bluuebunny/crossref_metadata_2025_split huggingface dataset:
Crystallization conditions and formation of orthorhombic paracetamol from ethanolic solution
Authors: Al-Zoubi N , Nikolakakis I , Malamataris S 
Published: October 2002

Abstract
Orthorhombic paracetamol exhibits far better tabletability than the monoclinic form and its bulk crystallization from solution attracts much interest. In this study, temperature changes in supersaturated ethanolic solution have been recorded after seeding with orthorhombic crystals under different cooling temperatures (TC) and agitation rates (AR). Average cooling rate (CR), time for maximum temperature deviation (tmax) and area confined between curves of measured and reference temperature plots (AUC) were calculated and correlated with crystal yield (Y). The micromeritic (size and shape) and the compression properties, the density and the orthorhombic content of the crystalline product were evaluated and related to the main crystallization conditions applied (TC and AR). Conditions for optimal crystal yield and orthorhombic content were elucidated. It was found that crystal yield (Y) increased with AR and decreased with TC. The ratio tmax/CR provided good prediction of crystal yield (Y = 58.92 −1.386 tmax/CR, r2 = 0.964 and P = 0.0001). TC and AR linearly affected crystal size and the size distribution, probably due to alterations in supersaturation, but they did not affect the crystal shape significantly. Density and compression properties (yield pressure and elastic recovery) were determined by the content of the orthorhombic form, which increased linearly with AR (P = 0.009) and with TC (P = 0.039) when agitation was between 300 and 500 rev min−1, while tmax decreased. At 700 rev min−1 orthorhombic content was maximized and became independent to TC. Higher orthorhombic content and crystal yield was expected for lower TC and for lower tmax, which corresponded to higher AR and might have also been affected by alteration of seeding and harvesting procedure.
Receptor regulatory properties evident in the molecular similarity of dopamine receptor ligands and purine nucleotides
Authors: Williams W R , Pugh W J , Nicholls P J 
Published: October 2002

Abstract
Computational studies have revealed similarities in the relative configurations of purine nucleotides and ligands for histamine, acetylcholine and adrenergic receptors. In common with other G-protein-regulated receptors, dopamine receptors are associated with specific changes in nucleotide levels during signal transduction processes. The purpose of this study was to investigate molecular similarity in dopamine receptor ligands and purine nucleotides. Molecular superimposition and fitting data for D1-like receptor ligands identified a pharmacophore in the adenine and ribose rings of ATP. D2-like agonists and antagonists related to a pharmacophore in the guanine and ribose rings of GTP. The results are consistent with the hypothesis that the dopamine receptor family may have evolved from receptors for the ATP and GTP nucleotides.
Enteric-coating capsulation of insulinomimetic vanadyl sulfate enhances bioavailability of vanadyl species in rats
Authors: Fugono Jun , Yasui Hiroyuki , Sakurai Hiromu 
Published: October 2002

Abstract
In recent years, there have been improvements in the treatment of type 2 diabetes by oral administration of vanadyl sulfate (VOSO4, VS). The maintenance of vanadyl levels in the blood of subjects with type 2 diabetes was found to be important for the insulinomimetic activity of VS. However, owing to low bioavailability of VS and the development of mild gastrointestinal symptoms and side-effects in some subjects, it is necessary to design more effective and safer dosages of VS. After discovering that VS is absorbed more thoroughly at the ileum than at other gastrointestinal sites, we investigated the absorption processes following oral administration of VS by preparing enteric-coated capsules (ECC). Although Cmax values were unchanged by the dosage forms, Tmax and MRT values associated with the enteric-coating capsulation were prolonged when compared with those observed with use of gelatin capsules (GC). An important finding was that the bioavailability of VS from ECC (9.8%) was almost double that of VS from either GC (4.0%) or the solution (4.8%). Administration of VS-containing ECC to diabetic patients is proposed to improve vanadyl absorption over that achieved by the administration of either GC or the solution.
Synthesis and evaluation of N1-substituted-3-propyl-1,4-benzodiazepine-2-ones as cholecystokinin (CCK2) receptor ligands
Authors: Lattmann Eric , Sattayasai Jintana , Billington David C , Poyner David R , Puapairoj Prapawadee , Tiamkao Siriporn , Airarat Wanchai , Singh Harjit , Offel Michael 
Published: October 2002

Abstract
A novel synthetic approach towards N1-alkylated 3-propyl-1,4-benzodiazepineswas developed in five synthetic steps from 2-amino-4-chlorobenzophenone, in which the N-oxide 4 served as a key intermediate. The structure-activity relationship optimization of this 3-propyl-1,4-benzodiazepine template was carried out on the N1-position by selective alkylation reactions and resulted in a ligand with an improved affinity on the cholecystokinin (CCK2) receptor. The N-allyl-3-propyl-benzodiazepine 6d displayed an affinity towards the CCK2 (CCK-B) receptor of 170 nM in a radiolabelled receptor-binding assay. The anxiolytic activity of this allyl-3-propyl-1,4-benzodiazepine 6d was subsequently determined in in-vivo psychotropic assays. This novel lig and had ED50 values of 4.7 and 5.2 mg kg−1 in the black and white box test and the x-maze, respectively, and no significant sedation/muscle relaxation was observed.
Pharmacokinetic and pharmacodynamic analysis of TS-943, a selective non-peptide platelet glycoprotein-IIb/IIIa (GPIIb/IIIa) receptor antagonist, using a nonlinear mixed effect model in dogs
Authors: Furuya A , Nozawa M , Gotoh J , Jingu S , Akimoto M , Higuchi S , Suwa T , Ogata H 
Published: October 2002

Abstract
A simultaneous analysis of the pharmacokinetics and pharmacodynamics of TS-943, a selective non-peptide platelet glycoprotein-IIb/IIIa (GPIIb/IIIa) receptor antagonist, was made in dogs using a nonlinear mixed effect model. Plasma concentrations of TS-943 were determined after bolus intravenous injection, constant infusion and bolus plus constant infusion. Pharmacokinetic/pharmacodynamic data were fitted using NONMEM software. The pharmacokinetics of TS-943 fitted a two-compartment open model with first-order elimination. The pharmacodynamic model that best fitted platelet aggregation was an inhibitory sigmoid Emax model. The final estimates for E0 (baseline effect), Emax (maximum effect), IC50 (50% inhibitory concentration) and γ (Hill coefficient) were 66.3%, 64.3%, 104 ng mL−1 and 1.37, respectively. Correlations betweenTS-943 plasma concentration and extension of template bleeding time were examined by fitting with an exponential model. The TS-943 plasma concentration necessary to double bleeding time (C2-BTE) was approximately 209 ng mL−1. The model estimated that the C2-BTE/IC50 (inhibition of platelet aggregation) ratio was approximately 2.0-fold in dogs. Our results suggest that the ratio values for dogs and man are comparable. A nonlinear mixed effect model was a useful tool for exploring the concentration-effect relationship for both efficacy and safety of TS-943 in dogs and man. In this study, the dog was found to be a useful model for screening of efficacy and safety of TS-943 in man.
Dexamethasone reduces morphine-induced straub reaction in mice
Authors: Capasso Anna , Casciano Carmela , Loizzo Alberto 
Published: October 2002

Abstract
This study examined the effect of dexamethasone on morphine-induced straub reaction in mice. When morphine was administered in doses of 7.5, 15 and 30 mg kg−1 intraperitoneally, a dose-dependent straub reaction was produced. Dexamethasone per-se (0.1–10 mg kg−1 i.p.) did not modify the tail of control mice.
Pre-treatmentwith dexamethasone 120 min before morphine injection caused a dose-dependent reduction of straub reaction. Cycloheximide (1 5 mg kg−1 i.p.) administered 2 h before morphine did not change morphine-induced straub reaction, but was able to prevent the effects of dexamethasone on morphine-induced straub reaction. The glucocorticoid receptor antagonist RU-38486 (15 mg kg−1 i.p.) did not affect morphine-induced straub reaction, whereas it was able to block the effects of dexamethasone on morphine-induced straub reaction. Results of this study indicate that dexamethasone reduced morphine-mediated straub reaction in mice, indicating a further important functional interaction between dexamethasone and the opioid system. The ability of cycloheximide and RU-38486 to block dexamethasone's effects indicates that the steroid's interference with morphine-mediated straub reaction involves a protein-synthesis-dependent mechanism via gluco-corticoid receptors.
Hormone replacement therapy and breast carcinoma risk in Hispanic and non‐Hispanic women
Authors: Li Rui , Gilliland Frank D. , Baumgartner Kathy , Samet Jonathan 
Published: October 2002

AbstractBACKGROUNDHormone replacement therapy (HRT) alleviates menopausal symptoms and prevents osteoporosis, but there is concern that long‐term use may have an adverse impact on breast carcinoma risk. Epidemiologic studies report inconsistent findings regarding the relationship between HRT and postmenopausal breast carcinoma risk and there is little information on the HRT‐associated risk among minority women.METHODSTo investigate the effects of HRT on breast carcinoma risk among Hispanic women, we examined data from the New Mexico Women's Health Study (NMWHS), a statewide case–control study comprising 366 postmenopausal women with breast carcinoma and 403 controls. Conditional logistic regression was used to estimate the odds ratios (OR) and 95% confidence intervals (95% CI).RESULTSAfter adjustment for sociodemographic, medical, and reproductive factors, we found an increased risk associated with long‐term users of estrogen replacement therapy (ERT; OR for ERT use longer than 140 months was 2.57, 95%CI, 1.25–5.28, compared with ERT use shorter than 17 months). In addition, there was a positive trend with the duration of ERT use (P < 0.01). Hispanic postmenopausal women appeared to be at a significantly greater risk than non‐Hispanic white women (OR for ERT use longer than 140 months in Hispanics was 5.53, 95%CI, 1.47–20.87; OR in non‐Hispanics was 2.65, 95%CI, 0.95–7.34, compared with ERT use shorter than 17 months). In contrast, no significant association was observed for combined estrogen‐progesterone use in either Hispanic or non‐Hispanic women.CONCLUSIONSThe results of this study indicated that postmenopausal women had significantly increased breast carcinoma risk for long‐term ERT use. The risks among Hispanic women were substantially higher than among non‐Hispanic white women although they were not statistically significant. Cancer 2002;95:960–8. © 2002 American Cancer Society.DOI 10.1002/cncr.10791
Viral genotypes and response to interferon in patients with acute prolonged hepatitis B virus infection of adulthood in Japan
Authors: Kobayashi Mariko , Arase Yasuji , Ikeda Kenji , Tsubota Akihito , Suzuki Yoshiyuki , Saitoh Satoshi , Kobayashi Masahiro , Suzuki Fumitaka , Akuta Norio , Someya Takashi , Matsuda Marie , Sato Junko , Takagi Kimiko , Miyakawa Yuzo , Kumada Hiromitsu 
Published: October 2002

AbstractAcute hepatitis B virus (HBV) infection was diagnosed in 57 adults admitted to Toranomon Hospital in Tokyo, Japan. Genotypes of HBV were determined by a serological method and compared to those in 1,077 patients with chronic hepatitis B. The distribution of genotypes were: genotype A (acute, 22.8% vs. chronic, 1.9%; P < 0.00001); B (14.0% vs. 9.4%); C (43.9% vs. 87.7%, P = 0.004); D (1.8% vs. 0.2%); F (1.8% vs. 0.2%); and unable to be typed (15.8% vs. 0.6%, P = 0.001). The infection persisted in seven (12%) of them. They included six (86%) of the seven patients who received prednisolone or glycyrrhizin during an acute phase of illness and one of the 41 (2%) who did not (P = 0.01). Interferon was given to the seven patients with acute prolonged HBV infection, and four of them responded by clearing hepatitis B e antigen (HBeAg) and surface antigen (HBsAg) from serum. Of the four responders, one was infected with HBV genotype B and three with genotype C. HBsAg persisted in the remaining three patients all of whom were infected with HBV genotype A, and HBeAg stayed positive in one of them. These results indicate that HBV genotype A prevails in Japanese patients with acute hepatitis B, and suggest a high efficacy of interferon in the adult patients with acute prolonged HBV infection, except in those infected with HBV genotype A. J. Med. Virol. 68:522–528, 2002. © 2002 Wiley‐Liss, Inc.
An expectancy‐equity model of productive system performance
Authors: Powell Gary N. , Johnson George A. 
Published: October 2002

AbstractAlthough numerous behavioral variables (e.g., personality traits, incentives, nature of supervision) have documented relationships with quantity and quality of output, i.e., performance, in production systems, existing production and operations management models are dominated by technological variables. The article addresses three questions: 1. Which technological and behavioral variables influence productive system performance? 2. How do behavioral and technological variables interact? 3. Which variables are most important under different circumstances in determining performance?An expectancy‐equity model, patterned on research by Lawler [22], presents proposed relationships among variables in production systems, which are classified along a continuum from high to low process predictability. Predominant determinants of performance in various types of systems (e.g., continuous process, job shop, R&D project) are considered in light of the model. Implications for designers and analysts of productive systems and for future research are discussed.
A study of the MRP implementation process
Authors: White Edna M. , Anderson John C. , Schroeder Roger G. , Tupy Sharon E. 
Published: October 2002

AbstractThis paper reports on a large‐scale survey of companies involved in MRP implementation. Survey responses are used to develop a profile of problems typically encountered during the implementation process. Discriminant analysis is used to determine which of those problems, and additional factors, appear to affect the success or failure of MRP implementation. Finally, comparisons are made between the problems encountered during implementation and problems which were found to significantly discriminate between successful and unsuccessful MRP implementors.
An availability model for the evaluation of equipment alternatives
Authors: Lingaraj B.P. , Kuo Way 
Published: October 2002

AbstractAn availability based model for the evaluation of alternatives in equipment replacement analysis is presented. The expected annual cost of an equipment alternative is developed as a function of availability. The least cost alternative for the desired availability is identified from cost vs. availability curves of the alternatives. A simulation approach is used to determine the availability of existing equipment. The methodology is applied to the evaluation of alternate equipment for the analysis of serum samples in a hospital laboratory.
Job shop scheduling with modified due dates
Authors: Baker Kenneth R. , Kanet John J. 
Published: October 2002

AbstractThis paper introduces a new dispatching rule to job shop scheduling, extending earlier results to a multi‐machine environment. This new rule, which uses modified due dates is compared to other popular dispatching methods over a range of due date tightnesses at two utilization levels. The results for mean tardiness indicate that the modified operation due date (MOD) rule compares very favorably with other prominent dispatching methods.The modified due date is a job's original due date or its early finish time, whichever is larger. For an individual operation, it is the operation's original due date or the operation's early finish time, whichever is larger. A comparison of the job‐based version with the operation‐based version indicated that the operation‐based version tended to be more effective at meeting due dates.The main performance measure was mean job tardiness, although the proportion of tardy jobs was also reported, and the two measures together imply the conditional mean tardiness. The MOD rule was compared to several well‐known tardiness‐oriented priority rules, such as minimum slack‐per‐operation (S/OPN), smallest critical ratio (SCR), and COVERT. The MOD rule tended to achieve lower levels of mean tardiness than the other rules, except under conditions where due dates were quite loose. In this situation, very little tardiness occurs for any of the rules. The MOD rule appeared to be more robust than the other rules to changes in the tightness of due dates, and similar results occurred at both high and low utilizations.
Two heuristics for the deterministic, single operator, multiple machine, multiple run cyclic scheduling problem
Authors: Aronson Jay E. 
Published: October 2002

AbstractThe semiautomatic nature of machinery often makes it economical to assign more than one machine to a single operator. Multi‐machine assignments are common in the textile, tooling and molding industries. They are also found where numerically controlled (NC) machinery are used and, more recently, where flexible manufacturing systems (FMS) are employed. Previous work on deterministic cyclic scheduling models has focused on determining the optimal number of usually identical machines with single runs to assign to an operator. In practice, the schedules are represented by man/machine charts.When, due to production requirements, we mix different types of runs with known times on non‐identical machines, we have the deterministic, single operator, multiple machine, multiple run, cyclic scheduling problem. We present two heuristics for solving this more realistic generalization of earlier problems. For the nonidentical, multiple run case, the scheduling of the runs is crucial in minimizing the cycle time of the system. The integer programming formulation of small problems is large, and solving it directly could require excessive computation time on a large mainframe computer.Heuristic 1 selects the next machine run to schedule by minimizing the total immediate waiting cost of the operator and machines. The hourly machine costs reflect the relative merit of utilizing certain machines over others. Heuristic 2 first schedules the machine with the longest automatic processing time of run one. It then follows Heuristic 1 until the long processing time of the first run has ended. The next available run with the longest automatic processing time is then scheduled, and the process repeats. The underlying notion is that many short runs may be performed during the long automatic run of a machine.The heuristics are polynomially bounded, can be easily implemented on a mini‐ or micro‐computer and in practice should be much faster than integer programming methods. In addition to the heuristics, we compute a lower bound on the cycle time. We use this bound as a measure of the effectiveness of a solution. If for a given schedule, the cycle time equals its lower bound, then the solution is optimal.Both heuristics were coded in FORTRAN on a CDC‐6600 computer. An interactive version was also developed for a DEC PDP11/70. A detailed computational study is presented. In it, both heuristics solved 50 machine, 5 run problems in less than 10 CPU seconds on the CDC‐6600. Computational experience indicates that the heuristics are efficient and often find schedules which have cycle times within 10% the lower bound.
A vacation scheduling algorithm for military flight crews: Maximizing satisfaction while maintaining military preparedness
Authors: Chong Philip S. , Strevell Michael W. 
Published: October 2002

AbstractThis article develops a quantitative method of assigning leave to crewmembers in an operational military flying squadron. The objective of the assignment process is to maximize crew preferences. This objective is limited by manning constraints which limit the number of crews that can be on leave at the same time. The basis of the assignment process is a point system which allows each crew to bid for the periods they prefer. The periods are then assigned to the highest bidder. In this way, each crew is assured of an influence in the leave assignment process, and the results are entirely in the hands of the crews themselves. The method now used to assign leave was developed and refined during a three year period from 1981 to 1983. The 1983 method includes a two‐phase partially open bidding system.In Phase I, crews signed up on a posted calendar for the periods they wanted, but they did not assign points to the periods. During this phase, crews could change their period request as they saw what other crews requested. This allows crews to sequence themselves to avoid conflicts. At the end of Phase I, the juggling process was closed, and crews could no longer change their period request. Crews were given a week between the close of Phase I and the start of Phase II to see how many other crews they were competing with. Then in Phase II, they submitted their points via closed bid.This system was very effective in both distributing the demand and preventing “gaming.” There was a strong disincentive from changing a period request at the last minute. If they did, the competition had a week to see whom they were competing with and could then bid accordingly. It was to everyone's advantage to avoid competition.Statistical analysis and positive feedback from crews and scheduling personnel have proven this method to be significantly superior to the former system.
Staffing and equipment decisions for services: An experimental analysis
Authors: Mabert Vincent A. 
Published: October 2002

AbstractMany service‐oriented firms face demand/work load variations that occur both within and between days, and seasonally during the year. These service firms tend to develop staffing plans based on peak periods, resulting in substantial idle time during low demand periods. To counter this, some firms hire part‐time employees to work peak periods to improve productivity. In this way, the cost per customer/transaction (unit) can be reduced.However, the staffing decision is more complex than just determining the number and timing of the work force. The development of good staffing plans must consider the impact of available work stations like telephone consoles and data entry terminals. To use effectively more personnel during peak periods, the firm must have sufficient work stations to assign this work force. Effective staff scheduling must consider simultaneously the work load variations, employ capabilities, and equipment requirements. This article presents a model that incorporates these factors into the decision‐making process and examines their interaction.The model analysis illustrates how uncertainty in work load forecasts and staffing flexibility influence expected cost performance and equipment requirements. A set of computer simulation experiments are conducted using operating data from the proof and encoding departments for Ohio National Bank and Chemical Bank. The results suggest that increased staffing flexibility reduces the needed equipment investment, since part time staff can be scheduled more conveniently to meet varying work loads. Also, basing capital equipment decisions on peak work load levels can substantially increase total operating costs. With these costs explicitly estimated, managers can weigh them against desired service level goals to determine the appropriate balance.