Bupivacaine hydrochloride raw Powder CAS 138-52-3 Bupivacaine hcl

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Bupivacaine hydrochloride Usage and Synthesis.

Bupivacaine hydrochloride injection was used for local infiltration anesthesia, peripheral nerve block and intraspinal block. Lidobupivacaine injection for anesthesia of local or regional peripheral nerves during eye surgery (e.g. extra-ocular, retrobulbar or facial anesthesia).

Peculiarity of Bupivacaine hydrochloride.

(1) The anesthetic force is strong (about 4 times that of capocaine);

(2) the duration is longer (generally up to about 5 hours, up to more than 10 hours);

(3) Less impact on the respiratory system and circulatory system;

(4) Pregnant women use this product is not easy to spread and affect the fetus. In foreign countries, this product has been a relatively mature product (has been included in the 1973 edition of the British Pharmacopoeia), and the literature reports on its synthesis are also relatively rich, and the synthesis route is also introduced in detail in many domestic literature reports. The invention mainly relates to the last step of the alkylation reaction and the salting reaction. According to the literature, most of the alkylation reactions are carried out in the solvent DMF, and after the reaction is completed, the alkylation reaction is added to the ice water to obtain the bupivacaine base. The salting reaction is to dissolve the bupivacaine base in isopropyl alcohol, and then pass hydrogen chloride gas to filter the bupivacaine hydrochloride. Or after the reaction is finished in DMF, dilute hydrochloric acid is added directly, and then cooled and crystallized to get bupivacaine hydrochloride. The disadvantages of the preparation methods reported in the existing literature are large usage of DMF, difficult recovery, and high production cost.

Pharmacological action of Bupivacaine hydrochloride.

Bubicarsine hydrochloride is a long-acting local anesthetic of amides, its anesthetic time is 2 to 3 times longer than lidocaine hydrochloride, and its dispersion is similar to that of lidocaine hydrochloride. It has little effect on circulation and respiration, no irritation to tissues, and does not produce methemoglobinemia. Normal dosage has no effect on cardiovascular function, and large dosage can cause blood pressure to drop and heart rate to slow down. There was no apparent rapid tolerance.

Product Method of Bupivacaine hydrochloride.

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