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A technology of composition and water-based composition, which is applied in the direction of drug combination, drug delivery, non-active ingredients of polymer compounds, etc.
Pending Publication Date: 2021-06-25
SEIKAGAKU KOGYO CO LTD
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These target both immediate pain relief and long-term pain relief by improving functional impairment, but are still in the development stage and have not yet been licensed.
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[0196] Preferred embodiments of the present invention are exemplified below.
[0197] [1] A pharmaceutical composition comprising a compound represented by formula (1) and component (A):
[0198] Component (A): selected from nonionic surfactants, hydroxyalkylated cyclodextrins, C 1 ~C 3 Monohydric alcohol, C 2 ~C 3 Diol, C 3 ~C 6 At least one compound selected from the group consisting of triols, polyalkylene glycols, γ-lactones, polyvinylpyrrolidone, chlorogenic acids, alkyl sulfates, and salts thereof,
[0199]
[0200] In formula (1), a is not less than 0.01 and not more than 0.7, a+b is 1, n is an integer not less than 25 and not more than 25000, and the arrangement of each disaccharide structural unit is optionally random or block-like. R in the sugar structural unit is each independently a carboxyl group or a carboxylate group.
[0201] [2] The pharmaceutical composition according to [1] above, wherein the component (A) is selected from the group consisting of ...
Embodiment
[0279] Hereinafter, preferred embodiments of the present invention will be described in more detail using examples, but the present invention is not limited at all by the following examples.
Synthetic example
[0281]According to the method described in the examples of International Publication No. 2005 / 066214, hyaluronic acid derivatives (compounds represented by formula (1)) were synthesized (a: 0.18, n: 2 k, the mass average molecular weight of hyaluronic acid :800 000).
[0282] More specifically, it was synthesized by the following method.
[0283] Dissolve 2.155 g (10.5 mmol) of 2-bromoethylamine hydrobromide in 20 mL of dichloromethane, add 1.463 mL (10.5 mmol) of triethylamine under ice-cooling, and then add di-tert-butyl dicarbonate (Boc 2 O) 5 mL of a dichloromethane solution of 2.299 g (10.5 mmol) was stirred. After stirring at room temperature for 90 minutes, ethyl acetate was added, followed by liquid-separation washing with a 5% by weight aqueous citric acid solution, water, and saturated brine. After dehydration with sodium sulfate, the solvent was distilled off under reduced pressure to obtain Boc-aminoethyl bromide.
[0284] Ice-cool 5 mL of a dimethylformamide (D...
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Abstract
The purpose of the present invention is to provide a pharmaceutical composition that comprises a hyaluronic acid derivative represented by formula (1) in the description or a pharmaceutically acceptable salt thereof, a method for producing the same, and a method for inhibiting the formation of diclofenac lactam from a compound represented by formula (1). Provided is a method for inhibiting the formation of diclofenac lactam from a compound represented by formula (1) in the description, said method comprising allowing the compound of formula (1) to coexist with component (A) that is at least one kind of compound selected from the group consisting of a nonionic surfactant, a hydroxyalkylated cyclodextrin, a C1 to C3 monoalcohol, a C2 to C3 dialcohol, a C3 to C6 trialcohol, a polyalkylene glycol, gamma-lactone, polyvinylpyrrolidone, a chlorogenic acid, an alkyl sulfate and salts thereof. Also provided are a method for producing a pharmaceutical composition that comprises a compound represented by formula (1) and component (A), and a pharmaceutical composition produced thereby.
Description
technical field [0001] The present invention relates to pharmaceutical compositions comprising hyaluronic acid derivatives. Background technique [0002] Osteoarthritis (hereinafter, also referred to as "OA" in this specification), which is a dysfunction caused by joint pain and joint degeneration, is the most common joint disease in the world, and it has become a problem in the daily life of elderly people in particular. One of the leading causes of physical disability. Moreover, like OA, rheumatoid arthritis (hereinafter, also referred to as "RA" in this specification.) known as polyarthritis is known as a disease accompanied by joint swelling and pain. In RA, if the condition persists for a long time and the symptoms progress, the cartilage and bone are destroyed to cause degeneration and deformation, resulting in a physical disorder that causes problems in daily life such as narrowing the range of joint motion. [0003] Currently, preparations using hyaluronic acid and...
Claims
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