) is a widely administered non-steroidal anti-inflammatory drug (NSAID) in Japan, with annual sales exceeding 50 billion Japanese yen. Although it is a very versatile drug and is often administered to breastfeeding women, the information available regarding its mammary gland transfer is inadequate. Therefore, in this study, we analyzed loxoprofen levels in the blood and milk of four breastfeeding women who received the drug for pain relief. These women visited the Obstetrics and Gynecology Department of Hanwa Sumiyoshi General Hospital for consultation or a cesarean section. One tablet of Loxonin ® (loxoprofen 60 mg) was orally administered to each of the four women, and blood and milk samples were collected 0, 30, 90, 150 and 330 min after drug administration. Twenty microliters of ethanol was added to the blood and milk samples (10 μL), and the mixture was centrifuged at 12000 g for 15 min. The supernatant was analyzed by high-performance liquid chromatography (HPLC). Loxoprofen levels in blood peaked 90 min after its oral administration in all four patients, with the highest level being 4.5 μg/mL in patient II, whereas loxoprofen level in milk was below the detection limit (0.1 μg/mL) at all time points. Taken together, the data suggest low mammary gland transfer of loxoprofen, and thereby a low lactation risk.
Consumption of alcohol concomitantly with a drug may increase absorption of the active ingredients, leading to dose dumping. In this study, ibuprofen was administered to mice along with rice wine or beer. Blood concentrations of ibuprofen were lower when taken with alcohol than when taken with water. The ibuprofen formulation was suspended in rice wine, beer, 15% ethanol, or 20% mannitol, and then administered to male ddY mice. In a separate experiment, mice were pretreated with rice wine per os (p.o.) or loperamide (p.o.) 30 min before administering ibuprofen with water. Ibuprofen doses for oral administration and tail vein injection were 40 mg/kg and 0.75 mg/kg, respectively. Maximum blood concentrations (C max ) were lower in mice pretreated with rice wine or beer. There were no significant differences in ibuprofen clearance between animals pretreated with rice wine by tail vein injection and controls. Pretreatment with 20% mannitol or loperamide lowered the blood concentration of ibuprofen. These results suggest that alcoholic beverages affect drug pharmacokinetics. In particular, absorption may be affected by an increase in osmotic pressure and inhibition of gastrointestinal transit.
In the medical scene of drug administration via tubes, catheter-type syringes should be changed whenever sliding of the syringe plunger deteriorates. We encountered a situation where the syringe plunger sliding worsened earlier than other preparations. However, there have been no reports investigating factors that impair plunger sliding. In this report, we evaluated the grime on the plunger gasket in relationship to the force for sliding resistance of the plunger. Prescription drugs studied included "Gaster ® Tablets 20 mg" and other four drugs. The number of pixels on the image corresponded to the amount of grime. The force applied on the plunger was measured using a digital force gauge. We observed a correlation, albeit weak (R = 0.51), between the number of pixels and the force required to move the plunger. The force and particle number values were high for "Gaster ® Tablets 20 mg". We repeated the measurements with "Gaster ® D Tablets 20 mg". Lower values were obtained for "Gaster ® D tablets 20 mg". Talc, showed higher values so that the smaller the particle sizes, the higher the contents. Conversely, low substituted hydroxypropylcellulose and anhydrous dibasic calcium phosphate, of the type present in "Gaster ® Tablets 20 mg" as an additive, gave lower values. In conclusion, the grime on gaskets is a sign that the syringes need to be changed, and the content and particle size of the talc, which was an additive agent, is one of the factors that impair syringe plunger sliding.
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