Other

Sinew Pharma Inc.

National Defense Education and Research Foundation

Avalon Hepapoc Limited

Oliver Yoa-Pu Hu

Cheng-Huei Hsiong

Tung-Yuan Shih

Hsin-Tien Ho

Li-Heng Pao

Ping Yang

Benjamin Pei-Chung Kuo

Fangchen Lee

Shung-Tai Ho

Yung-En Wu

Chieh Fu Chen

Hsi-Hui Tang

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

A new compound composition that is free of a side effect to a liver and used for alleviating the toxicity of an acetaminophen (APAP) medicament to the liver. The compound composition comprises (a) a pharmaceutically effective amount of acetaminophen and (b) a frequently-used safe and pharmaceutically acceptable excipient that can be combined with one or more than two medicaments that can reduce the toxicity of a drug via liver enzyme CYP2E1 metabolism to the liver. The compound is selected from the following group: Tween 20, microcrystalline cellulose, dicalcium phosphate, polyoxyethylene 23 lauryl ether, saccharin, mannitol, polyoxyethylene alkyl ether, sucralose, pyrrolidone, sodium starch glycolate, acrylic resin S100, carboxymethyl cellulose sodium, polyoxyethylene polyoxypropylene, menthol, low-substituted hydrocarbon propyl cellulose, pregelatinized starch, Dextrates NF hydrated, citric acid, polyoxyethylene castor oil, colloidal silica, polyethylene glycol monostearate aliphatic ester, sorbic acid, lemon oil, hydroxypropyl cellulose, sorbitol, acesulfame potassium, hypromellose phthalate, lactose monohydrate, maltodextrin, Brij 58, Brij 76, Tween 80, Tween 40, PEG 400, PEG 4000, PEG 2000, and the like, so as to reduce the side effect of the toxicity caused by acetaminophen to the liver.

Hepatotoxicity-free pharmaceutical composition containing acetaminophen drugs

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 methods and compositions for preventing or treating fatty liver, protecting liver function or ameliorating liver diseases caused by fatty liver or other associated disorders.

Methods and compositions for preventing or treating fatty liver, protecting liver function or ameliorating liver diseases caused by fatty liver or other associated disorders

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.

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.

Stable galactose injection solutions

The nalbuphine polyester derivative is related to a novel long acting agent. The nalbuphine polyester derivative is R&mdash;&lsqb;CO-NAL&rsqb;,wherein n is an integer from 2-4 and, in which the R is selected from a saturated or nonsaturated, substituted or unsubstituted, aliphatic or aromatic group having 1 to 40 carbon atoms. The process for producing the derivative includes esterifying nalbuphine with a saturated or unsaturated fatty acid or a halogen compound of the fatty acid with an acid anhydride. A pharmaceutical composition contains the derivative and a pharmaceutically acceptable carrier, which can be administered to an animal or person for treating pain.

Long analgesic acting nalbuphine polyester derivative and method of use

The present invention is related to a trandermal preparation of oxicams. In preparation, it is comprised of 0.1% to 50% of an oxicam, 0.1% to 70% of pure compositions from Chinese herbal enhancers as enhancers, as well as other necessary excipients for transdermal delivery of an active ingredient. This transdermal preparation is intended to be used for anti-inflammatory cases, but with few gastrointestinal side effects. Based on results from testing this preparation on nude mice skin, rabbit skin, and human leg skin, it was found that skin penetration of the transdermal preparation containing 20% terpineol oil was 157.6 times higher than that of the control group.

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Taipei, Taiwan

Oliver Yoa-Pu Hu