Penicillin G sodium salt, The Chinese name is penicillin sodium, which is a typical β - lactam antibiotic. The appearance is a white to off white crystalline powder with hygroscopicity. It is highly soluble in water, soluble in ethanol, and insoluble in fatty oil, liquid paraffin. When exposed to acids, bases, oxidants, penicillinase, etc., it can cause the β - lactam ring of penicillin to open and become ineffective. Crystalline penicillin sodium salt has relatively stable properties, but its aqueous solution is prone to failure at room temperature and cannot be boiled for disinfection. It mainly interferes with the synthesis of bacterial cell walls, acts as a bactericidal agent during bacterial reproduction, and has antibacterial effects on Gram positive bacteria (G ⁺) and some Gram negative bacteria (G ⁻), including diphtheria, tetanus, anthrax bacteria, spirochetes, Clostridium difficile, actinomycetes, and some Bacteroides. At the same time, it is mainly used in clinical practice for the treatment of bacterial infections such as streptococcus, pneumococcal, and meningococcal. Moreover, when combined with cholestyramine, it can reduce the absorption of penicillin sodium, possibly due to the binding of penicillin to cholestyramine; When combined with Jiangdanning, the plasma level of penicillin sodium decreased by 78% 79%, and the area under the plasma concentration time curve (AUC) decreased by 75% 85%; When used in combination with methotrexate, the competition for tubular secretion can reduce the renal clearance rate of methotrexate and increase its toxicity.
Additional information of chemical compound:
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Chemical Formula |
C16H17N2O4S- |
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Exact Mass |
333.09 |
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Molecular Weight |
333.38 |
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m/z |
333.09(100.0%),334.09(17.3%),335.09(4.5%),335.10(1.4%) |
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Elemental Analysis |
C, 57.64; H, 5.14; N, 8.40; O, 19.20; S, 9.62 |
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Melting point |
209-212℃ |
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Density |
1.41 |
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Storage conditions |
2-8℃ |
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Penicillin G Sodium Salt, also known as penicillin G sodium salt, is an important raw material for antibiotics. The manufacturing process of this substance involves several key steps, including strain selection, fermentation cultivation, extraction and purification, crystallization and drying, as well as formulation processing. The following is a detailed description of the manufacturing information.
Strain Selection and Fermentation Cultivation
The production of penicillin G sodium salt begins with the selection of the strain. Currently, Penicillium chrysogenum is the main production strain in industry. Through mutagenesis breeding or genetic engineering methods, high-yield and stable strains can be obtained. These strains are cultivated in specific media, such as liquid media containing lactose, corn starch, phosphate, etc. During the fermentation process, parameters such as temperature, pH value, and dissolved oxygen content need to be strictly controlled to optimize the growth of the strain and the synthesis of penicillin G. Generally, the fermentation period lasts from several days to one week, and after the fermentation is completed, the concentration of penicillin G in the fermentation broth can reach a certain level.
Extraction and Purification
After the fermentation process is completed, the fermentation broth needs to be extracted and purified to obtain high-purity penicillin G. This process usually involves the following steps:
Filtering: Firstly, the fungus bodies and other solid impurities in the fermentation broth are removed through filtration, resulting in a clear filtrate.
Extraction: By taking advantage of the distribution coefficient difference of penicillin G between organic solvents and aqueous phase, the organic solvent (such as butyl acetate, ethyl acetate, etc.) is used for extraction to transfer penicillin G from the aqueous phase to the organic phase.
Re-extraction: The organic phase containing penicillin G is contacted with an alkaline aqueous solution to transfer penicillin G in the form of sodium salt to the aqueous phase, achieving the preliminary purification of penicillin G.
Decolorization and Filtration: Through activated carbon decolorization and filtration, impurities are further removed to improve the purity of penicillin G.
Crystallization and Drying
After extraction and purification, the penicillin G sodium salt solution obtained needs to undergo crystallization and drying to obtain a solid product. The crystallization process is usually carried out by controlling parameters such as temperature, concentration, and pH to make penicillin G sodium salt crystallize in the form of crystals. Subsequently, through filtration, washing, and drying steps, dry penicillin G sodium salt crystals are obtained. During this process, strict control of crystallization conditions and drying temperature is required to avoid product degradation or increase in impurity content.
Preparation Processing
The sodium salt crystals of penicillin G can be further processed into various dosage forms, such as powder injectables for injection and injection solutions. During the preparation process, appropriate excipients (such as stabilizers, solubilizers, etc.) need to be added, and steps like sterilization and aseptic filling are carried out to ensure the quality and safety of the preparations. For example, the injectable powder of penicillin G sodium salt usually requires mixing penicillin G sodium salt with an appropriate amount of glucose or sodium chloride and other excipients evenly, and then conducting filling and sterilization processes.
Quality Control
Quality control is a crucial step in the manufacturing process of penicillin G sodium salt. From strain selection to formulation processing, each step requires strict quality control to ensure that the purity and activity of the product meet the standards. For example, during the fermentation process, the content of penicillin G in the fermentation broth and the growth of the strain need to be regularly monitored; in the extraction and purification process, the yield and purity changes of each step need to be monitored; in the formulation processing, indicators such as pH value, sterility, and content uniformity of the formulation need to be tested.
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Penicillin G Sodium Salt is a widely used β-lactam antibiotic in clinical practice. Its core mechanism of action is to exert bactericidal effects by inhibiting the synthesis of bacterial cell walls. It is particularly effective against Gram-positive bacteria and some Gram-negative bacteria. The following explains its usage from five aspects: administration route, dosage adjustment, medication for special populations, combination therapy, and precautions.
Administration Route and Indications
Penicillin G sodium salt can be administered via intravenous injection (IV) or intramuscular injection (IM). The specific route of administration depends on the severity of the infection and the patient's condition.
Intravenous injection
Suitable for severe infections or scenarios where a rapid effective blood drug concentration needs to be achieved, such as sepsis, meningitis, endocarditis, etc. For example, when treating meningitis caused by sensitive bacteria, the adult daily dose can reach 24 million units, administered intravenously in 4-6 divided doses. The treatment course varies depending on the pathogen and lasts 10-21 days.
Muscle injection
Used for mild to moderate infections, such as streptococcal pharyngitis, skin and soft tissue infections, etc. The conventional adult dose is 800,000-2,000,000 units per day, administered in 3-4 divided doses. It is important to choose a large muscle area (such as the gluteus maximus) for injection to reduce local pain.
Dose Adjustment Principles
The dose should be dynamically adjusted according to the type of infection, the sensitivity of the pathogen, and the patient's physiological condition:
Infection type: For patients with meningitis, due to increased permeability of the blood-brain barrier, a higher dose is required (for example, for Streptococcus pneumoniae meningitis, 2-4 million units/kg per day, administered in multiple doses); while urinary tract infections may have a higher concentration of the drug in urine, the dose can be appropriately reduced.
Renal insufficiency: Penicillin G is mainly excreted through the kidneys. Patients with impaired renal function need to adjust the dose according to the creatinine clearance rate. For example, when the creatinine clearance rate is 30-50 ml/min, the dose is halved; when it is lower than 10 ml/min, the administration interval is extended to 12-18 hours.
Children and the elderly: The dose for children is calculated based on body weight (500,000-2,000,000 units/kg per day), while for the elderly, due to reduced renal function, the dose should be adjusted carefully and renal function should be closely monitored.
Medication for Special Populations
Pregnant and lactating women
Penicillin G sodium salt is classified as Category B by the FDA. Its use during pregnancy is relatively safe, but the indications must be strictly controlled; after lactating women take the medication, the drug can be slightly secreted into breast milk, but usually no interruption of breastfeeding is necessary.
Newborns
Premature infants, due to immature liver and kidney functions, need to have a longer dosing interval (such as once every 12 hours) and their blood drug concentrations should be monitored to avoid toxicity.
Allergic patients
Before taking the medication, a detailed history of allergies must be inquired and a skin test (such as penicillin skin test) should be conducted. If the skin test is positive, penicillin and cephalosporin classes should be prohibited (cross-allergy risk), and other antibiotics should be used instead.
Drug Combination and Interactions
Synergistic effect
When used in combination with aminoglycosides (such as gentamicin), it can enhance the bactericidal effect against Gram-negative bacteria. However, it is necessary to be aware of the nephrotoxicity of aminoglycosides and avoid mixing and dripping them in the same container.
Antagonistic effect
When used in combination with antibacterial agents such as tetracyclines and chloramphenicol, the efficacy may be reduced because the antibacterial agents can inhibit bacterial reproduction and reduce the target sites of penicillin G.
Drug interactions
When used in combination with probenecid (butazolidin), it can reduce the renal tubular secretion of penicillin G, prolong its half-life, but be vigilant of toxicity accumulation; when used in combination with anticoagulants (such as warfarin), it may enhance the anticoagulant effect, and monitoring of coagulation function is required.
Precautions for Medication Use
Drug compatibility contraindications
The sodium salt solution of penicillin G is prone to deteriorate at room temperature. It should be prepared and used immediately, and it must not be mixed with calcium-containing solutions (such as Ringer's solution) to avoid precipitation.
Adverse reaction monitoring
Common adverse reactions include allergic reactions (such as rash, urticaria, and severe cases can lead to anaphylactic shock), electrolyte disorders (large-dose intravenous infusion may cause hypernatremia), and central nervous system toxicity (such as convulsions, which are more common in cases of renal insufficiency or excessive dosage).
Course management
After the infection symptoms subside, the medication should be continued until the end of the course (for streptococcal pharyngitis, it needs to be taken for 10 days) to avoid recurrence or the emergence of drug-resistant bacteria.
FAQ
1. Question: Why is penicillin G administered intravenously in clinical settings and not in the form of an oral tablet?
Answer: The main reason is that the chemical structure of penicillin G is extremely unstable. It will be rapidly and almost completely hydrolyzed and lose its efficacy in the highly acidic stomach acid. Therefore, it cannot achieve an effective blood concentration through oral administration and must be administered by bypassing the digestive tract (such as intramuscular or intravenous injection). This is one of the key differences between it and many modern penicillin-based drugs.
2. Question: Where did the unit "international unit" for penicillin G come from, and why is it not expressed in milligrams like modern drugs?
Answer: Penicillin G was initially extracted from microbial fermentation broth as a mixture. Its purity and activity could not be accurately measured by weight. Therefore, the scientific community defined the "international unit" based on its inhibitory effect on standard Staphylococcus aureus, which was a way to measure its potency. Even though high-purity crystals can now be produced, due to historical conventions and the continuity of clinical medication, the "unit" is still used for indication (approximately 1 milligram equals 1667 units), reflecting the early history of the antibiotic industry.
3. Question: Why is Penicillin G referred to as one of the "narrow-spectrum" penicillins? What challenges does this pose for modern medication?
Answer: Penicillin G is mainly highly effective against Gram-positive cocci in the proliferative phase, some bacilli, and a few Gram-negative cocci (such as Neisseria gonorrhoeae). Its antibacterial spectrum is very "classic" and narrow. In modern clinical practice, due to widespread drug resistance, it is mainly limited to treating pathogens that are still highly sensitive to it, such as Treponema pallidum, Streptococcus, and Neisseria meningitidis, among a few infections. Therefore, although it is the "ancestor", it has become a "precise" weapon that requires precise diagnosis as support, rather than a broad-spectrum first-choice drug.
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