IP Library Patent Application 11551543
Patent Application
App. No. 11/551,543

COMPOSITIONS CAPABLE OF FACILITATING PENETRATION ACROSS A BIOLOGICAL BARRIER

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Patent No.
US None
App. No.
11/551,543
Abstract

This invention relates to novel penetrating compositions including one or more effectors included within a water soluble composition, immersed in a hydrophobic medium. The invention also relates to methods of treating or preventing diseases by administering such penetrating compositions to affected subjects.

Claims (57)

1 . A composition comprising:

a) a therapeutically effective amount of at least one effector;

b) one or more membrane fluidizing agents; and

c) a hydrophobic medium,

wherein the composition, when administred to a subject, provides effective translocation of the effector across a biological barrier.

2 . The composition of claim 1 further comprising (d) one or more surface active agents.

3 . The composition of claim 1 further comprising (e) one or more stabilizers.

4 . The composition of claim 1 , wherein element (a) is included within a water soluble composition, wherein said water soluble composition is solubilized in a hydrophilic or partially hydrophilic solvent.

5 . The composition of claim 4 , wherein said water soluble composition is a lyophilized particle.

6 . A composition comprising:

a) a therapeutically effective amount of at least one effector;

b) polyvinyl pyrrolidone or dextran;

c) CaCl 2 or MgCl 2 ;

d) sodium dodecanoate;

e) sodium octanoate;

f) geraniol;

g) 1-octanol;

h) sorbitan monopalmitate;

i) lecithin phosphatidyl choline;

j) glycerol glycryl mono-oleate;

k) ethyl isovalerate;

l) caster oil; and

wherein the composition, when administered to a subject, provides effective translocation of the effector across a biological barrier.

7 . The composition of claim 6 , further comprising silicon dioxide.

8 . The composition of claim 6 , further comprising poloxamer.

9 . The composition of claim 6 , further comprising glyceryl tributyrate.

10 . A composition comprising:

a) a therapeutically effective amount of at least one effector;

b) polyvinyl pyrrolidone or dextran;

c) CaCl 2 or MgCl 2 ;

d) sodium dodecanoate;

e) sodium octanoate;

wherein (a)-(e) are included within a water soluble composition, which is solubilized in a hydrophilic or partially hydrophilic solvent, lyophilized, and immersed in a mixture comprising:

f) castor oil;

g) geraniol;

h) 1-octanol;

i) sorbitan monopalmitate;

j) phosphatidyl choline;

k) glyceryl monooleate;

l) ethyl isovalearate;

wherein the composition, when administered to a subject, provides effective translocation of the effector across a biological barrier.

11 . The composition of claim 10 , further comprising silicon dioxide.

12 . The composition of claim 10 , further comprising poloxamer.

13 . The composition of claim 10 , further comprising glyceryl tributyrate.

14 . A composition comprising, a membrane fluidizing agent and an effector in solid form, wherein the effector is suspended in a hydrophobic medium, and wherein the composition, when administered to a subject, provides at least 5% adsorption of the effector across a biological barrier.

15 . The composition of claim 14 , further comprising one or more surface active agents.

16 . The composition of claim 14 , further comprising one or more stabilizers.

17 . The composition of claim 14 , wherein said membrane fluidizing agent is a medium chain alcohol which has a carbon chain length of from 5 to 15 carbon atoms.

18 . The composition of claim 17 , wherein said medium chain alcohol is selected from the group consisting of linear alcohols, branched alcohols, cyclic alcohols, and aromatic alcohols.

19 . The composition of claim 18 , wherein said linear alcohol is selected from the group consisting of: pentanol, hexanol, heptanol, octanol, nonanol, decanol, undecanol, dodecanol, tridecanol, tetradecanol, and pentadecanol.

20 . The composition of claim 18 , wherein said branched alcohol is geraniol, rhodinol, citronellol, or farnesol.

21 . The composition of claim 18 , wherein said cyclic alcohol is terpineol, myrtenol, perillyl alcohol.

22 . The composition of claim 14 , wherein said aliphatic hydrophobic medium is selected from the group consisting of: mineral oil, paraffin, fatty acids, mono-glycerides, di-glycerides, tri-glycerides, ethers, and estrs, and combinations thereof.

23 . A method for treating obesity comprising administering a composition comprising a composition of claim 1 , wherein the effector is growth hormone.

24 . A method for treating a bone disorder comprising administering a composition comprising a composition of claim 1 , wherein the effector is parathyroid hormone.

25 . The method of claim 24 , wherein the bone disorder is selected from osteoporosis, osteopenia or Paget's disease.

26 . The method of claim 24 , wherein the parathyroid hormone is PTH(1-34).

Assignments (3)
RELEASE OF SECURITY INTEREST Recorded Feb 28, 2013
From: GENERAL ELECTRIC CAPITAL CORPORATION
To: CHIASMA, INC.
Reel/Frame 029896/0773 →
SECURITY AGREEMENT Recorded Sep 26, 2012
From: CHIASMA, INC.
To: GENERAL ELECTRIC CAPITAL CORPORATION, AS AGENT
Reel/Frame 029043/0400 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded May 30, 2007
From: BEN-SASSON, SHMUEL A.
To: CHIASMA INC
Reel/Frame 019352/0715 →