公开(公告)号：US06576250B1

公开(公告)日：2003-06-10

申请号：US09664870

申请日：2000-09-19

申请人： S. Indiran Pather ,  Joseph R. Robinson ,  Jonathan D. Eichman ,  Rajendra K. Khankari ,  John Hontz

发明人： S. Indiran Pather ,  Joseph R. Robinson ,  Jonathan D. Eichman ,  Rajendra K. Khankari ,  John Hontz

IPC分类号： A61K902

CPC分类号： A61K9/006 ,  A61K9/0007 ,  A61K9/0056 ,  A61K9/2072 ,  A61K9/2866 ,  A61K9/2886 ,  A61K31/4468 ,  A61K31/5415

摘要： The pharmaceutical compositions of the present invention comprise rectally and vaginally administerable dosage forms that contain effervescent agents as penetration enhancers for drugs. Effervescence occurs in the rectum or vagina, once the dosage form is administered or at a predetermined time following administration. The effervescent agents can be used alone or in combination with pH adjusting substance, which further promote dissolution and absorption of the active ingredient.

摘要翻译： 本发明的药物组合物包含含有泡腾剂作为药物渗透促进剂的直肠和阴道给药剂型。 在直肠或阴道中发生泡腾，一旦施用剂型或在施用后的预定时间。 泡腾剂可以单独使用或与pH调节物质组合使用，这进一步促进活性成分的溶解和吸收。

公开(公告)号：US06368625B1

公开(公告)日：2002-04-09

申请号：US09372738

申请日：1999-08-11

申请人： John M. Siebert ,  Rajendra K. Khankari ,  Unchalee Kositprapa ,  S. Indiran Pather

发明人： John M. Siebert ,  Rajendra K. Khankari ,  Unchalee Kositprapa ,  S. Indiran Pather

IPC分类号： A61K920

CPC分类号： A61K9/0007 ,  A61K9/0056 ,  A61K9/2009 ,  A61K9/2054 ,  A61K9/2081 ,  A61K9/5042 ,  A61K9/5047

摘要： A dosage form which rapidly disintegrates in the mouth and forms a viscous slurry of either microcapsules or a powder is described. The rapidly disintegrating dosage form is meant for direct oral administration by placing a tablet or capsule in the mouth of a patient. Upon disintegration, a viscosity of the resulting slurry increases so as to form an organoleptically pleasant viscous material which retards the spread of insoluble materials including the drug.

摘要翻译： 描述了在口中快速崩解并形成微胶囊或粉末的粘性浆液的剂型。 快速崩解的剂型意在通过将片剂或胶囊置于患者的口中直接口服给药。 在分解时，所得浆料的粘度增加，以形成感官愉悦的粘稠材料，其阻止包括药物在内的不溶物质的铺展。

公开(公告)号：US08802130B2

公开(公告)日：2014-08-12

申请号：US11511098

申请日：2006-08-28

申请人： S. Indiran Pather ,  Rajendra K. Khankari ,  Jonathan D. Eichman ,  Joseph R. Robinson ,  John Hontz

发明人： S. Indiran Pather ,  Rajendra K. Khankari ,  Jonathan D. Eichman ,  Joseph R. Robinson ,  John Hontz

IPC分类号： A61F13/00

CPC分类号： A61K9/0007 ,  A61K9/0056 ,  A61K9/006 ,  A61K31/4468 ,  A61K31/5415

摘要： A pharmaceutical dosage form adapted to supply a medicament to the oral cavity for buccal, sublingual or gingival absorption of the medicament which contains an orally administrable medicament in combination with an effervescent for use in promoting absorption of the medicament in the oral cavity. The use of an additional pH adjusting substance in combination with the effervescent for promoting the absorption drugs is also disclosed.

摘要翻译： 一种药物剂型，其适于向口腔中提供药物的口腔，舌下或牙龈吸收，所述药物包含与可用于促进所述药物在口腔中的吸收的泡腾剂相结合的可口服给药的药物。 还公开了与泡腾剂结合使用另外的pH调节物质以促进吸收药物。

公开(公告)号：US06641838B2

公开(公告)日：2003-11-04

申请号：US10021109

申请日：2001-10-29

申请人： S. Indiran Pather ,  Joseph R. Robinson ,  Jonathan D. Eichman ,  Rajendra K. Khankari ,  John Hontz ,  Sangeeta V. Gupte

发明人： S. Indiran Pather ,  Joseph R. Robinson ,  Jonathan D. Eichman ,  Rajendra K. Khankari ,  John Hontz ,  Sangeeta V. Gupte

IPC分类号： A61K928

CPC分类号： A61K9/2886 ,  A61K9/0007 ,  A61K9/2072 ,  A61K9/2866 ,  A61K9/5084 ,  Y10S514/96

摘要： The pharmaceutical compositions of the present invention comprise orally administerable dosage forms that use effervescence as a penetration enhancer for drugs known, or suspected, of having poor bioavailability. Effervescence can occur in the stomach, once the tablet or other dosage form is ingested. In addition to effervescence in the stomach, or as alternative technique, by the use of appropriate coatings and other techniques, the effervescence can occur in other parts of the gastrointestinal tract, including, but not limited to, the esophagus, duodenum, and colon. The site of effervescence and drug release is chosen to correspond with the segment of the gastrointestinal tract displaying maximal absorption of the formulated drug, or to gain some other therapeutic advantage.

公开(公告)号：US06764696B2

公开(公告)日：2004-07-20

申请号：US10346829

申请日：2003-03-18

申请人： S. Indiran Pather ,  Joseph R. Robinson ,  Jonathan D. Eichman ,  Rajendra K. Khankari ,  John Hontz ,  Sangeeta V. Gupte

发明人： S. Indiran Pather ,  Joseph R. Robinson ,  Jonathan D. Eichman ,  Rajendra K. Khankari ,  John Hontz ,  Sangeeta V. Gupte

IPC分类号： A61K924

CPC分类号： A61K9/2886 ,  A61K9/0007 ,  A61K9/2072 ,  A61K9/2866 ,  A61K9/5084 ,  Y10S514/96

摘要： The pharmaceutical compositions of the present invention comprise orally administerable dosage forms that use effervescence as a penetration enhancer for drugs known, or suspected, of having poor bioavailability. Effervescence can occur in the stomach, once the tablet or other dosage form is ingested. In addition to effervescence in the stomach, or as alternative technique, by the use of appropriate coatings and other techniques, the effervescence can occur in other parts of the gastrointestinal tract, including, but not limited to, the esophagus, duodenum, and colon. The site of effervescence and drug release is chosen to correspond with the segment of the gastrointestinal tract displaying maximal absorption of the formulated drug, or to gain some other therapeutic advantage.

摘要翻译： 本发明的药物组合物包含口服给药剂型，其使用泡腾作为已知或怀疑具有差的生物利用度的药物的渗透增强剂。 一旦片剂或其他剂型被摄取，起泡可能发生在胃中。 除了在胃中起泡或作为替代技术，通过使用适当的包衣和其它技术，泡腾可以发生在胃肠道的其它部分，包括但不限于食道，十二指肠和结肠。 选择泡腾和药物释放的部位以与显示配制药物的最大吸收的胃肠道的部分相对应，或获得一些其他治疗优势。

公开(公告)号：US06692771B2

公开(公告)日：2004-02-17

申请号：US09792659

申请日：2001-02-23

申请人： S. Indiran Pather ,  Sangeeta V. Gupte ,  Rajendra K. Khankari ,  John Hontz ,  Ramya Kumbale

发明人： S. Indiran Pather ,  Sangeeta V. Gupte ,  Rajendra K. Khankari ,  John Hontz ,  Ramya Kumbale

IPC分类号： A61K916

CPC分类号： A61K9/143

摘要： Novel emulsion compositions which improve the rate and/or extent of absorption of drugs are disclosed. The novel emulsion compositions of the present invention include drug-containing emulsions adsorbed onto solid particles which may be further formulated into solid dosage forms, methods of preparing such emulsion compositions and their uses thereof. The emulsion compositions and their dosage forms improve the drug-load and the bioavailability of a wide range of drugs including drugs that are known or suspected of having poor bioavailability by the utilization of several different mechanisms.

摘要翻译： 公开了提高药物吸收速率和/或程度的新型乳液组合物。 本发明的新型乳液组合物包括吸附在固体颗粒上的含药乳液，其可以进一步配制成固体剂型，制备这种乳液组合物的方法及其应用。 乳剂组合物及其剂型通过利用几种不同的机制改善了广泛范围的药物，包括已知或怀疑具有差的生物利用度的药物的药物负载和生物利用度。

公开(公告)号：US06509036B2

公开(公告)日：2003-01-21

申请号：US10021486

申请日：2001-10-29

申请人： S. Indiran Pather ,  Joseph R. Robinson ,  Jonathan D. Eichman ,  Rajendra K. Khankari ,  John Hontz ,  Sangeeta V. Gupte

发明人： S. Indiran Pather ,  Joseph R. Robinson ,  Jonathan D. Eichman ,  Rajendra K. Khankari ,  John Hontz ,  Sangeeta V. Gupte

IPC分类号： A61K914

CPC分类号： A61K9/2886 ,  A61K9/0007 ,  A61K9/2072 ,  A61K9/2866 ,  A61K9/5084 ,  Y10S514/96

摘要： The pharmaceutical compositions of the present invention comprise orally administerable dosage forms that use effervescence as a penetration enhancer for drugs known, or suspected, of having poor bioavailability. Effervescence can occur in the stomach, once the tablet or other dosage form is ingested. In addition to effervescence in the stomach, or as alternative technique, by the use of appropriate coatings and other techniques, the effervescence can occur in other parts of the gastrointestinal tract, including, but not limited to, the esophagus, duodenum, and colon. The site of effervescence and drug release is chosen to correspond with the segment of the gastrointestinal tract displaying maximal absorption of the formulated drug, or to gain some other therapeutic advantage.

公开(公告)号：US6139874A

公开(公告)日：2000-10-31

申请号：US302105

申请日：1999-04-29

申请人： S. Indiran Pather ,  Joseph R. Robinson ,  Jonathan D. Eichman ,  Rajendra K. Khankari ,  John Hontz ,  Sangeeta V. Gupte

发明人： S. Indiran Pather ,  Joseph R. Robinson ,  Jonathan D. Eichman ,  Rajendra K. Khankari ,  John Hontz ,  Sangeeta V. Gupte

摘要： The pharmaceutical compositions of the present invention comprise orally administerable dosage forms that use effervescence as a penetration enhancer for drugs known, or suspected, of having poor bioavailability. Effervescence can occur in the stomach, once the tablet or other dosage form is ingested. In addition to effervescence in the stomach, or as alternative technique, by the use of appropriate coatings and other techniques, the effervescence can occur in other parts of the gastrointestinal tract, including, but not limited to, the esophagus, duodenum, and colon. The site of effervescence and drug release is chosen to correspond with the segment of the gastrointestinal tract displaying maximal absorption of the formulated drug, or to gain some other therapeutic advantage.

公开(公告)号：US07670617B2

公开(公告)日：2010-03-02

申请号：US10936185

申请日：2004-09-08

申请人： S. Indiran Pather ,  John Hontz ,  John M. Siebert

发明人： S. Indiran Pather ,  John Hontz ,  John M. Siebert

IPC分类号： A61F9/02

CPC分类号： A61K9/0034 ,  A61K9/025 ,  A61K9/2054 ,  A61K9/2081 ,  A61K31/48

摘要： The invention relates to methods and composition for improving absorption and dissolution of active ingredients of drugs. The invention provides a method of administration of an active ingredient to a mammal through a transmucosal route that includes delivering the active ingredient to a desired site in a body of the mammal, and, sequentially, at the desired site, promoting dissolution and absorption of the active ingredient. In a preferred embodiment, the pH of the localized environment of the active ingredient is sequentially modified to promote dissolution and absorption.

摘要翻译： 本发明涉及用于改善药物活性成分吸收和溶解的方法和组合物。 本发明提供了通过经粘膜途径向哺乳动物施用活性成分的方法，其包括将活性成分递送至哺乳动物体内的期望部位，并且依次在所需位点促进溶解和吸收 有效成分。 在优选的实施方案中，活性成分的局部环境的pH被依次修饰以促进溶解和吸收。

公开(公告)号：US06391335B1

公开(公告)日：2002-05-21

申请号：US09613270

申请日：2000-07-10

申请人： S. Indiran Pather ,  Joseph R. Robinson ,  Jonathan D. Eichman ,  Rajendra K. Khankari ,  John Hontz ,  Sangeeta V. Gupte

发明人： S. Indiran Pather ,  Joseph R. Robinson ,  Jonathan D. Eichman ,  Rajendra K. Khankari ,  John Hontz ,  Sangeeta V. Gupte

IPC分类号： A61K946

CPC分类号： A61K9/2886 ,  A61K9/0007 ,  A61K9/2072 ,  A61K9/2866 ,  A61K9/5084 ,  Y10S514/96

摘要： The pharmaceutical compositions of the present invention comprise orally administerable dosage forms that use effervescence as a penetration enhancer for drugs known, or suspected, of having poor bioavailability. Effervescence can occur in the stomach, once the tablet or other dosage form is ingested. In addition to effervescence in the stomach, or as alternative technique, by the use of appropriate coatings and other techniques, the effervescence can occur in other parts of the gastrointestinal tract, including, but not limited to, the esophagus, duodenum, and colon. The site of effervescence and drug release is chosen to correspond with the segment of the gastrointestinal tract displaying maximal absorption of the formulated drug, or to gain some other therapeutic advantage.