Formulation preference, tolerability and quality of life assessment following a switch from lopinavir/ritonavir soft gel capsule to tablet in human immunodeficiency virus-infected patients

Abstract

BackgroundLopinavir/ritonavir (LPV/r) tablet compared to the soft gel capsule (SGC) formulation has no oleic acid or sorbitol, has no refrigeration or food-restriction requirements, and has less pharmacokinetic variability. We compared the tolerability, quality of life (QoL), and formulation preference after switching from LPV/r SGC to the tablet formulation.MethodsIn a prospective, single-arm, cohort study-design, 74 human immunodeficiency virus (HIV) infected subjects stable on LPV/r-based therapy were enrolled prior to (n = 25) or 8 weeks (n = 49) after switching from SGC to tablet. Baseline data included clinical laboratory tests, bowel habit survey (BHS) and QoL questionnaire (recalled if enrolled post-switch). Global Condition Improvement (GCI)-score, BHS-score, QoL-score, and formulation preference data were captured at weeks 4 and 12.ResultsAt week 12 post-enrollment; the tablet was preferred to the SGC (74% vs. 10%, p < 0.0001). GCI-overall-tolerability score was 2.46 ± 3.30 on a scale of -7 to +7, with 90% admitting to feeling better or about the same. Stool frequency, consistency, volume, and ± blood improved, however the improvement was significant in "consistency" only (p = 0.03). Aggregate Bowel Habit-Profile improved (BHS-score change = -0.227, p = 0.01). Inverse relationship existed between GCI and BHS (slope = -1.2, p = 0.02) at week-4, suggesting that improved overall-tolerability was related to better gastrointestinal (GI)-tolerance. QoL-scores were stable. Mean reductions in total cholesterol of 9.20 mg/dL (p = 0.02), in triglycerides of 33 mg/dL (p = 0.04), and in HDL of 4.50 mg/dL (p = 0.01) unrelated to lipid-lowering therapy, were observed at week 12.ConclusionsLPV/r-tablet was well tolerated and preferred to the SGC in HIV infected subjects, with stable QoL and appreciable improvement in GI-tolerability. The unexpected changes in lipid profile deserve further evaluation.

Lopinavir/Ritonavir Dosage Form Affects Quality of Life During Monotherapy in HIV-Positive Adults

“…Our findings are consistent with 3 studies evaluating quality of life, tolerability, and satisfaction in patients who were switched from the SGC to the tablet formulation. 11,24,25 Diarrhea has been associated with increased health care costs, lost work days, need for assistance with care, and is a negative predictor of survival. [26][27][28] In a prospective caseÀcontrol study of 192 HIV-infected participants with and without diarrhea, MOS-HIV quality-of-life scores were significantly higher in all domains for participants without diarrhea (average differences ranged from þ8 for physical and cognitive functioning to þ19 for social functioning) and significantly associated with diarrhea severity.…”

Palm Oil in Lipid-Based Formulations and Drug Delivery Systems

“…The pharmaceutical industry and drug manufacturers favour LBF because of improved drug-loaded bioavailability profile [66,67,68], safeness for consumption [69], a good profile of drug absorption [70], protection provided to the loaded drug in formulation [71], reducing food effect [72] and promoting high drug payload despite its low dose formulation [73]. On the contrary, the disadvantages of LBF include oxidation of excipient, specific storage requirement, higher frequency of drug intake required compared to solid dosage form and, to some extent, GIT-adverse effects [74,75]. Among the latest Federal Drug Administration (FDA) approved LBF drugs are calcifediol [76], nintedanib [77], enzalutamide [78], isotretinoin [79] and loratadine [80].…”