70 results about "Dose dumping" patented technology

The present invention relates to compositions for oral administration. The invention preferably comprises at least one abuse-resistant drug delivery composition for delivering a drug having potential for dose dumping in alcohol, related methods of preparing these dosage forms, and methods of treating a patient in need thereof comprising administering the inventive compositions to the patient. Most preferably, the dosage form includes verapamil. These formulations have reduced potential for abuse. In another formulation, preferably the abuse relevant drug is an opioid and the non-abuse relevant drug is acetaminophen or ibuprofen. More preferably, the opioid is hydrocodone, and the non-abuse relevant analgesic is acetaminophen. In certain preferred embodiments, the dosage forms are characterized by resistance to solvent extraction; tampering, crushing or grinding. Certain embodiments of the inventions provide dosage forms that provide an initial burst of release of drug followed by a prolonged period of controllable drug release.

The invention provides formulations that resist dose dumping in the presence of ethanol and methods of use thereof. The formulations can be used to prevent dose dumping, to increase safety of drugs, and to reduce abuse of drugs prone to such abuse. The formulations comprise at least one drug and a sustained release delivery system. In one embodiment, the drug is an opioid.

The present invention relates to compositions for oral administration. The invention preferably comprises at least one abuse-resistant drug delivery composition for delivering a drug having potential for dose dumping in alcohol, related methods of preparing these dosage forms, and methods of treating a patient in need thereof comprising administering the inventive compositions to the patient. Most preferably, the dosage form includes verapamil. These formulations have reduced potential for abuse. In another formulation, preferably the abuse relevant drug is an opioid and the non-abuse relevant drug is acetaminophen or ibuprofen. More preferably, the opioid is hydrocodone, and the non-abuse relevant analgesic is acetaminophen. In certain preferred embodiments, the dosage forms are characterized by resistance to solvent extraction; tampering, crushing or grinding. Certain embodiments of the inventions provide dosage forms that provide an initial burst of release of drug followed by a prolonged period of controllable drug release.

Robust sustained release formulations, solid dosage forms comprising robust sustained release formulations, and methods for making and using these formulations and solid dosage forms are provided. Robustness of the sustained release formulation is related to the particle size of the hydrophilic gum. Sustained release formulations resist dose-dumping when ingested with alcohol. The formulations are useful for treating a patient suffering from a condition, e.g., pain. The formulations comprise at least one drug. In one embodiment, the drug is an opioid, e.g., oxymorphone.

Abuse resistant polyglycol-based pharmaceutical compositions are disclosed. The composition contains one or more polyglycols and one or more active substances and it is resistant to crushing, melting and / or extraction. Moreover, such compositions have the same or lower solubility in ethanolic-aqueous medium, i.e. they are not subject to ethanol-induced dose dumping effect.

The object of the present invention is to minimize the risks of dose dumping associated with the concomitant consumption of alcohol and certain modified-release pharmaceutical or dietetic forms. The invention relates to an oral form comprising microparticles of the reservoir type for the modified release of at least one active principle (AP), characterized in that it is resistant to immediate dumping of the dose of AP in the presence of alcohol. In particular, the oral form according to the invention is characterized in that the time taken to release 50% of the AP in an alcoholic solution is not reduced more than 3-fold relative to the time taken to release 50% of the AP in an alcohol-free aqueous medium. The form comprises an agent D, which is a pharmaceutically acceptable compound whose hydration or solvation rate or capacity is greater in an alcohol-free aqueous medium than in alcoholic solution

The present invention provides alcohol resistant oral dosage pharmaceutical forms and methods of using such oral dosage forms to avoid dose dumping if the dosage form is taken together with alcohol.

Robust sustained release formulations, solid dosage forms comprising robust sustained release formulations, and methods for making and using these formulations and solid dosage forms are provided. Robustness of the sustained release formulation is related to the particle size of the hydrophilic gum. Sustained release formulations resist dose-dumping when ingested with alcohol. The formulations are useful for treating a patient suffering from a condition, e.g., pain. The formulations comprise at least one drug. In one embodiment, the drug is an opioid, e.g., oxymorphone.

The invention relates to a tamper-resistant, oral pharmaceutical dosage form comprising a pharmacologically active ingredient having psychotropic action and an ethylene-vinyl acetate (EVA) polymer which provides resistance against solvent extraction, resistance against grinding, and resistance against dose-dumping in aqueous ethanol.

A pharmaceutical composition is disclosed. The composition comprises a core comprising an active substance or a salt thereof; a separating layer comprising at least one sugar; and a functional layer comprising at least one pharmaceutically acceptable polymer, wherein the composition is resistant to dose dumping in presence of alcohol.

Disclosed are methods of sustained release administration of opioids, including but not limited to hydromorphone and oxycodone, that exhibit improved properties with respect to co-ingestion with aqueous alcohol.

The invention provides ilaprazole enteric-coated tablets and a preparation method thereof. Each enteric-coated tablet contains an enteric-coated pellet and pharmaceutically acceptable tablet excipients, wherein the enteric-coated pellet contains a pellet layer, a medicine loading layer, an isolation layer and an enteric coating layer; and the medicine loading layer contains ilaprazole or pharmaceutically acceptable salt thereof and a stabilizer. The enteric-coated pellet tablets prepared from the ilaprazole have good acid resistance; barrier substances such as an antiacid, a surfactant, an organic solvent, a hydrophobic substance and the like are not contained in the prescription, so that the enteric-coated pellet tablets have health benefits and are safe; the preparation method is easy to operate, the organic solvent is not used, and an active substance is quickly and stably released; and in addition, the pellets in the tablets can be widely and uniformly distributed in an intestinal tract after being taken, the dose dumping is dispersed, and the distribution area of a medicine on the surface of the intestinal tract is increased, so the irritation of the medicine to the intestinal tract can be reduced or eliminated, and the bioavailability of the medicine can be improved.

The invention relates to modified release oral formulations of therapeutic agents, including gamma hydroxybutyrate (GHB), paracetamol, codeine or oxycodone, which are resistant to alcohol induced dose dumping. Provided are formulations that have improved resistance to rapid release of the active ingredient in the presence of increasing amounts of alcohol. Also provided are formulations that can reduce or prevent the release of the active ingredient following exposure to alcohol-containing media. The invention also relates to methods of making the formulations, and methods of their use for the treatment of sleep disorders such as apnea, sleep time disturbances, narcolepsy, cataplexy, sleep paralysis, hypnagogic hallucination, sleep arousal, insomnia, and nocturnal myoclonus.

A tamper-resistant pharmaceutical dosage form comprising a pharmacologically active ingredient embedded in a prolonged release matrix, which comprises a prolonged release matrix material selected from the group consisting of nonionic acrylic polymers and waxy materials and which provides prolonged release of the pharmacologically active ingredient, resistance against solvent extraction, resistance against grinding, and resistance against dose-dumping in aqueous ethanol.

A method of reducing the risk of alcohol-induced dose-dumping of a therapeutically active ingredient comprising administering to human subjects who have ingested alcohol an oral controlled release tablet; said tablet comprising:a core comprisingan upper compressed layer comprising a swelling agent, anda lower compressed layer comprising at least one therapeutically active ingredient, and pharmaceutically acceptable excipient wherein at least one excipient is a release rate controlling excipient and wherein the percent by weight of excipients that are soluble in alcohol does not exceed 35% by weight of the layer and;a coating surrounding the said core, the coating comprising a polymer insoluble in an aqueous medium comprising from 0% v / v to 40% v / v of alcohol, whereby upon contact with aqueous gastrointestinal fluids, the upper compressed layer swells to cause removal of the coating from the upper surface of the upper compressed layer and then said upper layer disintegrates allowing the release of the active ingredient from the defined surface area of the upper surface of said lower compressed layer with the coating covering its bottom and side surfaces.

The invention relates to an oral pharmaceutical dosage form providing resistance against dose dumping in aqueous ethanol and comprising a pharmacologically active ingredient embedded in a matrix material,wherein the matrix material comprises an alkyl cellulose and a heteropolysaccharide; andwherein the relative weight ratio of heteropolysaccharide to alkyl cellulose is within the range of from 1:20 to 20:1; andwherein the total content of alkyl cellulose and heteropolysaccharide is at least 35 wt.-%, relative to the total weight of the dosage form. A process of producing the dosage form and methods of using the dosage form, for example to treat pain, are also disclosed.

The invention relates to a DMF (dimethyl fumarate) enteric-coated micropellet and a preparation method thereof. The DMF enteric-coated micropellet comprises a pellet core and a double-layer enteric coating, wherein the pellet core is coated with the double-layer enteric coating. The enteric-coated micropellet is prepared by the following steps: the pellet core is prepared with the extrusion-spheronization method; and the pill-containing pellet core is coated with the double-layer enteric coating to form the enteric-coated micropellet. The obtained DMF enteric-coated micropellet is simple in preparation technology, complete in drug release and good in reproducibility, and external dose dumping risk is reduced.

An abuse deterrent drug product is provided wherein the drug product comprises a matrix and a drug substance in the matrix wherein the drug substance is defined as a 1:1 salt of a pharmaceutically active compound and BNDO.

The object of the present invention is to minimize the risks of dose dumping associated with the concomitant consumption of alcohol and certain modified-release pharmaceutical or dietetic forms.The invention relates to an oral form comprising microparticles of the reservoir type for the modified release of at least one active principle (AP), characterized in that it is resistant to immediate dumping of the dose of AP in the presence of alcohol. In particular, the oral form according to the invention is characterized in that the time taken to release 50% of the AP in an alcoholic solution is not reduced more than 3-fold relative to the time taken to release 50% of the AP in an alcohol-free aqueous medium.The form comprises an agent 13, which is a pharmaceutically acceptable compound whose hydration or solvation rate or capacity is greater in an alcohol-free aqueous medium than in alcoholic solution.

The invention discloses a slow-release medicine carrier with improved performance, which includes (a) fatty glyceride whose melting point in vivo and vitro is more than 37 DEG C; (b) additive particles which are soluble in water, has low viscosity and no irritation; (c) an acidic (or alkalic) polymer with water swelling ability and water insolubility; (d ) an alkalic (or acidic) surfactant; and (e) a medicament. The medicament carrier has better medicament-release characteristic, high salt poisoning resistance, low irritation to mucous membrane, better biological compatibility and better medicament-release homogeneity and better relieves or solves the problem of end release; and meanwhile it is not easy to generate medicament safety problems such as burst release or dose dumping of medicament.

Robust sustained release formulations, solid dosage forms comprising robust sustained release formulations, and methods for making and using these formulations and solid dosage forms are provided. Robustness of the sustained release formulation is related to the particle size of the hydrophilic gum. Sustained release formulations resist dose-dumping when ingested with alcohol. The formulations are useful for treating a patient suffering from a condition, e.g., pain. The formulations comprise at least one drug. In one embodiment, the drug is an opioid, e.g., oxymorphone.

It is intended to avoid dose dumping of a drug and improve the dissolution properties of the drug in the lower gastrointestinal tract, and thereby provide a sustained-release pellet preparation for oral administration that reliably exhibits its main pharmacological effect when orally administered once or twice a day. The present invention provides a sustained-release preparation obtained by mixing of (A) a pharmacologically active drug, (B) hydroxypropyl methylcellulose acetate succinate, (C) a plasticizer, and (D) polyethylene glycol followed by extrusion granulation.

The invention discloses a drug carrier capable of realizing sustained release of a drug, which improves the performances and contains (a) an aliphatic additive, wherein the in vivo melting point and the in vitro melting point are higher than the temperature of 37 DEG C; (b) water-soluble additive particles with low viscosity and no irritation; (c) a water-insoluble acidic (or alkaline) polymer with water swelling property; (d) an alkaline (or acidic) surfactant; and (e) the drug. The drug carrier has better drug release property, higher resistance to salt poisoning, lower mucosa irritation, better biocompatibility and better drug release uniformity, can better ease or solve the problem of end release, and is difficult to cause initial burst release of the drug or dose dumping and other drug safety problems.

A pharmaceutical composition comprising a drug substance consisting essentially of a pharmaceutically acceptable organic acid addition salt of an amine containing pharmaceutically active compound wherein the amine containing pharmaceutical active compound is selected from the group consisting of racemic or single isomer ritalinic acid or phenethylamine derivatives and the drug substance has a physical form selected from amorphous and polymorphic.

A liquid or semi-solid matrix or magma or paste which is non-newtonian, thixotropic and pseudoplastic and composed of one or more controlled release agent, and / or one or more clays such as bentonite and / or one or more fillers in a non aqueous vehicle, and optionally materials selected from disintegrants, humectants, surfactants and stabilizers. The composition and physicochemical properties makes it harder or prevents dose dumping of narcotic analgesics in the presence of alcohol and harder to abuse opiod agonists or narcotic analgesics and discourages drug abuse via crushing, milling or grinding the dosage form to powder or heating the dosage form to vapour and snorting or inhalation by the nasal route or dissolving to abuse via the parenteral route.

The invention discloses a slow-release drug carrier with improved performance. The drug carrier contains (a) an aliphatic additive in vivo-in vitro fusing points of which is higher than 37 DEG C, (b) low-viscosity water-soluble nonirritant additive particles, (c) a water-swelling and water-insoluble acidic (or alkaline) polymer, (d) an alkaline (or acidic) surfactant, and (e) a medicament. The drug carrier has the advantages of better drug release character, higher 'salt poisoning' resistance effect, lower mucosal irritation, better biocompatibility and better drug release uniformity, thus better relieving or solving 'terminal release' problem and avoiding medication safety problems such as burst drug release or dose dumping and the like.

It is intended to avoid dose dumping of a drug and improve the dissolution properties of a drug in the lower gastrointestinal tract, and thereby provide a sustained-release solid preparation for oral administration that reliably exhibits its main pharmacological effect when orally administered once or twice a day. The present invention provides a sustained-release solid preparation containing (A) a pharmacologically active drug, (B) carboxyvinyl polymer, (C) povidone, and (D) carmellose sodium, xanthan gum, or sodium carboxymethyl starch.

It is intended to avoid dose dumping of a drug and improve the dissolution properties of the drug in the lower gastrointestinal tract, and thereby provide a sustained-release matrix preparation for oral administration that reliably exhibits its main pharmacological effect when orally administered once or twice a day. The present invention provides a sustained-release preparation obtained by mixing of (A) a pharmacologically active drug, (B) hydroxypropyl methylcellulose acetate succinate having a median size (D50) of 40 μm or smaller, (C) a cellulose derivative, and (D) a saccharide or a nonionic water-soluble polymer followed by molding.

Disclosed are methods of sustained release administration of opioids, including but not limited to hydromorphone and oxycodone, that exhibit improved properties with respect to co-ingestion with aqueous alcohol.