| Size | Price | Stock | Qty |
|---|---|---|---|
| 25g |
|
||
| 50g |
|
||
| 100g |
|
||
| Other Sizes |
Gelucire 14/44 is an absorption enhancer that can improve the absorption of poorly absorbable drugs including insulin and calcitonin by pulmonary delivery.
| ln Vivo |
Gelucire 44/14 is a potentially effective and safe absorption enhancer that can be inhaled to help better absorb medications that are hard for the body to absorb, like calcitonin and insulin. The findings demonstrated that Gelucire 44/14 improved lung absorption of FD4, FD10, and FD70 to variable degrees in a concentration-dependent manner; the maximum absorption enhancement effect was observed when Gelucire 44/14 concentration reached 2.0%. (w/v). It was also discovered that the molecular weight of the model drug is connected to Gelucire Gelucire 44/14's capacity to promote absorption. Gelucire Gelucire 14/44 has the maximum absorption promotion ratio as the molecular weight of the model medication approaches 10,000. Da[1].
Gelucire 44/14 (0.1-2.0% w/v) enhanced the pulmonary absorption of poorly absorbable model drugs in rats in a concentration-dependent manner. The absorption enhancement was evaluated by measuring plasma concentration-time profiles or pharmacodynamic markers (plasma glucose for insulin, plasma calcium for calcitonin). [1] The maximal absorption-enhancing effect was observed at a concentration of 2.0% (w/v) Gelucire 44/14. [1] The absorption-enhancing effect of Gelucire 44/14 correlated with the molecular weight of the model drugs. The highest absorption enhancement ratio was observed for fluorescein isothiocyanate-dextran with an average molecular weight of 10,000 (FD10), with an enhancement ratio of 7.3 at 2.0% Gelucire 44/14. The enhancement ratios for FD70 (70,000 Da) and FD4 (4,400 Da) at the same concentration were 3.5 and 2.4, respectively. The absorption of low molecular weight 5(6)-carboxyfluorescein (CF, ~376 Da) was not significantly enhanced. [1] For therapeutic peptides/proteins, Gelucire 44/14 (2.0% w/v) increased the absorption enhancement ratio (based on pharmacodynamic effect) to 2.9 for both insulin and calcitonin. [1] |
|---|---|
| Animal Protocol |
The pulmonary absorption experiments were conducted in male Sprague Dawley rats (230-250 g). Rats were fasted overnight with free access to water. [1]
Rats were anesthetized with sodium pentobarbital (40 mg/kg, intraperitoneal injection). A tracheal incision was made, and a polyethylene tube was inserted. A single dose of 100 µL of the drug solution (with or without Gelucire 44/14) was injected into the lungs. [1] Blood samples (~0.25 mL) were collected from the jugular vein at predetermined time intervals up to 240 minutes post-administration. Plasma was separated by centrifugation for analysis. [1] |
| Toxicity/Toxicokinetics |
This study evaluated the potential pulmonary membrane toxicity of Gelucire 44/14 in rats. Four hours after intrapulmonary administration of Gelucire 44/14 (0.1%, 0.5%, 2.0% w/v), protein levels and lactate dehydrogenase (LDH) activity in bronchoalveolar lavage fluid (BALF) were not elevated compared to the control group (PBS), indicating no significant membrane damage or cellular leakage. [1]
Following exposure to Gelucire 44/14 (0.1–2.0% w/v), lung histology (H&E staining) showed no significant morphological changes, inflammatory cells, or necrotic/damaged cells compared to the control group. [1] Preliminary studies suggest that higher concentrations (5% w/v) of Gelucire 44/14 may cause mild mucosal toxicity, manifested as elevated protein levels in bronchoalveolar lavage fluid (BALF). Therefore, this study determined its safe and effective concentration range to be 0.1-2.0% (w/v). [1] |
| References | |
| Additional Infomation |
Gelucire 44/14 is an amphiphilic mixture consisting primarily of surfactants (monoesters and diesters of polyethylene glycol), cosurfactants (monoglycerides), and an oil phase (diglycerides and triglycerides). It is generally considered safe and inert. [1] Its mechanisms of promoting absorption may include: Gelucire 44/14-mediated reduction of alveolar tissue air-liquid interface surface tension, as a linear correlation has been observed between the enhanced absorption and the reduction of surface tension in insulin solution. [1] Given its hydrophilic-lipophilic balance, it may modulate P-glycoprotein activity. [1] It may open tight junctions between alveolar epithelial cells as it enhances the uptake of paracellular markers (fluorescein). [1]
|
| CAS # |
121548-04-7
|
|---|---|
| Appearance |
Off-white to light yellow ointment
|
| SMILES |
[Gelucire 14/44]
|
| HS Tariff Code |
2934.99.9001
|
| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
|
| Solubility (In Vitro) |
Ethanol : ~100 mg/mL
|
|---|---|
| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
Products are for research use only; We do not sell to patients
Copyright 2020 InvivoChem LLC | All Rights Reserved
