Technical Information June 2013 Supersedes issue dated March 2012 Kollicream Grades Kollisolv MCT Grades 03_111144e-02/Page 1 of 8 Last change WF-No. 123227 = Registered trademark of BASF Emollients for topical applications.
03_111144e-02 June 2013 Page 2 of 8 Kollicream Grades In this technical information we would like to give you an overview on our pharmaceutical grade emollients for topical applications. BASF s emollient portfolio features excipients that feel like cosmetics on the skin, milder formulations for minimal irritation, and easy-to-apply products for large areas. Our offering includes high-performance emollients for efficient topical drug delivery including of oil-soluble APIs. Rebranding As a result of the integration of former Cognis excipients in the BASF portfolio a rebranding was decided. The rebranding should increase the reliability and compliance for the supply of pharmaceutical excipients. In the following table you can find a comparison of old versus new trade names. former Cetiol LC PH Cetiol SN PH Cetion V PH Kollicream CP 15 Cutina CP PH Eutanol G PH HD Eutanol V PH Isopropyl Myristate PH Kollisolv MCT 60 Myritol 312 Kollisolv MCT 70 Myritol 318 Table 1: New s Old s PRD-No. CAS-No. Article-No. 30554439 95912-86 50253219 30554440 111937-03-02 50253251 30554441 3687-46-5 50253252 Kollicream CP 15 30554443 95912-87-1 50253253 30554460 5333-42-6 50253259 30554462 68002-94-8 50253265 50253266 30554463 110-27-0 50253267 Kollisolv MCT 60 30554488 85409-09-2 50253408 Kollisolv MCT 70 30554489 73398-61-5 50253413 Tabele 2: PRD-, CAS- and Article-Numbers.
03_111144e-02 June 2013 Page 3 of 8 Kollicream Grades Specifications See separate documents: Standard Specification (not for regulatory purposes) available via BASF s WorldAccount: https://worldaccount.basf.com (registerd access) Regulatory Status In table 3 you can find all the monographs that the Kollicream grades and the Kollisolv MCT oils meet. Compendial name Ph. Eur.: Cocoyl Caprylocaprate Ph. Eur.: Cetostearyl Isononanoate Ph. Eur.: Decyl Oleate Kollicream CP 15 Ph. Eur.: Cetyl Palmitate 15 Ph. Eur.: Octyldodecanol USP/NF: Octyldodecanol Ph. Eur.: Oleyl Alcohol USP/NF: Oleyl Alcohol Ph. Eur.: Isopropylmyristate USP/NF: Isopropylmyristate Kollisolv MCT 60 Ph. Eur.: Triglycerides -chain USP/NF: Medium Chain Triglycerides Kollisolv MCT 70 Ph. Eur.: Triglycerides -chain USP/NF: Medium Chain Triglycerides Table 3: Compendial names Application Kollicream types and the Kollisolv MCT oils can be used as emollients in creams and lotions. Our high performance emollients offer incredible flexibility and efficiency for topical drug delivery systems allowing you to adapt variables such as spreading value, molecular weight, or water permeability in line with your needs. With their moisture retention effect, fattening and re-fattening power, these topical excipients are able to care and protect the skin. Within the formulation they also have an impact on the consistency and appearance of the cream or lotion. Our offering also includes high-performance emollients for efficient topical drug delivery including of oil-soluble APIs.
03_111144e-02 June 2013 Page 4 of 8 Kollicream Grades Spreading The spreading value of an emollient has an important impact on the skin-feel of the emulsion. Using a high amount of fast spreading emollients in your formulation will result in a high immediate smoothness on the skin, but this feel will disappear fast. In contrary using a high amount of slow spreading emollients will result in low initial smoothness, but this feel will last for a long time. Just a combination of emollient with different spreading behavior will lead to a constant smooth skin feel over long time. Picture 1 is visualizing this effect. Initial Smoothness quick slow Evaluation time Picture 1: Spreading cascade of emollient for the perfect skin feel of a emulsion. The Spreading is defined as the surface area of skin (mm 2 ) covered in a specific period of time (10 min) by the emollient. It can be measured in- vivo and in-vitro. Test design on human skin: 4 mg lipids 4 separate measurements per person 10 min spreading time 23 C room temperature 60% relative humidity Reference oil (parafin oil) Emollient Picture 2: Test design of spreading on human skin
03_111144e-02 June 2013 Page 5 of 8 Kollicream Grades In table 4 you can find the spreading values for all BASF emollients in pharma quality. (Kollicream grades and Kollisolv MCT oils) Emollient Chemical name Spreading value in mm 2 Isopropyl 1200 Fast Light (IPM PH) myristate Emollience Coco-caprylate/ 800 Medium Medium (Cetiol LC PH) caprate Cetostearyl 700 Medium Medium (Cetiol SN PH) isononanoate Decyl oleate 700 Medium Medium (Cetiol V PH) Oleyl alcohol 700 Medium Medium (HD-Eutanol V PH) Octyldodecanol 600 Medium Medium (Eutanol G PH) Kollisolv MCT 60 Medium-chain 550 Medium Medium (Myritol 312 PH) triglycerides Kollisolv MCT 70 Medium-chain 550 Medium Medium (Myritol 318 PH) triglycerides Kollicream CP 15 Cetyl palmitate Slow Rich (Cutina CP PH) Table 4: Spreading value for BASF emollients (if molten) Our broad portfolio of emollients allows to generate desired skin feelings and to support the delivery of actives. Stability against hydrolysis The Hydrolytic Stability of an Emollient is important for applications using very high or low ph value. Very stable against hydrolysis is the Guerbet Alcohol and our. Degree of Saturation Emollient esters can be both saturated and unsaturated. The Iodine value indicates the degree of unsaturation. A low Iodine value indicates better oxidative stability. Unsaturated materials with higher Iodine values can be protected with antioxidants. Iodine Value [Ph. Eur. 2.5.4 method A] max. 1.0 max. 1.0 55 70 Kollicream CP 15 max. 2.0 max. 8.0 85 95 USP <401> max. 1.0 Kollisolv MCT 60 max. 1.0 Kollisolv MCT 70 max. 1.0 Table 5: Iodine Value for BASF emollients
03_111144e-02 June 2013 Page 6 of 8 Kollicream Grades Polarity The polarity of an emollient impacts its solubilisation properties and ease of emulsification. In general, polar emollients help to stabilize oil in water emulsions. In water in oil systems, the degree of polarity can be critical. Investigations have shown that emollients of polarity give the best stability. Emollients can also be combined to give polarity in its mix. For solubilisation of oil-soluble actives there is the general rule, that the more polar oil also have better solubilisation properties. Kollicream CP 15 Kollisolv MCT 60 Kollisolv MCT 70 Polarity low low strong strong Table 6: Polarity of BASF emollients Water Permeability on Skin The permeability/occlusivity of an applied film describes the ability to allow/prevent the passage of water through it. A highly occlusive material prevents moisture transfer e.g. Petrolatum. Occlusivity is an important consideration for pharmaceutical formulation. The selection of emollients influences the permeability of an emulsion. Kollicream CP 15 Kollisolv MCT 60 Kollisolv MCT 70 Water Permeability to low low high Table 7: Water permeability of BASF emollients
03_111144e-02 June 2013 Page 7 of 8 Kollicream Grades Skin Tolerance All Kollicream grades and the Kollisolv MCT oils have a good skin tolerance. In general there are no restrictions in usage concentration. The only exception is. We do not recommend using this emollient in concentrations higher than 10%, because of the possible comedogenic effect. Raw material origin All Kollicream types and Kollisolv MCT grades are based on vegetable and synthetic raw materials. Toxicology The toxicological abstracts are available on request. Individual reports can be shared under secrecy agreement. Stability and storage You can find the stability datas for the Kollicream types and Kollisolv MCT oils in the table below, If they are stored In original sealed container and protected from moisture and stored at less than 30 C. Kollicream CP 15 Kollisolv MCT 60 Kollisolv MCT 70 1 year 1 year 1 year Handling and Disposal Please refer to the individual Material Safety Data Sheet (MSDS) for instructions on safe and proper handling and disposal. Formulation examples Oil in Water emulsion: Ingredient Name Amount I Kolliwax GMS II Glyceryl Monostearate 40-55 Type II 4.0% Kolliwax CSA 50 Cetostearyl Alcohol 2.8% Kolliphor CS 20 Macrogol Cetostearyl Ether 20 1.6% Kolliphor CS 12 Macrogol Cetostearyl Ether 20 0.8% Kollicream CP 15 Cetyl Palmitate 15 0.8% Isoproplymyristate 5.0% Cocoyl Caprylocaprate 5.0% Octyldodecanol 5.0% II Kollisolv G 99 Glycerin 5.0% Preservative q.s. Water 70.0% Preparation 1. Melt the components listed under I. at 80 85 C and stir until homogeneous. 2. Heat the components listed under II. at 80 85 C, stir till homogeneous and add slowly to phase II while stirring. Stir for 5 minutes at this temperature. 3. Allow the emulsion to cool down to 30 C with stirring in such a way that it remains in continual motion. Finally adjust the ph-value and add the preservative.
03_111144e-02 June 2013 Page 8 of 8 Kollicream Grades Diclofenac Gel-Cream Ingredient Name Amount I Diclofenac Sodium Diclofenac Sodium 1.0% Kollisolv PG Propylene Glycol 15.0% II Kollisolv MCT 70 Medium Chain Triglyderides 10.0% Water dem. 54.0% III Kolliphor P 407 Poloxamer 407 20.0% Preperation Dissolve Diclofenac Sodium in Propylene Glycol, add the mixture of water and Kollicream MCT 70. Dissolve the Kolliphor P 407 in this well stirred mixture at 4 6 C (or at >70 C). Maintain the temperature until the air bubbles have escaped. Note This document, or any answers or information provided herein by BASF, does not constitute a legally 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 full 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. June 2013 BASF Nutrition & Health www.pharma-ingredients.basf.com