Immediate release formulations of 1-aminocyclohexane compounds, memantine and neramexane

a technology of neramexane and memantine, which is applied in the direction of antiparasitic agents, biocides, drug compositions, etc., can solve the problems of not specifically revealing compositions containing memantine or neramexane, unpleasant taste of casein, etc., and achieve dose-proportional bioavailability and advantageous effects

Inactive Publication Date: 2006-01-05
FOREST LAB HLDG LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Benefits of technology

[0009] According to the present invention, it has now been found that 1-aminocyclohexanes, such as memantine (1-amino-3,5-dimethyladamantane) and neramexane (1-amino-1,3,3,5,5-pentamethylcyclohexane), and their salts, including the hydrochloride, hyd...

Problems solved by technology

However, casein has an unpleasant taste; it is associated with the undesirable effect of exacerbating some side effects as disclosed in U.S. Pat. No. 6,413,556; and displays instability in varying pH.
However, this patent does not speci...

Method used

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  • Immediate release formulations of 1-aminocyclohexane compounds, memantine and neramexane
  • Immediate release formulations of 1-aminocyclohexane compounds, memantine and neramexane
  • Immediate release formulations of 1-aminocyclohexane compounds, memantine and neramexane

Examples

Experimental program
Comparison scheme
Effect test

example 1

Preparation of Memantine HCl Immediate Release Tablets

[0212] The present example describes the process of developing memantine hydrochloride immediate release tablets in 2.5, 5, 10, 15, 20, 40, 60, and 80 mg dosages.

Materials and Methods

[0213] The following tables provide the makeup of immediate release tablets including the active components, coating agent, and other excipients for the specified dosage forms with specific target release time periods. Tables 1 and 2 provide the makeup of tablets with lactose and contain the same data expressed respectively in absolute (mg) or relative (% w / w) terms.

TABLE 12.5 mg to 80 mg Dose Proportional Formulations (with lactose / MCC)Component oringredient (mg)Content (mg)Memantine HCl2.55101520406080Microcrystalline13.0326.0552.1078.15104.20208.40312.60416.8CelluloseLactose Monohydrate43.6987.38174.75262.13349.50699.001048.501398.0Colloidal Silicone0.320.631.251.882.505.007.5010.0DioxideTalc2.795.5711.1516.7222.3044.6066.9089.2Magnesium Stea...

example 2

Pharmacokinetic Study of Memantine

[0233] The present example presents the bioavailability of immediate release memantine tablets as compared to modified release memantine tablets.

Materials and Methods

[0234] The study design in the present example was a 57-day single-center, open-label study in 24 young healthy subjects, ages ranging from 18 to 35 years old. Subjects underwent a screening evaluation consisting of a complete medical history, complete physical examination with vital signs, 12-lead ECG, clinical laboratory evaluations, consisting of a CBC (including differential), clinical chemistry, urinalysis, RPR / VDRL, Anti HIV 1 and 2 tests, drugs of abuse screen (including alcohol and nicotine), Anti-HCV and HbsAg. Female subjects had a β-hCG serum pregnancy test performed at screening and a urine pregnancy test on Day-1.

[0235] Inclusion criteria included informed consent, normal physical examination, healthy adults between 18 and 35 years of age, non-smokers, within 15% of ide...

example 3

Preparation of Memantine HCl 30-Minute Immediate Release Tablets

[0257] The present example demonstrates the makeup of 30-minute immediate release memantine tablets, with and without lactose monohydrate.

[0258] The methods of making the tablets are the same as those disclosed in Example 1. Specifically, the tablets are made of the following active components, coating agent, and other excipients as presented below in Tables 9 and 10. Tables 9 and 10, summarizing the tablets with lactose monohydrate, contain the same data expressed respectively in absolute (mg) or relative (% w / w) terms.

TABLE 930 min release tablets with lactose monohydrate / MCC(weights in mg / tablet)PreferredComponent / Ingredient (mg)RangesExact Composition (mg)Memantine HCl5.080.05.010.015.020.0Microcrystalline Cellulose23.4458.526.152.178.2104.2Lactose Monohydrate78.61537.987.4174.8262.1349.5Colloidal Silicone Dioxide0.611.10.61.31.92.5Talc5.098.05.611.216.722.3Magnesium Stearate0.36.50.40.81.11.5Hydroxypropyl3.466....

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Abstract

The present invention relates to an immediate release solid oral dosage form containing 1-aminocyclohexanes, preferably memantine or neramexane, and optionally a pharmaceutically acceptable coating, wherein the active ingredient exhibits dose proportionality and is released at a dissolution rate of more than about 80% within about the first 60 minutes following entry of said form into a use environment. The dosage form is direct compressed and has a hardness within the range of between about 3 and about 40 Kp, exhibits an average Tmax within the range of about 2 to about 8 hours with an active ingredient load within the range of about 2.5 to about 150 mg. The formulation allows for dose-proportional compositions for once daily or b.i.d. dosing, while maintaining a steady average range of Tmax.

Description

CROSS-REFERENCE TO RELATED APPLICATIONS [0001] This application claims priority under 35 U.S.C. § 119, based on U.S. Provisional Application Ser. No. 60 / 581,244 filed Jun. 17, 2004, and U.S. Provisional Application Ser. No. 60 / 636,899 filed Dec. 16, 2004, both of which are hereby incorporated by reference in their entirety.FIELD OF THE INVENTION [0002] The present invention is directed to pharmaceutical solid, oral dosage forms of compositions of 1-aminocyclohexane compounds which exhibit an immediate release profile, possess advantageous stability profiles and additionally disintegrate rapidly in aqueous solutions. The invention is particularly suitable for solid pharmaceutical dosage forms of 1-aminocyclohexane compounds in which a therapeutically effective amount of the active ingredient is available in the use environment shortly after administration. These compositions can be provided as dispersible tablets for administration as aqueous oral solution. In one embodiment, the act...

Claims

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Application Information

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IPC IPC(8): A61K9/20A61K31/13
CPCA61K9/2866A61K31/13A61K47/38A61K9/28A61K9/2846A61P1/16A61P25/00A61P25/04A61P25/08A61P25/16A61P25/24A61P25/28A61P27/06A61P31/14A61P33/06Y02A50/30
Inventor YANG, YANJANJIKHEL, RAJIVRAO, NIRANJANPERICLOU, ANTONIAABRAMOWITZ, WATTANAPORNDEDHIYA, MAHENDRA G.SEILLER, ERHARDHAUPTMEIER, BERNHARD
Owner FOREST LAB HLDG LTD
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