Delving into the Latest Updates on Laboratoires UPSA SAS with Synapse

Overview

A novel, 96-well plate-based assay to measure drug solubility is presented.The drugs were introduced into the wells of a microtiter plate, and water was subsequently added to each well.Then, after stirring, the suspensions were filtered under vacuum in all wells at once and drug concentration was measured by spectrophotometry.Two protocols to measure the aqueous solubility under a 96-well plate format were investigated.When the drug powder was weighted directly into the wells (protocol A), solubility values were quite reproducible (variation coefficient below 28% for 5 experiments) and not significantly different from those reported in the literature.However, this procedure was rather cumbersome.To overcome the tedious weighting of the substance, another protocol was developed.The drug was first solubilized in acetonitrile, and an aliquot of the solution was pipeted into the well.Acetonitrile was subsequently evaporated before adding the water (protocol B).In that case, the results were more scattered than those using protocol A.In addition, this protocol is not suitable for efflorescent drugs, as seen with caffeine.However, for screening purposes, protocol B is easy to use and faster.For both protocols, it is recommended to use at least 4 wells for each drug to test.Approx. 15 drugs can be tested in a single 96-well plate.It is reproducible, accurate, and easy to use.It can also accommodate a large range of solubility (from approx. 0.003 to approx. 20 mg/mL in this study).

01 Jan 1999·Clinical Drug Investigation

Placebo-Controlled Study of the Analgesic Efficacy of a Paracetamol 500mg /Codeine 30mg Combination Together with Low-Dose vs High-Dose Diclofenac in Rheumatoid Arthritis

Author: J. Glowinski ; E. Boccard

Objective: This double-blind randomized study was designed to compare paracetamol 500mg/codeine 30mg (PC) [3 times daily] plus diclofenac 50mg once a day with diclofenac 50mg twice a day (DI) over 7 days in two parallel groups of 30 patients with residual persisting pain despite adjusted basic therapy for rheumatoid arthritis (RA).Patients and Methods: Ten men and 50 women (aged 21 to 73 yr, mean 57 yr) with RA were included.The two groups were comparable before treatment.Efficacy was assessed by the patient every evening by: (a) pain scores rated on a 100mm visual analog scale [VAS]; (b) discomfort scores defining the activity level reduction [none, mild, moderate, severe]; (c) duration of morning stiffness; and (d) number of awakenings caused by the pain during the previous night.At the end of the study overall efficacy was assessed by the patient on a 5-point verbal scale and by the desire to continue the treatment (yes, no).Pain scores on VAS and on a 5-point verbal scale and Ritchie Index were assessed before [day 0 (D0)] and after (D7) treatment.Any adverse effects were recorded continuously during the study and overall tolerability was assessed at the end of the study.Results: Analgesic efficacy was not significantly different between the two groups on all criteria: global efficacy (good or very good: PC = 47%, DI = 44%), desire to continue the treatment (PC = 57%, DI = 47%), evolution of daily VAS pain score, difference from D0 to D7 on VAS (PC = -31.5mm, DI = -23.4mm) and the Ritchie index (PC = -2.2, DI = -2.2), duration of morning stiffness, number of awakenings.The number of patients presenting adverse effects (PC = 8, DI = 9), the number of withdrawals as a result of adverse effects causing cessation of treatment (PC = 3, DI = 1), and the overall tolerability assessment were not significantly different (good or very good: PC = 82%, DI = 87%).Conclusion: In RA, an inflammatory disease, the analgesic combination of paracetamol 500mg and codeine 30mg allowed a decrease in the NSAID dose for comparable relief of a residual persisting pain.

01 Dec 1997·Clinical Drug Investigation

Parenteral versus Oral Route Increases Paracetamol Efficacy

Author: O. Jarde ; E. Boccard

The analgesic efficacy and tolerability of parenteral versus oral paracetamol 1g were compared in 323 patients immediately after a hallux valgus plasty performed with local anaesthesia (31 men, 292 women, mean age 52 years). Using a multicentre, double-blind, double-placebo, randomised, parallel-group design, the effects of a single dose of propacetamol (PR) 2g [= paracetamol (PA) 1g], oral PA 1g and placebo (PL) were compared in the recovery room 5 hours (mean) after surgery in three parallel groups of patients with at least moderate pain on a 5-point verbal scale. Efficacy was assessed on pain scores rated on a 5-point verbal scale before administration (T0) and 0.25, 0.5, 0.75, 1, 2, 3, 4, 5 and 6 hours after administration and with an overall efficacy 5-point verbal score. Any adverse effects were recorded throughout the duration of the study. PR was statistically superior to PL on pain intensity difference (PID) from T30 minutes to T6 hours (Dunnett test), on maximum pain intensity difference (MAXPID) [p < 0.05] and summed pain intensity difference (SPID) [p < 0.05]. PA was statistically superior to PL at T1, T2, T4, T5 hours (Dunnett test), on MAXPID (p < 0.05) and SPID (p < 0.10). PR was statistically superior to PA on PID from T30 minutes to T4 hours, on MAXPID (p < 0.03) and SPID (p < 0.01). Overall efficacy was found by the patients to be superior with PR vs PA (p < 0.01), PR vs PL (p < 0.05), and PA vs PL (p < 0.10). The remedication time was significantly different between the three groups (p < 0.05). 10 patients experienced 1 adverse effect, PR: 3 (injection site pain, headache, vomiting), PA: 6 [nausea, tremor, injection site pain (3), malaise], PL: 1 (injection site pain). In conclusion, PR 2g (i.e. PA 1g) provided a significantly greater and longer analgesic effect than the same dosage in oral form.

100 Deals associated with Laboratoires UPSA SAS

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100 Translational Medicine associated with Laboratoires UPSA SAS

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Pipeline

Pipeline Snapshot as of 11 Jun 2025

The statistics for drugs in the Pipeline is the current organization and its subsidiaries are counted as organizations,Early Phase 1 is incorporated into Phase 1, Phase 1/2 is incorporated into phase 2, and phase 2/3 is incorporated into phase 3

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Current Projects

Drug(Targets)	Indications	Global Highest Phase

UP-257-13 ( AT1R )	Hypertension More	Discontinued
UP-275-22 ( AT1R )	Hypertension More	Discontinued
UP-116-77 ( TBXA2R )	Thromboembolism More	Discontinued
UP-202-32 ( Adenosine receptor )	Pain More	Pending
UP-45421 ( COX-2 )	Pain More	Pending