High penetration compositions and their applications

A penetrating, compositional technology for the prevention, diagnosis and/or treatment of symptoms or diseases in humans, animals and plants, capable of addressing patient pain, needle sticks, infections, etc.

Inactive Publication Date: 2012-01-04
于崇曦
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Poor gastrointestinal absorption of antibiotics when administered orally
Intravenous, subcutaneous, intramuscular injections are not only painful to the patient, must be administered by trained professionals, and may pose other risks such as needle sticks, infection, and other injuries

Method used

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  • High penetration compositions and their applications
  • High penetration compositions and their applications
  • High penetration compositions and their applications

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0321] Example 1: Preparation of HPCs from parent drug

[0322] HPCs are prepared from parent drugs containing at least one carboxyl group.

[0323] In certain embodiments, structural formula F 1 The parent drug represented by -OH can be transformed into a HPC represented by structural formula L-1:

[0324] f 1 -L 2 -T

[0325] Structural formula L-1

[0326] Stereoisomers and pharmaceutically acceptable salts thereof are included, wherein T is defined to be consistent with T in paragraph 0076.

[0327] In certain embodiments, structural formula L-1(F 1 -L 2 -T) represented HPC by structural formula F 1 -W a The represented parent compound or its derivatives (such as acid halides, mixed anhydrides, etc. of the parent drug) are the same as those of the structural formula T-L in Fig. 2 The compound represented by -H is prepared by organic synthesis reaction, wherein: W a selected from OH, halogen, alkylcarbonyloxy, arylcarbonyloxy, alkoxycarbonyloxy, and aryloxycarbon...

Embodiment 2

[0370] Example 2. HPCs capable of penetrating biological barriers

[0371] The rate of penetration of HPCs through human skin is measured in vitro using a modified Franz cell. The Franz cell has two chambers, a top sample chamber and a bottom receiving chamber. Human skin tissue (360-400 [mu]m thick) separating the apical and receptive compartments was obtained from the anterior and posterior regions of the thigh.

[0372] The test compounds are N-acetyl-3-(3,4-diacetoxy-phenyl-L-alanine diethylaminoethyl ester hydrochloride (A), diethylaminopropyl N-acetyl Base-D-3,5,3',5'-tetraiodothyronine hydrochloride (B), 1-piperidinyl-2[4-(4-chlorobenzoyl)phenoxy -2-methyl-propionate hydrochloride (C), 5-(2,5-dimethylphenoxy)-2,2-dimethylpentanoic acid 3-piperidine methyl ester hydrochloride (D ), (S)-3-(Benzamidomethyl)-5-methylhexanoic acid diethylaminoethyl ester hydrochloride (E), N-acetyl-3-(3,4-diacetyl Oxy-phenyl-L-alanine (F) sodium salt, N-acetyl-D-3,5,3',5'-tetraiodothyron...

Embodiment 3

[0378] Example 3: After transdermal administration of the HPC, the distribution of the parent drug and related compounds in the body.

[0379] The HPC of ibuprofen in this example is diethylaminoethyl 2-(p-isobutylphenyl)propionate citrate. The HPC is rapidly converted to its parent drug in vivo, so the concentration detected is that of the parent drug and its related compounds.

[0380] 3.1 After the HPC transdermal administration of ibuprofen, detect the distribution of parent drug and related compounds in rats

[0381] The ibuprofen HPC (10% aqueous solution) of 0.3mmol / kg is coated on the back (10cm 2 ). Table 3 shows the distribution of ibuprofen and diethylaminoethyl 2-(p-isobutylphenyl) propionate hydrochloride (bulomide) in rat organs 2 hours after administration.

[0382] Table 3.1 Distribution of ibuprofen and ibuproamine in rat organs

[0383]

[0384] 3.2 The HPC of ibuprofen can disperse the mother drug ibuprofen and its related compounds to various organs ...

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Abstract

High penetration compositions (HPC) of a parent compound, which are capable of crossing biological barriers with high penetration efficiency. The HPCs are capable of being converted to parent drugs or parent drug-related compounds such as metabolites after crossing one or more biological barriers and thus can render treatments for the conditions that the parent drugs or parent drug-related compounds can. Additionally, the HPCs are capable of reaching areas that their parent drugs or parent drug-related compounds may not be able to access or to render a sufficient concentration at the target areas HPCs of NSAIA, for example, have demonstrated indications such as treating hair loss. A HPC can be administered to a subject through various administration routes, e. g., locally delivered to an action site of a condition with a high concentration or systematically administered to a biological subject and enter the general circulation with a faster rate.

Description

[0001] priority statement [0002] This patent application claims priority to US Patent No. 61 / 120,052, filed December 4, 2008, which is incorporated by reference in this disclosure. technical field [0003] The present invention relates to a composition and a pharmaceutical composition capable of penetrating one or more layers of biological barriers, and methods for using the pharmaceutical composition to prevent, diagnose and / or treat symptoms or diseases of humans, animals and plants. Background technique [0004] Active agents or drugs that are effective in vitro may not be therapeutic in vivo due to difficulty in transport in vivo, especially due to limited ability to cross one or more biological barriers before reaching the site of disease in vivo. [0005] At present, most drugs are administered systemically to reach the site of symptoms or diseases, such as oral administration or parenteral administration. In order for the drug to reach the remote location, systemi...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D209/32A61K31/352A61K45/00
CPCC07D295/088A61K31/352C07D417/04C07D211/34C07D231/14A61K47/48023C07D491/048C07D207/34C07D313/14C07D501/22C07D215/18C07D209/42C07D277/56A61K31/10A61K31/165A61K31/5575A61K31/567A61K31/57A61K31/64A61K47/54A61P1/00A61P1/04A61P1/08A61P1/16A61P1/18A61P11/00A61P11/14A61P15/00A61P15/04A61P15/08A61P15/18A61P17/00A61P17/02A61P17/06A61P17/10A61P17/14A61P17/16A61P19/08A61P19/10A61P21/00A61P21/04A61P25/00A61P25/04A61P25/16A61P25/28A61P27/00A61P27/02A61P27/06A61P27/12A61P29/00A61P3/00A61P3/04A61P31/00A61P31/04A61P31/12A61P33/14A61P35/00A61P35/02A61P3/06A61P37/02A61P37/06A61P37/08A61P43/00A61P5/14A61P5/16A61P5/34A61P7/02A61P9/00A61P9/10A61P9/12A61P3/10Y02A50/30C07C229/32C07C229/36A61K31/198A61K8/31A61K31/015C07C15/30C07C15/38
Inventor 于崇曦
Owner 于崇曦
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