366results about How to "Improve therapeutic index" patented technology

The present invention encompasses a combination of at least one conjugate and one or more chemotherapeutic agent(s) which when administered exerts an unexpectedly enhanced therapeutic effect. The therapeutic effectiveness of the combination is greater than that of the conjugate alone or the administration of one or more of the drug(s) without the conjugate. The present invention is also directed to compositions comprising at least one conjugate and at one or more of chemotherapeutic agent and to methods of treating cancer using at least one conjugate and at least one or more of chemotherapeutic agent (s). The present invention also provides methods of modulating the growth of selected cell populations, such as cancer cells, by administering a therapeutically effective amount of one or more chemotherapeutic agent(s) and at least one conjugate. In each case, such combination has therapeutic synergy or improves the therapeutic index in the treatment of cancer over the anticancer agent(s) alone.

The invention is directed to biocompatible conjugated polymer nanoparticles including a copolymer backbone, a plurality of sidechains covalently linked to said backbone, and a plurality of platinum compounds dissociably linked to said backbone. The invention is also directed to dicarbonyl-lipid compounds wherein a platinum compound is dissociably linked to the dicarbonyl compound. The invention is also directed to methods of treating cancer or metastasis. The methods includes selecting a subject in need of treatment for cancer or metastasis and administering to the subject an effective amount of any of the nanoparticles, compounds, or compositions of the invention.

The present invention relates to novel estrogen-related steroidal quinols and their use as drugs for estrogen replacement therapy. The quinols of the present invention provide improved physicochemical properties, increased bioavailability, and improved distribution into tissues, bone, in the cardiovascular system, and in the CNS (central nervous system) with only a slight estrogenic action or no estrogenic action in the uterus. The compounds are suitable for the production of pharmaceutical agents for use in numerous indications (for example, estrogen replacement therapy, prevention and treatment of osteoporosis).

A method of treating a patient undergoing pharmacotherapy with a selected drug for treatment of a medical disorder is provided which comprises: (a) administering the selected drug to said patient at a first time point, to treat the medical disorder; and (b) applying an electrical signal to a vagus nerve of the patient at a second time point, wherein the signal is selected so as to modulate at least one pharmacologic and / or pharmacokinetic property of the selected drug in the body of the patient. The vagus nerve stimulation (VNS) modulated drug therapy may be performed secondarily to, and in conjunction with, application of a primary VNS therapy to the patient for treatment of the same or a different medical disorder, to enhance treatment of the patient.

Certain substituted urea derivatives selectively modulate the cardiac sarcomere, for example by potentiating cardiac myosin, and are useful in the treatment of systolic heart failure including congestive heart failure.

Pharmaceutical preparations, compositions, systems, and devices including medical devices and diagnostic or therapeutic agents, and methods to treat disease by modification of local tissue environment to modulate the therapeutic index of locally or systemically delivered therapeutic or diagnostic agents. Improved ability to reduce sympathetic nerve activity in the adventitia and perivascular tissues around arteries and veins in the body. Modulation of the local tissue environment around an artery to enable more effective denervation with or without a therapeutic agent. Modulation may include adjustment of the pH of the tissue.

The invention relates to a neo-gambogic acid SLN (solid lipid nanoparticle) and a preparation method thereof. The neo-gambogic acid SLN comprises a therapeutically effective amount of neo-gambogic acid, medicinal phosphatide, a surfactant and a lipid material. In the invention, the neo-gambogic acid is prepared into SLNs (solid lipid nanoparticles), thereby improving the solubility of the neo-gambogic acid, reducing the irritability, improving the bioavailability, and prolonging the action time of medicaments in a human body, in addition, the neo-gambogic acid SLNs can be gathered partially in the human body so as to play the targeted action of the SLNs and exert the anti-cancer therapeutic action of the SLNs better.

New methods of treating schizophrenia and schizoaffective disorder by administration of pharmaceutical compositions comprising an antipsychotic compound and a VMAT2 inhibitor to a subject in need thereof are provided.

A composition for facilitating delivery of biological agents, comprising a therapeutic or diagnostic agent and a supramolecular complex, the latter comprising (i) a block copolymer, having at least one nonionic, water soluble segment and at least one polyionic segment, and (ii) at least one charged surfactant having hydrophobic groups. The charge of the surfactant is opposite to the charge of the polyionic segment of the block copolymer. The constituents of the supramolecular complex are bound by interaction between the opposite charges thereof and between surfactant hydrophobic groups. The therapeutic or diagnostic agent may be an ionic substance, in which case the ionic substance has a net charge opposite to that of the block copolymer, the net charge being no more than 10.

The invention relates to a preparation method and application of 9-bit substituent double-functional group berberine derivatives. In-vitro biological activity assay research shows that the 9-bit substituent double-functional group berberine derivatives provided by the invention has acetylcholinesterase inhibition activity higher than that of berberine serving as a leading compound, and also has higher inhibition activity on butyrylcholine esterase. After being further optimized and screened, the derivatives have favorable foreground of being developed into medicaments for treating diseases such as AD disease, vascular dementia, cognitive dysfunction and the like. The general formula of the derivatives is shown as the following formula, wherein X, Y and Z are defined in specifications.

The invention relates to nanoliposome human papillomavirus (HPV) resistant and gynecological inflammation pathogen resistant specific complex IgY and a combined preparation for the same. Laying poultry is preferred to respectively prepare laying poultry for immunity of tumor somatic cells, viral protein complex antigens, gene recombination protein antigens and bacterial virus complex antigens; and human papillomavirus resistant special IgY and gynecological inflammation pathogen resistant specific IgY undergo affinity chromatography and purification and are converted into nanoliposomes, and then the nanoliposome special complex IgY is prepared. The nanoliposome human papillomavirus (HPV) resistant and gynecological inflammation pathogen resistant specific complex IgY and the combined preparation for the same have the advantages that: the nanoliposome technology is applied to increase the infiltration capacity and the prolongation effect and improve the curative effect. The nanoliposome human papillomavirus (HPV) resistant and gynecological inflammation pathogen resistant specific complex IgY and the combined preparation for the same can be prepared into various vaginal spraying agents, other spraying agents, lotion, gel, capsules, suppository, vaginal membranes, tablets, effervescent tablets, ointment, cream and so on. The nanoliposome complex IgY can infiltrate into a vagina mucosa to effectively remove HPV viruses and gynecological inflammation pathogens which are absorbed on the vaginal surface layer and in the vagina mucosa, is absorbed through the vagina mucosa and enters into the body to give play to the functions of prevention and treatment, and also can effectively prevent recrudescence.

This disclosure relates to methods for improving the therapeutic index of a chemotherapeutic drug in the treatment of patients afflicted with cancer, by reducing chemotherapy-related toxicity to a level that allows the chemotherapeutic drug to be used in humans.

The invention discloses hydrochloric acid Fasudil liposome injection and new application thereof. The injection mainly comprises the following components according to parts by weight: 1 part of hydrochloric acid Fasudil, 2 to 20 parts of phospholipid, 0.5 to 10 parts of cholesterol and 1 to 8 parts of polysorbate 80. Simultaneously, the hydrochloric acid Fasudil liposome injection also can be used for treating vertebral artery type cervical spondylosis.

The present invention relates to methods and compositions for anti-aging therapy and for the treatment and prophylaxis of age-related diseases and disorders in a human subject in need of such therapy or treatment, the methods comprising the pulmonary administration to the subject, preferably via inhalation, of composition comprising rapamycin, or a prodrug or derivative thereof.

The invention provides a curcumenol solid lipid nanoparticle and its preparation method, which comprises curcumenol 1 part, phospholipids 3-10 parts, grease material 5-100 parts, surface active agent 10-200 parts and excipient 10-400 parts.

A peptide which selectively inhibits αvβ3 integrin which comprises the deamidation product of a peptide comprising the NGR motif.

The invention discloses a liposome solid preparation of a losartan potassium hydrochlorothiazide pharmaceutical composition and a preparation method thereof. In the invention, active components of losartan potassium and hydrochlorothiazide and specific combined hydrogenated yolk lecithin, cholesterol and poloxamer 188 are prepared into a liposome which is then mixed with other pharmaceutical accessories to prepare the solid preparation, thereby greatly improving the pharmaceutical stability and bioavailability and having stable and lasting effect, small side effect and obvious curative effect.

The invention discloses 6-cyclohexyl methyl substituted S-DABO type compound, the synthesis method and the application, belonging to the medical technical field. The invention relates to a 5-alkyl-6-cyclohexyl methyl-2-(alkyl, naphthenic base, naphthenic base methyl, substituted phenylethanone) thiouracil type compound, which has general formula as shown in (I): wherein, R1 is alkyl of C1-3; alkyl, naphthenic base and naphthenic base methyl of R2=C1-8 are as shown in (II); wherein, X=OCH3, H, OH, halogen. Chloromethyl cyclohexane or cyclohexyl acetic acid is respectively used as raw material to prepare Beta- keto ester which is made into a key intermediate 5-alkyl-6-cyclohexyl methyl thiouracil together with thiourea through close loop condensation under the catalyzing of sodium alkoxide; target molecule is prepared through S-alkylation guiding C2-side chain. The invention has the advantages of simple and easy synthesis method, obvious anti-HIV virus activity and anti-resistance for the drugs and ability to be used as an alternative for anti-HIV drug.

This invention provides substituted benzimidazole compounds shown in common formula (I) and their pharmacologically permitted salts. The definitions of R1, R2, R3, R4 and n in common formula (I) are mentioned in the instruction. Pharmacological experiments show that, this kind of compounds and their pharmacologically permitted salts or their solvates or hydrates perform excellent anti-hepatitis B virus (anti-HBV) activities and are especially inhibitory to DNA replication of HBV. They are thus promising as anti-HBV drugs. This invention also provides a method to prepare this kind of compounds.

The present invention is (-)-meptazinol carbamate derivative as shown and / or its salt and their preparation process and use in preparing medicine for treating dementia including Alzheimer disease. The said compound, extracorporeal experiment shows, has very high AChE and BChE inhibiting activity, hundreds times higher than that of available medicine.

The invention discloses the application of koumine to the preparation of medicines for treating chronic pains and belongs to the application of gelsemium alkaloid monomer. The analgesic experiments of the koumine on chronic pains of animals prove that the koumine has potent dose-dependent analgesic effect, the analgesic potency is superior to that of the classical antipyretic-analgesic and anti-inflammatory drugs which are aspirin and indomethacin, the therapeutic index of the koumine is much higher than that of the total alkaloids of gelsemium, the koumine possibly has no tolerance, no addiction and little side effect, which indicates that the koumine has potent and low-toxicity analgesic effect, the mechanism of action of the koumine is possibly different from those of clinically common opium analgesics or aspirin analgesics, the koumine and the pharmaceutically acceptable salt thereof have the application of preparing of the medicines for treating chronic pains and have no serious disadvantages of the clinically common analgesics and can be developed into a novel analgesic which has potent analgesic effect in treating chronic pains such as inflammatory pain, neuropathic pain, cancer pain and the like, has no tolerance and addiction and little side effect, thus the koumine has bright industrialization prospect.

The invention relates to a clindamycin phosphate lipidosome freeze-dried preparation and a preparation method thereof. The clindamycin phosphate lipidosome freeze-dried preparation is characterized by comprising the following components in portion by weight: 15 to 25 portions of clindamycin phosphate, 10 to 40 portions of dimyristyl acid lecithin, 1 to 10 portions of cholesterol, 1 to 5 portions of antioxidant, and 5 to 25 portions of cryoprotectant.

The invention relates to an edaravone lipid microsphere formulation and a preparation method thereof. The edaravone lipid microsphere formulation is prepared by taking the mixed emulsifier of granulesten and poloxamer188 with specific rate as an emulsifier and injection soybean oil as oil phase solvent, and also contains pharmaceutically regular antioxidant. Not only does the prepared edaravone lipid microsphere injection have simple process, low cost and easy industrial production, but also obviously improved stability compared with the existing edaravone injection.

Provided are novel antibody drug conjugates (ADCs), and methods of using such ADCs to treat proliferative disorders.

The invention provides a Prasugrel liposome solid preparation, which is characterized by being prepared by the following main components in parts by weight: 1 part of Prasugrel, 2-18 parts of yolk phosphatidylglycerol, 0.6-9 parts of cholesterol, 1.2-12 parts of sodium glycyl-cholate and 4-80 parts of other pharmaceutically accepted excipients. The Prasugrel liposome prepared by the invention has high entrapment rate and little side effect, improves stability of aqueous solubility thereof greatly and is favor of dissolving medicinal preparation out.

The invention provides liposome injection of an amoxicillin sodium sulbactam sodium medicinal composition. The liposome injection consists of amoxicillin sodium, sulbactam sodium, liposome carriers, freeze-drying supporting agents and optional antioxidant, wherein the liposome carriers are dipalmitoyl phosphatidyl choline and deoxysodium cholate. The liposome injection has high stability; in the freeze-drying process, a phenomenon of breaking liposome caused by dehydration, fusion, ice crystal generation and the like does not occur; and the liposome can remain good encapsulation ratio after being hydrated and redissolved.

The invention discloses levocarnitine liposomes injection, which is characterized by comprising the following active ingredients in parts by weight: 1 part of levocarnitine, 3-15 parts of soybean lecithin, 0.4-7.5 parts of cholesterol and 0.02-1 part of antioxidant, and a pharmaceutically acceptable carrier, wherein, the antioxidant is one or more of L-cysteine, thiourea, vitamin E and butylated hydroxyanisole and is most preferably the vitamin E. The invention also discloses a preferable preparation method of the levocarnitine liposomes injection, namely ammonium sulphate pH gradient method.The invention provides levocarnitine liposomes injection which has excellent stability, high entrapment rate and low leakage rate in the process of long-term storage. The acute toxicity tests, unusualtoxicity tests and heat source tests adopting the levocarnitine liposomes injection all conform to the specifications and are applicable to industrialized production.