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Hydrogel-driven drug dosage form

A pharmaceutical dosage form and dosage form technology, which is applied in the field of hydrogel-driven pharmaceutical dosage forms, can solve the problems of increasing the dosage form of drugs, and achieve rapid delivery and good effect

Inactive Publication Date: 2003-12-10
PFIZER PRODS ETAT DE CONNECTICUT
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0010] Nevertheless, the prior art still needs a controlled-release dosage form, which can efficiently release the drug into the use environment with little residual drug; can increase the dose of the drug and reduce the size of the dosage form; immediately after entering the use environment Initiate drug release; and limit the amount of necessary ingredients

Method used

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  • Hydrogel-driven drug dosage form
  • Hydrogel-driven drug dosage form
  • Hydrogel-driven drug dosage form

Examples

Experimental program
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preparation example Construction

[0097] After the preparation of the core 12, the coating 18 process is carried out. The coating 18 should not only have high enough water permeability to release the drug within the desired time, but also have high strength and be relatively easy to prepare. Water permeability controls the rate at which water enters the core, thereby controlling the rate at which the drug is released into the environment of use. If high doses of low solubility drugs are required, the combination of low solubility and high doses requires a highly permeable coating to achieve drug release while maintaining an appropriate dosage form size. The need for high strength is to ensure that the coating will not be damaged when the core is wetted and swelled, resulting in uncontrolled release of the drug. Application of the coating should be relatively easy. Furthermore, the coating should be insoluble and non-erodible during release of the drug-containing composition, i.e., the coating should be suffi...

Embodiment 1

[0117] The three-layer geometry of a typical dosage form of the invention is depicted in Figure 1 of the accompanying drawings. The composition of the three-layer core is that the drug-containing composition is uniformly distributed on the top and bottom of the tablet layer and the water-swellable composition is contained in the middle layer.

[0118] To form the medicated composition, the following was wet granulated (see Table A): 35% by weight of 1-[4-ethoxy(6,7-dihydroxy-1-methyl-7-oxo-3-propane Base-1H-pyrazolino[4,3-d]pyrimidin-5-yl)benzenesulfonyl]-4-methylpiperazine citrate, also known as sildenafil (sildenafil) citrate ( Herein referred to as drug 1) with a solubility of about 20 g / ml at pH=6, 30 wt% xylitol (commercial name XYLITAB200), 29 wt% PEO with an average molecular weight of 600,000 Daltons, 5 wt% sodium starch glycolate (commercial name EXPLOTAB), and 1 wt% magnesium stearate. The ingredients of the drug-containing composition, in the absence of magnesium ...

Embodiment 2A-2D

[0126] These examples describe the release of different drugs of the invention from three-layer tablets. For the tablet of Example 2A, the drug-containing composition contains 28 wt% of sertraline hydrochloride (drug 2), the solubility of which is about 0.2 mg / ml at pH=7, 37 wt% of XYLITAB 200, and an average molecular weight of 29 wt% 600,000 Daltons of PEO, 5 wt% of EXPLOTAB, and 1 wt% of magnesium stearate. The ingredients of the medicinal composition, except the magnesium stearate, are first mixed in a TURBULA mixer for 20 minutes. Next, grind with a hammer mill and pass through a 0.065-inch screen. The materials were mixed for an additional 20 minutes in the TURBULA mixer. Additional magnesium stearate was added and mixing continued for 4 minutes.

[0127] To prepare the water-swellable composition, the following materials were mixed: 72.5% by weight of EXPLOTAB, 25% by weight of microcrystalline cellulose (AVICEL PH102), and 2.5% by weight of magnesium stearate. The ...

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Abstract

A controlled release dosage form has a coated core with the core comprising a drug-containing composition and a water-swellable composition, each occupying separate regions within the core. The coating around the core is water-permeable, water-insoluble and has at least one delivery port therethrough. A variety of geometric arrangements are disclosed.

Description

Background of the invention [0001] The present invention relates to a dosage form for controlled release of an effective agent or drug into the environment of use. [0002] Osmotic and hydrogel-driven drug release designs are known in the art. Typical pharmaceutical dosage forms include the following: a tablet, which contains a semi-permeable wall surrounding the drug unit and a swellable hydrogel layer, wherein the release of the drug is through the swelling of the hydrogel Completed by channels in a permeable wall, as described in US Patent 4,327,725; another tablet consists of a liquid-permeable but drug-impermeable wall surrounded by a cell containing two osmotic agents, two swelling polymers and drugs, as described in US Patent 4612008; a drug dispersed in a swellable hydrogel matrix core, which releases the drug into the use environment by diffusion, as described in US Patent 4624848; hydrogel units of stable pellets, each with a wall surrounding a drug core, as descri...

Claims

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Application Information

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IPC IPC(8): A61K9/00A61K9/20A61K9/22A61K9/24A61K31/135A61K31/353A61K31/4178A61K31/4422A61K31/496A61K31/519A61K31/5377A61K47/02A61K47/10A61K47/12A61K47/16A61K47/26A61K47/30A61K47/34A61K47/36A61K47/38A61K47/42
CPCA61K9/2077A61K9/0004A61K9/2086A61K9/209A61K9/20
Inventor 利厄·E·阿佩尔沃尔特·C·巴布科克罗纳德·A·拜尔林克马克·B·奇德劳威廉·J·柯拉托洛德韦恩·T·弗里森斯科特·M·赫比格阿维纳什·G·托姆布里
Owner PFIZER PRODS ETAT DE CONNECTICUT
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