54 results about "Bupivacaine" patented technology

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.

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.

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.

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.

Embodiments of the present application relate to compositions bupivacaine multivesicular liposomes (MVLs) prepared by a commercial manufacturing process with large particle diameter span.

Embodiments of the present application relate to batches of bupivacaine multivesicular liposomes (MVLs) prepared by a commercial manufacturing process using independently operating dual tangential flow filtration modules.

A sterile and ready-to-use bupivacaine solution is contained in a polymeric bag and is substantially free of any buffer, excipient, and preservative. Advantageously, the solution and the polymeric material allow for autoclaving to sterility without a significant pH drift towards lower pH values and for maintaining active ingredient in solution.

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.

A process for preparing bupivacaine encapsulated multivesicular liposomes (MVLs) comprising mixing a first aqueous solution comprising phosphoric acid and a volatile water-immiscible solvent solution

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.

The invention relates to a bupivacaine sustained-release gel injection as well as a preparation method and application thereof. The bupivacaine sustained-release gel injection comprises the following components: bupivacaine, a degradable polymer, an alkaline additive and a biocompatible organic solvent. The bupivacaine sustained-release gel injection provided by the invention has higher drug loading capacity and lower burst release level, is convenient to administrate, can release entrapped bupivacaine within 5-7 days, takes effect quickly, and can play a continuous analgesic role in vivo.

The present invention discloses a biodegradable microsphere sustained-release preparation loaded with bupivacaine and a preparation method thereof. Using a biodegradable polymer material as a carrier, the sustained-release microspheres loaded with bupivacaine are prepared by an electrostatic spraying method. The mass percentages of the components in the microspheres respectively account for the total weight of the microspheres as follows: polymer material: 50% - 93%; bupivacaine: 7% - 50%. Compared with the traditional complex preparation methods of drug microspheres, the microspheres prepared by the present invention have uniform particle sizes; the encapsulation rate and drug loading rate of the loaded microspheres are relatively high, the encapsulation rate is above 80%, and the drug loading rate can reach 50%; the drug can be slowly released for 72 hours, and the burst release rate is relatively low, and the drug release in the first 4 hours is below 35%; the preparation method is simple and feasible; the reaction conditions require low; it is easy to be prepared and scaled up in the laboratory.

Embodiments of the present application relate to batches of bupivacaine multivesicular liposomes (MVLs) prepared by a commercial manufacturing process using independently operating dual tangential flow filtration modules.

The present invention relates to an injectable pharmaceutical composition comprising bupivacaine or a pharmaceutically acceptable salt thereof. In particular, the present invention further relates to an aqueous multivesicular liposomal composition of bupivacaine or a pharmaceutically acceptable salt thereof, and a process of preparation thereof.

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.

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.

Embodiments of the present disclosure relate to methods of using bupivacaine multivesicular liposomes for stellate ganglion block to treat or ameliorate anxiety disorders or traumatic brain injury associated with the over-active or unbalanced sympathetic nervous system, including but not limited to versatile anxiety disorders, panic disorders, and post-traumatic stress disorders.

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.

Prodrugs and derivatives of anesthetics (e.g., capsaicin, bupivacaine) and methods of using the same.

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 invention relates to the field of medicine synthesis, and discloses a synthesis method of a bupivacaine EP impurity C. The method comprises the following steps: dissolving a compound 1, a compound 2 and an amidation reagent in a first organic solvent, carrying out a stirring reaction at a first temperature, and carrying out column chromatography separation to obtain a compound 3; dissolving the compound 3, alkali and tetrabutylammonium iodide in a second organic solvent, carrying out stirring reaction at a second temperature, and carrying out column chromatography separation to obtain a compound 4; dissolving the compound 4 in a dry third organic solvent, adding a catalyst under the protection of inert gas, stirring and reacting at a third temperature, and performing column chromatography separation to obtain the bupivacaine EP impurity C. The invention also discloses a preparation method of the bupivacaine EP impurity. In the embodiment of the invention, a synthesis mode which is simple in purification, high in yield and stable in intermediate substance and does not use highly toxic and explosive dangerous articles and the like is provided.

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.