Other

Sinew Pharma Inc.

National Defense Medical Center

Avalon Hepapoc Limited

Cheng-Huei Hsiong

Oliver Yoa-Pu Hu

Tung-Yuan Shih

Hsin-Tien Ho

Li-Heng Pao

Ping Yang

Benjamin Pei-Chung Kuo

Yoa-Pu Hu Oliver

Mei-Ting Wang

Compounds are of the structure of Formula (II) wherein: each X is —C(═O)—; Ris a C-Calkyl polyol; Ris a saccharide group of formula (G); G is a monosaccharide residue, where (i) at least one of the —OH groups in (G)is substituted by a halogen atom, and (ii) the saccharide group of formula (G)is linked to —O— through a —CHgroup; p is 1 or 2; and m is 1, 2, 3, 4, 5, 6, 7, 8, 9 or 10. The compounds are effective in treating hepatotoxicity and fatty liver diseases.

Substituted esters containing polyols and saccharides for treating hepatotoxicity and fatty liver diseases

The present invention relates to compounds effective in treating hepatotoxicity and fatty liver diseases and uses thereof. The present compound is represented by Formula (II), which has the formula: R&#x2014;O&#x2014;X&#x2014;(CH)&#x2014;X&#x2014;O&#x2014;R, wherein: each X is &#x2014;C(&#x2550;O)&#x2014;; Ris a C-Calkyl polyol: Ris a saccharide group of formula (G); G is a monosaccharide residue, where (i) at least one of the &#x2014;OH groups in (G)is substituted by a halogen atom, and (ii) the saccharide group of formula (G)is linked to &#x2014;O&#x2014; through a &#x2014;CHgroup; p is 1 or 2; and m is 1, 2, 3, 4, 5, 6, 7, 8, 9 or 10.

A galactose oral composition having galactose, an antioxidant and a buffer. The galactose oral composition contains 1%-80% by weight of galactose. The antioxidant is selected from Vitamin A, Vitamin C, Vitamin E, Ethylenediaminetetraacetic acid (EDTA), sodium bisulfite, flavonoids, polyphenols, Diethylenetriaminepentaacetic acid (DTPA), and NTA-Nitrilotriacetate acid (NTA). The buffer is selected from ascorbic acid buffer, citrate buffer, phosphate buffer, acetate buffer, carbonate buffer, and triethanolamine buffer. The galactose oral composition can be applied to detect individual galactose metabolic ability to assess liver function.

Galactose oral composition and use thereof

The present invention relates to compounds effective in treating hepatotoxicity and fatty liver diseases and uses thereof. The present compound is represented by Formula (II), which has the formula: R&#x2014;O&#x2014;X&#x2014;(CH)&#x2014;X&#x2014;O&#x2014;R, wherein: each X is &#x2014;C(&#x2550;O)&#x2014;; Ris a C-Calkyl polyol; Ris a saccharide group of formula (G); G is a monosaccharide residue, where (i) at least one of the &#x2014;OH groups in (G)is substituted by a halogen atom, and (ii) the saccharide group of formula (G)is linked to &#x2014;O&#x2014; through a CHgroup; p is 1 or 2; and m is 1, 2, 3, 4, 5, 6, 7, 8, 9 or 10.

A UGT2B inhibitor capable of increasing the bio-availability of a drug, is a compound in a free base or a pharmaceutically acceptable salt form that is selected from the group consisting of: capillarisin, isorhamnetin, &#x3b2;-naphthoflavone, &#x3b1;-naphthoflavone, hesperetin, terpineol, (+)-limonene, &#x3b2;-myrcene, swertiamarin, eriodictyol, cineole, apigenin, baicalin, ursolic acid, isovitexin, lauryl alcohol, puerarin, trans-cinnamaldehyde, 3-phenylpropyl acetate, isoliquritigenin, paeoniflorin, gallic acid, genistein, glycyrrhizin, protocatechuic acid, ethyl myristate, umbelliferone, PEG (Polyethylene glycol) 400, PEG 2000, PEG 4000, Tween 20, Tween 60, Tween 80, BRIJ&#xae; 58, BRIJ&#xae; 76, Pluronic&#xae; F68, Pluronic&#xae; F127, and a combination thereof. A UGT2B enhancer capable of enhancing a clearance rate of morphine-like analgesic agents, is a compound in a free base or a pharmaceutically acceptable salt form that is selected from the group consisting of: nordihydroguaiaretic acid, wogonin, trans-cinnamic acid, baicalein, quercetin, daidzein, oleanolic acid, homoorientin, hesperetin, narigin, neohesperidin, (+)-epicatechin, hesperidin, liquiritin, eriodictyol, formononetin, quercitrin, genkwanin, kaempferol, isoquercitrin, (+)-catechin, naringenin, daidzin, (&#x2212;)-epicatechin, luteolin-7-glucoside, ergosterol, rutin, luteolin, ethyl myristate, apigenin, 3-phenylpropyl acetate, umbelliferone, glycyrrhizin, protocatechuic acid, poncirin, isovitexin, 6-gingerol, cineole, genistein, trans-cinnamaldehyde, and a combination thereof.

Inhibitors and enhancers of uridine diphosphate-glucuronosyltransferase 2B (UGT2B)

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: &#x3b1;-naphthoflavone, &#x3b2;-naphthoflavone, apigenin, baicalein, &#x3b2;-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.

Cytochrome P450 3A inhibitors and enhancers

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.

Orally administered analgesic compositions containing nalbuphine

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.

Controlled-release pharmaceutical preparation containing nalbuphine and a process for preparing the same

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&deg; C. for at least 2 weeks.

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Taipei, Taiwan

Cheng-Huei Hsiong