D9-THC for Marijuana Addiction

描述（由申请人提供）：？9-四氢大麻酚（？9-THC）已被证明可以缓解大麻戒断症状，因此具有治疗大麻素依赖的潜力。然而，生物利用度？9-口服四氢大麻酚的效果较差，且变化不定。此外，它还需要每天多次给药。提高生物利用度和/或降低给药频率的制剂预计将提高？9-四氢大麻酚 在第一阶段，我们的技术目标是开发改进的口服和/或贮库制剂？9-THC基于生物制药原理，并选择具有可接受的体外控释特性的稳定制剂。? 9-THC是非常疏水和氧敏感的，这两个因素都是制备口服生物可利用和稳定的制剂的挑战。利用专有的超流体（商标）技术，我们建议封装？9-THC在可生物降解的聚合物纳米球，将允许运输到胃，提高其稳定性和提高生物利用度。 在II期，我们将对开发的制剂进行药理学、毒理学和药代动力学评价。我们还将提供在动物模型和/或人体中具有可接受的体外和体内生物利用度的稳定剂型的GMP放大。 叙述：开发的控制释放，口服制剂？9-THC将被商业化用于治疗大麻依赖和戒断症状、癌症疼痛、与癌症化疗相关的恶心和艾滋病恶病质或消瘦。

DESCRIPTION (provided by applicant): ?9-tetrahydrocannabinol (?9-THC) has been shown to alleviate marijuana withdrawal symptoms and thus has potential for treating cannabinoid dependence. However, the bioavailability of ?9-THC administered orally is poor and variable. In addition, it also requires drug administration several times a day. Formulations to improve bioavailability and/or to reduce dosing frequency would be expected to improve the therapeutic effectiveness of ?9-THC. In Phase I, our technical objectives are to develop improved oral and/or depot formulations of ?9-THC based on biopharmaceutical rationale, and select a formulation that is stable with acceptable in vitro controlled release characteristics. ?9-THC is very hydrophobic and oxygen-sensitive, both factors that are challenges in making formulations that are orally bioavailable and stable. Utilizing proprietary SuperFluids(tm) technologies, we propose to encapsulate ?9-THC in biodegradable polymer nanospheres that will allow transport to the stomach, improve its stability and enhance bioavailability. In Phase II, we will carry out pharmacological, toxicological and pharmacokinetic evaluations of the developed formulation(s). We will also provide a GMP scale-up of a stable dosage form with acceptable in vitro and in vivo bioavailability in animal models and/or in humans. Narrative: The developed controlled release, oral formulation of ?9-THC will be commercialized for treating marijuana dependence and withdrawal symptoms, cancer pain, nausea associated with cancer chemotherapy and AIDS cachexia or wasting.