公开(公告)号：US20120148675A1

公开(公告)日：2012-06-14

申请号：US12965703

申请日：2010-12-10

Applicant: Basawaraj Chickmath ,  Chandrashekar Giliyar ,  Chidambaram Nachiappan ,  Mahesh V. Patel ,  Srinivansan Venkateshwaran

Inventor： Basawaraj Chickmath ,  Chandrashekar Giliyar ,  Chidambaram Nachiappan ,  Mahesh V. Patel ,  Srinivansan Venkateshwaran

IPC: A61K31/568 ,  A61P19/00 ,  A61P15/10 ,  A61K9/14 ,  A61P5/26

CPC classification number: A61K9/2031 ,  A61K9/14 ,  A61K9/146 ,  A61K9/148 ,  A61K9/1652 ,  A61K9/1676 ,  A61K9/1694 ,  A61K9/2013 ,  A61K9/2018 ,  A61K9/205 ,  A61K9/2054 ,  A61K9/282 ,  A61K9/2853 ,  A61K9/286 ,  A61K9/2866 ,  A61K9/4866 ,  A61K9/4875 ,  A61K31/568 ,  A61K47/10 ,  A61K47/36 ,  A61K47/38 ,  A61K47/40

Abstract: 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.

Abstract translation: 本公开涉及含有十一酸睾酮的药物组合物和口服剂型，以及相关的治疗方法。 在一个实施方案中，口服剂型可以包括治疗有效量的十一酸睾酮和药学上可接受的载体。 可以配制剂型，使得当使用USP II型装置在1000mL的8重量％Triton X-100在水中在37℃和100rpm下测量时，口服剂型释放至少20％以上的睾酮 十一酸十一酸酯比不含药学上可接受的载体的含有口服剂型的等效剂量十一酸睾酮。

公开(公告)号：US20150038475A1

公开(公告)日：2015-02-05

申请号：US14500438

申请日：2014-09-29

Applicant: Basawaraj Chickmath ,  Chandrashekar Giliyar ,  Chidambaram Nachiappan ,  Mahesh Patel ,  Srinivasan Venkateshwaran

Inventor： Basawaraj Chickmath ,  Chandrashekar Giliyar ,  Chidambaram Nachiappan ,  Mahesh Patel ,  Srinivasan Venkateshwaran

IPC: A61K9/20 ,  A61K47/10 ,  A61K47/36 ,  A61K31/568

CPC classification number: A61K9/2031 ,  A61K9/14 ,  A61K9/146 ,  A61K9/148 ,  A61K9/1652 ,  A61K9/1676 ,  A61K9/1694 ,  A61K9/2013 ,  A61K9/2018 ,  A61K9/205 ,  A61K9/2054 ,  A61K9/282 ,  A61K9/2853 ,  A61K9/286 ,  A61K9/2866 ,  A61K9/4866 ,  A61K9/4875 ,  A61K31/568 ,  A61K47/10 ,  A61K47/36 ,  A61K47/38 ,  A61K47/40

Abstract: 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.

Abstract translation: 本公开涉及含有十一酸睾酮的药物组合物和口服剂型，以及相关的治疗方法。 在一个实施方案中，口服剂型可以包括治疗有效量的十一酸睾酮和药学上可接受的载体。 可以配制剂型，使得当使用USP II型装置在1000mL的8重量％Triton X-100在水中在37℃和100rpm下测量时，口服剂型释放至少20％以上的睾酮 十一酸十一酸酯比不含药学上可接受的载体的含有口服剂型的等效剂量十一酸睾酮。

公开(公告)号：US20150018324A1

公开(公告)日：2015-01-15

申请号：US14500498

申请日：2014-09-29

Applicant: Basawaraj Chickmath ,  Chandrashekar Giliyar ,  Chidambaram Nachiappan ,  Mahesh V. Patel ,  Srinivasan Venkateshwaran

Inventor： Basawaraj Chickmath ,  Chandrashekar Giliyar ,  Chidambaram Nachiappan ,  Mahesh V. Patel ,  Srinivasan Venkateshwaran

IPC: A61K9/28 ,  A61K47/38 ,  A61K47/10 ,  A61K9/20 ,  A61K31/568 ,  A61K47/36

CPC classification number: A61K9/2031 ,  A61K9/14 ,  A61K9/146 ,  A61K9/148 ,  A61K9/1652 ,  A61K9/1676 ,  A61K9/1694 ,  A61K9/2013 ,  A61K9/2018 ,  A61K9/205 ,  A61K9/2054 ,  A61K9/282 ,  A61K9/2853 ,  A61K9/286 ,  A61K9/2866 ,  A61K9/4866 ,  A61K9/4875 ,  A61K31/568 ,  A61K47/10 ,  A61K47/36 ,  A61K47/38 ,  A61K47/40

Abstract: 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.

公开(公告)号：US08951996B2

公开(公告)日：2015-02-10

申请号：US13193571

申请日：2011-07-28

Applicant: Chandrashekar Giliyar ,  Srinivasan Venkateshwaran ,  Basawaraj Chickmath ,  Satish Kumar Nachaegari ,  Chidambaram Nachiappan ,  Mahesh V. Patel

Inventor： Chandrashekar Giliyar ,  Srinivasan Venkateshwaran ,  Basawaraj Chickmath ,  Satish Kumar Nachaegari ,  Chidambaram Nachiappan ,  Mahesh V. Patel

IPC: A61K31/56 ,  A61K9/48 ,  A61K31/57 ,  A61K9/20 ,  A61K9/14 ,  A61K9/16

CPC classification number: A61K31/57 ,  A61K8/63 ,  A61K9/0053 ,  A61K9/14 ,  A61K9/145 ,  A61K9/1617 ,  A61K9/1623 ,  A61K9/1635 ,  A61K9/1641 ,  A61K9/1652 ,  A61K9/1676 ,  A61K9/2013 ,  A61K9/2018 ,  A61K9/2031 ,  A61K9/2054 ,  A61K9/2059 ,  A61K9/4841 ,  A61K9/4858 ,  A61K9/4866 ,  A61K47/10 ,  A61K47/12 ,  A61K47/14 ,  A61K47/20 ,  A61K47/22 ,  A61K47/26 ,  A61K47/32 ,  A61K47/44 ,  A61K2800/10 ,  A61Q11/00

Abstract: The present invention provides for bioavailable oral dosage forms containing esters of 17-hydroxyprogesterone as well as related methods. The oral dosage forms can be formulated for pregnancy support and can include a therapeutically effective amount of an ester of 17-hydroxyprogesterone and a pharmaceutically acceptable carrier. In another embodiment, a pharmaceutically acceptable oral dosage form for pregnancy support is provided. The pharmaceutically acceptable oral dosage can include a therapeutically effective amount of an ester of 17-hydroxyprogesterone and a pharmaceutically acceptable carrier. The oral dosage form can, when measured using a USP Type-II dissolution apparatus in 900 mL of deionized water with 0.5 (w/v) of sodium lauryl sulfate at 50 RPM at 37° C., release at least 20 wt % of the dose of the ester of 17-hydroxyprogesterone after 60 minutes, or in the alternative release at least 20 wt % more after 60 minutes than an equivalently dosed oral dosage form without the carrier.

Abstract translation: 本发明提供含有17-羟孕酮酯的生物可利用的口服剂型以及相关方法。 口服剂型可以配制用于妊娠支持，并且可以包括治疗有效量的17-羟孕酮和药学上可接受的载体的酯。 在另一个实施方案中，提供了用于妊娠支持的药学上可接受的口服剂型。 药学上可接受的口服剂量可以包括治疗有效量的17-羟孕酮和可药用载体的酯。 口服剂型可以使用USP Type-II溶出装置在90mL的90RPM的90mL去离子水和0.5（w / v）十二烷基硫酸钠的条件下测量，在37℃下以50RPM释放至少20wt％ 60分钟后17-羟孕酮酯的剂量，或在替代释放中60分钟后至少20重量％比不含载体的等效给药口服剂型更多。

公开(公告)号：US20140377317A1

公开(公告)日：2014-12-25

申请号：US14477771

申请日：2014-09-04

Applicant: Chandrashekar Giliyar ,  Srinivasan Venkateshwaran ,  Basawaraj Chickmath ,  Satish Kumar Nachaegari ,  Chidambaram Nachiappan ,  Mahesh V. Patel

Inventor： Chandrashekar Giliyar ,  Srinivasan Venkateshwaran ,  Basawaraj Chickmath ,  Satish Kumar Nachaegari ,  Chidambaram Nachiappan ,  Mahesh V. Patel

IPC: A61K8/63 ,  A61Q11/00

CPC classification number: A61K31/57 ,  A61K8/63 ,  A61K9/0053 ,  A61K9/14 ,  A61K9/145 ,  A61K9/1617 ,  A61K9/1623 ,  A61K9/1635 ,  A61K9/1641 ,  A61K9/1652 ,  A61K9/1676 ,  A61K9/2013 ,  A61K9/2018 ,  A61K9/2031 ,  A61K9/2054 ,  A61K9/2059 ,  A61K9/4841 ,  A61K9/4858 ,  A61K9/4866 ,  A61K47/10 ,  A61K47/12 ,  A61K47/14 ,  A61K47/20 ,  A61K47/22 ,  A61K47/26 ,  A61K47/32 ,  A61K47/44 ,  A61K2800/10 ,  A61Q11/00

Abstract: The present invention provides for bioavailable oral dosage forms containing esters of 17-hydroxyprogesterone as well as related methods. The oral dosage forms can be formulated for pregnancy support and can include a therapeutically effective amount of an ester of 17-hydroxyprogesterone and a pharmaceutically acceptable carrier. In another embodiment, a pharmaceutically acceptable oral dosage form for pregnancy support is provided. The pharmaceutically acceptable oral dosage can include a therapeutically effective amount of an ester of 17-hydroxyprogesterone and a pharmaceutically acceptable carrier. The oral dosage form can, when measured using a USP Type-II dissolution apparatus in 900 mL of deionized water with 0.5 (w/v) of sodium lauryl sulfate at 50 RPM at 37° C., release at least 20 wt % of the dose of the ester of 17-hydroxyprogesterone after 60 minutes, or in the alternative release at least 20 wt % more after 60 minutes than an equivalently dosed oral dosage form without the carrier.

Abstract translation: 本发明提供含有17-羟孕酮酯的生物可利用的口服剂型以及相关方法。 口服剂型可以配制用于妊娠支持，并且可以包括治疗有效量的17-羟孕酮和药学上可接受的载体的酯。 在另一个实施方案中，提供了用于妊娠支持的药学上可接受的口服剂型。 药学上可接受的口服剂量可以包括治疗有效量的17-羟孕酮和可药用载体的酯。 口服剂型可以使用USP Type-II溶出装置在90mL的90RPM的90mL去离子水和0.5（w / v）十二烷基硫酸钠的条件下，在37℃下以50RPM释放至少20wt％ 60分钟后17-羟孕酮酯的剂量，或在替代释放中60分钟后至少20重量％比不含载体的等效给药口服剂型更多。

公开(公告)号：US20150165049A1

公开(公告)日：2015-06-18

申请号：US14633545

申请日：2015-02-27

Applicant: Chandrashekar Giliyar ,  Srinivasan Venkateshwaran ,  Basawaraj Chickmath ,  Satish Kumar Nachaegari ,  Chidambaram Nachiappan ,  Mahesh Patel

Inventor： Chandrashekar Giliyar ,  Srinivasan Venkateshwaran ,  Basawaraj Chickmath ,  Satish Kumar Nachaegari ,  Chidambaram Nachiappan ,  Mahesh Patel

IPC: A61K47/44 ,  A61K9/14 ,  A61K47/14 ,  A61K47/10 ,  A61K47/20 ,  A61K47/32 ,  A61K9/20 ,  A61K47/12 ,  A61K47/22 ,  A61K31/57 ,  A61K47/26

CPC classification number: A61K31/57 ,  A61K8/63 ,  A61K9/0053 ,  A61K9/14 ,  A61K9/145 ,  A61K9/1617 ,  A61K9/1623 ,  A61K9/1635 ,  A61K9/1641 ,  A61K9/1652 ,  A61K9/1676 ,  A61K9/2013 ,  A61K9/2018 ,  A61K9/2031 ,  A61K9/2054 ,  A61K9/2059 ,  A61K9/4841 ,  A61K9/4858 ,  A61K9/4866 ,  A61K47/10 ,  A61K47/12 ,  A61K47/14 ,  A61K47/20 ,  A61K47/22 ,  A61K47/26 ,  A61K47/32 ,  A61K47/44 ,  A61K2800/10 ,  A61Q11/00

Abstract: The present invention provides for bioavailable oral dosage forms containing esters of 17-hydroxyprogesterone as well as related methods. The oral dosage forms can be formulated for pregnancy support and can include a therapeutically effective amount of an ester of 17-hydroxyprogesterone and a pharmaceutically acceptable carrier. In another embodiment, a pharmaceutically acceptable oral dosage form for pregnancy support is provided. The pharmaceutically acceptable oral dosage can include a therapeutically effective amount of an ester of 17-hydroxyprogesterone and a pharmaceutically acceptable carrier. The oral dosage form can, when measured using a USP Type-II dissolution apparatus in 900 mL of deionized water with 0.5 (w/v) of sodium lauryl sulfate at 50 RPM at 37° C., release at least 20 wt % of the dose of the ester of 17-hydroxyprogesterone after 60 minutes, or in the alternative release at least 20 wt % more after 60 minutes than an equivalently dosed oral dosage form without the carrier.

Abstract translation: 本发明提供含有17-羟孕酮酯的生物可利用的口服剂型以及相关方法。 口服剂型可以配制用于妊娠支持，并且可以包括治疗有效量的17-羟孕酮和药学上可接受的载体的酯。 在另一个实施方案中，提供了用于妊娠支持的药学上可接受的口服剂型。 药学上可接受的口服剂量可以包括治疗有效量的17-羟孕酮和可药用载体的酯。 口服剂型可以使用USP Type-II溶出装置在90mL的90RPM的90mL去离子水和0.5（w / v）十二烷基硫酸钠的条件下，在37℃下以50RPM释放至少20wt％ 60分钟后17-羟孕酮酯的剂量，或在替代释放中60分钟后至少20重量％比不含载体的等效给药口服剂型更多。

公开(公告)号：US20120244215A1

公开(公告)日：2012-09-27

申请号：US13485807

申请日：2012-05-31

Applicant: Chandrashekar Giliyar ,  Basawaraj Chickmath ,  Chidambaram Nachiappan ,  Mahesh V. Patel ,  Srinivansan Venkateshwaran

Inventor： Chandrashekar Giliyar ,  Basawaraj Chickmath ,  Chidambaram Nachiappan ,  Mahesh V. Patel ,  Srinivansan Venkateshwaran

IPC: A61K9/48 ,  A61P15/08 ,  A61K31/568

CPC classification number: A61K31/568 ,  A61K9/0053 ,  A61K9/4858 ,  A61K9/4875 ,  A61K47/12 ,  A61K47/22 ,  A61K47/44 ,  G01N33/743

Abstract: 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.

Abstract translation: 本公开涉及含有十一酸睾酮的药物组合物和口服剂量胶囊以及相关方法。 胶囊包括胶囊壳和胶囊填充物。 基于总胶囊填充，胶囊填充物可以包含增溶剂和约14重量％至约35重量％的十一酸睾酮。 口服剂量胶囊使得当向男性受试者单次口服给予一种或多种具有总睾酮十一烷酸酯的胶囊剂，每日剂量约350mg至约650mg时，其提供血清睾酮C max与血清睾酮的比例约为 2.7以下。 在另一个实施方案中，提供了一种用于在目标血清睾酮浓度范围内为男性受试者提供睾酮血清浓度的方法。

公开(公告)号：US20120135074A1

公开(公告)日：2012-05-31

申请号：US12957206

申请日：2010-11-30

Applicant: Chandrashekar Giliyar ,  Basawaraj Chickmath ,  Chidambaram Nachiappan ,  Mahesh V. Patel ,  Srinivansan Venkateshwaran

Inventor： Chandrashekar Giliyar ,  Basawaraj Chickmath ,  Chidambaram Nachiappan ,  Mahesh V. Patel ,  Srinivansan Venkateshwaran

IPC: A61K9/52 ,  A61K9/48 ,  A61P15/00 ,  A61K31/568

CPC classification number: A61K31/568 ,  A61K9/148 ,  A61K9/4875 ,  A61K47/12

Abstract: 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.

Abstract translation: 本公开涉及含有十一酸睾酮的药物组合物和口服剂量胶囊以及相关的治疗方法。 在一个实施方案中，本发明提供了包含治疗有效量的十一酸睾酮和增溶剂的药物组合物。 十一酸睾酮被溶解在组合物中，并且存在的量使得它占总组合物的约14重量％至约35重量％。

公开(公告)号：US20150224059A1

公开(公告)日：2015-08-13

申请号：US14691229

申请日：2015-04-20

Applicant: Chandrashekar Giliyar ,  Basawaraj Chickmath ,  Chidambaram Nachiappan ,  Mahesh V. Patel ,  Srinivasan Venkateshwaran

Inventor： Chandrashekar Giliyar ,  Basawaraj Chickmath ,  Chidambaram Nachiappan ,  Mahesh V. Patel ,  Srinivasan Venkateshwaran

IPC: A61K9/48 ,  A61K31/568

CPC classification number: A61K31/568 ,  A61K9/0053 ,  A61K9/4858 ,  A61K9/4875 ,  A61K47/12 ,  A61K47/22 ,  A61K47/44 ,  G01N33/743

Abstract: 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.

Abstract translation: 本公开涉及含有十一酸睾酮的药物组合物和口服剂量胶囊以及相关方法。 胶囊包括胶囊壳和胶囊填充物。 基于总胶囊填充，胶囊填充物可以包含增溶剂和约14重量％至约35重量％的十一酸睾酮。 口服剂量胶囊使得当向男性受试者单次口服给予一种或多种具有总睾酮十一烷酸酯的胶囊剂，每日剂量约350mg至约650mg时，其提供血清睾酮C max与血清睾酮的比例约为 2.7以下。 在另一个实施方案中，提供了一种用于在目标血清睾酮浓度范围内为男性受试者提供睾酮血清浓度的方法。

公开(公告)号：US09034858B2

公开(公告)日：2015-05-19

申请号：US13485807

申请日：2012-05-31

Applicant: Chandrashekar Giliyar ,  Basawaraj Chickmath ,  Chidambaram Nachiappan ,  Mahesh V. Patel ,  Srinivansan Venkateshwaran

Inventor： Chandrashekar Giliyar ,  Basawaraj Chickmath ,  Chidambaram Nachiappan ,  Mahesh V. Patel ,  Srinivansan Venkateshwaran

IPC: A61P15/08 ,  A61K9/48 ,  A61K31/568

CPC classification number: A61K31/568 ,  A61K9/0053 ,  A61K9/4858 ,  A61K9/4875 ,  A61K47/12 ,  A61K47/22 ,  A61K47/44 ,  G01N33/743

Abstract: 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.