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Proliposomal testosterone undecanoate formulations

A proliposome and testosterone undecanoate technology, which can be used in liposome delivery, medical preparations containing active ingredients, drug combinations, etc., and can solve problems such as significant performance differences

Inactive Publication Date: 2018-09-28
WESTERN UNIV OF HEALTH SCI +1
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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

Method used

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  • Proliposomal testosterone undecanoate formulations
  • Proliposomal testosterone undecanoate formulations
  • Proliposomal testosterone undecanoate formulations

Examples

Experimental program
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preparation example Construction

[0046] Preparation of Proliposome Powder Dispersion

[0047] The proliposomal powder dispersion of the present invention can be prepared by dissolving TU in a solvent. Heat (eg, 45 to 55° C.) can optionally be applied during dissolution. The solvent is any solvent in which TU dissolves, but is preferably a water-miscible solvent such as ethanol; however, the solvent should generally not contain 10% or more water (vol / vol). Other exemplary solvents include methanol, chloroform, dichloromethane, acetone, isopropanol, and diethyl ether. After TU was dissolved (ie the solution became clear), DSPC was also dissolved in the TU solution until the solution became clear again. The solvent is removed by any suitable technique, such as by evaporation, by placing the solution under vacuum, by spray drying, or by use of a drying gas or the like. The solvent removal process was continued until a dry mass of TU and DSPC dispersion was formed. The average particle size of the resulting ...

Embodiment

[0067] Example 1. Testosterone Undecanoate Uncoated, Lipid Free Control Formulation TU1-044. To prepare TU1-044, 95 mg of testosterone undecanoate (TU) purchased from Pfizer Inc., Kalamazoo, MI was weighed and manually filled to uncoated size 1 Plus capsules.

[0068] Example 2. Enteric-coated testosterone undecanoate, lipid-free control preparation TU1-076. To prepare TU1-076, 95 mg of testosterone undecanoate (TU) purchased from Pfizer Inc., Kalamazoo, MI was weighed and manually filled to uncoated size 1 Plus capsules. The filled capsules were coated with methacrylic acid copolymer NF, type C ( L 30D-55). Plus capsules contain United States Pharmacopeia (USP) grade hydroxypropyl methylcellulose and water.

Embodiment 3

[0069] Example 3. Testosterone undecanoate + DSPC + cholesterol (1.0:0.9:0.1) preparation TU1-040. To prepare TU1-040, TU (3.95 g) was dissolved in 19 mL of EtOH at 45 to 55 °C and mixed until a clear solution formed. Distearoylphosphatidylcholine (DSPC) (3.55 g) and cholesterol (0.395 g) were added to the drug solution, and the mixture continued to mix at 45 to 55° C. until a clear solution formed. Mixing and heating were continued under vacuum until a dried mass formed. Pass the dried material through a No. 60 screen. Fill dried and sieved powder to uncoated size "0" Plus capsules.

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Abstract

Novel testosterone undecanoate (TU) formulations are disclosed in which TU is incorporated into proliposomal powder dispersions of TU and distearoyl phosphatidylcholine (DSPC). The proliposomal powderdispersions of the invention can also be combined with pharmaceutically acceptable excipients, and incorporated into enterically coated oral dosage forms that are useful for testosterone replacementtherapy.

Description

[0001] Cross References to Related Applications [0002] This application claims priority to US Provisional Application No. 62 / 276,452, filed January 08, 2016, and US Provisional Application No. 62 / 394,576, filed September 14, 2016. technical field [0003] The present invention relates to proliposomal powder dispersion formulations and oral dosage forms for improved delivery of testosterone undecanoate. Background technique [0004] The goal of testosterone replacement therapy (TRT) is to restore plasma testosterone levels to the normal range and relieve symptoms suggestive of hormone deficiency or, in some individuals, a more androgenic appearance and characteristics. This can be achieved in a number of ways, but a convenient form of TRT relies on the oral administration of testosterone undecanoate (TU). 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...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/127
CPCA61K9/0053A61K9/4866A61K9/4891A61K31/568A61K9/1277A61K31/685A61P1/16A61P13/12A61P5/06A61P15/08A61P5/24A61P5/26A61K2300/00A61K9/1617A61K9/1652C07J9/005
Inventor 古鲁·贝塔格里拉马钱德兰·提鲁科特维兰·高达·卡达吉纳塔拉詹·文卡特桑
Owner WESTERN UNIV OF HEALTH SCI
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