 1,*, Gopal NATH 2 and Jayanta K. PANDIT 1
1 Department of Pharmaceutics, Institute of Technology, Banaras Hindu University, Varanasi, Uttar Pradesh – 221 005, India
2 Department of Microbiology, Institute of Medical Science, Banaras Hindu University, Varanasi, Uttar Pradesh – 221 005, India
Sci. Pharm. 2010, 78(4), 941-958; https://doi.org/10.3797/scipharm.1004-24 - 26 Sep 2010
Cited by 78 | Viewed by 2534
Abstract
The objective of this study was to formulate sodium alginate based ophthalmic mucoadhesive system of gatifloxacin and its in vitro antibacterial potential on pathogenic microorganisms, Staphylococcus aureus and Escherichia coli. Sodium carboxymethylcellulose (NaCMC) was added to the formulations to enhance the gel [...] Read more.
The objective of this study was to formulate sodium alginate based ophthalmic mucoadhesive system of gatifloxacin and its in vitro antibacterial potential on pathogenic microorganisms, Staphylococcus aureus and Escherichia coli. Sodium carboxymethylcellulose (NaCMC) was added to the formulations to enhance the gel bioadhesion properties. The prepared formulations were evaluated for their in vitro drug release, gelation behaviour, rheological behavior, and mucoadhesion force. All formulations in non-physiological and physiological condition showed pseudo plastic behavior. Increase in the concentration of sodium alginate and sodium CMC enhanced the mucoadhesive force significantly. In vitro release of gatifloxacin from the system in simulated tear fluid (STF, pH – 7.4), was influenced significantly by the properties and concentration of sodium alginate, NaCMC. Significant reduction in total bacterial count was observed between control and treatment groups with both the test organisms. Full article
18 pages, 302 KiB  
Article
Carbopol/Chitosan Based pH Triggered In Situ Gelling System for Ocular Delivery of Timolol Maleate
by Swati GUPTA 1,2,* and Suresh P. VYAS 2
1 Nanomedicine Research Center, Department Of Pharmaceutics, I.S.F. College Of Pharmacy, Moga 142 001 (PB), India
2 Drug Delivery Research Laboratory, Department of Pharmaceutical Sciences, Dr. Hari Singh Gour Vishwavidyalaya, Sagar (MP) 470 003, India
Sci. Pharm. 2010, 78(4), 959-976; https://doi.org/10.3797/scipharm.1001-06 - 5 Oct 2010
Cited by 132 | Viewed by 4867
Abstract
The poor bioavailability and therapeutic response exhibited by conventional ophthalmic preparations due to rapid precorneal elimination, dilution and nasolacrimal drainage of the drug may be vanquished by the use of in situ gelling systems that are instilled as drops in to the eye [...] Read more.
The poor bioavailability and therapeutic response exhibited by conventional ophthalmic preparations due to rapid precorneal elimination, dilution and nasolacrimal drainage of the drug may be vanquished by the use of in situ gelling systems that are instilled as drops in to the eye and undergo a sol-gel transition in the cul-de-sac. Timolol eye drops may cause systemic side effects in glaucoma patients due to absorption of the drug into systemic circulation. In situ gelling system of this drug can provide localized effect with reduced contraindications, improved patient compliance and better therapeutic index. The present work describes the formulation and evaluation of an ophthalmic delivery system of an antiglaucoma drug, timolol maleate (TM) based on the concept of pH-triggered in situ gelation. Polyacrylic acid (carbopol) was used as the gelling agent in combination with chitosan (amine polysaccharide), which was acted as a viscosity-enhancing agent. Formulations were evaluated for pH, viscosity, gelling capacity and drug content. The 0.4% w/v carbopol/0.5% w/v chitosan based in situ gelling system was in liquid state at room temperature and at the pH formulated (pH 6.0) and underwent rapid transition into the viscous gel phase at the pH of the tear fluid (lacrimal fluid) (pH 7.4). The in vitro drug release and in vivo effects of the developed in situ gelling system were compared with that of Glucomol® (a 0.25% TM ophthalmic solution), 0.4% w/v carbopol solution as well as liposomal formulation. The results clearly demonstrated that developed carbopol-chitosan based formulation was therapeutically efficacious and showed a fickian (diffusion controlled) type of release behaviour over 24 h periods. The developed system is thus a viable alternative to conventional eye drops and can also prevent the rapid drainage as in case of liposomes. Full article
7 pages, 210 KiB  
Article
Permeability Evaluation Through Chitosan Membranes Using Taguchi Design
by Vipin SHARMA, Rakesh Kumar MARWAHA and Harish DUREJA *
Faculty of Pharmaceutical Sciences, M. D. University, Rohtak – 124 001, India
Sci. Pharm. 2010, 78(4), 977-984; https://doi.org/10.3797/scipharm.1009-08 - 21 Oct 2010
Cited by 7 | Viewed by 1290
Abstract
In the present study, chitosan membranes capable of imitating permeation characteristics of diclofenac diethylamine across animal skin were prepared using cast drying method. The effect of concentration of chitosan, concentration of cross-linking agent (NaTPP), crosslinking time was studied using Taguchi design. Taguchi design [...] Read more.
In the present study, chitosan membranes capable of imitating permeation characteristics of diclofenac diethylamine across animal skin were prepared using cast drying method. The effect of concentration of chitosan, concentration of cross-linking agent (NaTPP), crosslinking time was studied using Taguchi design. Taguchi design ranked concentration of chitosan as the most important factor influencing the permeation parameters of diclofenac diethylamine. The flux of the diclofenac diethylamine solution through optimized chitosan membrane (T9) was found to be comparable to that obtained across rat skin. The mathematical model developed using multilinear regression analysis can be used to formulate chitosan membranes that can mimic the desired permeation characteristics. The developed chitosan membranes can be utilized as a substitute to animal skin for in vitro permeation studies. Full article
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