A dosage form contains a biologically active ingredient for treating or preventing a disease in the animal or human body, where treatment or prevention requires release of 50% or more of the biologically active ingredient in the small intestine within the pH range from 3 to 5.5. The dosage form contains: a) a core, containing the biologically active ingredient; b) an intermediate coating layer (ICL) onto or above the core, containing an alkaline agent; and c) an enteric coating layer (ECL) onto or above the ICL, containing an enteric polymer. The relation of alkaline agent to enteric polymer is 5 to 95% when calculated by the formula:

[00001]$\frac{\mathrm{quantity}\mathrm{of}\mathrm{alkaline}\mathrm{agent}\mathrm{in}\mathrm{grams}\mathrm{in}\mathrm{the}\mathrm{ICL}\times 100}{\begin{array}{c}(\mathrm{quantity}\mathrm{of}\mathrm{alkaline}\mathrm{agent}\mathrm{in}\mathrm{grams}\mathrm{in}\mathrm{the}\mathrm{ICL}+\\ \mathrm{quantity}\mathrm{of}\mathrm{enteric}\mathrm{polymer}\mathrm{in}\mathrm{grams}\mathrm{in}\mathrm{the}\mathrm{ECL}).\\ \mathrm{The}\mathrm{ICL}\mathrm{has}a\mathrm{thickness}\mathrm{of}\mathrm{about}22\mu m\mathrm{or}\mathrm{more}.\end{array}}$

There is provided a composition comprising a plurality of particles of a weight-, number-, or volume-, based mean diameter that is between amount 10 nm and about 700 .Math.m, which particles are made up of: (a) a solid core, which solid core preferably comprises a biologically active agent; (b) one or more discrete layers surrounding said core, said one or more layer s each comprising at least one separate coating material; and (c) a final overcoating layer of a coating material, which overcoating layer surrounds, encloses and/or encapsulates said core and said previously-applied layers of coating material, and which final layer is of a thickness that is less than said previously-applied layers. Said layers (b) and (c) are preferably applied by way of a gas phase coating technique, such as atomic layer deposition. When the cores comprise biologically active agent, the compositions may provide for the delayed or sustained release of said active agent without a burst effect.

The invention is directed to oral modified/controlled release drug formulations which provide a rapid initial onset of effect and a prolonged duration of effect. Preferably, the peak concentration is lower than that provided by the reference standard for immediate release formulations of the drug, and the duration of effect falls rapidly at the end of the dosing interval.

The present invention is drawn to novel topiramate compositions as well as methods for effecting weight loss, e.g., in the treatment of obesity and related conditions, including conditions associated with and/or caused by obesity per se. The present invention features an escalating dosing regimen adapted for the administration of topiramate and optionally a sympathomimetic agent such as phentermine or bupropion, in the treatment of obesity and related conditions.

A dosage form contains a) a core, containing a biologically active ingredient, which is stable to a degree of at least 95% at a pH of 3 for 2 hours at 22° C.; b) an intermediate coating layer (ICL) onto or above the core, containing an alkaline agent; and c) an enteric coating layer (ECL) onto or above the intermediate coating layer, containing an enteric polymer. The relation in percent of the alkaline agent in the ICL to the enteric polymer in the ECL is 5 to 95% when calculated by the formula:

[00001]$\frac{\begin{array}{cc}\mathrm{quantity}\mathrm{of}\mathrm{alkaline}\mathrm{agent}\mathrm{in}\mathrm{grams}\mathrm{in}\mathrm{the}\mathrm{ICL}& \times 100\end{array}}{\left(\mathrm{quantity}\mathrm{of}\mathrm{alkaline}\mathrm{agent}\mathrm{in}\mathrm{grams}\mathrm{in}\mathrm{the}\mathrm{ICL}+\mathrm{quantity}\mathrm{of}\mathrm{enteric}\mathrm{polymer}\mathrm{in}\mathrm{grams}\mathrm{in}\mathrm{the}\mathrm{ECL}\right).}$

There is provided a process for the preparation of composition in the form of a plurality of particles having a weight-, number-, and/or volume-based mean diameter that is between amount 10 nm and about 700 μm, which particles comprise: (a) solid cores, preferably comprising a biologically active agent; and (b) two or more sequentially applied, discrete layers, each of which comprises at least one separately applied coating material, and which two or more layers together surround, enclose and/or encapsulate said cores, which process comprises the sequential steps of: (1) applying an initial layer of at least one coating material to said solid cores by way of a gas phase deposition technique; (2) discharging the coated particles from the gas phase deposition reactor and subjecting the coated particles to agitation to disaggregate particle aggregates formed during step (1) by way of mechanical sieving technique; (3) reintroducing the disaggregated, coated particles from step (2) into the gas phase deposition reactor and applying a further layer of at least one coating material to the reintroduced particles; and (1) optionally repeating steps (2) and (3) one or more times to increase the total thickness of the at least one coating material that enclose(s) said solid core. The gas phase deposition technique is preferably atomic layer deposition. When the cores comprise biologically active agent, the compositions may provide for the delayed or sustained release of said active agent without a burst effect.

An immediate release, unit doses of GHB or one of the therapeutically acceptable salts thereof administered via oral route. Such unit doses contain between 0.37 and 1.75 g of GHB, when under the form of granules, these granules have the following composition (weight % relative to the total weight of the granule): Active ingredient (sodium oxybate): 50 to 60%; Effervescent agent: 5 to 15%; Diluent: 2 to 18%; Binder: 3 to 10%; Substrate (Solid core of the granule): 15 to 25%; Coating agent/flavouring agent/sweetening agent/lubricant: 3 to 6%. Application for maintaining abstinence from alcohol of patients with mild or moderate alcohol dependence or with severe or very severe alcohol dependence, either suffering or not from liver disease.

An implantable device for delivery of a macromolecular drug compound is provided. The device comprises a core having an outer surface and a membrane layer positioned adjacent to the outer surface of the core. The core comprises a core polymer matrix within which is dispersed a drug compound having a molecular weight of about 0.5 kDa or more, the polymer matrix containing a hydrophobic polymer. Further, the membrane layer comprises a membrane polymer matrix within which the macromolecular drug compound is optionally dispersed. The concentration of the macromolecular drug compound in the core is greater than the concentration of the macromolecular drug compound in the membrane layer.

An implantable device for delivery of a macromolecular drug compound is provided. The device comprises a core having an outer surface and a membrane layer positioned adjacent to the outer surface of the core. The core comprises a core polymer matrix within which is dispersed a drug compound having a molecular weight of about 0.5 kDa or more, the polymer matrix containing a hydrophobic polymer. Further, the membrane layer comprises a membrane polymer matrix within which the macromolecular drug compound is optionally dispersed. The membrane polymer matrix contains a hydrophobic polymer in combination with a hydrophilic compound, and the weight ratio of the hydrophobic polymer to the hydrophilic compound within the membrane polymer matrix ranges from about 0.25 to about 200.

The present invention discloses an extended release multi-particulate sprinkle composition comprising a plurality of discrete units, each discrete unit comprising quetiapine or a pharmaceutically acceptable salt thereof and one or more pharmaceutically acceptable excipients.