Solid compositions comprising a GLP-1 agonist and a salt of N-(8-(2-hydroxybenzoyl)amino)caprylic acid
A technology of GLP-1 and hydroxybenzoyl, which can be used in drug combinations, medical preparations containing active ingredients, pill delivery, etc., and can solve problems such as low exposure bioavailability
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preparation example Construction
[0056] In some embodiments, the method of preparing the tablet comprises: a) wet granulating a mixture comprising a GLP-1 agonist, a delivery agent, and a binder; b) optionally drying the wet granules; c) granulating The dried wet granulation is mixed with at least one filler, and at least one lubricant or glidant; then d) compressing the mixture into tablets. The granulation may be wet granulation or dry granulation.
[0057] Disintegration time: In some embodiments, the tablet has a disintegration time of 7 minutes to 15 minutes, such as 8 minutes to 13 minutes. The disintegration time can be determined using a Pharma Test PTZ AUTO disintegration tester. The disintegration apparatus consisted of a basket with 2x6 plastic tubes open at the top and at the bottom, the bottom of which was covered by a screen. Tablets are placed in a plastic tube and a disk for automatic disintegration detection is placed above the tablet. In a 1 L beaker, the basket was immersed in 800 ml ...
Embodiment approach
[0078] 1. A solid composition for oral administration, comprising a GLP-1 agonist and N-(8-(2-hydroxybenzoyl)amino) octanoate, wherein the N-(8-(2-hydroxy The amount of benzoyl)amino)octanoate is at least 0.6 mmol.
[0079] 2. A solid composition for oral administration, comprising a GLP-1 agonist and N-(8-(2-hydroxybenzoyl) amino) octanoate, wherein the N-(8-(2-hydroxy The amount of benzoyl)amino)octanoate is at least 0.8 mmol.
[0080] form of composition
[0081] 3. The composition according to any one of the preceding embodiments, wherein said composition is in the form of a tablet.
[0082] 4. The composition according to any one of the preceding embodiments, wherein the tablet has a weight of 175-1000 mg.
[0083] 5. The composition according to any one of the preceding embodiments, wherein the tablet has a weight of 200-800 mg.
[0084] 6. The composition according to any one of the preceding embodiments, wherein the weight of the tablet is selected from 200 mg, e...
Embodiment 1
[0143] The aim of this study was to evaluate the oral bioavailability of a series of compositions comprising semaglutide and SNAC in beagle dogs.
[0144] method
[0145] Animals, Dosing and Blood Collection
[0146] Twenty-four male and 24 female Beagle dogs, weighing 6-11 kg during the study period, were used in the study. Dogs were dosed on an empty stomach. The compositions were administered to groups of Beagle dogs, each group consisting of 4 male and 4 female dogs, by a single oral administration. Blood samples were collected at the following time points: predose, postdose 0.25, 0.5, 0.75, 1, 1.5, 2, 2.5, 3, 4, 6, 8, 24, 48, 72, 96, 120, 144, 192 and 240 hours.
[0147] An intravenous (i.v.) solution (20 nmol / mL in a pH 7.4 solution containing 0.1 mg / ml Tween 20, 5.5 mg / ml phenol, 1.42 mg / ml Na2HPO4, and 14 mg / ml propylene glycol) was dissolved in 0.1 mL The dose volume per kg was administered to the same group of dogs in one dosing group (n=8). Blood samples w...
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Abstract
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