67 results about "Midazolam" patented technology

A pharmaceutical composition with improved safety includes a selected amount of a vomit-inducing agent, wherein the selected amount is less than an amount needed to induce vomit in a user; and a therapeutic agent. The therapeutic agent may be selected from a sleeping pill, an anxiolytic, a hypnotic, a contraceptive agent. The therapeutic agent may also be selected from diazepam, flunitrazepam, alprazolam, triazolam, fludiazepam, midazolam, estazolam, zopiclone, and a combination thereof. The vomit-inducing agent may be selected from emetine, cephaeline, and a combination thereof.

This invention provides methods for the amelioration, termination and/or abortion of a seizure by the intrapulmonary administration of a benzodiazepine, for example, midazolam.

Compositions of midazolam, a benzodiazapine, in concentrations of 35-100 mg/ml are disclosed for the treatment of anxiety, epilepsy and epileptic seizures, invasive surgical procedures and diagnostic procedures and sedation. These compositions are particularly characterized by a solubilizer such an propylene glycol. Preferably, the compositions are aqueous solutions for intranasal administration.

The invention provides a kit for determining antianxiety/hypnotic type drugs in serum and plasma through liquid chromatography tandem mass spectrometry. The kit comprises the following constituents: drug standards comprising bromazepam, clonazepam, diazepam, lorazepam, midazolam, nitrazepam, oxazepam and Temazepam; drug internal standard compounds comprising alprazolam-d5, clonazepam-d4, diazepam-d5, lorazepam-d4, midazolam-d4, nitrazepam-d5, oxazepam-d5 and Temazepam-d5; drug extraction compositions comprising, by volume, 60% of methanol solution, 20% of acetonitrile solution, 10% of isopropanol solution and 10% of purified water; negative plasma; and diluent: 50% of carbinol water solution. The kit can be used for simultaneously determining antianxiety/hypnotic type drugs and active metabolites thereof, and has the advantages of short determination time and high flux.

The invention belongs to fields of pharmacy and pharmaceutics and relates to a midazolam medicament composition as well as a preparation method and application thereof. Particularly, the midazolam medicament composition comprises midazolam and/or pharmaceutically acceptable salts of midazolam, serving as main medicament components, and pharmaceutically acceptable auxiliary materials, wherein the content of the main medicament components is 0.2%-2%. The midazolam medicament composition provided by the invention is administered through an orifice, so that the bioavailability and curative effectof the midazolam medicament are improved, and favorable compliance can be achieved.

The invention belongs to the field of medical chemistry, and particularly relates to an impurity A and an impurity B of midazolam or a pharmaceutical composition of midazolam and a preparation methodthereof, and application of the impurity A and the impurity B as reference standard substances for quality control of midazolam or the pharmaceutical composition of midazolam.

The invention relates to a method for preparation of 4H-imidazo[1, 5-a][1, 4]benzodiazepine, especially midazolam through a selective decarboxylation reaction of formula (VII) with a DBU (1,8-diazabicyclo[5.4.0.]-undec-7-ene) novel catalyst in an NMP (N-methyl pyrrolidone) solvent. According to the invention, isomerization of 4H-imidazo[1, 5-a][1, 4]benzodiazepine is avoided, the midazolam synthesis yield is enhanced, and the post-treatment difficulty is reduced.

A drug for sedating a patient, and especially a smoker, during eye surgery. The drug includes a sedative such as midazolam in a mix with nicotine. The mixture is injected into the patient prior to the eye surgery.

The invention belongs to the field of medicines and pharmaceutics, and relates to a midazolam combination, a preparation method of the midazolam combination, and the application of the midazolam combination. Specifically, the midazolam combination comprises 2.5 to 8.0 percent (g/ml) of midazolam, 5 to 30 percent (g/ml) of cyclodextrin and 30 to 80 percent (ml/ml) of polyols through being calculated according to the total volume of the midazolam combination, wherein the cyclodextrin is carefully selected from one or more of beta cyclodextrin, hydroxypropyl-beta cyclodextrin, gamma cyclodextrin, dimethyl beta cyclodextrin, trimethyl beta cyclodextrin, hydroxypropyl beta cyclodextrin and HE-beta cyclodextrin; and the polyols are selected from one or more of propylene glycol, glycerol, polyoxyethylene castor oil and polyethylene glycol. The concentration of the midazolam in the combination can reach above 25mg/ml and the pH (potential of hydrogen) value of the midazolam is between 4.5 and 10.0. The invention additionally relates to the preparation method of the combination and the application of the combination during the preparation of medicines for curing epilepsy and achieving the effects of anti-anxiety, sedation, peaceful sleeping, muscular relaxation or anti-convulsion.

The present invention refers to a process for the preparation of 4H-imidazo[1,5-a][1,4]benzodiazepines, in particular Midazolam, through an efficient and selective decarboxylation reaction of the derivative compound of the 5-aminomethyl-1-phenyl-1H-imidazole-4-carboxylic acid of formula (II)

avoiding the formation of the 6H-imidazo[1,5-a][1,4]benzodiazepines by-products and the ensuing process for the isomerisation of a 4H-imidazo[1,5-a][1,4]benzodiazepine product.

A pre-operative composition for sedation or analgesia is used to sedate a patient before a medical procedure. The pre-operative composition is formulated to prevent negative effects felt by the patient after the medical procedure. The pre-operative composition includes dexmedetomidine, midazolam, and some kind of pharmaceutical carrier. The pre-operative composition can be administered in a variety of methods to the patient. The preferred method of administering the pre-operative composition is either orally or by a syringe.

The invention discloses a method for testing influence of midazolam on development of testicular interstitial cells cultured in vitro. Comprising the following steps: culturing rats, separating CD90 positive cells, culturing testicular mesenchymal stem cells (SLC), detecting the influence of midazolam on proliferation and differentiation, amplifying the SLCs and detecting the cell activity, carrying out DAPI dyeing and counting, analyzing cells by a flow cytometer, analyzing testosterone (T) and progesterone (P4), carrying out mRNA and protein expression detection through QPCR (Quantitative Polymerase Chain Reaction) and WB (White Brown) experiments, and determining significant differences and drawing a chart through SNK (Sodium Nitrogen Kinase) detection. The steps are simple, and the influence of midazolam medicine on proliferation and differentiation of the testicular mesenchymal stem cells can be effectively verified.

The invention discloses a compound anesthetic for a rat and a preparation method thereof and belongs to the field of preparation and application of animal compound anesthetics. The invention discloses the compound anesthetic for the rat for the first time. The compound anesthetic comprises dexmedetomidine, midazolam, oxycodone, a buffer solution and water for injection. The invention further discloses the preparation method of the compound anesthetic for the rat. The preparation method comprises the following steps: dissolving the above components in the water for injection; diluting; filtering; pilling in an ampoule bottle; and sterilizing to obtain. The compound anesthetic for the rat disclosed by the invention is quick in anesthesia induction, long in anesthesia maintenance time, good in antalgic and sedative effects and stable in revival, and the main influence on physiological and biochemical indexes of the rat is within the physiological range tolerance. The compound anesthetic is simple to operate and can be used for complex or long-term operations of the rat.

The invention discloses a 2-(2-chlorophenyl) quinazoline-4 (3H)-one derivative shown in formula (I) or pharmaceutically acceptable salts thereof. Compared with the existing first-line sedative and hypnotic drugs diazepam and midazolam, the compound has stronger drug effect and faster metabolism speed, can reduce the next-day residual effect, and is expected to be developed into a novel high-efficiency low-toxicity sedative and hypnotic drug.

The invention discloses a compound anesthetic for racoon dogs as well as a preparation method and application thereof, and belongs to the fields of preparation and application of compound anesthetics for racoon dogs. The compound anesthetic for the racoon dogs comprises the following components: dexmedetomidine, midazolam and water for injection. The invention further discloses a method for preparing the compound anesthetic for the racoon dogs, and the method comprises the following steps: (1) mixing the dexmedetomidine and the midazolam; (2) adding the water for injection and mixing evenly to obtain the compound anesthetic for the racoon dogs. Animal experiments prove that the compound anesthetic for the racoon dogs has an excellent anesthetic effect on the racoon dogs, and is quick and steady in induction and waking, and excellent and balanced in calming, pain easing and muscle relaxation effects; the compound anesthetic has a marginal effect on the circulatory system, the respiratory system, blood indexes and partial liver and kidney indexes, and can be applied to preparing the clinical anesthetics for the racoon dogs.

The invention relates to an infusion container comprising a sterile, ready-to-use, stable aqueous solution of Midazolam or a pharmaceutically acceptable salt thereof, suitable for direct intravenous infusion to a patient in need thereof. The invention also relates to a novel infusion container having plurality of ports that is suitable for delivering or receiving a sterile fluid, such as the said stable aqueous solution of Midazolam or a pharmaceutically acceptable salt thereof

The invention provides an midazolam nanocrystal suspension as well as a preparation method and application thereof. The midazolam nanocrystal suspension is neutral, and is relatively small in irritation and good in safety; and in addition, the nanocrystal suspension improves the problem of insolubility of midazolam, improves the bioavailability, and has a good curative effect. The midazolam nanocrystal suspension is stable in preparation process and suitable for industrial production, and the nanocrystal suspension obtained through the process is good in stability, free of particle aggregationand layering phenomena and good in release and dissolution.

The invention provides an application of a midazolam nanocrystal and a composition thereof in medicines for improving blood-brain barrier permeability. According to the midazolam nanocrystal, the solubility problem is solved, the bioavailability is improved, the problem that the treatment effect is poor when tablets and injection are used as anticonvulsant and antiepileptic drugs is solved, and the midazolam nanocrystal can effectively penetrate through a blood brain barrier and is used for treating epilepsy. In addition, the invention provides a technical platform, and the blood-brain barrierpermeability of the brain medicine is improved by the nanocrystalline preparation in the presence of a space protective agent and a charge stabilizer.

The present invention relates to an industrial production method of a midazolam derivative. The industrial production method is characterized in that a compound A and a compound B are subjected to a ring-forming reaction under the condition of a catalyst. According to the present invention, the production method is simple, and is different from the complex production way and the stringent production conditions in the prior art; the synthesis of the target product can be achieved through the one step; the yield can be increased by at least 50% compared to the multi-step synthesis in the prior art; and the production process and the synthesis route are optimized, such that the advantages of less side reaction, convenient post-treatment and mild production condition during the production process are provided, and the method is suitable for the industrial production mode.