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Solid dosage formulations of narcotic drugs having improved buccal adsorptionRelated Patent Categories: Drug, Bio-affecting And Body Treating Compositions, Identification Or Warning Feature, Printed Or Embossed Unitary Dosage FormSolid dosage formulations of narcotic drugs having improved buccal adsorption description/claimsThe Patent Description & Claims data below is from USPTO Patent Application 20070020186, Solid dosage formulations of narcotic drugs having improved buccal adsorption. Brief Patent Description - Full Patent Description - Patent Application Claims
[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 that adding a non-toxic amine to a buccal formulation, the penetration capacity of drugs is significantly improved, allowing to reach an higher and earlier blood concentration of drugs in comparison with formulations without amines. [0005] The amount of amine required in the formulation ranges between 0.1 to 500% of the moles of active component(s), more preferably 0.5 to 300% and most preferably 1 to 200%. [0006] Examples of amines used in order to improve bioavailability according to the invention include Histidine, Arginine, Lysine, Triethanolamine, Trimethylamine, Betaine, Pyrrolidine, Guanidine, Cysteamine, Taurine and derivatives and analogues thereof. Arginine is a preferred non-toxic amine. [0007] Examples of active components that may be advantageously formulated in solid dosage form according to the invention include: [0008] Alfentanil, Buprenorphine Butorphanol, Codeine, Diphenoxylate, Fentanyl, Heroin, Hydrocodone, Hydromorphone, Oxymorphone, Levophanol, Levallorphan, Loperamide, Meperidine, Morfine, Nalbuphine, Nalmefene, Nalorphine, Naloxone, Naltrexone, Remifentanyl, Sufentanil. Fentanyl is preferred. [0009] The invention is illustrated by the following Examples: 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 [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. Continue reading about Solid dosage formulations of narcotic drugs having improved buccal adsorption... Full patent description for Solid dosage formulations of narcotic drugs having improved buccal adsorption Brief Patent Description - Full Patent Description - Patent Application Claims Click on the above for other options relating to this Solid dosage formulations of narcotic drugs having improved buccal adsorption patent application. ###  How KEYWORD MONITOR works... a FREE service from FreshPatents1. Sign up (takes 30 seconds). 2. Fill in the keywords to be monitored. 3. Each week you receive an email with patent applications related to your keywords. Start now! - Receive info on patent apps like Solid dosage formulations of narcotic drugs having improved buccal adsorption or other areas of interest. ### Previous Patent Application: Pharmaceutical formulation containing irritant Next Patent Application: Solid dosage formulations of narcotic drugs having improved buccal adsorption Industry Class: Drug, bio-affecting and body treating compositions ### FreshPatents.com Support Thank you for viewing the Solid dosage formulations of narcotic drugs having improved buccal adsorption patent info. IP-related news and info Results in 0.1182 seconds Other interesting Feshpatents.com categories: Accenture , Agouron Pharmaceuticals , Amgen , AT&T , Bausch & Lomb , Callaway Golf 174 |
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