CS267935B1 - Theophylline containing pharmaceutival - Google Patents
Theophylline containing pharmaceutival Download PDFInfo
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- CS267935B1 CS267935B1 CS876111A CS611187A CS267935B1 CS 267935 B1 CS267935 B1 CS 267935B1 CS 876111 A CS876111 A CS 876111A CS 611187 A CS611187 A CS 611187A CS 267935 B1 CS267935 B1 CS 267935B1
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Abstract
RTeil sa liečivý prlpravok z indikačnej skupiny antiastmatických iiekov. Riešenie liekovej formy obchádza složité chemické cesty pripravy zvýšenia rozpustnosti teofylinu - účinnej látky - - ktoré sú potřebné k doslahnutiu programované! liekovej formy. Táto forma je výhodná pre dlhodobé llečenie astmotlkov. Technické riešenie je z výrobného hladiska jednoduché, nfe sú potřebné anf zložité galenické operácie k doslahnutiu žiadaného účinku. Potřebný efekt je dosfahnutý konkrétným zloženim pripravku podta predmetu vynálezu, teda poměru teofylin a ostatné pomocné látky, resp. vzájomným pomerom pomocných látok.The drug formulation was indicated groups of antiasthmatic drugs. Solving the dosage form bypasses complicated chemical pathways to increase solubility theophylline - the active substance - - which are needed to reach programmed! dosage form. This form is advantageous for long-term treatment of astmotlkov. Technical solution is from production looking simple, nfe are needed anf complex galenical operations to reach desired effect. The necessary effect is reached particular composition of the formulation of the invention, i.e. theophylline ratio and other excipients, respectively. relative to each other.
Description
Vynález sa týká perorálneho kusového přípravku s obsahom teofylinu, z ktorého sa uvedená liečivá látka postupné počas niekoíkých hodin uvolňuje. Riadené uvolnovanie je umožněné fyzikátnou zmeoou zmesou kyseliny arainooctovej /glycínu/ s teofylínom v tiekovej formě.The present invention relates to an oral particulate preparation containing theophylline from which said drug substance is gradually released over a period of several hours. Controlled release is enabled by the physical mixing of arainoacetic acid (glycine) with theophylline in liquid form.
Teofylin je vo vodě poměrně tažko rozpustný /1 : 120/, preto patři medzi látky, ktoré sa poměrně lažko spracovávajú do časovo riadenej liekovej formy. Skupina l ieČi vých látok so zniženou rozpustnosίου vo vodě vykazuje nízké hladiny účinnej látky v krvi a často dochádza ku kolisaniu hladin - najeli následkem velkosti kryštálu - v krvnej plazme.Theophylline is relatively sparingly soluble in water (1: 120), so it is one of the substances that is relatively easily processed into a time-controlled dosage form. The group of drugs with reduced solubility in water shows low levels of the active substance in the blood and often fluctuates the levels - driven due to the size of the crystal - in the blood plasma.
Z uvedeného dovodu snahou je to aby UeČivá látka bola čím vodorozpustnejŠi a a lehko ovládatelná z hlediska uvolňovania dalšími pomocnými látkami např.voskami,akrylátmi alebo inými živicemi a definovanou riadiacou achopnosíou odovzdávania aktivnej látky a liekovej formy.For this reason, the aim is to make the drug as water-soluble as possible and easy to control in terms of release by other excipients such as waxes, acrylates or other resins and a defined control rate of delivery of the active substance and dosage form.
Konkrétné v případe teofylinu jestvuje poměrně velký počet organických solí, ktoré zabezpeČujú jeho vyššiu rozpustnost vo vodě. Najznámejšie sů etyIend 1 am1 nová, cholínová a glycínová sol teofylinu.In the case of theophylline in particular, there are a relatively large number of organic salts which ensure its higher solubility in water. The best known salts are the ethylene, choline and glycine salts of theophylline.
Nevýhodou týchto chemickou cestou připravených solí je nízký obsah teofylinu v chemickej substancii, relativné komplikovaná výroba a v případe najviac používanej soli - e ty I endi am i ná tu teofylinu - toxický e f e k t. o rg an i c k e j bázy /Petrozzi J. E., Shore R. N. / 1976/ Generalized exfoliative dermatitis from etyI end 1 ami ne 1 12, 525, Arch. Derma to I . / .The disadvantages of these chemically prepared salts are the low content of theophylline in the chemical substance, the relatively complicated production and, in the case of the most widely used salt - the theft of theophylline - the toxic effect. o rg an i c k e j bázy (Petrozzi J. E., Shore R. N. / 1976) Generalized exfoliative dermatitis from ethyl end 1 ami ne 1 12, 525, Arch. Derma to I. /.
Nedráždivé, chemickou cestou vzniknuté soli ako napr. teofylinát sodnej soli glycinu obsahuje len 46 X hmot, účinnej látky, preto nie je vhodný pre přípravu liekových foriems vysokým obsahom teofylinu v tabletovej forme.Non-irritating, chemically formed salts such as glycine sodium theophylline contains only 46% by weight of active substance, therefore it is not suitable for the preparation of dosage forms with a high content of theophylline in tablet form.
Uvedené nepriaznivé efekty rieši předložený vynález tým sposobom, že využívá zvýšenu rozpustnost teofylinu s kyselinou aminooctovou v prostředí tráviacich štiav. Zmes je jednoduchá, fyzikálna, bez použitia syntetických metod.The present invention addresses these adverse effects by utilizing the increased solubility of theophylline with aminoacetic acid in digestive environments. The mixture is simple, physical, without the use of synthetic methods.
Podstatou vynálezu je to, že xantinové deriváty v prostředí tráviacich štiav v zmesi s kyselinou aminooctovou v hmot nos tnom. pomere teofylin - glycin 2 až 3:1 už natolko zvySujú svoju rozpustnost - z 1:120 na 1:40 až 60/ že prídavkom regulujúcich pomocných· látok ako např. syntetických akrylátov sú vhodné k vyhotoveniu liekovej formy s riadeným uvolňovanim.The essence of the invention is that xanthine derivatives in the environment of digestive juices in a mixture with aminoacetic acid in weight. the theophylline-glycine ratio of 2 to 3: 1 already increases its solubility to such an extent - from 1: 120 to 1:40 to 60) that by the addition of regulating auxiliaries such as e.g. synthetic acrylates are suitable for making a controlled release dosage form.
Postup je nasledovný: teofylin, kyselina aminooctová, práškované akryláty, plnivo napr. manitol, mastenec a stearan kovu alkalickej zeminy sa zmieša a bez dalšej úpravy sa priamo tabletuje.The procedure is as follows: theophylline, aminoacetic acid, powdered acrylates, filler e.g. mannitol, talc and alkaline earth metal stearate are mixed and tableted directly without further treatment.
Výhodou uvedeného postupu je nenáročná technologie, nízké energetické nároky c dóvodu vynechania granulačnej a sušiacej fázy, vysoký obsah účinnej látky v kusovej * liekovej forme.The advantage of this process is the undemanding technology, low energy requirements due to the omission of the granulation and drying phase, high content of the active substance in the unit dosage form.
V ďalšom je predmet vynálezu objasněný na dvoch príkladoch bez toho, že by sa na tieto výlučné obmedzoval.In the following, the subject matter of the invention is illustrated by two examples without being limited thereto.
Příklad 1'Example 1 '
Zloženie tablety: Teofylin bezvodý Oz25OOgTablet composition: Theophylline anhydrous O of 25OOg
Kyselina aminooctová 0,2000gAminoacetic acid 0.2000g
Hani tol 0,0630gHani tol 0.0630g
Kopolimerizát kyseliny /met-/akrylovej 0,0300g/ Met- / acrylic acid copolymer (0.0300 g)
Stearan vápenatý 0,0060gCalcium stearate 0.0060g
Claims (4)
Priority Applications (1)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
CS876111A CS267935B1 (en) | 1987-08-20 | 1987-08-20 | Theophylline containing pharmaceutival |
Applications Claiming Priority (1)
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CS876111A CS267935B1 (en) | 1987-08-20 | 1987-08-20 | Theophylline containing pharmaceutival |
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CS611187A1 CS611187A1 (en) | 1989-07-12 |
CS267935B1 true CS267935B1 (en) | 1990-02-12 |
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CS876111A CS267935B1 (en) | 1987-08-20 | 1987-08-20 | Theophylline containing pharmaceutival |
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1987
- 1987-08-20 CS CS876111A patent/CS267935B1/en not_active IP Right Cessation
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CS611187A1 (en) | 1989-07-12 |
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Legal Events
Date | Code | Title | Description |
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IF00 | In force as of 2000-06-30 in czech republic | ||
MM4A | Patent lapsed due to non-payment of fee |
Effective date: 20020820 |