1.What is Cortisone Acetate
Definition:
Cortisone acetate is a corticosteroid, which was first discovered in 1935. Detailed research was carried out on it in 1949 to deeply understand its pharmacokinetics and pharmacodynamics, after which the drug received FDA approval on 13th June 1950.
It has both glucocorticoid and mineralocorticoid activities, and, just like other corticosteroids, it has anti-inflammatory and immunomodulatory properties. Therefore, it is used to treat multiple diseases, including several inflammatory conditions, endocrine disorders (Grave's disease), allergic reactions, respiratory disorders such as asthma, gastrointestinal diseases (Irritable bowel disease), arthritis, and even some neoplastic conditions like lymphomas.
It is usually available as 5, 10, 0r 25 mg tablets.
Chemical & Physical features:
Chemical Structure:
Synonyms: Cortone acetate, Cortisone 21-acetate, Incortin
Molecular weight: 402.5
Molecular formula: C23H30O6
CAS number: 50-04-4
DrugBank Accession number: DB01380
IUPAC Name: [2-[(8S,9S,10R,13S,14S,17R)-17-hydroxy-10,13-dimethyl-3,11-dioxo-1,2,6,7,8,9,12,14,15,16-decahydrocyclopenta[a]phenanthren-17-yl]-2-oxoethyl] acetate
Melting point: 227 - 229
Storage temperature:
Form: White, odorless crystalline powder
Solubility: Insoluble in water, poorly soluble in acetone, somewhat soluble in alcohol, soluble in dioxane, and freely soluble in chloroform
Brand name:
Cortone
2.Cortisone acetate forms and specifications
Cortisone Acetate injection
The formula is available in powder form for hydrocortisone-acetate injections in several strengths, including 100, 250, 500, and 1000 mg. The storage temperature for unopened products is between 20-25°C. The injections were approved by the FDA in April 1955 and are now available under a prescription. They are used to treat rheumatoid arthritis, ulcerative colitis, asthma, skin allergies, and other inflammatory conditions.
The injection is administered intramuscularly or intravenously, either with or without an IV fluid bag. The general recommended dose for an adult is 100-500 mg given every 2, 4, or 6 hours, depending on the condition.
Cortisone acetate tablets
Cortisone acetate tablets USP contain 25 mg of cortisone acetate in each tablet, along with anhydrous lactose, colloidal silicon dioxide, magnesium stearate, microcrystalline cellulose, sodium lauryl sulfate, and sodium starch glycolate as inactive ingredients.
These tablets are also available in strengths of 5 and 10 mg, having calcium stearate, corn starch, lactose, mineral oil, sorbic acid, and sucrose as inactive ingredients. Similar to injections, they are used to treat various inflammatory conditions.
Cortisone acetate suspension
A 25 mg/ml hydrocortisone-acetate suspension is available as Hydrocortisab injection, which is the medicinal name of the product. Along with this, each ml also contains 10 ml of benzoyl alcohol. The drug is administered as an intra-articular or periarticular injection. It can also be injected into tendon sheaths and bursae. It can treat swollen, inflamed joints due to different conditions like osteoarthritis and rheumatoid arthritis.
In its most natural form, the drug is available as a white, crystalline powder which is also odorless. It is available at the rate of 24.18 USD per gram.
Different suppliers also sell the drug in different dosage forms, one of them being hydrocortisone acetate 1 % topical ointment, which is a colorless ointment. It is stored in a dark and dry place at 15-30°C.
The topical form is mostly used for several inflammatory dermatologic conditions, such as eczema, dermatitis, skin allergies, etc.
3.Cortisone vs cortisone acetate
Cortisone is a hormone that is naturally produced by the adrenal glands in the human body. The acetate salt form of this hormone is cortisone acetate, which is formed when an ester group is attached to it.
4.Cortisone acetate vs. hydrocortisone
Cortisone acetate to hydrocortisone conversion
When an ester group is attached to the glucocorticoid cortisone, the chemical is now water-soluble and is known as cortisone acetate.
The glucocorticoid that the human body produces itself is cortisol, which is also known as hydrocortisone.
All of these come under the class of corticosteroids and have a lot of importance in the medical field.
Since cortisone is biologically inactive, it is modified to its active product, cortisol, to exert its effects. Once administered orally or injected into the body, the enzyme 11β-Hydroxysteroid dehydrogenase type 1 converts it into cortisol.
While cortisone acetate is mostly taken orally, hydrocortisone is also found as an OTC product in the form of topical creams and rectal formulations. The uses and side effects of both are quite similar. However, when comparing the prices, cortisone is more expensive.
5. Mechanism of action of Cortisone Acetate
Cortisone acetate binds to the glucocorticoid receptor in the cytosol, and this receptor-ligand complex is translocated into the nucleus. It binds to glucocorticoid response elements (GRE) in the promoter region of target genes and increases their expression. This leads to the initiation of anti-inflammatory actions of corticosteroids.
These actions include inhibition of phospholipase A2 formation, inhibiting NF-Kappa B and other inflammatory transcription factors. Meanwhile, anti-inflammatory genes like interleukin-10 are promoted.
These anti-inflammatory actions are seen at lower doses of corticosteroids, while at higher doses, the immune system is suppressed.
6.Cortisone Acetate manufacturing process
The entire manufacturing process consists of several steps. The first reaction is an oxidizing reaction at a temperature between the range of -15 to 40°C. The oxygenant is selected from chromium trioxide, sodium dichromate 99, potassium bichromate, chromic acid pyridine mixture, pyridinium dichromate, N-Bromo ethanamide, Dai Si-Martin oxygenant, or Jones reagent.
The second reaction is cyanogenation using a cyanate reagent from acetone cyanohydrin, sodium cyanide, potassium cyanide, or trimethyl silicane cyanogen. The product then undergoes silicon etherification.
The fourth reaction is a replacement-hydrolysis reaction, in which a basic compound from lithium diisopropyl amido, hexamethyldisilazane lithium, hexamethyldisilazane sodium, or hexamethyldisilazane potassium is added first. Then an acidic compound, such as hydrochloric acid, sulfuric acid, or hydrogen bromide, is added to obtain the product. This product then finally undergoes acetate generation replacement(metathesis)reaction, and the final compound is formed.
7.Cortisone Acetate uses
It is a drug of high importance in health and medicine, sold by several suppliers worldwide, and is indicated for multiple diseases. Some of its uses include being prescribed for the treatment of endocrine disorders, such as congenital adrenal hyperplasia, several dermatologic diseases like severe psoriasis and skin allergies, rheumatic disorders such as rheumatoid arthritis and ankylosing spondylitis, respiratory, hematologic disorders, gastrointestinal diseases, and other miscellaneous conditions, such as tuberculous meningitis as well.
A cortisone injection is also prescribed to reduce swelling at a joint or tendon, especially the knee, elbow, and shoulder joints.
8.Cortisone Acetate dosage
The value for initial dosages varies from 25 to 300 mg. For less severe diseases, doses less than 25 mg are sufficient, and for more severe diseases, a high dose like 300 mg is prescribed.
The drug is taken once a day with food to avoid gastrointestinal side effects.
9.Cortisone Acetate side effects
According to the research carried out on the drug, several systemic side effects have been seen, some of which include muscle weakness, peptic ulcers, hypertension, headache and vertigo, impaired wound healing, and menstrual irregularities.
10.Cortisone Acetate API price
381 USD/kg
11.Cortisone Acetate API manufacturers in china
Below are some manufacturers in China who make active pharma ingredients.
HUBEI GOTO BIOPHARM CO., LTD.
The company is one of the largest manufacturers of steroid hormone API in China and was established in 2006. With a total staff number of around 300-349, and three R&D centers, its main sales markets include North America, Central/South America, Western Europe, Eastern Europe, Australia, Asia, Middle East, and Africa.
The contact number of the supplier, Zou Lei: +86-710-3423122-815
Jiangsu Jiaerke Pharmaceuticals Group Corp., Ltd.
It was established in 1993, and with over 20 years of experience in producing steroid hormones and other organic chemical products, it is now an ISO14001 certified company for APIs and intermediates. The factory is located in Jiangsu Changzhou, and its main sales markets are North America, Central/South America, Western Europe, Eastern Europe, Australia, and Asia.
The contact number of the supplier, Wu Yaojun: +86-519-88930815
Zhejiang Xianju Xianle Pharmaceutical Co., Ltd.
Controlled by China Grand Group, this company was established in 1995 and is a professional steroid manufacturer. Their main products include betamethasone series, dexamethasone series, cyproterone acetate series, and prednisone series such as prednisone acetate, prednisolone acetate, hydrocortisone acetate, and prednisolone.
The company was built in 1993 and is located in Xiqing District of Tianjin, China. The main products sold by the company are hydrocortisone base, hydrocortisone acetate, spironolactone, dexamethasone base, dexamethasone acetate, cortisone acetate, prednisone, prednisolone, etc. Just like several pharmaceutical companies in China, this one has a functional website too.
Zhejiang Xianju Junye Pharmaceutical Co., Ltd.
Established in 1998, this company specializes in the production and marketing of steroid hormone APIs and intermediates. With its factory based in Taizhou, Zhejiang Province in China, the company is a supplier of these for several countries in North America, Central/South America, Western Europe, Eastern Europe, Australia, Eastern Europe, Asia, Middle East, and Africa.
The contact number of the supplier, Jin Xiaolei: +86-576-88476367
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References:
1. https://www.rxlist.com/cortone-drug.htm
2. https://pubchem.ncbi.nlm.nih.gov/compound/Cortisone-acetate#section=2D-Structure
3. https://patents.google.com/patent/CN104098642A/en
4. https://www.medicinenet.com/hydrocortisone_acetate-injection/article.htm
5. https://www.medicines.org.uk/emc/product/6703/smpc
6. https://go.drugbank.com/drugs/DB01380
7. https://www.webmd.com/drugs/2/drug-500-780/hydrocortisone-acetate-topical/hydrocortisone-acetate-topical/details
8. https://en.wikipedia.org/wiki/Cortisone
9. https://www.singlecare.com/blog/hydrocortisone-vs-cortisone/
10. https://www.pharmacompass.com/price/hydrocortisone-acetate
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