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Technical Information
Tretinoin
January 2010
Supersedes issue dated February 2009

03_030752e-06/Page 1 of 6
USP, Ph. Eur.
Pharma Ingredients
& Services
1. Medical indication
Tretinoin is a synthetic vitamin A acid derivative used for the treatment of severe forms of acne, such as acne conglobata and acne cystica, which are mostly resistant to other forms of treatment. Tretinoin is a stereoisomer of Isotretinoin. Formulations for the treatment of acne are mostly creams, gels or solutions. Fur- thermore, there is also an oral formulation marketed for the treatment of special A teratogenic effect in humans, as known for Isotretinoin, has not been reported in published papers. However, there are publications reporting a teratogenic ef ect in animals. Therefore, precautions must be taken if Tretinoin is to be used by women: Contraceptive measures should be used starting one month before and ending one month after treatment with Tretinoin. Tretinoin must not be administered during pregnancy. All formulations of Tretinoin are prescription drugs. Pharmacology
Tretinoin reduces the production of sebum in the skin and the size of the Pharmacokinetics
Absorption rates in topical application vary greatly, ranging between 0.5% and 25%, depending on the formulation and quantity applied on the skin. No detailed data on Tretinoin’s kinetic profile is available. 2. Chemical information
Synonymous names
All-trans-vitamin A acid, all-trans-retinoic acid, all-A vitamin acid EINECS-No.
Structural formula
Empirical formula
Molecular weight
3. Grades
PRD-No.
30035131
Tretinoin
Retest period
See separate documentation: “Q&R PI (not for regulatory purposes)” available at BASF’s WorldAccount: https://worldaccount.basf.com (registered access).
4. Physical and chemical properties
Appearance
Yellow to yellowish-orange crystalline powder Solubility
5. Regulatory status
Meets current USP and Ph. Eur. monographs. The open part of the DMF is available.
6. Safety aspects
Published papers suggest a high teratogenic potential of Tretinoin in animals. “It is unlawful to sell or offer for sale dangerous substance without indicating the dangers relating to the substance in accordance with § 3 a, Section 1.” 7. Specification
See separate document: “Standard Specification (not for regulatory purposes)” available via BASF‘s WorldAccount: https://worldaccount.basf.com (registered 8. Storage conditions
Store in air-tight containers below 25 °C and protected from air and light. Containers that have been opened must be kept under nitrogen or argon and should be used up as quickly as possible. Once opened, containers must be 9. Particle characterization The particle size is measured by laser light dif ractometry in an aqueous suspension.
Typical values of particle size distribution:D 0.1 10. General information
Only peroxide-free pharmaceutical excipients should be used for the formulation. on the processing of
Ingredients that tend to form peroxides should be strictly avoided. Tretinoin
Butylhydroxytoluene is recommended as an antioxidant. Opened packages should be flushed with nitrogen or argon, tightly closed again 11. Formulating examples
Tretinoin Cream (50 mg/100 g)
1. Formulation
I.
2. Production
Separately prepare solution I and mixture II by heating to about 75 °C. Heat mixture III until a clear solution is formed. Add solution I to the warm mixture II, then add mixture III and cool by stirring.
3. Chemical stability (20 – 25 °C, dark)
Analytical method: Spectrophotometric at 358 nm in chloroform + Tretinoin Gel (50 mg/100 g)

1. Formulation
I.
2. Production
Prepare suspension II and add solution III to the well-stirred suspension. When a clear mixture is formed, add solution I.
3. Properties
Tretinoin + Dexpanthenol Gel (50 mg + 2,500 mg/100 g)
1. Formulation
I.
2. Production
Add I slowly to the clear solution I at about 40 °C. Heat to about 50 °C and dissolve about 4 g of I I in I/I . Cool to about 6 °C and dissolve the rest of I I. Keep cool until 3. Properties
4. Chemical stability (12 months, 23 °C, dark)
Tretinoin
5. Remark
It is important to protect the gel from light to prevent the isomerization and degradation This document, or any answers or information provided herein by BASF, does not constitute a legal y binding obligation of BASF. While the descriptions, designs, data and information contained herein are presented in good faith and believed to be accurate, it is provided for your guidance only. Because many factors may affect processing or application/use, we recommend that you make tests to determine the suitability of a product for your particular purpose prior to use. It does not relieve our customers from the obligation to perform a ful inspection of the products upon delivery or any other obligation. NO WARRANTIES OF ANY KIND, EITHER EXPRESS OR IMPLIED, INCLUDING WARRANTIES OF MERCHANTABILITY OR FITNESS FOR A PARTICULAR PURPOSE, ARE MADE REGARDING PRODUCTS DESCRIBED OR DESIGNS, DATA OR INFORMATION SET FORTH, OR THAT THE PRODUCTS, DESIGNS, DATA OR INFORMATION MAY BE USED WITHOUT INFRINGING THE INTELLECTUAL PROPERTY RIGHTS OF OTHERS. IN NO CASE SHALL THE DESCRIPTIONS, INFORMATION, DATA OR DESIGNS PROVIDED BE CONSIDERED A PART OF OUR TERMS AND CONDITIONS OF SALE. BASF SE - Care Chemicals Division - Pharma Ingredients & Services - 67117 Limburgerhof - www.pharma-ingredients.basf.com

Source: http://www.pharma-ingredients.basf.com/Statements/Technical%20Informations/EN/Pharma%20Solutions/03_030752e_Tretinoin.pdf

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