Carisoprodol: an unrecognized drug of abuse.
During a 6-month monitoring period, carisoprodol was detected in the urine specimens of 19 patients for whom drug screening had been ordered for purposes of patient care. The clinical history suggested that in 7 cases the drug was abused or implicated in a suicide attempt or gesture. In another 7 cases, the drug was used primarily for medical purposes, and in 5 cases the reason for use could not be determined. One patient ingested homemade tablets that were found to contain carisoprodol. In an additional case, the drug was detected in breast milk. Physical findings, clinical history, and treatment are described, and the profile of a typical carisoprodol user is discussed. It seems that carisoprodol has become an unrecognized drug of abuse, at least in our community. This drug and its metabolite, meprobamate, should be included in comprehensive drug screening. (+info)
Application of eudragit RS to thermo-sensitive drug delivery systems. I. Thermo-sensitive drug release from acetaminophen matrix tablets consisting of eudragit RS/PEG 400 blend polymers.
In order to develop the polymer materials having temperature-sensitive and high biological safety, Eudragit RS-PO and polyethylene glycol 400 (PEG 400) blend polymers (EPG) were prepared. The EPGs that have the glass transition temperature (Tg) at around the body temperature were prepared by the addition of 5--13% PEG 400 to Eudragit RS. As glassy polymers are not in thermodynamic equilibrium below their Tg, the effects of isothermal aging on the T(g)s of Eudragit RS and EPG containing 10% PEG 400 (10% EPG) were also studied at various aging temperatures. The Tg values of Eudragit RS increased with the aging time and after 30 d of aging, they apparently reached constant values which markedly differed depending on the aging temperatures. On the other hand, the Tg values of 10% EPG were almost independent of the aging temperature and reached around 33 degrees C at 30 d after aging. The ability as thermo-sensitive polymer of EPG was evaluated by the dissolution test of the acetaminophen (AAP) matrix tablets prepared with EPG. The AAP release rate from the EPG matrix tablets slightly changed below the Tg of tablets, and then, it markedly increased above the Tg. Considering high biological safety of Eudragit RS and PEG 400, EPG might be available to develop the novel thermo-sensitive drug delivery systems. (+info)
Vitreous penetration of levofloxacin in the uninflamed phakic human eye.
AIMS: To assess the vitreous penetration of oral levofloxacin (a new fluoroquinolone antibiotic with improved Gram positive activity) in uninflamed phakic eyes. METHODS: 15 patients for macula hole surgery were recruited to the study. 10 received a single 500 mg dose of levofloxacin by mouth preoperatively. Five acted as controls. Serum and undiluted vitreous samples were obtained at surgery and analysed by HPLC. RESULTS: Levofloxacin was detectable 2.5 hours after administration in the vitreous. A peak concentration of 1.6 microg/ml (or mg/l) was measured between 2.5 and 4 hours post-dose. CONCLUSION: Oral levofloxacin reaches the vitreous rapidly in the uninflamed phakic eye. Levels did not reach MIC(90) for the commonest infecting organisms. Nevertheless, levofloxacin would be expected to be active against a higher proportion of infecting organisms than either ciprofloxacin or ofloxacin. (+info)
Observation on the therapeutic effect of Shu Feng Huo Luo Pian for treatment of osseous arthritis.
OBJECTIVE: To evaluate the therapeutic effect of Chinese patent drug Shu Feng Huo Luo Pian ([symbol: see text] Pill for Dispelling Wind and Activating Collaterals) for the treatment of osseous arthritis. METHOD: 50 cases of osseous arthritis were divided randomly into two groups, the Shu Feng Huo Luo Pian group (the experimental group), including 30 cases (aged 63.5 +/- 4 years), treated with 2 such pills, p.o., bid; and the control group, including 19 cases (aged 63 +/- 5 years), treated with Sulindac 0.2 g, p.o., bid. The two groups were all supplemented by medication of calcium Caltrate D 0.6 g, p.o., qd. The above-mentioned medications were administered for 2 courses, 2 weeks constituting a course. RESULT: The total effective rate of the experimental group evaluated by the doctors was 83.3%, and that evaluated by the patients was 90%, with mild side effects. CONCLUSION: Shu Feng Huo Luo Pian is an effective Chinese patent drug for treating osseous arthritis, with less and mild side effects. (+info)
Comparison of two nimodipine formulations in healthy volunteers.
The objective of this study was to assess the pharmacokientic parameters of regular nimodipine (Bayer), 30 mg, given every 6 h and nimodipine AP (nimodipine in micro particles with programmed action contained in tablets, developed by Biocontrolled-Leti Group Laboratories), 120 mg, given every 24 h. Subjects (19 healthy volunteers, five female; 14 male: age: 21 +/- 0.7 years) received one formulation over 5 days. Then, after a washout period of 7 days, the other formulation was given. The analyst was blinded to the relationship in formulation received. Antecubital blood samples were taken before the first tablet was taken and after 15, 45, 60 min and 2, 4, 6, 8, 12, 13, 18 and 24 h on day 1 and five of each formulation. Nimodipine blood levels were analysed by HPLC. At steady-state regular nimodipine reached a C-max of 10.208 +/- 0.317 ng/ml, at a t-max of 1 h; minimum concentration 6 h after dosage was 1.2929 +/- 0.411 ng/ml, half-life was estimated in 2.9 h. Meanwhile nimodipine AP 120 mg reach a C-max of 11.885 +/- 0.403 ng/ml; a t-max of 1 h with a minimum concentration 24 h after the last dose of 4.2387 +/- 0.353 ng/ml (P < 0.001). Apparent half-life was calculated in 17.8 h (P < 0.001). Area under the curve for the 24 h period was 143.76 ng/ml/min for regular nimodipine and 183.7 ng/ml/min for nimodipine AP 120 mg (P < 0.001), indicating better bioavailability. In conclusion nimodipine in AP formulation 120 mg produced similar peak plasma levels (C-max) than regular nimodipine, but with higher trough (C-min) values and stable plasma levels with one administration every 24 h. This formulation would be more suitable when nimodipine chronic therapy is indicated. (+info)
Extraction of lead(II) and copper(II) from salicylate media by tributylphosphine oxide.
Tributylphosphine oxide (TBPO) is proposed as an extractant for the extraction of lead(II) and copper(II) from salicylate media. The optimum conditions were evaluated by varying the experimental parameters, such as the pH, sodium salicylate concentration, tributylphosphine oxide (TBPO) concentration, shaking period and various diluents. The probable extracted species, deduced from log-log plots were Pb(HSal)2.2TBPO and Cu(HSal)2.2TBPO. The extraction took place through a solvation mechanism. The method permits the binary separation of lead(II) and copper(II) from commonly associated elements as well as the mutual separation of lead(II) and copper(II). The method is applicable to the determination of lead(II) and copper(II) in various alloys as well as environmental and pharmaceutical samples. (+info)
The effect of tablet formulation and hardness on in vitro release of cephalexin from Eudragit L100 based extended release tablets.
Eighteen batches of cephalexin extended release tablet were prepared by wet granulation method by using Eudragit L100. The effect of the concentration of Eudragit L100, microcrystalline cellulose and tablet hardness on cephalexin release was studied. The formulated tablets were also characterized for physical and chemical parameters. The dissolution results showed that a higher amount of Eudragit in tablet composition and higher tablet hardness resulted in reduced drug release. An increased amount of microcrystalline cellulose in tablet composition resulted in enhanced drug release. Tablet composition of 13.3% w/w Eudragit L100 and 6.6 to 8% w/w microcrystalline cellulose with hardness of 7-11 kg/cm2 gave predicted release for 6 h. The in vitro release was compared with a marketed tablet. Physical and chemical parameters of all formulated tablets were within acceptable limits. The effect of storage on in vitro release and physicochemical parameters of tablets was evaluated and two batches among formulated eighteen batches found to be in acceptable limits. (+info)
Determination of the active ingredient loperamide hydrochloride in pharmaceutical caplets by high performance thin layer chromatography with ultraviolet absorption densitometry of fluorescence quenched zones.
A quantitative method using silica gel HPTLC plates with fluorescent indicator, automated sample application, and automated UV absorption densitometry of the fluorescence quenching zones was developed and validated for determination of loperamide hydrochloride in anti-diarrheal medications. Samples of three brands of caplets assayed within 96.0-105% of the 2 mg label value. Repeatability was 3.3%, 1.6%, and 2.8% (RSD) for replicate analyses (n=6) of three tablets. The errors of a blank-spike and standard analyses performed to evaluate accuracy were 2.00% and 2.02%, respectively. The method is suitable for application in a drug manufacturing quality control or regulatory analysis laboratory. (+info)