A Competent and Commercially Viable Process for the Synthesis of the Anti-Hypertensive Drug Olmesartan Medoxomil

Drug product purity and potency are of most significance in the regulatory market as we notice many recalled batches worldwide, particularly in the US and Japan. Olmesartan Medoxomil is an anti-hypertensive drug. The present invention relates to a process for the preparation of Olmesartan Medoxomil with 99.9% purity in an overall 62% yield. The synthesis includes three isolations and one purification with easy plant operations. This process describes the formation and control of each individual impurity in all stages. This process for Olmesartan Medoxomil and its intermediates is competent for industrial production in very short reaction time intervals with an appreciable yield and high purity.     

Synthesis and Characterization of Impurities in the Production Process of Lopinavir

Lopinavir is an antiretroviral drug used for the inhibition of HIV protease. Four related substances of lopinavir were observed during the manufacturing process of lopinavir in the laboratory and they were identified. The present work describes the origin, synthesis, characterization, and control of these related substances.     

Constraining eye movement when redirecting walking trajectories alters turning control in healthy young adults

Humans use a specific steering synergy, where the eyes and head lead rotation to the new direction, when executing a turn or change in direction. Increasing evidence suggests that eye movement is critical for turning control and that when the eyes are constrained, or participants have difficulties making eye movements, steering control is disrupted. The purpose of the current study was to extend previous research regarding eye movements and steering control to a functional walking and turning task. This study investigated eye, head, trunk, and pelvis kinematics of healthy young adults during a 90° redirection of walking trajectory under two visual conditions: Free Gaze (the eyes were allowed to move naturally in the environment), and Fixed Gaze (participants were required to fixate the eyes on a target in front). Results revealed significant differences in eye, head, and trunk coordination between Free Gaze and Fixed Gaze conditions (p < 0.001). During Free Gaze, the eyes led reorientation followed by the head and trunk. Intersegment timings between the eyes, head, and trunk were significantly different (p < 0.05). In contrast, during Fixed Gaze, the segments moved together with no significant differences between segment onset times. In addition, the sequence of segment rotation during Fixed Gaze suggested a bottom-up postural perturbation control strategy in place of top-down steering control seen in Free Gaze. The results of this study support the hypothesis that eye movement is critical for the release of the steering synergy for turning control.     

Do stand-alone interbody spacers with integrated screws provide adequate segmental stability for multilevel cervical arthrodesis?

Background contextSome postoperative complications after anterior cervical fusions have been attributed to anterior cervical plate (ACP) profiles and the necessary wide operative exposure for their insertion. Consequently, low-profile stand-alone interbody spacers with integrated screws (SIS) have been developed. Although SIS constructs have demonstrated similar biomechanical stability to the ACP in single-level fusions, their role as a stand-alone device in multilevel reconstructions has not been thoroughly evaluated.PurposeTo evaluate the acute segmental stability afforded by an SIS device compared with the traditional ACP in the setting of a multilevel cervical arthrodesis.Study designIn vitro human cadaveric biomechanical analysis.MethodsThirteen human cadaveric cervical spines (C2–T1) were nondestructively tested with a custom 6 df spine simulator under axial rotation, flexion-extension, and lateral bending loading. After intact analysis, eight single-levels (C4–C5/C6–C7) from four specimens were instrumented and tested with ACP and SIS. Nine specimens were tested with C5–C7 SIS, C5–C7 ACP, C4–C7 ACP, C4–C7 ACP+posterior fixation, C4–C7 SIS, and C4–C7 SIS+posterior fixation. Testing order was randomized with each additional level instrumented. Full range of motion (ROM) data were obtained and analyzed by each loading modality, using mean comparisons with repeated measures analysis of variance. Paired t tests were used for post hoc analysis with Sidak correction for multiple comparisons.ResultsNo significant difference in ROM was noted between the ACP and SIS for single-level fixation (p>.05). For multisegment reconstructions (two and three levels), the ACP proved superior to SIS and intact condition, with significantly lower ROM in all planes (p<.05). When either the three-level SIS or ACP constructs were supplemented with posterior lateral mass fixation, there was a greater than 80% reduction in ROM under all testing modalities (p<.05), with no significant difference between the ACP and SIS constructs (p>.05).ConclusionsThe SIS device may be a reasonable option as a stand-alone device for single-level fixation. However, SIS devices should be used with careful consideration in the setting of multilevel cervical fusion. However, when supplemented with posterior fixation, SIS devices are a sound biomechanical alternative to ACP for multilevel fusion constructs.     

A randomized, double-masked trial of topical ketorolac versus artificial tears for treatment of viral conjunctivitis

OBJECTIVE: To determine if topical ketorolac 0.5% relieves the symptoms and signs of viral conjunctivitis better than artificial tears. DESIGN: Randomized, controlled trial. PARTICIPANTS: One hundred seventeen patients with a clinical diagnosis of viral conjunctivitis were randomized to the treatment group or control group. METHODS: Physicians and patients were masked to treatment. Patients in the treatment group received topical ketorolac 0.5% four times daily. Patients in the control group received artificial tears four times daily. Symptom and sign scores were recorded on the day of recruitment and at the time of a follow-up examination 3 to 4 days later. MAIN OUTCOME MEASURES: Change in six symptoms of conjunctivitis (overall discomfort, itching, foreign body sensation, tearing, redness, and lid swelling) and four signs of conjunctivitis (conjunctival injection, conjunctival chemosis, conjunctival mucus, and lid edema). Adverse effects were also studied. RESULTS: A total of 105 patients returned for their 3- to 4-day follow-up. Both the artificial tear and ketorolac groups showed improvement in all symptom scores at their 3- to 4-day follow-up visit. There was no statistically significant difference between the change in symptom scores between the treatment group and control group in any symptom category except redness. Patients in the control group were more likely to report improvement in redness than those in the treatment group, P = 0.012. There was no statistically significant difference between the change in sign scores between the treatment and control groups. Ketorolac 0.5% was more likely to produce stinging than artificial tears, 59.2% versus 18.8%, P < 0.001. CONCLUSIONS: Topical ketorolac 0.5% used four times daily is no better than artificial tears at relieving the symptoms or signs of viral conjunctivitis and produces more stinging than artificial tears.