master.on
New Member
By dissolving Testosterone or any of its esters in
hydroxypropyl-P-cyclodextrin
https://www.caymanchem.com/product/16169
By doing so, a WAY better absoption than Andriol is achieved
(8-13 TIMES better absoption!)
Patent EP2925369A1 - Aqueous oral solutions of steroid hormones and hydroxypropyl-beta-cyclodextrin with optimised bioavailability
Example 9 - Comparative pharmacokinetic tests (Testosterone)
The solutions described in example 8 were used in a comparative clinical study of pharmacokinetics (Figura 8 Tables 6-8). Three healthy female subjects , non or ex-smokers, with an age of between 18 and 75 years received, according to a crossover design, a single dose of 26 mg of Testosterone dissolved in the aforementioned solution or 40 mg of Testosterone undecanoate corresponding to 25.26 mg of Testosterone, in soft capsules (reference formulation on the market, Andriol). Tables 6-8 shows the results of the pharmacokinetics parameters obtained by the clinical study: Table 6 and 7 refer to the Testosterone formulations, object of the present patent, with respectively a molar ratio between HP CD and Testosterone of 2: 1 and 3: 1, whereas Table 8 refers to the commercial reference formulation (Andriol).
The results reported in Tables 6 and 7 show that the present composition generates an overall exposure per unit dose (AUC/dose) 13-fold ca. higher than that obtained with the Reference formulation (Table 8) ***(Andriol)*** in the case of a complex with molar ratio HPBCD:Tst 2: 1 and of 8 times higher than that obtained with the Reference formulation (Table 8) in the case of a complex with molar ratio HPBCD:Tst 3: 1. Similarly the peak concentrations per unit dose (Cmax/Dose) are, for both complex solutions, higher than that obtained with the reference formulation. Moreover, the peak time (tmax) achieved with the HPBCD:Tst solutions is substantially lower as compared to that of the Reference formulation. The results confirm those obtained in Experiment 5 (figures 5 and 6) and shown that the HPBCD:Tst complexes maintain a remarkable bioavailability despite being likely subject to the hepatic first-pass effect. A dose-effective treatment of Testosterone complexes with HP CD via the oral route (more patient-friendly than e.g. complexes with HPβCD via the oral route (more patient- friendly than e.g. the sublingual/ buccal/ nasal route) is therefore obtained. As a further advantage, the composition of the invention makes it possible to significantly reduce the inter-individual variability of the plasma levels, expressed in the table by the CV% of AUC and Cmax, with respect to the commercial formulation of Table 8.
Just for information purposes as it seems to be an active patent about it.
(idk if they would give a shit about patents as Test is already a controlled substance in most countries).
hydroxypropyl-P-cyclodextrin
https://www.caymanchem.com/product/16169
By doing so, a WAY better absoption than Andriol is achieved
(8-13 TIMES better absoption!)
Patent EP2925369A1 - Aqueous oral solutions of steroid hormones and hydroxypropyl-beta-cyclodextrin with optimised bioavailability
Example 9 - Comparative pharmacokinetic tests (Testosterone)
The solutions described in example 8 were used in a comparative clinical study of pharmacokinetics (Figura 8 Tables 6-8). Three healthy female subjects , non or ex-smokers, with an age of between 18 and 75 years received, according to a crossover design, a single dose of 26 mg of Testosterone dissolved in the aforementioned solution or 40 mg of Testosterone undecanoate corresponding to 25.26 mg of Testosterone, in soft capsules (reference formulation on the market, Andriol). Tables 6-8 shows the results of the pharmacokinetics parameters obtained by the clinical study: Table 6 and 7 refer to the Testosterone formulations, object of the present patent, with respectively a molar ratio between HP CD and Testosterone of 2: 1 and 3: 1, whereas Table 8 refers to the commercial reference formulation (Andriol).
The results reported in Tables 6 and 7 show that the present composition generates an overall exposure per unit dose (AUC/dose) 13-fold ca. higher than that obtained with the Reference formulation (Table 8) ***(Andriol)*** in the case of a complex with molar ratio HPBCD:Tst 2: 1 and of 8 times higher than that obtained with the Reference formulation (Table 8) in the case of a complex with molar ratio HPBCD:Tst 3: 1. Similarly the peak concentrations per unit dose (Cmax/Dose) are, for both complex solutions, higher than that obtained with the reference formulation. Moreover, the peak time (tmax) achieved with the HPBCD:Tst solutions is substantially lower as compared to that of the Reference formulation. The results confirm those obtained in Experiment 5 (figures 5 and 6) and shown that the HPBCD:Tst complexes maintain a remarkable bioavailability despite being likely subject to the hepatic first-pass effect. A dose-effective treatment of Testosterone complexes with HP CD via the oral route (more patient-friendly than e.g. complexes with HPβCD via the oral route (more patient- friendly than e.g. the sublingual/ buccal/ nasal route) is therefore obtained. As a further advantage, the composition of the invention makes it possible to significantly reduce the inter-individual variability of the plasma levels, expressed in the table by the CV% of AUC and Cmax, with respect to the commercial formulation of Table 8.
Just for information purposes as it seems to be an active patent about it.
(idk if they would give a shit about patents as Test is already a controlled substance in most countries).
