Buprenorphine is a potent analgesic agent, it has been shown to be as effective as morphine. The main clinical application of buprenorphine is to relief postoperative pains or for patients in the terminal phase of cancer. The chance of becoming addiction and abuse is low, therefore it is pretty safe for clinical use. The half life of buprenorphine is short, since its hepatic extraction (extraction ratio is 0.7 to 0.9) and metabolism are high. For these reasons, oral administration of buprenorphine becomes impractical due to the need of giving drug frequiently. The present invention is related to enhancers used in transdermal preparations of narcotic analgesic agents. This invention employs pure components of Chinese herbs in a fixed ratio as transdermal penetration enhancers. Compositions of these transdermal preparations usually include 0.1 to 50% of narcotic analgesic agent, 0.1 to 70% of pure components from Chinese herb as transdermal penetration enhancers, and other necessary excipients for transdermal delivery. Studies for the present invention in nude mice revealed that a transdermal preparation containing 10% of terpineol can delivery 15 mg of buprenorphine through 10 cm.sup.2 skin area in 48 hours, which satisfied the need of practical use.

National Science Council

Transdermal delivery of buprenorphine preparations

The present invention provides cytochrome P450 3A (CYP3A) inhibitors and enhancers. Examples of the CYP3A inhibitors include free bases or pharmacologically acceptable salts of at least one of the following compounds: .alpha.-naphthoflavone, .beta.-naphthoflavone, apigenin, baicalein, .beta.-myrcene, catechin, 3-phenylpropyl acetate, formononetin, gallic acid, hesperetin, hesperidin, isoquercitrin, lauryl alcohol, luteolin, luteolin-7-glycoside, narigin, nordihydroguaiaretic acid, quercitrin, swertiamarin, terpineol, and trans-cinnamaldehyde. Examples of the CYP3A enhancers include free bases or pharmacologically acceptable salts of at least one of the following compounds: apigenin, formononetin, and luteolin-7-glycoside. The CYP3A inhibitors can be used, alone or co-administered with a drug, to improve the drug bioavailability. The CYP3A inhibitors can also be used as chemopreventors to prevent biotransformation of procarcinogenic compounds into carcinogens via CYP3A activity or for treatment of intestinal or hepatic cancer by inhibit the CYP3A activity. The CYP3A enhancers can be used to improve the enzymatic activity of CYP3A so as to improve the biotransformation and degradation of active drugs or the sustrates of CYP3A from the body. The CYP3A inhibitors and enhancers of the present invention are natural substances extracted from herbs and non-toxic.

terpineol/zhubný nádor

Transdermal delivery of buprenorphine preparations

Cytochrome P450 3A inhibitors and enhancers

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