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Compositions and dosage forms for enhanced absorption of gabapentin and pregabalin

A technology of metformin and metformin base, which is applied in the field of metformin-releasing compositions, and can solve the problem of insufficiency

Inactive Publication Date: 2007-01-24
ALZA CORP
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

For example, the proposed Glucophage XR  As a once-daily formulation, but the time to release 90% of the dose in vitro is about 6 hours, far from the 15-20 hours proposed for the once-daily dosage form

Method used

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  • Compositions and dosage forms for enhanced absorption of gabapentin and pregabalin
  • Compositions and dosage forms for enhanced absorption of gabapentin and pregabalin
  • Compositions and dosage forms for enhanced absorption of gabapentin and pregabalin

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0079] A specific example of the steps used to prepare the metformin-transport moiety complex is provided in Example 1, using Figure 4C Description, wherein the transport part is a fatty acid. Metformin base was prepared from the hydrochloride salt using the ion exchange method. The fatty acid solution is contacted with metformin base in a solvent to reform the metformin-fatty acid complex.

[0080] In Example 1, complexes are formed with lauric acid as an exemplary fatty acid transport moiety. It is understood that lauric acid is exemplary only and that the procedure for its preparation is equally applicable to other substances suitable for use as transport moieties, as well as to fatty acids of any carbon chain length. For example, metformin forms complexes with various fatty acids or salts of fatty acids, the fatty acids having 6-18 carbon atoms, more preferably 8-16 carbon atoms, even more preferably 10-14 carbon atoms. Fatty acids or salts thereof may be saturated or ...

Embodiment 4

[0136] Example 4 describes similar Figure 11 Preparation of the dosage forms shown in .

[0137] Figure 12 is a schematic diagram of another exemplary osmotic dosage form. Such dosage forms are described in detail in US Patent Nos. 4,612,008, 5,082,668, and 5,091,190, which are incorporated herein by reference. Briefly, the dosage form 40 shown in cross-section has a semi-permeable wall 42 defining an interior compartment 44 . The inner compartment 44 contains a bilayer compressed core with a drug layer 46 and a push layer 48 . As will be described below, the pusher layer 48 is a displacement displacement composition placed in the dosage form, during use the pusher layer expands and the material forming the drug layer exits the dosage form through one or more outlets such as outlet 50 . The push layer can be placed in an alignment layer in contact with the drug layer, e.g. Figure 12 Alternatively, the push layer may have one or more intermediate layers separating the p...

Embodiment 2

[0185] In vivo colonic absorption using an oral gavage rat model

[0186] Eight rats were randomly divided into two treatment groups. After a 12-24 hour fast, the first group was orally gavaged with 40 mg / kg free base equivalents of metformin hydrochloride. A second group was orally gavaged with 40 mg / kg of the free base equivalent of metformin laurate complex prepared as described in Example 1. Blood samples were collected from the tail vein at 15 minutes, 30 minutes, 1 hour, 1.5 hours, 2 hours, 3 hours, 4 hours, 6 hours and 8 hours after oral gavage. Metformin plasma concentrations were analyzed by LC / MS / MS. The result is as Figure 7 shown in .

[0187] At the conclusion of the study, the rats were sacrificed and the gastrointestinal tract of the experimental animals was evaluated visually for signs of irritation. No stimulatory effect was observed in rats treated with the complex or metformin hydrochloride.

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Abstract

A complex comprised of metformin and a transport moiety, such as a fatty acid, is described. The complex has an enhanced absorption in the gastrointestinal tract, particularly the lower gastrointestinal tract. The complex, and compositions and dosage forms prepared using the complex, provide for absorption by the body of the drug through a period of ten to twenty-four hours, thus enabling a once-daily dosage form for metformin.

Description

field of invention [0001] The present invention relates to compositions and dosage forms for delivering metformin. In more detail, the present invention relates to complexes of metformin and a transport moiety, wherein the complex provides increased absorption of metformin in the gastrointestinal tract, more particularly in the lower gastrointestinal tract. Background of the invention [0002] The development of conventional pharmaceutical dosage forms is based on two aspects, one is to obtain a stable dosage form, and the other is to obtain a dosage form with maximum absorption in the upper gastrointestinal tract. Since most pharmaceutical dosage forms are designed for immediate drug release, dosage forms are designed to dissolve better in the upper gastrointestinal (G.I.) tract, which has a much greater surface area for drug absorption than the lower GI tract. The lower GI tract or colon lacks the microvilli present in the upper GI tract. The presence of microvilli great...

Claims

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Application Information

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IPC IPC(8): A61K9/00A61K9/20A61K31/155A61K31/20A61P3/10C07C279/00
Inventor 黄锡礼晏东G·V·圭塔
Owner ALZA CORP
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