摘要:
The present invention provides compositions for the treatment of cancer. The compositions include liposomes containing a phosphatidylcholine lipid, a sterol, a PEG-lipid, and elinafide, wherein less than 20% of the elinafide is released in vitro from the liposome within 40 hours. The present invention also provides liposomal compositions for the treatment of cancer comprising administering to a patient in need thereof a liposome, wherein the liposome comprises: a phosphatidylcholine lipid; a sterol; a PEG-lipid; and elinafide, wherein the administration of the liposomal composition has a reduced occurrence of side effects, such as for example, muscle myopathy in the patient.
摘要:
The present invention provides a composition for the treatment of cancer including zwitterionic liposomes consisting essentially of: 50-65 mol % of a phosphatidylcholine lipid, 30-45 mol % of cholesterol, and 2-8 mol % of a PEG-lipid; and cisplatin. Cisplatin is encapsulated in the liposomes in an amount such that the ratio of the total lipid weight to the cisplatin weight is from about 65:1 to about 95:1. Methods for the preparation of liposomal cisplatin and the treatment of cancer are also disclosed.
摘要:
The present invention provides methods for delivery of therapeutic agents to a subject using multi-component liposomal systems. The methods include administration of a therapeutic liposome containing an active agent, followed by a administration of an attacking liposome that induces release of the agents from the therapeutic liposome.
摘要:
The present disclosure provides pharmaceutical compositions and processes for making solid dosage form pharmaceutical compositions that provide immediate release of active ingredients and have abuse deterrent properties. The pharmaceutical compositions provided herein comprise at least one pharmaceutically active ingredient, at least one low molecular weight hydrophilic polymer, at least one high molecular weight hydrophilic polymer, and an effervescent system.
摘要:
The present disclosure relates generally to a process for the synthesis of 1,4,7,10-tetraazacyclododecane ligands, chelates, and derivatives thereof. In particular, the present disclosure is directed to a process for the synthesis of 1,4,7,10-tetraaza-1,4,7,10-tetrakis(carboxymethyl)cyclododecane (DOTA) ligands, corresponding DOTA-metal chelates, and various derivatives thereof.
摘要:
A pharmaceutical composition comprising at least one active pharmaceutical ingredient (API) or a pharmaceutically acceptable salt thereof, a glucomannan, a first polyalkylene oxide having an average molecular weight of no more than 300,000, and a second polyalkylene oxide having an average molecular weight of at least 1,000,000 and methods of making. The pharmaceutical composition provides extended release of the API and has abuse deterrent features.
摘要:
The present disclosure provides extended release pharmaceutical compositions comprising oxycodone and acetaminophen that produce a quick initial onset of analgesia, yet, maintain analgesia for about 12 hours after administration of the composition to a subject in need thereof. The pharmaceutical compositions disclosed herein also reduce the levels of acetaminophen in a subject's blood near the end of the dosing interval because the acetaminophen released by the pharmaceutical composition is being eliminated by a subject's body faster than it is being absorbed.
摘要:
The present invention provides (+)-morphinans comprising Toll-like receptor 9 (TLR9) antagonist activity, as well as methods for using the (+)-morphinans to treat pain. Also provided are pharmaceutical combination compositions comprising a (+)-morphinan and an opioid agonist/monoamine reuptake inhibitor, as well as methods for using the combination compositions to treat pain.
摘要:
Processes for preparing 3-substituted phenylalkylamines comprising reacting a phenyl boronic compound with an α-β unsaturated carbonyl-containing compound via an asymmetric 1,4-addition reaction, followed by reductive alkylation. The processes may be useful in the synthesis of tapentadol.
摘要:
The present invention provides processes for the synthesis of substituted berbine compounds. Also provided are intermediates used in the synthesis of substituted berbine compounds.