Controlled release nasal testosterone gel, method for nasal administration, and pre-filled multi-dose applicator system

A testosterone, gel technology, applied in the field of controlled release nasal testosterone gel, for nasal administration and prefilled multi-dose applicator system, can solve unnecessary, high testosterone protein binding, short hormone elimination half-life and other issues, to achieve the effect of safe use, good tolerance, and easy mass production

Pending Publication Date: 2019-12-27
ACERUS BIOPHARMA INC
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Again, this rate is unnecessary for sex hormone replacement therapy and is undesirable given the short elimination half-life of hormones
[0017] In addition to the above "release / absorption" issues related to sex hormones and bioavailability and almost exclusively critical hepatic metabolism and short half-life issues, there is also the issue of protein binding of high testosterone in circulating plasma in both men and women

Method used

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  • Controlled release nasal testosterone gel, method for nasal administration, and pre-filled multi-dose applicator system
  • Controlled release nasal testosterone gel, method for nasal administration, and pre-filled multi-dose applicator system
  • Controlled release nasal testosterone gel, method for nasal administration, and pre-filled multi-dose applicator system

Examples

Experimental program
Comparison scheme
Effect test

preparation example Construction

[0120] The preparation of intranasal testosterone gel is carried out by thickening oil mixture and blow-fill-seal technology packaging.

[0121] A lipophilic vehicle, eg, castor oil, and a supersolvent, eg, DMI, (step 1) are introduced into a mixing vessel (eg, FrymaKoruma Vacuum-Mixing, Dispersing and Homogenising machine type Dinex700). The support and supersolvent mixture is blanketed with nitrogen (step 2) to vent oxygen and preheated, eg, to about 40°C to about 50°C.

[0122] The sieved (mesh size about 2mm) testosterone (step 3) was added to the carrier and supersolvent mixture and processed to obtain the intermediate product as follows.

[0123] Controlling the temperature of the vehicle and supersolvent mixture is necessary in the following steps to prevent a significant increase in temperature due to the shear strength applied to dissolve the testosterone.

[0124]

[0125] Homogenization of the intermediate product is carried out by controlling the temperature of...

preparation Embodiment

[0165] Examples of testosterone gels of the present invention are exemplified in Tables 1-3 below.

[0166] Table 1

[0167]

[0168] * Applied micronization

[0169] Table 2

[0170]

[0171] *Preferably applied micronization

[0172] table 3

[0173]

[0174] *Preferably applied micronization

[0175] Intranasal testosterone gel formulations 14-21 are further examples (per 100 parts) of gel formulations contemplated by the present invention. Testosterone in micronized form is preferred.

[0176] gel 14

[0177]

[0178] gel 15

[0179]

[0180] gel 16

[0181]

[0182]

[0183] gel 17

[0184]

[0185] gel 18

[0186]

[0187] gel 19

[0188]

[0189] gel 20

[0190]

[0191]

[0192] gel 21

[0193]

[0194] Italicized is "surfactant"

[0195] gel 22

[0196]

[0197] gel 23

[0198]

[0199] gel 24

[0200]

[0201]

[0202] gel 25

[0203]

[0204] gel 26

[0205]

[0206] gel 27

...

Embodiment 2

[0221] Two dosage levels of an intranasal testosterone gel formulation, Trimel, in healthy adult male subjects Biopharma, Inc., Compleo of Canada TM Bid opening, balanced, random selection, crossover, two-group, two-treatment (dose level 1 and 2), two-stage pharmacokinetic study

[0222] Test product for: Testosterone gel for nasal administration.

[0223] Profile Level 1:

[0224] A syringe, prefilled with 4.5% testosterone gel, delivering 6.75 mg of testosterone per nostril (manufactured by Trimel Biopharma, Inc. Canada). The formulation is as follows:

[0225] 4.5% Testosterone

[0226] 4% M1944

[0227] 3% (SiO 2 )

[0228] 88.5% castor oil.

[0229] Profile Level 2:

[0230] Compleo TM Syringe, prefilled with 6.5% testosterone gel, delivering 9.75 mg testosterone per nostril (manufactured by Trimel Biopharma, Inc. Canada), based on 150 mg Compleo TM Gel prefill weight. Compleo TM The gel formulation is as follows:

[0231]

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Abstract

The present invention relates to a controlled release nasal testosterone gel, a method for nasal administration, and a pre-filled multi-dose applicator system. Specifically, the present invention relates to an intranasal testosterone gel for controlled release of testosterone into the systemic circulatory system of males and females, thereby providing a constant effective testosterone blood levelafter nasal administration without causing an undesirable peak in testosterone blood level. The intranasal testosterone gel of the present invention is safe, convenient to use, good in tolerance, stable, and easy and reproducible for large-scale production. The novel intranasal testosterone gel of the present invention is uniquely suitable for testosterone replacement or supplemental treatment andis effective in treating males diagnosed with, for example, male testosterone deficiency and females diagnosed with, for example, female sexual dysfunction. The invention also relates to a method fornasal administration of the nasal testosterone gel of the invention and a pre-filled multi-dose airless applicator system.

Description

[0001] This application is an application number 201280035162.8, the application date is May 15, 2012, and the invention title is "Controlled Release Nasal Testosterone Gel, Method for Nasal Administration and Prefilled Multi-dose Applicator System" in China A divisional application of a patent application. technical field [0002] The present invention relates to intranasal testosterone gels for the controlled release of testosterone into the systemic circulation in men and women after nasal administration, providing constant effective testosterone blood levels over the life of the dose without causing unwanted Peak testosterone blood levels, which are indicated for testosterone replacement or supplementation therapy and are effective in treating men and women in need of testosterone replacement or supplementation therapy, for example, testosterone deficiency in men or sexual dysfunction in women. The present invention also relates to methods and prefilled multi-dose applicat...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/06A61K31/568A61K47/10A61K47/14A61K47/44A61M31/00A61P5/26A61P15/00A61P15/08A61P25/24
CPCA61K9/0043A61K31/568A61K47/34A61K47/44A61M31/00A61P15/00A61P15/02A61P15/08A61P15/10A61P25/24A61P5/24A61P5/26A61K9/06A61K47/02
Inventor W·克雷普聂S·福加尔蒂W·奥别瑞吉尔P·J·P·M·梅斯
Owner ACERUS BIOPHARMA INC
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