CS267935B1 - Medicinal product containing theophylline - Google Patents

Abstract

RTeil is a medicinal product from the indication group of antiasthmatic drugs. The solution of the dosage form bypasses the complex chemical routes of preparation of theophylline solubility increase - active substance - - which are required to achieve the programmed! dosage form. This form is advantageous for long-term treatment of asthmatics. The technical solution is simple from a production point of view, no complex galenic operations are required to achieve the desired effect. The required effect is achieved by the specific composition of the preparation according to the subject of the invention, i.e. the ratio of theophylline and other excipients, or. the mutual ratio of excipients.

Description

CS 267935 B1 1

BACKGROUND OF THE INVENTION The present invention relates to an oral, theophylline-containing lump composition, which is released over a period of several hours. The released release is accomplished by a physical mixture of aroacetic acid glycerol with a lithium form.

Theophylline is relatively poorly soluble in water (1: 120), and therefore belongs to the intermediates which are relatively difficult to process into the time-cooled flake form. The group of lactic acid substances with reduced water solubility exhibits low levels of compound blood in the blood, and often there is a level of fluctuation in the blood plasma, in particular due to crystal size. Accordingly, it is desirable that the compound be water-soluble and controllable by other excipients, for example, by acrylic or other resins, and by a defined control capability of delivery of the active ingredient and dosage form.

Particularly in the case of theophylline, there is a relatively large number of organic salts which ensure its water solubility. Ethylendol and amylolefin, glycoline and theophylline salts are best known.

The disadvantage of these chemical salts is the low content of theophylline chemical substance, the relatively complicated production and, in the case of the most widely used, theophylline-ethylendlarainate, the toxic effect of the organic base ZPetrozzl J.E., ShoreR. N. (1976) Ceneralized exfoliatlve dermatltls from etylendlamlne 112, 525, Arch. Bec-natol./.

The non-irritating salt formed by the chemical, such as the glycol sodium theophyllate, contains only 46% by weight. therefore, it is not suitable for the preparation of lotions containing a lot of phthalate in the tablet form.

The non-antioxidant effects of the present invention in that they utilize the increased solubility of theophylline with ammonium acetic acid in the digestive medium. The mixture is simple, physically, without synthetic methods.

SUMMARY OF THE INVENTION The present invention provides that xanthine derivatives in the environment of digestive juices are mixed with aminoacetic acid in the theophylline-glycine 2 to 3: 1 ratio, which no longer exerts its soluble - from 1: 120 to 1:40 to 60 - by the addition of regulating excipients such as synthetic acrylates, suitable for use as a sustained release dosage form.

The process is as follows: theophylline, amino-acetic acid, powdered acrylic, fill, e.g., mannitol, talc and alkaline earth metal stearate are blended and tableted without further treatment. The advantage of this process is the low-tech, low-energy-consuming technology of the granulation and drying phase, the high content of solids in lump molds. In the following, the invention is illustrated by two examples without being limited thereto. Example 1

Compound tablets: Theophylline anhydrous 0.2500 g

Ammonium acetic acid 0.2000 g

Hanitol 0,0630g

Acid acid copolymer

Methyl / acrylic 0.0300 g

Calcium stearate 0.0060 g

Claims (4)

1. A medicament containing theophylline, characterized in that the controlled release of the active substance theophylline is achieved by a composition of a fixed piece ratio of theophylline - aminoacetic acid of 25:20, theophylline - mannitol 25: 6.3, theophylline - copolymer of 11 measures of acid Z met-Zakrylova 25: 3, theophylline - colloidal silicon dioxide 25: 0.1, theophylline - calcium or mag. - ezlum stearate 25: 0.6. 2. The medicament according to item 1, characterized in that the ratio of aminoacetic acid to mannitol is 20: 6.3. 3. The medicament according to items 1 and 2, characterized in that the ratio of aminoacetic acid to Zmet-Zakrylic acid copolymer is 20: 3. 4. The medicament according to items 1, 2 and 3, characterized in that the ratio of mannitol to Zmet-Zakryl acid merisate copolymer is 6.3: 3.