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Quickly soluble oral film dosage containing steviosides as a unpleasant taste masking agent

Inactive Publication Date: 2012-06-21
CHA BIOTECH
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Benefits of technology

[0011]The present inventors have made efforts to overcome the foregoing shortcomings and found that use of at least one selected from a group consisting of aspartame, acesulfame potassium, sucralose and neotame together with stevioside and / or its derivative can mask a bitter and / or nasty taste even without substantially altering a process of preparing an oral film dosage.
[0012]In other words, in order to solve conventional problems and to develop an improved quickly soluble oral film dosage containing active ingredients as the most preferable formulation, a great deal of studies and investigation have been conducted by the present inventors. As a result, they found that the bitter and / or nasty taste may be efficiently masked without additional coating processes if stevioside and / or derivatives thereof having a strong sweet aftertaste among high potency sweeteners are used together with any typical high potency sweetener, and then, completed the present invention.
[0013]Accordingly, it is an object of the present invention to provide a quickly soluble oral film dosage including a therapeutically effective amount of active pharmaceutical ingredient, stevioside and / or its derivative, at least one high potency sweetener, a film forming agent, and at least one of pharmaceutically available additives.
[0014]Another object of the present invention is to provide a quickly soluble oral film dosage capable of efficiently masking a nasty taste caused by a therapeutically effective amount of active pharmaceutical ingredient and, in addition, being promptly dissolved in an oral cavity.
[0016]The proposed oral film dosage has excellent effects of masking a nasty taste and may be easily prepared by a simple process at low cost, thereby being preferably used in various applications such as an oral cleanser, a bad breath remover, a carrier for a nutrient supplementary agent, and a tongue soluble formulation enabling absorption of drugs in the oral cavity as well as the stomach and bowels, and so forth.

Problems solved by technology

Especially, since they have difficulties in swallowing typical tablets or capsules, an alternative oral dosage formulation for aged persons may be required.
However, such liquid formulation has disadvantages such as deteriorated stability and incorrect dosage.
However, a film formulation easily dissolved in an oral cavity enables a drug to be absorbed in the oral mucosa, causing a bitter or nasty taste of the drug during absorption.
However, the ion-exchange resin contained in a water-soluble polymer may cause scratches during forming and require a complicated processing.
However, sodium hydrocarbonate has limitations in masking a strong bitter taste.
However, the foregoing film formulation is prepared by a complicated method for considerably preventing absorption of the formulation to the oral mucosa and may not provide beneficial effects for protection of the stomach and bowels.
Such coating process may complicate the preparation of film.

Method used

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  • Quickly soluble oral film dosage containing steviosides as a unpleasant taste masking agent
  • Quickly soluble oral film dosage containing steviosides as a unpleasant taste masking agent
  • Quickly soluble oral film dosage containing steviosides as a unpleasant taste masking agent

Examples

Experimental program
Comparison scheme
Effect test

example 14

[0093]Ondansetron based quickly soluble film prepared according to Example 9 of the present invention was subjected to dissolution experiments at pH 1.2 in comparison with a conventional product named Zofran Zydis tablet containing ondansetron available from GlaxoSmithKline Co. (CSK) based on Notice of the Food and Drug Administration and the experimental results are shown in FIG. 1. As shown in the accompanying drawings, there was no substantial difference in elution between both of the formulations.

example 15

[0094]Ondansetron based quickly soluble film prepared according to Example 9 of the present invention was subjected to pharmacokinetic tests in comparison with a conventional product named Zofran® Zydis tablet containing ondansetron available from GlaxoSmithKline Co. (GSK). The experiments is conducted for healthy fourteen (14) adult men and women with Latin square method based on Notice of bioequivalence test standard of the Food and Drug Administration.

[0095]The experimental results are shown in Table 9 and FIG. 2. It was confirmed that the inventive film of this example has the bioequivalence as shown in Table 9 and FIG. 2.

TABLE 9Pharmacokinetic test result of ondansetron film formulationsParameterGroup 1Group 2AUCO~24(ng · hr / mL)244.78 ± 91.83 259.64 ± 87.10Cmax(ng / mL)30.93 ± 10.7133.16 ± 8.89Tmax(hr)1.86 ± 0.71 1.94 ± 0.75Note 1)Group 1 is Ondansetron film formulations (8 mg). Group 2 is Zorfran ®Zydis ODTs

example 16 to 20

[0096]As active pharmaceutical ingredients, sildenafil free base, sildenafil lactate, sildenafil citrate, granisetron, and montelukast sodium were added to prepare films having constitutional compositions shown in the following Table 10. The sensory test was randomly conducted and test results were that unpleasant aftertaste was well masked.

TABLE 10Exam-Exam-Exam-Exam-Exam-ple 15ple 16ple 17ple 18ple 19Ingredient(wt. %)(wt. %)(wt. %)(wt. %)(wt. %)Sucralose1.7221.50.5Neotame120Acesulfame0.50.510.5potassiumRebaten 97%22220.5Citric acid0.20.20.20.60.6Hydroxypropyl22232starchSpan200.10.50.10.40.4Menthol0.42.30.333Carageenan0.10.10.10.10.2Pigment0.10.10.10.10.1Polysorbate 800.40.50.30.30.3Peppermint oil0.82.70.633Pullulan62.377.555.181.578.9Microcrystalline1.41.40.71.54celluloseBeta0.7cyclodextrinLemon flavor220.81.51.5Sildenafil25free baseSildenafil4.2lactateSildenafil35citrateGranisetron1hydrochlorideMontelukast5sodiumTotal weight100.0100.0100.0100.0100.0

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Abstract

Disclosed is a quickly soluble oral film dosage for masking a nasty taste, in particular, a quickly soluble oral film dosage comprising a stevioside based sweetener and a high potency sweetener in a ratio by weight (w / w) of 1:3 to 3:1, which may efficiently mask a bitter or nasty taste of a medicine and may be quickly dissolved in a mouth without water, thereby improving an aftertaste thereof thus enhancing dosage acceptability of a patient.

Description

BACKGROUND OF THE INVENTION[0001]This application claims priority to Korean Patent Application No. 10-2009-0057276, filed on Jun. 25, 2009 and Korean Patent No. 10-2010-0057450, filed on Jun. 17, 2010, in the Korean Intellectual Property Office, the entire contents of which are hereby incorporated by reference.FIELD OF THE INVENTION[0002]The present invention relates to a quickly soluble oral film dosage for effectively masking a unpleasant taste and, more particularly, to a quickly soluble oral film dosage comprising a stevioside based sweetener and a high potency sweetener in a ratio by weight (w / w) of 1:3 to 3:1, which may efficiently mask a bitter or nasty taste of a medicine and may be quickly dissolved in a mouth without water, thereby improving an aftertaste thereof thus enhancing dosage acceptability of a patient.BACKGROUND OF THE RELATED ART[0003]A social distribution ratio of aged population has currently increased owing to an extended span of human life. Old people genera...

Claims

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Application Information

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IPC IPC(8): A61K39/00A23L27/30
CPCA61K9/0056A61K9/006A61K47/36A61K31/09A61K31/14A61K9/7007A61P1/02A61P43/00
Inventor PARK, JIN-KYUYANG, WON-SUKJUNG, KYOUNG TAE
Owner CHA BIOTECH
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