FORMULATION HANDBOOK Rev. December/2007
A Guide for R+D
FORMULATION HANDBOOK Table of Contents Page 1/2
WORLDWIDE HEADQUARTERS JRS PHARMA
GMBH+CO.KG
Holzmühle 1 D-73494 Rosenberg (Germany) Phone: + 49 (0) 79 67 / 1 52-0 Fax: + 49 (0) 79 67 / 1 52-345 E-mail:
[email protected] www.jrspharma.de www.jrs.de Customer Service: +49 (0) 7967 / 152-312
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USA + CANADA JRS PHARMA LP 2981 Route 22, Suite 1 Patterson, NY 12563-2359 Toll-Free: (800) 431-2457 Phone: +1 (845) 878-3414 Fax: +1 (845) 878-3484 E-mail:
[email protected] www.jrspharma.com
4282_001.GB0.00712pdf
Table of Contents Introduction Excipients Table of Contents Guide Formulations Acetylsalicylic Acid (High Dosage) [No. 4282-001] Acetylsalicylic Acid (Effervescent) [No. 4282-023] Acetylsalicylic Acid (OD Tablets) [No. 4282-029] Allopurinol [No. 4282-002] Ambroxol Hcl [No. 4282-003] Amoxicillin [No. 4282-024] Atenolol [No. 4282-030] Azitrhomycin 1000 mg Direct Compression [No. 4282-033] Boswellia Serrata [No. 4282-004] Calcium + Vitamin D3 [No. 4282-034] Cefalexin [No. 4282-040] Chromium Picoliante [No. 4282-005] Cimetidin [No. 4282-025] Ciprofloxacin Hcl [No. 4282-006] Citramon Chewable Tablet [No. 4282-041] Citramon Direct Compression [No. 4282-042] Creatine Monohydrate [No. 4282-028] Diazepam [No. 4282-022] Enalapril [No. 4282-007] Enalapril Hydrochlorothiazide [No. 4282-043] Extract of Cartilage [4282-008] Ginkgo Biloba [No. 4282-009] Glucosamine [No. 4282-010] Glucosamine-Chondroitin [No. 4282-035] Guafenesin [No. 4282-011] Ibuprofen (Direct Compression) [No. 4282-012] Ibuprofen (Direct Compression) [No. 4282-013] Ibuprofen (Wet Granulation) [No. 4282-014] Lecithin [No. 4282-031] Liu’wei’di’huang TCM Fluid Bed Drying + Direct Compression [No. 4282-027] Metformin [No. 4282-015] Metformin [No. 4282-026]
Customer Service: +1 (845) 878-3414
FORMULATION HANDBOOK Table of Contents Page 2/2
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WORLDWIDE HEADQUARTERS JRS PHARMA
GMBH+CO.KG
Holzmühle 1 D-73494 Rosenberg (Germany) Phone: + 49 (0) 79 67 / 1 52-0 Fax: + 49 (0) 79 67 / 1 52-345 E-mail:
[email protected] www.jrspharma.de www.jrs.de Customer Service: +49 (0) 7967 / 152-312
USA + CANADA JRS PHARMA LP 2981 Route 22, Suite 1 Patterson, NY 12563-2359 Toll-Free: (800) 431-2457 Phone: +1 (845) 878-3414 Fax: +1 (845) 878-3484 E-mail:
[email protected] www.jrspharma.com
4282_001.GB0.00712pdf
Metoprolol (Direct Compression) [No. 4282-016] Metoprolol (Direct Compression) [No. 4282-017] Multivitamin Chewable Tablets [No. 4282-032] Multivitamin Effervescent Tablet [4282-039] Natural Herbal Laxative Cassia Senna + Melissa off. [No. 4282-018] Paracetamol 500 mg [No. 4282-038] Peppermint Oil (Direct Compression) [No. 4282-037] Piroxicam [No. 4282-019] Ranitidine Hcl [No. 4282-020] Silymarin [No. 4282-036] Simethicone [No. 4282-021] Simethicone Direct Compression [No. 4282-045] Vitamin C + Zink [No. 4282-044]
Customer Service: +1 (845) 878-3414
FORMULATION HANDBOOK Introduction
Dear Customer, "LEADING THE WORLD IN EXCIPIENTS" summarizes our commitment to the full range of technical services and support that we provide for formulation development. Take advantage of the experience and application know-how available from our JRS PHARMA's Technical Competence Centers in all questions relating to solid dosage forms. This Formulation Handbook provides you with practical examples and ideas together with an understanding of, and guides for diverse applications. Use our suggestions and examples as the first steps (creative ideas) for your own solutions. Further technical details and product information can be found on the Internet under www.jrspharma.com. Our experts will be happy to answer any questions. We look forward to a co-operative discussion with you. JRS PHARMA Technical Competence and Service Centers
USA + CANADA JRS PHARMA LP Patterson, NY 12563-2359
WORLDWIDE HEADQUARTERS JRS PHARMA
GMBH+CO.KG
Holzmühle 1 D-73494 Rosenberg (Germany) Phone: + 49 (0) 79 67 / 1 52-0 Fax: + 49 (0) 79 67 / 1 52-345 E-mail:
[email protected] www.jrspharma.de www.jrs.de Customer Service: +49 (0) 7967 / 152-312
USA + CANADA JRS PHARMA LP 2981 Route 22, Suite 1 Patterson, NY 12563-2359 Toll-Free: (800) 431-2457 Phone: +1 (845) 878-3414 Fax: +1 (845) 878-3484 E-mail:
[email protected] www.jrspharma.com
4282_001.GB0.00712pdf
WORLDWIDE HEADQUARTERS JRS PHARMA GMBH+CO.KG D-73494 Rosenberg (Germany)
Customer Service: +1 (845) 878-3414
FORMULATION HANDBOOK JRS Excipients
Product Overview Page 1/3
The High Functionality Excipient
Insoluble Tablet Binders:
PROSOLV SMCC®
VIVAPUR® and EMCOCEL®
Silicified Microcrystalline Cellulose (Microcrystalline Cellulose, Ph.Eur., NF, JP & Silica, Colloidal Anhydrous, Ph.Eur. & Colloidal Silicon Dioxide NF & Light Anhydrous Silicic Acid JP)
Microcrystalline Cellulose, Ph.Eur., NF, JP
PROSOLV SMCC® is the most significant innovation in high functionality excipients today. Used with simple direct compression, it emulates the outcome of alternative granulations while significantly reducing the number and quantity of excipients. PROSOLV SMCC® is the high functionality ingredient that offers significant benefits in terms of tablet size, production yield and overall cost. Early use in formulation development can result in early market entry, direct compression formulas and smaller tablets that consumers prefer. PROSOLV SMCC ‘s characteristics are high compactibility, high intrinsic flow, enhanced lubrication efficiency and improved blending properties. Its benefits are proven in formulation, manufacturing, marketing and regulatory approval. ®
Regulatory approvals have been simplified by the recognition that PROSOLV SMCC® is comprised of compendial excipients. Submissions have been approved in the USA, Europe and Japan. It is listed in the Inactive Ingredients Guide (IIG) of the US Food and Drug Administration (FDA) website.
These brands of MCC are preferred excipients in tablet manufacturing due to their high compactibility, inherent flow and ability to initiate disintegration. JRS Pharma has the benefit of multiple manufacturing plants for worldwide availability.
EMCOMPRESS® Calcium Hydrogen Phosphate Dihydrate, Ph.Eur., Dibasic Calcium Phosphate, Dihydrate, USP The first direct compression excipient. Its particles are of a size, shape, and density to maximize flow in high-speed tablet production and to reduce tablet weight variation. ANHYDROUS EMCOMPRESS® : In addition to excellent flow enhancement in direct compression. It does not contain water of crystallization and can be used with moisture sensitive actives. It is very often used in capsule formulations and to accelerate formulation development.
Soluble Tablet Binders: EMDEX® Dextrates, NF
A synergistic co-processing platform resulting in a co-processed API which becomes directly compressible, becomes a highly effective binder/carrier, has maximized flow and content uniformity, stabilizes hygroscopic actives. PROSOLV SMCC® co-processing provides the ultimate deaggregation and dispersion of the API.
Ideal for chewable products, it is the only compendial spherical dextrate available for direct compression that delivers the required flow, compaction and flavor carrying capacity for consumer products. EMDEX® has a great taste masking effect.
WORLDWIDE HEADQUARTERS JRS PHARMA
GMBH+CO.KG
Holzmühle 1 D-73494 Rosenberg (Germany) Phone: + 49 (0) 79 67 / 1 52-0 Fax: + 49 (0) 79 67 / 1 52-345 E-mail:
[email protected] www.jrspharma.de www.jrs.de Customer Service: +49 (0) 7967 / 152-312
USA + CANADA JRS PHARMA LP 2981 Route 22, Suite 1 Patterson, NY 12563-2359 Toll-Free: (800) 431-2457 Phone: +1 (845) 878-3414 Fax: +1 (845) 878-3484 E-mail:
[email protected] www.jrspharma.com
4282_001.GB0.00712pdf
PROSOLV® TECHNOLOGY:
Customer Service: +1 (845) 878-3414
FORMULATION HANDBOOK JRS Excipients
Product Overview Page 2/3
CANDEX® Dextrates A plant sourced tablet and capsule dextrate.
SUGARTAB® Compressible Sucrose
Disintegrants: EXPLOTAB® Sodium Starch Glycolate, Type (A) Ph.Eur., NF Sodium Carboxymethyl Starch, JPE
Excellent for chewable products, particularly vitamin formulations. It offers good flow, excellent compressibility and flavor masking.
The classical Super Disintegrant based on starch. The material shows excellent swelling properties and gives fast disintegration times in combination with water insoluble excipients. EXPLOTAB® corresponds to type A (Ph.Eur.), other types are available as well.
COMPACTROL®
VIVASTAR®
Calcium Sulfate Dihydrate, Ph.Eur., NF
Sodium Starch Glycolate, Type (A) Ph.Eur., NF Sodium Carboxymethyl Starch, JPE
A non-hygroscopic and free-flowing product that offers excellent and long-term stability. It can be used as a binder
Super disintegrant having great disintegration power and cost savings.
in wet granulation, especially in combination with starch or powdered cellulose. Due to its high bulk density and flowing characteristics, it imparts a high degree of fluidity which is
VIVASTAR® PSF is innovative in improving stability of certain drugs by removing residual solvents.
essential for high-speed compaction and capsule filling.
VIVASOL® Croscarmellose Sodium, Ph.Eur., NF, JPE
Functional Fillers: ARBOCEL® Powdered Cellulose, Ph.Eur., NF, JP Plant derived unique functional filler for capsules and tablets that shows excellent synergistic effect in hardness when used in combination with lactose and starch.
VIVAPRESS® Calcium Carbonate, Ph.Eur., USP Precipitated Calcium Carbonate, JP
Starch-free super disintegrant that adds excellent results at low use levels.
EMCOSOY® Soy Polysaccharides An all natural super disintegrant, which does not contain starch or sugar. Being a dietary fiber, it has excellent application in nutritional products.
SATIALGINE® A pharmaceutical grade alginic acid that offers rapid swelling in an aqueous medium. It can be moistened and dried without significant loss in disintegration and combines both a wicking and swelling mechanism to promote disintegration in either wet or dry granulations.
4282_001.GB0.00712pdf
Alginic Acid, NF A direct compressible, calcium containing filler. VIVAPRESS® meets Proposition 65 for lead content.
FORMULATION HANDBOOK JRS Excipients
Product Overview Page 3/3
Lubricants and Modified Release:
Thickener and Stabilizer:
PRUV ®
VIVAPUR® MCG
Sodium Stearyl Fumarate, Ph.Eur., NF, JPE
Microcrystalline Cellulose and Carboxymethylcellulose Sodium, NF
PRUV ® is a unique tablet lubricant that is more hydrophilic than traditional lubricants, less sensitive to blending and relatively inert. This results in tablets with improved disintegration and dissolution, harder tablets and better drug stability. It can be used in all tablet formulations including chewables and effervescent tablets.
An excellent thixotropic gelling agent to stabilize suspensions and emulsions. It is pH stable and could be used in hot and cold medium.
LUBRITAB® Hydrogenated Vegetable Oil, NF, BP Hydrogenated Oil, JP Less chemically reactive than most common lubricants, it can also be used as an auxiliary dry binder and controlled release matrix.
Carriers: NON-PAREIL SEEDS Sugar Spheres, NF Sugar spheres are used in multiple drug units for improved content uniformity, consistent and controlled drug release and high drug stability.
Coating and Sustained Release: VIVAPHARM®
Low viscosity types - the economical coating polymer for protecting tablets against moisture, light oxydation, and increased patients compliance.
Disclaimer: The information provided is based on thorough research and is believed to be completely reliable. Application suggestions are given to assist our customers, but are for guidance only. Circumstances in which our material is used vary and are beyond our control. Therefore, we cannot assume any responsibility for risks or liabilities, which may result from the use of this technical advice.
4282_001.GB0.00712pdf
Hydroxylpropyl Methylcellulose, Hypromellose, Ph.Eur., USP
FORMULATION HANDBOOK Table of Contents Guide Formulations
Acetylsalicylic Acid (Effervescent)
4282-001
Acetylsalicylic Acid (High Dosage)
4282-023
Acetylsalicylic Acid (OD Tablets)
4282-029
Allopurinol
4282-002
Ambroxol HCl
4282-003
Amoxicillin
4282-024
Atenolol
4282-030
Azitrhomycin
4282-033
Boswellia Serrata
4282-004
Calcium + Vitamin D3
4282-034
Cefalexin
4282-040
Chromium Picoliante
4282-005
Cimetidin
4282-025
Ciprofloxacin HCl
4282-006
Citramon Chewable Tablet
4282-041
Citramon Direct Compression
4282-042
Creatine Monohydrate
4282-028
Diazepam
4282-022
Enalapril
4282-007
Enalapril Hydrochlorothiazide
4282-043
Extract of Cartilage
4282-008
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GMBH+CO.KG
Holzmühle 1 D-73494 Rosenberg (Germany) Phone: + 49 (0) 79 67 / 1 52-0 Fax: + 49 (0) 79 67 / 1 52-345 E-mail:
[email protected] www.jrspharma.de www.jrs.de Customer Service: +49 (0) 7967 / 152-312
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USA + CANADA JRS PHARMA LP 2981 Route 22, Suite 1 Patterson, NY 12563-2359 Toll-Free: (800) 431-2457 Phone: +1 (845) 878-3414 Fax: +1 (845) 878-3484 E-mail:
[email protected] www.jrspharma.com
4282_001.GB0.00712pdf
No.
ARBOCEL® Powdered Cellulose EMCOMPRESS ® Calcium Hydrogen Phosphate EMCOSOY ® Soy Polysaccharides EMDEX ® Dextrates EXPLOTAB ® Sodium Starch Glycolate PROSOLV SMCC ® Silicified Microcrystalline Cellulose PRUV® Sodium Stearyl Fumarate VIVAPRESS ® Calcium Carbonate VIVAPUR® Microcrystalline Cellulose VIVASOL® Croscarmellose Sodium VIVASTAR® Sodium Starch Glycolate
Page 1/3
Customer Service: +1 (845) 878-3414
FORMULATION HANDBOOK Table of Contents Guide Formulations
Ginkgo Biloba
4282-009
Glucosamine
4282-010
Glucosamine-Chondroitin
4282-035
Guafenesin
4282-011
Ibuprofen (Direct Compression)
4282-012
Ibuprofen (Direct Compression)
4282-013
Ibuprofen (Wet Granulation)
4282-014
Lecithin
4282-031
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Liu’wei’di’huang TCM Fluid Bed Drying + Direct Compression 4282-027 Metformin
4282-015
Metformin
4282-026
Metoprolol (Direct Compression)
4282-016
Metoprolol (Direct Compression)
4282-017
Multivitamin Chewable Tablet V1
4282-032
Multivitamin Chewable Tablet V2
4282-039
Natural Herbal Laxative Cassia Senna + Melissa off.
4282-018
Paracetamol 500 mg
4282-038
Peppermint Oil (Direct Compression)
4282-037
Piroxicam
4282-019
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WORLDWIDE HEADQUARTERS JRS PHARMA
GMBH+CO.KG
Holzmühle 1 D-73494 Rosenberg (Germany) Phone: + 49 (0) 79 67 / 1 52-0 Fax: + 49 (0) 79 67 / 1 52-345 E-mail:
[email protected] www.jrspharma.de www.jrs.de Customer Service: +49 (0) 7967 / 152-312
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USA + CANADA JRS PHARMA LP 2981 Route 22, Suite 1 Patterson, NY 12563-2359 Toll-Free: (800) 431-2457 Phone: +1 (845) 878-3414 Fax: +1 (845) 878-3484 E-mail:
[email protected] www.jrspharma.com
4282_001.GB0.00712pdf
No.
ARBOCEL® Powdered Cellulose EMCOMPRESS ® Calcium Hydrogen Phosphate EMCOSOY ® Soy Polysaccharides EMDEX ® Dextrates EXPLOTAB ® Sodium Starch Glycolate PROSOLV SMCC ® Silicified Microcrystalline Cellulose PRUV® Sodium Stearyl Fumarate VIVAPRESS ® Calcium Carbonate VIVAPUR® Microcrystalline Cellulose VIVASOL® Croscarmellose Sodium VIVASTAR® Sodium Starch Glycolate
Page 2/3
Customer Service: +1 (845) 878-3414
FORMULATION HANDBOOK Table of Contents Guide Formulations
No. Ranitidine HCl
4282-020
Simethicone
4282-021
Simethicone (Direct Compression)
4282-045
Silymarin
4282-036
Vitamin C + Zink
4282-044
ARBOCEL® Powdered Cellulose EMCOMPRESS ® Calcium Hydrogen Phosphate EMCOSOY ® Soy Polysaccharides EMDEX ® Dextrates EXPLOTAB ® Sodium Starch Glycolate PROSOLV SMCC ® Silicified Microcrystalline Cellulose PRUV® Sodium Stearyl Fumarate VIVAPRESS ® Calcium Carbonate VIVAPUR® Microcrystalline Cellulose VIVASOL® Croscarmellose Sodium VIVASTAR® Sodium Starch Glycolate
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WORLDWIDE HEADQUARTERS JRS PHARMA
GMBH+CO.KG
Holzmühle 1 D-73494 Rosenberg (Germany) Phone: + 49 (0) 79 67 / 1 52-0 Fax: + 49 (0) 79 67 / 1 52-345 E-mail:
[email protected] www.jrspharma.de www.jrs.de Customer Service: +49 (0) 7967 / 152-312
USA + CANADA JRS PHARMA LP 2981 Route 22, Suite 1 Patterson, NY 12563-2359 Toll-Free: (800) 431-2457 Phone: +1 (845) 878-3414 Fax: +1 (845) 878-3484 E-mail:
[email protected] www.jrspharma.com
4282_001.GB0.00712pdf
Disclaimer: The information provided is based on thorough research and is believed to be completely reliable. Application suggestions are given to assist our customers, but are for guidance only. Circumstances in which our material is used vary and are beyond our control. Therefore, we cannot assume any responsibility for risks or liabilities, which may result from the use of this technical advice.
Customer Service: +1 (845) 878-3414
Back to Table of Contents
FORMULATION HANDBOOK Key Words:
# 4282-001 Acetylsalicylic Acid Direct Compression
High Dosage, Direct Compression
JRS Products: VIVAPUR® 102, VIVASTAR® P
Page 1/2
Comments: Acetylsalicylic acid (ASA) is an old, very well known active substance with analgesic and antipyretic properties. It is a non-steroidal anti-inflammatory drug which also inhibits platelet aggregation.
The common acetylsalicylic acid (ASA) dosage is 500 mg. In the following formulation VIVAPUR ® 102 is used as filler and binder, and VIVASTAR ® P as disintegrant.
Formulation Acetylsalicylic Acid (ASA) VIVAPUR® 102 (Microcrystalline Cellulose) VIVASTAR® P (Sodium Starch Glycolate) Magnesium Stearate Fumed Silica (Aerosil®)
Active content (mg) 500.0
mg/tablet 500.0 140.0 23.4 3.3 3.3
Contribution (%) 74.6 20.9 3.5 0.5 0.5
Tablet Characteristics Tablet Weight: Tablet Diameter: Compaction Force: Hardness: Disintegration Time:
670 mg 13 mm 27 - 28 kN 79.1 N 40 sec
Procedure Blending:
WORLDWIDE HEADQUARTERS JRS PHARMA GMBH+CO.KG
USA + CANADA JRS PHARMA LP
Holzmühle 1 D-73494 Rosenberg (Germany) Phone: + 49 (0) 79 67 / 1 52-0 Fax: + 49 (0) 79 67 / 1 52-345 E-mail:
[email protected] www.jrspharma.de www.jrs.de
2981 Route 22, Suite 1 Patterson, NY 12563-2359 Toll-Free: (800) 431-2457 Phone: +1 (845) 878-3414 Fax: +1 (845) 878-3484 E-mail:
[email protected] www.jrspharma.com
Customer Service: +49 (0) 7967 / 152-312
4282_001.GB0.00709pdf
Acetylsalicylic Acid (ASA), VIVAPUR® 102 and VIVASTAR® P were blended to homogeneity for 15 minutes. Then a sieved mixture of magnesium stearate and Aerosil® were added and mixed for another 5 minutes. The powder mix is ready for direct compression.
Customer Service: +1 (845) 878-3414
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FORMULATION HANDBOOK Key Words:
# 4282-001 Acetylsalicylic Acid Direct Compression
High Dosage, Direct Compression
JRS Products: VIVAPUR® 102, VIVASTAR® P
Page 2/2
Equipment: Tablet Press: Turbula Mixer: Hardness Tester: Friability Tester: Disintegration Tester: Dissolution Tester: Spectrophotometer:
Korsch EK 0, instrumented Type T2A Pharmatest PTB 311, n=6 ERWEKA TAP ERWEKA ZT 3 Pharmatest PTW II, with 6 vessels, flat blade paddle Shimadzu UV-2101 PC
Dissolution Test: Dissolution Medium: 900 ml 0.1 N HCl, 37°C, n=6 Samples are taken after 5, 10, 20, 30, 45 and 60 minutes. The sample volume is 3 ml. The determination of the active ingredient is done by an UV-spectrophotometer at = 280 nm.
120
Dissolved Active Ingredient (%)
110 100 90 80 70 60 50 40 30 20 10 0
0
5
10
15
30
45
60
Time (min) Diagram 1: Typical Dissolution Profile Diagram of an Acetylsalicylic Acid 500 mg Tablet, Produced According to the Above Given Formulation.
WORLDWIDE HEADQUARTERS JRS PHARMA GMBH+CO.KG
USA + CANADA JRS PHARMA LP
Holzmühle 1 D-73494 Rosenberg (Germany) Phone: + 49 (0) 79 67 / 1 52-0 Fax: + 49 (0) 79 67 / 1 52-345 E-mail:
[email protected] www.jrspharma.de www.jrs.de
2981 Route 22, Suite 1 Patterson, NY 12563-2359 Toll-Free: (800) 431-2457 Phone: +1 (845) 878-3414 Fax: +1 (845) 878-3484 E-mail:
[email protected] www.jrspharma.com
Customer Service: +49 (0) 7967 / 152-312
4282_001.GB0.00709pdf
Disclaimer: The information provided is based on thorough research and is believed to be completely reliable. Application suggestions are given to assist our customers, but are for guidance only. Circumstances in which our material is used vary and are beyond our control. Therefore, we cannot assume any responsibility for risks or liabilities, which may result from the use of this technical advice.
Customer Service: +1 (845) 878-3414
Back to Table of Contents
FORMULATION HANDBOOK
# 4282-023 Acetylsalicylic Acid Effervescent Tablet Direct Compression
Key Words:
Acetylsalicylic Acid, Direct Compression, Effervescent Tablet JRS Products: EMDEX ®, PRUV ®
Page 1/2
Comments: The acetylsalicylic acid is an old and very well known active with analgesic, antipyretic, antiinflammatory and antiaggregant
properties. Its lipophility and low water solubility make the development of an effervescent formulation a big challenge.
Formulation Acetylsalicylic Acid (ASA) PRUV ® (Sodium Stearyl Fumarate) Citric Acid NaHCO3 Glycine HCl Aspartame Flavour EMDEX® (Dextrates)
mg/Tablet 500.0 12.0 348.0 400.0 128.0 76.0 36.0 2500.0
Contribution (%) 12.5 0.3 8.7 10.0 3.2 1.9 0.9 62.5
4000.0
100.0
Total
Tablet Characteristics Compression Force Hardness Diameter Disintegration Time
20 kN 10.0 kp 25 mm 176 sec.
Procedure Blending: All ingredients except PRUV ® were blended for 15 minutes. The PRUV ® was added and the tabletting powder was mixed for another 3 min. Ready for direct compression.
Equipment: Korsch EK 0, instrumented 25 mm, biplane, Schleuniger 2E Pharmatest Standard PTZ Pharmatest PTW 2 Cecil Spektralphotometer, Series 1000
WORLDWIDE HEADQUARTERS JRS PHARMA GMBH+CO.KG
USA + CANADA JRS PHARMA LP
Holzmühle 1 D-73494 Rosenberg (Germany) Phone: + 49 (0) 79 67 / 1 52-0 Fax: + 49 (0) 79 67 / 1 52-345 E-mail:
[email protected] www.jrspharma.de www.jrs.de
2981 Route 22, Suite 1 Patterson, NY 12563-2359 Toll-Free: (800) 431-2457 Phone: +1 (845) 878-3414 Fax: +1 (845) 878-3484 E-mail:
[email protected] www.jrspharma.com
Customer Service: +49 (0) 7967 / 152-312
4282_023.GB0.00709pdf
Tablet Press: Tablet Diameter: Hardness Tester: Disintegration Tester: Dissolution Tester: Spectrophotometer:
Customer Service: +1 (845) 878-3414
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FORMULATION HANDBOOK
# 4282-023 Acetylsalicylic Acid Effervescent Tablet Direct Compression
Key Words:
Acetylsalicylic Acid, Direct Compression, Effervescent Tablet JRS Products: EMDEX ®, PRUV ®
Page 2/2
Dissolution Test: Dissolutuion Medium: 900 ml 0.1 N HCl, 37 °C, n=6 Samples are taken after 5, 10, 15, 30, 60, 120, 180 and 300 minutes. The sample volume is 3 ml. The probes were diluted if necessary. The determination of the acetylsalicylic acid was done by an UV-spectrophotometer at = 232.0 nm.
120 110 100
Dissolved Active (%)
90 80 70 60 50 40 30 20 10 0
0
20
40
60
80
100
120
140
160
180
200
220
240
260
280
300 320
Time (min) Diagram 1: Dissolution Profile of Acetylsalicylic Acid Effervescent Tablet, Produced According to the Above Given Formulation.
WORLDWIDE HEADQUARTERS JRS PHARMA GMBH+CO.KG
USA + CANADA JRS PHARMA LP
Holzmühle 1 D-73494 Rosenberg (Germany) Phone: + 49 (0) 79 67 / 1 52-0 Fax: + 49 (0) 79 67 / 1 52-345 E-mail:
[email protected] www.jrspharma.de www.jrs.de
2981 Route 22, Suite 1 Patterson, NY 12563-2359 Toll-Free: (800) 431-2457 Phone: +1 (845) 878-3414 Fax: +1 (845) 878-3484 E-mail:
[email protected] www.jrspharma.com
Customer Service: +49 (0) 7967 / 152-312
4282_001.GB0.00709pdf
Disclaimer: The information provided is based on thorough research and is believed to be completely reliable. Application suggestions are given to assist our customers, but are for guidance only. Circumstances in which our material is used vary and are beyond our control. Therefore, we cannot assume any responsibility for risks or liabilities, which may result from the use of this technical advice.
Customer Service: +1 (845) 878-3414
Back to Table of Contents
FORMULATION HANDBOOK Key Words:
# 4282-029
Acetylsalicylic Acid, Direct Compression, Fast Disintegration
JRS Products: PROSOLV SMCC ® 90, PURV ®, EXPLOTAB® , VIVASOL® , EMCOMPRESS ®
Acetylsalicylic Acid OD Tablets; DC Formulations Page 1
Comments: The acetylsalicylic acid is an old and very well known active with analgesic, antipyretic, antiinflammatory and antiaggregant properties. The permanently growing interest on ODT (Orally Disintegrating Tablets) in the last few years stimulate us to create these formulations.
Formulation Formulation Acetylsalicylic Acid PROSOLV SMCC® 90 (Silicified Microcrystalline Cellulose) Adipic Acid Citric Acid Sodium Hydrogencarbonate EMCOMPRESS® (Calcium Hydrogen Phosphate) EXPLOTAB® (Sodium Starch Glycolate) VIVASOL® (Croscarmellose Sodium) PRUV ® (Sodium Stearyl Fumarate)
1 71.43 20.00 4.00 2.86 1.00 0.71
Total
Substance (%) 2 3 70.43 70.43 20.00 14.00 4.00 4.00 2.86 2.86 1.00 5.00 2.00 2.00 0.71 0.71
4 70.43 14.00 7.50 6.36 1.00 0.71
100
100
100
100
29 0.68 13.40 7.10
27 0.61 14.30 6.80
28 0.87 20.00 7.10
40 1.18 22.10 8.10
Tablet Characteristics Disintegration Time (sec) Friability (%) Compression Force (kN) Hardness (kp)
Procedure All ingredients except PRUV ® were blended for 15 minutes. The PRUV ® was added and the tabletting powder was mixed for another 3 min. Ready for direct compression. Note: The mentioned above formulations do not contain taste masking substances!
WORLDWIDE HEADQUARTERS JRS PHARMA GMBH+CO.KG
USA + CANADA JRS PHARMA LP
Holzmühle 1 D-73494 Rosenberg (Germany) Phone: + 49 (0) 79 67 / 1 52-0 Fax: + 49 (0) 79 67 / 1 52-345 E-mail:
[email protected] www.jrspharma.de www.jrs.de
2981 Route 22, Suite 1 Patterson, NY 12563-2359 Toll-Free: (800) 431-2457 Phone: +1 (845) 878-3414 Fax: +1 (845) 878-3484 E-mail:
[email protected] www.jrspharma.com
Customer Service: +49 (0) 7967 / 152-312
4282_029.GB0.00708pdf
Disclaimer: The information provided is based on thorough research and is believed to be completely reliable. Application suggestions are given to assist our customers, but are for guidance only. Circumstances in which our material is used vary and are beyond our control. Therefore, we cannot assume any responsibility for risks or liabilities, which may result from the use of this technical advice.
Customer Service: +1 (845) 878-3414
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FORMULATION HANDBOOK Key Words:
# 4282-002
Poor Flowability, Direct Compression
JRS Products: VIVAPUR® 102, VIVASTAR® P
Allopurinol Direct Compression Page 1/2
Comments: Allopurinol is used to treat chronic gout (gouty arthritis). This condition is caused by too much uric acid in the blood. It is also used to prevent or treat other medical problems that may occur if too much uric acid is present in the body.
These include certain kinds of kidney stones or other kidney problems. Allopurinol can be directly compressed using VIVAPUR® Microcrystalline Cellulose as a binder.
Formulation Allopurinol VIVAPUR ® 102 (Microcrystalline Cellulose) VIVASTAR ® P (Sodium Starch Glycolate) Magnesium Stearate Fumed Silica (Aerosil® 200)
Active content (mg) 100.0
mg/tablet 100.0 72.0 6.2 0.9 0.9
Contribution (%) 55.5 40.0 3.5 0.5 0.5
Tablet Characteristics Tablet Weight: Tablet Diameter: Compaction Force: Hardness: Disintegration Time:
180 mg 9 mm 24 - 25 kN 91.3 N 11 sec
Procedure Blending: Allopurinol, VIVAPUR ® 102 and VIVASTAR ® P were mixed in a Turbula mixer for 15 minutes. Then a sieved mixture of magnesium stearate and Aerosil® were added and mixed for another 3 minutes. The powder mix was ready for direct compression.
Equipment: Korsch EK 0 eccentric press, 9 mm punch,biplane Type T2A Pharmatest PTB 311, n=6 Erweka TAP Erweka ZT 3 Pharmatest PTW II, with 6 vessels, flat blade paddle Shimadzu UV-2101 PC
WORLDWIDE HEADQUARTERS JRS PHARMA GMBH+CO.KG
USA + CANADA JRS PHARMA LP
Holzmühle 1 D-73494 Rosenberg (Germany) Phone: + 49 (0) 79 67 / 1 52-0 Fax: + 49 (0) 79 67 / 1 52-345 E-mail:
[email protected] www.jrspharma.de www.jrs.de
2981 Route 22, Suite 1 Patterson, NY 12563-2359 Toll-Free: (800) 431-2457 Phone: +1 (845) 878-3414 Fax: +1 (845) 878-3484 E-mail:
[email protected] www.jrspharma.com
Customer Service: +49 (0) 7967 / 152-312
4282_002.GB0.00709pdf
Tablet Press: Turbula Mixer: Hardness Tester: Friability Tester: Disintegration Tester: Dissolution Tester: Spectrophotometer:
Customer Service: +1 (845) 878-3414
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FORMULATION HANDBOOK Key Words:
# 4282-002
Poor Flowability, Direct Compression
JRS Products: VIVAPUR® 102, VIVASTAR® P
Allopurinol Direct Compression Page 2/2
Dissolution Test: Dissolution Medium: 900 ml 0.1 N HCl, 37°C, n=6 Samples are taken after 5, 10, 20, 30, 45 and 60 minutes. The sample volume is 3 ml. Samples were diluted if necessary. The determination of the active ingredient is done by an UV-spectrophotometer at = 248.8 nm. 120 100
Dissolved Active Ingredient (%)
90 80 70 60 50 40 30 20 10 0
0
5
10
15
20
25
30
35
40
45
50
55
60
65
Time (min) Diagram 1: Typical Dissolution Profile Diagram of a Allopurinol Tablet, Produced According to the Above Given Formulation.
WORLDWIDE HEADQUARTERS JRS PHARMA GMBH+CO.KG
USA + CANADA JRS PHARMA LP
Holzmühle 1 D-73494 Rosenberg (Germany) Phone: + 49 (0) 79 67 / 1 52-0 Fax: + 49 (0) 79 67 / 1 52-345 E-mail:
[email protected] www.jrspharma.de www.jrs.de
2981 Route 22, Suite 1 Patterson, NY 12563-2359 Toll-Free: (800) 431-2457 Phone: +1 (845) 878-3414 Fax: +1 (845) 878-3484 E-mail:
[email protected] www.jrspharma.com
Customer Service: +49 (0) 7967 / 152-312
4282_002.GB0.00709pdf
Disclaimer: The information provided is based on thorough research and is believed to be completely reliable. Application suggestions are given to assist our customers, but are for guidance only. Circumstances in which our material is used vary and are beyond our control. Therefore, we cannot assume any responsibility for risks or liabilities, which may result from the use of this technical advice.
Customer Service: +1 (845) 878-3414
Back to Table of Contents
FORMULATION HANDBOOK Key Words:
# 4282-003 Ambroxol HCl Direct Compression
Poorly Soluble, Low Dosage, Direct Compression
JRS Products: VIVAPUR® 12, ARBOCEL® A 300, VIVASOL®
Page 1/2
Comments: Ambroxol Hydrochloride is an example for a poorly soluble active substance used in low concentrations. It can be compressed directly by using VIVAPUR ® Microcrystalline Cellulose as a dry binder and ARBOCEL® Powdered Cellulose as a plantderived filler.
Ambroxol HCl is a mucolytic agent which is widely used in chronic bronchitis in Europe. Ambroxol HCl is very popular as an Active Pharmaceutical Ingredient (API) for children.
Formulation Ambroxol HCl VIVAPUR® 12 (Microcrystalline Cellulose) ARBOCEL® A 300 (Powdered Cellulose) VIVASOL® (Croscarmellose Sodium) Magnesium Stearate Fumed Silica (Aerosil® 200)
Active content (mg) 30.0
mg/tablet 30.00 69.30 46.20 3.00 0.75 0.75
Contribution (%) 20.0 46.2 30.8 2.0 0.5 0.5
Tablet Characteristics Tablet Weight: Tablet Diameter: Compaction Force: Hardness: Disintegration Time: Friability:
150 mg 8 mm 12.5 kN 64.0 N 13 sec
