The study measured the plasma concentration-time profile of Parishin B in beagle dogs after intragastric administration of Tall Gastrodia capsules, but did not evaluate its in vivo pharmacological efficacy (e.g., anti-tumor, neuroprotective effects) in an animal disease model. [1]

Animals: Adult male beagle dogs (weighing approximately 12 kg) were used. [1]
Drug Administration: Dogs were fasted for 12 hours before administration. They were randomly divided into three groups and received a single intragastric administration of Tall Gastrodia capsule contents at doses of 0.125, 0.25, or 0.5 g/kg body weight. The capsule contents were ultrasonically dissolved in pure water to form suspensions with concentrations of 5, 10, and 20 mg/mL for administration. [1]
Blood Sampling: Serial blood samples (approximately 2.00 mL) were collected from the foreleg vein into heparinized tubes at time points of 10, 20, 30, 45, 60, 120, 180, 240, 480, 720, and 1440 minutes after administration. Plasma was separated by centrifugation and stored at -20°C until analysis. [1]

Absorption and Exposure: Following intragastric administration of Tall Gastrodia capsules to beagles, Parishin B was absorbed into the systemic circulation. Peak plasma concentration (Cmax) and time to peak concentration (Tmax) were dose-dependent. The mean Cmax values at low (0.125 g/kg), medium (0.25 g/kg), and high (0.5 g/kg) doses were 526 ± 143 ng/mL, 746 ± 320 ng/mL, and 1220 ± 562 ng/mL, respectively. The corresponding mean Tmax values were 1.25 ± 0.69 h, 1.80 ± 0.45 h, and 2.00 ± 0.71 h, respectively. [1]
Systemic exposure: The area under the plasma concentration-time curve (AUC(0-t)) from time zero to the last measurable time point also increased with increasing dose: 1550 ± 530 ng/mL·h for the low-dose group, 2700 ± 1130 ng/mL·h for the medium-dose group, and 4700 ± 2330 ng/mL·h for the high-dose group. A similar trend was observed in the AUC from time zero to infinity (AUC(0-∞)): 1570 ± 533 ng/mL·h for the low-dose group, 2720 ± 1140 ng/mL·h for the medium-dose group, and 4720 ± 2330 ng/mL·h for the high-dose group. [1]
Elimination: The mean elimination half-life (t1/2) of Parishin B was relatively short and consistent across the dose groups: 1.08 ± 0.11 hours for the low-dose group, 1.18 ± 0.29 hours for the medium-dose group, and 1.17 ± 0.22 hours for the high-dose group. [1]
Clearance and mean residence time: The mean plasma clearance (CL) for the three dose groups was 0.72 ± 0.39 L/h/kg, 0.78 ± 0.23 L/h/kg, and 1.11 ± 0.84 L/h/kg, respectively. The mean residence time (MRT(0-t)) from time zero to the last measurable time point was 2.25 ± 0.26 hours, 2.78 ± 0.42 hours, and 2.76 ± 0.44 hours, respectively. [1]
Metabolism/Transformation: Correlation analysis was performed on the compounds measured in this study. The study found a strong correlation between Parishin B and parishin E (mean correlation coefficient: 0.95), and a strong correlation between Parishin B and parishin (mean correlation coefficient: 0.76). This suggests that these parishin compounds may undergo biotransformation in vivo, consistent with reports in the literature that parishin can be metabolized into parishin B and other analogues. However, this study did not identify the specific metabolic pathways and enzymes. [1]

[1]. An Optimized and Sensitive Pharmacokinetic Quantitative Method of Investigating Gastrodin, Parishin, and Parishin B, C and E in Beagle Dog Plasma using LC-MS/MS after Intragastric Administration of Tall Gastrodia Capsules. Molecules. 2017 Nov 10;22(11).

[2]. Comparison of Bioactive Compounds and Antioxidant Activities of Maclura tricuspidata Fruit Extracts at Different Maturity Stages. Molecules. 2019 Feb 4;24(3).

Parishin B is a glycoside. It has been reported that Parishin B exists in Artemisia absinthium, and there are related data reports. Parishin B is one of the characteristic Parishin compounds found in the traditional Chinese medicine Gastrodia elata Blume. [1] In this study, the potential bioactive components of Gastrodia elata capsules, including Parishin B, gastrodin, Parishin, Parishin C and Parishin E, were quantitatively analyzed. [1] In this study, a highly sensitive LC-MS/MS method was established and validated for the simultaneous determination of the content of these five compounds in beagle plasma. The limit of quantification (LLOQ) of Parishin B was 0.40 ng/mL. The method showed good linearity (R² > 0.999) in the concentration range of 18–2000 ng/mL. Recovery from plasma ranged from 95.3% to 98.5%, with a matrix effect of 96.6% to 103%. [1] After administration of Tall Gastrodia capsules, the concentration of Parishin B was measured to be 2.258 mg/g. [1] Pharmacokinetic studies showed that the plasma concentration of Parishin B was about one-third that of gastrodin, making it one of the Parishin analogues with relatively high concentrations in vivo after capsule administration. [1]

C32H40O19

728.6486

728.216

174972-79-3

44715528

White to off-white solid powder

1.6±0.1 g/cm3

1048.2±65.0 °C at 760 mmHg

330.0±27.8 °C

0.0±0.3 mmHg at 25°C

1.650

-2.72

10

19

17

51

1130

10

C1=CC(=CC=C1COC(=O)CC(CC(=O)O)(C(=O)OCC2=CC=C(C=C2)O[C@H]3[C@@H]([C@H]([C@@H]([C@H](O3)CO)O)O)O)O)O[C@H]4[C@@H]([C@H]([C@@H]([C@H](O4)CO)O)O)O

UNLDMOJTKKEMOG-IWOWLDPGSA-N

InChI=1S/C32H40O19/c33-11-19-23(38)25(40)27(42)29(50-19)48-17-5-1-15(2-6-17)13-46-22(37)10-32(45,9-21(35)36)31(44)47-14-16-3-7-18(8-4-16)49-30-28(43)26(41)24(39)20(12-34)51-30/h1-8,19-20,23-30,33-34,38-43,45H,9-14H2,(H,35,36)/t19-,20-,23-,24-,25+,26+,27-,28-,29-,30-,32?/m1/s1

3-hydroxy-5-oxo-5-[[4-[(2S,3R,4S,5S,6R)-3,4,5-trihydroxy-6-(hydroxymethyl)oxan-2-yl]oxyphenyl]methoxy]-3-[[4-[(2S,3R,4S,5S,6R)-3,4,5-trihydroxy-6-(hydroxymethyl)oxan-2-yl]oxyphenyl]methoxycarbonyl]pentanoic acid

2934.99.9001

Powder      -20°C    3 years

                     4°C     2 years

In solvent   -80°C    6 months

                  -20°C    1 month

Note: This product requires protection from light (avoid light exposure) during transportation and storage.

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

H2O : ~50 mg/mL (~68.62 mM)
DMSO : ~50 mg/mL (~68.62 mM)

Solubility in Formulation 1: ≥ 2.5 mg/mL (3.43 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 25.0 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: ≥ 2.5 mg/mL (3.43 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.

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Solubility in Formulation 3: ≥ 2.5 mg/mL (3.43 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.

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