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Artificial Intelligence in Pharmaceutical Research : Theory and Applications |
p. 509 |
| P Moudgil, A. K Tiwary, S Gupta Artificial intelligence includes methods, tools and systems devoted to simulate human brain. The brain activity comprises of logical-cum-inductive knowledge acquisition and reasoning for solving problems. The future seems to be closely tied to research programs in artificial intelligence. The theory of neural network operation and potential applications of neural network based artificial intelligence in pharmaceutical sciences are reviewed in the present article. |
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Recent Advances in Modulated Drug Delivery Systems |
p. 515 |
| Sushama Talegaonkar, P. R Mishra, R. K Khar Modern therapeutic system has often been criticized for the toxicity associated with the drugs. To minimize this drawback, many researchers have focussed attention towards developing modulated drug delivery systems capable of releasing therapeutic agents in response to physiological requirements. Another class of modulated drug delivery systems are those in which pulsatile release of drugs is triggered by external signals. The former is known as self-regulated or responsive systems while the latter is known as externally regulated or pulsatile delivery systems. This article briefly describes the fundamental principles of various types of pulsatile as well as responsive drug delivery systems. Recent developments in the field of pulsatile systems based on external triggers such as electrical, ultrasound, magnetic and massages have been reported. This article also traces recent research in the field of polymer based temperature-sensitive, pH-responsive, inflammation-responsive and glucose-and other saccharide-sensitive systems; enzymebased urea-responsive, glucose-responsive and morphine-triggered systems; systems based on antibody interactions, and systems utilizing chelation. |
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Formulation and Dissolution Properties of Meloxicam Solid Dispersion Incorporated Suppositories |
p. 525 |
| K Gowthamarajan, T Giriraj Kulkarni, G Venkateswaran, M. K Samanta, B Suresh β-Cyclodextrin complexes of meloxicam were prepared by solvent evaporation technique in different ratios to enhance the solubility of the drug. The complex was characterized by infrared spectroscopy and differential scanning calorimetry studies. There was no interaction between drug and carrier. Based on physical characters and in vitro drug release pattern, 1:3 drug-carrier ratio was selected as ideal batch for suppositories. A water-soluble base, polyethylene glycol, was selected as ideal base for the preparation of suppositories. The suppositories were prepared by moulding technique. The ideal batch of solid dispersion was incorporated into suppository base. The prepared suppositories were characterized for hardness, melting point, disintegration time and drug content. All these properties were found to be ideal. The in vitro drug release pattern was determined by rotating dialysis bag method. The in vitro release of. meloxicam from its solid dispersion incorporated suppositories was significantly improved when compared to the intact bulk drug incorporated suppositories. |
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Solubility Enhancement Of Nimesulide And Ibuprofen By Solid Dispersion Technique  |
p. 529 |
| R. N Saha, C Sajeev, K Padma Priya, C Sreekhar, G Shashikanth An attempt has been made to enhance solubility and dissolution of nimesulide and ibuprofen by solid dispersion techniques and complexation using various hydrophilic excipients. Drug-excipients solid dispersions and complexes of nimesulide were prepared by solvent evaporation method. Solid dispersions of ibuprofen were prepared by fusion, solvent evaporation and fusion-solvent method. Solubility profiles of the drug from the solid dispersions and complexes of nimesulide were studied in buffered pH 6.6, whereas the solubility of drug-excipients dispersions of ibuprofen were evaluated in 0.1 N sodium hydroxide media. Solid dispersions of nimesulide with PEG-6000 enhanced the solubility of nimesulide by more than 1000%. Dispersion of ibuprofen in sorbitol showed maximum enhancement of solubility (up to 75%). Dispersions in combined carriers: PVP k-30-MCC and PVP k-30-PEG-6000 also markedly increased the solubility of ibuprofen. Inclusion complexes of nimesulide in β-cyclodextrin also increased the solubility by 663%. Intrinsic dissolution rate studies of solid dispersions of nimesulide with PEG-6000 and ibuprofen with sorbitol were further studied. The intrinsic dissolution rate constant (K1) for the dispersions of these drugs were 1.62 (+62%) and 1.80 (+80 %) times that of pure nimesulide and ibuprofen, respectively. |
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Synthesis And Antiinflammatory Activity Of Aminomethylisoxazolinyl/Azopyrazolinyl Diphenylamine Derivatives |
p. 535 |
| P Rani, V. K Srivastava, A Kumar Chalcones (2-5), isoxazolines (6-9), Mannich bases (10-25), pyrazolines (26-29) and azo derivatives (30'-33) of diphenylamine were synthesized and screened against carrageenan-induced edema in rats at 50 mg/kg, orally. All the compounds of this series have shown promising anti-inflammatory activity. Compound (29) [1-acetyl-5-(4-methoxypheny1)-2-pyrazoliny diphenylamine was found to be the most potent, even more that the standard, phenylbutazone. This compound was also evaluated for ulcerogenicity and acute toxicity. |
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Simultaneous Analysis Of Phenylpropanolamine, Chlorpheniramine And Bromhexine In Syrups By Derivative Spectrophotometry |
p. 540 |
| S. K Panda, A. K Sharma, L. K Sahu The absorbance maxima of phenylpropanolamine and chlorpheniramine maleate in 0.1 N hydrochloric acid are 257, 265 nm, respectively, whereas, bromhexine hydrochloride shows absorbance maxima at 245 and 311 nm. This paper presents two methods based on first derivative spectrophotometry for simultaneous estimations of these three drugs in combination in pharmaceutical formulations. The first derivative amplitude at 264, 280.6 and 327 nm is utilized for simultaneous estimation. Linearity was validated by Least Squares Method. The results of analysis have been validated statistically. The proposed methods are simple, economical, accurate, reproducible and rapid. |
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Synthesis And Biological Activity Of Some Amino Acid Conjugates Of Oxaprozin |
p. 545 |
| S. J Kachhwaha, Sheeba Varghese, D Gupta, Deepali Mhaske, S. R Dhaneshwar Amino acid conjugates between various amino acid methyl esters and the carboxylic acid group of oxaprozin were synthesized using N,N’-dicyclohexylcarbodiimide as a coupling agent. These compounds were characterized by analytical and spectral data. Kinetics of hydrolysis of these conjugates was studied. The esters were evaluated for analgesic and antiinflammatory activity and ulcerogenicity. The esters showed comparable analgesic and anti-inflammatory activity with negligible ulcerogenicity. |
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Clinical Pharmacy Interventions In A Secondary Care Hospital In South India |
p. 550 |
| Lakhvinder S Batolar, S. D Rajendran, B Suresh A prospective study of interventions was carried out at Government Head Quarters Hospital, Ootacamund in order to document the nature and frequency of interventions made by clinical pharmacists at the hospital. Approval of the hospital's ethics committee was obtained. Intervention Data Record included information on patient demographics, admission details, past medical and drug history, present diagnosis and treatment and intervention. Data was collected for a period of seven months between September 1998 and April 1999 from selected wards. Reactive interventions occurred in 8.2% of the 1840 patients admitted, of whom 54.3% were males and 45.7% were females. The mean age of the patients was 44.9 years (±15.3). lnterventions were accepted on 147 of 151 cases. Frequency of interventions in various wards included female medical ward (38%), male medical ward (36.7%), intensive care unit (21%) and intensive cardiac care unit (4%). Clinical conditions in which interventions occurred included congestive cardiac failure (15.9%), chronic obstructive pulmonary disease (15.9%) and diabetes mellitus (13.2%). Drugs most frequently involved in the interventions were antibiotics (31.8%), insulin (10.6%) digoxin and frusemide (8.6% each). Intervention to discontinue a drug (29.8%) was the most common recommendation made. Majority of recommendations addressed the issue of inappropriate or unnecessary drug or drug regimen (31.1%). Recommendations for appropriate drug therapy were made in 29.8% of interventions. Outcomes could be measured in 37.1% of interventions, of which, 89.2% were beneficial. |
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Synthesis And Evaluation Of Pharmacological Activities Of Cyclodextrin Conjugates Of Flurbiprofen |
p. 558 |
| Sheeba Varghese, D Gupta, Deepali Mhaske, S. S Kadam, S. R Dhaneshwar In the present investigation flurbiprofen prodrugs of α and γ cyclodextrins were synthesized. Here the primary hydroxy group of α and γ cyclodextrins were used to block the acid group. The synthesis involved a series of protection and deprotection reaction. The esters were evaluated for their stability in simulated gastric and intestinal fluid. The hydrolysis of cyclodextrin conjugates in colon is confirmed by the hydrolysis kinetics studies in rat faecal material. The esters were evaluated for their analgesic and antiinflammatory activities. The ulcerogenicity of the esters was also studied. The results of these studies revealed that the esters have comparable antiinflammatory and analgesic activity with the parent drug, flurbiprofen. The esters showed no ulcers even at a dose 12 times greater than normal dose. |
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Development And Evaluation Of Muco-Adhesive Buccal Tablets Of Lignocaine Hydrochloride |
p. 563 |
| N Parviez, Alka Ahuja, R. K Khar Lignocaine hydrochloride was formulated as a buccal tablet to provide prolonged relief from pain associated with tooth extraction. The tablet was prepared using suitable mucoadhesive polymers. Optimized tablets contained lignocaine hydrochloride 15 mg, Carbopol-934P 15.2 mg, sodium carboxy methyl cellulose 60.8 mg, mannitol 4 mg, Polyvinyl pyrrolidone-K30 5 mg, magnesium stearate 2 mg, saccharin sodium 0.2 mg and mint flavor (dried) 0.1 mg. Dissolution studies showed 86.66% release of drug in 360 min. Bio-adhesive strength was found to be 31.96 g. Adhesion time was greater than 6 h. Surface pH was found to be 7.02. The formulation was also subjected to in vitro permeation studies, in situ release studies, in vitro swelling studies and in vivo evaluation in healthy volunteers. The optimized tablets were also subjected to other quality control tests. Stability studies showed that the formulation was stable for more than two years. |
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Molecular Inclusion Of Sparfloxacin With Hydroxypropyl Beta Cyclodextrin |
p. 568 |
| V. K Mourya, T. R Saini, V Balasubramaniyam, J. S Shete, G. S Jadhav The formation of an inclusion complex between hydroxypropyl-β-cyclodextrin and sparfloxacin is described. The 1:1 stoichiometry of the components is suggested by phase solubility studies and Benesi-Hildebrand plot showing the regression y=0.0087x+32.273 with the coefficient of correlation 0.7706 at slit width 1 nm. Stability constant evaluated by phase solubility analysis and Benesi-Hildebrand plot showed deviations. Thermodynamic parameters for the inclusion complex have been also estimated. The formation of the complex is detected by differential scanning calorimetry, potentiometry, UV, FTlR and fluorescence spectral methods. The complex displays enhanced aqueous solubility and dissolution. |
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Influence Of Terpene Lactones Treatment On Brain Lipid Peroxidation And Antioxidant Defense Systems Of Rats After Focal Ischaemia |
p. 573 |
| Yu-Yang Zhang, Qing Hai Yu, Song You, Li Sheng, Yi-Mei Wang, Yu-Li Wan The influence of terpene lactones on the lipid peroxide product, malcndialdehyde, glutathione and catalase, glutathione peroxidase, superoxide dismutase activities in rat brain as well as lactate dehydrogenase and creatine kinase activities in rat blood serum after occlusion of middle cerebral artery following reperfusion was investigated. Experimental model of the reversible middle cerebral artery occlusion without craniectomy of rat focal cerebral ischaemia-reperfusion was used. Compared to sham-operated animals, rats subjected ischaemia followed reperfusion exhibited severe neurologic deficits, ischaemia followed reperfusion increased blood serum lactate dehydrogenase and creatine kinase activities as well as brain glutathione peroxidase activity and decreased superoxide dismutase activity as well as glutathione and malondialdehyde content. Administration of terpene lactones (4,8,16 mg/kg, i.p.x2) at 15 min and 6 h after induction of just ischaemia could improve the movement function and normalize the lactate dehydrogenase and creatine kinase activities of the rat serum. Terpene lactones were also able to increase catalase and superoxide dismutase activity, ameliorate the abnormal increment of glutathione peroxidase activity but did not change glutathione content. Significant decrement of malondialdehyde content in cortex and striatum was also observed when terpene lactones were administrated. These results suggested that terpene lactones could affect the process of oxidative damage. This perhaps was related to the beneficial role in the protection against ischaemia-reperfusion injury. |
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Effect Of Ancymidol On The Production Of Forskolin From Cell Cultures Of Coleus Forskohlii |
p. 579 |
| R Mamtha, CH Prasad Babu, C. S Reddy, C. K Kokate, C Veeresham The treatment of cell cultures of Coleus forskohlii Briq with 50µm of ancymidol a inhibitor of gibberellin biosynthesis enhanced the bioproduction of forskohlin by 150%, using production medium in six well plate as culture vessel. |
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Spectrophotometric Determination Of Indinavir With Precipitation Reagents |
p. 581 |
| C. S. N Sarma, C Kamala Sastri, C. S. P Sastry Indinavir sulphate forms insoluble molecular complex with ammonium molybdate (method A), phosphomoiybdic acid (method B) or tannic acid (method C) under acid conditions. In addition, colour reactions have been combined to estimate each precipitant and in turn indinavir sulphate. They are based on the colour formation with released precipitant from the precipitate with chromogenic reagents such as potassium thiocyanate (λmax 480 nm for method A) or cobalt nitrate ethylene diamine tetra acetic acid disodium salt complex (λmax 840 nm for method B) or metolchromium (VI) (λmax 590 nm for method C). The methods are statistically validated and found to be precise and accurate. |
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Development Of A New Spectrophotometric Method For The Analysis Of Atropine Sulphate |
p. 584 |
| K. M Bhat, V Kumar, K. I Molvi, N. S Parmar A new spectrophotometric method for the assay of atropine sulphate has been developed. This utilized the well known reaction of tropic acid, Vitalimonium reaction. The sample when digested with nitric acid and treated with 3% methanolic potassium hydroxide develops a blue chromophore. The absorbance of the resulting solution was measured exactly after one minute at 570 nm. This method has a linearity range of 2-20 µg/ml and compares well with official procedure. |
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Studies On The Antimicrobial Potential Of Berberis Tinctoria Lesch Root And Root Bark |
p. 586 |
| B Duraiswamy, M Abraham, G. S Saritha, M. J Nanjan, B Suresh Chloroform and methanol extracts of Berberis tinctoria Lesch (Berberidaceae) root and root bark were investigated for antibacterial potential against Bacillus subtilis NCIM-2349, Bacillus coagulans NCIM-2323 Staphylococcus aureus NCIM-2492, Escherichia coli NCIM-2345 and antifungal potential against Candida albicans 6, 8, 11 and 27 (different strains of Candida albicans), Aspergillus flavus, Aspergillus niger, Aspergillus xylinum and Aspergillus fumigatus. Both the extracts showed significant antibacterial and antifungal activity against all the microorganisms tested and the effect so produced was comparable to those of the standards, ampicillin and clotrimazole. However, the antifungal activity of the chloroform extract of the root was found to be negligible against Aspergillus species tested. |
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Development Of Dissolution Medium For A Poorly Water Soluble Drug, Celecoxib  |
p. 588 |
| G. V Murali Mohan Babu, V Gouri Shankar, K Hima Sankar, A Seshasayana, N Kishore Kumar, K. V Ramana Murthy Celecoxib, a non-steroidal antiinflammatory drug is poorly water soluble. In the present study a new dissolution medium was developed, as there is no official dissolution medium. The composition of the medium was selected on the basis of solubility data of celecoxib at 37º. Solubility data revealed that water consisting of 2% w/v sodium lauryl sulphate could be a suitable dissolution medium. The discriminating power of the selected dissolution medium (2% w/v sodium lauryl sulphate in water) relative to other dissolution mediums was evaluated and the results further justified the usage of 2% w/v sodium lauryl sulphate in water as dissolution medium for celecoxib. |
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Design And Fabrication Of A Special Punch For Buccoadhesive Core-In-Cup Tablets |
p. 591 |
| H. G Shivakumar, K. H Desai, T. M Pramodkumar A special punch was designed and fabricated to prepare buccoadhesive core-in cup tablets by making protrusion in the 11 mm upper flat-faced punch. The buccoadhesive cups were prepared by direct compression method using polymers like carbopol 934P and hydroxy propyl methylcellulose on a Cadmach single station tabletting machine. The cups were evaluated for uniformity of weight, depth and thickness. |
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In Vitro Permeation Of Verapamil Hydrochloride From Polymeric Membrane Systems Across Rat And Human Cadaver Skin |
p. 593 |
| R. V Kulkarni, H Doddayya In this article various polymeric membrane systems of poly vinyl pyrrolidone, ethyl cellulose, Eudragit RS100 and ethylene vinyl acetate, containing verapamil hydrochloride, along with glycerol and dibutyl phthalate as plasticizers have been fabricated for transdermal use. Both monolithic and membrane controlled systems were prepared by the method of casting on mercury surface and evaluated for thickness uniformity, drug content uniformity, tensile strength, Percentage of elongation and skin irritation. In vitro drug permeation through rat abdominal skin and human cadaver skin was performed using Keshary-Chien diffusion cells. Results indicated that, the order of permeation of the drug from different polymeric membranes was poly vinyl pyrrolidone>ethyl cellulose>Eudragit RS100>ethylene vinyl acetate. The drug release mechanism from all monolithic systems was diffusion controlled, where as membrane controlled systems followed nearly zero order kinetics, as the thickness of rate controlling membrane was increased from 100 to 200µ, the drug release was decreased. Compared to rat skin, a low permeation rate of the drug was observed through human cadaver skin, this indicates meeting the target flux in rat skin does not guarantee it's good permeability in human skin. |
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Formulation And Evaluation Of Nimesulide Dispersible Tablets |
p. 598 |
| G Chandra Sekhara Rao, K. E. V Nagoji, M. E Bhanoji Rao Dispersible tablets of nimesulide using primojel as dispersing agent with starch, lactose and dicalcium phosphate as diluents were prepared and evaluated as per official (BP) requirements and compared with commercial dispersible tablets. The formulations with starch and lactose as diluents showed fast and rapid dissolution when compared to that of commercial tablets whereas the formulations with dicalcium phosphate as diluent showed less dissolution rate. |
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Antibacterial And Antifungal Activities Of Some Novel 2,3-Disubstituted Quinazolin-4(3H)-Ones |
p. 600 |
| V Alagarsamy A series of novel 2,3-disubstituted quinazolin-4(3H)-ones have been synthesized by condensing the aromatic primary amino group of quinazoline with different aldehydes and ketones. When these compounds were evaluated for antibacterial and antifungal activities, all the compounds inhibited the growth of bacteria and fungi significantly. The compounds VII and IX exhibited equlpotent activity with the standard ciprofloxacin against Shigelia flexneri, and Pseudomonas aeruginosa, and the compound Vlll exhibited equivalent activity to ciprofloxacin against Bacillus subtilis and Citrobacter ferundii. The compounds V,VI and IX were found to be equipotent with the standard clotrimazole against Aspergillus niger and Microsporum gypseum; and the compound VI was equipotent with standard clotrimazole against Trichophyton mentagrophytes. |
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Spectrophotometric Investigations On The Assay Of Phenothiazine Drugs |
p. 603 |
| A. G Sajjan, K. C Ramesh, J Seetharamappa, J Keshavayya A rapid, accurate and sensitive spectrophotometric method for the quantitative determination of four phenothiazine drugs either in pure form or in pharmaceutical preparations has been developed. The method is based on the development of red coloured products by the interaction of
phenothiazines with diazotised anthranilic acid in hydrochloric acid medium. The reaction proceeds via the oxidation of the phenothiazine nucleus into a semiquinonoid radical. The optimum reaction conditions and other analytical parameters are evaluated. The common excipients employed do not interfere in the determination of phenothiazine drugs. Results of analysis of pure drugs and their dosage forms by the proposed method are in good agreement with those of the official method. |
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Intellectual Property Rights |
p. 607 |
| S Ahuja, S. K Bagga, R Keith, G. G Nair, A. V Singh, R. V. S. V Vadlamudi Cyber-based American-Indian Pharmaceutical Education And Research Group is offering a common platform for expressing ideas on any aspect of pharmaceutical sciences and its allied subjects. Drug development needs a close interaction of several allied scientific areas and the American-Indian Pharmaceutical Education And Research Group is open to members of the Bioinformatics, Biotechnology, Clinical Research, Immunology, Life Sciences, Pharmacology, SAS -Programming and Pharmaceutical industry or Academia. One of the unique features of the American- Indian Pharmaceutical Education And Research Group is the monthly discussion and during October 2002, these group members have exchanged views on intellectual Property Rights. A concise report on this topic is presented here. In future, the American-Indian Pharmaceutical Education And Research Group has plans to conduct online symposia and conferences. |
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