Source: http://www.google.com/patents/US7727552?dq=5,838,906
Timestamp: 2016-09-29 01:39:04
Document Index: 552110478

Matched Legal Cases: ['Application No. 01', 'Application No. 01', 'Application No. 01', 'Application No. 01', 'Application No. 01', 'Application No. 01']

Patent US7727552 - Oral pharmaceutical preparations decreased in bitterness by masking - Google PatentsSearch Images Maps Play YouTube News Gmail Drive More »Sign inPatentsA composition of an oral medicine or an oral medicine which can prevent an unpleasant taste of the medicine is herein disclosed. It is granules, powders, syrups and the like which is prevented from an unpleasant taste, comprising a basic medicine having an unpleasant taste and an anionic polymer such...http://www.google.com/patents/US7727552?utm_source=gb-gplus-sharePatent US7727552 - Oral pharmaceutical preparations decreased in bitterness by maskingAdvanced Patent SearchTry the new Google Patents, with machine-classified Google Scholar results, and Japanese and South Korean patents.Publication numberUS7727552 B1Publication typeGrantApplication numberUS 09/380,310PCT numberPCT/JP1998/001360Publication dateJun 1, 2010Filing dateMar 26, 1998Priority dateMar 28, 1997Fee statusPaidAlso published asDE69836207D1, DE69836207T2, EP0974366A1, EP0974366A4, EP0974366B1, WO1998043675A1Publication number09380310, 380310, PCT/1998/1360, PCT/JP/1998/001360, PCT/JP/1998/01360, PCT/JP/98/001360, PCT/JP/98/01360, PCT/JP1998/001360, PCT/JP1998/01360, PCT/JP1998001360, PCT/JP199801360, PCT/JP98/001360, PCT/JP98/01360, PCT/JP98001360, PCT/JP9801360, US 7727552 B1, US 7727552B1, US-B1-7727552, US7727552 B1, US7727552B1InventorsKoji Ukai, Tsutomu Hrada, Yasuyuki SuzukiOriginal AssigneeEisai R&D Management Co., Ltd.Export CitationBiBTeX, EndNote, RefManPatent Citations (60), Non-Patent Citations (18), Referenced by (8), Classifications (23), Legal Events (3) External Links: USPTO, USPTO Assignment, EspacenetOral pharmaceutical preparations decreased in bitterness by masking
US 7727552 B1Abstract
A composition of an oral medicine or an oral medicine which can prevent an unpleasant taste of the medicine is herein disclosed. It is granules, powders, syrups and the like which is prevented from an unpleasant taste, comprising a basic medicine having an unpleasant taste and an anionic polymer such as carrageenan.
For masking a medicine having an unpleasant taste, a lot of techniques have been developed. For example, there is known a method for coating a granulated agent with a water-soluble film (JP-A 4-282312), and a method for obtaining a powder and the like by melting a waxy substance having a melting point in the range of 40 to 100� C. wherein a medicine having an unpleasant taste is allowed to be dispersed and then solidified (JP-A 7-267850). On the other hand, for liquids, in order to improve the feeling of taking medicine, there is known a method to use liquids on oral administration such as syrups, which is widely used as a dosage form suitable for infants, aged people, etc. Although syrup is a dosage form with a sweet taste, when a melted medicine has an unpleasant taste, it is difficult to administer it, because a mere sweet taste cannot prevent an unpleasant taste, and in addition, compliance of a patient is lowered. Moreover, in JP-A 4-346937, as a method for reducing a bitter taste, there has been disclosed a method for reducing a bitter taste which comprises the step of adding a gelling agent selected from agar, gelatin or κ-carrageenan, and a seasoning agent to a substance having a bitter taste, so that a jelly state for seasoning is obtained. This method reduces a contact of a bitter taste substance with a tongue by making a jelly state, and a partly melted bitter taste substance masks a bitter taste by the use a seasoning agent.
2 mg/ml of an aqueous donepezil hydrochloride solution was prepared. After 50 mg of κ-carrageenan, chondroitin sulfate or dextran sulfate was dissolved in 5 ml of the aqueous solution. Afterward, two examinees (which were represented by A and B in Table 1) hold the whole amount of the solution in their mouths, and then evaluated the degree of a bitter taste and numbness in accordance with five grades. The results are shown in Table 1.
By the use of ticlopidine hydrochloride (20 mg/ml), maprotiline hydrochloride (5 mg/ml) and iphenprodil tartaric acid (4 mg/ml), an effect of carrageenan preventing a bitter taste and numbness was examined. A method of examination and a standard of evaluation were based on Test 1. The results are shown in Table 2.
Sodium alginate, sodium chondroitin sulfate, K carrageenan, 1-carrageenan, mannitol, cornstarch, copolyvidon and the like were blended with (RS)-1-(isopropoxycarbonyloxy)ethyl(+)-(6R,7R)-7{(z)-2-(2-aminothiazole-4-yl)-2-hydroxyiminoacetamide}-3-N,N-dimethylcarbamoyloxymethyl-8-oxo-5-thia-1-azabicyclo-[4.2.0]octo-2-en-2-carboxylate hydrochloride salt (which was shown as a compound A in Table 3) in ratios shown in Table 2, and granules were prepared in accordance with the method of Example 3. The test was carried out by three examinees holding 0.5 g of each granule for examination in their mouths, and the judgment was done by an evaluation standard of seven grades shown as follows.
According to the treatment shown in Table 4, ticlopidine hydrochloride, κ-carrageenan, cornstarch, mannitol and hydroxypropylcellulose (which was represented by HPC-L in Table 4) were sufficiently mixed and water was then added, and they were granulated to obtain granules. Two examinees held 0.5 g of this granules in their mouths, and the judgment was done. The evaluation standard was based on Example 1. The result was shown in Table 4.
100 mg of donepezil hydrochloride, 300 mg of sodium saccharin and 14 g of povidone were dissolved in 50 g of purified water, and separately, 700 mg of κ-carrageenan was added to 50 g of purified water, and it was were heated at 80� C. to be dissolved. After it was cooled down, both solutions were mixed, and 300 mg of methylparabene and 20 mg of propylparabene were dissolved in a small quantity of propyleneglycol to be added to the above mixture, so that syrups were manufactured.
40 g of xylitol was added to 50 g of purified water, and they were heated at 80� C. to be dissolved. And separately, 200 mg of donepezil hydrochloride was dissolved in 50 ml of purified water, and wherein 0.56 g of κ-carrageenan, 1.0 g of λ-carrageenan, 0.15 g of locust bean gum, 0.22 g of gerun gum, 0.15 g of xanthan gum, 0.19 g of sodium citrate, 0.19 g of calcium lactate, 0.94 g of lactose and 40 g of powdered hydrogenated maltose starch syrup were added, and in addition, the previously prepared xylitol-containing purified water was added therein, and they were stirred at 90� C. After the mixture was cooled down to 80� C., 0.6 g of citric acid was mixed therein, to which purified water was added, so that the total weight was 200 g. It was pipetted into vessels in a portion of 10 g and then cooled down to manufacture jellies.
15 g of (RS)-1-(isopropoxycarbonyloxy)ethyl(+)-(6R,7R)-7{(z)-2-(2-aminothiazole-4-yl)-2-hydroxyiminoacet-amide}-3-N,N-dimethylcarbamoyloxymethyl-8-oxo-5-thia-1-azabicyclo[4.2.0]octo-2-en-2-carboxylate hydrochloride salt, g of κ-carrageenan, 30 g of cornstarch and 40 g of mannitol were mixed by the use of the rolling granuator, and about 20 ml of water was slowly added therein and wet mass was manufactured, and then dried through a screen with 32 meshes, so that granules were manufactured.
15 g of the drug substance medicine used in Example 3, 15 g of sodium condroitin sulfate and 70 g of mannitol were mixed by the use of the granulator, and about 20 ml of water was slowly added therein and wet mass was manufactured, and then dried through a screen with 32 meshes, so that granules were manufactured.
15 g of the drug substance used in Example 3, 15 g of carrageenan (mixture of ι-carrageenan and κ-carrageenan), 15 g of copolyvidon and 55 g of mannitol were mixed by the use of the granulator, and about 15 ml of water was slowly added therein and wet mass was manufactured, and then dried through a screen with 32 meshes, so that granules were manufactured.
58 g of the drug substance used in Example 3, 58 g of κ-carrageenan, 120 g of cornstarch, 130 g of mannitol and 16 g of aerosil were mixed, whereon 8 g of sodium alginate dissolved in 392 ml of water and a slight amount of Red-102 pigment were sprayed by the use of the fluidized bed granulator, and then they were dried. Next, 2 g of strawberry essence was sprayed thereon and they were dried, wherein 8 g of aspartame was mixed, so that fine granules were manufactured.
15 g of the drug substance used in Example 3, 14.5 g of κ-carrageenan, 30 g of cornstarch and 40 g of mannitol were mixed, whereon 0.5 g of λ-carrageenan dissolved in 25 ml of water was sprayed by the use of the fluidized bed granulator, so that fine granules were manufactured.
10 g of cefcapene pivoxil hydrochloride, 10 g of κ-carrageenan, 30 g of cornstarch, 48 g of mannitol and 2 g of aspartame were mixed by the use of a rolling granulator, and 20 ml of water was slowly added thereto and wet mass was manufactured, and then dried through a screen with 32 meshes, so that granules were manufactured.
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No. 10/203,687 dated Oct. 20, 2004.18Wade and Weller-Editors: Handbook of Pharmaceutical Excipients, Povidone, p. 392, 1994.* Cited by examinerReferenced byCiting PatentFiling datePublication dateApplicantTitleUS8715715Oct 29, 2009May 6, 2014Nal Pharmaceuticals Ltd.Dosage form for insertion into the mouthUS9018193Sep 13, 2011Apr 28, 2015Bev-Rx, Inc.Aqueous drug delivery systemUS9114073May 16, 2014Aug 25, 2015Nal Pharmaceuticals, Ltd.Dosage form for insertion into the mouthUS9114074May 16, 2014Aug 25, 2015Nal Pharmaceuticals, Ltd.Dosage form for insertion into the mouthUS9114075Jun 19, 2014Aug 25, 2015Nal Pharmaceuticals, Ltd.Dosage form for insertion into the mouthUS9119776Jun 19, 2014Sep 1, 2015Nal Pharmaceuticals, Ltd.Dosage form for insertion into the mouthUS20100112050 *Oct 29, 2009May 6, 2010Je Phil RyooDosage Form For Insertion Into The MouthUS20110124577 *Jun 15, 2009May 26, 2011Suntory Holdings LimitedPreparation for oral administration comprises quercetin glycoside and a water-based solvent extract of cartilage containing chondroitin sulfate* Cited by examinerClassifications U.S. Classification424/489, 424/465, 424/481, 424/485, 514/974, 514/772.4, 424/488, 424/441, 424/479International ClassificationA61K9/20, A61K9/68, A61K9/34, A61K47/32, A61K47/36, A61K9/00, A61K9/16Cooperative ClassificationA61K47/36, A61K9/1652, Y10S514/974, A61K9/0095European ClassificationA61K9/00Z6, A61K9/16H6F, A61K47/36Legal EventsDateCodeEventDescriptionAug 31, 1999ASAssignmentOwner name: EISAI CO., LTD.,JAPANFree format text: ASSIGNMENT OF ASSIGNORS INTEREST;ASSIGNORS:UKAI, KOJI;HARADA, TSUTOMU;SUZUKI, YASUYUKI;REEL/FRAME:010313/0752Effective date: 19990816Jun 29, 2007ASAssignmentOwner name: EISAI R&D MANAGEMENT CO., LTD.,JAPANFree format text: ASSIGNMENT OF ASSIGNORS INTEREST;ASSIGNOR:EISAI CO., LTD.;REEL/FRAME:019500/0673Effective date: 20061228Owner name: EISAI R&D MANAGEMENT CO., LTD., JAPANFree format text: ASSIGNMENT OF ASSIGNORS INTEREST;ASSIGNOR:EISAI CO., LTD.;REEL/FRAME:019500/0673Effective date: 20061228Nov 22, 2013FPAYFee paymentYear of fee payment: 4RotateOriginal ImageGoogle Home - Sitemap - USPTO Bulk Downloads - Privacy Policy - Terms of Service - About Google Patents - Send FeedbackData provided by IFI CLAIMS Patent Services