Proliposome testosterone undecanoate preparation

A technology of proliposome and testosterone undecanoate, which can be applied in the directions of liposome delivery, medical preparations with non-active ingredients, and medical preparations containing active ingredients, etc., and can solve problems such as performance differences.

Pending Publication Date: 2022-06-24
TESORX PHARMA LLC
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, the performance of currently marketed oral dosage forms of TU varies significantly depending on when an individual ingests the dosage form relative to meal times, see Yin et al.

Method used

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  • Proliposome testosterone undecanoate preparation
  • Proliposome testosterone undecanoate preparation
  • Proliposome testosterone undecanoate preparation

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0087] In vitro testing of TU proliposomal powder dispersion candidate formulations: TU release in phosphate buffer (pH 6.8). The percentage of TU released over time in phosphate buffer (pH 6.8) was determined for the following encapsulated TU proliposomal powder dispersion formulations: TSX-011; TSX-048; TSX:049 ; TSX-056; and TSX-057. For TSX-011 and TSX-048, n=3. n=6 for TSX-049, TSX-056 and TSX-057. The ingredients of each test formulation are described in Table 1. For solubility testing, one capsule was added, each to 250 mL of 0.2 M sodium triphosphate containing 1% w / v SLS. The final concentration of SLS in the composite medium was 0.25% w / v. The pH of the medium was adjusted to 6.8 using 2N HCl or 2N NaOH, and the dissolution conditions were maintained at 37±0.5°C for 4 hours at 75 RPM. Aliquots were collected at 0, 15, 30, 60, 90, 120 and 240 minutes and filtered using a 5μ glass fiber filter and then evaluated using high pressure liquid chromatography (HPLC). H...

Embodiment 2

[0092] In vitro testing of TU proliposomal powder dispersion candidate formulations: TU release under simulated small intestinal fluid fed state. The percentage of TU released over time in 0.1N HCl solution was determined for the following encapsulated TU proliposomal powder dispersion formulations: TSX-011; TSX-048; TSX:049; TSX-056; and TSX-057. n=6 for each formulation. The ingredients of each test formulation are described in Table 1. The 0.1N HCl dissolution medium simulates the fed state in small intestinal fluid. The dissolution of each capsule was performed in 750 mL of 0.1 N HCl and maintained at 37 ± 0.5 °C for 4 hours at 75 RPM. Aliquots were collected at 0, 15, 30, 60, 90, 120 and 240 minutes and filtered using a 5μ glass fiber filter and then evaluated using HPLC as described in Example 1. Solubility data such as figure 2 reported.

Embodiment 3

[0094] A single-dose study was designed to evaluate dose-response rates in female dogs. Dose response rates in dogs were assessed for TSX-011; TSX-048; TSX:049; TSX-056 and TSX-057. Each formulation was administered orally to female beagle dogs under fasting conditions. The ingredients of the application formulations are described in Table 1 . For the study, the dogs were fasted overnight and dosing (1 capsule / formulation / dog) was administered orally the next morning. The formulation dose for each formulation was normalized based on the body weight of each dog (mg of formulation administered / kg of body weight). See Table 2.

[0095] Table 2 Standardized formulation doses for dogs (administered per kg body weight)

[0096]

[0097] Blood samples were collected from each dog by jugular puncture 1 hour before oral administration, and then at 2, 4, 6, 8, 12, 15, 18, 21, and 24 hours after administration.

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Abstract

The present invention relates to a proliposome powder dispersion of testosterone undecanoate (TU) and a phospholipid, comprising a dispersion of TU and dipalmitoyl phosphatidylcholine (DPPC) wherein the weight / weight (w / w) ratio of TU: DPPC in the proliposome powder dispersion is about 1: 2; or TU and dimyristoyl phosphatidylcholine (DMPC), wherein the weight / weight (w / w) ratio of TU: DMPC in the proliposome powder dispersion is about 1: 3; or TU and 1-myristoyl-2-palmitoyl lecithin (MPPC), wherein the weight / weight (w / w) ratio of TU: MPPC in the proliposome powder dispersion is about 1: 3.

Description

[0001] CROSS-REFERENCE TO RELATED APPLICATIONS [0002] This application claims priority to US Application No. 62 / 884,919, filed August 9, 2019, which is incorporated herein in its entirety. technical field [0003] The present invention relates to proliposomal powder dispersions of testosterone undecanoate and phospholipids, and improved bioavailability of orally administered testosterone undecanoate. [0004] technical background [0005] The goal of testosterone replacement therapy (TRT) is to restore low endogenous plasma levels of testosterone to normal physiological levels. Restoring the patient's normal physiological levels can alleviate symptoms suggestive of hormone deficiencies or, for some individuals, lead to a more positive appearance and identity. A convenient form of TRT relies on oral administration of testosterone undecanoate (TU). However, the performance of currently marketed oral dosage forms of TU varies significantly depending on when an individual ing...

Claims

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Application Information

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IPC IPC(8): A61K9/00A61K9/127A61K9/48
CPCA61K9/4891A61K9/0053A61K9/1277A61K31/568A61P1/16A61P5/06A61P5/24A61P5/26A61P13/12A61P15/08A61K9/145A61K9/127A61K9/0095A61K47/24A61K47/26
Inventor V·G·卡达吉N·温卡德森N·K·斯瓦纳卡T·洪R·提鲁科特G·V·贝塔格里
Owner TESORX PHARMA LLC
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