Rapidly dissoluble medicinal dosage unit and method of manufacture

Claim 2

A spdn fibrous pharmaceutical composition according to claim 1, wherein said medicament is an antihistaminic labyrinthine function depressant.

Claim 3

A spun fibrous pharmaceutical composition according to claim 1, wherein said medicament is a decongestant. A spun fibrous pharmaceutical composition according to claim 1, wherein said medicament is acetaminophen.

Claim 4

A spun fibrous pharmaceutical composition according to claim 1, wherein said medicament is diethylcarbamazine citrate.

Claim 5

A spun fibrous pharmaceutical composition according to claim 1, wherein said composition further comprises an adhesion promoter for promoting adhesion between said sugar material and said medicament.

Claim 6

A spun fibrous pharmaceutical composition according to claim 7, wherein said adhesion promoter comprises polyvinylpyrrolidone.

Claim 7

A spun fibrous pharmaceutical composition according to claim 8, wherein said medicament comprises diethylcarbamazine citrate.

Claim 8

A spun fibrous pharmaceutical composition according to claim 1, wherein said sugar is selected from the group consisting of maltose, fructose, sorbitol, dextrose, mannitol, sucrose, lactose, and combinations thereof.

Claim 9

A spun fibrous pharmaceutical composition according to claim wherein said mass of spun fibers is in the form of a compacted unit-dose body of said fibers where the fibers have retained their fibrous identity.

Claim 10

A spun fibrous pharmaceutical composition according to any one of claims 1 to 9, wherein said mass of spun fibers is in the form of a compacted unit-dose body of said fibers where the fibers have retained their fibrous identity. I Ii L.ii. LI i SI t, 22

Claim 11

A spun fibrous pharmaceutical composition according to any one of claims 1 to 9, wherein said sugar comprises at least 10% lactose and the remainder sucrose.

Claim 12

A spun fibrous pharmaceutical composition according to any one of claims 1 to 13, wherein said medicament is of the type that is rapidly assimilated when in contact with the tissues of the oral cavity. A pharmaceutic dosage unit comprising compacted spun fibers of a spinnable, readily water soluble sugar material and an effective amount of a medicament distributed on or incorporated in said fibers, said sugar material having a melting point below that temperature at which said medicament might decompose or otherwise break down.

Claim 14

A system according to claim 16, wherein form is hydrophilic.

Claim 15

A system according to claim 16 or claim ingredient is essentially lactose.

Claim 19

A multicameral container for intravenous said ingredient in fiber 17, wherein said 16 to 18, wherein said 16 to 18, wherein said 16 to 18, wherein said 16 to 18, wherein said activity. or intramuscular administration comprising a first compartment containing a pharmaceutically acceptable solvent, and a second compartment containing a spun fibrous pharmaceutical composition comprising a mass of spun fibers of a sugar material capable of being spun into fibers that are readily water-soluble and a medicament distributed on or Incorporated in said mass of spun fibers. such as methyl cellulose, ethyl cellulose, hydroxy methyl or 4 23

Claim 20

A multicameral container according to claim 23, wherein said material is a sugar selected from the group consisting of maltose, fructose, sorbitol, dextrose, mannitol, sucrose, lactose, and combinations thereof. A multicameral container according to claim 23, wherein said mass of spun fibers is in the form of a compacted body of said fibers where the fibers have retained their fibrous identity.

Claim 21

A multicameral container according to claim 25, wherein said sugar comprises about 10% lactose and the remainder sucrose.

Claim 23

A method according to claim 27, wherein said medicament is combined with a melt spinnable compatible water soluble sugar to provide an intermediate product, and said intermediate product is converted to a mass of spun fibers by melt spinning said product. S29. A method according to claim 27 or claim 28, wherein said sugar comprises a mixture of sucrose and lactose. A method according to claim 29, wherein said lactose is combined with said sucrose in the ratio of about 1:9 by weight.

Claim 25

A method according to claim 28, wherein said intermediate product is produced by coating granules of said sugar with a slurry of said medicament where the vehicle for said slurry is not a solvent for said sugar.

Claim 26

A method according to claim 32, wherein said vehicle is isopropyl alcohol.

Claim 27

A method according to claim 33, wherein said granules of sugar are added to said slurry and the slurry coated granules are thereafter dried then spun to produce said fibers. S A/0189f 1 .i i. li TtiLz, SI 24- A method according to claim 33 or claim 34, wherein said slurry is produced by admixing acetaminophen with isopropyl alcohol to produce a

Claim 28

60-70% w/v solution of said medicament in said vehicle. 36. A method according to claim 33 or claim 34, wherein said slurry is produced by adding 2-3% by weight of polyvinylpyrrolidone to isopropyl alcohol and admixing the resulting solution with diethylcarbamazine citrate to obtain a slurry containing about 60% w/v of said medicament in said vehicle. 37. A method according to claim 28, wherein the spun fiber product resulting from said melt spinning of said intermediate product is compacted to produce a body whose enclosed volume is substantially less than the as-spun enclosed volume, and the compacted product is thereafter subdivided into dosage units. 38. A method according to claim 37, wherein said compaction step is performed to produce said body with an enclosed volume at least 30% less than said as-spun enclosed volume, said compaction step being limited to less than that compaction which would result in noticeable fracturing of said fibers. 39. A spun fibrous pharmaceutical composition, substantially as herein described with reference to Example 1 or Example 3 or any one of *:Goo: Test Nos 1, 2, or 4 to 16 of Example 4. A pharmaceutic dosage unit comprising compacted spun fibers of a spinnable, readily water soluble sugar material and an effective amount of medicament, which dosage unit is substantially as herein described with reference to Example 1 or Example 3 or any one of Test Nos 1, 2, or 4 to 16 of Example 4. 41. A system for topical delivery of a medicament as defined in claim 16 and substantially as herein described. 42. A multicameral container for intravenous or intramuscular S' administration as defined in claim 23 and substantially as herein described. I 25 43. A method for preparing a pharmaceutical dosage unit for delivering a medicament, comprising producing a mass of medicament bearing spun fibers, which method is substantially as herein defined with reference to Example 1 or Example 3 or any one of Test Nos 1, 2 or 4 to 16 of Example 4. DATED this EIGHTEENTH day of JANUARY 1991 Fuisz Pharmaceutical Ltd Patent Attorneys for the Applicant SPRUSON FERGUSON 0 0 S. 0 0 S 0 00 0 S q 5@ STA/0189f i produces a fibrous product after spinning that is I 4,; INTERNATIONAL SEARCH REPORT International Aoplication NPCT/US88/0 1 199 I- I. CLASSIFICATION OF SUBJECT M'ATTER (if several classification symbols apply, indicate all) 6 According to International Patent Classification (IPC) or to both Nallonal'Classification and IPC IPC(4): A61K 9/00 A61K 9/70 U.S.C1.: 424/400 424/443 424/440 II. FIELDS SEARCHED Minimum Documentation Searched 7 Classiication System Classification Symbols U.S. 264/177. 13 424/400, 424/439, 424/400, 424/443, 424/449 426/516, 426/517, 426/658, 426/660 Documentation Searched other than Minimum Documentation to the Extent that such Documents are Included in the Fields Searched a III. DOCUMENTS CONSIDERED TO BE RELEVANT 9 Cateqory Citation of Document, t1 with indication, where appropriate. of the relevant passages 12 Relevant to Claim No. 13 A A, 3,019,745 (DUBOIS ET AL) 6 1,2,3,12 February 1962. (See the entire document). A A, 3,036,532 (BOWE) 29 May 1962. 1,2,3,12 (See the entire document). A A, 3,070,045 (BOWE) 25 December 1,2,3,12

Claim 29

(See the entire document). A A, 3,073,262 (BOWE) 15 January 1,2,3,12.

Claim 30

(See the entire document). A A, 3,324,061 (TANQUARY) 6 June 9,10,

Claim 31

(See the entire document). 31 to 44 A A, 3,557,717 (CHIVERS) 26 January 1,2,3,12

Claim 32

(See the entire document). A A, 3,595,675 (ASH ET AL) 27 July 1,2,3,12 1971. (See the entire document). SSpecial categories of cited documents: o later document published after the international filing date document defining the general state of the art which is not or priority date and not in conflict with the application but considered to be of particular relevance cited to understand the principle or theory underlying the invention earlier document but published on or alter the international invention filing date document of particular relevance: the claimed invention cannot be considered rovel or cannot be considered to document which may throw doubts on priority claim(s) or involve an inventive step which is cited to establish the publication date of another documet of particula relevance the laimed nventon citation or other special reason (as specified) d o cu m en t of particular relevance; the claimed invention Sr cannot be considered to involve an inventive step when the document referring to an oral disclosure, use. exhibition or document is combined with one or more other such docu- other means ments, such combination being obvious to a person skilled document oublished prior to the international filing date but in the art. later than the priority date claimed document member of the same patent family IV. CERTIFICATION Date of the Actual Completion of the International Search Date of Mailing of this International Search Report 07 JULY_.9J8. 0 8 AUG 1988 International Searching Authority Signature ol Authorized Officer ISA/US SHEP ROSE Form PCTAS,21t0 (icond show) (ev.t 1-87) i i iii;l i Interntiional Applicaition No PCT/US88/O 1199 Ill, DOCUMENTS CONSIDERED TO BE RELEVANT (CONTINUED FROM THE SECOND SHEET) Categarv Cootron of Documient, with indication, where appropriate, of the relevant passages Rlvn oCamN A A: A: At A, 3,875,300 (HOM4M ET' AL) 1 April

Claim 33

(See the entire document) A, 3,930,043 (WARNING ET AL) 30 December 1975. (See the entire document). A, 3,967,623 (BUTTERWORTH ET AL) 6 July 1976. (See the entire document). A, 4,496,592 (KUWAHARA ET' AL) 29 January 1985. (See the entire document). A, 4,526,525 (OISO ET AL) 2 July

Claim 34

(See the entire document). A, 2,826,169 (LeVEEN) 12. March 1958. (See the entire document). U.S, A, 4,136,145 (FUCHS FET AL) 23 January 1979. (See the entire document). 1,2,9,13, 14,1-"7, 18, 31 to 44 1,2,3,12 1,2,9,13, 14, 17, 18, 31 to 44 13, 14 13, 14 18,19,24 18,19,24 Paoh PCTJSAj2Io(emtasrieu) lReV.1l.87)