- Dilip Parikh added an answer:20Can Hypromellose (HPMC) added in wet granulation process act as a protection film?Can Hypromellose (HPMC) added in wet granulation process act as a protection film in order to isolate granules from extra granular ingredients in formula or from moisture and other environmental factors?
My colleagues believe it can be done. But I can not find any references discussing about this function of HPMC. Furthermore, I don't buy their premise since the contact surface of granules is too large for HPMC to cover. Do you have any ideas?
BY using high molecular weight polymer you can granulate in conventional high shear mixer and form a film that will form retarded release of your drug. Depending on the concentration of polymer used, the solvent used in the granulation may be very hard to evaporate even if you FBDFollowing
- Brannon Mccullough added an answer:4Any suggestions on drug targets for preventing traumatic neuroma formation in amputees?
Main theoretical goal is to inhibit formation of growth cone in uncontrolled regenerating peripheral axons. The opposite of SCI studies suggests upregulating RhoA/ROCK2/LIMK pathway will deactivate Cofilin and MLC phosphatase causing collapse of the growth cone. Permanent activation using allosteric agonist of the autoinhibitory Rho associated kinase 2 however will be difficult and likely have bad side effects. Any more specific or generalized suggestions from a medicinal chemistry perspective eg. stimulating CSPGs receptors or preventing microtubule formation in cone?
Several ROCK, LIMK, MLC inhibitors have been developed if you are interested in targeting that specific pathway.Following
- Kulvinder Singh Saini added an answer:5Where can we source New Chemical Entities (NCEs) against breast cancer, which failed in phase-1 or 2 clinical trials?
Does anyone know, if global pharmaceutical/biotech companies/NIH, USA/USFDA, NGOs, etc. will be willing to give/sell us small amounts (mg quantity) of their small molecule compounds (NCEs), where possible toxicity issues hampered their clinical development as cancer therapeutics? We are interested in further exploring Toxicogenomics and mechanism-of-actions of these NCEs in a mouse model of breast cancer? Even NCEs which failed in clinical development against other cancers will be of great research interest to us.
Please check this URL from AstraZenecaFollowing
- Atit Pandey added an answer:3What is the logic behind carrying out uniformity of dispersion test through 22 mesh?
Uniformity of dispersion test for tablets is carried out by passing through 22 mesh, is there any physiological relation with that?
Dear Harshita Madam,
Disintegration test is carried out through 10 mesh as specified in USP, whereas Dispersion is through 22 mesh. Can you clarify the reason behind that??Following
- R. Selvam added an answer:4Does anyone know where I can obtain lyophilized herceptin for preclinical R&D?
I am looking for lyophilized herceptin. Would anyone (not affiliated with Genentech) be willing to provide this material? Or do they know of another company that will sell it (or the generic version) to me?
Dear Thad Wadas,
Send your quires to us, www.gmrfoundation.com , we can able to provide lyophilized herceptin, if you need any other specification also inform us, For only R&D use, not for any human use.,
Good Luck & Regards
- Gajendra Pal Singh Raghava added an answer:2What are the major platforms in computation and in vitro techniques for measuring oral bioavailability?
We are interested to screen molecules particularly peptides that can be delivered orally. Please write name of software or web server which we can use for predicting oral-delivery potential of a molecule. I will appreciate if you write free (open source software) for predicting bio availability of molecules particularly peptides and proteins. Please also write in vitro techniques (assays ) that correlate with in vivo bio availability of molecules.
- Ramesh Chandra added an answer:2What is the reason behind pharmacopoeial specification of 10 mesh size in USP disintegration apparatus?
Any physiological logic behind the mesh size?
in this guidance the size of sprinkle granules, coated beads etc was proposed to be
0.82 to 3.04 mm before swallowing and the average value will be 1.93 i.e 2 if you round it .so 2mm 10# is the regular size for a particle to get dissolved as per US.Following
- Ramkumar Ponnuraj added an answer:4How can one prepare a tablet of pre-liposomes to govern in situ formation of liposomes?
I have seen many Research Articles starting with the topic "Tablets of pre-liposomes govern in situ formation of liposomes"
Can anyone share the open access of such article?
If not can anyone share me how to prepare the pre-liposomes?
Your valuable suggestion is really appreciated.
Thanks in advance
It not possible for me to access full text from science direct, but I got the article from author. Thanks to Ms Natasa.Following
- Narong Chamkasem added an answer:4I am trying to develop
I am trying to develop a HPLC method for
If you have polar analytes that not well retained on the C18 or have the same retention time, and you want to separate them well in a single run, I would recommend you to explore the mixed-phase mode or HILIC. The idea is to retain by ion-exchange and elute with pH or salt. Attached file is the example for you to consider.Following
- Bruce Koch added an answer:6What are the best kinase inhibition profiling assays and microsome stability test systems for anti-tumor property screening?
We test small molecule compounds for anti-tumor properties. We would like to test the kinase inhibition activity of our lead candidate. We don't know its biological target yet. No prior experience in these types of assays.
Which is your favorite company/screening technology (in the United States) to test the kinase inhibition activity of your compound? Is a functional assay necessary or is a binding assay sufficient in this case?
Also, which assay kit/company do you use for testing the microsome stability of your compound?
Our experience is that assaying a subset of the kinome is not very informative. Inhibitors are often selective between closely related kinases, but then hit somewhere else in the kinome. You might check out DiscoverX KinomeScan (formerly Ambit).Following
- R. Jagathesh Chandra Bose added an answer:4How to determine the % cumulative drug release from PLGA microparticles?I am determining the in vitro drug release profile from micro-particles, where I have 10 mg microparticles suspended in 5 ml release medium and at each time points I withdraw 1 ml of supernatant (replacing with 1 ml of fresh release medium) and analyze it with HPLC. However, I am getting a bit confused regarding % cumulative release calculations. Do I simply add up the percentage release values at each time points? My confusion is that since I withdraw just 1 ml (out of 5 ml) for analysis, do I need to account for total volume and how do I account for dilution when I replace with 1 ml fresh media? Any help will be appreciated. Thank you.Following
- Majid Avijgan added an answer:7Where can I test and confirm Anti-tuberculosis and Anti-HIV activity for Plant extract samples?
Hi friends, I wish to do Antituberculosis and Anti HIV activity for Plant samples. Do you people know about any one doing out sourcing these experiments. I am ready to pay for this work. Or I will give authorship This work is my own interest on natural drug discovery.
I have several studies on the echinophora platyloba as an anti fungal herb. I have experience of what you are looking for. It is easy and simple, just invite from one of the pharmaceutic for co-operation. I have one co-worker in my paper as Dr Mohadese Mahboubi. Her email is as firstname.lastname@example.orgFollowing
- M. Eugenio Vazquez added an answer:6Does anyone know a simple technique for studying small molecule-DNA interactions, especially binding type kinetics?.
By the way, we have also used single-molecule fluorescence to study the dynamics of the binding process. Take a look at:
J. Bordello, M.I. Sánchez, M.E. Vázquez, J.L. Mascareñas, W. Al-Soufi, M. Novo, Chem. Eur. J., 2014, (DOI: 10.1002/chem.201404926).
J. Bordello, M.I. Sánchez, M.E. Vázquez, J L. Mascareñas, W. Al-Soufi, M. Novo. Angew. Chem. Int. Ed., 2012, 51, 7541–7544. (DOI: 10.1002/anie.201201099).Following
- Patrick M Dansette added an answer:3Does anyone know an in-vitro protocol for inhibition of Monoamine Oxidase-A and B? can you send Protocol or share some useful articles?
Hi, all researcher I want to check activity of plant extracts against Monoamine Oxidase-A and B. If someone have its few or detailed protocol kindly send it to me. Every single effort will be highly appreciate.
In principle seleginine (deprenyl) will inhibit MAO B (suicide inhibitor)
and clorgynine will inactivate MAO-A (you could also use isoproniazide.
We used these inhibitors in the joined paperFollowing
- Arpana Mishra added an answer:10Is aluminum a good material for electrodes regarding an In vivo Electroporation project?
I will be conducting an in vivo test to define transdermal delivery via topical/skin electroporation. I will be applying a drug to the patients skin and using an in vivo electrode to carry the drug into the dermis. I need help however when it comes to the electrode. I want to make 'meander' electrodes, and I would like to know if aluminum is a good material to make electrodes from. Here is a schematic drawing of meander electrodes: http://www.nature.com/gt/journal/v11/n18/images/3302337f1.gif (picture A.)
I will be using the btx ecm 830 electroporator. If not aluminum, then what other metal besides gold or platinum could I use? I intend on buying a sheet of said metal and cutting it into the meander electrode shape, then mounting this onto a handle(in a nutshell!). So please, do list a metal that can be readily purchased in sheets. Thank you!
In my opinion Aluminium is best metal for use as electrode . Reasons are low cost,easily available ,less oxidation at anod and cathode which is removable ,less toxic than iron ions ions.
Due to these properties of Aluminium it used in HT lines of electricity.Following
- Ali Abdil Razzaq Muhammed Noori Aldallal added an answer:2Does the volume of injection affect the bioavailability by intraperitoneal route?
Does the volume of injection affect the bioavailability by intraperitoneal route? Will it improve the F value significantly? For example, if I need to give 10 mg/kg of drug to a rat. In one set I dissolved the same dose in 0.4 ml and in other set I dissolved it in 2 ml and gave all of these volumes. The drug is a zwitterion, polar molecule. Any thoughts on F value variations, since the dose is kept constant? I am thinking it might improve the onset of action but the over all F should remain constant since it is the AUC which matters during F value calculations.Following
- Sudip Mukherjee added an answer:4What is the serum concentration we should use for drug release study?
Fbs can be used for drug release study. But shall we use 100% FBS or 50%?
Thanks Mr. George Dakwar for your answer.Following
- James Kilgore added an answer:3Why was development of T1249 halted as a second generation fusion inhibitor besides having promising results in Phase I and Phase II clinical trials?
This question is related to HIV drug class called fusion inhibitors. There is only one Fusion inhibitor called T20 (Enfuvirtide) approved by the FDA. I couldn't find the exact reason why the Roch and its partner company halted the development of T1249 in the middle of Phase II clinical trials despite of having good results!
If people are looking for lessons learned with T20, you might look at the peptide design issues. T20 was a 36-mer made of all proteinogenic amino acids. There are two immediate issues with this: Firstly, nearly all successful peptide drugs incorporate either D-AAS or otherwise non-proteinogenic units to slow proteolysis. Secondly, the length put it in a range where fermentative preparation wasn't really a good option, but the all-synthetic method used was extremely expensive, hence a 5-figure per-patient annual price-tag. I have no information about how quickly the drug loses effectiveness as it's metabolized but it's hard to imagine that this isn't a drawback of the design.
A lot of optimizaiton has gone into producing T20, T1249, Enfuride and related drugs. The 30 amino acids separating the pocket binding domain and the lipophilic anchoring region in the HIV sequence the fusion-blocking peptides are based on have been reduced to 23 in T1249, but that still leaves a 40-mer peptide overall. A group in Portugal showed that cholesterol can serve as the peptide lipid binding region (an 8-mer segment in T1249). It really seems that the drugs should be chimeras with non-peptide linkers such as PEG bridging the necessary recognition sequences, resulting in minimum peptide lengths and modifications to extend half-lives (and possibly reduce reactions at the injection site?)
Lets all check back in 5-10 years to see if that;s right.Following
- Chiranjeevi Srinivasa Rao Vusa added an answer:3Can someone help me in understanding the comparative catalytic properties of d-metals?
Are there any books/research papers/reviews to understand the comparative catalytic properties of transition metals, something like periodic trends(acidity,basicity,etc) or properties of elements?
I did refer JD LEE, but i did not get any info regarding my question. Can you please tell me that in which chapter you have come a cross this info?Following
- Pichan Prabhasankar added an answer:12Is anybody interested in forming an international collaboration for research into formulation development and in vivo evaluation?
Our major area of research is formulation development and in vivo evaluation. We are doing consultancy for industries too for the same. We would also like to do some collaboration under various schemes of Indian governments between two country researchers. We believe that such collaboration will always strengthen the research activities due to involvement of experts. Any one interested for the same, please contact me.
Yes, I am interested for collaboration. Please let me know terms and conditionsFollowing
- Nashwan Yousif added an answer:4Could anyone suggest the best method for storage and shelf life of Gemcitabine after reconstitution?
I am using a Pharmaceutical preparation of Gemcitabine which is reconstituted in saline for use, in animal models and cell function assays. As I do not have storage information beyond one week after reconstitution, I am trying to use it before that by storing at 4 degrees for that week. Please help if you have any experience with storage beyond one week after reconstitution.
Dear Mr. Srinivasa
I think that you should depend on the storage conditions stated on the label of the product available to you as these conditions were determined depending on stability study after reconstitution where the product may degrade into ineffective or lower potency products after that. Extending the period of storage should depend on a study to justify that , otherwise, use it as stated on the label or you may not get the expected and reliable results from your experiment
- Madhukar Baburao Deshmukh added an answer:5How to separate flavonoids from methanolic extract?I have macerated the crude powder with petroleum ether 60-80 and have further extracted with methanol using soxhlet apparatus. After that, I have used rotary vacuum evaporator to concentrate the extract and used freeze drier to dry. Now, how can I separate flavonoids from the extract?
You can separate flavonoids from methanolic extract by column chromatography using solvent Methanol:Chloroform in the proportion ( 0.5 :9.5) by volume.Following
- Nirmala S.V.S.G added an answer:3Does anyone have experience on the pH of crevicular fluid in the periodontal pocket)?The available literature is not conclusive, since we find changes that leave the pocket with basic pH (> 8-9) until researchers those postulate the pH is acidic closer to that of the establishment of dental caries process (<4.5). Can anyone help me? I'm in a line of research with polymeric bioadhesive systems for sustained release of drugs into periodontal pocket.
I think you get sufficient information given by Noori AldallalFollowing
- Ramkumar Ponnuraj added an answer:7Do antioxidants in topical formulation act on the surface of skin or do they need to penetrate the Stratum Corneum Layer?
We know that there are lot of antioxidant topical creams in the market. These antioxidant help to reduce the radicals and prevents for oxidative stress and aging. But I am confused whether these antioxidants act on surface of skin or it need to penetrate into the skin (stratum corneum) to act. Anyone aware about this can help me out. Thanks in advance.
Thanks Nashwan & Hosam for your reply
My drug is natural and it will not create any problem if it gets absorbed into systemic circulation. I thought to improve the therapeutic response of the topical cream on its application.
As rightly pointed out I need find the physico-chemical properties of Resveratrol and its penetration and will try to find that.
I will try to get it done using penetration cell enhancer.
If any of one could find any other additional details I will be great to hear.Following
- Swapnil Borse added an answer:6What are novel techniques for the estimation of drug interactions pre-clinically?Pre-clinical drug-drug interaction (DDI) assessment using in-vivo animal models along with in-vitro human systems based assays, aids in early prediction of clinical interactions possibilities and may help to prevent late phase failure of drug in clinic.
But DMEs and transporters of animals vary remarkably from humans, thus limiting their use for clinical predictions. Owing to these limitations "humanized" animal models are developed, which serves as a better model for prediction of metabolism and potential DDI in humans.
Apart from these humanized animal models what are other pre-clinical novel methodologies which are used for investigating/ predicting clinical DDI?
@AKM Mahmudul Haque, Dear Its freely available : http://cdn.intechopen.com/pdfs-wm/25226.pdfFollowing
- Andrii V. Proskochylo added an answer:1Can anyone suggest which solvent to use to obtain chromatogram from Contramid?Contramid is a high amylose starch use for controlled release of drugs.
Dear Mr. Imran Khan. Unfortunately I have not found any mentions about the chromatographic study of Contramid. Other methods are discussed in the attached document.Following
- Wayne Briner added an answer:3Does anyone have a manual or a link for the old Szent-Gyorgi & Blum Continuous flow system? Anyone have a manual for this?It seems like it might be useful, but not sure what else I would need.
Thank you so much for your efforts. Not really the info I am looking for however.Following
- Valentino Dhiyu added an answer:3Why does paracetamol need a certain moisture level and binder concentration for good compression into a tablet?With acceptable hardness and friability.
I had experience in making paracetamol tablets and met problems exactly as same as yours. 1) yes, paracetamol granules has elastic property make it vulnerable for tablet capping 2) beside optimize the binder and moisture, please also optimize the tablet shape. it will be better to choose caplet shape.Following
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