Absorption, Distribution and Excretion
Penicillin G is rapidly absorbed after both intramuscular and subcutaneous injection. Initial blood concentrations are high after parenteral administration, but the duration of absorption is short. In healthy individuals on an empty stomach, oral absorption is only about 15-30% because it is readily hydrolyzed by acid. Penicillin G is primarily excreted via the kidneys. Non-renal clearance routes include hepatic metabolism and a small amount of bile excretion. The daily blood concentration in adults with normal renal function is 0.53-0.67 L/kg. The daily blood concentration in healthy individuals is 560 ml/min. …Widely distributed throughout the body…its apparent volume of distribution accounts for approximately 50% of total body fluids. Over 90% of the drug in the blood is found in plasma, and less than 10% is found in red blood cells; approximately 65% is reversibly bound to plasma albumin. Low protein concentration…low binding degree…drug efficacy. Significant active drug components are found in the liver, bile, kidneys, semen, lymph, and intestines. ...When the meninges are normal, penicillin does not readily enter the cerebrospinal fluid. After oral administration of 500 mg potassium penicillin, the urinary penicillin concentration is 600 μg/mL within 2 hours and 300 μg/mL within 4 hours. ...The low placental transport efficiency is consistent with the low lipid solubility and low ionization constant of penicillin G, and there is no evidence of placental transport. ...It is rapidly cleared from the body, primarily through the kidneys, but in small amounts through bile and other routes. Due to incomplete renal development, clearance is significantly lower in newborns and infants... For more complete data on the absorption, distribution, and excretion of penicillin G (21 types), please visit the HSDB records page.

---

Metabolism/Metabolites
Approximately 16-30% of the intramuscular dose is metabolized to penicillic acid, an inactive metabolite. Small amounts of 6-aminopenicillanic acid have been detected in the urine of patients taking penicillin G. Small amounts of the drug appear to be hydroxylated into one or more active metabolites, which are also excreted in the urine. Approximately 16-30% of intramuscularly injected penicillin G sodium is metabolized to penicillic acid, which is microbiologically inactive. Small amounts of 6-aminopenicillanic acid (6-APA) have also been found in the urine of patients treated with penicillin G. Furthermore, the drug appears to undergo minor hydroxylation, generating one or more microbiologically active metabolites, which are also excreted in the urine.
Biological Half-Life
The biological half-life of penicillin in adults with normal renal function is reported to be 0.4-0.9 hours.
The elimination half-life in normal adults is approximately 30 minutes.
The half-life of penicillin in human serum increases from approximately 25 minutes in young adults to 2 hours in older adults, and drugs actively secreted by the renal tubules also have a significantly prolonged half-life. /Penicillin/
The half-life of penicillin G in the serum of adults with normal renal function is reported to be 0.4-0.9 hours.
The half-life of penicillin G in neonatal serum is inversely proportional to age and appears to be independent of birth weight. According to reports, the serum half-life of newborns aged 6 days and under is 3.2-3.4 hours, that of newborns aged 7-13 days is 1.2-2.2 hours, and that of newborns aged 14 days and over is 0.9-1.9 hours.

Use of Penicillin G During Pregnancy and Lactation ◉ Overview of Use During Lactation
Limited information suggests that low concentrations of penicillin G in breast milk are not expected to have adverse effects on breastfed infants. There are reports that penicillin-type drugs occasionally disrupt the infant's gut microbiota, leading to diarrhea or thrush, but these effects have not been fully assessed. Penicillin G is safe for use by breastfeeding women. ◉ Effects on Breastfed Infants
A one-month-old breastfed infant with congenital syphilis developed a Herxheimer reaction 6 hours after his mother received an intramuscular injection of 2.4 million units of benzathine penicillin G. However, the infant also received 10 units of penicillin G concurrently with the mother's injection. This reaction was likely caused by penicillin in the breast milk. ◉ Effects on Lactation and Breast Milk
No relevant published information was found as of the revision date.

---

Protein Binding
Bound to serum proteins (45-68%), primarily albumin.

---

Interaction
A 49-year-old male patient reported that high-dose parenteral administration of penicillin G significantly enhanced the hypoprothrombinemia effect of warfarin. Penicillin G induces a warfarin-protein binding substitution interaction.
Penicillin is generally inactivated in the presence of high temperatures, alkaline or acidic pH, oxidants, alcohols, ethylene glycols, and metal ions such as copper, mercury, or zinc. Currently marketed penicillin drugs will completely lose their antibacterial activity if any part of their core structure (including the β-lactam ring) is broken. The main cause of penicillin inactivation is the hydrolysis of the β-lactam ring. The hydrolysis process and the nature of the degradation products can vary and are generally affected by pH. /Penicillin/
Penicillin G may have physical and/or chemical incompatibility with some drugs, including aminoglycosides and tetracyclines, but this compatibility depends on a variety of factors (e.g., drug concentration, specific diluent used, final pH, temperature).
Penicillin is typically inactivated by high temperatures, alkaline or acidic pH levels, oxidizing agents, alcohols, ethylene glycols, and the presence of metal ions such as copper, mercury, or zinc. Currently marketed penicillin drugs will completely lose their antibacterial activity if any part of the molecular core (including the β-lactam ring) is broken. The main cause of penicillin inactivation is the hydrolysis of the β-lactam ring. The hydrolysis process and the properties of the degradation products can vary and are generally affected by pH. /Penicillin/
For more complete data on the interactions of penicillin G (18 types), please visit the HSDB record page.

Therapeutic Uses

Constipation; GABA modulator; Penicillin
Gingivitis, lung infections, and genital diseases caused by the synergistic effects of Fusobacterium nucleatum (fusiform bacteria) and spirochetes present in the respiratory tract can be easily treated with penicillin. /Penicillin/
Two microorganisms that cause rat-bite fever are sensitive to penicillin G. ...It is the first-line drug for treating mononuclear infections...The only Pasteurella bacteria highly sensitive to penicillin is Pasteurella multocida. The pathogen of erysipelas is sensitive to penicillin.
Penicillin G is almost ideal for treating syphilis; it is a safe, inexpensive, and highly effective drug. ...It is the first-line drug for treating all clinical manifestations of actinomycosis, anthrax, and gas gangrene.
For more complete data on the therapeutic uses of penicillin G (35 types), please visit the HSDB records page.
Drug Warnings

When using high doses of penicillin G sodium, a large sodium load is introduced, which can dilate the extracellular space and may cause edema in patients with heart failure. Penicillin G Sodium: Hypersensitivity reactions to the procaine component are possible, but other toxic effects of procaine are very rare. Anuria can prolong the half-life of penicillin G from the normal 0.5 hours to approximately 10 hours. While penicillin G preparations for inhalation therapy and topical application to the skin and mucous membranes (PrePN) are still available, their use is not recommended due to a lack of sufficient evidence of their efficacy and a high incidence of hypersensitivity reactions. For more complete data on drug warnings for penicillin G (23 in total), please visit the HSDB records page. Pharmacodynamics: Penicillin G is a penicillin-type β-lactam antibiotic used to treat bacterial infections caused by susceptible strains, typically Gram-positive bacteria. The name "penicillin" can refer to several existing penicillin derivatives or to a class of antibiotics derived from penicillin. Penicillin G has in vitro activity against Gram-positive and Gram-negative aerobic and anaerobic bacteria. The bactericidal activity of penicillin G stems from its inhibition of cell wall synthesis and exerts its effect by binding to penicillin-binding proteins (PBPs). Penicillin G is stable against the hydrolytic activity of a variety of β-lactamases, including penicillinase, cephalosporinase, and extended-spectrum β-lactamase.

C16H18N2O4S

334.4

334.098

61-33-6

Penicillin G potassium;113-98-4;Penicillin G sodium salt;69-57-8;Streptomycin;57-92-1;Penicillin G procaine hydrate;6130-64-9;Penicillin G benzathine;1538-09-6;Penicillin G benzathine tetrahydrate;41372-02-5;Penicillin G-d7 potassium;352323-25-2

5904

AMORPHOUS WHITE POWDER

1.4±0.1 g/cm3

663.3±55.0 °C at 760 mmHg

214-217 °C
214 - 217 °C

355.0±31.5 °C

0.0±2.1 mmHg at 25°C

1.655

1.67

112.01

2

5

4

23

530

3

CC1([C@@H](N2C([C@@H](NC(CC3=CC=CC=C3)=O)[C@H]2S1)=O)C(O)=O)C

JGSARLDLIJGVTE-MBNYWOFBSA-N

InChI=1S/C16H18N2O4S/c1-16(2)12(15(21)22)18-13(20)11(14(18)23-16)17-10(19)8-9-6-4-3-5-7-9/h3-7,11-12,14H,8H2,1-2H3,(H,17,19)(H,21,22)/t11-,12+,14-/m1/s1

(2S,5R,6R)-3,3-dimethyl-7-oxo-6-[(2-phenylacetyl)amino]-4-thia-1-azabicyclo[3.2.0]heptane-2-carboxylic acid

Galofak CilopenBenzylpenicillin Pradupen

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)

May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples

注意: 如下所列的是一些常用的体内动物实验溶解配方，主要用于溶解难溶或不溶于水的产品（水溶度<1 mg/mL）。 建议您先取少量样品进行尝试，如该配方可行，再根据实验需求增加样品量。

---

注射用配方1: DMSO : Tween 80： Saline = 10 : 5 : 85 (如： 100 μL DMSO → 50 μL Tween 80 → 850 μL Saline)
*生理盐水/Saline的制备：将0.9g氯化钠/NaCl溶解在100 mL ddH ₂ O中，得到澄清溶液。
注射用配方 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (如： 100 μL DMSO → 400 μL PEG300 → 50 μL Tween 80 → 450 μL Saline)
注射用配方 3: DMSO : Corn oil = 10 : 90 (如： 100 μL DMSO → 900 μL Corn oil)
示例: 以注射用配方 3 (DMSO : Corn oil = 10 : 90) 为例说明, 如果要配制 1 mL 2.5 mg/mL的工作液, 您可以取 100 μL 25 mg/mL 澄清的 DMSO 储备液，加到 900 μL Corn oil/玉米油中, 混合均匀。

View More

注射用配方 4: DMSO : 20% SBE-β-CD in Saline = 10 : 90 [如：100 μL DMSO → 900 μL (20% SBE-β-CD in Saline)]
*20% SBE-β-CD in Saline的制备（4°C，储存1周）：将2g SBE-β-CD (磺丁基-β-环糊精) 溶解于10mL生理盐水中，得到澄清溶液。
注射用配方 5: 2-Hydroxypropyl-β-cyclodextrin : Saline = 50 : 50 (如： 500 μL 2-Hydroxypropyl-β-cyclodextrin (羟丙基环胡精)→ 500 μL Saline)
注射用配方 6: DMSO : PEG300 : Castor oil : Saline = 5 : 10 : 20 : 65 (如： 50 μL DMSO → 100 μL PEG300 → 200 μL Castor oil → 650 μL Saline)
注射用配方 7: Ethanol : Cremophor : Saline = 10： 10 : 80 (如： 100 μL Ethanol → 100 μL Cremophor → 800 μL Saline)
注射用配方 8: 溶解于Cremophor/Ethanol (50 : 50), 然后用生理盐水稀释。
注射用配方 9: EtOH : Corn oil = 10 : 90 (如： 100 μL EtOH → 900 μL Corn oil)
注射用配方 10: EtOH : PEG300：Tween 80 : Saline = 10 : 40 : 5 : 45 (如： 100 μL EtOH → 400 μL PEG300 → 50 μL Tween 80 → 450 μL Saline)

---

口服配方 1: 悬浮于0.5% CMC Na (羧甲基纤维素钠)
口服配方 2: 悬浮于0.5% Carboxymethyl cellulose (羧甲基纤维素)
示例: 以口服配方 1 (悬浮于 0.5% CMC Na)为例说明, 如果要配制 100 mL 2.5 mg/mL 的工作液, 您可以先取0.5g CMC Na并将其溶解于100mL ddH2O中，得到0.5%CMC-Na澄清溶液；然后将250 mg待测化合物加到100 mL前述 0.5%CMC Na溶液中，得到悬浮液。

View More

口服配方 3: 溶解于 PEG400 (聚乙二醇400)
口服配方 4: 悬浮于0.2% Carboxymethyl cellulose (羧甲基纤维素)
口服配方 5: 溶解于0.25% Tween 80 and 0.5% Carboxymethyl cellulose (羧甲基纤维素)
口服配方 6: 做成粉末与食物混合

---

注意: 以上为较为常见方法，仅供参考， InvivoChem并未独立验证这些配方的准确性。具体溶剂的选择首先应参照文献已报道溶解方法、配方或剂型，对于某些尚未有文献报道溶解方法的化合物，需通过前期实验来确定（建议先取少量样品进行尝试），包括产品的溶解情况、梯度设置、动物的耐受性等。

---

请根据您的实验动物和给药方式选择适当的溶解配方/方案：
1、请先配制澄清的储备液(如：用DMSO配置50 或 100 mg/mL母液(储备液));
2、取适量母液，按从左到右的顺序依次添加助溶剂，澄清后再加入下一助溶剂。以 下列配方为例说明 (注意此配方只用于说明，并不一定代表此产品 的实际溶解配方):
10% DMSO → 40% PEG300 → 5% Tween-80 → 45% ddH2O (或 saline);
假设最终工作液的体积为 1 mL, 浓度为5 mg/mL: 取 100 μL 50 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀/澄清；向上述体系中加入50 μL Tween-80，混合均匀/澄清；然后继续加入450 μL ddH2O (或 saline)定容至 1 mL；
3、溶剂前显示的百分比是指该溶剂在最终溶液/工作液中的体积所占比例;
4、 如产品在配制过程中出现沉淀/析出，可通过加热(≤50℃)或超声的方式助溶;
5、为保证最佳实验结果，工作液请现配现用！
6、如不确定怎么将母液配置成体内动物实验的工作液，请查看说明书或联系我们;
7、 以上所有助溶剂都可在 Invivochem.cn网站购买。