Uzbelger Feldman Daniel, Laun Billy B, Patel Chirag, Pande Sonal V, Boddu Sai H S
Department of Endodontology, Temple University Kornberg School of Dentistry, 3223 N. Broad Street, Philadelphia, PA 19140, USA.
Oral & Maxillofacial Surgery Carbondale, 1111 E. Walnut St Suite B, Carbondale, IL 62901, USA.
Pharmaceutics. 2024 Aug 12;16(8):1058. doi: 10.3390/pharmaceutics16081058.
Lidocaine hydrochloride (HCl) 2% with 1:100,000 epinephrine (LW/E) is widely used to prevent pain during dental procedures and has been associated with injection sting, jittering effects, slow onset, and a bitter aftertaste. Since LW/E's introduction in 1948, no significant modifications have been proposed. This study aims to design and characterize an improved dental lidocaine HCl injectable formulation without epinephrine (LW/O/E) via buffers, sweeteners, and amino acids. LW/O/E injections were prepared with pH and osmolality values of 6.5-7.0 and 590-610 mOsm/kg. Using the electronic tongue (ETongue), the LW/O/E injectable formulations were characterized for viscosity, injectability, and taste analysis. The results were compared with the LW/E control. In vivo efficacy and anesthetic duration of the samples were measured through radiant heat tail-flick latency (RHTFL) and hot plate (HP) tests and local toxicity was assessed after a single intra-oral injection in Sprague Dawley rats (SDR). The viscosity and injectability values of the LW/O/E samples were found to be comparable to the LW/E injection. ETongue taste analysis showed an improvement in bitterness reduction of the LW/O/E samples compared to the LW/E formulation. Toxicity studies of samples in SDR showed minor and transient signs of erythema/eschar and edema. Anesthetic duration via RHTFL and HP paw withdrawal latency time in SDR were found to be comparable for the LW/O/E Sample 3A and the LW/E injection ( < 0.05). In conclusion, the buffered, higher osmolality and reduced bitterness developed LW/O/E formulation (Sample 3A) could be considered a promising alternative to the LW/E formulation for dental use.
2%盐酸利多卡因与1:100,000肾上腺素（LW/E）被广泛用于预防牙科手术中的疼痛，但其与注射刺痛、震颤效应、起效缓慢和回味苦涩有关。自1948年LW/E问世以来，尚未提出重大改进方案。本研究旨在通过缓冲剂、甜味剂和氨基酸设计并表征一种不含肾上腺素的改良牙科用盐酸利多卡因注射剂配方（LW/O/E）。制备的LW/O/E注射液的pH值和渗透压分别为6.5 - 7.0和590 - 610 mOsm/kg。使用电子舌（ETongue）对LW/O/E注射剂配方的粘度、注射性和味道进行分析。将结果与LW/E对照进行比较。通过辐射热甩尾潜伏期（RHTFL）和热板（HP）试验测量样品的体内疗效和麻醉持续时间，并在Sprague Dawley大鼠（SDR）单次口腔内注射后评估局部毒性。发现LW/O/E样品的粘度和注射性值与LW/E注射液相当。电子舌味道分析表明，与LW/E配方相比，LW/O/E样品的苦味降低有所改善。SDR中样品的毒性研究显示有轻微和短暂的红斑/焦痂和水肿迹象。发现SDR中通过RHTFL和HP爪退缩潜伏期时间评估的LW/O/E样品3A和LW/E注射液的麻醉持续时间相当（<0.05）。总之，所开发的具有缓冲、较高渗透压和降低苦味的LW/O/E配方（样品3A）可被视为牙科用LW/E配方的一种有前景的替代品。
