What Is Prednisolone?

Prednisolone (prednisolone) chemical name 11, 17, 21-trihydroxyprogesterone-1,4-diene-3,20-dione, white or off-white crystalline powder; odorless, slightly bitter ; Has moisture absorption. Dissolved in methanol or ethanol, slightly soluble in acetone or dioxane, slightly soluble in chloroform, and very slightly soluble in water. The molecular formula is C21H28O5, the molecular weight is 360.44400, the density is 1.31 g / cm3, the melting point is 240 ° C (dec.) (Lit.), and the boiling point is 570.6ºC at 760 mmHg.

Chinese name: Prednisolone
Foreign name: prednisolone

CAS number: 50-24-8
Molecular formula: C21H28O5

Introduction to Prednisolone compounds

Prednisone Basic Information

Chinese name:

Chinese alias: 11Beta, 17Alpha, 21-trihydroxyprogestin-1,4-diene-3,20-dione; 11, 17, 21-trihydroxyprogestin-1,4-diene-3,20- Dione; Progesterone-1,4-diene-11, 17, 21-triol-3,20-dione; 1,4-Pregnadiene-11, 17, 21-triol-3,20-dione; to Hydrocortisone;

English name: prednisolone

English alias: STEROLONE; ulacort; Pregna-1,4-diene-3,20-dione, 11,17,21-trihydroxy-, (11)-; steran; dicortol;

CAS number: 50-24-8

Molecular formula: C ₂₁ H ₂₈ O ₅

Molecular weight: 360.44400

Structural formula:

Exact mass: 360.19400

PSA: 94.83000

LogP: 1.55760

MDL number: MFCD00003649

EINECS number: 200-021-7

RTECS number: TU4152000

BRN number: 1354103

PubChem number: 24987725 ^[1]

Physical and Chemical Properties of Prednisone

Appearance and properties: crystalline solid

Density: 1.31 g / cm

Melting point: 240 ° C (dec.) (Lit.)

Boiling point: 570.6ºC at 760 mmHg

Flash point: 313ºC

Refractive index: 100 ° (C = 1, Dioxane)

Storage conditions: -20ºC Freezer ^[1]

Prednisone molecular structure data

1. Molar refractive index: 95.48

2. Molar volume (cm / mol): 274.7

3. Isotonic specific volume (90.2K): 766.8

4. Surface tension (dyne / cm): 60.7

5. Polarizability (10-24cm3): 37.85 ^[2]

Prednisone production method

Brief description of the production method: Griseofulvin is an antibiotic obtained by extracting from the culture fermentation broth of Penicilli-um griseofulvum. ^[1]

Prednisone uses

This product has an inhibitory effect on a variety of dermatophytes, including Dermatophytes, Dermatophytes and Microsporum. It is ineffective against Trichophyton versicolor, Candida albicans and Fine. This product acts as an antibacterial agent and is effective against vigorously growing fungi. This product is used for tinea capitis, onychomycosis, ringworm, tinea pedis and body ringworm caused by sensitive fungi. ^[1]

Prednisone Pharmacopoeia Standard

Prednisone source (name), content (potency)

This product is 11, 17, 21-trihydroxyprogesterone-1,4-diene-3,20-dione. Calculated on dry basis, containing C ₂₁ H ₂₈ O ₅ should be 97.0% 102.0%. ^[3]

Prednisone traits

This product is white or off-white crystalline powder; odorless, slightly bitter; hygroscopic.

This product is soluble in methanol or ethanol, slightly soluble in acetone or dioxane, slightly soluble in chloroform, and very slightly soluble in water.

The specific rotation is taken from this product, accurately weighed, dissolved in dioxane and quantitatively diluted to make a solution containing about 10 mg per 1ml. According to the law, the specific rotation is + 96 ° to + 103 °.

The absorption coefficient is taken from this product, accurately weighed, dissolved in ethanol and quantitatively diluted to make a solution containing about 10 g per 1 ml. According to the ultraviolet-visible spectrophotometry, the absorbance is measured at a wavelength of 243 nm, and the absorption coefficient is 400-430. ^[3]

Prednisone identification

(1) Take 10mg of this product, add 1ml of methanol to dissolve it, add 1ml of alkaline copper tartrate test solution, and heat to form an orange-red precipitate.

(2) Take about 2mg of this product, add 2ml of sulfuric acid, gradually dark red, no fluorescence; add 10ml of water, the red fades, and a gray flocculent precipitate is formed.

(3) In the chromatogram recorded under the content determination item, the retention time of the main peak of the test solution should be consistent with the retention time of the main peak of the reference solution.

(4) The infrared light absorption spectrum of this product should be the same as that of the control ("Infrared Spectra of Drugs" 284). ^[3]

Prednisone check

relative substance

Take this product, add chloroform-methanol (9: 1) to dissolve and dilute to make a solution containing about 3mg per Im1 as the test solution; take 2ml of precise amount, put it in a 100ml measuring bottle, and use chloroform Methanol (9: 1) is diluted to the mark, shake well, and used as a control solution. According to the thin layer chromatography test, draw 5 l of each of the two solutions, point them on the same silica gel G thin layer plate, and use dichloromethane-ether-methanol-water (77: 12: 6: 0.4) as the developing agent to develop. , Air-dried, dried at 105 ° C for 10 minutes, allowed to cool, sprayed with an alkaline tetrazolium blue test solution, and inspected immediately. For the test solution, if there are more than three spots of impurities, the color of the test solution must not be darker than the main spots of the control solution.

Loss on drying

Take this product and dry it at 105 to constant weight, and the weight loss shall not exceed 1.0%. ^[3]

Determination of prednisone content

As determined by high performance liquid chromatography.

Chromatographic conditions and system suitability tests

Octadecylsilane-bonded silica gel was used as the filler; methanol-water (65:35) was used as the mobile phase; the detection wavelength was 240 nm. The number of theoretical plates should not be less than 1000 as calculated by the prednisone peak. The resolution of the prednisone peak and the internal standard peak should be greater than 3.5.

Preparation of internal standard solution

Take norethindrone, add methanol to dissolve and dilute to make a solution containing about 1.5mg per 1ml.

Assay

Take this product, weigh it accurately, add methanol to dissolve and quantitatively dilute to make a solution containing about 1mg per 1ml; precisely measure 5ml each of this solution and the internal standard solution, place them in a 50ml measuring flask, dilute to the mark with methanol, Take 10l into the liquid chromatograph and record the chromatogram; take another prednisolone reference substance and measure it in the same way. Calculate the peak area according to the internal standard method. ^[3]

Prednisolone Compound Related Drugs

Prednisolone drug name:

[Common name] Prednisolone tablets

[English name] Prednisolone Tablets

[Chinese Pinyin] Po Ni Song Long Pian ^[4]

Prednisone category:

Chemical Drugs and Biological Products >> Tumor Drugs >> Antitumor Drugs >> Hormonal Antitumor Drugs

Chemicals & Biological Products >> Drugs Affecting Immune Function >> Immunosuppressants >> Adrenal Corticosteroids

Chemical Drugs and Biological Products >> Metabolic and Endocrine System Drugs >> Adrenal Corticosteroids >> Glucocorticoids ^[4]

Prednisone characteristics:

This product is a white tablet. ^[4]

Prednisone indications

Mainly used for allergic and autoimmune inflammatory diseases, collagen diseases such as rheumatism, rheumatoid arthritis, lupus erythematosus, severe bronchial asthma, nephrotic syndrome, thrombocytopenic purpura, granulocytopenia, acute lymph Leukemia, various adrenal insufficiency, exfoliative dermatitis, pemphigus, neurodermatitis, eczema, etc. ^[4]

Prednisone specifications:

5mg ^[4]

Prednisone usage dosage

It is used to treat allergic and inflammatory diseases. Adults start daily doses of 15-40 mg according to their severity, 60 mg when needed, or 0.5-1 mg / kg daily. Fever patients take three doses. Those with normal temperature start daily in the morning. One serving. After the disease is stable, it should be gradually reduced, and the maintenance amount is 5-10mg, depending on the condition. ^[4]

Prednisone adverse reactions:

Glucocorticoids have no obvious adverse effects when applying physiological dose replacement therapy, and most of the adverse reactions occur when applying pharmacological doses, and are closely related to the course of treatment, dose, usage and route of administration. The common adverse reactions are as follows:
1. Long-term use can cause the following side effects: iatrogenic Cushing's syndrome, face and body shape, weight gain, lower limb edema, purple markings, tendency to bleed easily, poor wound healing, acne, menstrual disorders, ischemic necrosis of the humerus or femoral head, bone Osteoporosis and fractures (including vertebral compression fractures, long bone pathological fractures), muscle weakness, muscle atrophy, hypokalemia syndrome, gastrointestinal irritation (nausea, vomiting), pancreatitis, peptic ulcer or perforation, child growth Suppressed, glaucoma, cataracts, benign intracranial pressure syndrome, impaired glucose tolerance, and exacerbation of diabetes.
2. Patients may experience psychiatric symptoms: euphoria, agitation, delirium, restlessness, disorientation, or depression. Mental symptoms include those who are prone to suffer from chronic wasting diseases and those who have had mental disorders in the past.
3 Concomitant infection is the main adverse reaction of adrenocortical hormone. Mainly fungi, tuberculosis, staphylococcus, proteus, Pseudomonas aeruginosa and various herpes viruses.
4 Glucocorticoid withdrawal syndrome. Sometimes patients have dizziness, fainting tendency, abdominal pain or back pain, low fever, loss of appetite, nausea, vomiting, muscle or joint pain, headache, fatigue, weakness after discontinuation of medication. Careful inspection can rule out adrenal insufficiency and the original disease. The re-ignition can be considered as glucocorticoid dependence syndrome. ^[4]

Prednisone taboo:

1. Those who are allergic to this product and other steroid hormones are contraindicated.
2. Patients with the following diseases are generally unsuitable for use. Special circumstances should be weighed against pros and cons, but attention should be paid to the possible deterioration of the condition: severe mental illness (past or present) and epilepsy, active peptic ulcer disease, recent gastrointestinal anastomosis, fractures, and trauma repair Corneal ulcers, adrenal hyperfunction, hypertension, diabetes, pregnant women, infections that cannot be controlled by antibacterials, such as chicken pox, measles, fungal infections, and severe osteoporosis. ^[4]

Prednisone precautions:

1. Induced infection: Under the action of hormones, the infection that has been controlled can move. The most common one is recurrence of tuberculosis infection. Application of hormones in certain infections can reduce tissue damage, reduce exudation, and reduce symptoms of infection poisoning, but must be treated with effective antibiotics at the same time, closely observe changes in the condition, after short-term medication, it should be quickly reduced and discontinued.
2. Interference to diagnosis:
(1) Glucocorticoids can increase blood glucose, blood cholesterol and blood fatty acids, blood sodium levels, and decrease blood calcium and potassium.
(2) The effect on peripheral blood image is decreased lymphocytes, eukaryotic cells, eosinophils, and basophils, multinucleated leukocytes and platelets, and the latter can also decrease.
(3) Long-term high-dose glucocorticoids can cause false negative skin test results, such as tuberculin test, histoplasmin test, and allergic skin test.
(4) It can also reduce the thyroid I uptake rate, weaken the response of thyroid stimulating hormone (TSH) to TSH release hormone (TRH) stimulation, and make the TRH excitation test result false positive. Interfering with the results of the luteinizing hormone-releasing hormone (LHRH) excitement test.
(5) Make isotope brain and bone imaging weaken or thin.
3 The following conditions should be used with caution: heart disease or acute heart failure, diabetes, diverticulitis, emotional instability and psychosis, systemic fungal infections, glaucoma, liver damage, herpes simplex, hyperlipoproteinemia, hypertension , Hypothyroidism (increased glucocorticoid effect at this time), myasthenia gravis, osteoporosis, gastric ulcer, gastritis or esophagitis, impaired renal function or stones, tuberculosis, etc.
4 Follow-up inspection: Those who have been using glucocorticoid for a long time should regularly check the following items:
(1) Blood glucose, urine glucose or glucose tolerance test, especially those with diabetes or diabetes tendency.
(2) Pediatrics should be regularly tested for growth and development.
(3) Eye examination, pay attention to the occurrence of cataract, glaucoma or eye infection.
(4) Serum electrolyte and fecal occult blood.
(5) Examination of hypertension and osteoporosis, especially in the elderly. ^[4]

Prednisolone for pregnant and lactating women:

1. Medication during pregnancy: Glucocorticoids can pass through the placenta. Animal experimental studies have confirmed that administration during pregnancy can increase the incidence of embryonic cleft palate, placental insufficiency, spontaneous abortion and intrauterine growth retardation. Human use of pharmacological doses of glucocorticoids can increase the incidence of placental insufficiency, neonatal weight loss, or stillbirth.
2. Drugs for lactation: Because glucocorticoids can be excreted from milk, it has adverse effects on infants, such as growth inhibition and adrenal cortex function inhibition.
Pregnant women and lactating women should avoid using it as much as possible while weighing the pros and cons. ^[4]

Prednisolone for children:

Pediatric use of adrenal corticosteroids must be very careful. ^[4]

Prednisolone medication for the elderly:

Elderly patients are prone to hypertension and diabetes with glucocorticoids. The use of glucocorticoids in elderly patients, especially postmenopausal women, is likely to worsen osteoporosis. ^[4]

Prednisolone drug interactions:

1. Non-steroidal anti-inflammatory analgesics can enhance their ulcer-causing effects.
2. Can enhance the liver toxicity of acetaminophen.
3 Combined with amphotericin B or carbonic anhydrase inhibitors, it can aggravate hypokalemia, and long-term combined with carbonic anhydrase inhibitors, prone to hypocalcemia and osteoporosis.
4 Combined with protein anabolic hormones, it can increase the incidence of edema and make acne worse.
5. Long-term combination with anticholinergic drugs (such as atropine) can cause increased intraocular pressure.
6. Tricyclic antidepressants can aggravate the mental symptoms they cause.
7. When combined with hypoglycemic agents such as insulin, the dose of hypoglycemic agents should be adjusted appropriately because it can increase blood sugar in patients with diabetes.
8. Thyroid hormone can increase its metabolic clearance. Therefore, the dose of the latter should be adjusted appropriately in combination with thyroid hormone or antithyroid drugs.
9. Combined with contraceptives or estrogen preparations, it can enhance its therapeutic effect and adverse reactions.
10 Combined with cardiac glycoside, it can increase the toxicity of digitalis and heart rhythm disturbance.
11. Combined with potassium-releasing diuretics, it can cause severe hypokalemia, and weaken the sodium-releasing and diuretic effects of diuretics due to water and sodium retention.
12. Combined with ephedrine, it can enhance its metabolic clearance.
13. Combined with immunosuppressants, it can increase the risk of infection and may induce lymphoma or other lymphoplastic diseases.
14. May increase isoniazid metabolism and excretion in the liver, reduce isoniazid blood concentration and efficacy.
15. Can promote the metabolism of mexiletine in the body and reduce blood concentration.
16. Used in combination with salicylate to reduce plasma salicylate concentration.
17. Combined with growth hormone, can inhibit the growth-promoting effect of the latter. ^[4]

Prednisolone overdose:

Can cause adrenal-like hyperfunction syndrome. ^[4]

Prednisolone pharmacology and toxicology:

Corticosteroids. Super physiological amount of glucocorticoids has a variety of pharmacological effects such as anti-inflammatory, anti-allergic and immune suppression.
1. Anti-inflammatory effect: Glucocorticoids reduce and prevent tissues from responding to inflammation, thereby reducing the manifestation of inflammation.
2. Immunosuppressive effects: prevent or suppress cell-mediated immune responses, delayed allergic reactions, reduce the number of T lymphocytes and monocyte eosinophils, reduce the ability of immunoglobulins to bind to cell surface receptors, and inhibit interleukin Synthesis and release, which reduces the conversion of T cells to lymphoblasts and reduces the expansion of the primary immune response.
3 Anti-toxic and anti-shock effects: Glucocorticoids can counteract the stimulating response of bacterial endotoxins to the body, reduce cell damage and protect the body. ^[4]

Prednisone pharmacokinetics:

This product is easily absorbed by the digestive tract, and it exists in an active form. It does not need to be transformed by the liver to exert its biological effect. The plasma plasma concentration reached a peak about 1 to 2 hours after oral administration, and t1 / 2 was 2 to 3 hours. Most of the products in the blood are bound to plasma proteins (but the binding rate is lower than that of hydrocortisone), free and bound metabolites are excreted from the urine, some are excreted in their original form, and a small part can be excreted through milk. ^[4]

Prednisone Expert Reviews

The method of local injection of this product and local anesthetics is used to treat acute dysentery strain, and the treated cases have achieved rapid relief or cure. It is usually cured once, supplemented by a rest for 1 week, and those with more residual symptoms can be injected again after 1 week. According to domestic reports, 1,000 patients were treated with prednisolone with local pain points, and their condition was alleviated and cured, accounting for 95.7% of the total. The local pain point injection method simply uses prednisolone, the drug concentration is relatively large, and the amount of solution is small, which is convenient for injection of dense parts of tissues such as hands, feet, limbs, etc., and the drug spreads slowly, and the local anti-inflammatory effect is large. Strong benign stimuli similar to traditional Chinese medicine acupuncture to regulate the body, the effect is better than closed methods such as prednisone diluted with procaine. Of the 1,000 cases, except for 11 patients who had redness and tenderness after local injections, and had improved after topical hot compresses and anti-infective treatment, none of them had purulent infection. ^[5]