Patent classifications
A61P23/02
LONG-ACTING ROPIVACAINE PHARMACEUTICAL COMPOSITION, PREPARATION METHOD THEREFOR AND USE THEREOF
Provided are a long-acting ropivacaine pharmaceutical composition, a preparation method therefor and use thereof. The pharmaceutical composition comprises: ropivacaine; a pharmaceutical solvent; a pharmaceutical phospholipid; a pharmaceutical oil; and an efficacy enhancer, an optional antioxidant and an optional acid-base regulator. The pharmaceutical composition has a controllable release behavior and a sustained release effect, can significantly reduce the peak plasma concentration of the drug, maintain a stable plasma concentration in the body, prolong the effective treatment time, reduce the effective therapeutic dose, improve the utilization of the drug, and reduce the risk of neurotoxicity. The pharmaceutical composition has a long-acting analgesic effect and can be used for pain treatment.
LONG-ACTING ROPIVACAINE PHARMACEUTICAL COMPOSITION, PREPARATION METHOD THEREFOR AND USE THEREOF
Provided are a long-acting ropivacaine pharmaceutical composition, a preparation method therefor and use thereof. The pharmaceutical composition comprises: ropivacaine; a pharmaceutical solvent; a pharmaceutical phospholipid; a pharmaceutical oil; and an efficacy enhancer, an optional antioxidant and an optional acid-base regulator. The pharmaceutical composition has a controllable release behavior and a sustained release effect, can significantly reduce the peak plasma concentration of the drug, maintain a stable plasma concentration in the body, prolong the effective treatment time, reduce the effective therapeutic dose, improve the utilization of the drug, and reduce the risk of neurotoxicity. The pharmaceutical composition has a long-acting analgesic effect and can be used for pain treatment.
TREATMENT OF PAIN BY SUBARACHNOID ADMINISTRATION OF SUSTAINED-RELEASE LIPOSOMAL ANESTHETIC COMPOSITIONS
In some embodiments provided herein is a method of treating pain, the method comprising injecting into the subarachnoid space of the subject a pharmaceutical composition comprising: a) a multivesicular liposome comprising: at least one amphipathic lipid, and at least one neutral lipid; and b) an aqueous phase comprising bupivacaine phosphate, wherein the aqueous phase is encapsulated within the multivesicular liposome.
TREATMENT OF PAIN BY SUBARACHNOID ADMINISTRATION OF SUSTAINED-RELEASE LIPOSOMAL ANESTHETIC COMPOSITIONS
In some embodiments provided herein is a method of treating pain, the method comprising injecting into the subarachnoid space of the subject a pharmaceutical composition comprising: a) a multivesicular liposome comprising: at least one amphipathic lipid, and at least one neutral lipid; and b) an aqueous phase comprising bupivacaine phosphate, wherein the aqueous phase is encapsulated within the multivesicular liposome.
ANALGESIC FORMULATIONS AND METHODS FOR REDUCED POSTOPERATIVE NAUSEA AND VOMITING AND ENHANCED POSTOPERATIVE PAIN RELIEF
A multimodal antiemetic anesthetic/analgesic formulation for pain control not limited to postoperative pain control is described herein. The opioid-free/sparing anesthetic/analgesic formulation comprises a local anesthetic, an N-methyl-D-aspartate (NMDA) receptor antagonist, and a cyclooxygenase (COX) inhibitor such as Bupivacaine Hydrochloride, Ketamine Hydrochloride, and Ketorolac Tromethamine, which is effective to significantly reduce postoperative nausea and vomiting and enhance postoperative pain relief as compared to existing prior art anesthetics/analgesics. The formulation is administered to a mammal in need of anesthesia/analgesia and can be used as a preemptive and preventative multimodal analgesic. The formulation may have a buffer to enhance its shelf life and improve pharmacokinetics. The formulation may further comprise an alpha agonist, a steroid, a Transient Receptor Potential Channel agonist or antagonist, a beta-lactam antibiotic, a protein kinase inhibitor, a competitive or non-competitive glycine or glutamate antagonist, a glutamate or glycine inhibitor, a cyclooxygenase 3 inhibitor, or combinations thereof.
Vasoconstriction compositions and methods of use
The invention generally relates to compositions for inducing vasoconstriction. The compositions comprise highly selective alpha-2 adrenergic receptor agonists, at low concentrations, such as below 0.05% weight by volume. The compositions preferably comprise brimonidine. The compositions preferably have pH between about 5.5 and about 6.5.
Intravesical drug delivery device with retention frame and drug tablets
Intravesical drug delivery devices that include a device body, a number of solid drug tablets, and a retention frame. The device body includes a drug reservoir lumen and a retention frame lumen. The drug tablets is positioned in the drug reservoir lumen, and the retention frame is positioned in the retention frame lumen.
Topical anesthetics
The present disclosure provides compounds useful as anesthetics, such as topical anesthetics, of general formula (I): ##STR00001##
wherein: R.sub.1 is H, —OMe, Me, or one or more electron withdrawing groups; R.sub.2 and R.sub.3 are each independently H or alkyl or, taken together, form a 4- to 8-membered heterocyclic ring with the adjacent nitrogen atom; R.sub.4 is H or alkyl; R.sub.5 is H or one or more electron donating groups; and n is 1 to 4.
Topical anesthetics
The present disclosure provides compounds useful as anesthetics, such as topical anesthetics, of general formula (I): ##STR00001##
wherein: R.sub.1 is H, —OMe, Me, or one or more electron withdrawing groups; R.sub.2 and R.sub.3 are each independently H or alkyl or, taken together, form a 4- to 8-membered heterocyclic ring with the adjacent nitrogen atom; R.sub.4 is H or alkyl; R.sub.5 is H or one or more electron donating groups; and n is 1 to 4.
OROMUCOSAL FILM COMPOSITIONS COMPRISING EPINEPHRINE PARTICLES
The invention provides an oromucosal film composition comprising: a therapeutically effective amount of epinephrine solid particles having a particle size in the range of from about 0.01 um to about 100 um; and a pharmaceutically acceptable polymer wherein the epinephrine solid particles are dispersed in and/or disposed on a polymeric layer. The film compositions can be used for the treatment of anaphylactic shock, cardiac arrest, asthma, bronchial asthma, bronchitis, emphysema, respiratory infections, and allergic reactions. The film compositions may further contain local anesthetics and used for providing local anesthesia, such as for the treatment or prevention of tooth pain and treatment of mouth ulcers.