55 results about "Nalbuphine" patented technology

Methods and compositions for treating, managing or ameliorating pain in a subject (preferably, a mammal, and more preferably, a human) comprising administration of a centrally acting (i.e., crosses the blood brain barrier) agonist of a kappa-opioid receptor and a centrally acting opioid antagonist such that the analgesia achieved by this administration is greater than with administration of either the kappa-opioid receptor agonist or the opioid antagonist alone. Preferably the kappa-opioid receptor is nalbuphine or a salt or prodrug of nalbuphine and the opioid antagonist is naloxone or a salt or prodrug of naloxone. Preferred methods of administration include mucosal (e.g. intranasal or pulmonary) and intravenous. Other kappa-opioid receptors include pentazocine and butorphanol.

A composition comprising the tannate of an opioid. Suitable opioids include alfentanil, buprenorphine, butorphanol, carfentanil, cocaine, codeine, dezocine, diacetylmorphine, dihydrocodeine, dihydromorphine, diphenoxylate, diprenorphine, etorphine, fentanyl, heroin, hydrocodone, hydromorphone, beta-hydroxy-3-methylfentanyl, levo-alpha-acetylmethadol, levorphanol, lofentanil, meperidine, methadone, morphine, nalbuphine, nalmefene, o-methylnaltrexone, naloxone, naltrexone, oxycodone, oxymorphone, pentazocine, pethidine, propoxyphene, remifentanil, sufentanil, tilidine and tramadol. The opioid tannate may be readily prepared by reacting an opioid free base with tannic acid, either neat or in the presence of up to about 30 wt. % water, at a temperature of about 60 to about 150° C. and thereafter recovering the resultant opioid tannate. The opioid tannate may also be prepared by an alternative process that involves reacting the opioid free base with water at a temperature such that not more than about 10 wt. % of the opioid tannate will be decomposed and thereafter removing the water by freeze-drying.

Sustained release formulations of nalbuphine or pharmaceutically acceptable salts thereof; methods for making the sustained release formulations of nalbuphine or pharmaceutically acceptable salts thereof; and methods for using the sustained release formulations of nalbuphine or pharmaceutically acceptable salts thereof to treat patients suffering from pain are provided.

Sustained release formulations of nalbuphine or pharmaceutically acceptable salts thereof; methods for making the sustained release formulations of nalbuphine or pharmaceutically acceptable salts thereof; and methods for using the sustained release formulations of nalbuphine or pharmaceutically acceptable salts thereof to treat patients suffering from pain are provided.

The present invention is aimed at providing an opioid antagonist compound and preparation method thereof, and its medical use. The medical use for opioid antagonists such as the compound of formula (I) (shown below) include complete or partial reversal of narcotic depression, including respiratory depression, induced by opioids including natural and synthetic narcotics, such as heroin, fentanyl, oxycodone, hydrocodone, morphine, propoxyphene, methadone and certain narcotic-antagonist analgesics, such as nalbuphine, pentazocine and butorphanol. An opioid antagonist may also be useful as an adjunctive agent to increase blood pressure in the management of septic shock. Further, opioid antagonists also have been shown to reduce the craving for alcohol.

Sustained release formulations of nalbuphine or pharmaceutically acceptable salts thereof; methods for making the sustained release formulations of nalbuphine or pharmaceutically acceptable salts thereof; and methods for using the sustained release formulations of nalbuphine or pharmaceutically acceptable salts thereof to treat patients suffering from pain are provided.

An immediate-release oral pharmaceutical formulation comprising nalbuphine, or a pharmaceutically acceptable salt thereof, and at least one hydrophilic granulation substrate, one hydrophilic binder and one lubricant.

The present invention relates to methods for treating patients with chronic cough with nalbuphine compositions as well as treating cough, breathlessness, or dyspnea associated with IPF with nalbuphine compositions, wherein the method provides a therapeutic effect in a patient.

The invention discloses a preparation method of nalbuphine free alkali, i.e., (-)-17-(cyclobutylmethyl)-4,5alpha-epoxymorphine-3,6alpha,14-hydroxyl. A synthetic route of the preparation method is shown in the specification. According to the novel method, a new reduction reaction condition is adopted, so the purity of nalbuphine free alkali in a reduction product reaches 99%, and the problems of excessive generation of 6-beta isomers of the reduction product and difficulty in purification of the free alkali are avoided.

The invention discloses compound anesthetic for minks and a preparation method and application of the compound anesthetic and belongs to the fields of preparation and application of the compound anesthetic for minks. The compound anesthetic for minks comprises detomidine, lorazepam and nalbuphine. The preparation method incudes: (1) mixing the detomidine, lorazepam and nalbuphine; (2) adding water of injection with uniform mixing to obtain the compound anesthetic. The compound anesthetic is quick in anesthesia induction on minks, long in anesthesia duration, good in analgesia, sedation and muscle relaxation effects, smooth and steady in analepsia and simple to operate, has slight impact on all clinical conventional indexes and special indexes, almost has no side effect and can be used in operations such as long-distance mink transportation, electro-ejaculation, cesarean section, trauma and fracture needing chemical restraints or sedation.

The present invention relates to methods for treating patients with chronic cough with nalbuphine compositions as well as treating cough, breathlessness, or dyspnea associated with IPF with nalbuphine compositions, wherein the method provides a therapeutic effect in a patient.

The invention purposes of a medical composition in preparation of medical compositions used for treating skin itching and is characterized in that the medical composition contains effective dose of hydrochloric acid nalbuphine and excipients acceptable as medicines.

The invention discloses a synthesis and purification method of a nalbuphine intermediate, the synthesis route of the method is as shown in the specification, and the method comprises the following steps: (1) in a reaction solvent, carrying out oxidation reaction on a compound I and peroxide to generate a compound II; (2) quenching, concentrating and extracting the reaction liquid containing the compound II obtained in the step (1), concentrating an extracted organic phase, adding a recrystallization solvent, and recrystallizing at-5 DEG C to 30 DEG C to obtain the compound II; wherein the recrystallization solvent is a mixed solvent of methyl tert-butyl ether and a low-polarity solvent, and the volume ratio of the methyl tert-butyl ether to the low-polarity solvent is (1-9): (1-4). According to the method, the purity of the compound II and the recrystallization yield are remarkably improved, side reactions in the subsequent nalbuphine synthesis process can be reduced, the cost is reduced, and industrial production is facilitated.

The present invention relates to opioid-derived compositions and antagonists thereof for use in the field of opioid receptor modulation related therapies. The invention discloses a 3-hexadienoic acid ester modifier of an opioid drug. The 3-hexadienoic acid ester modifier is used for improving the combination of the opioid drug and an opioid receptor during oral administration. A 3-hexadienoate modifier of nalbuphine or a pharmaceutically acceptable salt thereof is formulated for improving the quality of pain management during intravenous, intranasal, transdermal, sublingual, rectal, local, intramuscular, subcutaneous or inhalation administration. The 3-hexadienoic acid ester modifier of the opioid antagonist is prepared and is used for improving the inhibition effect on an opioid receptor during oral administration. Also formulated is a 3-hexadienoic acid ester modifier of naloxone or a pharmaceutically acceptable salt thereof for use in improving sobering quality during intravenous, intranasal, transdermal, sublingual, rectum, local, intramuscular, subcutaneous or inhalation administration.

The invention relates to a senalbuphine depot preparation, belongs to the field of medical treatment, and particularly relates to a low-viscosity nalbuphine sebacate depot precursor composition which comprises acylglycerol, phosphatidylcholine, at least one oxygen-containing organic solvent, at least one nonionic stable amphiphilic substance and nalbuphine sebacate, the obtained low-viscosity depot precursor composition has higher drug loading capacity and smaller injection volume, and can reduce pain and stimulation of an injection site.

The invention presented is a remedial opioid overdose mixture that includes a therapeutically effective dose of an opioid receptor antagonist; and, a therapeutically effective dose of an opioid receptor agonist. In one embodiment, the opioid receptor antagonist is naloxone while the opioid receptor agonist is nalbuphine. One specific naloxone derivative is NX-90 and a specific nalbuphine derivative is NB-33. The mixture can be administered intranasally, intravenously and by autoinjector. In some dose mixtures, reversal time is about three minutes.

Provided herein are methods of treating nalbuphine-treatable disorders in an elderly patient.

The invention discloses a method for refining nalbuphine acid salt. The steps are as follows: a). The crude product of nalbuphine is dissolved in an organic solvent, decolorized, filtered, concentrated under reduced pressure and left to stand for crystallization to obtain nalbuphine; b). ).Nalbuphine is dissolved in purified water by heating at 60-70°C, adding dilute acid dropwise to adjust the pH to 3-4, and then undergoing operations such as crystallization to obtain the acid salt of nalbuphine. The method can significantly improve the product quality and purity of the nalbuphine acid salt raw material drug, and prepare the nalbuphine acid salt raw material drug that meets the requirements of dosage forms used in injections. In addition, the refining method of the present invention is simple in operation, high in yield, and easy to realize industrial production.

The present invention discloses the use of opioid drugs in the preparation of melanoma therapeutic drugs. The present invention first studies and finds that the opioid drug nalbuphine can inhibit the activation of the Src / AKT / NF‑κB pathway in melanoma cells, thereby inhibiting the proliferation, migration and invasion of melanoma cells, thereby achieving the purpose of promoting melanoma cell apoptosis; indicating that nalbuphine or opioid drugs with the same or similar functions as nalbuphine can be used to prepare melanoma therapeutic drugs, thereby providing a new approach for the treatment of melanoma.

The present invention relates to processes useful in the preparation of morphine analogs and derivatives, such as naltrexone, naloxone and nalbuphine and intermediates in the synthesis of said morphine analogs and derivatives. In a particular example, the process begins with for example oxymorphone, oxycodone, 14-hydroxycodeinone or 14-hydroxymorphinone, and includes the formation of an oxazolidine-containing intermediate using catalytic oxidation.

The invention discloses compound anesthetic for minks and a preparation method and application of the compound anesthetic and belongs to the fields of preparation and application of the compound anesthetic for minks. The compound anesthetic for minks comprises detomidine, lorazepam and nalbuphine. The preparation method incudes: (1) mixing the detomidine, lorazepam and nalbuphine; (2) adding water of injection with uniform mixing to obtain the compound anesthetic. The compound anesthetic is quick in anesthesia induction on minks, long in anesthesia duration, good in analgesia, sedation and muscle relaxation effects, smooth and steady in analepsia and simple to operate, has slight impact on all clinical conventional indexes and special indexes, almost has no side effect and can be used in operations such as long-distance mink transportation, electro-ejaculation, cesarean section, trauma and fracture needing chemical restraints or sedation.

A recombinant microbial host cell having improved in vivo conversion of reticuline and derivatives thereof (such as thebaine and / or oripavine) to relevant downstream opioids (such as neopinone, oripavine, northebaine, nororipavine or morphinone) and related compounds (such as heroin, morphine, codeine, thebaine, oripavine, oxycodone, hydrocodone, hydromorphone, oxymorphone, buprenorphine, naltrexone, naloxone or nalbuphine), wherein the microbial (such as fungal) host cell is heterologously expressing at least one functional transporter protein capable of transporting reticuline or a derivative thereof (such as thebaine and / or oripavine) and a heterologously expressed enzyme capable of acting upon reticuline or a derivative thereof. The invention also relates to uses of the microbial host cells and methods of making an opioid compound and / or opioid precursor compound and / or opioid derivative of interest.

The oxazolidine derived from the reaction of oxymorphone with the Burgess reagent, temporarily protected at 0-3 and C-6, reacts with Grignard or other suitable metallic or organometallic reagents to directly provide, for example, A / -allyl, A / -methylcyclopropyl and / V-methylcyclobutyl derivatives that are further converted into naltrexone, naloxone, nalbuphone and nalbuphine in excellent yields. These morphine analogs can be prepared from the oxazolidine in a one-pot synthesis.

The invention discloses an anaesthesia method capable of protecting neurological functions of gastroscope patients and belongs to the technical field of anaesthesia methods. A control group comprisesNS+propofol of 1mg / kg, a fentanyl group including fentanyl of 0.8ug / kg and propofol of 1mg / kg; a remifentanil group including remifentanil of 0.5ug / kg and propofol of 1mg / kg; a sufentanil group including sufentanil of 0.08ug / kg and propofol of 1mg / kg; and a nalbuphine group including nalbuphine of 0.10mg / kg and propofol of 1mg / kg. After the dosage of medicines is calculated according to the weightof a gastroscopy patient, the components in each group are diluted to 1ml / kg with a 0.9% sodium chloride injection solution, besides, medicine injection sequence is arranged, the injection speeds ofthe front two medicines are respectively controlled to be 60s according to the scheduled medicine injection sequence and according to a chronograph by a person specially assigned, the medicine injection time at intervals is 60s, the third medicine is continuously injected, the pushing injection speed of the propofol is 1ml / 6s, after eyelash reflection disappears, gastroscopy is begun, the propofolof 0.5-1mg / kg is additionally injected appropriately for body movement during a surgery, the pulse rate during the surgery is lower than 50 times / minute, intravenous injection of atropine is performed, the contractive pressure is 30% lower than a basic value, intravenous injection of ephedrine is performed, SPO2 is lower than 90%, and a face guard is used for assisting in breathing.

Provided is a topical composition of nalbuphine, comprising nalbuphine or a pharmaceutically acceptable salt thereof and at least one pharmaceutically acceptable excipient comprising a penetration enhancer, a thickening agent, a solvent, or any combination thereof. Also provided are a kit comprising a unit dosage of the topical composition of nalbuphine and a method treating pruritus condition, pain, or inflammatory condition by using the topical composition of nalbuphine.

The present invention relates to an injectable delayed-release pharmaceutical preparation comprising a nalbuphine ester prodrug, a preparation method and a medical application of the preparation, and the nalbuphine ester prodrug is homogeneously dissolved in pharmaceutically acceptable oil and an oil mixture Solubility remains in the solution of the solvent. The present invention also provides a method of adjusting the duration of action of the formulation by changing the ratio of the pharmaceutically acceptable oil and the oil miscibility maintaining solvent.

The present invention relates to methods for treating patients with chronic cough with nalbuphine compositions as well as treating cough, breathlessness, or dyspnea associated with IPF with nalbuphine compositions, wherein the method provides a therapeutic effect in a patient.