Compositions and methods for enhancing transmucosal delivery

A composition, oral mucosa technology, applied in the directions of drug combination, drug delivery, pill delivery, etc., can solve problems such as unsatisfactory

Inactive Publication Date: 2010-06-23
DERMA YOUNG LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Specifically, effective rapid delivery of analgesics, anti-inflammatory drugs, drugs for erectile dysfunction, for migraines, or for menopausal symptoms; There is an unmet need for the delivery of active agents for obesity or eating disorders

Method used

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  • Compositions and methods for enhancing transmucosal delivery

Examples

Experimental program
Comparison scheme
Effect test

preparation example Construction

[0142] Preparation of the composition of the present invention

[0143]Exemplary solid forms for oromucosal (eg, sublingual and buccal) administration include films, dispersible fluid or semisolid compositions, and solid forms. Solid dosage forms intended for distribution on or over the oral mucosa may conveniently be presented in the form of hard candies or chewable confectionaries. Other forms may include tablets, pills, capsules, powders, and granulated materials for dispersion in the oral cavity. These solid compositions may include pharmaceutically acceptable inert ingredients such as diluents (such as calcium carbonate, sodium chloride, lactose, calcium phosphate, sodium phosphate, and similar diluents); granulating agents and disintegrants (such as potato starch, Alginic acid and similar granulating and disintegrating agents); Binders (such as starch, gelatin, acacia and similar binders); Lubricants (such as magnesium stearate, stearic acid, talc and similar lubrican...

Embodiment 1

[0181] Example 1. Preparation of compositions containing DL-phenylalanine

[0182] A soft buccal dosage formulation was prepared in the form of chocolate chips, each weighing 3 grams.

[0183] Each tablet contains:

[0184] DL-Phenylalanine 150mg

[0185] Methylsulfonylmethane (MSM) 100mg

[0186] Vegetable Oil 30%

[0187] Cocoa Butter 30%

[0188] Sucralose 0.1%

[0189] Calcium Carbonate 10%

[0190] Lecithin 10%, and

[0191] Add purified water to 100%.

[0192] The method for preparing said composition comprises the following steps:

[0193] Step 1: Pour 20ml of deionized water into the homogenization system and heat to a temperature of 50°C.

[0194] Step 2: Add MSM to water and homogenize well.

[0195] Step 3: Add phenylalanine to water and homogenize well.

[0196] Step 4: Add the sucralose to the water and homogenize well.

[0197] Step 5: Mix the ingredients well for 30 minutes to produce Solution A.

[0198] Step 6: Add lecithin to solution A and mix w...

Embodiment 2

[0203] Example 2. Comparison of the bioavailability of formulations containing DL-phenylalanine in the presence or absence of methylsulfonylmethane (MSM)

[0204] Tablets prepared by the method described in Example 1 were administered to three healthy adult male subjects at a dose of 450 mg DL-phenylalanine per subject in the oral cavity between the gum and the cheek. (A) MSM-free formulation, 60 second retention time (intraoral); (B) MSM-containing formulation, 30-second retention time (intraoral); and (C) MSM-containing formulation, 60-second retention time (intraoral). These subjects fasted from 12 hours before administration until the end of the test.

[0205] Blood samples (3 ml) were taken before administration and 20, 40, 60 and 80 minutes after administration of the formulation. The determination of DL-phenylalanine in blood was carried out according to the following analytical method.

[0206] After separation of blood, plasma was stored at -20°C until chemical ana...

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Abstract

The present invention provides transmucosal pharmaceutical or nutraceutical compositions and methods for enhancing transmucosal delivery of pharmaceutical and nutraceutical ingredients through use of methylsulfonylmethane (MSM) as a transmucosal delivery enhancer. In particular, the invention provides transmucosal compositions comprising an active agent selected from a non-steroid anti-inflammatory drug (NSAID); an analgesic; a migraine medication; a menopause medication; a sleep disorder medication; an erectile dysfunction medication, an appetite suppressant, a vitamin, a food supplement and a macromolecule. In certain particular exemplary formulations the appetite suppressant is DL-phenylalanine, and the vitamin is B12.

Description

field of invention [0001] The present invention relates to compositions and methods for transmucosal delivery of pharmaceutical agents, including macromolecular compounds, and nutraceutical ingredients. The present invention includes the use of methylsulfonylmethane as a transmucosal delivery enhancer. Background of the invention [0002] Drug delivery via the oral mucosa [0003] Drugs taken orally and swallowed are first absorbed into the blood perfusing the gastrointestinal (GI) tract. Venous drainage from the GI tract is first delivered to the blood that perfuses the liver. This means that drugs absorbed from the lumen of the gastrointestinal tract are immediately delivered to the liver - the main detoxification organ in the body. In addition to protecting the organism from ingestion of toxins, the liver metabolizes drugs so that they can be inactivated by first-pass metabolism in the liver. Liver blood then returns to the left side of the heart via the hepatic port...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/70
CPCA61K47/20A61K9/006A61K9/2068A61P3/02A61P3/04A61P15/10A61P15/12A61P25/04A61P25/06A61P25/20A61P29/00A61K31/10A61K31/192A61K47/44
Inventor 约瑟夫·鲁宾斯坦
Owner DERMA YOUNG LTD
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