Abstract: The present invention provides dermal cytochrome P450 1A (CYP1A) inhibitors, which include free base or pharmacologically acceptable salt of (−)-epicatechin, (+)-epicatechin, (+)-limonene, 3-phenylpropyl acetate, &agr;-naphthoflavone, apigenin, baicalein, baicalin, &bgr;-myrcene, catechin, &bgr;-naphthoflavone, cineole, daidzein, daidzin, diosmin, ergosterol, formononetin, gallic acid, genistein, glycyrrhizin, glycyrrhizic acid, hesperetin, hesperidin, isoquercitrin, kaempferol, lauryl alcohol, luteolin, luteolin-7-glycoside, narigenin, narigin, nordihydroguaiaretic acid, oleanolic acid, paeoniflorin, quercetin, quercitrin, rutin, swertiamarin, terpineol, trans-cinnamaldehyde, trans-cinnamic acid, umbelliferone, genkwanin, homoorientin, isovitexin, neohesperidin, wongonin, capillarisin, liquiritin, ethyl myristate, poncirin, and ursolic acid.

Abstract: 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: &agr;-naphthoflavone, &bgr;-naphthoflavone, apigenin, baicalein, &bgr;-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.

Abstract: A controlled-release pharmaceutical preparation containing an oil suspension which comprises an analgesic and an injectable oil. The analgesic is either a nalbuphine free base or a pharmaceutical salt of nalbuphine such as nalbuphine HCl. The injectable oil is preferably sesame oil. The oil suspension contains microparticles in the size range of 1 to 100 &mgr;m, preferably less than 50 &mgr;m, which is produced by treating the analgesic and injectable oil in an ultra high energy mixing equipment. The controlled-release preparation permits nalbuphine free base or nalbuphine HCl to have a longer duration of action in relieving pain, and allows the administration of lower doses. A process for preparing the injectable oil suspension is also disclosed.

Abstract: The present invention provides orally administered pharmaceutical compositions which contains an effective amount of free base or pharmaceutcially acceptable salts of nalbuphine and/or nalbuphine ester, an oily substance, and a solubility-assisting agent. The oily substance is preferably sesame oil. The solubility-assisting agent is preferably benzyl benzoate. The pharmaceutical composition is useful as an analgesic. The compositions achieves a much higher bioavailability rate and yields much longer lasting effects on nalbuphine than other nalbuphine products currently in the market.

Abstract: The present invention provides stable galactose injection solutions, which contain 1 to 50% by weight of galactose, 0.01 to 1 M of a buffer solution, and 0.01 to 5% of an antioxidant. The preferred buffer solution is citrate buffer. The preferred anti-oxidant is sodium bisulfite. The galactose injection solution of the present invention has a pH between 4.0 and 9.0 and is stable at 80° C. for at least 2 weeks.