Pharmaceutical formulations for sustained release dinalbuphine sebacoyl
A technology of dinalbuphine sebacoyl and pharmaceutical preparations, applied in the field of pharmaceutical compositions, capable of solving problems such as impractical or undesired by patients
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[0099] The present invention also provides a preparation method for the preparation of the nalbuphine ester prodrug sustained-release preparation with a predetermined release period, each of which includes:
[0100] 1) Providing an oil-miscible retention solvent and a pharmaceutically acceptable oil, wherein the weight ratio of the oil-miscible retention solvent to the pharmaceutically acceptable oil ("retention solvent / oil ratio") is based on a predetermined release period adjust; and
[0101] 2) The nalbuphine ester prodrug is mixed with the oil miscibility maintaining solvent and the pharmaceutically acceptable oil to form a homogeneously dissolved solution.
[0102]In some embodiments, the step of admixing said prodrug with said holding solvent and said oil comprises mixing said prodrug with a mixture of said oil miscible holding solvent and said pharmaceutically acceptable oil. For example, if the predetermined release period is set to be greater than 14 days, the holdin...
Embodiment 1
[0139] Example 1. In vitro release studies of formulations of the invention with different BB / oil ratios
[0140] (1) Preparation of the preparation of the present invention
[0141] Eight formulations of the invention were prepared according to Table 1A and Table 1B with various SDE concentrations (50 mg / mL-150 mg / mL) and various weight ratios of benzyl benzoate to sesame oil ("BB / oil ratio"), or various weight ratios ("BB+BA / oil ratio") of a mixture of benzyl benzoate and benzyl alcohol to sesame oil (0.5-19). Among them, AF4, R2, N7 and N9 preparations are prepared according to the following method A.
[0142] Method A:
[0143] Solvent systems (i.e., benzyl benzoate (with or without benzyl alcohol) and sesame oil mixture). The resulting solvent mixture was vortexed or stirred at room temperature to thoroughly mix the ingredients. Predetermined amounts of SDE were weighed according to the SDE concentrations listed in Tables 1A and 1B, respectively, and added to volumet...
Embodiment 2
[0162] Example 2. Comparison between Method A and Method B
[0163] (1) When the ratio of BB / oil is about 1, the suspension with sediment prepared via method A
[0164] SDE was added directly to the mixture of sesame oil and benzyl benzoate (ie Method A of Example 1) to prepare two samples (1 and 2). For sample 1, 5.5 mL of sesame oil and 4.5 mL of benzyl benzoate were mixed to form an oily solvent mixture, and then 750 mg of SDE was added to the solvent mixture. The resulting mixture was ultrasonically oscillated for at least 2 hours, left overnight at room temperature, and then centrifuged at 3000 rpm for 10 minutes, and the supernatant clear solution was collected and analyzed by high performance liquid chromatography (HPLC). Sample 2 was prepared according to the procedure for preparing sample 1, except that the amount of SDE was changed to 1000 mg. The ratio of "weight of original added SDE" to "volume of benzyl benzoate and sesame oil" was 75 mg / mL and 100 mg / mL for sa...
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Abstract
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