Pharmacokinetics and safety of repirinast tablets in healthy Chinese subjects

ABSTRACT Repirinast is a new, synthetic, disodium cromoglycate-like antiallergic agent for oral administration in humans. This study evaluated the safety, tolerability and pharmacokinetics of repirinast tablets in healthy Chinese volunteers. This was a phase I, open-label, randomized, single- and multiple-dose study. Subjects were assigned to receive a single dose of repirinast tablet at either 150, 300, or 450 mg, or multiple doses of 150 mg twice daily for 5 days. Plasma samples were analyzed with LC-MS/MS. Pharmacokinetic parameters of active metabolite MY-1250 (deesterified repirinast) were calculated using non-compartmental analysis with WinNonlin software. Statistical analysis was performed using SPSS software. All adverse events (AEs) were mild and of limited duration. No serious adverse event (SAE), death or withdrawal from the study was observed. In the single-dose study, Cmax was reached at about 0.75 hour, and the mean t1/2 was approximately 16.21 hours. Area under curve (AUC) and Cmax increased with dose escalation, but dose proportionality was not observed over the range of 150 to 450 mg. In the multiple-dose study, the steady-state was reached within 3 days with no accumulation. Repirinast tablet was well tolerated in healthy Chinese subjects.

Single lesion leprosy pacients multicentric cohort treated with single dose drug therapy: findings on three-year follow-up and public health perspective in Brazil

Single skin lesion, paucibacillary (SSL-PB) leprosy is considered and early disease manifesation. This study the clinical outcome of a cohort of 259 newly diagnosed SSL-PB treated with one dose of rifampicin, ofloxacin, minocycline (ROM) and followed-up for three-years. Patients were recruited from the North, Central West and Southeast regions in Brazil (1997-2001). The result expected with ROM therapy was disappearance or the reduction of lesion size. Manifestation that required additional intervention were considered as poor clinical outcome: type-1 reaction (T1R) with or without neuritis alone, increase in lesion size and shift from paucibacillary to multibacillary. The incidence of poor clinical outcome was calculated by person-month and with the Kaplan-Meier methods. 61.8% of the participants were females, mean age 32.2, and 67,2% had borderline tuberculoid (BT) or tuberculoid forms. T1R was the predominant event; shift from paucibacillary to multibacillaru was rare. 92.0% of the volunteers shown no events during the first year, the same occurring to 80.6% of them after 3 years of clinical monitoring. The probability of remaining event-free was highest among those 40 years old or younger. Poor outcome predominated among BT patients. Extended monitoring of SSL-PB leprosy cases under minimal therapy provided valuable case management information for reference centers.