Formulation for controlled release of drugs by combining hydrophilic and hydrophobic agents
a technology of hydrophilic and hydrophobic agents, applied in the field of biodegradable implants, can solve the problems of insufficient medical treatment of ocular diseases, insufficient use of ocular diseases,
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example 1
Manufacture and Testing of a Drug Delivery System (DDS) without a Release Modulator
[0042] Release of the hydrophobic drug dexamethasone from an extended release drug delivery system was measured. The drug delivery system was made with dexamethasone and polylactic acid / polyglycolic acid copolymer. Dexamethasone powder and a powder of polylactic acid polyglycolic acid (PLGA) copolymer were mixed throughly at a ratio of 50 / 50. The well mixed powder was filled into an extruder, and heated for 1 hour at 95° C., then extruded through a 20 gauge orifice. Six DDS of approximately 100-120 μg were cut from the extruded filaments for drug release assessment.
[0043] Each individual DDS was placed in a glass vial filled with receptor medium (9% NaCl in water). To allow for “infinite sink” conditions, the receptor medium volume was chosen so that the concentration would never exceed 5% of saturation. To minimize secondary transport phenomena, e.g. concentration polarization in the stagnant bound...
example 2
Manufacture and Testing of A DDS with a Pharmaceutically Active Release Modifier
[0046] A drug delivery system was manufactured as described in Example 1, except that ciprofloxacin HCl, a pharmaceutically active, hydrophilic compound, was included as a release modifier. The combinations of drug, polymer and HPMC shown in Table 2 were used.
TABLE 2ReleaseLot #PLGAModifierDrugXT0295—5 dexamethasoneXT03242 ciprofloxacin4 dexamethasoneXT0305—5 ciprofloxacin
[0047] The release of dexamethasone is increased with the addition of ciprofloxacin HCl, as shown by the data in FIG. 2A. The actual drug release is almost doubled when compared to the DDS without a modifier. In addition to the benefits of increased drug delivery, there are therapeutic benefits introduced with the antibiotic activity of ciprofloxacin. The release of ciprofloxacin from from the same DDS is shown in FIG. 2B. The release rate is higher than that of dexamethasone. However, the overall release of ciprofloxacin is slower ...
example 3
Manufacture and Testing of A DDS with Multiple Release Modifiers
[0048] A drug delivery system was formulated with hydroxymethylcellulose, cirpofloxacin HCl and dexamethasone, according to the Table 3.
TABLE 3Lot #PLGAHPMCCiprofloxacinDexamethasoneXT0353.40.42.43.8
The data show that after an initial higher release in the first day, an almost zero-order release there after can be observed. The overall release characteristic would be therapeutically acceptable from a therapeutic efficiency aspect.
[0049] It is evident from the above results that biodegradable implants formulated with an active agent and release modulator provide for release kinetics where the drug is released at a constant rate over long periods of time, avoiding the need of a patient to administer drugs in much less effective ways, such as topically. The implants provide an improved method of treating ocular and other conditions, by avoiding peaks and troughs of drug release.
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