GB2596184A

GB2596184A - Non-aqueous solutions for oral dosage

Info

Publication number: GB2596184A
Application number: GB2105225.3A
Authority: GB
Inventors: Nagar Swati; Mehta Sandip; Umrethia Manish; Mandal Jayanta
Original assignee: Lm Mfg Ltd; FTF Pharma Pvt Ltd
Current assignee: Lm Mfg Ltd; FTF Pharma Pvt Ltd
Priority date: 2018-09-13
Filing date: 2019-09-13
Publication date: 2021-12-22
Also published as: WO2020053662A2; GB202105225D0; WO2020053662A3

Abstract

Pharmaceutical compositions comprising a vehicle, a solubilizer, and a surfactant are disclosed to be used in conjunction with non-chemotherapeutic active pharmaceutical ingredients which are water soluble, or insoluble, or which are sensitive to water, but miscible in oil. Such non-chemotherapeutic active pharmaceutical ingredients may include topiramate, felodipine, fesoterodine, isradipine, nifedipine, nimodipine, nisoldipine, sodium valproate, omeprazole, Esomeprazole, Rabeprazole, Pentoprazole, methimazole, a derivative thereof, or a combination thereof. The pharmaceutical compositions may be administered as an oral solution. Other embodiments are directed towards methods of using and methods of making such formulations.

Claims

1. A pharmaceutical composition comprising an active pharmaceutical ingredient, a solubilizer, a surfactant, and a vehicle, wherein the active pharmaceutical ingredient is present at about 0.01 wt% to about 30 wt% of the composition; the surfactant is present from about 1 wt% to about 10 wt% of the composition; the solubilizer is present from about 0.1 wt% to about 40 wt% of the composition; the vehicle is present from about 0. 1 wt% to about 99 wt % of the composition; and wherein the composition is a non-aqueous solution.

2. The pharmaceutical composition of claim 1, wherein the active pharmaceutical ingredient is selected from topiramate, felodipine, fesoterodine, isradipine, nifedipine, nimodipine, nisoldipine, sodium valproate, omeprazole, Esomeprazole, Rabeprazole, Pentoprazole, methimazole, a derivative thereof, and a combination thereof.

3. The pharmaceutical composition of claim 1, wherein the active pharmaceutical ingredient is topiramate.

4. The pharmaceutical composition of claim 1, wherein the solubilizer is an alcohol.

5. The pharmaceutical composition of claim 1, wherein the solubilizer is selected from ethanol, propylene glycol, glycerol, polyvinyl alcohol, propylene glycol, ethylene glycol, and a combination thereof

6. The pharmaceutical composition of claim 1, wherein the surfactant is selected from sorbitan esters, polyethoxylated sorbitan esters, Caprylocaproyl macrogol-8 glycerides, Lauroyl macrogol-32 glycerides, stearoyl macrogol- 32 glycerides, polyethoxylated castor oil, hydroginated castor oil, PEG-40 hydrogenated castor oil, PEG-60 hydrogenated castor oil, PEG-35 castor oil, polyoxyl 35 castor oil, Macrogol (25) cetostearyl ether, polyethoxylated ethers, polyethylene glycol, poloxamer, alpha tocopherol, polyoxyethylene lauryl ether, polyvinyl caprolactam-polyvinylacetate- polyethyleneglycol graft copolymer, PEG-35 castor oil, polyoxyl 35 castor oil, and a combination thereof.

7. The pharmaceutical composition of claim 1, wherein the vehicle is selected from caproic acid (C6), caprylic acid (C8), capric acid (C10), lauric acid (C12), coconut oil, arachis oil, soya bean oil, castor oil, com oil, safflower oil, olive oil, apricot kernel oil, sesame oil, cotton seed oil, sunflower seed oil, palm oil, rapeseed oil, mineral oil, vegetable oil, caproic triglyceride, caprylic triglyceride, capric triglyceride, lauric triglyceride, medium-chain (6 to 12 carbons) fatty acid esters of glycerol, coconut oil, Kollisolv, palm kernel oil, camphor tree drupes, or a combination thereof.

8. The pharmaceutical composition of claim 1, wherein the composition comprises the active pharmaceutical ingredient in a therapeutically effective amount.

9. The pharmaceutical composition of claim 1, wherein the composition comprises the active pharmaceutical ingredient in an amount of about 1 mg/mL to about 50 mg/mL.

10. The pharmaceutical composition of claim 1, wherein the composition comprises the solubilizer in an amount of about 0.1 wt% to about 10 wt% of the composition.

11. The pharmaceutical composition of claim 1, wherein the composition comprises the surfactant in an amount of about 1 wt% to about 5 wt% of the composition.

12. The pharmaceutical composition of claim 1, wherein the active pharmaceutical ingredient is topiramate, the solubilizer is ethanol, the surfactant is polyethoxylated glyceride, and the vehicle is a medium chain triglyceride.

13. The pharmaceutical composition of claim 1, wherein the composition comprises about 0.01 wt% to about 2 wt% of the active pharmaceutical ingredient, about 1 wt% to about 5 wt% of the surfactant, about 0.1 wt% to about 5 wt% of the solubilizer, and about 0.1 wt% to about 90 wt% of the vehicle.

14. The pharmaceutical composition of claim 1, wherein the composition comprises about 2 wt% topiramate, about 3 wt% caprylocaproyl macrogol-8 glyceride, about 5 wt% ethanol, about 89.8 wt% medium chain triglyceride, and further comprises about 0.03 wt% sucralose, and 0.2 wt% flavoring agent.

15. A method of treating a disease or disorder in a subject in need thereof, the method comprising administering a pharmaceutical composition in the form of a liquid oral solution comprising topiramate, a solubilizer, a surfactant, and a vehicle.

16. The method of claim 15, wherein the disease or disorder is selected from the group consisting of seizures, partial onset seizures, seizures associated with Lennox-Gastaut syndrome, generalized tonic-clonic seizures, migraine headaches, bipolar disorder, epilepsy, alcoholism, ***e and tobacco addiction, diabetes, neuropathic pain, diabetic neuropathic pain, obesity, sleep disorders, sleep-related eating disorders, post-traumatic stress disorder, depression, cluster headaches, and a combination thereof.