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Table 1 Summary of clinical and related trials of inhaled insulin

From: The lung as a route for systemic delivery of therapeutic proteins and peptides

   Subjects   
  Dosage forms/ (diabetics or   
Insulin doses delivery devices volunteers) Pharmacokinetic profiles and therapeutic outcome Reference
1–2 inhalations per dose Inhaled insulin 70 (type 1) HbA1c (%): 8.51 (INH), 8.53 (SC) [29]
    Pulmonary functions: no changes  
    Acceptance/preference of INH: ≥ 80%.  
1–2 inhalations per dose Inhaled insulin 51 (type 1) HbA1c (%): 8.7 (INH), 7.8 (SC) [30]
    Pulmonary functions: no changes  
    Acceptance/preference of INH: 92%  
250 U and 500 U AERx DMS 11 (volunteers) Tmax (min): 7 and 16 for INH 250 and 500 U, respectively [34]
    Cmax (μU/ml): 29.7 and 23.8 for INH 250 and 500 U, respectively  
    tGmax (min): 66 and 76 for INH 250 and 500 U, respectively  
4–6 inhalations per dose Inhaled insulin 16 (type 2) Baseline glucose change: 100 to 53 mg/dl (INH); [28]
    100 to 57 mg/dl (SC)  
    Pulmonary functions: no change  
    Reproducibility: INH similar to SC  
1–2 inhalations per dose AERx DMS 20 (type 1) Glucose change from baseline (mg/dl): 82 (60 min), 79 (120 min) and –11 (300 min) for AERx DMS; [36]
    89 (60 min), 82 (120 min) and –25 (300 min) for SC  
    Deleterious effect: none  
1–2 inhalations per dose Inhaled insulin 69 (type 2) Baseline HbA1c (%) before therapy: 9.92 (oral agent alone); 9.78 (oral agent + INH) [38]
    Change in HbA1c (%) after 2 weeks: –0.13 (oral agent alone); 2.28 (oral agent + INH)  
100 U TI MedTone inhaler (TI) 12 (type 2) GIRmax (mg/kg per min): 5.8 (INH), 2.2 (SC) [25]
  (PDC)   GIRtmax (min) = 55 (INH), 276 (SC)  
  USA   Early tGIR50% (min): 17 (INH), 122 (SC)  
    Late tGIR50% (min): 128 (INH), 335 (SC)  
Not mentioned Inhaled insulin 70 (type 1) Preference of INH over SC: 81% [32]
    Switch from SC to INH: 79%  
    Continuance of SC: 21%  
    Satisfaction: 38% (INH), 14% (SC)  
    Convenience/ease of use: 46% (INH), 12% (SC)  
Not mentioned Inhaled insulin Number not stated HbA1c (%): 8.9 (baseline), 8.0 (after 3 months), 8.1 (after 12 months), 8.0 (after 18 months), 8.0 (after 24 months) [33]
   (type 1 and type 2)   
    FEV1 (l): 3.2 (baseline), 3.1 (after 12 months), 3.1 (after 18 months), 3.2 (after 24 months)  
    DLCO (ml/min per mmHg): 25.6 (baseline), 24.7 (after 12 months), 24.7 (after 18 months), 24.4 (after 24 months)  
Not mentioned Inhaled insulin 56 (type 2) Mean improvement in patient satisfaction (%): 38 (INH), [31]
    14 (SC)  
    INH preference to SC based on: ease of use, comfort and convenience  
0.3–1.8 U/kg AERx DMS 18 (type 1) Tmax (min): for INH 49, 48, 62 and 65 at doses 0.3, 0.6, 1.2 and 1.8 U/kg, respectively; for SC 119 at dose 0.12 U/kg [37]
    GIRmax (mg/kg per min): for INH 1.6, 2.5, 4.7 and 6.5 at doses 0.3, 0.6, 1.2 and 1.8 U/kg, respectively; for SC 3.2 at dose 0.12 U/kg  
    tGIRmax (min): for INH 94, 136, 157 and 218 at doses 0.3, 0.6, 1.2 and 1.8 U/kg, respectively; for SC 189 at dose 0.12 U/kg  
25–100 U MedTone inhaler (TI) 12 (volunteers) GIRmax (mg/kg per min): concentration dependent [26]
  (PDC)   GIRtmax (min): 47, 52, 56 for TI 25, 50 and 100 U, respectively; 192 for SC  
    Tmax (min): 12, 18, and 21 for TI 25, 50 and 100 U, respectively; for SC 153  
    Bioavailability (relative to SC for 3 h): 46, 42 and 28% for TI 25, 50 and 100 U, respectively  
  1. Cmax, maximum insulin concentration; DLCO, diffusion capacity; DMS, diabetic management system; FEV1, forced expiratory volume in 1 s; GIRmax, maximum glucose infusion rate; GIRtmax, time to maximum glucose infusion rate; HbA1c, glycated haemoglobin (glycaemic control index); INH, inhaled insulin; PDC, Pharmaceutical Discovery Corporation (Elmsford, NY, USA); SC, subcutaneous; tGIR50%, time to late half maximum glucose infusion rate; tGmax, time to maximum glycemic effect; Tmax, time to maximum concentration of insulin.