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Composition and method for oral delivery of androgen prodrugs

a technology of androgen prodrugs and composition methods, applied in the field of health sciences, can solve the problems of less than desirable efficacy or safety of pharmaceuticals, pharmacokinetic variability seen based on food effects, and the effect of orally administered lipophilic drugs

Inactive Publication Date: 2018-08-09
LIPOCINE
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Benefits of technology

[0006]The present inventors have surprisingly discovered oral testosterone undecanoate compositions that can be effectively administered to hypogonadal males with a meal without the fat content of the meal substantially effecting bioavailability. This result is unexpected and in direct contrast to the bioavailability performance reported for many other testosterone undecanoate oral formulations, which conclude that bioavailability is affected by meal fat content.

Problems solved by technology

A particularly difficult problem in regards to orally administered lipophilic drugs is pharmacokinetic variability seen based on food effects.
More complicated or specific food requirements for dosing can lead to less than desirable efficacy or safety of the pharmaceutical since; in general, a target population has quite variable eating habits.
These variables are difficult to control in a real world setting.

Method used

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Examples

Experimental program
Comparison scheme
Effect test

example 1

ct Clinical Study

[0110]This study was a single-center, open-label, randomized, cross-over, single-dose, four period, four-treatment study to examine the effect of food (fasted vs. high fat) and fat content of food on pharmacokinetics of testosterone & metabolites. 14 subjects were enrolled and 13 completed the study. 225 mg of TU (2 capsules (capsule fill containing 112.5 mg TU at about 15 wt % loading, 63 wt % Maisine 35-1, 16 wt % Cremophor RH 40, and 6 wt % PEG 8000) administered with:[0111]Treatment A: Standard-Fat with 20-35 wt % fat;[0112]Treatment B: Low-Fat with ˜15 wt % fat;[0113]Treatment C: High-Fat with ˜50 wt % fat; and[0114]Treatment D: overnight fasting, to hypogonadal males.

[0115]The meals were as follows in Table I with quantity specified as grams (g) or [% total calories].

TABLE ITotalEnergyTreatment(kcal)CarbohydratesProteinsLipidsA: Standard842.5115.2 g27.7 g30.1 gFat[54.7 wt %][13.2 wt %][32.1 wt %]B: Low Fat911.7  173 g17.8 g16.5 g[75.9 wt %][7.8 wt %][16.3 wt %...

example 2

lent Formulations and Oral Dosage Forms

[0119]The ordinary skilled artisan in view of these results can design and test formulations for bioequivalence (e.g., food effect bioequivalence) using the present disclosure.

[0120]Formulations for testing in a food effect study as described in Example 1 (or another appropriate designed study) can be designed e.g., by:

(1) varying the loading of testosterone undecanoate;

(2) varying the amount of Maisine 35-1, exchanging Maisine 35-1 for another lipophilic additive (in varying amounts) or including one or more additional lipophilic additives in addition to Maisine 35-1 (in varying amounts);

(3) varying the amount of Cremophor RH 40, exchanging Cremophor RH 40 for another hydrophilic additive (in varying amounts) or including one or more additional hydrophilic additives in addition to Cremophor RH 40 (in varying amounts);

(4) varying the amount of PEG 8000 (or not include PEG 8000), exchanging PEG 8000 for another solidifying agent (in varying amou...

example 3

Trial to Show Bioequivalence

[0122]To determine if a Test formulation is bioequivalent to the formulation used in Example 1, a bioequivalence study is performed under the same or similar conditions. One of ordinary skill in the art can design and perform a bioequivalence study in view of the results presented in Example 1. Test formulations can be generated according to this disclosure or more particularly Example 2. The bioequivalence study is one that may support the filing of an Abbreviated New Drug Application at the US FDA or similar application in jurisdictions outside of the United States with the appropriate regulatory agency.

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PUM

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Abstract

Provided oral testosterone undecanoate compositions can be administered to hypogonadal males with a meal without the fat content of the meal substantially effecting bioavailability.

Description

PRIORITY DATA[0001]This application is a continuation of U.S. patent application Ser. No. 15 / 183,691, filed Jun. 15, 2016, which claims the benefit of U.S. Provisional Application No. 62 / 175,931 filed Jun. 15, 2015 and U.S. Provisional Application No. 62 / 253,292 filed Nov. 10, 2015, each of which are incorporated by reference in their entireties.FIELD OF THE INVENTION[0002]Described herein are methods of treatment with pharmaceutical compositions and dosage forms. Accordingly, the present disclosure generally involves health sciences, the fields of chemistry, pharmaceutical sciences, and medicine.BACKGROUND OF THE INVENTION[0003]A particularly difficult problem in regards to orally administered lipophilic drugs is pharmacokinetic variability seen based on food effects. Many pharmaceuticals have important dosing requirements based on the effect of food on their pharmacokinetics. Some pharmaceuticals need to be taken without food. Some pharmaceuticals need to be taken with food. Other...

Claims

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Application Information

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Patent Type & Authority Applications(United States)
IPC IPC(8): A61K31/568A61K9/48A61J7/00A61J1/06A61J1/03A61K9/00A61J1/10
CPCA61K9/4866A61K9/4858A61J7/0076A61K31/568A61J1/06A61J1/035A61K9/0053A61J1/10
Inventor PATEL, MAHESH V.CHIDAMBARAM, NACHIAPPANNACHAEGARI, SATISH K.
Owner LIPOCINE
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