公开(公告)号：US20240398717A1

公开(公告)日：2024-12-05

申请号：US18789155

申请日：2024-07-30

Applicant: New Jersey Institute of Technology

Inventor： Rajesh N. Dave ,  Sangah Selene Kim ,  Zhixing Lin

IPC: A61K9/50

Abstract: A method of employing a mixture of two different types of silica as a binary dry coating material to benefit properties of fine milled pharmaceuticals, such as ibuprofen, milled to the mean particle size of ˜10 μm or smaller. Synergistic effects of reduction in agglomerate size, and improved surface wettability was found by employing a mixture of two different types of silica as the dry coating material in specific ratios. The silica used up to weight percent to 2.31 wt % of a minority component, typically an API or excipient. The silica amount in the entire blend was less than 0.1 wt %. The surface coverage of API was optimized to 50%. Properties were increased when surface coverage by binary coating agents was controlled so that no excess coating agent was available to form agglomerates on the surface.

公开(公告)号：US20140106059A1

公开(公告)日：2014-04-17

申请号：US13651977

申请日：2012-10-15

Applicant: NEW JERSEY INSTITUTE OF TECHNOLOGY

Inventor： Rajesh N. Dave ,  Daniel To ,  Maxx Capece

IPC: A61K9/14 ,  B05D7/00 ,  B82Y40/00 ,  B82Y5/00

CPC classification number: A61K9/5042 ,  A61K9/5063 ,  A61K9/5073 ,  A61K9/5089 ,  A61K35/00

Abstract: The present invention is a solventless method of producing polymer coated active pharmaceutical ingredient that is taste-masked and may be released in relatively short time. It employs high energy vibrations or acoustic mixing of API particles, water soluble coating material particles and hydrophobic polymer particles, with or without use of other pharmaceutically relevant powders as media. Additionally the method is capable of producing individually coated drug particles without agglomeration or the long drying times associated with solvent based coating methods.

Abstract translation: 本发明是一种制造聚合物涂覆的活性药物成分的无溶剂方法，其具有掩味作用并且可在较短时间内释放。 它使用API​​颗粒，水溶性涂层材料颗粒和疏水性聚合物颗粒的高能量振动或声音混合，有或没有使用其它药学上相关的粉末作为介质。 此外，该方法能够产生单独涂覆的药物颗粒而不发生附聚或与溶剂型涂布方法相关的长时间干燥时间。

公开(公告)号：US20160022599A1

公开(公告)日：2016-01-28

申请号：US14777191

申请日：2014-03-17

Applicant: NEW JERSEY INSTITUTE OF TECHNOLOGY

Inventor： Rajesh N. Dave ,  Ramani Susarla ,  Boris Khusid ,  Anagha A. Bhakay ,  Ecevit A. Bilgili ,  Fernando Muzzio

IPC: A61K9/70 ,  A61K47/38 ,  B29C39/14 ,  A61K31/216 ,  B29C39/00 ,  A61K31/343 ,  A61K47/32

CPC classification number: A61K9/7007 ,  A61F13/00063 ,  A61K9/0056 ,  A61K9/006 ,  A61K31/216 ,  A61K31/343 ,  A61K47/32 ,  A61K47/38 ,  B29C39/003 ,  B29C39/14 ,  B29L2007/008

Abstract: The present disclosure provides improved stripfilm based pharmaceutical products (e.g., for enhancing dissolution and bioavailability). More particularly, the present disclosure provides improved systems/methods for fabricating stripfilm based pharmaceutical products by utilizing higher viscosity film forming precursors and drying methods that accomplish improved/faster drying and provide improved/excellent content uniformity of active pharmaceutical agents in the stripfilm based pharmaceutical products. Exemplary systems/methods advantageously use high viscosity, bio-compatible polymeric precursors, (optional use of surface modified drug powders), and convective drying for fabrication of thin films loaded with nano and/or micro sized particles of poorly water-soluble active pharmaceutical ingredients (APIs) to achieve improved active content uniformity and very fast dissolution from poorly water soluble actives, while accomplishing fast drying during the fabrication process. The present disclosure provides for the fast drying (e.g., via low temperature forced convection) of biocompatible polymer films loaded with poorly water-soluble drug nano-particles.

Abstract translation: 本公开提供了改进的基于薄膜的药物产品（例如，用于增强溶解和生物利用度）。 更具体地，本公开提供了通过利用更高粘度的成膜前体和干燥方法来制造基于薄膜的药物产品的改进的系统/方法，所述前体和干燥方法实现改进/更快的干燥，并且提供基于带状薄膜的药物产品中活性药剂的改进/优异的含量均匀性 。 示例性系统/方法有利地使用高粘度，生物相容性聚合物前体（任选使用表面改性药物粉末）和对流干燥以制备装载有水溶性差的活性药物成分的纳米和/或微尺寸颗粒的薄膜 （API），以实现改善的活性成分均匀性和非常快的水溶性活性物质的溶出，同时在制造过程中实现快速干燥。 本公开内容提供了装载有不良水溶性药物纳米颗粒的生物相容性聚合物膜的快速干燥（例如通过低温强制对流）。

公开(公告)号：US20140106058A1

公开(公告)日：2014-04-17

申请号：US13651829

申请日：2012-10-15

Applicant: NEW JERSEY INSTITUTE OF TECHNOLOGY

Inventor： Daniel To ,  Rajesh N. Dave

IPC: B05D5/00

CPC classification number: A61K9/501 ,  A61K9/5026 ,  A61K9/5042 ,  A61K9/5089

Abstract: A taste masked particulate pharmaceutical formulation include a core that comprises an active pharmaceutical ingredient; at least a partial nanoparticle material layer on the core that comprises a nanoparticle material with a median particle size not greater than 100 nm; a first polymer layer that is at least partially water soluble and a second polymer layer that is water insoluble. The active pharmaceutical ingredient is completely released in 30 minutes in the USP Dissolution Test. A process of making the particulate pharmaceutical formulation using sequential fluidized bed coating steps under controlled conditions is also described.

Abstract translation: 掩味的颗粒药物制剂包括包含活性药物成分的核心; 所述芯上至少包含中值粒径不大于100nm的纳米颗粒材料的部分纳米颗粒材料层; 至少部分水溶性的第一聚合物层和水不溶性的第二聚合物层。 在USP溶出度测试中，活性药物成分在30分钟内完全释放。 还描述了在受控条件下使用顺序流化床涂布步骤制备颗粒药物制剂的方法。

公开(公告)号：US10646452B2

公开(公告)日：2020-05-12

申请号：US14777191

申请日：2014-03-17

Applicant: New Jersey Institute of Technology

Inventor： Rajesh N. Dave ,  Ramani Susarla ,  Boris Khusid ,  Anagha A. Bhakay ,  Ecevit A. Bilgili ,  Fernando Muzzio

IPC: B29C39/14 ,  A61K9/70 ,  A61K9/00 ,  A61K31/216 ,  A61K31/343 ,  A61K47/32 ,  A61K47/38 ,  B29C39/00 ,  A61F13/00 ,  B29L7/00

Abstract: The present disclosure provides improved stripfilm based pharmaceutical products (e.g., for enhancing dissolution and bioavailability). More particularly, the present disclosure provides improved systems/methods for fabricating stripfilm based pharmaceutical products by utilizing higher viscosity film forming precursors and drying methods that accomplish improved/faster drying and provide improved/excellent content uniformity of active pharmaceutical agents in the stripfilm based pharmaceutical products. Exemplary systems/methods advantageously use high viscosity, bio-compatible polymeric precursors, (optional use of surface modified drug powders), and convective drying for fabrication of thin films loaded with nano and/or micro sized particles of poorly water-soluble active pharmaceutical ingredients (APIs) to achieve improved active content uniformity and very fast dissolution from poorly water soluble actives, while accomplishing fast drying during the fabrication process. The present disclosure provides for the fast drying (e.g., via low temperature forced convection) of biocompatible polymer films loaded with poorly water-soluble drug nano-particles.

公开(公告)号：US20190099373A1

公开(公告)日：2019-04-04

申请号：US16150931

申请日：2018-10-03

Applicant: New Jersey Institute of Technology

Inventor： Rajesh N. Dave ,  Lu Zhang ,  Guluzar Gorkem ,  Eylul Cetindag

IPC: A61K9/16 ,  A61K9/70 ,  A61K47/38 ,  A61K47/10 ,  A61K47/20 ,  A61K45/06

Abstract: The present disclosure provides improved film based pharmaceutical products containing uniformly distributed drug or active agent particles (e.g., to achieve improved/excellent dissolution control including enhancing dissolution and bioavailability and/or product uniformity). More particularly, the present disclosure provides improved systems/methods for fabricating film based pharmaceutical products by utilizing higher surface modified micronized drug or active agent powders and film forming precursors and drying methods that accomplish improved/efficient drying and provide improved/excellent content uniformity of active pharmaceutical agents in the fabricated film based pharmaceutical products. In exemplary embodiments, the present disclosure provides for an easier means of directly incorporating dry micronized poorly water-soluble drugs or active agent particles (e.g., fenofibrate (“FNB”)) into films. The present disclosure demonstrates some advantages of direct incorporation of surface modified-micronized poorly water-soluble drug or active agent powders in film manufacturing.

公开(公告)号：US12076440B2

公开(公告)日：2024-09-03

申请号：US18221143

申请日：2023-07-12

Applicant: New Jersey Institute of Technology

Inventor： Rajesh N. Dave ,  Sangah Kim ,  Zhixing Lin

IPC: A61K9/14 ,  A61K9/16 ,  A61K31/192 ,  A61K45/06 ,  B82Y5/00 ,  B82Y30/00

CPC classification number: A61K9/143 ,  A61K9/1682 ,  A61K31/192 ,  A61K45/06 ,  B82Y5/00 ,  B82Y30/00

Abstract: High (greater than 30%) and/or low (less than 10%) loaded multiple API powdered/nanoparticle were tabulated with increased flowability and physical properties. Properties include blend flowability and uniformity, bulk packing density, compactability, tensile strength, and dissolution. Blending is done through solventless dry mechanical coating of at least one minority API component defined as the API component with the least weight per volume surface coated with nano-sized powders in lesser amounts by wt % of the blend, and preferably less than 10% dry coated of the minority API. An excipient may be dry coated in the lesser amount wherein the excipient is a minority component. Both minority excipient and minority API may be dry coated. Using dry coating instead of dry granulation and/or wet granulation techniques in producing tablets saves manufacturing steps, costs, and produces higher quality tablets with surprisingly higher properties than expected for low flowability solid powdered ingredients.

公开(公告)号：US20240024241A1

公开(公告)日：2024-01-25

申请号：US18221143

申请日：2023-07-12

Applicant: New Jersey Institute of Technology

Inventor： Rajesh N. Dave ,  Sangah Kim ,  Zhixing Lin

IPC: A61K9/14 ,  A61K31/192 ,  A61K45/06 ,  A61K9/16

CPC classification number: A61K9/143 ,  A61K31/192 ,  A61K45/06 ,  A61K9/1682 ,  B82Y5/00

Abstract: High(greater than 30%) and/or low(less than 10%) loaded multiple API powdered/nanoparticle were tabulated with increased flowability and physical properties. Properties include blend flowability and uniformity, bulk packing density, compactability, tensile strength, and dissolution. Blending is done through solventless dry mechanical coating of at least one minority API component defined as the API component with the least weight per volume surface coated with nano-sized powders in lesser amounts by wt % of the blend, and preferably less than 10% dry coated of the minority API. An excipient may be dry coated in the lesser amount wherein the excipient is a minority component. Both minority excipient and minority API may be dry coated. Using dry coating instead of dry granulation and/or wet granulation techniques in producing tablets saves manufacturing steps, costs, and produces higher quality tablets with surprisingly higher properties than expected for low flowability solid powdered ingredients.

公开(公告)号：US10918602B2

公开(公告)日：2021-02-16

申请号：US16150931

申请日：2018-10-03

Applicant: New Jersey Institute of Technology

Inventor： Rajesh N. Dave ,  Lu Zhang ,  Guluzar Gorkem Buyukgoz ,  Eylul Cetindag

IPC: A61K9/16 ,  A61K9/70 ,  A61K45/06 ,  A61K47/10 ,  A61K47/20 ,  A61K31/343 ,  A61K9/00 ,  A61K31/216 ,  A61K47/38 ,  A61K9/50

Abstract: The present disclosure provides improved film based pharmaceutical products containing uniformly distributed drug or active agent particles (e.g., to achieve improved/excellent dissolution control including enhancing dissolution and bioavailability and/or product uniformity). More particularly, the present disclosure provides improved systems/methods for fabricating film based pharmaceutical products by utilizing higher surface modified micronized drug or active agent powders and film forming precursors and drying methods that accomplish improved/efficient drying and provide improved/excellent content uniformity of active pharmaceutical agents in the fabricated film based pharmaceutical products. In exemplary embodiments, the present disclosure provides for an easier means of directly incorporating dry micronized poorly water-soluble drugs or active agent particles (e.g., fenofibrate (“FNB”)) into films. The present disclosure demonstrates some advantages of direct incorporation of surface modified-micronized poorly water-soluble drug or active agent powders in film manufacturing.

公开(公告)号：US09107851B2

公开(公告)日：2015-08-18

申请号：US13651977

申请日：2012-10-15

Applicant: New Jersey Institute of Technology

Inventor： Rajesh N. Dave ,  Daniel To ,  Maxx Capece

IPC: A61K35/00 ,  A61K9/50

CPC classification number: A61K9/5042 ,  A61K9/5063 ,  A61K9/5073 ,  A61K9/5089 ,  A61K35/00

Abstract: The present invention is a solventless method of producing polymer coated active pharmaceutical ingredient that is taste-masked and may be released in relatively short time. It employs high energy vibrations or acoustic mixing of API particles, water soluble coating material particles and hydrophobic polymer particles, with or without use of other pharmaceutically relevant powders as media. Additionally the method is capable of producing individually coated drug particles without agglomeration or the long drying times associated with solvent based coating methods.

Abstract translation: 本发明是一种制造聚合物涂覆的活性药物成分的无溶剂方法，其具有掩味作用并且可在较短时间内释放。 它使用API​​颗粒，水溶性涂层材料颗粒和疏水性聚合物颗粒的高能量振动或声音混合，有或没有使用其它药学上相关的粉末作为介质。 此外，该方法能够产生单独涂覆的药物颗粒而不发生附聚或与溶剂型涂布方法相关的长时间干燥时间。