Pharmaceutical compositions and oral dosage forms of a levodopa prodrug and methods of use
원문보기
IPC분류정보
국가/구분
United States(US) Patent
등록
국제특허분류(IPC7판)
A61K-009/02
A61K-009/24
출원번호
US-0941971
(2010-11-08)
등록번호
US-8435562
(2013-05-07)
발명자
/ 주소
Mao, Chen
Pargaonkar, Nikhil
Maurer, Laura E.
Ma, Sarina Grace Harris
출원인 / 주소
XenoPort, Inc.
대리인 / 주소
Kilpatrick Townsend & Stockton LLP
인용정보
피인용 횟수 :
0인용 특허 :
48
초록
Pharmaceutical compositions and oral dosage forms of (2R)-2-phenylcarbonyloxypropyl (2S)-2-amino-3-(3,4-dihydroxyphenyl)propanoate mesylate and methods of treating diseases comprising orally administering such pharmaceutical compositions and dosage forms are disclosed.
대표청구항▼
1. A pharmaceutical composition comprising granules, wherein the granules are prepared using high shear wet granulation and comprise: 90 wt % to 99 wt % anhydrous crystalline (2R)-2-phenylcarbonyloxypropyl (2S)-2-amino-3-(3,4-dihydroxyphenyl)propanoate mesylate; and0.5 wt % to 2 wt % C6-18 alkylsulf
1. A pharmaceutical composition comprising granules, wherein the granules are prepared using high shear wet granulation and comprise: 90 wt % to 99 wt % anhydrous crystalline (2R)-2-phenylcarbonyloxypropyl (2S)-2-amino-3-(3,4-dihydroxyphenyl)propanoate mesylate; and0.5 wt % to 2 wt % C6-18 alkylsulfate or pharmaceutically acceptable salt thereof. 2. The pharmaceutical composition of claim 1, wherein the C6-18 alkylsulfate or pharmaceutically acceptable salt thereof is sodium lauryl sulfate. 3. The pharmaceutical composition of claim 1, comprising one or more pharmaceutically acceptable excipients. 4. A pharmaceutical composition comprising: about 50 wt-% to about 90 wt-% anhydrous crystalline (2R)-2-phenylcarbonyloxypropyl (2S)-2-amino-3-(3,4-dihydroxyphenyl)propanoate mesylate;about 0.5 wt-% to about 2.0 wt-% C6-18 alkylsulfate or pharmaceutically acceptable salt thereof;about 6 wt-% to about 20 wt-% hydroxypropylmethylcellulose; andabout 0.5 wt-% to about 2.0 wt-% magnesium stearate;wherein wt-% is based on the total dry weight of the composition. 5. The pharmaceutical composition of claim 1, comprising an L-aromatic amino acid decarboxylase inhibitor, a catechol-O-methyltransferase inhibitor, or a combination of an L-aromatic amino acid decarboxylase inhibitor and a catechol-O-methyltransferase inhibitor. 6. An oral tablet dosage form comprising granules prepared using high shear wet granulation, wherein the granules comprise: anhydrous crystalline (2R)-2-phenylcarbonyloxypropyl (2S)-2-amino-3-(3,4-dihydroxyphenyl)propanoate mesylate; anda C6-18 alkylsulfate or pharmaceutically acceptable salt thereof. 7. The dosage form of claim 6, wherein the C6-18 alkylsulfate or pharmaceutically acceptable salt thereof is sodium lauryl sulfate. 8. The dosage form of claim 6, comprising one or more pharmaceutically acceptable excipients. 9. An oral tablet dosage form comprising: about 50 wt-% to about 90 wt-% anhydrous crystalline (2R)-2-phenylcarbonyloxypropyl (2S)-2-amino-3-(3,4-dihydroxyphenyl)propanoate mesylate;about 0.5 wt-% to about 2.0 wt-% C6-18 alkylsulfate or pharmaceutically acceptable salt thereof;about 6 wt-% to about 20 wt-% hydroxypropylmethylcellulose; andabout 0.5 wt-% to about 2 wt-% magnesium stearate;wherein wt-% is based on the total dry weight of the dosage form. 10. The dosage form of claim 7, comprising an L-aromatic amino acid decarboxylase inhibitor, a catechol-O-methyltransferase inhibitor, or a combination of an L-aromatic amino acid decarboxylase inhibitor and a catechol-O-methyltransferase inhibitor. 11. The dosage form of claim 6, which when placed in 0.1 N HCl, pH 1.2 at 37° C. and agitated at 50 rpm, releases about 28% to about 58% of the anhydrous crystalline (2R)-2-phenylcarbonyloxypropyl (2S)-2-amino-3-(3,4-dihydroxyphenyl)propanoate mesylate within about 2 hours, about 40% to about 70% within about 4 hours, about 67% to about 97% within about 9 hours, and greater than about 80% within about 18 hours. 12. The dosage form of claim 6, which is a bilayer tablet dosage form comprising: a first layer comprising granules comprising anhydrous crystalline (2R)-2-phenylcarbonyloxypropyl (2S)-2-amino-3-(3,4-dihydroxyphenyl)propanoate mesylate and a C6-18 alkylsulfate or pharmaceutically acceptable salt thereof; anda second layer comprising an L-aromatic amino acid decarboxylase inhibitor. 13. The dosage form of claim 12, wherein the C6-18 alkylsulfate or pharmaceutically acceptable salt thereof is sodium lauryl sulfate, and the L-aromatic amino acid decarboxylase inhibitor is carbidopa. 14. An oral tablet dosage form, which a is bilayer tablet dosage form, wherein: the first layer comprises the granules comprising about 70 wt-% to about 95 wt-% anhydrous crystalline (2R)-2-phenylcarbonyloxypropyl (2S)-2-amino-3-(3,4-dihydroxyphenyl)propanoate mesylate and about 0.5 wt-% to about 3 wt-% C6-18 alkylsulfate or pharmaceutically acceptable salt thereof; andthe second layer comprises about 15 wt-% to about 30 wt-% of an L-aromatic amino acid decarboxylase inhibitor. 15. The dosage form of claim 12, which when placed in 0.1 N HCl, pH 1.2 or pH 5.0 at 37° C. and agitated at 50 rpm, releases about 28% to about 58% of the anhydrous crystalline (2R)-2-phenylcarbonyloxypropyl (2S)-2-amino-3-(3,4-dihydroxyphenyl)propanoate mesylate within about 2 hours, about 50% to about 80% within about 4 hours, and greater than about 80% within about 12 hours. 16. A method of treating a disease in a patient comprising administering to a patient in need of such treatment a therapeutically effective amount of the pharmaceutical composition of claim 1, wherein the disease is chosen from schizophrenia, a cognitive impairment disorder, restless legs syndrome, a periodic limb movement disorder, tardive dyskinesia, Huntington's disease, hypertension, and excessive daytime sleepiness. 17. A method of treating Parkinson's disease in a patient comprising administering to a patient in need of such treatment a therapeutically effective amount of the pharmaceutical composition of claim 1. 18. A method of treating a disease in a patient comprising administering to a patient in need of such treatment the tablet dosage form of any one of claim 6 and 12, wherein the disease is chosen from schizophrenia, a cognitive impairment disorder, restless legs syndrome, a periodic limb movement disorder, tardive dyskinesia, Huntington's disease, hypertension, and excessive daytime sleepiness. 19. A method of treating Parkinson's disease in a patient comprising administering to a patient in need of such treatment the tablet dosage form of any one of claim 6 and 12. 20. The pharmaceutical composition of claim 1, wherein the granules are substantially free of crystalline (2R)-2-phenylcarbonyloxypropyl (2S)-2-amino-3-(3,4-dihydroxyphenyl)propanoate mesylate, hydrate. 21. The oral dosage form of claim 6, wherein the granules are substantially free of crystalline (2R)-2-phenylcarbonyloxypropyl (2S)-2-amino-3-(3,4-dihydroxyphenyl)propanoate mesylate, hydrate.
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