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Books: 0	Journals: 1	Articles: 4

Original

Pharmacokinetic and tolerability of i.m. disodium clodronate 200 mg/lidocaine 1%, given twice monthly, in comparison with i.m. disodium clodronate 100 mg/lidocaine 1%, given weekly, in healthy postmenopausal female patients

Milko Radicioni, Giovanni Cremonesi, Enrica Baraldi, Chiara Leuratti and Fabrizia Mariotti

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Volume 51 p. 313 - 322

Abstract

International Journal of Clinical Pharmacology and Therapeutics, Vol. 51 – No. 4/2013 (313-322)

Milko Radicioni¹, Giovanni Cremonesi², Enrica Baraldi², Chiara Leuratti³ and Fabrizia Mariotti²

¹CROSS Research S.A., Phase I Unit, Arzo, Switzerland, ²Chiesi Farmaceutici S.p.A., Parma, Italy and ³CROSS S.A., Arzo, Switzerland
Background: Clodronate is a bisphosphonate effective in the prevention and treatment of osteoporosis in postmenopausal women. Non-adherence to bisphosphonates, however, is a major issue in clinical practice. Simplifying dose regimens may increase compliance. Objectives: To assess bioequivalence between an intramuscular (i.m.) clodronate 200 mg/lidocaine 1% twice-a-month formulation and a clodronate 100 mg/lidocaine 1% weekly formulation in 32 postmenopausal women. Methods: In this double-blind, randomized, two-way crossover study, test and reference formulations were administered in single dose, with a 2-week wash-out between administrations. The primary endpoint was clodronic acid cumulative excretion in the first 24 hours after injection (Xu_0–24h). Cumulative excretion in the 72 hours post-dose (Xu_0–72h) and maximum excretion rate (Rate_max) were also evaluated. Bioequivalence was assumed if the 90% confidence intervals (CIs) of the geometric means ratios of the dose-normalized parameters were within the 80.00 – 125.00% range. Local tolerability was evaluated. Results: Mean Xu_0–24h values were 114.03 ±23.13 mg and 55.22 ±9.73 mg for clodronate 200 mg and 100 mg. The 90% CIs for dose-normalized Xu_0–24h, Xu_0–72h and Rate_max ere 95 –110%, 94 –107% and 95 – 113%. Local tolerability of both treatments was good. The differences in pain intensity between formulations were not sigificantly different at most assessment times. Headache was the only treatment-related adverse event. Conclusions: Bioequivalence of the two formulations was confirmed in terms of dose-normalized rate and amount of clodronic acid excretion. This result, together with the favorable tolerability of the novel 200 mg formulation, suggests the possibility of reducing the number of i.m. administrations from once-a-week to twice-a-month.Correspondence to:
Dr. Enrica Baraldi
Chiesi Farmaceutici S.p.A.
Medical Affairs DFI Department
Via Palermo, 26/A, 43100 Parma, Italy
Email: [email protected]

Bioavailability Section

Bioequivalence study of a novel orodispersible tablet of meloxicam in a porous matrix after single-dose administration in healthy volunteers

Milko Radicioni, Sandra Connolly, Federico Stroppolo, Gabriele Granata, Luca Loprete and Chiara Leuratti

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Volume 51 p. 234 - 243

Abstract

International Journal of Clinical Pharmacology and Therapeutics, Vol. 51 – No. 3/2013 (234-243)

Bioequivalence study of a novel orodispersible tablet of meloxicam in a porous matrix after single-dose administration in healthy volunteers

Milko Radicioni¹, Sandra Connolly², Federico Stroppolo³, Gabriele Granata³, Luca Loprete¹ and Chiara Leuratti⁴

¹CROSS Research S.A., Arzo, Switzerland, ²MDS Pharma Services (now Celerion), Early Clinical Research, Neptune, NJ, USA, ³Alpex Pharma S.A., Mezzovico, and ⁴CROSS S.A., Arzo, Switzerland
Background: Meloxicam is a non-steroidal anti-inflammatory drug, indicated for osteoarthritis exacerbations, rheumatoid arthritis and ankylosing spondylitis symptomatic treatment. Objective: To compare the bioavailability of a 15 mg meloxicam orodispersible tablet (ODT) and a reference 15 mg tablet in healthy volunteers. Methods: Two randomized, crossover, bioequivalence studies were conducted. In both studies, 28 volunteers were randomly assigned to receive test ODT and reference tablet formulations in single dose under fasting conditions in two study periods, with a 7-day (Study I) or 14-day (Study II) wash-out between administrations. Blood samples were collected at pre-specified times. Pharmacokinetic parameters were obtained by noncompartmental analysis. Bioequivalence was assumed if the 90% confidence interval of the test/reference ratio of the least-squares means for C_max, AUC_0–t and AUC_0–∞were within the 80.00 –125.00% range, according to the current guidelines. Results: All 28 subjects in Study I and 26 subjects in study II completed the study and were included in the analysis. The 90% confidence intervals of the geometric means ratios for the logtransformed C_max, AUC_0–t and AUC_0–∞were 87 – 96%, 88 – 96% and 87 – 96% in Study I, and 99 – 105%, 98 – 104% and 108 – 120% in Study II. Test product was characterized by a slightly earlier tmax than the reference, i.e., 4.9 ± 1.1 vs. 5.8 ± 2.6 hours in Study I (p = 1.000) and 3.8 ± 2.0 vs. 4.8 ±1.6 hours in Study II (p = 0.0054). The two drugs were well tolerated. Conclusions: Test and reference formulations met the regulatory criteria for bioequivalence in the fasting healthy volunteers enrolled.Correspondence to:
Dr. Chiara Leuratti
Cross S.A.
via L. Lavizzari 18
6850 Mendrisio, Switzerland
Email: [email protected]

Original

A novel finasteride 0.25% topical solution for androgenetic alopecia: pharmacokinetics and effects on plasma androgen levels in healthy male volunteers

Maurizio Caserini, Milko Radicioni, Chiara Leuratti, Ottavia Annoni, and Renata Palmieri

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Volume 52 p. 842 - 849

Abstract

International Journal of Clinical Pharmacology and Therapeutics, Vol. 52 – No. 10/2014 (842-849)

A novel finasteride 0.25% topical solution for androgenetic alopecia: pharmacokinetics and effects on plasma androgen levels in healthy male volunteers

Maurizio Caserini¹, Milko Radicioni², Chiara Leuratti², Ottavia Annoni², and Renata Palmieri¹

¹Polichem S.A., Lugano-Pazzallo, and ²CROSS Research S.A., Arzo, Switzerland
Objective: Finasteride, a selective inhibitor of type 2 5-α reductase isoenzyme, inhibits the conversion of testosterone to dihydrotestosterone (DHT) and is indicated in the treatment of male androgenetic alopecia. The study objective was to evaluate a newly developed finasteride 0.25% topical solution in comparison to the marketed finasteride 1 mg tablet, with respect to finasteride pharmacokinetics and suppressive effects on plasma DHT. Methods: 24 healthy men with androgenetic alopecia were randomized in a single center, open-label, parallel-group, exploratory study, and received either multiple scalp applications of the topical solution b.i.d. or oral doses of the reference tablet o.d. for 7 days. Plasma finasteride, testosterone and DHT concentrations were determined. Results: After multiple doses, mean (± SD) finasteride C_max and AUC_0–t corresponded to 0.46 ± 0.28 ng/mL and 6.64 ± 7.50 ng/mL×h for the topical solution and to 6.86 ± 1.78 ng/mL and 57.93 ± 29.38 ng/mL×h for the tablet. Plasma DHT was reduced by ~ 68 – 75% with the topical solution and by ~ 62 – 72% with the tablet. No relevant changes occurred for plasma testosterone with either treatment. No clinically significant adverse events occurred. Conclusions: A strong and similar inhibition of plasma DHT was found after 1 week of treatment with the topical and tablet finasteride ormulations, albeit finasteride plasma exposure was significantly lower with the topical than with the oral product (p < 0.0001).Correspondence to:
Dr. Renata Palmieri
Polichem S.A.
Via Senago 42D
CH-6912, Lugano-Pazzallo, Switzerland
Email: [email protected]

Original

Effects of a novel finasteride 0.25% topical solution on scalp and serum dihydrotestosterone in healthy men with androgenetic alopecia

Maurizio Caserini, Milko Radicioni, Chiara Leuratti, Emanuela Terragni, Matilde Iorizzo, and Renata Palmieri

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Volume 54 p. 19 - 27

Abstract

International Journal of Clinical Pharmacology and Therapeutics, Vol. 54 – No. 1/2016 (19-27)

Effects of a novel finasteride 0.25% topical solution on scalp and serum dihydrotestosterone in healthy men with androgenetic alopecia

Maurizio Caserini¹, Milko Radicioni², Chiara Leuratti², Emanuela Terragni², Matilde Iorizzo³, and Renata Palmieri¹

¹Polichem S.A., Lugano-Pazzallo, ²CROSS Research S.A., Phase I Unit, Arzo, and ³Private Practice in Dermatology, Bellinzona, Switzerland
Objective: The effects on scalp and serum dihydrotestosterone (DHT) of different doses of a novel topical solution of 0.25% finasteride (P-3074), a type 2 5α-reductase, were investigated in men with androgenetic alopecia. Methods: Two randomized, parallel-group studies were conducted. Study I: 18 men received 1 mL (2.275 mg) P-3074, applied to the scalp once a day (o.d.) or twice a day (b.i.d), or 1 mg oral tablet o.d. for 1 week. Study II: 32 men received P-3074 at the dose of 100 (0.2275 mg), 200 (0.455 mg), 300 (0.6285 mg), or 400 (0.91 mg) μL or the vehicle o.d. for 1 week. Scalp and serum DHT and serum testosterone were evaluated at baseline and treatment end. Results: Change from baseline in scalp DHT was –70% for P-3074 o.d. and approx. –50% for P-3074 b.i.d. and the tablet. Serum DHT decreased by 60 – 70%. The doses of 100 and 200 μL P-3074 resulted in a –47/–52% scalp DHT reduction, similar to the 300 and 400 μL doses (i.e., –37/–54%). A –5.6% inhibition was observed for the vehicle. Serum DHT was reduced by only –24/–26% with 100 and 200 μL P-3074 and by –44/–48% with 300 and 400 μL P-3074. No relevant changes occurred for serum testosterone. Conclusions: The novel finasteride 0.25% solution applied o.d. at the doses of 100 and 200 μL results in an appropriate inhibition of scalp DHT potentially minimizing the untoward sexual side-effects linked to a systemic DHT reduction.Correspondence to:
Renata Palmieri
Polichem S.A.
Via Senago 42D
CH-6912, Lugano-Pazzallo, Switzerland
Email: [email protected]

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