Methods and dosage forms for increasing solubility of drug compositions for controlled delivery
A composition, low solubility technology, applied in the field of increasing the solubility of pharmaceutical active agents to promote the controlled delivery of pharmaceutical active agents, high doses of poorly soluble drugs in solid dosage form systems, can solve related problems such as limited capacity
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Embodiment 1
[0158] Method for implementing the invention
[0159] The drug layer of the present invention is prepared as follows. Aqueous solutions of 5 surfactants were prepared. The surfactants chosen were 4 grades of ethylene oxide / propylene oxide / ethylene oxide (Lutrol grades F127, F87, F108 and F68) and PEG-40 stearate (Myrj 52). Solutions were prepared at concentrations of 1, 5 and 15 weight percent. If necessary, the aqueous surfactant blend was cooled to facilitate complete dissolution of the surfactant prior to dosage form drug solubility studies. Each surfactant has a different HLB value and ranges from 16.9-29 HLB units.
[0160] The aqueous surfactant solution was then equilibrated to a constant temperature in a water bath at 37°C. Neat topiramate drug was then added slowly while stirring, in approximately 10 mg increments into the surfactant solution, until no more drug was dissolved. A drug control sample dissolved in deionized water without surfac...
Embodiment 2
[0175] A drug core composition of 9.0 grams of micronized Lutrol F 127 was dry mixed with 16.5 grams of topiramate. Topiramate has a nominal particle size of 80 microns. Next 3.45 grams of Polyox N80 and 0.9 grams of polyvinylpyrrolidone were screened below 40 mesh and blended into the mixture. Then 5 grams of absolute ethanol was added slowly while stirring to form a wet mass. Pass the wet mass through a #16 mesh screen and air dry overnight at ambient temperature. Pass the resulting dried noodles through a #16 mesh sieve again. Then 150 mg magnesium stearate was passed through a #60 mesh screen over the dried granules and tumble blended into the granules. The concentration of the surfactant in the drug core composition particles is 30% by weight.
[0176] Swellable push layer particles were prepared by passing 63.67 grams of Polyox 303, 30 grams of sodium chloride, and 5 grams of hydroxypropyl methylcellulose through a #40 mesh screen and dry mixing into a homogeneous bl...
Embodiment 3
[0181] The system was prepared as described in Example 2, except that Surfactant 33 included a blend of two solubilizing surfactants. The drug core composition particles were prepared according to the procedure in Example 2, but the surfactant consisted of 15 weight percent micronized Lutrol F 127 and 15 weight percent Myrj 52 instead of 30 weight percent micronized Lutrol F127. The weighted average of the HLB of the two surfactants yielded an HLB value of 19.5, which is midway between the HLB values of the two single surfactants.
[0182] The delivery mode of the resulting system is attached Figure 11 shown in . The system delivered at an essentially zero order rate between hours 4-12. The system released 88% of the dose within 24 hours.
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