Formulations for treatment of mucosal associated conditions with an immune response modifier

A technology of immune response and regulator, applied in the direction of antiviral agents, medical preparations with non-active ingredients, medical preparations containing active ingredients, etc., can solve the problems of obstruction, poor systemic transmission, poor permeability, etc.

Inactive Publication Date: 2004-12-15
3M INNOVATIVE PROPERTIES CO
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0004] While some beneficial effects of IRMs are known, the provision of therapeutic efficacy by topical application of IRMs for the treatment of specific conditions at

Method used

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  • Formulations for treatment of mucosal associated conditions with an immune response modifier
  • Formulations for treatment of mucosal associated conditions with an immune response modifier
  • Formulations for treatment of mucosal associated conditions with an immune response modifier

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0272] Example 1 Safety, pharmacokinetics (PK) and Pharmacodynamic (PD) assessment

[0273] method

[0274] This was a single-dose, randomized, double-blind dose-escalation study (controlled with placebo) evaluating 5 doses of imiquimod. A cream formulation of 50, 100, 150, 200 and 250 mg of imiquimod was applied to the cervix for 8 hours. The ingredients of the imiquimod cream (Formulation A) used in this study are listed in Table I below. Each dose group consisted of 8 subjects (6 active drug, 2 placebo), two subjects were treated as dose leaders and the remaining 6 were treated following dose leader acceptable response. Safety was assessed by adverse events (AEs), laboratory tests and, if required, colposcopy with a cervical photographic recorder pre-dose, 24 hours post-dose and 48 hours post-dose. Systemic exposure (PK) was determined by measuring imiquimod and its metabolites in 48 hours post-dose, by cytokine: TNF-α ( TNF-α), interferon-α (IFN-α), interleukin-1 ...

Embodiment 2

[0279] Example 2 Preparation of Pharmaceutical Formulation B

[0280] This example describes a novel formulation for vaginal application which is a stable formulation with high viscosity and good shelf life, passing the EP Preservative Effectiveness Test (PET) criteria. The w / w% of the components of this formulation (Formulation B) are listed in Table 2 below.

[0281] Imiquimod and Span85 were dissolved in isostearic acid. Pluronic F68, EDTA, Carbopol 974P, Propylene Glycol, Sorbic Acid and Methylparaben are dissolved in water. After emulsification to form an oil-in-water emulsion, sodium hydroxide is added to reach a pH of about 5.2. The pH range of the formulation is about 4.8-6.0.

[0282] Table 2

[0283] components

Embodiment 3

[0284] Example 3 Preparation of Pharmaceutical Formulations C-F

[0285] Pharmaceutical formulations C-F were prepared with the components in Table 3 below. Formulations C-F were prepared in the same manner as Formulation B in Example 2.

[0286] components

[0287] * PG is propylene glycol

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PUM

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Abstract

Immune response modifier (IRM) compounds - imidazoquinoline amines, imidazopyridine amines, 6,7-fused cycloalkylimidazopyridine amines, 1,2-bridged imidazoquinoline amines, thiazolo- and oxazolo- quinolinamines and pyridinamines, imidazonaphthyridine and tetrahydroimidazonaphthyridine amines - are useful for the treatment of conditions at and below the mucosal surfaces by administering a therapeutically effective amount of such compounds to the mucosal surface. Novel pharmaceutical formulations are provided. In one embodiment, the pharmaceutical formulations are advantageous for treatment of cervical conditions such as cervical dysplasias including cervical intraepithelial neoplasias.

Description

field of invention [0001] The present invention relates to immunomodifying imidazoquinolinamines, imidazopyridineamines, 6,7-fused cycloalkylimidazopyridineamines, 1,2-bridged imidazoquinolinamines, thiazolo- and oxazolo- Pharmaceutical formulations and methods for the administration of quinolinamines and pyridinamines, imidazolidines and tetrahydroimidazolidines to mucosal surfaces. In one embodiment, the present invention provides formulations and methods for topical administration to the cervix, particularly useful in the treatment of cervical conditions, such as cervical dysplasia, including those associated with human papillomavirus (HPC). Background of the invention [0002] Many imidazoquinolinamines, imidazopyridineamines, 6,7-fused cycloalkylimidazopyridineamines, 1,2-bridged imidazoquinolinamines, thiazolo- and oxazolo-quinolinamines and Pyridinamine, imidazolidine and tetrahydroimidazolidine compounds possess potent immunostimulatory, antiviral and antitumor (inc...

Claims

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Application Information

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IPC IPC(8): C07D471/04A61K9/00A61K31/437A61K31/44A61K31/4745A61K47/10A61K47/12A61K47/14A61K47/26A61K47/32A61P1/00A61P1/16A61P7/02A61P15/00A61P15/02A61P17/00A61P17/06A61P25/28A61P29/00A61P31/20A61P31/22A61P35/00A61P37/02A61P37/04C07D498/04C07D513/04
CPCA61K31/437C07D471/04A61K47/12A61K9/0034A61K47/10A61K9/0014A61K31/4745A61K31/44A61P1/00A61P1/16A61P15/00A61P15/02A61P17/00A61P17/06A61P25/28A61P29/00A61P31/12A61P31/20A61P31/22A61P35/00A61P37/02A61P37/04A61P7/02
Inventor K·帕利斯J·Z·李M·J·约维科夫斯基R·L·米勒R·D·斯科维尔奇英斯基T·F·布什
Owner 3M INNOVATIVE PROPERTIES CO
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