Two novel abietane diterpenes from Salvia miltiorrhiza

Two new abietane-type pigments named tanshinol A (1) and tanshinol B (2) have been isolated from the roots of Salvia miltiorrhiza B. (Labiatae) as minor components together with sixteen other related tanshinone pigments 3-18. The structures of the two novel components 1 and 2 were established by means of spectral analyses.     

Batch variation and pharmacokinetics of oral sustained release melatonin-loaded sugar spheres in human subjects

The three different batches of an oral sustained release melatonin (MT) delivery system were prepared by aqueous-based fluid-bed coating of the sugar spheres for the evaluation ofin vitro release characteristics and plasma concentration profiles in human subjects. The MT contents in 20% coated sugar spheres of three batches (B1, B2 and B3) were 3.3+/-0.08, 2.4+/-0.1 and 2.5+/-0.13 mg per gram of coated sugar spheres, respectively. The release profiles of three different batches had a very similar fashion. However, the release half-lives (T(50%)) of MT from B1, B2 and B3 was 3.70+/-0.2, 5.2+/-0.2 and 4.9+/-0.07h, respectively. Plasma concentration profiles of sustained release 0.2mg melatonin-loaded sugar spheres containing 10% immediate release melatonin in gelatin capsules (B1 and B2) were then evaluated in human subjects. Thein vivo plasma concentration profiles of the two batches (B1 and B2) were very similar each other and located between the physiological endogenous ranges. The time to reach the peak concentration (T(max)) was more advanced in case of B1 when compared to B2. However, there was no statistically significant difference in the maximum concentration (C(max)) and the area under the curve (AUC) between B1 and B2. The AUC of melatonin-loaded sugar spheres containing 10% and 20% immediate release MT in human subjects had a good linearity between dose and AUC, regardless of the fraction of immediate release MT, indicating the first order elimination process of MT within these doses. The current oral sustained release MT delivery system may be utilized to treat circadian rhythm disorders if it is proven to be more clinically useful when compared to immediate release MT.     

Aneurysm of persistent primitive hypoglossal artery

A patient with a ruptured intracranial aneurysm of the right persistent primitive hypoglossal artery is described. Clipping of the aneurysmal neck was achieved by a far lateral approach together with drilling of the jugular tubercle, and it was concluded that this approach should be followed for safe and complete clipping.     

Comparing sulindac with indomethacin for closure of ductus arteriosus in preterm infants

Objectives: A prospective study comparing the efficiacy and side-effects of oral sulindac with intravenous indomethacin in clinically stable preterm infants (<1750 g) requiring non-invasive closure of haemodynamically significant patent ductus arteriosus.
Methodology: As maturity and birthweight are the two major determinants of ductal closure, infants were matched as closely as possible for these parameters. An eligible patient was first assigned to the sulindac group and a subsequent patient with similar gestational age (± 1 week) and birthweight (±100 g) to the previously recruited infant would automatically receive indomethacin. A total of eight infants were enrolled in each group.
Results: The ductus arteriosus was successfully closed in all eight infants receiving indomethacin, and in seven of eight infants receiving sulindac. No significant differences were found with regards to the ductal size between the two groups at diagnosis or on each of the consecutive days of treatment ( P >0.25). More renal adverse effects were encountered in the indomethacin group. Significant differences in changes from baseline value for urine output, plasma sodium, urea and creatinine concentrations were noted at 24, 48 and 72 h after commencement of treatment between the two groups ( P <0.05). All the parameters returned to normal or pre-treatment levels 48 h after stopping therapy. Unexpectedly, severe gastrointestinal complications were encountered in the sulindac group.
Conclusions: Sulindac is capable of promoting ductal constriction in clinically stable preterm infants without compromising the renal function. The spectrum of gastrointestinal complications observed in sulindac treated infants were similar to those described for indomethacin. The use of sulindac for ductal closure in the preterm infant should remain experimental.     

Trapeziometacarpal joint instability affects the moment arms of thumb motor tendons

This study measured the changes in moment arm length of thumb motor tendons after simulated ligamentous instability and subsequent reconstruction of the trapeziometacarpal joint. Excursions of thumb motor tendons were measured simultaneously with the trapeziometacarpal joint angulation during flexion to extension and abduction to adduction motion. Tendon moment arms were calculated based on joint and tendon displacement techniques in the intact joint, after sequential sectionings of the capsuloligamentous restraints, and after the reconstruction procedure of Eaton and Littler. The results showed that moment arms of the abductor pollicis longus and extensor pollicis brevis tendons increased significantly as compared with those for normal joints during flexion to extension motion after sectioning the palmar capsuloligamentous components. After the ulnopalmar structures were cut, the moment arm of the extensor pollicis longus tendon had a statistically significant increase during abduction to adduction motion, and those of the extensor and flexor pollicis longus tendons decreased significantly during flexion to extension motion. Changed moment arms were restored to a normal level after the ligamentous reconstruction. These results indicate that ligamentous disruptions alter the mechanical balance of thumb motor tendons, which may contribute to joint deformities observed in trapeziometacarpal joint arthritis. Restoring joint stability is important to correct mechanical imbalance of the tendons.     

Development of cyclosporin A-loaded hyaluronic microsphere with enhanced oral bioavailability

To develop a hyaluronic microsphere with the improved oral bioavailability of poorly water-soluble cyclosporin A (CsA), the microspheres were prepared with varying ratios of sodium hyaluronate (HA)/sodium lauryl sulfate (SLS)/CsA using a spray-drying technique. The effects of HA and SLS on the dissolution and solubility of CsA in microspheres were investigated. The CsA-microsphere prepared with HA/SLS/CsA at the ratio of 4/2/1 gave the highest solubility and dissolution rate of CsA among those formulae tested. As solubility and dissolution rate of CsA were increased about 17- and 2-fold compared to CsA powder, respectively, this CsA-microsphere was selected as an optimal formula for oral delivery in rats. The CsA-microsphere and Sandimmun neoral sol gave significantly higher blood levels compared with CsA powder alone. Moreover, the AUC, T(max) and C(max) values of CsA in CsA-microsphere were not significantly different from those in Sandimmun neoral sol in rats, indicating that CsA-microsphere was bioequivalent to the commercial product in rats. Our results demonstrated that the CsA-microsphere prepared with HA and SLS, with improved bioavailability of CsA, might have been useful to deliver a poorly water-soluble CsA.     

Supercritical CO2 Curing of Resource-Recycling Secondary Cement Products Containing Concrete Sludge Waste as Main Materials

This study aims to develop highly durable, mineral carbonation-based, resource-recycling, secondary cement products based on supercritical carbon dioxide (CO₂) curing as part of carbon capture utilization technology that permanently fixes captured CO₂. To investigate the basic characteristics of secondary cement products containing concrete sludge waste (CSW) as the main materials after supercritical CO₂ curing, the compressive strengths of the paste and mortar (fabricated by using CSW as the main binder), ordinary Portland cement, blast furnace slag powder, and fly ash as admixtures were evaluated to derive the optimal mixture for secondary products. The carbonation curing method that can promote the surface densification (intensive CaCO₃ formation) of the hardened body within a short period of time using supercritical CO₂ curing was defined as “Lean Carbonation”. The optimal curing conditions were derived by evaluating the compressive strength and durability improvement effects of applying Lean Carbonation to secondary product specimens. As a result of the experiment, for specimens subjected to Lean Carbonation, compressive strength increased by up to 12%, and the carbonation penetration resistance also increased by more than 50%. The optimal conditions for Lean Carbonation used to improve compressive strength and durability were found to be 35 °C, 80 bar, and 1 min.