416 results about "Controlled-Release Formulations" patented technology

Sustained release dosage forms for twice daily oral dosing to a human patient for providing relief from pain are provided. The sustained release dosage form comprises an immediate release component and a sustained release component, wherein the immediate release component and the sustained release component collectively contain a therapeutically effective amount of an opioid analgesic and a therapeutically effective amount of nonopioid analgesic. In a preferred embodiment, the nonopioid analgesic is acetaminophen and the opioid analgesic is hydrocodone and pharmaceutically acceptable salts thereof, and in preferred embodiments, the pharmaceutically acceptable salt is bitartrate. The dosage forms produce plasma profiles in a patient characterized by a Cmax for hydrocodone of between about 0.6 ng / mL / mg to about 1.4 ng / mL / mg and an AUC for hydrocodone of between about 9.1 ng*hr / mL / mg to about 19.9 ng*hr / mL / mg (per mg hydrocodone bitartrate administered) and a Cmax for acetaminophen of between about 2.8 ng / mL / mg and 7.9 ng / mL / mg and an AUC for acetaminophen of between about 28.6 ng*hr / mL / mg and about 59.1 ng*hr / mL / mg (per mg acetaminophen administered) after a single dose.

An oral delivery system for Class II drugs that have low oral bioavailability due to their insolubility in water and slow dissolution kinetics and method for making such a drug delivery system are disclosed herein. The formulation may be a controlled release or immediate release formulation. The immediate release formulation contains a Class II drug, together with a hydrophobic polymer, preferably a bioadhesive polymer. In one embodiment, the drug and polymer are co-dissolved in a common solvent. The solution is formed into small solid particles by any convenient method, particularly by spray drying. The resulting particles contain drug dispersed as small particles in a polymeric matrix. The particles are stable against aggregation, and can be put into capsules or tableted for administration. The controlled release formulations contain a BCS Class II drug and a bioadhesive polymer. The controlled release formulations may be in the form of a tablet, capsules, mini-tab, microparticulate, or osmotic pump. Enhancement of oral uptake of the drug from use of bioadhesive polymers occurs through (1) increased dissolution kinetics due to stable micronization of the drug, (2) rapid release of the drug from the polymer in the GI tract; and (3) prolonged GI transit due to bioadhesive properties of the polymers. The combination of these effects allows the preparation of a compact, stable dosage form suitable for oral administration of many class II drugs.

An extended release dosage composition of pharmaceutically active substances that have a water contact angle (θ) such that cos θ is between +0.9848 and −0.9848 presented as a matrix tablet containing the said pharmaceutically active substances, with / without suitable pharmaceutical excipients in intimate mixture with two groups of intelligent polymers having opposing wettability characteristics, one demonstrating a stronger tendency towards hydrophobicity and the other a stronger tendency towards hydrophilicity, the polymer combination being between the ratios of 1:50 and 50:1 amounts effective to control the release of said pharmaceutically active substances in a mathematically predictable manner, wherein the polymer demonstrating a stronger tendency towards hydrophobicity is not less than 5% wt / wt and preferably between 5-70% wt / wt of the final formulation composition. The intelligent polymers being ethylcellulose (EC) as a more strongly hydrophobic and hydroxyethylcellulose (HEC) and / or hydroxypropyl methylcellulose (HPMC) as more strongly hydrophilic (the ratio of HEC to HPMC being between 1:100 and 100:1). The matrix tablet is optionally coated with an enteric coat, 0-5%-15% wt / wt to prevent the initial burst effect seen in such systems and to impart gastrointestinal tract (GIT) “stealth” characteristics especially in the presence of food.

A sustained release dosage form is comprising a pharmaceutically active agent and pharmaceutically acceptable salts thereof and adapted to release as an erodible solid over a prolonged period of time, wherein the dosage form provides an ascending rate of release of the pharmaceutically active agent for at least about 4 hours. The dosage form is able to deliver high doses of poorly soluble or slowly dissolving active agents. When additional pharmaceutically active agents are present, the agents are released from the dosage form at rates that are proportional to the respective weights of each active agent in the dosage form. Methods of using the dosage forms to treat disease or conditions in human patients are also disclosed.