MINOCYCLINE ORAL DOSAGE FORMS FOR THE TREATMENT OF ACNE
First Claim
Patent Images
1. A minocycline oral dosage form for treatment of acne, comprising minocycline or apharmaceutically acceptable salt thereof;
- andan amount of a controlled-release carrier, said controlled-release carrier comprising a slow dissolving carrier, an intragranular fast dissolving carrier, and an extragranular fast dissolving carrier, wherein said controlled-release carrier provides a release rate in gastric fluid of the minocycline or a pharmaceutically acceptable salt thereof that is either about 25% to about 52% within 1 hour, about 53% to about 89% within 2 hours, and at least 90% within about 4 hours, or about 30% to about 52% within 1 hour, about 53% to about 84% within 2 hours, and at least 85% within about 4 hours, so that there is a reduction in adverse side effects, and a patient receives, without an initial load dose, about 0.75 mg/kg/day to about 1.5 mg/kg/day of the minocycline or the pharmaceutically acceptable salt thereof by a once daily administration.
14 Assignments
0 Petitions
Accused Products
Abstract
Minocycline oral dosage forms containing a controlled release carrier are useful for the treatment of acne.
92 Citations
44 Claims
-
1. A minocycline oral dosage form for treatment of acne, comprising minocycline or a
pharmaceutically acceptable salt thereof; - and
an amount of a controlled-release carrier, said controlled-release carrier comprising a slow dissolving carrier, an intragranular fast dissolving carrier, and an extragranular fast dissolving carrier, wherein said controlled-release carrier provides a release rate in gastric fluid of the minocycline or a pharmaceutically acceptable salt thereof that is either about 25% to about 52% within 1 hour, about 53% to about 89% within 2 hours, and at least 90% within about 4 hours, or about 30% to about 52% within 1 hour, about 53% to about 84% within 2 hours, and at least 85% within about 4 hours, so that there is a reduction in adverse side effects, and a patient receives, without an initial load dose, about 0.75 mg/kg/day to about 1.5 mg/kg/day of the minocycline or the pharmaceutically acceptable salt thereof by a once daily administration. - View Dependent Claims (2, 3, 4, 5, 6, 7, 8, 9, 10, 11, 12, 23, 24, 25, 26)
- and
-
13. An oral dosage form for the treatment of acne, comprising:
-
an amount of minocycline free base equivalent of minocycline hydrochloride, wherein the amount is one selected from the group consisting of 45 mg, 90 mg and 135 mg; a matrix-forming polymer, wherein the matrix-forming polymer is in an amount of 108 mg for 45 mg or 90 mg dosage forms, and in an amount of 94 mg for 135 mg dosage form; an intragranular lactose monohydrate; and an extragranular lactose monohydrate, wherein the dosage form provides a patient with about 0.75 mg/kg/day to about 1.5 mg/kg/day of the minocycline in a slow, continuous fashion, without an initial load dose, that effectively treats acne of the patient and reduces adverse vestibular side effects by a once daily administration of the dosage form. - View Dependent Claims (14, 15, 16, 17, 18)
-
-
19. A minocycline oral dosage form for the treatment of acne, comprising:
-
45 mg of minocycline hydrochloride; 108 mg of the matrix-forming polymer hydroxypropyl methylcellulose; 197 mg of intragranular lactose; 41 mg of extragranular lactose monohydrate; and wherein the dosage form provides a patient with about 1 mg/kg/day of the minocycline in a slow, continuous fashion, without an initial load dose, that effectively treats acne of the patient and with a reduction in normal adverse vestibular side effects by a once daily administration of the dosage form. - View Dependent Claims (20)
-
-
21. A minocycline oral dosage form for the treatment of acne, comprising:
-
135 mg of minocycline hydrochloride; 94 mg of the matrix-forming polymer hydroxypropyl methylcellulose; 121 mg of intragranular of lactose monohydrate; 41 mg of extragranular lactose monohydrate; and wherein the dosage form provides a patient with about 1 mg/kg/day of the minocycline in a slow, continuous fashion, without an initial load dose, that effectively treats acne of the patient and with a reduction in normal adverse vestibular side effects by a once daily administration of the dosage form. - View Dependent Claims (22)
-
-
27. A method of administering an oral dosage form for the treatment of acne comprising:
-
(i) administering to a patient the oral dosage form, the oral dosage form comprising; minocycline or a pharmaceutically acceptable salt thereof; and a controlled release carrier that comprises a fast dissolving carrier and a slow dissolving carrier, wherein the fast dissolving carrier has an intragranular fast dissolving carrier, and an extragranular fast dissolving carrier, said controlled release carrier being present in the range from about 20% to about 30%, by weight based on the total weight of the oral dosage form; wherein the extragranular fast dissolving carrier and the slow dissolving carrier are at a weight ratio of 0.3 to about 0.5 of the extragranular fast dissolving carrier to the slow dissolving carrier, and wherein the minocycline or a pharmaceutically acceptable salt thereof is released in a slow, continuous release in the patient, without an initial load dose, and at a release rate in gastric fluid that is either about 25% to about 52% within 1 hour, about 53% to about 89% within 2 hours, and at least 90% within about 4 hours, or about 30% to about 52% within 1 hour, about 53% to about 84% within 2 hours, and at least 85% within about 4 hours; and wherein the oral dosage form administered, once daily, to the patient provides the patient with about 0.75 mg/kg/day to about 1.5 mg/kg/day of the minocycline or a pharmaceutically acceptable salt thereof that is effective to treat the acne with a reduced incidence of at least one adverse effect; and (ii) providing information to the patient, which information comprises results of performed clinical trials including a comparison of the oral dosage form to placebo with respect to an aspect of the at least one adverse effect. - View Dependent Claims (28, 29, 30, 31, 32, 33, 34, 35)
-
-
36. A method of administering an oral dosage form for the treatment of acne comprising:
-
selecting an oral dosage form from amongst at least 45 mg, 90 mg and 135 mg dosage forms, the oral dosage form having an amount of minocycline; a matrix-forming polymer, the matrix-forming polymer being present in the range between 20% to 30% by weight based on the total weight of the oral dosage form; an intragranular lactose monohydrate; and an extragranular lactose monohydrate; administering to a patient the oral dosage form once daily, wherein the patient is provided with about 0.75 mg/kg to 1.5 mg/kg of the minocycline in a slow, continuous fashion, without an initial load dose, that effectively treats acne of the patient and with a reduction in adverse vestibular side effects by the once daily administration of the oral dosage form. - View Dependent Claims (37, 38, 39, 40, 41, 42, 43, 44)
-
Specification
-
- Resources
Litigation Campaign Assessment
Thank you for your request. You will receive a custom alert email when the Litigation Campaign Assessment is available.
×
-
Current AssigneeMedicis Pharmaceutical Corporation (Bausch Health Cos., Inc.)
-
Original AssigneeMedicis Pharmaceutical Corporation (Bausch Health Cos., Inc.)
-
InventorsPatel, Bhiku, Plott, R. Todd, Wortzman, Mitchell, Bhatia, Kuljit
-
Granted Patent
-
Time in Patent OfficeDays
-
Field of Search
-
US Class Current424/488
-
CPC Class CodesA61K 31/65 TetracyclinesA61P 17/10 Anti-acne agents
