50 results about "Dexmedetomidine" patented technology

The objective of the present invention is to provide a dexmedetomidine transdermal composition and transdermal patch which are highly stable, non-irritating to the skin, significantly safe to be attached to the human body, and capable of achieving a sustained release effect for 2 to 5 days, as well as a method for preparing and using the same. [Solution] This application discloses a dexmedetomidine transdermal composition, a transdermal patch, and the preparation method and application thereof. The composition includes dexmedetomidine, propylene glycol, and a metal chelating crosslinker, or includes dexmedetomidine, propylene glycol, a metal chelating crosslinker, and a pressure-sensitive adhesive. In addition, this application adds propylene glycol as a solubilizing agent to the dexmedetomidine transdermal composition, which can reduce the generation of impurities and improve the compatibility of raw materials and auxiliary materials, and uses a metal chelating crosslinker and a pressure-sensitive adhesive together to jointly form the skeletal structure of the product, which significantly improves the adhesive performance and provides a better adhesion to patients.

The invention discloses a corneal endothelial cell protection liquid for reducing corneal endothelial cell metabolism, which takes dextran or a combination of dextran and chondroitin sulfate as a dehydrating agent, takes beta-hydroxybutyric acid and dexmedetomidine as antioxidants, and simultaneously contains two buffer systems of sodium bicarbonate and HEPES. According to the invention, the metabolism of corneal endothelial cells can be reduced, and the form of the corneal endothelial cells in vitro can be better maintained.

This specification discloses a method for administering dexmedetomidine or a pharmaceutically acceptable salt thereof to human subjects. The disclosed method is particularly suitable for the treatment of agitation associated with neurodegenerative diseases and / or neuropsychiatric disorders or disorders (e.g., Alzheimer's disease).

To provide methods of providing sedation or analgesia to a pediatric patient.SOLUTION: The presently disclosed subject matter relates to methods of administering an effective amount of dexmedetomidine to a pediatric patient in order to reduce the incidence of neurological damage. More specifically, the presently disclosed subject matter relates to methods of providing sedation or analgesia to a pediatric patient by administering a dexmedetomidine infusion and optionally a loading dose. The dexmedetomidine can be administered before, during or after surgery.SELECTED DRAWING: Figure 1

The invention discloses a soluble microneedle composition for improving sleep and a microneedle and application of the soluble microneedle composition, and belongs to the technical field of medical care, the soluble microneedle composition comprises a needle tip section composition and a substrate composition, comprising 1%-70% of dexmedetomidine or a salt thereof, 1.5%-10% of glycerin, 1.5%-15% of mannitol and the balance of water. The substrate composition is an aqueous solution of a high-molecular compound. The soluble microneedle composition for improving sleep provided by the invention can prevent dexmedetomidine or a salt thereof from diffusing in a microneedle product, so that carried drugs are concentrated at a needle tip part, a technical support is provided for effective transmission of active components and accurate sustained and controlled release drug delivery, and quantitative drug delivery of dexmedetomidine or a salt thereof is realized.

The invention discloses a dexmedetomidine derivative, application of the dexmedetomidine derivative and a quality control or detection method of a dexmedetomidine transdermal patch preparation, the dexmedetomidine derivative can be used as a standard substance for quality control of the dexmedetomidine transdermal patch preparation, and meanwhile, the invention provides a preparation method of the dexmedetomidine derivative.

The present disclosure relates to compositions, formulations, and associated methods for treating neurodegenerative diseases, wherein the compositions include an alpha-1 adrenergic agonist, such as midodrine, and an alpha-2A adrenergic agonist, such as dexmedetomidine. Upon administering to a human subject, the alpha-2A adrenergic agonist crosses the subject's blood-brain barrier thereby acting upon the subject's central nervous system, whereas the alpha-1 adrenergic agonist does not cross the subject's blood-brain barrier. The alpha-1 adrenergic agonist minimizes or eliminates the systemic vascular effects induced by the alpha-2A adrenergic agonist that causes the negative cerebral autoregulatory response, thereby enabling the alpha-2A adrenergic agonist to increase glymphatic flow in the subject's brain.

The present invention relates to methods of treating agitation using transdermal delivery patches containing dexmedetomidine.

This invention relates to pharmaceutical compositions, including compositions adapted for intranasal administration, comprising an active ingredient, including dexmedetomidine, pomalidomide, a selective phosphodiesterase type 4 inhibitor such as roflumilast, or combinations thereof, useful in the treatment of traumatic brain injury (TBI), including to prevent or reduce the neurological sequalae of TBI.

The present disclosure relates to the treatment of agitation caused by noradrenergic hyperarousal in an agitated subject. The present disclosure provides oromucosal dosage forms comprising effective amounts of latrepirdine either alone or in combination with dexmedetomidine or pharmaceutically acceptable salts thereof and one or more pharmaceutically acceptable carriers and / excipients. Methods of their use are also provided. The present disclosure also provides a method of treating depression by administering oromucosally a therapeutically effective amount of dexmedetomidine alone or in combination with latrepirdine.

The present application relates to the field of medicine biology, and particularly relates to a transdermal patch containing dexmedetomidine. By adding a penetration enhancer, the transdermal rate and the permeation amount are improved, the onset time is shortened, the patch content is reduced, the skin residue is reduced, and the skin redness / scarring at the administration site caused by the accumulation of the drug in the skin is effectively avoided.

The invention provides a dexmedetomidine sustained-release microneedle and a preparation process thereof. The dexmedetomidine sustained-release microneedle comprises a first section of matrix containing 3.5 W% of hyaluronic acid and 3.5 W% of polyvinylpyrrolidone, the matrix is degraded within about 10 minutes and can provide rapid preliminary drug release, and a second section of matrix containing 15 W% of polyvinyl methyl ether-alt-maleic acid, the matrix is slowly degraded within about 3 hours and can provide rapid preliminary drug release. And sustained drug release is provided. According to the dexmedetomidine sustained-release microneedle and the preparation process thereof, the sustained-release microneedle adopts a two-section structure, and high-performance materials such as hyaluronic acid, polyvinylpyrrolidone and polyvinyl methyl ether-alt-maleic acid are combined, so that the release process of a medicine is divided into two stages of quick effect taking and long-acting sustained release. The first section of matrix is degraded within 10 minutes, 30% of medicine can be rapidly released, and rapid effect taking is achieved.

The present invention discloses a class of 4-(1H)-imidazole derivatives represented by the following formula (I), their pharmaceutically acceptable salts, racemic mixtures, enantiomers, optical isomers and tautomers, as well as pharmaceutical compositions containing them, and their use as α2-adrenergic receptor agonists, especially as α 2A -agonists and their methods of use. Compared with the prior art, the compounds of the present invention show more potent agonist activity and higher selectivity for α 2A -AR, superior to the positive drug dexmedetomidine; and at the same time have a potent in vivo sedative effect. #imgabs0#

To provide a composition or the like for treating agitation or signs of agitation.SOLUTION: The present invention discloses a method of treating agitation or signs of agitation in a subject comprising sublingual administration of an effective amount of an alpha-2 adrenergic agent, more particularly dexmedetomidine or a pharmaceutically acceptable salt thereof. The method is particularly suitable for the treatment of agitation associated with neurodegenerative diseases and / or neuropsychiatric diseases. The present invention also discloses sublingual administration of an alpha-2 adrenergic agent, more specifically dexmedetomidine or a pharmaceutically acceptable salt thereof, at a dose that is effective to treat agitation or the symptoms of agitation but does not cause significant sedation in the subject.SELECTED DRAWING: Figure 1A

The invention relates to a dexmedetomidine film agent and a preparation method thereof, the prescription components of the dexmedetomidine film agent comprise dexmedetomidine or a pharmaceutically acceptable salt thereof and a film-forming agent, and the mass ratio of dexmedetomidine to the film-forming agent is 1: (20-200); the film-forming agent is glucose polymer ether. The glucose polymer ether can be a cellulose ether derivative and / or a starch ether derivative. When the glucose polymer ether is a starch ether derivative, the formula further comprises a plasticizer. The preparation method comprises the following steps: coating slurry to prepare a film, and drying; the slurry comprises the prescription components of the dexmedetomidine and water. And the obtained film agent product is stable in quality.

Aspects of the invention include methods of managing pain in a subject by applying a transdermal delivery device containing a dexmedetomidine composition formulated to deliver a pain relieving effective amount of dexmedetomidine to a subject. In practicing methods according to certain embodiments, a transdermal delivery device having a dexmedetomidine composition is applied to a subject and is maintained in contact with the subject in a manner sufficient to deliver an amount of dexmedetomidine effective to manage pain in the subject. In some embodiments, methods include hydrating the subject, such as by administering a hydration fluid composition to the subject. Methods according to certain embodiments may also include co-administering an opioid to the subject. Also provided is a transdermal delivery device configured to deliver dexmedetomidine sufficient for practicing the subject methods, as well as kits containing the transdermal delivery device.

The invention provides a dexmedetomidine transdermal patch which comprises a backing layer, a release film and a polymer matrix layer arranged between the backing layer and the release film, the polymer matrix layer comprises dexmedetomidine, povidone and a pressure-sensitive adhesive, based on the total mass of the polymer matrix layer, the dexmedetomidine accounts for 4-10%, the povidone accounts for 5-10%, and the pressure-sensitive adhesive accounts for 5-10%. The povidone accounts for 2-12%, and the pressure-sensitive adhesive accounts for 78-94%; the pressure-sensitive adhesive comprises at least one of polymers containing carboxyl or hydroxyl functionalization.

The application discloses a dexmedetomidine transdermal composition, a transdermal patch and a preparation method and application thereof. The composition comprises dexmedetomidine, propylene glycol, a metal chelate crosslinking agent or dexmedetomidine, propylene glycol, a metal chelate crosslinking agent and pressure-sensitive adhesive. In addition, by adding propylene glycol as a solubilizer in the dexmedetomidine transdermal composition, the generation of impurities can be reduced, the compatibility of raw and auxiliary materials is better, meanwhile, the metal chelate crosslinking agent and the pressure-sensitive adhesive are used to jointly form the skeleton structure of the product, so that the adhesion performance is significantly improved and the patient's fitting feeling is better. The product has good stability, no skin irritation, the safety of the product when being attached to the human body is significantly improved, and the slow-release effect of 2-5 days can be achieved.

The present disclosure relates to compositions, formulations, and associated methods for treating neurodegenerative diseases, wherein the compositions include an alpha-1 adrenergic agonist, such as midodrine, and an alpha-2A adrenergic agonist, such as dexmedetomidine. Upon administering to a human subject, the alpha-2A adrenergic agonist crosses the subject's blood-brain barrier thereby acting upon the subject's central nervous system, whereas the alpha-1 adrenergic agonist does not cross the subject's blood-brain barrier. The alpha-1 adrenergic agonist minimizes or eliminates the systemic vascular effects induced by the alpha-2A adrenergic agonist that causes the negative cerebral autoregulatory response, thereby enabling the alpha-2A adrenergic agonist to increase glymphatic flow in the subject's brain.

Described herein are compositions, devices, and methods useful for treating (reversing) and / or preventing fentanyl overdose resulting in respiratory failure or airway obstruction (FIVCC). Compositions are provided that include optimized amounts and / or ratios of two active ingredients, including: an alpha 2 adrenergic receptor agonist (e.g., lofexidine, dexmedetomidine, clonidine) and a short acting mu opioid receptor antagonist (e.g., naloxone); an alpha 2 adrenergic receptor agonist and a long acting mu opioid receptor antagonist (nalmefene); and an alpha 2 adrenergic receptor agonist and a fentanyl opioid analgesic. Methods and devices for concurrent delivery of combined active ingredients are also provided.

A preparation method of an external patch for preoperative sedation relates to the field of medical preparations containing organic effective components, and sequentially comprises the steps of preparing a main component pretreatment substance, preparing a matrix solution, preparing an ointment-containing paste and synthesizing the patch, the preparation method of the main component pretreatment substance comprises the following steps: preparing a mixed liquid by taking dexmedetomidine hydrochloride and floperidol as main components, carrying out spray granulation to obtain a composite solid dispersion, crushing the composite solid dispersion into powder, and mixing and stirring the powder with paraffin oil and superfine silica powder. In the patch prepared from dexmedetomidine hydrochloride and floperidol, the effective components can quickly penetrate through the skin mucous membrane, so that the effect of quickly taking effect is achieved, and a good sedative effect is achieved. The dispersion uniformity of main components in the patch is excellent, the RSD is within 2%, and the effect consistency of the patch is guaranteed. According to the dexmedetomidine hydrochloride tablet, the stability of dexmedetomidine hydrochloride is effectively improved, components are prevented from being decomposed in the long-term storage process, other impurities are not generated, and the shelf life is effectively prolonged to 24 months.

The present disclosure relates to methods of using transdermal delivery patches containing dexmedetomidine to treat agitation.

Disclosed herein are methods of administering relatively high doses of dexmedetomidine or a pharmaceutically acceptable salt thereof to a human subject, without also inducing significant sedation. The disclosed methods are particularly suitable for the treatment of agitation, especially when associated with neurodegenerative and / or neuropsychiatric diseases such as schizophrenia, bipolar illness such as bipolar disorder or mania, dementia, depression, or delirium.

This application relates to the use of dexmedetomidine in the preparation of a drug for protecting the glycocalyx structure of lung tissue, a formulation thereof, and its application, belonging to the field of lung injury technology. This application provides a formulation for protecting the glycocalyx structure of lung tissue, the formulation containing dexmedetomidine, which can protect the glycocalyx structure of lung tissue, thereby reducing lung injury and can be used to treat lung injury.

The present disclosure relates to methods of using transdermal delivery patches containing dexmedetomidine to treat agitation.

The present disclosure relates to methods of using dexmedetomidine for therapeutic purposes wherein the dexmedetomidine or a pharmaceutically acceptable salt thereof is administered at least once a day for at least two consecutive days.

The present disclosure relates to method of treating or preventing depression in a human subject having Major Depressive Disorder or a Major Depressive Episode, the method comprising (a) an induction phase, comprising administering to the subject a therapeutic amount of dexmedetomidine or a pharmaceutically acceptable salt thereof in combination with a therapeutic amount of a selective serotonin reuptake inhibitor (SSRI) / serotonin norepinephrine reuptake inhibitors (SNRI) from about 1 day to about 28 days, followed by (b) a maintenance phase comprising administering to the subject a therapeutic amount of the SSRI / SNRI.

The invention discloses application of dexmedetomidine in preparation of a medicine for treating pressure-induced multi-system related diseases of children and adolescents. Aiming at the physiological characteristic that children and adolescents are highly susceptible to pressure due to immature prefrontal cortex, the invention provides that dexmedetomidine can improve the mitochondrial function by regulating the prefrontal cortex GR mitochondrial translocation of the children and adolescents for the first time; therefore, dexmedetomidine is applied to preparation of the medicine for treating the pressure-induced multi-system related diseases of children and adolescents, and a new target is provided for research and development of medicines for depression or other pressure related diseases of children and adolescents which are highly sensitive to pressure. In addition, dexmedetomidine has good safety, and the pain points that existing drugs are insufficient in safety, neglect in growth and development requirements and poor in treatment effect in multi-system related disease people induced by pressure of children and teenagers are solved.

Disclosed herein are methods of administering dexmedetomidine or a pharmaceutically acceptable salt thereof to a human subject. The disclosed methods are particularly suitable for the treatment of agitation, especially when associated with neurodegenerative and / or neuropsychiatric diseases or disorders such as dementia and delirium.

The present disclosure relates to methods of using transdermal delivery patches containing dexmedetomidine to treat agitation.