44 results about "Testosterone undecanoate" patented technology

A pharmaceutical formulation of testosterone undecanoate is provided. Methods of treating a testosterone deficiency or its symptoms with the inventive formulations are also provided.

The present disclosure is drawn to pharmaceutical compositions and oral dosage forms containing testosterone undecanoate, as well as related methods of treatment. In one embodiment, the oral dosage form can include a therapeutically effective amount of testosterone undecanoate and a pharmaceutically acceptable carrier. The dosage form can be formulated such that, when measured using a USP Type II apparatus in 1000 mL of 8 wt % Triton X-100 in water at 37° C. and 100 rpm, the oral dosage form releases at least 20% more testosterone undecanoate after the first 120 minutes than an equivalent dose testosterone undecanoate containing oral dosage form without the pharmaceutically acceptable carrier.

The present invention relates to a method of preventing or treating benign estrogen sensitive gynecological disorders in a female mammal, wherein the method comprises the administration to said female mammal of a combination of progestogen and androgen in an amount that is therapeutically effective to prevent or reduce the symptoms of these disorders. The present method is particularly suitable for preventing or treating disorders selected from the group consisting of endrometriosis, adenomyosis, uterine fibroids, dysmenorrhoea, menorrhagia and metrorrhagia. Another aspect of the invention relates to a pharmaceutical kit comprising a plurality of oral dosage units which comprise a progestogen in an amount equivalent to 3-500 μg levonorgestrel and either 5 to 250 mg dehydroepiandrosterone or 1 to 50 mg testosterone undecanoate.

A formulation for male contraception comprising a progestin possessing both estrogenic and androgenic properties is remarkably effective for spermatogenesis suppression in males. The progestin Norethisterone (NET), particularly its derivatives Norethisterone acetate and Norethisterone enanthate in sufficient doses induce oligozoospermia or azoospermia in males. Formulations further comprising an androgen, such as a testosterone derivative such as a testosterone ester, particularly testosterone undecanoate, are especially effective male contraceptive formulations.

A formulation for male contraception comprising a progestin possessing both estrogenic and androgenic properties is remarkably effective for spermatogenesis suppression in males. The progestin Norethisterone (NET), particularly its derivatives Norethisterone acetate and Norethisterone enanthate in sufficient doses induce oligozoospermia or azoospermia in males. Formulations further comprising an androgen, such as a testosterone derivative such as a testosterone ester, particularly testosterone undecanoate, are especially effective male contraceptive formulations.

The present invention relates to pharmaceutical compositions, formulated for injectable administration, which comprises a testosterone ester, in particularly testosterone undecanoate, in a vehicle comprising castor oil and a co-solvent. Upon injecting the compositions according to a particular administration scheme, reliable levels of testosterone in serum in the normal physiological range is achieved for a long period. This allows for the use of the compositions in hormone replacement therapy and male contraception without concomitant monitoring of testosterone levels in serum by a physician.

The present disclosure is drawn to pharmaceutical compositions and oral dosage capsules containing testosterone undecanoate, as well as related methods. The capsule includes a capsule shell and a capsule fill. The capsule fill can include a solubilizer and about 14 wt % to about 35 wt % testosterone undecanoate based on the total capsule fill. The oral dosage capsule is such that when a single oral administration to a male subject of one or more capsules with a total testosterone undecanoate daily dose of about 350 mg to about 650 mg it provides a ratio of serum testosterone Cmax to serum testosterone Cave of about 2.7 or less. In yet another embodiment, a method for providing a serum concentration of testosterone within a target serum testosterone concentration Cave range for a male subject is provided.

The present invention relates to pharmaceutical compositions, formulated for injectable administration, which comprises a testosterone ester, in particularly testosterone undecanoate, in a vehicle comprising castor oil and a co-solvent. Upon injecting the compositions according to a particular administration scheme, reliable levels of testosterone in serum in the normal physiological range is achieved for a long period. This allows for the use of the compositions in hormone replacement therapy and male contraception without concomitant monitoring of testosterone levels in serum by a physician.

The present disclosure is drawn to pharmaceutical compositions and oral dosage capsules containing testosterone undecanoate, as well as related methods. The capsule includes a capsule shell and a capsule fill. The capsule fill can include a solubilizer and about 14 wt % to about 35 wt % testosterone undecanoate based on the total capsule fill. The oral dosage capsule is such that when a single oral administration to a male subject of one or more capsules with a total testosterone undecanoate daily dose of about 350 mg to about 650 mg it provides a ratio of serum testosterone Cmax to serum testosterone Cave of about 2.7 or less. In yet another embodiment, a method for providing a serum concentration of testosterone within a target serum testosterone concentration Cave range for a male subject is provided.

Methods for modulating one or more side effects of 5-α-reductase inhibitor therapy are provided, where the method includes administering a 5-α-reductase inhibitor and testosterone undecanoate. Also provided are methods of maintaining or restoring a DHT serum level in an individual undergoing 5-α-reductase inhibitor therapy, where the method includes administering testosterone undecanoate in addition to 5-α-reductase inhibitor. Further provided are methods of treating or preventing a DHT-related condition, such as benign prostate hyperplasia (BPH) or prostate cancer by administering a 5-α-reductase inhibitor and testosterone undecanoate.

The present disclosure is drawn to pharmaceutical compositions and oral dosage capsules containing testosterone undecanoate, as well as related methods. The capsule includes a capsule shell and a capsule fill. The capsule fill can include a solubilizer and about 14 wt % to about 35 wt % testosterone undecanoate based on the total capsule fill. The oral dosage capsule is such that when a single oral administration to a male subject of one or more capsules with a total testosterone undecanoate daily dose of about 350 mg to about 650 mg it provides a ratio of serum testosterone Cmax to serum testosterone Cave of about 2.7 or less. In yet another embodiment, a method for providing a serum concentration of testosterone within a target serum testosterone concentration Cave range for a male subject is provided.

Nanonized formulations of testosterone esters, especially testosterone undecanoate, and of testosterone are prepared which show an enhanced oral bioavailability compared to the existing oral products on the market. The drug is dissolved in a melted lipid phase, which is subsequently nanonized. The drug is associated with the lipid. The drug can also be nanonized without having lipid present yielding nanocrystals. The nanonized drug can be incorporated into tablets or capsules for oral administration, typically one unit is sufficient for delivery of a single dose.

A pharmaceutical formulation of testosterone undecanoate is provided. Methods of treating a testosterone deficiency or its symptoms with the inventive formulations are also provided.

The present disclosure is drawn to pharmaceutical compositions and oral dosage capsules containing testosterone undecanoate, as well as related methods. The capsule includes a capsule shell and a capsule fill. The capsule fill can include a solubilizer and about 14 wt % to about 35 wt % testosterone undecanoate based on the total capsule fill. The oral dosage capsule is such that when a single oral administration to a male subject of one or more capsules with a total testosterone undecanoate daily dose of about 350 mg to about 650 mg it provides a ratio of serum testosterone Cmax to serum testosterone Cave of about 2.7 or less. In yet another embodiment, a method for providing a serum concentration of testosterone within a target serum testosterone concentration Cave range for a male subject is provided.

The present disclosure is drawn to pharmaceutical compositions and oral dosage capsules containing testosterone undecanoate, as well as related methods of treatment. In one embodiment, the present invention provides for a pharmaceutical composition that includes a therapeutically effective amount of testosterone undecanoate and a solubilizer. The testosterone undecanoate is solubilized in the composition and is present in an amount such that it comprises about 14 wt % to about 35 wt % of the total composition.

Pharmaceutical products comprising a hypolipidemic agent and a testosterone ester such as testosterone undecanoate are provided. Methods of safely treating a testosterone deficiency or its symptoms with the inventive pharmaceutical products are also provided.

A formulation for male contraception comprising a progestin possessing both estrogenic and androgenic properties is remarkably effective for spermatogenesis suppression in males. The progestin Norethisterone (NET), particularly its derivatives Norethisterone acetate and Norethisterone enanthate in sufficient doses induce oligozoospermia or azoospermia in males. Formulations further comprising an androgen, such as a testosterone derivative such as a testosterone ester, particularly testosterone undecanoate, are especially effective male contraceptive formulations.

A self-emulsifying composite softgel of testosterone undecanoate is proportionally prepared from testosterone undecanoate, oil phase and emulsifier through dissolving testosterone undecanoate in oil phase, adding oil phase, stirring, and loading in softcapsule. It can be automatically emulsified in stomach for high curative effect.

The present disclosure is drawn to pharmaceutical compositions and oral dosage forms containing testosterone undecanoate, as well as related methods of treatment. In one embodiment, the oral dosage form can include a therapeutically effective amount of testosterone undecanoate and a pharmaceutically acceptable carrier. The dosage form can be formulated such that, when measured using a USP Type II apparatus in 1000 mL of 8 wt % Triton X-100 in water at 37° C. and 100 rpm, the oral dosage form releases at least 20% more testosterone undecanoate after the first 120 minutes than an equivalent dose testosterone undecanoate containing oral dosage form without the pharmaceutically acceptable carrier.

The present disclosure is drawn to pharmaceutical compositions and oral dosage capsules containing testosterone undecanoate, as well as related methods. The capsule includes a capsule shell and a capsule fill. The capsule fill can include a solubilizer and about 14 wt % to about 35 wt % testosterone undecanoate based on the total capsule fill. The oral dosage capsule is such that when a single oral administration to a male subject of one or more capsules with a total testosterone undecanoate daily dose of about 350 mg to about 650 mg it provides a ratio of serum testosterone Cmax to serum testosterone Cave of about 2.7 or less. In yet another embodiment, a method for providing a serum concentration of testosterone within a target serum testosterone concentration Cave range for a male subject is provided.

Pharmaceutical products comprising a hypolipidemic agent and a testosterone ester such as testosterone undecanoate are provided. Methods of safely treating a testosterone deficiency or its symptoms with the inventive pharmaceutical products are also provided.

The invention belongs to the technical field of medicines, and relates to testosterone undecanoate suspension, a preparation method thereof and an application, in particular to testosterone undecanoate suspension which comprises testosterone undecanoate, stabilizers and water. The content of the testosterone undecanoate is 10%-50%, the particle diameter D10 of the testosterone undecanoate is 0.2-0.5 micrometer, the particle diameter D50 of the testosterone undecanoate is 0.5-1.5 micrometers, the particle diameter D90 of the testosterone undecanoate is 2.2-6.0 micrometers, the stabilizers include first stabilizers and second stabilizers, the weight ratio of the first stabilizers to the second stabilizers is (1-10):(1-20), and the weight ratio of the testosterone undecanoate to the stabilizers is (1-20):(1-20). The testosterone undecanoate suspension is good in stability and high bioavailability and low in irritation, redissolved conditions after sedimentation are good, and in-vivo hormone level can be stably maintained for a long time.

The present invention relates to a method of preventing or treating benign estrogen sensitive gynaecological disorders in a female mammal, wherein the method comprises the administration to said female mammal of a combination of progestogen and androgen in an amount that is therapeutically effective to prevent or reduce the symptoms of these disorders. The present method is particularly suitable for preventing or treating disorders selected from the group consisting of endrometriosis, adenomyosis, uterine fibroids, dysmenorrhoea, menorrhagia and metrorrhagia. Another aspect of the invention relates to a pharmaceutical kit comprising a plurality of oral dosage units which comprise a progestogen in an amount equivalent to 3-500 μg levonorgestrel and either 5 to 250 mg dehydroepiandrosterone or 1 to 50 mg testosterone undecanoate.

The present invention relates to an injectable composition of testosterone ester for the treatment of testosterone deficiency. Particularly, the present invention relates to a pharmaceutical composition comprising testosterone undecanoate, which is capable of increasing the convenience for use in injection with the low viscosity and injection force, and has improved stability.

This invention relates to proliposomal powder dispersions of testosterone undecanoate (TU) and phospholipids, including dispersions of TU and palmitoylphosphatidylcholine (DPPC), wherein the weight / weight (w / w) ratio of TU:DPPC in the proliposomal powder dispersion is about 1:2; or TU and 1,2-dimyristoyl-sn-glycero-3-phosphocholine (DMPC), wherein the weight / weight (w / w) ratio of TU:DMPC in the proliposomal powder dispersion is about 1:3; or TU and a 1-myristoyl-2-palmitoyl-sn-glycero 3-phosphocholine (MPPC), wherein the weight / weight (w / w) ratio of TU:MPPC in the proliposomal powder dispersion is about 1:3.

The present invention features new testosterone undecanoate (TU) dosing regimens, e.g., for testosterone replacement therapy. The TU may be formulated with phytosterols or phytosterol esters.

The present disclosure is drawn to pharmaceutical compositions and oral dosage capsules containing testosterone undecanoate, as well as related methods. The capsule includes a capsule shell and a capsule fill. The capsule fill can include a solubilizer and about 14 wt % to about 35 wt % testosterone undecanoate based on the total capsule fill. The oral dosage capsule is such that when a single oral administration to a male subject of one or more capsules with a total testosterone undecanoate daily dose of about 350 mg to about 650 mg it provides a ratio of serum testosterone Cmax to serum testosterone Cave of about 2.7 or less. In yet another embodiment, a method for providing a serum concentration of testosterone within a target serum testosterone concentration Cave range for a male subject is provided.

The invention provides a testosterone undecanoate oral solid particle capable of being quickly released, the solubility of testosterone undecanoate in an aqueous solvent is greatly improved by using a special adsorbent and a preparation method, and the dissolution rate exceeds 40% under the condition of not containing a lipophilic solubilizer or a lipophilic surfactant. And more unexpectedly, the dissolution speed is extremely high, and complete dissolution can be realized within 5 minutes. The preparation method disclosed by the invention is simple, low in cost and relatively low in API loss.

The invention discloses a testosterone undecanoate capsule. The testosterone undecanoate capsule comprises the following components in percentage by mass: 15-65% of testosterone undecanoate, 13-68% of carrier, 10-30% of organic solvent, 0.5-3.0% of surfactant, 1.0-3.0% of micropowder silica gel and 5.0-20% of starch. The invention also discloses a preparation method of the testosterone undecanoate capsule. According to the invention, the testosterone undecanoate active compound is innovatively dispersed in a molecular form in the carrier material based on a solid dispersion technology, so that no troubles in the aspects of crystal form and granularity exist, and the in vivo release rate of the drug is greatly increased, thereby improving the bioavailability of the product. Thus, as a male hormone supplement preparation having the minimal side effect, the testosterone undecanoate has huge market prospects in the present era with the problem of population ageing.

The present invention is directed to stable pharmaceutical formulations. More specifically, the present invention is directed to stable pharmaceutical formulations of testosterone undecanoate.