Patent for Oral Pharmaceutical Composition for κ-Opioid Receptor Related Diseases
According to GlobalData’s company profile on Haisco Pharmaceutical Group, peptide nano-particle conjugates was a key innovation area identified from patents. Haisco Pharmaceutical Group‘s grant share as of June 2023 was 1%. Grant share is based on the ratio of number of grants to total number of patents.
A recently filed patent (Publication Number: US20230172866A1) describes an oral pharmaceutical composition for the treatment of diseases or conditions related to the κ-opioid receptor. The composition includes compound A as the active ingredient.
The composition also includes an absorption enhancer, which can be selected from various options such as N-[8-(2-hydroxybenzoyl)amino]octanoic acid or a pharmaceutically acceptable salt thereof, 4-[(4-chloro-2-hydroxy-benzoyl)amino]butyric acid or a pharmaceutically acceptable salt thereof, lauroyl-L-carnitine or a hydrochloride thereof, sodium caprylate, sodium caprate, capric acid, or caprylocaproyl macrogolglyceride.
The weight ratio of compound A to the absorption enhancer can vary depending on the specific enhancer used. For example, when using N-[8-(2-hydroxybenzoyl)amino]octanoic acid or its salt, the ratio is 1:20 to 1:80. When using 4-[(4-chloro-2-hydroxy-benzoyl)amino]butyric acid or its salt, the ratio is 1:20 to 1:200. When using lauroyl-L-carnitine or its hydrochloride, the ratio is 1:10 to 1:150. When using sodium caprate, the ratio is 1:50 to 1:200. And when using caprylocaproyl macrogolglyceride, the ratio is 1:600 to 1:3600.
The composition may also contain non-active ingredients such as fillers, binders, disintegrants, pH regulators, surfactants, and lubricants. The specific combination and weight ratios of these non-active ingredients can vary depending on the desired formulation. For example, if a lubricant is used, the weight ratio of compound A to the absorption enhancer to the lubricant is 1:(20-200):(0.2-2). Magnesium stearate is mentioned as a specific lubricant option.
The patent also describes various methods for preparing the oral pharmaceutical composition, including direct mixing of compound A, the absorption enhancer, and other non-active ingredients, wet granulation followed by filling into capsules or compression into tablets, dispersion in a hydrophobic medium, preparation of a solution in purified water, or dissolution, drying, and pulverization followed by filling into capsules or compression into tablets.
Overall, this patent presents an oral pharmaceutical composition containing compound A and an absorption enhancer for the treatment of diseases or conditions related to the κ-opioid receptor. The composition can be formulated with various non-active ingredients and prepared using different methods.
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