To this regard, the expiry of the patent on Sild citrate in several European countries allowed the opportunity to release of a number of new formulations of Sild. It should be noted that most of the Sild formulations available on the market today are actually approved as bioequivalent forms of the original FCT Leoni et al. These novel formulations find improved compliance in those populations of patients with difficulty in swallowing conventional solid dosages, such as children, geriatric patients, and dysphagic patients.
In addition, by providing higher oral drug availability, orally disintegrating formulations may represent valued systems to favor trans-mucosal, and in particular sub-lingual, absorption Kathpalia and Gupte, In this study, we aimed to evaluate the possible pharmacokinetic variations, and the corresponding pattern of ADR, deriving from favoring the trans-mucosal absorption of Sild through the sub-lingual administration of the two available orally disintegrating formulations of the drug. Results were compared with the original formulation of Sild, namely the FCTs.
Interestingly, we found a strict correlation, both in vitro and in vitro , between the bio-technological properties and the PKs of the different formulations. In particular, in spite of an equal drug dosage 50 mg and slightly reduced rate of drug release in the dissolution test, ODF was characterized by a greater time to disaggregation and higher rate of permeation in the trans-mucosal model on the one hand, and by an increased drug bio-availability within the first hour from dosing, on the other hand.
We might then hypothesize that sub-lingual Sild absorption is favored by a prolonged drug-mucosa contact. Indeed, this phenomenon is generally pursued for oral trans-mucosal drugs, where the use of mucoadhesive polymers is recommended to assure prolonged period of contact between the formulation and the oral mucosa Lam et al. These preliminary results are also suggestive of a possible improvement of the clinical efficacy for this class of drugs compared to original formulations.
Further studies are warranted to clarify these aspects. This evidence can be interpreted in the light of the principle that the incidence of a drug side effect increases by increasing serum levels and the exposure time to the drug itself Gupta et al. In spite of an unvaried global bio-availability compared to the other formulations analyzed, the sub-lingual administration of ODF showed a lower value of C max and a shorter t max , resulting in a significantly higher proportion of Sild bio-available within the first hour from dosing.
Thus, we might speculate that the sub-lingual administration of ODF combines an efficient absorption of the drug with the achievement of average lower serum levels of Sild and a consequent lower risk of ADRs. However, we acknowledge the low sample size as the main drawback of the study.
Further investigation on larger cohorts and with different dosages are required to confirm this issue. In conclusion, in this study we report that sublingual administration of Sild ODF improves the drug tolerability profile through the likely involvement of a modified pharmacokinetic compared to generator FCTs. We are developing further comparative studies to assess the clinical efficacy in psychogenic and organic ED patients.
LDT and CF coordinated the study and drafted the manuscript. MDRP evaluated and enrolled the patients. EF performed in vitro analysis. SDA performed the serum analysis. RP performed the pharmacokinetics comparison. The authors declare that the research was conducted in the absence of any commercial or financial relationships that could be construed as a potential conflict of interest. We thank Dr. Alberto Barosso, Dr. Giuseppe Maggioni, and Dr. Dimitri Portale for patients counseling, Dr.
Flavia Rosano and Dr. Alice Passadore for patients managing, and all the staff of the Unit of Andrology and Reproductive Medicine. Representative chromatograms and mass spectra of both Sild at the internal standard benzanilide in real samples are reported B. C Representative image of residual oro-dispersible film highlighted by a discontinuous line , persisting after the permeation test in the device used for the in vitro estimate of trans-mucosal absorption through a cellulose acetate membrane.
Banner, L. Integrated sildenafil and cognitive-behavior sex therapy for psychogenic erectile dysfunction: a pilot study. Bischoff, E. Potency, selectivity, and consequences of non selectivity of PDE inhibition. Boolell, M. Sildenafil: an orally active type 5 cyclic GMP-specific phosphodiesterase inhibitor for the treatment of penile erectile dysfunction.
PubMed Abstract Google Scholar. Caretta, N. Resumption of spontaneous erections in selected patients affected by erectile dysfunction and various degrees of carotid wall alteration: role of tadalafil. Cavernous artery intima-media thickness: a new parameter in the diagnosis of vascular erectile dysfunction. Carvalheira, A. In the meantime, to ensure continued support, we are displaying the site without styles and JavaScript. Deveci S et al. Int J Urol 11 : — Reprints and Permissions.
Sublingual administration of sildenafil. Nat Rev Urol 2, 6—7 Conclusions: 20 mg sublingual sildenafil is safe and effective in the treatment of erectile dysfunction. Sublingual administration has some advantages as it is not effected by food ingestion and quickly appears in the circulation.
These advantages provide a faster onset of action with a lower dose when compared to oral sildenafil. It works faster when placed under the tongue than swallowing. While sublingual drugs have some disadvantages and side effects, it is generally safe and effective treatment for erectile dysfunction. Ross Davis is a fervent health writer and expert who loves writing about erectile dysfunction drugs. An expert with hands-on knowledge of Sildenafil and Tadalafil, he strives to educate men of all ages about the use and working of these medically-proven sexual performance enhancers.
Ross loves to help men understand these drugs and maximize its benefits with correct usage. His writing demonstrates his extensive knowledge in this niche, and he relishes simplifying the complexities associated with the use of erectile dysfunction drugs. He is also an avid seeker of knowledge who is always on the lookout for an opportunity to learn something new.
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