Slow released antituberculotic preparation
A tuberculosis, slow-release agent technology, applied in the field of anti-tuberculosis drug slow-release agents, can solve the problems of difficult to obtain effective bactericidal concentration, increased dosage, and unsatisfactory effect of multidrug-resistant tuberculosis
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Embodiment 1
[0098] Put 90, 90 and 80 mg of polyphenylpropane (p-carboxyphenylpropane (p-CPP): sebacic acid (SA) at 20:80) copolymers into (A), (B) and (C) three Add 100 ml of dichloromethane to each container, dissolve and mix well, add 10 mg rifampicin, 10 mg rifamycin, 10 mg rifampicin and 10 mg rifamycin respectively, re-shake and spray dry Microspheres for injection containing 10% rifampicin, 10% rifamycin and 10% rifampicin and 10% rifamycin were prepared by method. Then suspend the microspheres in physiological saline containing 15% mannitol to prepare the corresponding suspension-type sustained-release injection. The viscosity of the injection is 300cp-600cp (at 20°C-30°C). The drug release time of the sustained release injection in physiological saline in vitro is 15-20 days, and the drug release time in mice subcutaneous is about 30-40 days.
Embodiment 2
[0100] The method step of being processed into slow-release injection is identical with embodiment 1, but difference is that contained anti-tuberculosis active ingredient and weight percentage thereof are:
[0101] (a) 2-40% rifampicin, rifamycin, rifapentine or utilbutin;
[0102] (b) 2-40% rifampicin in combination with 2-40% rifamycin, rifapentine or rifabutin;
[0103] (c) 2-40% rifamycin in combination with 2-40% rifapentine or rifabutin;
[0104] (d) Combination of 2-40% rifapentine and 2-40% urbutin.
Embodiment 3
[0106] Put 70 mg of polylactic acid (PLGA, 75:25) with a peak molecular weight of 65,000 into three containers (A), (B) and (C) respectively, and then add 100 ml of dichloromethane to each, dissolve and mix well , add 30mg rifampicin, 30mg rifapentine, 15mg rifampicin and 15mg rifapentine into three containers respectively, shake up again and use spray drying method to prepare 30% rifampicin, 30% rifapentine 15% rifampicin and 15% rifapentine injection microspheres. The dried microspheres are suspended in physiological saline containing 1.5% sodium carboxymethylcellulose to prepare the corresponding suspension-type sustained-release injection. The viscosity of the injection is 300cp-600cp (at 20°C-30°C). The drug release time of the slow-release injection in physiological saline in vitro is 10-15 days, and the drug release time in mice subcutaneous is about 20-30 days.
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