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𝗗𝗿𝘆 𝗔𝗺𝗼𝗿𝗽𝗵𝗶𝘇𝗮𝘁𝗶𝗼𝗻 𝗼𝗳 𝗜𝘁𝗿𝗮𝗰𝗼𝗻𝗮𝘇𝗼𝗹𝗲 𝗨𝘀𝗶𝗻𝗴 𝗠𝗲𝘀𝗼𝗽𝗼𝗿𝗼𝘂𝘀 𝗦𝗶𝗹𝗶𝗰𝗮 𝗮𝗻𝗱 𝗧𝘄𝗶𝗻-𝗦𝗰𝗿𝗲𝘄 𝗧𝗲𝗰𝗵𝗻𝗼𝗹𝗼𝗴𝘆 by Dr. Margarethe Richter, Dr. Simon Welzmiller , Fred Monsuur , Annika Völp and Dr. Joachim Quadflieg  Amorphization of an active pharmaceutical ingredient (API) can improve its dissolution and enhance bioavailability. Avoiding solvents for drug amorphization is beneficial due to environmental issues and potential solvent residues in the final product. Dry amorphization using a twin-screw extruder is presented in this paper. A blend of mesoporous silica particles and crystalline itraconazole was processed using a pharma-grade laboratory scale twin-screw extruder. The influence of different screw configurations and process parameters was tested. Particle size and shape are compared in scanning electron microscopy (SEM) images. Differential scanning calorimetry (DSC) and X-ray diffraction (XRD) are used to determine the residual amount of crystalline itraconazole in the final product. Read more in the article.

𝗔𝗱𝘃𝗮𝗻𝗰𝗲𝗺𝗲𝗻𝘁𝘀 𝗶𝗻 𝗖𝗼𝗹𝗼𝗻-𝗧𝗮𝗿𝗴𝗲𝘁𝗲𝗱 𝗗𝗿𝘂𝗴 𝗗𝗲𝗹𝗶𝘃𝗲𝗿𝘆: 𝗔 𝗖𝗼𝗺𝗽𝗿𝗲𝗵𝗲𝗻𝘀𝗶𝘃𝗲 𝗥𝗲𝘃𝗶𝗲𝘄 𝗼𝗻 𝗥𝗲𝗰𝗲𝗻𝘁 𝗧𝗲𝗰𝗵𝗻𝗶𝗾𝘂𝗲𝘀 𝘄𝗶𝘁𝗵 𝗘𝗺𝗽𝗵𝗮𝘀𝗶𝘀 𝗼𝗻 𝗛𝗼𝘁-𝗠𝗲𝗹𝘁 𝗘𝘅𝘁𝗿𝘂𝘀𝗶𝗼𝗻 𝗮𝗻𝗱 𝟯𝗗 𝗣𝗿𝗶𝗻𝘁𝗶𝗻𝗴 𝗧𝗲𝗰𝗵𝗻𝗼𝗹𝗼𝗴𝗶𝗲𝘀 This review investigates the progression and effectiveness of colon-targeted drug delivery systems, offering a comprehensive understanding of the colon’s anatomy and physiological environment. Recognizing the distinctive features of the colon is crucial for successfully formulating oral dosage forms that precisely target specific areas in the gastrointestinal tract (GIT) while minimizing side effects through mitigating off-target sites. This understanding forms the basis for designing effective targeted drug delivery systems. The article extensively examines diverse approaches to formulating drugs for colonic targeting, highlighting key polymers and excipients in their production. Special emphasis is given to innovative approaches such as hot-melt extrusion (HME) and three-dimensional printing (3D-P), renowned for their accuracy in drug release kinetics and intricate dosage form geometry. Read more in the article. #Pharmaceutical #ColonTargeting #3DPrinting #HME

𝗘𝘃𝗮𝗹𝘂𝗮𝘁𝗶𝗼𝗻 𝗼𝗳 𝘁𝗵𝗲 𝗶𝗺𝗽𝗮𝗰𝘁 𝗼𝗳 𝘁𝗵𝗲 𝗽𝗼𝗹𝘆𝗺𝗲𝗿 𝗲𝗻𝗱 𝗴𝗿𝗼𝘂𝗽𝘀 𝗮𝗻𝗱 𝗺𝗼𝗹𝗲𝗰𝘂𝗹𝗮𝗿 𝘄𝗲𝗶𝗴𝗵𝘁 𝗼𝗻 𝗶𝗻 𝘃𝗶𝘁𝗿𝗼 𝗮𝗻𝗱 𝗶𝗻 𝘃𝗶𝘃𝗼 𝗽𝗲𝗿𝗳𝗼𝗿𝗺𝗮𝗻𝗰𝗲𝘀 𝗼𝗳 𝗣𝗟𝗚𝗔 𝗯𝗮𝘀𝗲𝗱 𝗶𝗻 𝘀𝗶𝘁𝘂 𝗳𝗼𝗿𝗺𝗶𝗻𝗴 𝗶𝗺𝗽𝗹𝗮𝗻𝘁𝘀 𝗳𝗼𝗿 𝗸𝗲𝘁𝗼𝗽𝗿𝗼𝗳𝗲𝗻 In situ forming implants are appealing long-acting dosage forms for both preclinical and clinical applications due to their simple manufacturing process and easy delivery. This study aims to develop extended-release in situ forming solid implants for subcutaneous administration using two types of commercially available triblock poly (lactic-co-glycolic acid)-poly (ethylene glycol)-poly (lactic-co-glycolic acid) (PLGA-PEG-PLGA) polymers, with either an acid or ester end group. Both types of polymers instantly form in situ implants when injected directly into an aqueous medium. The performance of these implants, containing a model compound ketoprofen, was evaluated by comparing the in vitro drug release profiles with the in vivo performance following subcutaneous administration in rats. Analytical characterizations of two representative in situ implants were conducted to understand their structural impact on polymer degradation and drug release. All tested in situ forming implants demonstrated prolonged drug release profiles both in vitro and in vivo. This study illustrates the successful preparation of sustained-release in situ forming implant formulations for ketoprofen using commercially available polymers, with the molecular weight and the end group of the polymers affecting their degradation and the drug release from the in situ formed implants. #excipients #PLGA #PEG

𝗘𝗳𝗳𝗲𝗰𝘁 𝗼𝗳 𝗟𝗶𝗾𝘂𝗶𝗱 𝗟𝗼𝗮𝗱 𝗟𝗲𝘃𝗲𝗹 𝗮𝗻𝗱 𝗕𝗶𝗻𝗱𝗲𝗿 𝗧𝘆𝗽𝗲 𝗼𝗻 𝘁𝗵𝗲 𝗧𝗮𝗯𝗹𝗲𝘁𝗮𝗯𝗶𝗹𝗶𝘁𝘆 𝗼𝗳 𝗠𝗲𝘀𝗼𝗽𝗼𝗿𝗼𝘂𝘀 𝗦𝗶𝗹𝗶𝗰𝗮 𝗕𝗮𝘀𝗲𝗱 𝗟𝗶𝗾𝘂𝗶𝘀𝗼𝗹𝗶𝗱𝘀 Mesoporous silica offers an easy way to transform liquids into solids, due to their high loading capacity for liquid or dissolved active ingredients and the resulting enhanced dissolution properties. However, the compression of both unloaded and loaded mesoporous silica bulk material into tablets is challenging, due to poor/non-existing binding capacity. This becomes critical when high drug loads are to be achieved and the fraction of additional excipients in the final tablet formulation needs to be kept at a minimum. Our study aimed to investigate the mechanism of compression and tabletability dependent on the Liquid Load Level of the silica and type of filler/binder in binary tabletting mixtures. To this end, #Vivapur® 101, #FlowLac® 90, #Pearlitol® 200 SD and tricalcium citrate tetrahydrate were selected and mixed with #Syloid® XDP 3050 at various Liquid Load Levels. Compaction characteristics were analysed using the #StylOne® Classic 105 ML compaction simulator.  Read more in the article. JRS PHARMA MEGGLE Excipients Roquette Pharma Solutions W. R. Grace MEDELPHARM

𝗧𝗵𝗲 𝗥𝗼𝗹𝗲 𝗼𝗳 𝗖𝗼𝗮𝘁𝗶𝗻𝗴𝘀 𝗮𝗻𝗱 𝗣𝗹𝗮𝘀𝘁𝗶𝗰𝗶𝘇𝗲𝗿𝘀 𝗖𝗼𝗺𝗽𝗮𝘁𝗶𝗯𝗶𝗹𝗶𝘁𝘆 𝗶𝗻 𝗦𝘁𝗮𝗯𝗶𝗹𝗶𝘁𝘆 𝗼𝗳 𝗔𝗱𝘃𝗮𝗻𝗰𝗲𝗱 𝗚𝗮𝘀𝘁𝗿𝗼-𝗿𝗲𝘀𝗶𝘀𝘁𝗮𝗻𝘁 𝗦𝗲𝗹𝗳-𝗲𝗺𝘂𝗹𝘀𝗶𝗳𝘆𝗶𝗻𝗴 𝗣𝗲𝗹𝗹𝗲𝘁𝘀 𝗗𝗲𝘀𝗶𝗴𝗻𝗲𝗱 𝗳𝗼𝗿 𝘁𝗵𝗲 𝗗𝗲𝗹𝗶𝘃𝗲𝗿𝘆 𝗼𝗳 𝗩𝗼𝗹𝗮𝘁𝗶𝗹𝗲 𝗖𝗼𝗺𝗽𝗼𝘂𝗻𝗱𝘀: 𝗔 𝗖𝗼𝗺𝗯𝗶𝗻𝗲𝗱 𝗦𝗼𝗹𝗶𝗱-𝗦𝘁𝗮𝘁𝗲 𝗡𝗠𝗥 𝗮𝗻𝗱 𝗗𝗶𝘀𝘀𝗼𝗹𝘂𝘁𝗶𝗼𝗻 𝗦𝘁𝘂𝗱𝘆 The gastro-resistant behaviour of solid self-emulsifying drug delivery systems (S-SEDDS) represents a significant and innovative advancement in delivering poorly soluble drugs. Due to the complexity of these systems and the liquid nature of SEDDS, thorough investigation is essential. This study explored the stability of self-emulsifying (SE) pellets containing the volatile compound thymol coated with gastro-resistant #Eudragit® L 30 D-55 water dispersion. The SE pellet cores, composed of #Neusilin® US2 with adsorbed SEDDS (thymol, triacylglycerol, #Labrasol®, and propylene glycol), microcrystalline cellulose, and chitosan, were prepared using the extrusion/spheronization method and demonstrated optimal technological properties. #excipients by Evonik Health Care Fuji Chemical Industries Co., Ltd. Fuji Chemical Industries USA, Inc Gattefossé Pharmaceuticals

𝗜𝗻𝘃𝗲𝘀𝘁𝗶𝗴𝗮𝘁𝗶𝗻𝗴 𝘁𝗵𝗲 𝗘𝗳𝗳𝗲𝗰𝘁𝘀 𝗼𝗳 𝗙𝗼𝗿𝗺𝘂𝗹𝗮𝘁𝗶𝗼𝗻 𝗩𝗮𝗿𝗶𝗮𝗯𝗹𝗲𝘀 𝗼𝗻 𝘁𝗵𝗲 𝗗𝗶𝘀𝗶𝗻𝘁𝗲𝗴𝗿𝗮𝘁𝗶𝗼𝗻 𝗼𝗳 𝗦𝗽𝗿𝗮𝘆 𝗗𝗿𝗶𝗲𝗱 𝗔𝗺𝗼𝗿𝗽𝗵𝗼𝘂𝘀 𝗦𝗼𝗹𝗶𝗱 𝗗𝗶𝘀𝗽𝗲𝗿𝘀𝗶𝗼𝗻 𝗧𝗮𝗯𝗹𝗲𝘁𝘀 Amorphous solid dispersion (#ASD) tablets based on hydrophilic polymer carriers may encounter disintegration challenges. In this work, the effect of different formulation composition variables on the ASD tablet disintegration performance was systematically studied. GDC-0334: copovidone (#PVPVA) 60: 40 ASD prepared by spray drying was selected as the model ASD system. The effects of ASD loading, filler type and ratio, disintegrant type and level were then investigated using tablets made by direct compression process. Tablet disintegration time increased with the increase of ASD loading, especially when ASD loading exceeded 50%. At the same tablet solid fraction, when lactose was used as the soluble filler, faster tablet disintegration time was observed compared to the tablets with mannitol as the soluble filler. Among the three tested disintegrants, croscarmellose sodium performed the best in facilitating the ASD tablet disintegration, followed by sodium starch glycolate, and crospovidone was the poorest. When croscarmellose sodium was used as the disintegrant, 5% level was sufficient to enable ASD tablet disintegration at 60% ASD loading and further increase of croscarmellose sodium level to 8% did not provide additional benefit. Water uptake experiments were performed on selected tablets and the results demonstrated a positive correlation with tablet disintegration time, indicating water penetration is a major contributing step for the disintegration of our ASD tablets. Overall, this work provides a rationale for excipient selection and insights into building a platform formulation approach for developing immediate-release ASD tablets.

𝗕𝗶𝘀𝗼𝗽𝗿𝗼𝗹-𝗘𝘅𝗰𝗶𝗽𝗶𝗲𝗻𝘁 𝗖𝗼𝗺𝗽𝗮𝘁𝗶𝗯𝗶𝗹𝗶𝘁𝘆 𝗦𝘁𝘂𝗱𝗶𝗲𝘀 𝗙𝗼𝗿 𝗔𝗱𝘃𝗮𝗻𝗰𝗲𝗱 𝗗𝗿𝘂𝗴 𝗗𝗲𝗹𝗶𝘃𝗲𝗿𝘆 𝗦𝘆𝘀𝘁𝗲𝗺𝘀 𝗗𝗲𝘃𝗲𝗹𝗼𝗽𝗺𝗲𝗻𝘁 Fast dissolving drug delivery systems offers a solution for pediatric, geriatric, mentally ill people and those patients having difficulty in swallowing tablets or capsules. In the present study, an attempt had been made to prepare fast dissolving tablets of Bisoprolol Fumarate, an antihypertensive agent. The main objective of the present study was to the preformulation studies were performed to know the physio-chemical and mechanical properties of Bisoprolol Fumarate for formulation development of Bisoprolol Fumarate FDTs. The safety, efficacy, quality and stability of a formulation are major concepts of any API development process. In API development process, a detailed characterization of the API and other formulation components is usually carried out during the preformulation stage. #pharmaceutical #excipients

𝗥𝗲𝗮𝗹-𝘁𝗶𝗺𝗲 𝗽𝗿𝗲𝗱𝗶𝗰𝘁𝗶𝗼𝗻 𝗼𝗳 𝗱𝗶𝘀𝘀𝗼𝗹𝘂𝘁𝗶𝗼𝗻 𝗽𝗿𝗼𝗳𝗶𝗹𝗲𝘀 𝗼𝗳 𝗰𝗼𝗮𝘁𝗲𝗱 𝗼𝗿𝗮𝗹 𝗱𝗼𝘀𝗮𝗴𝗲 𝗳𝗼𝗿𝗺𝘀 by Stephan Sacher, Elisabeth Fink, Carolina Alva, Jesús Alberto Afonso Urich, Aygün Doğan, Vanessa Herndler, Ioannis Koutsamanis, Dr. Varun Kushwah, Anna Peter, Sharareh Salar-Behzadi, Katrina Wilfling, Sandra Stranzinger, Manuel Zettl, Xin Feng, Maxwell K., Huiquan Wu, Johannes Khinast Optical coherence tomography (#OCT) has emerged as an in-line monitoring technique for pharmaceutical coating processes based on a representative number of samples. In this study, an approach was developed to correlate the coating thickness measured in-line via OCT with the resultant tablet dissolution profile. This strategy enables prediction of the dissolution profile of coated oral dosage forms for each individual state of the coating process in real-time. Correlation models were developed for a tablet pan coating process and for a pellet fluid-bed coating process. The feasibility of the correlation models was tested using different process parameters and types of coating formulations. This work demonstrated that using the OCT data to predict dissolution could possibly form a unique way of assuring drug product quality and establishing a control strategy within the real-time release testing (RTRT) concept. #pharmaceutical #coating

𝗣𝗮𝘁𝗲𝗻𝘁 𝗼𝗻 𝗲𝘅𝘁𝗲𝗻𝗱𝗲𝗱 𝗿𝗲𝗹𝗲𝗮𝘀𝗲 𝗰𝗼𝗺𝗽𝗼𝘀𝗶𝘁𝗶𝗼𝗻𝘀 𝗰𝗼𝗺𝗽𝗿𝗶𝘀𝗶𝗻𝗴 𝗽𝘆𝗿𝗶𝗱𝗼𝘀𝘁𝗶𝗴𝗺𝗶𝗻𝗲 The following patent on “Extended release compositions comprising pyridostigmine” employs #CELLETS® as starter spheres made of Microcrystalline Cellulose. Read the article to learn more. ingredientpharm #MCC #Cellets