Solid dosage formulations of narcotic drugs having improved buccal adsorption

Inactive Publication Date: 2007-01-25
ALPEX PHARMA SA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Benefits of technology

[0023] Despite the dose of Fentanyl administered in the tablets described in example # 1A (200 mcg) is 50% of the dose described in example #1B (400 mcg), the pharmacokinetic parameters are similar, demonstrating a dramatic improvement of the Fentanyl bioavailability for the formulation of the invention.

Problems solved by technology

Sometimes, buccal administration does not unfortunately always allow to obtain a fast onset of action of the drug, as the result of difficulties of the drug to cross the skin barrier of mucosa and to penetrate into the blood stream.

Method used

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Examples

Experimental program
Comparison scheme
Effect test

example # 1

EXAMPLE #1

Example #1A

[0010] Preparation of a Oral Dispersible Tablet Containing Amine (Arginine)

[0011] Oral dispersible tablets containing 200 mcg of Fentanyl were obtained as follows:

[0012] A) 1.05 g of Fentanyl and 50 g of PEG 600 were dissolved into 90 g of purified water.

[0013] B) 335.62 g of Sorbitol, 516.67 g of Mannitol, 26.67 g of aspartame and 10 g of Citric acid, were granulated together with a water solution containing PEG and Fentanyl citrate.

[0014] C) At the end of granulation and drying, 43.33 g of arginine free base and 16.67 g of magnesium stearate were added.

[0015] D) The product was blended until homogeneity and compressed in toroidal tablets having a diameter of 10 mm and weighing 300 mg each

example # 1b

Example #1B

[0016] Preparation of an Oral Dispersable Tablet without Amine (Arginine)

[0017] Oral dispersible tablets containing 400 mcg of Fentanyl have been obtained as follows:

[0018] E) 2.1 g of Fentanyl and 50 g of PEG 600 was dissolved into 90 g of purified water.

[0019] F) 455.62 g of Sorbitol, 455.62 g of Mannitol, 26.67 g of aspartame and 10 g of Citric acid, were granulated together with a water solution containing PEG and Fentanyl citrate.

[0020] G) The product was blended until homogeneity and compressed in toroidal tablets having a diameter of 10 mm and weighing 300 mg each

example # 2

[0021] A pharmacokinetic study was carried out on 6 fasting healthy volunteers treated with a buccal formulation prepared in accordance with example # 1A containing 200 mcg of Fentanyl. The results were compared with a pharmacokinetic study carried out on 6 healthy volunteers treated with a buccal formulation prepared in accordance with example # 1B containing 400 mcg of Fentanyl.

[0022] The results are reported in the following Table:

Fentanylstrength perdosageTmaxCmaxAUCExample # 1A200 mcg48 minutes496 pg / mL2430Example # 1B400 mcg35 minutes491 pg / mL3331

[0023] Despite the dose of Fentanyl administered in the tablets described in example # 1A (200 mcg) is 50% of the dose described in example #1B (400 mcg), the pharmacokinetic parameters are similar, demonstrating a dramatic improvement of the Fentanyl bioavailability for the formulation of the invention.

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Abstract

The present invention provides solid dosage formulations of narcotic drugs with improved buccal adsorption. These improved characteristics are provided by the combination of the narcotic drug with an additional non-toxic soluble organic compound. The soluble organic compound contains a primary, secondary or tertiary amine group. The addition of this organic compound favorably alters the kinetics of mucosal penetration such that mucosal penetration times are decreased. This provides for a faster onset of action of the drug.

Description

[0001] The present invention concerns solid dosage formulations of narcotic drugs having improved buccal adsorption. [0002] The formulations of the invention are characterized by the introduction in a buccal formulation of a soluble organic compound having a primary, secondary or tertiary amine group. BACKGROUND OF THE INVENTION [0003] Buccal formulations are more and more popular for drug administrations. They exhibit in fact several advantages in comparison with other solid dosage forms; in particular, buccal formulations dissolve in the oral cavity without requiring water for ingestion, allowing the buccal adsorption of drugs coming into contact with the oral mucosa in dissolved form. Sometimes, buccal administration does not unfortunately always allow to obtain a fast onset of action of the drug, as the result of difficulties of the drug to cross the skin barrier of mucosa and to penetrate into the blood stream.DESCRIPTION OF THE INVENTION [0004] Surprisingly, it has been found ...

Claims

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Application Information

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IPC IPC(8): A61K31/485A61K9/44A61K31/445A61K9/20
CPCA61K9/0056A61K47/183A61K47/18A61K31/4468A61K9/2013A61P23/00A61P25/04A61P29/00A61K9/20A61K47/16
Inventor STROPPOLO, FEDERICOARDALAN, SHAHBAZ
Owner ALPEX PHARMA SA
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