PHARMACEUTICAL COMPOSITIONS CONTAINING ANHYDROUS CALCIPOTRIENE
A stable pharmaceutical composition in a semisolid dosage form comprising a therapeutic effective amount of solubilized calcipotriene in an anhydrous form is disclosed.
1 . (canceled)
2 . A stable pharmaceutical composition in a semisolid dosage form comprising a therapeutic effective amount of anhydrous calcipotriene in a solubilized form, wherein the calcipotriene has no more than about 0.5% of a single unknown impurity, as measured by HPLC, at 40° C. and 75% relative humidity after three months.
3 . (canceled)
4 . The composition of claim 2 , wherein the anhydrous calcipotriene is solubilized form in oil or a non-aqueous water soluble solvent.
5 . The composition of claim 4 , wherein the oil is selected from a mineral oil, vegetable oil, silicon oil, lanolin, refined animal oil, hydrocarbon ester derived from a plant-derived oil, marine-derived oil or animal-derived oil and mixtures thereof.
6 . The composition of claim 5 , wherein the vegetable oil is selected from isopropyl myristate, jojoba oil, almond oil, avocado oil, coconut oil, capric-caprylic triglyceride of fractionated coconut oil, nutmeg oil, PEG-6 apricot kernel oil, castor oil, olive oil and oleic acid, soybean oil, sunflower oil, peanut oil, canola oil and mixtures thereof.
7 . The composition of claim 4 , wherein the non-aqueous water soluble solvent is selected from polyethylene glycol, propylene glycol, glycerin, caffeine, xanthene, gentisic acid, cyclodextrin, isopropyl alcohol and mixture thereof.
8 . The composition of claim 4 , wherein the anhydrous calcipotriene is present in a concentration of about 0.001% to about 0.1% w/w.
9 . The composition of claim 8 , is in the form of a cream, a gel, a lotion, or paste.
10 .- 12 . (canceled)
13 . The composition of claim 4 , further comprising one or more pharmaceutically acceptable excipients.
14 . (canceled)
15 . A process for the preparation of a stable pharmaceutical composition in a semisolid dosage form comprising a therapeutic effective amount of anhydrous calcipotriene in a solubilized form comprising: (a) preparing an oil phase comprising solubilized calcipotriene in an anhydrous form; (b) preparing an aqueous phase comprising one or more buffering agents; (c) adding the oil phase of (a) to the aqueous phase of (b); and (d) emulsifying and homogenizing the product of (c).
16 . (canceled)
17 . The process of claim 15 , wherein the anhydrous calcipotriene is present in a concentration of about 0.001% to about 0.1% w/w.
18 . The process of claim 17 , wherein the pharmaceutical composition is in the form of a cream, a gel, a lotion, or paste.
19 . The process of claim 15 , wherein the anhydrous calcipotriene is solubilized in oil or a non-aqueous water soluble solvent.
20 . The process of claim 19 , wherein the oil is selected from a mineral oil, vegetable oil, silicon oil, lanolin, refined animal oil, hydrocarbon ester derived from a plant-derived oil, marine-derived oil or animal-derived oil and mixtures thereof.
21 . The process of claim 20 , wherein the vegetable oil is selected from isopropyl myristate, jojoba oil, almond oil, avocado oil, coconut oil, capric-caprylic triglyceride of fractionated coconut oil, nutmeg oil, PEG-6 apricot kernel oil, castor oil, olive oil and oleic acid, soybean oil, sunflower oil, peanut oil, canola oil and mixtures thereof.
22 . The process of claim 19 , wherein the non-aqueous water soluble solvent is selected from a polyethylene glycol, propylene glycol, glycerin, caffeine, xanthene, gentisic acid, cyclodextrin, isopropyl alcohol and mixture thereof.
23 . The method of treatment to a mammal in need thereof comprising administering a stable pharmaceutical composition in a semisolid dosage form comprising a therapeutic effective amount of anhydrous calcipotriene in a solubilized form.
24 . (canceled)
25 . The method of claim 23 , wherein the calcipotriene has no more than about 0.5% of a single unknown impurity, as measured by HPLC, at 40° C. and 75% relative humidity after three months.
26 .- 37 . (canceled)
38 . The process of claim 15 , wherein the calcipotriene has no more than about 0.5% of a single unknown impurity, as measured by HPLC, at 40° C. and 75% relative humidity after three months.