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    PH-MODULATED FORMULATIONS FOR PULMONARY DELIVERY
    2.
    发明申请
    PH-MODULATED FORMULATIONS FOR PULMONARY DELIVERY 审中-公开
    用于脉冲递送的PH调制配方

    公开(公告)号：US20100209538A1

    公开(公告)日：2010-08-19

    申请号：US12693739

    申请日：2010-01-26

    Applicant: David C. Cipolla ,  Igor Gonda

    Inventor： David C. Cipolla ,  Igor Gonda

    IPC: A61K33/24 ,  A61K31/43 ,  A61K31/545 ,  A61K31/65 ,  A61K31/496 ,  A61P11/00

    CPC classification number: A61K31/496 ,  A61K9/007 ,  A61K9/0078 ,  A61K9/12 ,  A61K31/43 ,  A61K31/545 ,  A61K31/65 ,  A61K33/24

    Abstract: An aerosolizable formulation comprised of a drug, a carrier and pH affecting component is disclosed. The drug is dissolved in the formulation at a concentration above which it remains in solution at neutral pH. This increases the concentration of the drug in solution making it possible to administer larger amounts of drug with the same or a smaller volume of formulation. When the formulation is aerosolized to small particles and inhaled into human lungs in small volumes (e.g. 0.05 to 0.5 mL) the fluids in the lungs neutralize the formulation causing the drug to participate out of solution. This results in the drug being delivered at a controlled rate below the rate at which drug is administered from a formulation initially at a neutral pH.

    Abstract translation: 公开了由药物，载体和pH影响组分组成的可雾化制剂。 将药物溶解在制剂中，浓度高于其，在中性pH下保留在溶液中。 这增加了溶液中药物的浓度，使得可以以相同或更小体积的制剂施用更大量的药物。 当将制剂雾化成小颗粒并以小体积（例如0.05至0.5mL）吸入人肺中时，肺中的流体中和制剂，导致药物从溶液中参与。 这导致以最初在中性pH下的制剂以低于药物施用速率的受控速率递送药物。

    PROCESSES FOR TASTE-MASKING OF INHALED FORMULATIONS
    4.
    发明申请
    PROCESSES FOR TASTE-MASKING OF INHALED FORMULATIONS 审中-公开
    吸入制剂的加工过程

    公开(公告)号：US20080138397A1

    公开(公告)日：2008-06-12

    申请号：US11876407

    申请日：2007-10-22

    Applicant: Jeffrey A. Schuster ,  David C. Cipolla ,  Stephen Farr

    Inventor： Jeffrey A. Schuster ,  David C. Cipolla ,  Stephen Farr

    IPC: A61K31/47 ,  A61K9/127 ,  A61P11/08

    CPC classification number: A61K31/47 ,  A61K9/0078 ,  A61K9/127 ,  A61K9/1273

    Abstract: The present invention provides novel processes and methodologies to minimize the bitter or otherwise unpleasant taste, to minimize the tendency to stimulate the cough reflex, or to minimize oropharyngeal deposition of medically-active compounds administered by the pulmonary/inhalation route and to deliver hydroxychloroquine (HCQ) either singularly or in combination with an antimalarial and aminoquinolone by the pulmonary/inhalation route in a sustained release or other formulation that minimizes the bitter or otherwise unpleasant taste of HCQ or any potential to stimulate the cough reflex, and to deliver a dopaminergic compound or its prodrug, including ABT-431 by the pulmonary/inhalation route in a sustained release or other formulation that minimizes the unpleasant taste of the drug or any potential to stimulate the cough reflex, and to deliver a lantibiotic, including duramycin by the pulmonary/inhalation route in a sustained release or other formulation that minimizes the unpleasant taste of the drug or any potential to stimulate throat irritation.

    Abstract translation: 本发明提供了最小化苦味或其他令人不快的味道的新方法和方法，以最小化刺激咳嗽反射的趋势，或最小化由肺/吸入途径施用的医用活性化合物的口咽沉积并递送羟氯喹（HCQ ）在持续释放或其它制剂中通过肺/吸入途径单独地或与抗疟药和氨基喹诺酮组合，其最小化HCQ的苦味或其他不愉快的味道或任何刺激咳嗽反射的潜力，并递送多巴胺能化合物或 其前药包括通过肺/吸入途径的持续释放或其它制剂中的ABT-431，其最小化药物的令人不快的味道或刺激咳嗽反射的任何潜能，以及通过肺/吸入递送包含耐久霉素的羊毛硫抗生素 以持续释放或其他使最不发达的方式制成的途径 药物的味道或任何刺激喉咙刺激的潜力。

    PROCESSES FOR TASTE-MASKING OF INHALED FORMULATIONS
    6.
    发明申请
    PROCESSES FOR TASTE-MASKING OF INHALED FORMULATIONS 审中-公开
    吸入制剂的加工过程

    公开(公告)号：US20110104259A1

    公开(公告)日：2011-05-05

    申请号：US12986884

    申请日：2011-01-07

    Applicant: Jeffrey A. Schuster ,  David C. Cipolla ,  Stephen Farr

    Inventor： Jeffrey A. Schuster ,  David C. Cipolla ,  Stephen Farr

    IPC: A61K9/127 ,  A61K9/12

    CPC classification number: A61K31/47 ,  A61K9/0078 ,  A61K9/127 ,  A61K9/1273

    Abstract: The present invention provides novel processes and methodologies to minimize the bitter or otherwise unpleasant taste, to minimize the tendency to stimulate the cough reflex, or to minimize oropharyngeal deposition of medically-active compounds administered by the pulmonary/inhalation route and to deliver hydroxychloroquine (HCQ) either singularly or in combination with an antimalarial and aminoquinolone by the pulmonary/inhalation route in a sustained release or other formulation that minimizes the bitter or otherwise unpleasant taste of HCQ or any potential to stimulate the cough reflex, and to deliver a dopaminergic compound or its prodrug, including ABT-431 by the pulmonary/inhalation route in a sustained release or other formulation that minimizes the unpleasant taste of the drug or any potential to stimulate the cough reflex, and to deliver a lantibiotic, including duramycin by the pulmonary/inhalation route in a sustained release or other formulation that minimizes the unpleasant taste of the drug or any potential to stimulate throat irritation.

    Abstract translation: 本发明提供了最小化苦味或其他令人不快的味道的新方法和方法，以最小化刺激咳嗽反射的趋势，或最小化由肺/吸入途径施用的医用活性化合物的口咽沉积并递送羟氯喹（HCQ ）在持续释放或其它制剂中通过肺/吸入途径单独地或与抗疟药和氨基喹诺酮组合，其最小化HCQ的苦味或其他不愉快的味道或任何刺激咳嗽反射的潜能，并递送多巴胺能化合物或 其前药包括通过肺/吸入途径的持续释放或其它制剂中的ABT-431，其最小化药物的令人不快的味道或刺激咳嗽反射的任何潜能，以及通过肺/吸入递送包含耐久霉素的羊毛硫抗生素 以持续释放或其他使最不发达的方式制成的途径 药物的味道或任何刺激喉咙刺激的潜力。

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