Compositions, methods, and systems relating to controlled crystallization and/or nucleation of molecular species

Patent metadata

Field	Value
Publication number	US-2016129019-A1
Application number	US-201514808992-A
Country	US
Kind code	A1
Filing date	Jul 24, 2015
Priority date	Aug 23, 2010
Publication date	May 12, 2016
Grant date	—

Abstract

The present invention generally relates to compositions, methods, and systems relating to controlled crystallization and/or nucleation of a molecular species. In some embodiments, the crystallization and/or nucleation of the molecular species may be controlled by tuning the surface chemistry and/or the morphology of a crystallization substrate. In some embodiments, the molecular species is a small organic molecule (e.g., pharmaceutically active agent).

First claim

What is claimed:

1 - 6 . (canceled)

7 . A method of making a pharmaceutical product, comprising:
crystallizing a pharmaceutically active agent on at least one surface of or associated with at least one excipient, wherein the at least one excipient promotes crystallization of the pharmaceutically active agent and the at least one excipient comprises an imprinted surface having a plurality of surface features selected to be complimentary to a known shape and/or angle(s) of a selected known crystal structure of the pharmaceutically active agent; and forming a pharmaceutically acceptable composition comprising the pharmaceutically active agent and the at least one excipient wherein the process is free or essentially free of mechanical steps for combining the pharmaceutically active agent with the at least one excipient.

8 - 11 . (canceled)

12 . The method of claim 7 , wherein the pharmaceutically active agent is aspirin or acetaminophen.

13 - 18 . (canceled)

19 . The method of claim 7 , wherein the at least one excipient comprises a polymeric material.

20 . The method of claim 19 , wherein the polymeric material is a hydrogel.

21 . The method of claim 20 , wherein the polymeric material is formed using UV polymerization.

22 . The method of claim 20 , wherein the polymeric material is formed by reacting at least one monomer and a crosslinking agent using UV irradiation.

23 - 24 . (canceled)

25 . The method of claim 7 , wherein the plurality of surface features comprises a plurality of wells.

26 . The method of claim 7 , wherein the shape of the surface features are triangles, squares, rectangles, trapezoids, pentagons, hexagons, or octagons.

27 . The method of claim 7 , wherein the surface features have an average cross section of greater than about 10 nm.

28 . The method of claim 7 , wherein the surface features have an average cross section between about 10 nm and about 1000 nm.

29 . The method of claim 28 , wherein the surface features have an average depth of less than about 10 mm.

30 . The method of claim 7 , wherein the surface features have an average depth of between about 50 nm and about 1 nm.

31 - 33 . (canceled)

34 . The method of claim 7 , wherein a portion of the surface comprises a plurality of functional groups complimentary to a plurality of functional groups of the pharmaceutically active agent.

35 . (canceled)

36 . The method of claim 34 , wherein the surface comprising the plurality of functional groups is the surface comprising the plurality of surface features.

37 . (canceled)

38 . The method of claim 34 , wherein the plurality of functional groups comprises a plurality of hydroxyl functional groups, a plurality of carboxylic acid ester functional groups, a plurality of nitrogen containing base functional group, a plurality of aryl functional groups, a plurality of carboxyl functional group, a plurality of tertiary amide functional groups, or combinations thereof.

39 . The method of claim 7 , wherein the surface features have an average cross section between about 10 nm and about 500 nm.

40 . The method of claim 7 , wherein the surface features have an average cross section between about 10 nm and about 100 nm.

41 . The method of claim 28 , wherein the surface features have an average depth of less than about 500 nm.

42 . The method of claim 28 , wherein the surface features have an average depth of less than about 5 nm.

43 . The method of claim 7 , wherein the surface features have an average depth of between about 30 nm and about 1 nm.

Assignees

• Massachusetts Inst Technology

Inventors

• Trout Bernhardt Levy
• Doyle Patrick S
• Hatton Trevor Alan
• Myerson Allan Stuart
• Diao Ying
• Helgeson Matthew E

Classifications

• A61K9/146

  with organic macromolecular compounds · CPC title

• A61K31/616 Primary

  by carboxylic acids, e.g. acetylsalicylic acid · CPC title

• A61K31/167

  having the nitrogen of a carboxamide group directly attached to the aromatic ring, e.g. lidocaine, paracetamol · CPC title

• B01D9/00

  Crystallisation (crystallisation directly from the vapour phase B01D7/02; making single crystals C30B {; crystallisation as part of the Bayer process also classified in C01F7/14}) · CPC title

• B82Y5/00

  Nanobiotechnology or nanomedicine, e.g. protein engineering or drug delivery · CPC title