Bulleyaconitine A and lidocaine compounded sterile powder for injection

Abstract

The invention relates to bulleyaconitine A and lidocaine compounded sterile powder for injection, belonging to a medicinal preparation containing effective organic components, in particular to a medicinal preparation containing bulleyaconitine A. A lidocaine solution with a concentration of 80mM is added to a bulleyaconitine A solution with a concentration of 0.20-0.35mM to prepare the sterile powder suitable for preparing sterile solutions, wherein the volume of the lidocaine solution accounts for 0.5-1.5 percent of that of the bulleyaconitine A solution; and the sterile powder is subpackaged in ampoules or other appropriate containers in specifications of 2ml, 5ml or 10ml according to a standard of 0.2-0.5mg and prepared into injections by using sterile solutions before using. The invention provides the bulleyaconitine A and lidocaine compounded sterile powder for injection, which is used as a non-narcotic painkiller and can be expected to reduce adverse reactions of the bulleyaconitine A to the human body.

Description

technical field [0001] The invention belongs to the medicine preparation containing effective organic components, especially the medicine preparation containing aconitin. Background technique [0002] Bulleyaconitine is an aconitine alkaloid, a diterpenoid alkaloid with strong anesthetic activity in vivo. Even at a very low concentration, citrin can reduce the sodium ion current of neurons, and it may eliminate the release of ectopic high-frequency currents that damage nerves, and relieve pain for patients with neuropathic pain. The solution and tablet of orientin have been used clinically for the treatment of chronic pain and arthritis. However, its underlying pharmacological mechanism remains unclear. In rat experiments, the injection of a single preparation of oratin into rat sciatica not only blocked the sensory and motor functions of the sciatic nerve, but also induced hyperexcitability of the sciatic nerve, causing sedation, arrhythmia and respiratory distress. Thes...

AI Technical Summary

Problems solved by technology

These effects or side effects are due to, on the one hand, when approaching the resting membrane potential, ruconidin causes the emergence of a sodium ion threshold current, irreversibly blocking the Na ion current, while the high affinity reversal of the open state sodium ion channel is relatively slow ; On the other hand, aconitin is highly fat-soluble and easily diffuses into the nerve sheath. These effects tend to block the function of rat sciatic nerve