XEL 002BP – Bulleyaconitine A Transdermal Matrix Patch

What is Bulleyaconitine A?

Bulleyaconitine A, one of diterpenoid Aconitum alkaloids isolated from Aconitum Longtounense T. Ming, was used in Chinese Herbal Medicine for years to relieve various pains. Compared to other conventional analgesics, the advantages of Bulleyaconitine A are excellent long-lasting analgesic effect, non opioid dependence after a long-term administration, less side effects and low toxicity. Its action on inflammation is an added benefit and superior to other analgesics.

Bulleyaconitine A has been approved by Chinese FDA since 1980's as a prescription medication for the treatment of late-stage cancer pain, rheumatism and other kinds of rheumatic arthritis, bursitis, osteoarthritis, arthralgia, joint sprains, the sciatica, the muscle fiber inflammation and the costal cartilage inflammation. Due to their physical and dose dependence and side effects of opioid analgesics, the cancer patients have a high demand on the non opioid dependence medication. Therefore, Bulleyaconitine A is now recommended by the Ministry of Public Health, China as analgesic for late-stage cancer pain.

The dosage forms available in China include subcutaneous injections, tablets and capsules.

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What is the Mechanism of Action?

The C19 diterpenoid alkaloid aconitine such as Bulleyaconitine A and their derivatives have been proven to be antinociceptive. It is known that alkaloid aconitine bind to site II of Na+ channel. The mode of action were investigated with the respect to their affinity for voltage-dependent Na+ channels, the action on synaptosomal Na+ and Ca+ homoeostasis and their antinociceptive, arrhythmogenic properties. The results show that Bulleyaconitine A strongly reduces neuronal Na+ currents at +50 mV in a use-dependent manner, and elicits long-lasting sensory and motor block of rat sciatic nerve functions after a single injection.

The analgesic effect of Bulleyaconitine A might be related to 5-HT level in the brain, and no physical dependence has been observed. Its relative analgesic effect is 65 and 7000 times as potent as morphine and aspirin, respectively.

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What are the Benefits?

  • Treatment of late-stage cancer pain
  • Treatment of rheumatism and other kinds of rheumatic arthritis, bursitis, osteoarthritis, arthralgia, joint sprains, and sciatica
  • Treatment of the muscle fiber inflammation and the costal cartilage inflammation
  • Treatment of belt-shaped blister measles

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Why is Transdermal Patch Better?

Transdermal drug delivery offers many advantages over tablets and other solid dosage forms, including reliable blood levels, improved drug absorption, minimized side effects, less frequent doses, and better patient compliance.

Our twice-a-week Bulleyaconitine A transdermal patch can provide a better therapy over the current oral dosage forms and minimize the side effect.

The pre-clinical study for the product development of Bulleyaconitine A transdermal patch shows that the prototype patch is feasible for the further product development. A15 cm2 patch can deliver 200 μg of Bulleyaconitine A per day for up to 4 days.

Daily Delivery of Bulleyaconitine A from 15 cm2 Transdermal Patches cross Human Cadaver Skin (twice-a-week applications)

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