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Pharmaceutical Compositions For Treating Acne

Abstract: The present application relates to pharmaceutical compositions comprising retinoic acid or its derivatives such as isotretinoin and processes for preparing thereof. It also provides methods for treating acne by administering such pharmaceutical composition to a patient in need thereof.

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Notices, Deadlines & Correspondence

Patent Information

Application #
Filing Date
30 November 2018
Publication Number
10/2019
Publication Type
INA
Invention Field
PHARMACEUTICALS
Status
Email
sumamaheshwari@drreddys.com
Parent Application

Applicants

Dr. Reddy’s Laboratories Limited
8-2-337, Road No. 3, Banjara Hills, Hyderabad

Inventors

1. Kailas Khomane
Flat No. 301, Louts Park Block-B, Plot No. 947, No. 19, Lane 1, HMT Swarnapuri Colony, Miyapur Hyderabad, 500049.
2. Saurabh Srivastava
Plot No. 1133/2, Om Prakash Sabhasad Nagar, Rajrooppur, Allahabad, 211011.
3. Yogesh Bapurao Pawar
Plot No.2, K.B. H. Nagar, SubStation road, Malegaon Camp, Dist.Nasik, 423105.
4. Bijay Kumar Padhi
Kaniapally, Post – Dhunkapada, Dist – Ganjam, 761118.
5. Rajeev Singh Raghuvanshi
605, Ivory Towers, South City – I, Gurgaon, 122001.

Specification

We claim:
1. A once daily pharmaceutical composition of isotretinoin comprising:
(i) isotretinoin or a pharmaceutically acceptable salt thereof,
(ii) at least one solubility improving polymer; and
(iii) at least one rate controlling agent,
wherein said composition exhibits at least one of the following dissolution profiles when measured in USP type I apparatus at 100 rpm in 900 ml of borate buffer with a pH of 8.0 at 37 °C:
(a) about 1% to about 10% of isotretinoin in 1 hour,
(b) about 10% to about 25% of isotretinoin in 2 hours,

(d) about 25% to about 45% of isotretinoin in 4 hours,
(e) about 45% to about 60% of isotretinoin in 6 hours, and (d) about 60% to about 80% of isotretinoin in 12 hours.

2. The composition of claim 1, wherein said solubility improving polymer is selected from ionizable polymer, non-ionizable polymer, and mixtures thereof.
3. The composition of claim 2, wherein said solubility improving polymer comprises from about 10% w/w to about 40% w/w of the composition.
4. The composition of claim 1, wherein said composition comprises solubility improving polymer and isotretinoin present in a weight ratio of not more than about 3.0: 1.0.
5. The composition of claim 1, wherein said rate controlling agent is selected from pH independent polymer, pH dependent polymer, and mixtures thereof.
6. The composition of claim 6, wherein said rate controlling agent comprises from about 5% w/w to about 20% w/w of the composition.
7. The composition of claim 1, wherein at least about 60% of said isotretinoin is in an amorphous form.

8. The composition of claim 1, wherein said composition comprises (i) an extended release (ER) portion and (ii) a delayed release (DR) portion and/or an immediate release (IR) portion, containing isotretinoin with one or more pharmaceutically acceptable excipients.
9. A method of treating acne in a patient in need thereof comprising orally administering to the patient a once daily pharmaceutical composition of isotretinoin comprising:
(i) a daily dose of isotretinoin or a pharmaceutically acceptable salt thereof,
(ii) at least one solubility improving polymer; and
(iii) at least one rate controlling agent,
wherein said composition upon administration to the patient exhibits at least one of the following plasma level differences for AUC0-24 compared to commercially available twice daily isotretinoin composition that provides the same daily dose:
(a) about 5 to about 10 % lower between 0 to 5 hours,
(b) about 15 to about 20 % higher between 5 to 14 hours; and
(c) about 4 to about 8 % lower between 14 to 24 hours.
10. The method of claim 15, wherein said composition upon administration to
the patient under fasting condition, exhibits at least one of the following
pharmacokinetic parameters: (a) a Cmax of about 350.00 ng/ml to about 600.00
ng/ml, (b) an AUC(0-t) of about 5500.00 ng.hr/ml to about 7700.00 ng.hr/ml, and
(c) an AUC(0-∞) ranging from about 5600.00 ng.hr/ml to about 7900.00 ng.hr/ml.

Documents

Application Documents

# Name Date
1 201847045242.pdf 2018-11-30
2 201847045242-STATEMENT OF UNDERTAKING (FORM 3) [30-11-2018(online)].pdf 2018-11-30
3 201847045242-FORM 1 [30-11-2018(online)].pdf 2018-11-30
4 201847045242-DRAWINGS [30-11-2018(online)].pdf 2018-11-30
5 201847045242-COMPLETE SPECIFICATION [30-11-2018(online)].pdf 2018-11-30
6 Form-1_After Filing_21-02-2019.pdf 2019-02-21
7 Correspondence by Agent_Form-1_21-02-2019.pdf 2019-02-21
8 201847045242-FORM 3 [25-03-2019(online)].pdf 2019-03-25
9 201847045242-FORM 18 [28-03-2019(online)].pdf 2019-03-28
10 201847045242-FORM 3 [22-11-2019(online)].pdf 2019-11-22
11 201847045242-FER.pdf 2019-12-11
12 201847045242-FORM 3 [16-03-2020(online)].pdf 2020-03-16
13 201847045242-PETITION UNDER RULE 137 [09-06-2020(online)].pdf 2020-06-09
14 201847045242-FORM 3 [09-06-2020(online)].pdf 2020-06-09
15 201847045242-FER_SER_REPLY [09-06-2020(online)].pdf 2020-06-09
16 201847045242-DRAWING [09-06-2020(online)].pdf 2020-06-09
17 201847045242-COMPLETE SPECIFICATION [09-06-2020(online)].pdf 2020-06-09
18 201847045242-CLAIMS [09-06-2020(online)].pdf 2020-06-09
19 201847045242-Annexure [09-06-2020(online)].pdf 2020-06-09
20 201847045242-REQUEST FOR ADJOURNMENT OF HEARING UNDER RULE 129A [03-12-2020(online)].pdf 2020-12-03
21 201847045242-US(14)-HearingNotice-(HearingDate-09-12-2020).pdf 2021-10-17
22 201847045242-US(14)-ExtendedHearingNotice-(HearingDate-09-02-2021).pdf 2021-10-17
23 201847045242-US(14)-ExtendedHearingNotice-(HearingDate-05-05-2021).pdf 2021-10-17

Search Strategy

1 2019-12-0911-47-16_09-12-2019.pdf