635751-84-7

Upstream product

• 138530-94-6 (R)-lansoprazole 
• 635751-18-7 2-[[4-(aminocarbonyl)phenyl]amino]ethyl acetate 
• 32315-10-9 bis(trichloromethyl) carbonate 
• 1194-02-1 4-fluorobenzonitrile 
• 98952-77-3 4-(N-2-hydroxyethyl)-aminobenzonitrile 

Relevant academic research and scientific papers

CONTROLLED RELEASE PREPARATION

A controlled release preparation wherein the release of active ingredient is controlled, which releases an active ingredient for an extended period of time by staying or slowly migrating in the gastrointestinal tract, is provided by means such as capsulating a tablet, granule or fine granule wherein the release of active ingredient is controlled and a gel-forming polymer. Said tablet, granule or fine granule has a release-controlled coating-layer formed on a core particle containing an active ingredient.

METHOD FOR PRODUCING GRANULES

In a production process of granules containing a biologically active substance, variation in the elution profile of the biologically active substance is reduced by heating the temperature of granules to about 50°C or higher and maintaining the temperature for about 1 minute or longer. By setting the spray speed to about 90 mg/min or more per 1 g of cores when a spray agent for a primary agent containing the biologically active substance is sprayed while spraying a binding liquid to the cores and setting the total feeding weight per unit area for a centrifugal fluidized bed coating granulation machine to about 1.5 g/cm2 or more, the variation in the elution profile of the biologically active substance from the granules is reduced.

DRUG COMPOSITION HAVING ACTIVE INGREDIENT ADHERED AT HIGH CONCENTRATION TO SPHERICAL CORE

Granule, fine particle or tablet of excellent leaching property, comprising a drug active ingredient in high content realized by forming a layer containing drug active ingredient on core particles through a combination of a method of dispersing and adhering an active ingredient while spraying or adding a binder with a method of spraying or adding a solution or suspension wherein an active ingredient and a binder are contained so as to effect adhesion. Further, there are provided a drug composition containing such a granule, fine particle or tablet and a process for producing the same.

CONTROLLED RELEASE COMPOSITION

The present invention provides a controlled release composition showing release of an active ingredient (proton pump inhibitor) controlled in two or more steps at different release rates, which contains1) a release-controlled part A capable of controlling release of the active ingredient to occur at a predetermined rate,2) a release-controlled part B capable of controlling release of the active ingredient to occur at a predetermined rate lower than the release rate of the release-controlled part A, and where necessary, 3) a release-controlled part C capable of controlling release of the active ingredient to occur at a predetermined rate faster than the release rate of the release-controlled part B, wherein the release of the active ingredient from the release-controlled part B precedes the release of the active ingredient from the release-controlled part A (when release-controlled part C is contained, the release of the active ingredient from the release-controlled part C precedes the release of the active ingredient from the release-controlled part B).

PRODRUGS OF IMIDAZOLE DERIVATIVES, FOR USE AS PROTON PUMP INHIBITORS IN THE TREATMENT OF E.G. PEPTIC ULCERS

An imidazole compound represented by the formula (I), a salt thereof and a compound of the formula (V), which is one of the intermediates thereof. wherein each symbol is as defined in the present specification. The compound of the present invention shows a superior anti-ulcer activity, a gastric acid secretion inhibitory action, a mucosa-protecting action, an anti-Helicobacter pylori action and the like. Since it shows low toxicity, the compound is useful as a pharmaceutical product.