Absorption, Distribution and Excretion
The absorption of topically applied chloroquine varies considerably. Reported absorption rates range from 4.2% to 23.5% of the administered dose. This is considerably lower than that of oral formulations, which in the same study achieved an absorption rate as high as 67.6%. Chloroquine is primarily excreted in the urine as sulfate. Approximately 2% is excreted unchanged. Metabolisms/Metabolites 98% of the drug is converted to sulfate and excreted via the kidneys.

Chloroquinard is a monohydroxyquinoline with the structure quinoline-8-ol, substituted with a methyl group at position 2 and chlorine at positions 5 and 7. It is an antifungal and antibacterial drug, formerly used topically to treat skin conditions and vaginal infections. It possesses antibacterial, antiseptic, and antiprobiotic properties. It is an organochlorine compound and a monohydroxyquinoline. Chloroquinard was previously used under the brand name Sterosan as a topical antiseptic. In the 1950s, it was marketed as a non-iodine alternative and is not associated with sulfonamides or hormones. Currently, chloroquinard is approved by the European Medicines Agency for use in combination with progesterone acetate tablets to treat bacterial vaginosis. Chloroquinard is a standardized chemical allergen. The physiological effects of chloroquinard are achieved through increased histamine release and cell-mediated immunity. It is a topical anti-infective agent used to treat skin, gastrointestinal, and vaginal infections caused by fungi, protozoa, and certain bacteria. In animal studies, it can cause central nervous system damage, therefore parenteral administration is not recommended. It can also be used as a preservative, antibacterial agent, or deodorant. Drug Indications Chloroquinol has historically been used as a topical antiseptic for treating skin infections. In European countries, it is still used in combination with progesterone vaginal tablets to treat vaginal infections. Mechanism of Action The mechanism by which chloroquinol exerts its bactericidal effect is unclear. 8-hydroxyquinoline compounds are known to be bidentate chelators of various metal ions, which are important enzyme cofactors. However, the addition of exogenous metal ions does not appear to alter the minimum inhibitory concentration (MIC) of Mycobacterium tuberculosis, suggesting that its primary mechanism of action is not dependent on chelation. Pharmacodynamics Chloroquinolol has bactericidal activity against both Gram-positive and Gram-negative bacteria. It is more effective against Gram-positive bacteria, particularly Staphylococcus.

C10H7CL2NO

228.0747

226.99

72-80-0

6301

Light yellow to brown solid powder

1.5±0.1 g/cm3

350.7±37.0 °C at 760 mmHg

108-112 °C (dec.)(lit.)

165.9±26.5 °C

0.0±0.8 mmHg at 25°C

1.679

4.21

1

2

0

14

214

0

ClC1=C([H])C(=C(C2=C1C([H])=C([H])C(C([H])([H])[H])=N2)O[H])Cl

GPTXWRGISTZRIO-UHFFFAOYSA-N

InChI=1S/C10H7Cl2NO/c1-5-2-3-6-7(11)4-8(12)10(14)9(6)13-5/h2-4,14H,1H3

5,7-dichloro-2-methylquinolin-8-ol

2934.99.9001

Powder      -20°C    3 years

                     4°C     2 years

In solvent   -80°C    6 months

                  -20°C    1 month

Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)

DMSO : ~50 mg/mL (~219.23 mM)

Solubility in Formulation 1: ≥ 2.08 mg/mL (9.12 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% 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 20.8 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL.
Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution.

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Solubility in Formulation 2: ≥ 2.08 mg/mL (9.12 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 20.8 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly.

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 (Please use freshly prepared in vivo formulations for optimal results.)