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Isotretinoin oral-mucosal formulations and methods for using same

A technology of tretinoin and mucoadhesion, which is applied in the direction of pill delivery, pharmaceutical formulations, medical preparations of non-active ingredients, etc.

Pending Publication Date: 2020-04-17
SKYLINE BIOSCI LLC
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Currently, there are no approved drug treatments for this type of oral precancerous lesion (OPL)

Method used

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  • Isotretinoin oral-mucosal formulations and methods for using same
  • Isotretinoin oral-mucosal formulations and methods for using same
  • Isotretinoin oral-mucosal formulations and methods for using same

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0124] Example 1. Drug Dissolution Test Protocol

[0125] The aim of this study was to develop a drug dissolution (drug release) method for isotretinoin oral mucoadhesive films. The criterion to be achieved is a dissolution rate greater than 85% at the end of the dissolution.

[0126] The dissolution apparatus used was a Logan DISSO III-7 (USP 3 and 7 dissolution apparatus in one unit) manufactured by Logan Instruments, Somerset, NJ. The program has been set up to run the tests with a USP 3 instrument. Sampling was performed using a LoganDSC-37 System Controller / Logan SYP-8L Syringe Pump and a Logan SCR-160 SamplerCollector.

[0127] Drug assays in dissolution media were determined using an in-house method by an Agilent HPLC / UV system equipped with ChemStation. The medium used for dissolution studies was 1% (w / w) aqueous solution of N,N-dimethyldodecylamine-N-oxide (DDAO), prepared from 30% DDAO solution, supplied by Sigma-Aldrich. Other operating parameters were: one memb...

Embodiment 2

[0129] Example 2. Mucoadhesive formulation A

[0130] Formulation A was formulated for an orally dissolvable and erodible thin flexible film with and without a soft (EVA polymer) backing film. The formulation is designed for slow release of the drug.

[0131] Table 1. 0.2% Oromucosal Patch Formulations

[0132]

[0133] Dissolve or disperse all components in acetone / ethanol / water (v / v / v ratio is 24 / 26 / 42) mixed solvent, and cast directly on the EVA polymer backing film or release liner, and in Dry at 75°C for 15 minutes to produce a dry film. For oral discs with film backing, the cast / dried film was peeled from the release liner to obtain a freestanding film. These films were die cut into 1 inch x 1 inch unit dose discs and tested accordingly.

[0134] In vitro drug release studies were performed using Formulation A and using the drug dissolution protocol described in Example 1. The results of the study indicated that the drug was completely released in about 60 minute...

Embodiment 3

[0137] Example 3. Mucoadhesive formulation B

[0138] Mucoadhesive Formulation B was formulated to shorten the drug release time in the oral cavity and to replace the non-ingestable EVA film with a dissolvable or ingestible backing film. The bioadhesive polymer of Formulation A (ie, Noveon AAl (polycarbophil)) was replaced with a more water-soluble, polyvinylpyrrolidone (PVP)-based polymer. Formulation B comprises two layers: a mucoadhesive layer and an ingestible layer formulated from a polymethacrylate (Eudragit) based polymer (Evonik), which is typically used as a tablet film coat for oral solid dosage forms. Two-layer configurations were prepared by two casting processes.

[0139] Table 2. 0.3% Isotretinoin Formulations for Immediate Release

[0140] Element Wet grams dry part Dry% water 4 ethanol 35 Kollidon 90F 8 8 68.1％ Kollidon VA64 2 2 17.0％ Isotretinoin 0.04 0.04 0.3％ PEG400 1.5 1.5 12.8％ Prop...

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Abstract

Disclosed herein, in part, is a pharmaceutical formulation comprising isotretinoin or a pharmaceutically acceptable salt thereof, and a mucoadhesive polymer. A method of treating a mucosal disease comprising administering a disclosed pharmaceutical formulation to a subject in need thereof is also provided herein.

Description

[0001] Cross References to Related Applications [0002] This application claims priority to U.S. Provisional Application No. 62 / 526,743, filed June 29, 2017, the contents of which are incorporated herein by reference in their entirety. [0003] technical background [0004] Isotretinoin is 13-cis-retinoic acid and is a derivative of vitamin A. Isotretinoin was originally developed and approved for the treatment of acne. However, it has been studied extensively for the treatment of a variety of diseases, including neuroblastoma, recurrent prostate cancer, leukemia, high-grade glioma, head and neck cancer, and multiple myeloma, certain skin disorders Examples include xeroderma pigmentosa, gram-negative folliculitis, intractable rosacea, pyoderma facial, lichen planus generalized, psoriasis, cutaneous lupus erythematosus, comedogenic eruptions, and squamous cell carcinoma, as well as mucosal disorders . Isotretinoin was initially developed as capsules, followed by gel and crea...

Claims

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Application Information

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IPC IPC(8): A61K9/00A61K9/20A61K31/203A61P31/00A61P35/00
CPCA61K9/006A61K9/2027A61K31/201A61K31/203A61K47/10A61K47/32A61P31/00A61P35/00A61K31/202A61K47/02
Inventor H·S·谭S·L·钟
Owner SKYLINE BIOSCI LLC
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