39 results about "Chemotherapy-induced nausea and vomiting" patented technology

In various embodiments, the present invention provides pharmaceutical compositions comprising delta-9-tetrahydrocannabinol and methods of administering such compositions prior to the administration of chemotherapy to prevent or reduce the development of delayed chemotherapy-induced nausea and vomiting.

This invention is for an improved method for making enhanced ginger capsules and for using these capsules for treating nausea and emesis in cancer patients.

The present invention provides conformationally-defined macrocyclic compounds that bind to and / or are functional modulators of the motilin receptor including subtypes, isoforms and / or variants thereof. These macrocyclic compounds, at a minimum, possess adequate pharmacological properties to be useful as therapeutics for a range of disease indications. In particular, these compounds are useful for treatment and prevention of disorders characterized by hypermotilinemia and / or gastrointestinal hypermotility, including, but not limited to, diarrhea, cancer treatment-related diarrhea, cancer-induced diarrhea, chemotherapy-induced diarrhea, radiation enteritis, radiation-induced diarrhea, stress-induced diarrhea, chronic diarrhea, AIDS-related diarrhea, C. difficile associated diarrhea, traveller's diarrhea, diarrhea induced by graph versus host disease, other types of diarrhea, dyspepsia, irritable bowel syndrome, chemotherapy-induced nausea and vomiting (emesis) and post-operative nausea and vomiting and functional gastrointestinal disorders. In addition, the compounds possess utility for the treatment of diseases and disorders characterized by poor stomach or intestinal absorption, such as short bowel syndrome, celiac disease and cachexia. The compounds also have use for the treatment of inflammatory diseases and disorders of the gastrointestinal tract, such as inflammatory bowel disease, ulcerative colitis, Crohn's disease and pancreatitis. Accordingly, methods of treating such disorders and pharmaceutical compositions including compounds of the present invention are also provided.

Novel 5-HT3 receptor modulators are disclosed. These compounds are used in the treatment of various disorders, including chemotherapy-induced nausea and vomiting, post-operative nausea and vomiting, and irritable bowel syndrome. Methods of making these compounds are also described in the present invention.

The present invention relates to novel conformationally-defined macrocyclic compounds that bind to and / or are functional modulators of the motilin receptor including subtypes, isoforms and / or variants thereof. These macrocyclic compounds are useful as therapeutics for a range of gastrointestinal disorders, in particular those in which suppression or inhibition of the migrating motor complex (MMC) is effective or malfunction of gastric motility or increased motilin secretion is observed, such as hypermotilinemia, imitable bowel syndrome, dyspepsia, including gallbladder dyspepsia, diarrhea, cancer treatment-related diarrhea, cancer-induced diarrhea, chemotherapy-induced diarrhea, radiation enteritis, radiation-induced diarrhea, stress-induced diarrhea, chronic diarrhea, AIDS-related diarrhea, C. difficile associated diarrhea, traveller's diarrhea, acute infectious diarrhea, diarrhea induced by graph versus host disease, other types of diarrhea, functional gastrointestinal disorders, chemotherapy-induced nausea and vomiting (emesis), post-operative nausea and vomiting, cyclic vomiting syndrome and functional vomiting. Accordingly, methods of treating such disorders with such macrocyclic compounds and pharmaceutical compositions thereof are also provided in addition to methods of modulating the migrating motor complex.

The present invention relates compounds of Formula (A) as NK-1 receptor antagonists, as well as their preparation and uses, and further relates pharmaceutical compositions comprising these compounds and their uses as modulators of dysfunctional glutamate transmission. The present invention also relates to the uses of the compounds or pharmaceutical compositions in treating or preventing certain disorders and diseases which relate to NK-1 receptor in humans. More specifically, the compounds and / or pharmaceutical compositions of the present invention are believed to potentially offer therapeutic benefits to patients who suffer, among others, chemotherapy-induced nausea and vomit (CINV) and / or post-operative nausea and vomit (PONV).

The present invention is directed to nanostructured Aprepitant compositions, process for the preparation thereof and pharmaceutical compositions containing them. The nanoparticles of Aprepitant according to the invention have an average particle size of less than about 200 nm. The stable nanostructured particles of the invention are presented by increased solubility, dissolution rate, permeability and bioequivalent or enhanced biological performance characterized by significantly decreased fed / fasted effect compared to the reference and marketed drug. Aprepitant is a chemical compound that belongs to a class of drugs called substance P antagonists (SPA). It mediates its effect by acting on neurokinin 1 receptor. Aprepitant is manufactured by Merck & Co. under the brand name Emend for prevention of acute and delayed chemotherapy-induced nausea and vomiting (CINV) and for prevention of postoperative nausea and vomiting.

A liquid pharmaceutical compositions comprising Aprepitant is preferably prepared as an oral suspension dosage form for the prevention and control of acute and delayed chemotherapy induced nausea and vomiting, and / or for prevention of postoperative nausea and vomiting.

Compounds of formulae (I) and (II) are disclosed as 5-HT3inhibitors. Those compounds that exhibit central activity are useful in treating chemotherapy-induced nausea and vomiting (CINV); those that peripheral receptors are useful to treat diarrhea-predominant Irritable Bowel Syndrome (IBS-D).

The invention provides a fosaprepitant dimeglumine composition for injection, and relates to the technical field of medicine manufacturing. The main medicine of the composition comprises fosaprepitant dimeglumine and melatonin, wherein the melatonin comprises a quick release part and a cyclodextrin-included slow release part. According to the fosaprepitant dimeglumine composition for injection provided by the invention, the therapeutic effect of fosaprepitant dimeglumine is improved, instability caused by oral administration of MT (Melatonin) is avoided and MT is quick to distribute and eliminate and the like, and the first pass effect of MT is reduced. The dosage of fosaprepitant dimeglumine is reduced. The design of dosage combining quick release and slow release is in accordance with secretion characteristic of MT, so that the problem of half-life period of MT is solved and the bioavailability of the product is improved. The composition has the synergistic effect to treat CINV (Chemotherapy Induced Nausea And Vomiting) by fosaprepitant dimeglumine, and fosaprepitant dimeglumine and melatonin are combined to not only treat CINV so as to improve the therapeutic effect of fosaprepitant dimeglumine to CINV and shorten the course of treatment, but also reduce the use level of fosaprepitant dimeglumine, reduce the side effect of fosaprepitant dimeglumine and improve the immunity of a human body. The stress response of organism can be effectively reduced by maintaining melatonin in a certain concentration in blood of a human body to the benefit of treatment of CINV.

The invention relates to a NK1 receptor-targeting antagonist and application of the same to chemotherapy-induced nausea and vomiting, belonging to the technical field of adjuvant therapeutics for tumor chemotherapy. The invention provides a compound as shown in a formula I which is described in the specification, or a racemate, stereoisomer, tautomer, isotopic label, oxynitride or pharmaceutically-acceptable salt thereof. The invention also provides a preparation method for the compound, a pharmaceutical compositions and the application of the compound or the racemate, stereoisomer, tautomer,isotopic label, oxynitride or pharmaceutically-acceptable salt thereof.

The present disclosure provides for sustained release pharmaceutical formulations which can deliver both a 5-hydroxytryptamine 3 (5HT3) receptor antagonist and a neurokinin-1 (NK1) receptor antagonist to a subject in need thereof. Formulations described herein are suitable for subcutaneous administration. Also described are methods of treatment of various disorders, including chemotherapy-induced nausea and vomiting (CINV). The disclosed compositions and methods provide for less frequent dosing of the therapeutic agents, thereby increasing subject comfort and compliance.

The present invention is directed to nanostructured Aprepitant compositions, process for the preparation thereof and pharmaceutical compositions containing them. The nanoparticles of Aprepitant according to the invention have an average particle size of less than about 200 nm. The stable nanostructured particles of the invention are presented by increased solubility, dissolution rate, permeability and bioequivalent or enhanced biological performance characterized by significantly decreased fed / fasted effect compared to the reference and marketed drug. Aprepitant is a chemical compound that belongs to a class of drugs called substance P antagonists (SPA). It mediates its effect by acting on neurokinin 1 receptor. Aprepitant is manufactured by Merck & Co. under the brand name Emend for prevention of acute and delayed chemotherapy-induced nausea and vomiting (CINV) and for prevention of postoperative nausea and vomiting.

Novel 5-HT3 receptor modulators are disclosed. These compounds are used in the treatment of various disorders, including chemotherapy-induced nausea and vomiting, post-operative nausea and vomiting, and irritable bowel syndrome. Methods of making these compounds are also described in the present invention.

The invention provides an aprepitant composition for injection, and relates to the technical field of medicaments and preparation of the medicaments. The composition comprises main drugs of aprepitant and melatonin, wherein the melatonin comprises a quick release part and a slow-released part cladded by cyclodextrin. By adopting the aprepitant composition for injection provided by the invention, the treatment effect of the aprepitant is improved; the instability, distribution, fast removal and the like caused by oral absorption of MT (melatonin) are avoided; the first-pass effect of the MT is reduced; the dosage of the aprepitant is reduced; the administration design of combining quick release with slow release accords with the physiological secretion characteristics of the MT; the short half-life period of the MT is solved; the product bioavailability is improved; the composition has synergism on treatment of CINV (chemotherapy induced nausea and vomiting) by the aprepitant; not only can the CINV be treated after combining the MT with the aprepitant, but also the treatment effect of the aprepitant on the CINV is improved; the treatment course is shortened; the dosage of the aprepitant is also reduced; the side effect of the aprepitant is reduced; the human immunity can be improved; certain concentration of melatonin is maintained in blood of a human body, so that the stress reaction of the organism can be effectively reduced; treatment of the CINV is facilitated.

The invention provides a ramosetron composition for injection, and relates to the technical field of medicines and medicine manufacturing. Main medicines of the composition are ramosetron and melatonin. The melatonin comprises a quick release part and a slow release part contained in cyclodextrin. The ramosetron composition for injection provided by the invention has the functions of improving the treatment effect of ranitidine, avoiding instability, fast distribution and elimination and the like of MT (Melatonin) caused by oral absorption, reducing the first pass effect of MT and reducing the dosage of ramosetron. Delivery design combining quick release and slow release meets the physiological secretion characteristic of MT, solves the problem of short half life of MT and improves the bioavailability of the product. The composition has a synergistic effect on treatment of CINV (Chemotherapy Induced Nausea And Vomiting) by ramosetron, and after the melatonin is combined with ramosetron, not only is the CINV treated, is the treatment effect of the ramosetron on the CINV improved and is the course of treatment shortened, but also the use level of the ramosetron and the side effect of the ramosetron are reduced, and the immunity of human body is improved. The melatonin in a certain concentration in human blood has the capability of effectively reducing melatonin of human body to the benefit of treatment of the CINV.

The invention relates to a lucid ganoderma active component composition as well as a preparation method and application thereof and belongs to the technical fields of traditional Chinese medicines andhealth-care food. The lucid ganoderma active component composition is prepared from polysaccharide, glycopeptides, ganoderic acid A, ganoderic acid B and ganoderic acid C2 according to the weight ratio of (5 to 55):(1.5 to 15):(1 to 8):(0.6 to 6):(0.5 to 5). The preparation method of the lucid ganoderma active component composition comprises the following steps: adding ethanol of 30 to 95 percent, which is 5 to 30 times relative to total weight of the raw materials into raw materials containing lucid ganoderma powder and broken spore lucid ganoderma powder; carrying out reflux extraction for1 to 3 times, with 1 to 8 hours each time; filtering, and recovering ethanol to obtain an ethanol extract; adding water which is 5 to 30 times that the total weight of the raw materials into extracteddregs, and extracting for 1 to 3 times, with 1 to 5 hours each time; filtering, and properly concentrating to obtain an aqueous extract; combining the ethanol extract with the aqueous extract to obtain the lucid ganoderma active component, wherein the weight ratio of the lucid ganoderma to the broken spore lucid ganoderma powder is (6 to 12) to (1 to 6). The lucid ganoderma active component composition disclosed by the invention has the effects of inhibiting chemotherapy-induced nausea and vomiting.

Compositions comprised of olanzapine and a 5-HT3 receptor antagonist and a polyorthoester polymer are provided to provide extended release of the active agents. Also described are compositions comprising olanzapine and a polyorthoester. The compositions are effective for the prophylactic treatment or treatment of subjects at risk of or suffering from nausea and / or vomiting. The compositions are particularly useful for the prevention or treatment of acute, delayed, breakthrough or refractory chemotherapy induced nausea and vomiting (CINV). The CINV may result from, e.g., highly or moderately emetogenic cancer chemotherapy. The compositions are suitable for delivery via, e.g., intramuscular injection, intradermal injection, and subcutaneous injection.

Novel 5-HT3 receptor modulators are disclosed. These compounds are used in the treatment of various disorders, including chemotherapy-induced nausea and vomiting, post-operative nausea and vomiting, and irritable bowel syndrome. Methods of making these compounds are also described in the present invention.

The invention provides an andansetron composition for injection, relating to the technical field of drugs and drug preparation. The main drugs of the andansetron composition include andansetron and melatonin, wherein the melatonin comprises a quick-release part and a cyclodextrin encapsulated slow-release part. The andansetron composition for injection, provided by the invention, has the advantages that the treatment effect of the andansetron is improved, the instability of the MT (melatonin), caused by the oral absorption of the MT and the fast distribution and elimination of the MT are avoided, the first-pass effect of the MT is reduced, the dosage of the andansetron is reduced, the quick-release and slow-release combined drug administration design is in line with the physiological secretion characteristic of the MT, the problem of short half-life period of the MT is solved, the biological availability of the product is improved, the melatonin has a synergistic effect on the andansetron for CINV (Chemotherapy Induced Nausea And Vomiting) treatment, after the melatonin and the andansetron are combined, the CINV can be treated, the treatment effect of the andansetron on the CINV are improved, the treatment course is shortened, the usage and the side effect of the andansetron are reduced, and the immunity of human bodies can be improved; and a certain concentration of melatonin maintained in the blood of the human body can be used for effectively reducing the stress reaction of organisms and is facilitated to the treatment of the CINV.

The invention provides a granisetron composition for injection and relates to the technical field of medicaments and medicament manufacturing. The main medicaments of the composition are granisetron and melatonin, wherein the melatonin comprises a quick release part and a slow release part contained in cyclodextrin. The granisetron composition for injection provided by the invention can be used for improving the treatment effect of the granisetron, avoiding instability, quick distribution and elimination and the like of MT ((Metal Thionein) caused by oral absorption, reducing the first-pass effect of the MT and reducing the dosage of the granisetron. The medicament administration design combining the quick release with the slow release satisfies physiological secretion characteristics of the MT, can be used for solving the problem that the half-life period of the MT is short, increasing the biological utilization rate of the granisetron composition, and achieving the synergism of the granisetron for treating CINV (Chemotherapy Induced Nausea And Vomiting). The quick release part and the slow release part are combined, so that not only can the CINV be treated, but also the treatment effect of the granisetron on the CINV can be improved, and therefore, the treatment course is shortened, the dosage of the granisetron is reduced, the side effect of the granisetron is lowered, and the body immunity can be improved. A certain concentration of melatonin is kept in the blood of the human body, so that the stress response of the organisms can be effectively lowered for facilitating the treatment of the CINV.

Compositions comprised of olanzapine and a 5-HT3 receptor antagonist and a polyorthoester polymer are provided to provide extended release of the active agents. Also described are compositions comprising olanzapine and a polyorthoester. The compositions are effective for the prophylactic treatment or treatment of subjects at risk of or suffering from nausea and / or vomiting. The compositions are particularly useful for the prevention or treatment of acute, delayed, breakthrough or refractory chemotherapy induced nausea and vomiting (CINV). The CINV may result from, e.g., highly or moderately emetogenic cancer chemotherapy. The compositions are suitable for delivery via, e.g., intramuscular injection, intradermal injection, and subcutaneous injection.

Novel 5-HT3 receptor modulators are disclosed. These compounds are used in the treatment of various disorders, including chemotherapy-induced nausea and vomiting, post-operative nausea and vomiting, and irritable bowel syndrome. Methods of making these compounds are also described in the present invention.

The invention provides a tropisetron composition for injection and relates to the technical fields of medicines and medicine preparation. The tropisetron composition is characterized in that the main medicines are tropisetron and melatonin, wherein the melatonin comprises a quick release part and a slow release part included by cyclodextrin. According to the tropisetron composition provided by the invention, the treating effect of the tropisetron is improved; problems of instability and rapidness in distribution and clearing caused when MT (melatonin) is orally absorbed are avoided, and a first-pass effect of the MT is reduced; the use level of the tropisetron is lowered; a medicine administration design in which a quick release manner and a slow release manner are combined is accordant with physiological secretion characteristics of the MT, the problem of the MT that the half-life period is short is solved, and the biological availability of a product is improved; the treatment of the tropisetron to CINV (Chemotherapy Induced Nausea and Vomiting) is enhanced, after the tropisetron and the melatonin are combined, not only the CINV can be treated, the treatment effect of the tropisetron to the CINV can be improved, the treatment course can be shortened, but also the use level of the tropisetron is lowered, the side effect of the tropisetron is reduced, and the immune capability of a human body can be improved; by maintaining the melatonin with a certain concentration in the blood of the human body, a stress reaction of the body can be effectively reduced, and the treatment of the CINV is benefited.

The invention relates to tropisetron hydrochloride composition injection capable of treating nausea and vomiting caused by chemotherapy, belonging to the technical field of medicines. The composition injection is composed of tropisetron hydrochloride and calcium chloride, wherein tropisetron hydrochloride is crystal, and an X-ray powder diffraction diagram obtained by Cu-Kalpha ray measurement is shown as figure I. The novel crystal form of tropisetron hydrochloride provided by the invention is different from the crystal structure in the prior art, through experimental verification, the inventor surprisingly finds that the compound with the novel crystal form is high in purity, good in mobility, high in stability, low in impurity content, and safe and reliable in clinic application, the moisture absorption probability is small, and the injection prepared by adopting the compound with the novel crystal is simple in component and good in stability.

A method for treating chemotherapy-induced nausea and vomiting in individuals undergoing chemotherapy and previously treated with, and whom failed to respond to, a 5-HT3 antagonist other than granisetron is described. Individuals who fail to respond to, for example, palonosetron, as evidenced by an inadequate prevention or attenuation of acute or delayed chemotherapy-induced nausea and vomiting, are treated with a semi-solid drug delivery vehicle that provides a sustained release of granisetron.

The invention discloses a food capable of stopping vomiting. The food is made from the following raw materials in parts by weight: 5-20 parts of radix codonopsis, 5-20 parts of poria cocos, 5-20 partsof bamboo shavings, 5-20 parts of wrinkled gianthyssop herbs, 5-20 parts of ginger, 5-20 parts of oligomerization mannose and 5-25 parts of bighead atractylodes rhizomes. The food disclosed by the invention has the beneficial effects that side effects caused by serious vomiting produced due to CINV (chemotherapy-induced nausea and vomiting) during chemotherapy of cancer patients can be effectively reduced, the raw materials are compounded from medicinal and edible food materials and are scientific in measurement and reasonable in compatibility, and modernized production is utilized; and a modern biological extraction technique is used, formula materials are subjected to extraction to be made into a food which is easy to take, non-irritating to the stomach and convenient to carry, and thedisadvantages that a traditional Chinese medicine preparation is slow to take effect, long in decoction time, high in dosage, bitter in taste and not acceptable by modern people can be effectively overcome.

The present invention relates compounds of Formula (A) as NK-1 receptor antagonists, as well as their preparation and uses, and further relates pharmaceutical compositions comprising these compounds and their uses as modulators of dysfunctional glutamate transmission. The present invention also relates to the uses of the compounds or pharmaceutical compositions in treating or preventing certain disorders and diseases which relate to NK-1 receptor in humans. More specifically, the compounds and / or pharmaceutical compositions of the present invention are believed to potentially offer therapeutic benefits to patients who suffer, among others, chemotherapy-induced nausea and vomit (CINV) and / or post-operative nausea and vomit (PONV).