PharmaExcipients.com’s Post

🔎🔎 Solubility of API in pharmaceutical solutions 🔸 Preformulation solubility studies usually include: • determinations of pKa. • temperature dependence. • pH solubility profile. • solubility products. • possible solubilization mechanisms. • rate of dissolution. 🔸 Factors effecting solubility: • pH • temperature • ionic strength • buffer concentrations. 🔎 For pH: - for weakly acid ⏩ increasing pH of solution Increasing solubility of API. - for weakly bases ⏩ increasing pH of solution decreasing solubility of API. ⚠️ It must be considerable for the STABILITY of the pharmaceutical solution: - the pH rate profile of API. - unionized/inonized ratio of API. - The possibility of acid-base catalysis of API in aqeous acidic or basic solution. 🔎 For ionic strength of API & interactions between two ionic moieties in same solutions: if your drug is ionic and reacts with one of the ionic additives of similar charges (e.g. the buffer components) make sure to keep the concentration of electrolytes in the formula as low as possible to slow down the degradation rate of the drug and visca varse with the different charges. 🔎 Common solubilization methods includes: • Co-solvency • Micronization • Using complexing agent • eutectic mixures by loading API on a Carrier. #pharmaceutical #solution #formulation #sterile #liquid

𝗢𝗽𝘁𝗶𝗺𝗶𝘇𝗮𝘁𝗶𝗼𝗻 𝗼𝗳 𝘄𝗲𝘁 𝗴𝗿𝗮𝗻𝘂𝗹𝗮𝘁𝗶𝗼𝗻 𝗽𝗿𝗼𝗰𝗲𝘀𝘀 𝗳𝗼𝗿 𝗺𝗮𝗻𝘂𝗳𝗮𝗰𝘁𝘂𝗿𝗶𝗻𝗴 𝗥𝗶𝘃𝗮𝗿𝗼𝘅𝗯𝗮𝗻 𝗴𝗲𝗻𝗲𝗿𝗶𝗰 𝗶𝗺𝗺𝗲𝗱𝗶𝗮𝘁𝗲-𝗿𝗲𝗹𝗲𝗮𝘀𝗲 𝘁𝗮𝗯𝗹𝗲𝘁𝘀 𝘂𝘀𝗶𝗻𝗴 𝗣𝗕𝗣𝗞 𝗺𝗼𝗱𝗲𝗹𝗶𝗻𝗴 𝗮𝗻𝗱 𝘀𝗶𝗺𝘂𝗹𝗮𝘁𝗶𝗼𝗻𝘀 Granulation is the critical process for the pharmaceutical development of poorly water-soluble drug products. Poorly formulated products have challenges in dissolution and bioequivalence studies. Rivaroxaban (RXB) is a poorly soluble drug and has 66% fasting bioavailability at a high strength of 20 mg. Learn more here: https://lnkd.in/eNKrsz9w #excipients

𝗔𝗻𝗮𝗹𝘆𝘀𝗶𝘀 𝗼𝗳 𝗣𝗼𝘄𝗱𝗲𝗿 𝗣𝗿𝗼𝗽𝗲𝗿𝘁𝗶𝗲𝘀 𝗼𝗳 𝗣𝗵𝗮𝗿𝗺𝗮𝗰𝗲𝘂𝘁𝗶𝗰𝗮𝗹 𝗘𝘅𝗰𝗶𝗽𝗶𝗲𝗻𝘁𝘀 𝗨𝘀𝗶𝗻𝗴 𝗮 𝗖𝗼𝗻𝘀𝘁𝗮𝗻𝘁-𝗩𝗼𝗹𝘂𝗺𝗲 𝗦𝗵𝗲𝗮𝗿 𝗧𝗲𝘀𝘁𝗲𝗿 Powders used in pharmaceuticals require good flowability. The angle of repose and compressibility index are often used to measure the flowability of pharmaceutical powders. However, confirming the relationship between external forces and flowability for smooth powder handling is necessary. Therefore, we measured pharmaceutical excipient powder using a lower cell direct movable constant-volume shear tester and evaluated the powder’s physical properties. In this study, we utilized microcrystalline cellulose, widely used as a pharmaceutical excipient and developed in many grades with different physical properties such as particle shape. We measured the shear parameters that describe the characteristic friction and cohesion properties of each microcrystalline cellulose grade. We found that the relative compression ratio (RCR) correlated with the angle of repose. Differences in the shape of the powder yield locus were observed among the grades, and the ratio of the upward convex area of the powder yield locus curve (APC) was defined as the value that quantified these differences. The study used various grades of #Ceolus #microcrystallinecellulose by Asahi Kasei

𝗙𝗼𝗿𝗺𝘂𝗹𝗮𝘁𝗶𝗼𝗻 𝗗𝗲𝘃𝗲𝗹𝗼𝗽𝗺𝗲𝗻𝘁, 𝗖𝗵𝗮𝗿𝗮𝗰𝘁𝗲𝗿𝗶𝘇𝗮𝘁𝗶𝗼𝗻, 𝗮𝗻𝗱 𝗘𝘃𝗮𝗹𝘂𝗮𝘁𝗶𝗼𝗻 𝗼𝗳 𝗕𝗲𝗱𝗮𝗾𝘂𝗶𝗹𝗶𝗻𝗲 𝗙𝘂𝗺𝗮𝗿𝗮𝘁𝗲 -𝗦𝗼𝗹𝘂𝗽𝗹𝘂𝘀® -𝗦𝗼𝗹𝗶𝗱 𝗗𝗶𝘀𝗽𝗲𝗿𝘀𝗶𝗼𝗻 Bedaquiline fumarate (BQF) is classified as a BCS class II drug and has poor water solubility and dissolution rate, which ultimately compromises bioavailability. The objective of this study is to improve the biopharmaceutical properties of BQF through a solid dispersion system by using Soluplus®. Two solid dispersion systems were prepared i.e., binary solid dispersion (BSD) and ternary solid dispersion (TSD) where 14.31-fold and 20.43-fold increase in solubility of BQF was observed with BSD and TSD in comparison to BQF. #pharmaceutical #excipient #Soluplus by BASF Pharma Solutions https://lnkd.in/ebq6Pd3W

𝗧𝗲𝗿𝗻𝗮𝗿𝘆 𝘀𝗼𝗹𝗶𝗱 𝗱𝗶𝘀𝗽𝗲𝗿𝘀𝗶𝗼𝗻𝘀 𝗼𝗳 𝗹𝗮𝗰𝗶𝗱𝗶𝗽𝗶𝗻𝗲: 𝗘𝗻𝗵𝗮𝗻𝗰𝗶𝗻𝗴 𝗱𝗶𝘀𝘀𝗼𝗹𝘂𝘁𝗶𝗼𝗻 𝗮𝗻𝗱 𝘀𝘂𝗽𝗲𝗿𝘀𝗮𝘁𝘂𝗿𝗮𝘁𝗶𝗼𝗻 𝗺𝗮𝗶𝗻𝘁𝗲𝗻𝗮𝗻𝗰𝗲 𝘁𝗵𝗿𝗼𝘂𝗴𝗵 𝘀𝘁𝗿𝗮𝘁𝗲𝗴𝗶𝗰 𝗳𝗼𝗿𝗺𝘂𝗹𝗮𝘁𝗶𝗼𝗻 𝗼𝗽𝘁𝗶𝗺𝗶𝘇𝗮𝘁𝗶𝗼𝗻 The study aimed to address the challenges related to insufficient dissolution and maintenance of supersaturation in binary solid dispersions. Lacidipine, categorized as a BCS class II drug, was employed as the model drug. A systematic screening of excipients was conducted to determine the most effective carriers for the formulations of the ternary solid dispersions, utilizing the solvent transfer method and equilibrium solubility measurements. Both binary and ternary solid dispersions were prepared via spray drying, and comprehensive physicochemical characterization confirmed the successful preparation of amorphous solid dispersions. #excipients #Soluplus by BASF Pharma Solutions #Gelucire by Gattefossé Pharmaceuticals

𝗔𝗻𝗮𝗹𝘆𝘀𝗶𝘀 𝗼𝗳 𝗣𝗼𝘄𝗱𝗲𝗿 𝗣𝗿𝗼𝗽𝗲𝗿𝘁𝗶𝗲𝘀 𝗼𝗳 𝗣𝗵𝗮𝗿𝗺𝗮𝗰𝗲𝘂𝘁𝗶𝗰𝗮𝗹 𝗘𝘅𝗰𝗶𝗽𝗶𝗲𝗻𝘁𝘀 𝗨𝘀𝗶𝗻𝗴 𝗮 𝗖𝗼𝗻𝘀𝘁𝗮𝗻𝘁-𝗩𝗼𝗹𝘂𝗺𝗲 𝗦𝗵𝗲𝗮𝗿 𝗧𝗲𝘀𝘁𝗲𝗿 Powders used in pharmaceuticals require good flowability. The angle of repose and compressibility index are often used to measure the flowability of pharmaceutical powders. However, confirming the relationship between external forces and flowability for smooth powder handling is necessary. Therefore, we measured pharmaceutical excipient powder using a lower cell direct movable constant-volume shear tester and evaluated the powder’s physical properties. In this study, we utilized microcrystalline cellulose, widely used as a pharmaceutical excipient and developed in many grades with different physical properties such as particle shape. We measured the shear parameters that describe the characteristic friction and cohesion properties of each microcrystalline cellulose grade. We found that the relative compression ratio (RCR) correlated with the angle of repose. Differences in the shape of the powder yield locus were observed among the grades, and the ratio of the upward convex area of the powder yield locus curve (APC) was defined as the value that quantified these differences. Learn more here: https://lnkd.in/eGD4jbZ8 The study used various grades of #Ceolus #microcrystallinecellulose by Asahi Kasei

Extrusion-spheronization is a cornerstone technique in pharmaceutical manufacturing, transforming drug substances and excipients into uniform, spherical granules (or pellets) with benefits including:  ✅ High drug load  ✅ Uniform distribution of API  ✅ Controlled release profiles  ✅ Enhanced dissolution rates  ✅ Improved bioavailability  ✅ Ease of coating Discover the critical roles of adsorption and absorption during the extrusion-spheronization process in our latest blog, and learn how these molecular forces contribute to optimised drug formulations for better therapeutic effects and improved patient outcomes. Find our latest blog here: https://lnkd.in/eJ3-wx6R #adsorption #absorption #adsorptionandabsorption #agglomeration #granulation #particletechnology #wetgranulation #extrusion #spheronization #pellets #granules #controlledrelease

𝗧𝗬𝗟𝗢𝗣𝗨𝗥® – 𝗪𝗮𝘁𝗲𝗿 𝘀𝗼𝗹𝘂𝗯𝗹𝗲 𝗰𝗲𝗹𝗹𝘂𝗹𝗼𝘀𝗲 𝗲𝘁𝗵𝗲𝗿𝘀 𝗯𝘆 𝗦𝗵𝗶𝗻-𝗘𝘁𝘀𝘂 TYLOPUR® is Hypromellose (HPMC) and a versatile pharmaceutical excipient. TYLOPUR® is manufactured at Tyloshin 2 plant at SE Tylose GmbH & Co. KG in Wiesbaden, Germany. This plant operates under GMP conditions and fulfills the requirements of the pharmaceutical industry. SE Tylose is a materials producer with an emphasis on a stable supply of high-quality products. One of TYLOPUR® applications is film coating and it is easy to use as a coating material to provide an excellent finish. In addition, TYLOPUR® is effective as a granulation binder since it does not interact with drugs, has superior stability and has a nonionic character. It is available in various viscosity grades for the granulation process. Read more about TYLOPUR® in the article. #excipient #Tylopur by Shin-Etsu SE Tylose GmbH & Co. KG

I am pleased to share our latest article published in the Journal of Pharmaceutical and Biomedical Analysis, titled "Novel multiple extraction thermal desorption approach prior to gas chromatography for the determination of residual solvents applied to modified cellulose." A novel extraction approach based on thermal desorption was developed and validated, providing alternatives for the determination of trace level volatile in field of pharmaceutical analysis. #thermal desorption-gas chromatography #residual solvents #multiple extraction #pharmaceutical analysis https://lnkd.in/e4u-ea3p

#inhalation#drugvaporization#lung#cbd#nanocapsules# Rapid heating and vaporization of solid API´s has been used by innovative pharmaceutical companies that is the point for Loxapine ( Stacatto Loxapine Ferrer Labs) and some other actives under development ( alprazolam, apomorphine for example) These developments are based on exipient-free drugs and aerosol creation by rapid heating with minimal degradation. The effects of exipients normally used in vape formulations could be related to health problems like lipoid pneumonia developed when fatty acids enter the lungs . Actually innovative CBD formulation based on polymer nanocapsules does not use those lipids. Flavoring e-liquid vape cigarettes to enhance taste can include chemicals like diacetyl which causes inflammation and may lead to permanent damage ot the smallest branches of the airways which can make breathing difficult Innovative vaporization of CBD (1000 mg / 1 ml) and other pharmaceutical API´s can be effectively achieved by Polymicrocaps nanoencapsulation technology.