Solid preparation

Details Solid preparation Solid preparation

2001-03-07

2003-07-01

Spear, James M. (Department: 1615)

Drug, bio-affecting and body treating compositions

Preparations characterized by special physical form

Tablets, lozenges, or pills

C424S465000, C514S781000

Reexamination Certificate

active

06586004

ABSTRACT:

TECHNICAL FIELD
The present invention relates to a solid preparation, especially a preparation capable of buccal disintegration or dissolution, having characteristics of fast disintegration or dissolution in the oral cavity even without water.
BACKGROUND ART
There has been a demand for development of a pharmaceutical preparation capable of buccal disintegration or dissolution, which can be, if necessary, administered readily even without water, by aged people and children anywhere or anytime. Examples of prior art references disclosing such preparation are shown below.
JP-A H9(1997)-48726 discloses rapid buccal dissolution type preparations comprising a drug and a material wetting in a mouldable way on humidifying and retaining a shape after moulding and drying. Such material is exemplified by sugars, sugar alcohols, and water-soluble polymers.
JP-A H5(1993)-271054 (EP-A 553777) discloses a method of producing a rapid buccal dissolution type tablets comprising a pharmacologically active ingredient and sugars.
JP-A H9(1997)-71523 discloses tablets with rapid disintegration in the oral cavity which comprise a drug, crystalline cellulose, low-substituted hydroxypropylcellulose and a lubricant.
However, these prior art references nowhere disclose a solid preparation comprising (1) a pharmaceutically active ingredient, (2) one or more water-soluble sugar alcohols selected from the group consisting of sorbitol, maltitol, reduced starch saccharide, xylitol, reduced palatinose and erythritol, and (3) low-substituted hydroxypropylcellulose having hydroxypropoxyl group contents of 7.0 to 9.9 percent by weight.
There has been a demand for development of a solid preparation which exhibits excellent buccal disintegration and dissolution and also an appropriate strength (hardness) such that the solid preparation never disintegrates or suffers damage in the course of the production steps or distribution stages.
DISCLOSURE OF INVENTION
The present invention relates to a solid preparation comprising (1) a pharmaceutically active ingredient, (2) one or more water-soluble sugar alcohol selected from the group consisting of sorbitol, maltitol, reduced starch saccharide, xylitol, reduced paratinose and erythritol (hereafter also referred to as a water-soluble sugar alcohol), and (3) low-substituted hydroxypropylcellulose having hydroxypropoxyl group contents of 7.0 to 9.9 percent by weight.
The present invention further relates to use of low-substituted hydroxypropylcellulose having hydroxypropoxyl group contents of 7.0 to 9.9 percent by weight for the manufacture of a pharmaceutical preparation capable of buccal disintegration or dissolution.
The present invention further relates to method of improving buccal disintegration or dissolution of a solid pharmaceutical preparation characterized by using low-substituted hydroxypropylcellulose having hydroxypropoxyl group contents of 7.0 to 9.9 percent by weight.
The pharmaceutically active ingredient to be used in the present invention may be in any optional form, for example, a solid, powder or granular, crystalline, oily or solution form.
As the pharmaceutically active ingredient, for instance, there may be mentioned one or more ingredients selected from the group consisting of nourishing and health-promoting agents, antipyretic-analgesic-antiinflammatory agents, antipsychotic drugs, antianxiety drugs, antidepressants, hypnotic-sedatives, spasmolytics, central nervous system affecting drugs, cerebral metabolism ameliolators, antiepileptics, sympathomimetic agents, gastrointestinal function conditioning agents, antacids, antiulcer agents, antitussive-expectorants, antiemetics, respiratory stimulants, bronchodilators, antiallergic agents, dental buccal drugs, antihistamines, cardiotonics, antiarrhythmic agents, diuretics, hypotensive agents, vasoconstrictors, coronary vasodilators, peripheral vasodilators, antihyperlipidemic agents, cholagogues, antibiotics, chemotherapeutic agents, antidiabetic agents, drugs for osteoporosis, skeletal muscle relaxants, antidinics, hormones, alkaloid narcotics, sulfa drugs, antipodagrics, anticoagulants, anti-malignant tumor agents, agents for alzheimer's disease, etc.
Examples of the nourishing and health-promoting agents include vitamins such as vitamin A, vitamin D, vitamin E (d-&agr;-tocopherol acetate, etc.), vitamin B
1
(dibenzoylthiamine, fursultiamine hydrochloride, etc.), vitamin B
2
(riboflavin butyrate, etc.), vitamin B
6
(pyridoxine hydrochloride, etc.), vitamin C (ascorbic acid, sodium L-ascorbate, etc.), vitamin B
12
(hydroxocobalamin acetate, etc.), etc.; minerals such as calcium, magnesium and iron; proteins, amino acids, oligosaccharides, crude drugs, etc.
Examples of the antipyretic-analgesic-antiinflammatory agents include aspirin, acetaminophen, ethenzamide, ibuprofen, diphenhydramine hydrochloride, dl-chlorpheniramine maleate, dihydrocodeine phosphate, noscapine, methylephedrine hydrochloride, phenylpropanolamine hydrochloride, caffeine, anhydrous caffeine, serratiopeptidase, lysozyme chloride, tolfenamic acid, mefenamic acid, diclofenac sodium, flufenamic acid, salicylamide, aminopyrine, ketoprofen, indomethacin, bucolome, pentazocine, etc.
Examples of the antipsychotic drugs include chlorpromazine, reserpine, etc.
Examples of the antianxiety drugs include alprazolam, chlordiazepoxide, diazepam, etc.
Examples of the antidepressants include imipramine, maprotiline, amphetamine, etc.
Examples of the hypnotic-sedatives include estazolam, nitrazepam, diazepam, perlapine, phenobarbital sodium, etc.
Examples of the spasmolytics include scopolamine hydrobromide, diphenhydramine hydrochloride, papaverine hydrochloride, etc.
Examples of the central nervous system affecting drugs include citicoline, rotirenine, etc.
Examples of the cerebral metabolism ameliolators include vinpocetine, meclofenoxate hydrochloride, etc.
Examples of the antiepileptics include phenytoin, carbamazepine, etc.
Examples of the sympathomimetic agents include isoproterenol hydrochloride, etc.
Examples of the gastrointestinal function conditioning agents include stomachic-digestives such as diastase, saccharated pepsin, scopolia extract, cellulase AP3, lipase AP, cinnamon oil, etc.; intestinal function controlling drugs such as perperine hydrochloride, resistant lactic acid bacterium,
Lactobacillus bifidus,
etc.
Examples of the antacids include magnesium carbonate, sodium hydrogen carbonate, magnesium aluminometasilicate, synthetic hydrotalcite, precipitated calcium carbonate, magnesium oxide, etc.
Examples of the antiulcer agents include lansoprazole, omeprazole, rabeprazole, pantoprazole, famotidine, cimetidine, ranitidine hydrochloride, etc.
Examples of the antitussive-expectorants include chloperastine hydrochloride, dextromethorphan hydrobromide, theophylline, potassium guaiacolsulfonate, guaifenesin, codeine phosphate, etc.
Examples of the antiemetics include diphenidol hydrochloride, metoclopramide, etc.
Examples of the respiratory stimulants include levallorphan tatrate, etc.
Examples of the bronchodilators include theophylline, salbutamol sulfate, etc.
Examples of the antiallergic agents include amlexanox, seratrodast, etc.
Examples of the dental buccal drugs include oxytetracycline, triamcinolone acetonide, chlorhexidine hydrochloride, lidocaine, etc.
Examples of the antihistamines include diphenhydramine hydrochloride, promethazine, isothipendyl hydrochloride, dl-chlorpheniramine maleate, etc.
Examples of the cardiotonics include caffeine, digoxin, etc.
Examples of the antiarryhythmic agents include procainamide hydrochloride, propranolol hydrochloride, pindolol, etc.
Examples of the diuretics include isosorbide, furosemide, etc.
Examples of the hypotensive agents include delapril hydrochloride, captopril, hexamethonium bromide, hydralazine hydrochloride, labetalol hydrochloride, manidipine hydrochloride, candesartan cilexetil, methyldopa, losartan, valsartan, eprosartan, irbesartan, tasosartan, telmisartan, pomisartan, ripisartan, forasartan, etc.
Examples of the vasoconstrictors include phenylephrine hydrochlo

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