| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| 50mg |
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| 100mg |
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| Other Sizes |
| Targets |
HPMCAS does not have a defined pharmacological target. It is a pharmaceutical excipient that functions by improving the solubility and bioavailability of poorly soluble drugs. Its mechanism of action is physicochemical: it forms solid dispersions with drug molecules, inhibiting drug crystallization and maintaining the drug in an amorphous, high-energy state that enhances dissolution and absorption.
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|---|---|
| ln Vitro |
In vitro, HPMCAS is used as a cosolvent for preparing solid dispersions (SDDs) of low-solubility agents. The polymer inhibits drug crystallization and maintains supersaturation of the drug in dissolution media. It is evaluated in dissolution studies to assess its ability to enhance the release and solubility of poorly soluble drugs compared to the pure drug or other formulations.
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| ln Vivo |
Rats treated with 2.5 g/kg po; single dose of hydroxypropylmethyl cellulose acetate succinate do not exhibit any appreciable acute toxicity [1]. Rats treated once a day for two months, six days a week, with 0.63, 1.25, and 2.5 g/kg of hydroxypropylmethyl cellulose acetate succinate po showed no appreciable subchronic toxicity [1]. Rats administered 1.25 g/kg or 2.5 g/kg of hydroxypropylmethyl cellulose acetate succinate orally once daily for two months, six days a week, did not exhibit substantial chronic toxicity [1].
In vivo, HPMCAS is used in pharmaceutical formulations to improve the oral bioavailability of poorly soluble drugs. It has been shown to be orally effective in animal models. When formulated as a solid dispersion, HPMCAS can significantly increase the area under the curve (AUC) and maximum concentration (Cmax) of poorly soluble drugs. |
| Enzyme Assay |
For in vitro dissolution testing, HPMCAS-based solid dispersions are evaluated using USP dissolution apparatus. The formulations are placed in dissolution media (e.g., simulated gastric fluid, simulated intestinal fluid) at 37°C, and samples are taken at various time points to measure drug concentration by HPLC. The ability of HPMCAS to maintain supersaturation is assessed by comparing dissolution profiles with the pure drug and other formulations.
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| Cell Assay |
For in vitro cell-based experiments, HPMCAS is not typically used directly in cell culture. It is a pharmaceutical excipient used to formulate drug-polymer solid dispersions that are subsequently tested in cell-based assays. The polymer's biocompatibility and lack of cytotoxicity make it suitable for use in oral drug delivery formulations.
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| Animal Protocol |
In vivo animal studies using HPMCAS are conducted to evaluate the oral bioavailability of drug-HPMCAS solid dispersions. Rodents are administered the formulations via oral gavage, and blood samples are collected at various time points. Plasma drug concentrations are measured by LC-MS/MS, and pharmacokinetic parameters such as Cmax, Tmax, AUC, and bioavailability are calculated and compared with the pure drug.
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| ADME/Pharmacokinetics |
Pharmacokinetic properties of HPMCAS as a standalone compound are not applicable, as it is a pharmaceutical excipient rather than a drug. The polymer is not significantly absorbed from the gastrointestinal tract. It is used to improve the pharmacokinetics of co-administered drugs by enhancing their solubility and dissolution.
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| Toxicity/Toxicokinetics |
HPMCAS is generally considered non-toxic and biocompatible. It exhibits no acute, subchronic, or chronic toxicity in rats, with an oral LD₅₀ > 2.5 g/kg. The compound is approved for use as a pharmaceutical excipient in various drug formulations. Standard laboratory safety practices should be followed when handling the compound.
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| References | |
| Additional Infomation |
See also: Hydroxypropyl methylcellulose acetate succinate 06081224 (3 Mm2/S) (Note moved to); Hydroxypropyl methylcellulose acetate succinate 12070923 (3 Mm2/S) (Note moved to); Hydroxypropyl methylcellulose acetate succinate 16070722 (3 Mm2/S) (Note moved to).
Hydroxypropylmethyl cellulose acetate succinate (HPMCAS, CAS 71138-97-1) is a pharmaceutical excipient, not an FDA-approved drug. Its primary applications are as a cosolvent for preparing solid dispersions of low-solubility drugs, as a coating agent, binder, and matrix former in drug delivery systems. No clinical trials or approved therapeutic indications exist for this compound as a drug. |
| Molecular Formula |
C10H22O9
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|---|---|
| Molecular Weight |
286.2763
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| Exact Mass |
286.126
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| CAS # |
71138-97-1
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| PubChem CID |
121950
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| Appearance |
White to off-white solid powder
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| Hydrogen Bond Donor Count |
6
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| Hydrogen Bond Acceptor Count |
9
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| Rotatable Bond Count |
4
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| Heavy Atom Count |
19
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| Complexity |
147
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| Defined Atom Stereocenter Count |
0
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| SMILES |
CC(CO)O.CC(=O)O.CO.C(CC(=O)O)C(=O)O
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| InChi Key |
ZUAAPNNKRHMPKG-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C4H6O4.C3H8O2.C2H4O2.CH4O/c5-3(6)1-2-4(7)8;1-3(5)2-4;1-2(3)4;1-2/h1-2H2,(H,5,6)(H,7,8);3-5H,2H2,1H3;1H3,(H,3,4);2H,1H3
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| Chemical Name |
acetic acid;butanedioic acid;methanol;propane-1,2-diol
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| HS Tariff Code |
2934.99.9001
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| 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)
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| Solubility (In Vitro) |
DMSO: 100 mg/mL
H2O: < 0.1 mg/mL |
|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (Infinity mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. Solubility in Formulation 2: ≥ 2.5 mg/mL (Infinity mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 3.4931 mL | 17.4654 mL | 34.9308 mL | |
| 5 mM | 0.6986 mL | 3.4931 mL | 6.9862 mL | |
| 10 mM | 0.3493 mL | 1.7465 mL | 3.4931 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
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.
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