Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Priority claimed from SE9003903Aexternal-prioritypatent/SE9003903D0/en
Application filed by Astra AbfiledCriticalAstra Ab
Publication of SI9111867ApublicationCriticalpatent/SI9111867A/en
Publication of SI9111867BpublicationCriticalpatent/SI9111867B/en
A preparation of a pharmaceutically active ionizable substance where the active substance is ionically complexed with an ion exchange resin which is worked into a hydrophilically eroding matrix, as well as a procedure for its preparation.
Claims (8)
1 Patentni zahtevki 1. Farmacevtski pripravek za podaljšano sproščanje farmacevtsko aktivne ionizabilne snovi, označen s tem, da obsega ionski kompleks aktivne ionske snovi z nasprotno nabito ionsko izmenjevalno smolo; pri čemer je ionski kompleks vdelan v hidrofdno erodirajočo matrico, ki obstoji iz 100 mas.% do 10 mas.% derivatizirane celuloze in 0 mas.% do 90 mas.% sintetičnega polimera; pri čemer je hidrofilna erodirajoča matrica v takem razmerju glede na kompleks, da povzroči linearno sproščanje aktivne snovi.A pharmaceutical preparation for the prolonged release of a pharmaceutically active ionizable substance, characterized in that it comprises an ionic complex of the active ionic substance with an opposite charged ion exchange resin; wherein the ionic complex is embedded in a hydrophobic eroding matrix consisting of from 100% to 10% by weight of derivatized cellulose and 0% to 90% by weight of a synthetic polymer; wherein the hydrophilic erosion matrix is in such a ratio with respect to the complex to cause a linear release of the active substance.2. Postopek za pripravo farmacevtskega pripravka po zahtevku 1, označen s tem, da obsega stopnje: (a) kompleksiranja aktivne snovi z nasprotno nabito ionsko izmenjevalno smolo v vodi ali etanolu, da se tvori ionski kompleks; (b) vdelave dobljenega suhega kompleksa v hidrofdno erodirajočo matrico, ki obstoji iz 100 mas.% do 10 mas.% derivatizirane celuloze in 0 mas.% do 90 mas.% sintetičnega polimera, da se tvori suha zmes, ki ima približno razmerje ionskega kompleksa proti hidrofdni matrici 1 : 3; in (c) oblikovanja dobljene zmesi v obliko tablet.A process for the preparation of a pharmaceutical preparation according to claim 1, characterized in that it comprises the steps of: (a) complexing the active substance with a counter charged ion exchange resin in water or ethanol to form an ionic complex; (b) incorporating the resulting dry complex into a hydrophobic eroding matrix consisting of from 100% to 10% by weight of derivatized cellulose and from 0% to 90% by weight of a synthetic polymer to form a dry mixture having a ratio of ionic complex against hydrophobic matrix 1: 3; and (c) forming the resulting mixture into tablet form.3. Farmacevtski pripravek za podaljšano sproščanje aktivne sestavine, označen s tem, da obsega: (a) ionizabilno aktivno sestavino; (b) ionsko izmenjevalno smolo, ki tvori ionski kompleks z aktivno sestavino; in (c) hidrofdno erodirajočo matrico, ki obstoji iz 100 mas.% do 10 mas.% derivatizirane celuloze in 0% do 90 mas.% sintetičnega polimera, kjer je ionski kompleks vdelan pri primernem masnem razmerju okoli 1 dela ionskega kompleksa proti 3 delom hidrofdne matrice. 2A pharmaceutical preparation for the prolonged release of the active ingredient, characterized in that it comprises: (a) an ionizable active ingredient; (b) an ion exchange resin forming an ionic complex with an active ingredient; and (c) a hydrophobic eroding matrix consisting of from 100% to 10% by weight of derivatized cellulose and from 0% to 90% by weight of a synthetic polymer, wherein the ionic complex is embedded in an appropriate weight ratio of about 1 part of the ion complex to 3 parts hydrophobic matrix. 24. Izboljšan oralni farmacevtski pripravek, učinkovit za podaljšano sproščanje farmakološko aktivne snovi iz pripravka, ki vsebuje ionizabilno aktivno snov, ionsko kompleksirano z ionsko izmenjevalno smolo v vodi, pri čemer je ionski kompleks vdelan po sušenju v hidrofilno erodirajočo matrico, ki obstoji iz 100 mas.% do 10 mas.% derivatizirane celuloze in 0 mas.% do 90 mas.% sintetičnega polimera, tako da povzroči hitrost sproščanja aktivne sestavine proti linearnosti, označen s tem, da izboljšanje pripravka obsega masno razmerje okoli 1 : 3 ionskega kompleksa proti hidrofilni erodirajoči matrici.An improved oral pharmaceutical preparation, effective for prolonged release of a pharmacologically active substance from a composition comprising an ionizable active substance ionically complexed with an ion exchange resin in water, the ionic complex being incorporated after drying into a hydrophilic eroding matrix consisting of 100 weight % to 10% by weight of derivatised cellulose and 0% to 90% by weight of a synthetic polymer, to cause the release rate of the active ingredient to linearity, characterized in that the improvement of the composition comprises a mass ratio of about 1: 3 of the ion complex to the hydrophilic eroding matrices.5. Oralni farmacevtski pripravek za podaljšano sproščanje vodotopne aktivne sestavine, označen s tem, da obsega: (a) ionizabilno vodotopno aktivno sestavino; (b) ionsko izmenjevalno smolo, ki tvori ionski kompleks z aktivno sestavino v vodi; in (c) suho hidrofilno erodirajočo matrico, ki obstoji iz 100 mas.% do 10 mas.% derivatizirane celuloze in 0 mas.% do 90 mas.% sintetičnega polimera; pri čemer je ionski kompleks vdelan po sušenju v hidrofilno matrico pri masnem razmerju okoli 1 : 3 in kjer je podaljšano sproščanje približno linearno.An oral pharmaceutical preparation for the prolonged release of a water soluble active ingredient, characterized in that it comprises: (a) an ionizable water soluble active ingredient; (b) an ion exchange resin forming an ionic complex with an active ingredient in water; and (c) a dry hydrophilic eroding matrix consisting of from 100% to 10% by weight of derivatized cellulose and 0% to 90% by weight of a synthetic polymer; wherein the ionic complex is embedded after drying into a hydrophilic matrix at a ratio of about 1: 3 and wherein the prolonged release is approximately linear.6. Farmacevtski pripravek za enakomerno podaljšano sproščanje farmakološko aktivne ionizabilne snovi, označen s tem, da obsega ionski kompleks aktivne ionske snovi z nasprotno nabito ionsko izmenjevalno smolo; pri čemer je ionski kompleks vdelan v hidrofilno erodirajočo matrico, ki obstoji iz hidroksipropilmetilceluloze, ki vsebuje 27-30% metoksi skupin in 7-12% hidroksipropoksi skupin; pri čemer je hidrofilna erodirajoča matrica v takem razmerju z ionskim kompleksom, da povzroči enakomerno podaljšano sproščanje aktivne snovi.Pharmaceutical preparation for uniformly prolonged release of a pharmacologically active ionizable substance, characterized in that it comprises an ionic complex of an active ionic substance with an opposite charged ion exchange resin; wherein the ionic complex is embedded in a hydrophilic eroding matrix consisting of hydroxypropylmethylcellulose containing 27-30% of methoxy groups and 7-12% of hydroxypropoxy groups; wherein the hydrophilic eroding matrix is in such a ratio with the ion complex to produce a uniformly prolonged release of the active substance.7. Oralni farmacevtski pripravek za enakomerno podaljšano sproščanje ionazibilne aktivne snovi, označen s tem, da obsega ionizabilno kislo aktivno snov z vodotopnostjo nad 10 mg/ml; ionizabilno kislo aktivno snov; 3 ionsko izmenjevalno smolo, ki obstoji iz premreženega polimera, ionsko kompleksiranega s kislo aktivno snovjo, da se tvori ionski kompleks, ki je vdelan v hidrofilno erodirajočo matrico, ki obstoji iz derivatizirane celuloze.An oral pharmaceutical preparation for a uniformly prolonged release of an ionizable active substance, characterized in that it comprises an ionizable acidic active substance with a solubility greater than 10 mg / ml; ionizable acidic active substance; 3 ion exchange resin consisting of a crosslinked polymer ionically complexed with an acidic active substance to form an ionic complex embedded in a hydrophilic eroding matrix consisting of derivatized cellulose.8. Oralni farmacevtski pripravek za enakomerno podaljšano sproščanje ionizabilne aktivne snovi, označen s tem, da obsega ionizabilno bazično aktivno snov z vodotopnostjo nad 10 mg/ml, izbrano iz skupine, ki obstoji iz metoprolola in terbutalina; kationsko izmenjevalno smolo, kije premreženi polimer in kije ionsko kompleksirana z bazično aktivno snovjo, da se tvori ionski kompleks; pri čemer je ionski kompleks vdelan v hidrofilno erodirajočo matrico, ki obstoji iz derivatizirane celuloze.An oral pharmaceutical preparation for uniformly prolonged release of an ionizable active substance, characterized in that it comprises an ionizable basic active substance with a solubility greater than 10 mg / ml selected from the group consisting of metoprolol and terbutaline; a cation exchange resin which is a crosslinked polymer and which is ionically complexed with a basic active substance to form an ionic complex; wherein the ionic complex is embedded in a hydrophilic eroding matrix consisting of derivatized cellulose.
SI9111867A1990-12-071991-11-27New pharmaceutical formulations containing active ionizable substance as well as procedure for their preparation
SI9111867B
(en)
PREPARATION PROCESS OF PHARMACEUTICAL COMPOSITIONS COMPOSING AN EXTRAGRANULAR EXCIPIENT, INSOLUBLE HYGROSCOPE IN WATER AND AN ACTIVE INGREDIENT, IN PARTICULAR CIMETIDINE