Sulfoalkyl ether cyclodextrin based controlled release solid pharmaceutical formulations

A technology of solid pharmaceutical preparations and sulfoalkyl ethers, which is applied in the field of controlled-release solid pharmaceutical preparations and can solve problems such as the complexity of the preparation process

Inactive Publication Date: 2002-09-18
CYDEX PHARMACEUTICALS INC
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

The steps involved in the methods of preparing such formulations require many monitoring and controlling processes and thus complicate the formulation process

Method used

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  • Sulfoalkyl ether cyclodextrin based controlled release solid pharmaceutical formulations
  • Sulfoalkyl ether cyclodextrin based controlled release solid pharmaceutical formulations
  • Sulfoalkyl ether cyclodextrin based controlled release solid pharmaceutical formulations

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 8

[0146] Example 8 details a method of preparing an exemplary embodiment of a multilayer tablet according to the present invention comprising at least one immediate release layer adjacent to a controlled release layer. Figure 23a Depicted is a bilayer tablet (1) comprising an immediate release layer (3) containing the major amount of drug and SAE-CD present together in a physical mixture, and a controlled release layer (2), and an immediate release layer (3) The matrix, while the controlled release layer contains a physical mixture of the main amount of drug, SAE-CD and release rate modifier. The immediate release layer disintegrates and releases the drug in the environment immediately after administration to the patient or addition of the tablet to the dissolution medium. Figure 23b depicts a three-layer tablet in which a controlled release layer (6) prepared as in Example 8 is sandwiched between two rapid release layers (5a, 5b) prepared as described in Example 8. It should ...

Embodiment 11

[0153] Example 11 describes the preparation of an osmotic pump that releases testosterone (TS) into an environment of use through a combination of diffusion and osmosis. Figure 25 TS, sugar, hydroxypropyl-β-cyclodextrin (HP-β-CD) and (SBE) are depicted 7m - Comparative profiles of β-CD release from various osmotic pump formulations. The first formulation contained a physical mixture of TS(○) and a sugar mixture (●, lactose and fructose, 1:1); the second formulation contained TS(□) and (SBE) 7m -β-CD (■); while the third formulation contained TS (◇) and HP-β-CD (◆). The results showed that, compared with osmotic pumps containing sugar mixture or HP-β-CD, containing (SBE) 7m -Osmotic pumps for β-CD released greater amounts of TS at a more acceptable rate.

[0154] The advantageous properties of the present formulation allow the preparation of drug release devices with combined and controlled diffusion and osmotic release of drug. These devices can be prepared by varying the...

Embodiment 1

[0218] Testosterone-(SBE) 7 -β-CD sustained release formulation

[0219] This example demonstrates the application of the present invention in the preparation of sustained-release preparations, wherein the pharmacologically active agent is testosterone as an example. Phase Solubility Studies

[0220] Add excess testosterone in 0.25ml of (SBE) 7 - In β-CD solution, the concentration range is 0.0-0.05 mmol / l. The dispersion was equilibrated for at least 24 hours in a shaking water bath (100 rpm, 25°C). The dispersion was centrifuged at 2500 rpm for 10 minutes, and 20 μl of the supernatant was sampled with an airtight 100 μl syringe (Hamilton Co., NV), diluted with mobile phase, and then analyzed for testosterone concentration in the solution by HPLC. With Higuchi and Connors for A L Testosterone-(SBE) by Type Diagram Method 7 -β-CD binding constant K 1∶1 . Preparation of tablet cores

[0221] With a 1:1 molar ratio of testosterone / (SBE) 7 - β-CD Preparation of...

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Abstract

The invention provides a controlled-release pharmaceutical preparation based on sulfoalkyl ether cyclodextrin (SAE-CD). The solid pharmaceutical formulations of the present invention consist of a core comprising one or more SAE-CD derivatives, optionally a release rate modifying agent, a therapeutic agent, and optionally a release rate modifying coating surrounding the core. Some therapeutic agents were not complexed with SAE-CD. The formulations of the present invention are easier to prepare than other SAE-CD based formulations, but still provide similar or better potency. SAE-CD is used to increase the bioavailability and/or bioabsorption rate of therapeutic agents. Also disclosed are multilayer dosage forms, osmotic pumps, coated and uncoated tablets, minitablets, pills, micropellets, granules, and powders.

Description

field of invention [0001] The present invention relates to cyclodextrin-based controlled-release solid pharmaceutical preparations. More specifically, the present invention relates to sulfoalkyl ether cyclodextrin (SAE-CD) based controlled release formulations in which most of the therapeutic agent is not complexed with the SAE-CD. Background of the invention [0002] Cyclodextrin / drug complexes are usually formed before their use in pharmaceutical formulations. US Patent No. 5,134,127 to Stella et al. (the '127 patent) relates to sulfoalkyl ether cyclodextrin (SAE-CD) derivatives. The use of SAE-CD derivatives as solubilizers for poorly water-soluble or water-insoluble drugs has been proposed in various pharmaceutical dosage forms. The '127 patent relates to compositions and formulations comprising drugs complexed with SAE-CD derivatives, wherein clathrate / drug complexes are formed or complexes are included. The pharmaceutical formulations envisaged therein relate to tho...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/00A61K9/16A61K9/20A61K9/22A61K9/24A61K9/26A61K9/28A61K9/32A61K9/50A61K9/54A61K9/58A61K31/573A61K47/40A61P5/40C08B37/16
CPCA61K9/205A61K9/2059A61K9/209A61K9/2826A61K9/2846A61K9/2853A61K9/2866A61K9/4808A61K47/40B82Y5/00A61K47/6951A61P5/40A61K9/20
Inventor 瓦伦蒂诺·J·斯特拉罗杰·A·拉耶夫斯基文卡特拉曼娜·M·拉奥詹姆斯·W·麦金尼蒂格罗尔德·L·莫舍
Owner CYDEX PHARMACEUTICALS INC
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