Sibutramine HCL Formulation
P-Chlorophenylacetonitrile, KOH and acetonitrile were mixed at 25%: 1,3-dibromopropane was slowly added dropwise.
>After completion of the dropwise addition, stirring was continued for 1 hour, and distilled water was added thereto, followed by extraction with ethyl acetate. The extract was washed with water, saturated with brine, and dried.
>Filtration, concentration under reduced pressure, and distillation, and fractions of 160 ° C / 2.13 kPa were collected to obtain a compound (I) in a yield of 73% to 74%.
>The magnesium flakes were dissolved in anhydrous THF, and isobutyl bromide was added dropwise, and then reacted for 1 h. Then, a solution of the compound (I) in anhydrous THF was slowly added dropwise, and the mixture was refluxed for 4 h and cooled to room temperature.
>This was dropped into a solution of KBH4 in isopropanol and refluxed for 4 h.
>Let it cool, add water and extract with ethyl acetate. The extract was washed with water and saturated saline and dried.
>After filtration, the filtrate was concentrated under reduced pressure and then distilled, and a fraction of 170 ° C / 0.67 kPa was collected to obtain a compound (II) in a yield of 76% to 79%.
The compound (II), formic acid and 1/2 formaldehyde solution were stirred at 90 to 92 ° C for 1 h.
>An additional 1/2 formaldehyde solution was added and the reaction was continued for 1 h. It was cooled to room temperature, and slowly poured into a crushed ice of sodium hydroxide with stirring, followed by extraction with diethyl ether. The extract was washed with saturated brine, washed with water and dried. Filtration and concentration of the filtrate gave a yellowish sibutramine in a yield of 94%.
>The analytical sample can be recrystallized from diethyl ether with a melting point of 52 to 53 °C.
>Sibutramine was dissolved in methanol, concentrated hydrochloric acid was added, and reacted at 50 to 60 ° C for 10 min. At least methanol was recovered by distillation under reduced pressure, and water was added thereto, stirred, and cooled in an ice bath.
>Filtration and washing, the crude sibutramine hydrochloride was obtained, and recrystallized from methanol-water to obtain white crystalline sibutramine hydrochloride, melting point 194 ° C, yield 83%.
Sibutramine hcl max is 1.2 h; food delays T max by approximately 3 h. Approximately 77% of a single oral dose is absorbed. Steady state is reached within 4 days.
Sibutramine hcl is extensively bound and is rapidly and extensively distributed into tissues. Highest concentrations are in liver and kidneys.
Sibutramine hcl undergoes extensive first-pass metabolism and is metabolized primarily by the CYP-450 3A4 isoenzyme. The pharmacologically active metabolites are mono- and di-desmethyl M 1 and M 2 .
Sibutramine hcl ½ is 1.1 h. Oral clearance is 1,750 L/h, and approximately 85% is excreted in urine.
Store at room temperature in a tightly closed container. Protect from heat and moisture.
Sibutramine hydrochloride is a kind of diet drug, which is the hydrochloride form of sibutramine. The pharmacological effect is exactly the same as that of sibutramine, but the stability and solubility are better than sibutramine.
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