Pharmaceutical Bulk Isotretinoin Powder

CAS:4759-48-2

MF: C20H28O2

MW: 300.44

EINECS: 200-403-3

Specification​: 99% min Isotretinoin Powder

Sample: Isotretinoin Powder

Packaging:1kg/bag, 25kg/drum

Brand: Henrikang

Appearance: White Powder

Storage: Cool Dry Place

Shelf Life: 2 Years

Test Method: HPLC

Isotretinoin Powder Usage and Synthesis.

Isotretinoin has low availability and postprandial administration increases bioavailability. The binding rate to plasma protein is greater than 99%. Mainly in the liver or intestinal wall metabolism, in the original form and metabolites into the enterohepatic circulation, unchanged original form of the drug from the feces, metabolites excreted through the urine. The elimination half-life is 10-20 hours.

Uses and functions of Isotretinoin.

It is a vitamin A drug with strong and rapid inhibition of the proliferation and differentiation process of skin glandular cells, which is highly effective in severe nodular cystic acne. It is better absorbed in the stomach and intestines, while topical application is ineffective.

It is used for severe acne, cystic acne, and party acne that are ineffective with other medications. It is also effective in skin disorders such as rosacea, ichthyosis, keratosis pilaris, and trichophytosis.

1. Isotretinoin is the drug of choice for refractory acne, especially for patients with severe nodular, cystic, and inflammatory acne that have failed traditional treatments;

2. generalised flat warts or warty epidermal dysplasia;

3. Keratosis pilaris;

4. Cutaneous lupus erythematosus;

5. Lichen planus, sclerosing atrophic moss.

Pharmacological Effects of Isotretinoin Raw Materials.

Pharmacological ActionsIsotretinoin is a first-generation retinoic acid, a stereoisomer of all-trans retinoic acid. It has an anti-seborrhoeic effect when taken orally and has shown particular efficacy in severe acne.

The mechanism of action is as follows:

① It has the effect of shrinking the sebaceous glands, inhibiting the activity of sebaceous glands, and reducing the secretion of sebaceous glands, thus inhibiting the reproduction of Propionibacterium acnes, which relies on the lipid environment for growth.

② It has the effects of antikeratinisation, inhibiting the over-proliferation of epidermal cells and promoting their differentiation, which can reduce the keratinisation of the follicular orifices and sebaceous gland ducts.

③It can also affect the function of monocytes and lymphocytes, inhibit the chemotaxis of neutrophils and have anti-inflammatory activity.

(iv) Selectively binds to retinoic acid nuclear receptors and exerts therapeutic effects. It inhibits the proliferation of Acinetobacter shortus and has immunostimulatory effect at low dose and immunosuppressive effect at high dose.

⑤ Inhibits the formation of collagenase and gelatinase in the skin and inhibits ornithine decarboxylase activity. Since the induction of ornithine decarboxylase can play a major role in skin mutations, isotretinoin can also inhibit tumourigenesis.

(6) When used topically, the mechanism of action of this product is similar to that of retinoic acid, which can induce epidermal cell proliferation, promote the differentiation of the granular layer of epidermal cells to the stratum corneum, and regulate the follicular sebaceous epithelium to keratinise the abnormal process of keratinous plugs, so as to play a therapeutic role.

Production method of Isotretinoin Raw Powder.

The reaction of β-violet ketone with ethylmagnesium chloride, followed by reaction with triphenylphosphine to form triphenylengravates, and then with cyclopentenone derivatives, produced isotretinoin and its 8Z isomer. Its 8Z isomer was isolated and isomerised to isotretinoin by the action of palladium nitrate.