32 results about "Bupivacaine" patented technology

The present application relates to a bupivacaine sustained-release gel injection and a preparation method and application thereof, the components of the bupivacaine sustained-release gel injection include bupivacaine, degradable polymer, alkaline adjuvant and biocompatible organic solvent.The bupivacaine sustained-release gel injection provided by the present application has higher drug loading and lower burst level, is convenient to administer, can prolong the release of the encapsulated bupivacaine to 5-7 days, has rapid onset, and can exert sustained analgesic effect in vivo.

The invention discloses a bupivacaine-containing pharmaceutical composition and a preparation method and application thereof.The pharmaceutical composition comprises bupivacaine, sucrose acetate isobutyrate, benzyl alcohol and a stabilizer.The bupivacaine preparation has good stability and a long-acting analgesic effect, the preparation process is simple, and the preparation method is suitable for industrial production. The method is suitable for large-scale production.

Embodiments of the present disclosure relates to commercial manufacturing process of making bupivacaine multivesicular liposomes with improved yield and desired particle size distribution.

Embodiments of the present disclosure relates to a new and improved large scale commercial manufacturing process of making bupivacaine multivesicular liposomes (MVLs). Batches of bupivacaine MVLs prepared by the new process have high yields, improved stabilities, and desired particle size distributions.

Compositions and methods of use related to formulations comprising anesthetics are generally described. Some embodiments are directed to compositions comprising a plurality of micelles and / or particles, and an anesthetic contained internally. These can be used to control and / or prolong the duration of IVRA while reducing the risk of systemic toxicity commonly due to administering anesthetics. The control and / or prolonged duration of IVRA may be due, at least in part, to the attachment of the sufficiently small micelles and / or particles to a biointerface (e.g., blood vessel surface) where the composition has been administered. Conventional IVRA methods commonly do not utilize potent and long-acting anesthetics (e.g., bupivacaine) due to the risks of cardiac toxicity. The compositions and methods described herein, however, provide a pathway for increased safety and efficiency of the use of such anesthetics, in certain embodiments. Resultantly, the performance (e.g., anesthetic distribution) of the micelles and / or particles internally containing an anesthetic may be comparatively better than the performance of free anesthetic, e.g., with respect to nerve blood and systematic drug distribution.

The invention provides bupivacaine multivesicular liposome, gel and composition as well as a preparation method and application of the bupivacaine multivesicular liposome and gel. The bupivacaine polycystic liposome disclosed by the invention is prepared from the following components: 8 to 20 mg / mL of phosphoric acid, 5 to 15 mg / mL of dierucyl phosphatidylcholine, 0.5 to 5 mg / mL of dipalmitoyl phosphatidyl glycerol, 0.5 to 5 mg / mL of tricaprylin, 2 to 10 mg / mL of cholesterol, 15 to 35 mg / mL of bupivacaine, 25 to 140 mg / mL of lysine, 55 to 400 mg / mL of osmotic pressure regulator and 15 to 20 mg / mL of sodium chloride. The gel containing the bupivacaine multivesicular liposome and the composition provided by the invention can improve the analgesic effect, prolong the analgesic time and play a slow-release analgesic role, and can be applied to the field of postoperative slow-release long-acting multimode analgesia, and the used materials are non-toxic and non-irritant, and have good biocompatibility and degradability.

The invention provides a liquid formulation comprising bupivacaine or a pharmaceutically acceptable salt thereof, a method for preparing the formulation, and a product which includes the formulation. The formulation of the invention may include a tonicity agent, and has an initial pH of from about 4.2 to about 4.5. The formulation of the invention is stable and ready-to-administer.

A compressed lozenge comprising a core and a first coat, wherein the core comprises bupivacaine or a salt thereof, at least one binding agent, and at least one excipient, and the first coat comprises bupivacaine or a salt thereof, and at least one film-forming agent. The compressed lozenge is preferably substantially free from oxidizing agents. The compressed lozenge is suitable for use in the treatment or alleviation of pain such as pain in the oral cavity.

A wound dressing including a porous biosynthetic polymer film comprising a poly(lactide-co-caprolactone) (“PLC”) copolymer or other suitable polymer matrix, and a local analgesic loaded therein, to provide pain relief over an extended period of time (e.g., for 5-7 days), e.g., for healing of a partial thickness dermal injury. The PLC copolymer may have a particular lactide / caprolactone molar ratio (e.g., from 2:1 to 9:1) to ensure slow, sustained release of the bupivacaine or other analgesic. The dressing may provide a water vapor transmission rate from 1000 g / m2·day to 3000 g / m2·day to facilitate fast healing and regrowth of new epithelial tissue beneath the dressing. The dressing is configured to remain positioned over the dermal injury, providing wound protection for about 14 days, after which is simply debrides away, falls off, or is easily and painlessly removed, once new epithelial tissue regrows.

The present disclosure provides for methods of producing analgesia in a subject. In some cases, methods produce analgesia in a subject undergoing arthroscopic subacromial decompression surgery. The present disclosure also relates to improved sustained release drug delivery systems. In some cases, a composition comprises an active pharmaceutical agent; at least one of sucrose acetate isobutyrate and a polyorthoester; an organic solvent; and 2,6-dimethylaniline, wherein the 2,6-dimethylaniline is present at a level less than 500 ppm. In some cases, a composition comprises bupivacaine N-oxide at a level less than 1 wt %, based on weight of the composition. In some cases, a composition comprises metal present at a level less than 5 ppm. Dosage forms and methods are also provided.

Embodiments of the present disclosure relate to the use of bupivacaine multivesicular liposomes (MVLs) as stellate ganglion block (SGB) for treating or ameliorating various diseases and conditions, including but not limited to cardiac electrical storm or cardiac arrythmia / dysrhythmia following heart surgery.

The application provides bupivacaine microspheres, a preparation method and application thereof, the preparation raw material of the bupivacaine microspheres comprises bupivacaine or a pharmaceutically acceptable salt type thereof, a degradable polymer, an adjuvant and an organic solvent; the molecular weight of the degradable polymer is 5000-25000 Dalton. The bupivacaine microspheres prepared by the application have moderate particle size, and can simultaneously avoid defects such as slow onset, injection pain or short sustained release time. The bupivacaine microspheres prepared by the application have high bioavailability, and can realize 3-5 days of sustained release effect. The preparation method provided by the application has the advantages of simple operation, stable process, easy industrial production, and high drug loading of the prepared bupivacaine microspheres.

A compressed lozenge comprising a core and a first coat, wherein the core comprises bupivacaine or a salt thereof, at least one binding agent, and at least one excipient, and the first coat comprises bupivacaine or a salt thereof, and at least one film-forming agent. The compressed lozenge is preferably substantially free from oxidizing agents. The compressed lozenge is suitable for use in the treatment or alleviation of pain such as pain in the oral cavity.

The group of inventions relates to the field of medicine, and more particularly to haemostatics and drugs for providing temporary haemostasis in the case of non-major bleeds. Proposed are a pharmaceutical composition containing tranexamic acid, chlorhexidine digluconate, bupivacaine, and water, in the following proportions: 13-16 wt.% tranexamic acid, 2.00 wt.% chlorhexidine digluconate, 0.5 wt.% bupivacaine, and 81.5-84.5 wt.% water, and a drug in aerosol or spray form comprising said pharmaceutical composition. Use of the group of inventions makes it possible to stop bleeds very quickly and reduce the risk of renewed bleeding. In addition, providing the drug in the form of an aerosol or spray allows easy and convenient use. The proposed composition and drug can be used for providing temporary haemostasis in the case of non-major bleeds in the fields of dentistry, veterinary medicine, military field medicine, disaster medicine, and the like.

The present disclosure relates to a new and improved large scale commercial manufacturing process of making bupivacaine multivesicular liposomes (MVLs) comprising DPEC, DPPG, cholesterol and tricaprylin. Batches of bupivacaine MVLs prepared by the new process have high yields, improved stability profiles, and desired particle size distributions.

Embodiments of the present disclosure relate to the use of bupivacaine multivesicular liposomes (MVLs) as stellate ganglion block (SGB) for treating or ameliorating various diseases and conditions, including but not limited to cardiac electrical storm or cardiac arrythmia / dysrhythmia following heart surgery.

The invention belongs to the technical field of anesthetic drugs, and particularly relates to an anesthetic drug and a preparation method thereof. The anesthetic is prepared by mixing 1000 parts by weight of bupivacaine liposome injection, 0.5-1 part by weight of magnesium sulfate and 3-5 parts by weight of dexmedetomidine hydrochloride. Wherein magnesium sulfate and dexmedetomidine hydrochloride are auxiliary agents, so that the anesthesia onset time is shortened. The anesthetic prepared by the invention is smaller in side effect, quick in effect taking and long in maintenance time, the injection frequency of the anesthetic can be reduced, the infection risk and the nursing cost can be reduced, the anesthetic effect is good, and the application prospect is wide.

Embodiments of the present disclosure relate to a new and improved large scale commercial manufacturing process of making bupivacaine multivesicular liposomes (MVLs). Batches of bupivacaine MVLs prepared by the new process have high yields, improved stabilities, and desired particle size distributions.

Embodiments of the present disclosure relate to a new and improved large scale commercial manufacturing process of making bupivacaine multivesicular liposomes (MVLs). Batches of bupivacaine MVLs prepared by the new process have high yields, improved stabilities, and desired particle size distributions.

Provided herein are methods of administration to the fibular and tibial nerves of a patient, wherein the methods comprise: (a) selecting an entry point of an injection needle at the leg of the patient; (b) inserting an injection needle into the entry point of the patient; (c) administering the saline and the pharmaceutical composition to the sciatic nerve of the patient through the injection needle; wherein the pharmaceutical composition comprises a multi-vesicular liposome, the multi-vesicular liposome comprises at least one amphiphilic lipid, at least one neutral lipid and bupivacaine phosphate, and the bupivacaine phosphate is encapsulated in the multi-vesicular liposome.

Embodiments of the present application relate to commercial manufacturing processes for making bupivacaine multivesicular liposomes (MVLs) using independently operating dual tangential flow filtration modules.

The application is suitable for the fields of biological medicine and medical devices, and provides a medicine and device composition for preventing pacemaker pocket complications and application, which is a single entity including a drug component and a medical device component; the drug component is a double-layer core-shell nanoparticle co-loading bupivacaine and a magnesium agent, wherein the double-layer core-shell nanoparticle has an inner core and an outer shell, the inner core is a PLGA nanoparticle loading the magnesium agent, and the outer shell is a lipid bilayer loading bupivacaine, and the lipid bilayer is wrapped on the outer surface of the inner core; the medical device component is a temperature-sensitive gel matrix and a drug delivery device, the double-layer core-shell nanoparticles are uniformly dispersed in the temperature-sensitive gel matrix to form a composite temperature-sensitive gel, and the drug delivery device is used for injecting the composite temperature-sensitive gel, and the application provides a multifunctional medicine and device composition integrating analgesia, anti-inflammation and anti-infection for preventing pacemaker pocket complications, and has important clinical transformation value.

The invention discloses a medicine for inhibiting tumor cell activity by combining arsenic trioxide and bupivacaine and application of the medicine, and belongs to the technical field of biological medicine. The medicine comprises arsenic trioxide and bupivacaine, the concentration of the arsenic trioxide is 2 microns, and the concentration of the bupivacaine is 200 microns. The solvent is a complete cell culture medium. The complete cell culture medium is prepared from 89vol% of DMEM (dulbecco modified eagle medium) high-glucose culture medium, 10vol% of fetal calf serum and 1vol% of penicillin-streptomycin solution. The combination of arsenic trioxide and bupivacaine can significantly inhibit proliferation and migration of liver cancer cells and has a synergistic anti-liver cancer effect, the proliferation and migration functions of the liver cancer cells can be significantly inhibited by single use of an ineffective small dose of arsenic trioxide and bupivacaine, and the application dose of arsenic trioxide can be reduced so as to reduce the toxic and side effects of arsenic trioxide.

This invention provides bupivacaine microspheres with controllable in vitro release and long-lasting analgesia. The microspheres use lactide-glycolic acid copolymer (PLGA) as the carrier material and bupivacaine as the drug; they have high drug loading, encapsulation efficiency and good sustained-release effect.

This invention relates to the field of pharmaceutical formulation technology, and more particularly to an injectable bupivacaine-meroxicam sustained-release solution, its preparation method, and its application. The sustained-release solution comprises the following components in the indicated mass fractions: bupivacaine or a pharmaceutically acceptable salt thereof 1.5%–3.5%; meloxicam or a pharmaceutically acceptable salt thereof 0.03%–0.15%; poloxamer 407 15%–25%; poloxamer 188 1%–8%; hydroxypropyl methylcellulose 0.5%–5%; an osmotic pressure regulator 0.7%–5%; a buffer salt 0.1%–1%; and the balance being water. This invention constructs a thermosensitive in-situ gel system, enabling the formulation to be a flowable solution at room temperature, which rapidly transforms into a semi-solid gel reservoir at body temperature after injection, achieving a long-lasting and stable sustained release of bupivacaine and meloxicam for over 24 hours. All components are safe pharmaceutical excipients with good biocompatibility; the preparation process is simple.

A wound dressing including a porous biosynthetic polymer film comprising a poly(lactide-co-caprolactone) (“PLC”) copolymer or other suitable polymer matrix, and a local analgesic loaded therein, to provide pain relief over an extended period of time (e.g., for 5-7 days), e.g., for healing of a partial thickness dermal injury. The PLC copolymer may have a particular lactide / caprolactone molar ratio (e.g., from 2:1 to 9:1) to ensure slow, sustained release of the bupivacaine or other analgesic. The dressing may provide a water vapor transmission rate from 1000 g / m2·day to 3000 g / m2·day to facilitate fast healing and regrowth of new epithelial tissue beneath the dressing. The dressing is configured to remain positioned over the dermal injury, providing wound protection for about 14 days, after which is simply debrides away, falls off, or is easily and painlessly removed, once new epithelial tissue regrows.

The present disclosure provides for methods of producing analgesia in a subject. In some cases, methods produce analgesia in a subject undergoing arthroscopic subacromial decompression surgery. The present disclosure also relates to improved sustained release drug delivery systems. In some cases, a composition comprises an active pharmaceutical agent; at least one of sucrose acetate isobutyrate and a polyorthoester; an organic solvent; and 2,6-dimethylaniline, wherein the 2,6-dimethylaniline is present at a level less than 500 ppm. In some cases, a composition comprises bupivacaine N-oxide at a level less than 1 wt %, based on weight of the composition. In some cases, a composition comprises metal present at a level less than 5 ppm. Dosage forms and methods are also provided.

The present disclosure relates to a new and improved large scale commercial manufacturing process of making bupivacaine multivesicular liposomes (MVLs) comprising DPEC, DPPG, cholesterol and tricapryl

The present disclosure relates to a new and improved large scale commercial manufacturing process of making bupivacaine multivesicular liposomes (MVLs) comprising DPEC, DPPG, cholesterol and tricaprylin. Batches of bupivacaine MVLs prepared by the new process have high yields, improved stability profiles, and desired particle size distributions.