Controlled release formulations using intelligent polymers
a technology of intelligent polymers and formulations, applied in the field of controlled release formulations, can solve the problems of affecting the efficacy of osmotic and press coated tablets, the active ingredient is often not delivered in a consistent and reproducible manner, and the production cost is particularly high, so as to maintain the therapeutically effective blood level and good absorbability of the selected active ingredient.
a technology of intelligent polymers and formulations, applied in the field of controlled release formulations, can solve the problems of affecting the efficacy of osmotic and press coated tablets, the active ingredient is often not delivered in a consistent and reproducible manner, and the production cost is particularly high, so as to maintain the therapeutically effective blood level and good absorbability of the selected active ingredient.
US20050214368A1Inactive Publication Date: 2005-09-29BIOVAIL LAB INT SRL
Examples
Experimental program
Comparison scheme
Effect test
example 1
ER 5 mg
[0047]
% compositionGlipizide1.83Hydroxypropyl methylcellulose20Ethylcellulose16.17Hydroxyethylcellulose4Lactose30Microcrystalline cellulose23Silicone dioxide0.6Sodium Lauryl sulfate4Magnesium stearate0.4
example 2
Hydrochloride ER 60 mg
[0048]
% compositionDiltiazem hydrochloride58.82Hydroxypropyl methylcellulose5Ethylcellulose5Hydroxyethylcellulose15Lactose5Microcrystalline cellulose9.18Talc1Magnesium stearate1
example 3
e ER 60 mg
[0049]
% compositionNifedipine20Hydroxypropyl methylcellulose20Ethylcellulose29Hydroxyethylcellulose3.8Lactose14Microcrystalline cellulose10Silicone dioxide1.2Na lauryl sulfate1Magnesium stearate1
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Abstract
A controlled release pharmaceutical composition comprises (a) at least one pharmaceutically active substance having a water contact angle (θ) such that cos θ is between +0.9848 and −0.9848, (b) a first intelligent polymer component; and (c) a second intelligent polymer component having opposite wettability characteristics to the first intelligent polymer component, the first and second polymer components being present in a ratio in the range of about 1:100 to about 100:1 by weight. The polymer components are effective for controlled release of the pharmaceutically active substance from the composition.
Description
FIELD OF THE INVENTION [0001] The present invention is directed to novel controlled release formulations of pharmaceutically active substances and methods for their preparation. More particularly, the present invention relates to an easily absorbable, controlled release pharmaceutical formulation utilizing groups of intelligent polymers having opposing wettability characteristics. BACKGROUND OF THE INVENTION [0002] Controlled release formulations of pharmaceutical agents is an extremely large market in the pharmaceutical and medical fields. A number of types of controlled release dosage forms are known, including matrix tablet systems incorporating active ingredients, fillers and various types of excipients. The very different properties of numerous different types of pharmaceutically active ingredients has necessitated the development of a number of different drug delivery systems utilizing polymer technology in order to provide an appropriate release of a particular medicament aft...
Claims
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Patent Timeline
29 Sep 2005
Publication
US20050214368A1
- IPC
- A61K9/14; A61K9/20; A61K9/22; A61K9/28; A61K31/716
- CPC
- A61K9/2054; A61K31/716; A61K9/2846; A61K9/2077
- Inventors
- KAWAKAMI, YUKICHIKA; SATO, NOBUO