Pharmaceutical performance powered by Gattefossé. Excipients for Rectal and Vaginal Drug Delivery

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1 Pharmaceutical performance powered by Gattefossé Excipients for Rectal and Vaginal Drug Delivery

2 about gattefossé About Gattefossé Our Business Gattefossé is an independent global leader in the production of specialty lipidic excipients and lipid-based drug delivery systems. Working with healthcare industries for over a century, our expertise in oleochemistry has inspired the development of a diverse portfolio of products and formulation technologies. Formulation expertise Gattefossé has dedicated laboratories for R&D and Formulation. Our research aims to improve understanding of the physicochemical nature of lipids and their behaviour in drug delivery systems, in vitro and in vivo. Our Formulation Laboratory provides consultancy in lipid formulations for rectal, topical and oral dosage forms; bioavailability and sustained release and processing techniques. Gattefossé products are manufactured in an ISO 9001 version 2000 certified facility. Quality and batch-to batch consistency are guaranteed by adhesion to the principles of GMP. Sustainable Development Gattefossé is committed to conducting environmentally responsible business and takes sustainable development seriously. Our environmental impact is pro-actively measured and controlled. Manufacturing processes are developed to be clean, using degradable catalysts and solvent-free extraction processes in oleochemistry. Our manufacturing is designed to utilize energy more efficiently and generate less waste. Production and Quality Gattefossé principal manufacturing site is based at the global headquarters in Saint-Priest, France. Production, quality and logistic operations are supported by SAP. Our manufacturing operations aim to be: Innovative in pilot and scale-up projects for custom product manufacturing Responsive to rapidly meet unexpected increases in demand Flexible in providing custom packaging and delivery solutions Responsible implementing production methods that positively manage environmental impact 2 Pharmaceutical performance powered by Gattefossé

3 standard and specialty products Standard and specialty products Gattefossé is a reputable global supplier of suppository bases. Suppocire products are hard fat semisynthetic bases produced by inter-esterification or direct esterification of fatty acids. Their composition consists of a mixture of C 12 C 18 triglycerides. The Suppocire catalogue offers Standard Products and Specialty Products. Superior semi-synthetic bases Suppocire semi-synthetic bases have superior performance features compared with certain natural or fully synthetic bases, these include: Clinical properties Excellent safety and mucosal tolerance due to non-toxicity and non-irritant properties Softening and diffusion properties that deliver efficient and uniform drug release. Formulation properties Chemically inert and therefore compatible with a wide variety of APIs Excellent dispersion of active ingredient in the suppository mass Proven physical and chemical stability: colour, odour, drug release profile, low risk of oxidation. Manufacturing properties Optimized solidification properties to minimise physical polymorphisms Different products provide solutions for a wide range of manufacturing equipment Gattefossé service Gattefossé has produced Suppocire for more than 50 years. We can genuinely help speed up your time to market by providing: Rapid identification of the right Suppocire product for the API Access to a library of over 2,000 suppository formulations Product customization and laboratory scale formulation assistance Production and validation of pilot batches Scale-up and manufacturing advice. Suppocire Quality performance Product quality and performance is assured by conformity to international monographs: EP, USP- NF, JPE Uniform physicochemical characteristics and batchto-batch consistency ensure reproducible analytical and functional outcomes Repeat batch release quality assurance tests are undertaken for more sensitive Suppocire products The Suppocire and Ovucire manufacturing sites have consistently passed international audits. Suppocire safety and regulatory status Excipient safety is supported by in vitro and in vivo toxicity studies as well as history of use in internationally approved medicinal products. The Suppocire and Japocire range is referenced in a Type IV Drug Master File registered with the U.S. FDA to assist clients with IND, NDA or ANDA filings. Pharmaceutical performance powered by Gattefossé 3Standard and specialty products

4 Suppocire standard products Suppocire standard products Suppocire Standard products contain a well-defined proportion of mono/di and triglycerides. Their physicochemical features are adapted to meet the needs of different Active Pharmaceutical Ingredient (API) properties, formulation and manufacturing operations. Melting range Drop point ( C) AI Range A Range The Suppocire Standard products are classified into five major melting point (drop point) ranges: AI, A, B, C, D Hydroxyl value (mg KOH/g) < > 30 NAI 25 A NAI 50 AM A AP NA 0 NA NA 15 NAI 25 B Range BM NB BP C Range CM D Range DM D 4 Pharmaceutical performance powered by Gattefossé

5 Standard AI, A, B, C & D Product Lines Suppository bases obtained by interesterification of hydrogenated palm oil and hydrogenated palm kernel oil. These are multipurpose vehicles covering a range of melting points (drop point). Result in a softer suppository unit which is self-lubricating due to the well-defined medium chain triglyceride content. Ideal for straightforward formulations and versatile for use with manual, semi and fully automated manufacturing equipment. Standard N line Bases obtained by direct esterification of selected fatty acids with glycerol. The long chain triglyceride content confers rapid solidification resulting in harder suppository units with high mechanical resistance. The low hydroxyl/low reactivity products provide: High crystallization rate in individual suppository unit. Appropriate for high through-put/high speed manufacturing equipment. Suitable for sensitive active ingredients. The higher hydroxyl value products provide versatility for lower volume/lower speed production equipment. P Grade M Grade Suppository bases derived from the AI, A, B, C and D product lines (obtained by inter-esterification of hydrogenated palm oil and hydrogenated palm kernel oil). The low hydroxyl value/low reactivity ensures: Minimal risk of interaction between free OH groups and acidic active ingredients. High crystallization rate in individual suppository units. Suitable for high-speed manufacturing. Suitable for sensitive APIs. Bases consist of polyglycolized glycerides synthesised by esterification of selected fatty acids with polyethylene glycol (PEG) and glycerol. The amphiphilic base provides bioavailability enhancement through improved solubilization and absorption of API. Suitable for difficult to formulate active ingredients. Pharmaceutical performance powered by Gattefossé 5

6 Suppocire specialty products Suppocire specialty products Suppocire Specialty products provide solutions for more challenging formulation and manufacturing needs. Functional and formulation properties are controlled by monoglyceride content and/or the inclusion of additives including phospholipids, beeswax, polyoxylethylene (POE) sorbitan esters. Melting range Drop point ( C) Hydroxyl value (mg KOH/g) < > 30 AIML NAIS 90 AML AS2 NAS 40 AS2X NAS 50 NAL NAS BML NAIS 10 BS2 BS2X NBL CS2X Letters indicate the type of modification and the resulting physicochemical and performance feature. 6 Pharmaceutical performance powered by Gattefossé

7 L Grade A phospholipid additive enables good dispersion of larger amounts of powdered API during formulation and homogenous distribution of drug in the suppository unit. S and S2 Grade Contain a modified monoglyceride content: Products with a higher monoglyceride content yield bases with enhanced hydrophilic properties. Appropriate when fast release of API is an essential therapeutic feature of the finished product. X Grade Contain an non-ionic emulsifying additive to enable the incorporation of API in aqueous solutions and/or hydroalcoholic extracts. Appropriate for use to prevent the exudation of API in solution from the solidified suppository unit. Pharmaceutical performance powered by Gattefossé 7

8 japocire and ovucire products Japocire and Ovucire Suppository bases specifically for Japanese healthcare industries. These products have physicochemical and performance features similar to those of the Suppocire Standard range, are registered with the appropriate Japanese authorities. Melting range ( C) Capillary Tube Hydroxyl value (mg KOH/g) Specification Japocire NA < 3 Versatile base, suitable for all types of production equipment. Produces high mechanical resistance suppositories. Japocire NA < 15 Low hydroxyl value, low reactivity base, suitable for acidic active ingredients. Suitable for high-throughput manufacturing but shock cooling should be avoided. Japocire NAS High hydroxyl value suitable for highthroughput productions with shock-cooling and/or larger volume of powder. Japocire DM Low hydroxyl value, low reactivity base, suitable for acidic active ingredients. Suitable for high-throughput manufacturing but shock cooling should be avoided. The Ovucire products are specifically for vaginal drug delivery. These are bases with hydrophilic properties offering a melting point range optimised for vaginal drug delivery. Melting range Drop Point ( C) Hydroxyl value (mg KOH/g) Specification Ovucire WL An emulsifying additive improves the dispersion and wettability of API Fast melting at body temperature. Forced cooling is necessary. Ovucire WL A versatile base with good mechanical resistance. Ovucire A versatile base with good mechanical resistance. 8 Pharmaceutical performance powered by Gattefossé

9 regulatory status USP-NF EP JPE USP-NF JPE Suppocire, Japocire Regulatory Status Suppocire : A, AM BM, CM, D, DM NA, NA 0, NA 15 NB NAs 40, nas 50, NAS 55 NAI 25, NAI 25 A, NAI 50 AS2, BS2 Japocire : NA 0, NA 15, NAS 50, DM Suppocire : AIML, AML, BML AS2X, BS2X, CS2X, NAL, NBL Abbreviations: USP/NF = US Pharmacopœia/National Formulary, EP = European Pharmacopeia, JPE = Japanese Pharmaceutical Excipients. regulatory status The Regulatory Data Sheets for Suppocire, Japocire and Ovucire products are available from your local Gattefossé representative. Suppocire, Japocire and Ovucire products have relevant in vitro and in vivo toxicity dossiers. Suppocire and Japocire products are referenced in a Type IV Drug Master File registered with the U.S. FDA. The Chinese pharmacopœia status of each Suppocire standard line is stated in the product Regulatory Data Sheet (RDS), please contact Gattefossé for further information. Suppocire is a registered trademark of Gattefossé sas. Further information To help select the right excipients for your drug development program and for further information about our formulation services please contact your local Gattefossé representative. The information included in this brochure is presented in good faith and we believe that it is correct, but no warranty as to accuracy of results or fitness for a particular use is given, nor is freedom from patent infringement to be inferred. It is offered solely for your consideration, investigation and verification. The user shall determine under his responsibility, the use and the security conditions of the information, and will remain the only one responsible in case of damageable consequences. Before using a Gattefossé product, or any other product mentioned in this literature, read, understand and follow the information contained in most recent Material Safety Data sheet. Pharmaceutical performance powered by Gattefossé 9

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12 Worldwide Locations regional affiliates Canada Gattefossé Canada, Inc. 170 Attwell Drive, Suite 580 Toronto, Ontario M9W 5Z5 Tel Fax China Gattefossé China Trading Co., Ltd Room 302, Building N 6, Lane 289 Bisheng Road ZhangJiang Hi-Tech Park Shanghai P.R. China Tel Fax France Gattefossé France 5 rue Montesquieu F NANTERRE Cedex Tel Fax Germany Gattefossé (Deutschland) GmbH Freiburger Strasse 19 D BAD KROZINGEN Tel Fax India Gattefossé India Pvt Ltd. Ground floor, Bombay College of Pharmacy C.S.T. Road, Kalina Santacruz (East) Mumbai Tel /32/33 Fax Italy Gattefossé Italia s.r.l. Via Durando, 38 I MILANO Tel Fax Spain Gattefossé España, s.a. Av. Diagonal A E BARCELONA Tel Fax Gattefossé España, s.a. C/Padilla, 73, 1 B E MADRID Tel /16 12 Fax Switzerland Gattefossé AG Haldenstrasse 11 CH-6006 Luzern Tel Fax United Kingdom Gattefossé (UK) Limited Arc House, Terrace Road South Binfield, Bracknell, Berkshire RG42 4PZ Tel Fax U.S.A. Gattefossé Corporation Plaza I, 115 West Century Road, Suite 340, Paramus New Jersey Tel Fax Rectal Drug Delivery-GB-10C2-154VV (2064 BE) Corporate Headquarters Gattefossé: 36 chemin de Genas - BP F Saint-Priest Cedex - France Tel Fax infopharma@gattefosse.com - GATTEFOSSé is an independent multinational company which creates, develops and manufactures specialized ingredients for the pharmaceutical and personal care industries. Present in almost 50 countries worldwide, Gattefossé provides extensive expertise in lipochemistry, biology and extraction from natural sources. Gattefossé offers the pharmaceutical industry innovative functional lipidic excipients for bioavailability improvement, sustained release formulation, lubrication, taste-masking, solubilization and penetration enhancement.