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：US20110312928A1

公开(公告)日：2011-12-22

申请号：US13204562

申请日：2011-08-05

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

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

IPC: A61K31/57 ,  A61P15/00 ,  A61P15/18 ,  A61P15/16 ,  A61P35/00 ,  A61P19/10

CPC classification number: A61K31/57 ,  A61K9/2013 ,  A61K9/2018 ,  A61K9/2054 ,  A61K9/2077 ,  A61K9/209 ,  A61K9/2846 ,  A61K9/4808 ,  A61K9/4858 ,  A61K9/4866

Abstract: The present invention provides for progesterone containing pharmaceutical oral dosage forms and related methods. The oral dosage forms can each include an amount of progesterone as well as a pharmaceutically acceptable carrier. The oral dosage forms can be formulated to have at least one of the following characteristics: the oral dosage form produces an pregnane metabolite mean blood plasma level of less than about 1000 nmol/L; the oral dosage form produces an pregnane metabolites mean blood plasma level, after administration of single dose of progesterone composition, such that the ratio of pregnane metabolite level to parent progesterone level of less than 10:1; has a dissolution rate in vitro, when measure using a USP Type-1 dissolution apparatus in 900 mL of deionized water with 2.0% (w/v) of sodium lauryl sulfate at 100 rpm, such that the oral dosage form releases at least 10 wt % of the progesterone within the first 30 minutes and/or releases less than 45 wt % in the first 4 hours; and the oral dosage form produces a ratio of mean plasma progesterone AUC to the amount of progesterone administered of more than 1.5×10−6 hr/mL:1.

Abstract translation: 本发明提供含有孕酮的药物口服剂型和相关方法。 口服剂型各自可以包含一定量的孕酮以及药学上可接受的载体。 口服剂型可以配制成具有以下特征中的至少一种：口服剂型产生的孕代谢物平均血浆水平低于约1000nmol / L; 口服剂型产生孕烷代谢物平均血浆水平，施用单次孕酮组合物后，孕妇代谢物水平与母体孕酮水平的比例小于10：1; 当使用USP1型溶出装置在900mL具有2.0％（w / v）月桂基硫酸钠的去离子水中以100rpm进行测量时，其体外溶出速率使得口服剂型释放至少10重量％ 在前30分钟内孕酮的百分比和/或在前4小时内释放小于45重量％ 并且口服剂型产生平均血浆孕酮AUC与施用孕酮量的比例大于1.5×10-6hr / mL：1。

公开(公告)号：US20110312927A1

公开(公告)日：2011-12-22

申请号：US12819125

申请日：2010-06-18

Applicant: Satish Kumar Nachaegari ,  Chandrashekar Giliyar ,  Chidambaram Nachiappan ,  Linus Fonkwe ,  Mahesh Patel ,  Srinivasan Venkateshwaran

Inventor： Satish Kumar Nachaegari ,  Chandrashekar Giliyar ,  Chidambaram Nachiappan ,  Linus Fonkwe ,  Mahesh Patel ,  Srinivasan Venkateshwaran

IPC: A61K31/57 ,  A61P15/00 ,  A61P15/08

CPC classification number: A61K31/57 ,  A61K9/2018 ,  A61K9/2077 ,  A61K9/209 ,  A61K9/2846 ,  A61K9/4808 ,  A61K9/4858

Abstract: The present invention provides for progesterone containing pharmaceutical oral dosage forms and related methods. The oral dosage forms can each include an amount of progesterone as well as a pharmaceutically acceptable carrier. The oral dosage forms can be formulated to have at least one of the following characteristics: the oral dosage form produces an pregnane metabolite mean blood plasma level of less than about 1000 nmol/L; the oral dosage form produces an pregnane metabolites mean blood plasma level, after administration of single dose of progesterone composition, such that the ratio of pregnane metabolite level to parent progesterone level of less than 10:1; has a dissolution rate in vitro, when measure using a USP Type-1 dissolution apparatus in 900 mL of deionized water with 2.0% (w/v) of sodium lauryl sulfate at 100 rpm, such that the oral dosage form releases at least 10 wt % of the progesterone within the first 30 minutes and/or releases less than 45 wt % in the first 4 hours; and the oral dosage form produces a ratio of mean plasma progesterone AUC to the amount of progesterone administered of more than 1.5×10−6 hr/mL:1

Abstract translation: 本发明提供含有孕酮的药物口服剂型和相关方法。 口服剂型各自可以包含一定量的孕酮以及药学上可接受的载体。 口服剂型可以配制成具有以下特征中的至少一种：口服剂型产生的孕代谢物平均血浆水平低于约1000nmol / L; 口服剂型产生孕烷代谢物平均血浆水平，施用单次孕酮组合物后，孕妇代谢物水平与母体孕酮水平的比例小于10：1; 当使用USP1型溶出装置在900mL具有2.0％（w / v）月桂基硫酸钠的去离子水中以100rpm进行测量时，其体外溶出速率使得口服剂型释放至少10重量％ 在前30分钟内孕酮的百分比和/或在前4小时内释放小于45重量％ 并且口服剂型产生平均血浆孕酮AUC与施用孕酮量的比例大于1.5×10-6小时/ mL：1

公开(公告)号：US20110142945A1

公开(公告)日：2011-06-16

申请号：US13029989

申请日：2011-02-17

Applicant: Feng-Jing Chen ,  Kathryn Gutke ,  Srinivasan Venkateshwaran ,  Mahesh V. Patel

Inventor： Feng-Jing Chen ,  Kathryn Gutke ,  Srinivasan Venkateshwaran ,  Mahesh V. Patel

IPC: A61K9/14 ,  A61K31/5685

CPC classification number: A61K38/13 ,  A61K9/4858 ,  A61K9/4866

Abstract: Compositions and methods for providing hydrophobic active agents in a bioavailable form are disclosed and described. In one aspect of the invention, pharmaceutical composition containing a testosterone ester is provided. The composition includes a testosterone ester in both dissolved form and as undissolved particles and the dissolved form comprises at least 35 wt % of the testosterone ester present in the composition. The composition further includes a solubilizer and a stabilizer.

Abstract translation: 公开和描述了以生物可利用形式提供疏水性活性剂的组合物和方法。 在本发明的一个方面，提供了含有睾酮酯的药物组合物。 组合物包括溶解形式的睾酮酯和未溶解的颗粒，溶解形式包含组合物中存在的至少35重量％的睾酮酯。 组合物还包括增溶剂和稳定剂。

公开(公告)号：US06365178B1

公开(公告)日：2002-04-02

申请号：US09764040

申请日：2001-01-17

Applicant: Srinivasan Venkateshwaran ,  David Fikstad ,  Charles D. Ebert

Inventor： Srinivasan Venkateshwaran ,  David Fikstad ,  Charles D. Ebert

IPC: A61K970

CPC classification number: A61K9/7053 ,  A61K9/7061

Abstract: A method of making a pressure sensitive matrix patch for transdermal delivery of a drug is disclosed. The method includes the steps of dissolving a hydrophilic salt form of the drug in the water phase of an aqueous dispersion of a hydrophobic pressure sensitive adhesive, casting the resulting mixture as a thin film, and evaporating the water. The physical stability of the drug in the film is excellent, and crystallization of the drug is inhibited. A method of increasing the transdermal flux of an acidic drug is also disclosed.

Abstract translation: 公开了制备用于药物透皮递送的压敏基质贴片的方法。 该方法包括以下步骤：将亲水盐形式的药物溶解在疏水性压敏粘合剂的水分散体的水相中，将所得混合物浇铸成薄膜，并蒸发水。 药物在膜中的物理稳定性优异，药物的结晶被抑制。 还公开了增加酸性药物的经皮通量的方法。

公开(公告)号：US5985317A

公开(公告)日：1999-11-16

申请号：US706624

申请日：1996-09-06

Applicant: Srinivasan Venkateshwaran ,  David Fikstad ,  Charles D. Ebert

Inventor： Srinivasan Venkateshwaran ,  David Fikstad ,  Charles D. Ebert

IPC: A61K9/70 ,  A61L15/58 ,  A61L15/16

CPC classification number: A61K9/703 ,  A61K9/7053 ,  A61K9/7061

Abstract: A method of transdermally or transmucosally delivering a hydrophilic salt form of a drug with a water-based pressure sensitive hydrophobic adhesive matrix patch optionally containing a permeation enhancer is disclosed. A matrix patch comprising a water-based pressure sensitive hydrophobic adhesive, a hydrophilic salt form of a drug, and optionally a permeation enhancer for transdermal or transmucosal delivery of the hydrophilic salt form of the drug is also disclosed.

Abstract translation: 公开了一种透皮或透粘膜递送药物的亲水盐形式的方法，该方法是使用任选含有渗透促进剂的基于水的压敏疏水性粘合剂基质片剂。 还公开了一种基质贴剂，其包含水基压敏疏水性粘合剂，药物的亲水盐形式和任选的用于透皮或经粘膜递送亲水盐形式的药物的渗透促进剂。

公开(公告)号：US09107921B2

公开(公告)日：2015-08-18

申请号：US14555043

申请日：2014-11-26

Applicant: Chandrashekar Giliyar ,  Satish Kumar Nachaegari ,  Chidambaram Machiappan ,  Mahesh V. Patel ,  Srinivasan Venkateshwaran

Inventor： Chandrashekar Giliyar ,  Satish Kumar Nachaegari ,  Chidambaram Machiappan ,  Mahesh V. Patel ,  Srinivasan Venkateshwaran

IPC: A61K31/485 ,  A61K31/194 ,  A61K31/4402 ,  A61K45/06 ,  A61K31/09 ,  A61K31/137 ,  A61K9/20

CPC classification number: A61K31/485 ,  A61K9/0053 ,  A61K9/2054 ,  A61K31/09 ,  A61K31/137 ,  A61K31/194 ,  A61K31/4402 ,  A61K45/06 ,  A61K2300/00

Abstract: A pharmaceutical tablet for oral administration once every 12 hours is provided. The tablet includes a first active agent that is a tri-oxy active agent, a second active agent, and a release rate controlling non-ionic oxyl-containing hydrophilic polymer. The tablet is a matrix tablet and a single-dose administration of one or more tablets to a subject under fasted conditions provides a mean Cm˜ for each of the first active agent and the second active agent that is 70% to 135% of a respective mean Cm˜ provided by administering an immediate release oral dosage form to a subject under fasted conditions every 4 to 6 hours over a 12 hour time period, wherein cumulative dosage amounts administered over the 12 hour time period of each active agent is equivalent to the respective amount of each active agent in the pharmaceutical tablet.

Abstract translation: 提供每12小时一次口服给药的药片。 片剂包括第一活性剂，其为三氧基活性剂，第二活性剂和释放速率控制非离子含氧基的亲水性聚合物。 片剂是基质片剂，并且在禁食条件下向受试者单剂量施用一种或多种片剂，为每种第一活性剂和第二活性剂提供平均Cm〜，其为相应的70％至135％ 平均Cm〜通过在禁食条件下每隔4至6小时在12小时时间内向受试者施用立即释放的口服剂型，其中在每个活性剂的12小时时间段内施用的累积剂量相当于相应的 药物片剂中每种活性剂的量。

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：US20070281927A1

公开(公告)日：2007-12-06

申请号：US11448597

申请日：2006-06-06

Applicant: Shanthakumar Tyavanagimatt ,  David Fikstad ,  Chandrashekar Giliyar ,  Mahesh Patel ,  Srinivasan Venkateshwaran

Inventor： Shanthakumar Tyavanagimatt ,  David Fikstad ,  Chandrashekar Giliyar ,  Mahesh Patel ,  Srinivasan Venkateshwaran

IPC: A61K31/5415

CPC classification number: A61K31/5415 ,  A61K9/2054 ,  A61K9/4858 ,  A61K9/5084

Abstract: Methods and compositions for delivering a meloxicam compound are disclosed and described. In one aspect, a method may include perorally administering to a subject a therapeutically effective amount of a meloxicam compound that provides a meloxicam plasma concentration within 1 hour which is at least about 40% of the maximum plasma concentration attained by the formulation. In another aspect, a composition may include a therapeutically effective amount of a meloxicam compound in a pharmaceutically acceptable carrier including at least one of an alkalizer or a solubilizer, with the meloxicam compound having a solubility in the carrier that is greater than about 1.0 mg/gm.

Abstract translation: 公开和描述了递送美洛昔康化合物的方法和组合物。 一方面，方法可以包括向受试者口服施用治疗有效量的美洛昔康化合物，所述美洛昔康化合物在1小时内提供美洛昔康血浆浓度，其为制剂达到的最大血浆浓度的至少约40％。 另一方面，组合物可以包括药学上可接受的载体中的治疗有效量的美洛昔康化合物，其包括碱化剂或增溶剂中的至少一种，其中美洛昔康化合物在载体中的溶解度大于约1.0mg / gm。