Study on the cross-linking degree of PVPP by NMR technology and its powder compressibility / 药学学报

In this paper, the low-field nuclear magnetic resonance technology CPMG (Carr-Purcell-Meiboom-Gill) echo method was used to determine the cross-linking degree and cross-linking density of crospovidone (PVPP) from different manufacturers. Based on the seven physical properties of PVPP, a fingerprint spectrum (radar chart) of twenty secondary quality indicators were obtained, and three compressibility evaluation indicators, index of the parameter (IP), index of parametric profile (IPP), index of good compression (IGC) were calculated by the fingerprint spectrum. It was found that the cross-linking degree and compressibility index IP of PVPP showed a strong correlation (r = 0.816) by the correlation analysis, indicating that the cross-linking degree is one of the key quality attributes for evaluating the compressibility of PVPP.

Formulation Development And Evaluation Of Orally Disintegrating Tablet Of Chlorpheneramine Maleate By Sublimation Technique

Objective: Chlorpheneramine maleate is a first-generation antihistamine drug used in the treatment of allergic conditions like rhinitis, urticaria, and cough cold, etc. In present work, the challenge has been made to develop an orally disintegrating tablet of chlorpheneramine maleate with an increase in bioavailability and patient compliance. Methods: The sublimation technique was used to prepare orally disintegrating tablets. Porous tablet prepared after sublimation of camphor at 60 °C in a hot air oven for 60 min. In the research work, 32full factorial design used to find out the effect of two variables like the amount of Crospovidone and Croscarmellose sodium. Results: All prepared formulations were analyzed for various parameters. DSC of pure drug and optimized formulation A (9) showed purity of sample and compatibility of all ingredients with each other. In FTIR study of pure drug and optimized formulation A (9) no major shifts were seen. An optimized formulation (A9) was found to have good hardness (3.2 kg/cm2), friability (<1%), disintegration time (26 s), % drug release (99.77 %) within 6 min. Conclusion: The result obtained showed that orally disintegrating tablet of chlorpheneramine maleate enhances dissolution rate, improves bioavailability which will improve patient compliance.

Formulation, in vitro Characterization and Stability Studies of Fast Dispersing Tablets of Diclofenac Sodium.

The present study was aimed to formulate, develop and evaluate the fast dissolving tablets of diclofenac sodium, used for the treatment of arthritis, inflammation, pain. Fast dissolving tablets of diclofenac sodium were prepared by direct compression method using crospovidone and sodium starch glycolate as superdisintegrants in concentrations of 5.3%, 6.6% and 8% w/w and in combination. In this work microcrystalline cellulose and mannitol are investigated as diluents. Prepared powder mixtures were evaluated for drug excipient compatibility with FTIR spectroscopy and DSC analysis. Prepared formulations are evaluated for In vitro dissolution, disintegration dispersion and wetting time. Formulation FCS6 prepared with combination of crospovidone and sodium starch glycolate at weight ratio of 6.6 and 2.3% showed better results compare with control. Post compression parameters like hardness (3.4 kg/cm2) and friability (0.31%) are at good acceptable levels in accordance with official compendia. FCS6 showed improved dissolution (99.8 %) and dispersion (75 seconds) profiles compared to control. The FTIR and DSC showed no interaction between the drug and excipients. The optimized formula FCS6 showed good drug release characteristics with acceptable mouth feel and fast dissolving properties.

Formulation & Evaluation of Fast Dissolving Tablets of Amlodipine Besylate by Using Co- Processed Superdisintegrants.

Aims: To formulate fast dissolving tablets of amlodipine besylate using co-processed superdisintigrant and evaluate the properties of fast dissolving tablets. Study Design: Formulation, evaluation of fast dissolving tablets of amlodipine besylate. Place and Duration of Study: Department of Quality Assurance S. N. D. College of Pharmacy Babhulgoan Yeola Dist Nashik 423401, between July 2012 to February 2013. Methodology: In the present study, novel co-processed superdisintegrants were developed by solvent evaporation method using crospovidone and sodium starch glycolate in different ratios (1:1, 1:2 1:3 2:1, 3:1) in the fast dissolving tablet formulations. Drug and the developed excipients were characterized for compatibility studies with FTIR and DSC. The co-processed superdisintigrant mixture was evaluated for angle of repose, Carr’s index and Hausner’s ratio in comparison with physical mixture of superdisintegrants. Fast dissolving tablets of Amlodipine Besylate were prepared using co-processed superdisintegrants and evaluated for pre-compression and postcompression parameters. Effect of co-processed superdisintegrants (crospovidone and sodium starch glycolate) on wetting time, disintegrating time, drug content, in-vitro release, and stability parameters have been studied. Results: The angle of repose of the developed excipients was found to be < 300 Compressibility (%) index in the range of 13.14 to 14.63 % and Hausner’s ratio in the range of 1.15-1.19. The prepared tablets were characterized by FTIR and DSC Studies there was no change in the result. Based on in-vitro dispersion time (approximately 40 sec), promising formulation CP5 was tested for in-vitro drug release pattern in phosphate buffer pH 6.8. Conclusion: Among the designed formulations, the formulation (CP5) containing coprocessed superdisintegrant (3:1 mixture of crospovidone and sodium starch glycolate) emerged as the overall best formulation based on drug release characteristics in phosphate buffer pH 6.8. From this study, it can be concluded that dissolution rate of amlodipine besylate could be enhanced by tablets containing co-processed superdisintegrant.

Formulation and in vitro evaluation of fast dissolving tablets of metoprolol tartrate

The demand for fast dissolving tablets has been growing during the last decade, especially for elderly and children who have swallowing difficulties. In the present work, fast dissolving tablets of metoprolol tartrate, were prepared using sodium starch glycolate, sodium croscarmellose and crospovidone as superdisintegrants, by the direct compression method. The tablets prepared were evaluated for various parameters including weight variation, hardness, friability, in vitro dispersion time, drug-polymer interaction, drug content water absorption ratio, wetting time, in vitro drug release, FTIR and DSC studies. The tablets prepared by the direct compression method had a weight variation in the range of 145 mg to 152 mg, which is below ± 7.5%, a hardness of 3.6 kg/cm² to 4.5 kg/cm², percentage friability of 0.46% to 0.73%, in vitro dispersion time of 18 s to 125 s, drug content uniformity of between 98.12% and 100.03%, a water absorption ratio of 67% to 87%, wetting time of 32 sec. to 64 sec., and an in vitro drug release of 53.92% - 98.82% within 15 min. The IR spectral analysis and DSC study showed no drug interaction with formulation additives of the tablet, and the formulations indicated no significant changes in hardness, friability, drug content or in vitro drug release. Fast dissolving tablets of metoprolol tartrate have enhanced dissolution and will lead to improved bioavailability and more effective therapy.

A exigência por comprimidos de dissolução rápida aumentou durante a última década, especialmente para idosos e crianças, com dificuldades de deglutição . No presente trabalho prepararam-se, pelo método de compressão direta, comprimidos de tartarato de metoprolol de rápida dissolução, utilizando glicolato sódico de amido, croscarmellose sódica e crospovidona como superdisintegrantes. Os comprimidos preparados foram avaliados em relação a diferentes parâmetros, como variação de peso, dureza, friabilidade, tempo de dispersão in vitro, interação fármaco-polímero, taxa de absorção de água pelo fármaco, tempo de umedecimento, liberação do fármaco in vitro,, FTIR e estudos de DSC. Os comprimidos preparados por compressão direta apresentaram variação de peso de 145 mg a 152 mg, abaixo de ±7,5%, dureza de 3,6 kg/cm² a 4,5 kg/cm² , porcentagem de friabilidade de 0,46% a 0,73%, tempo de dispersão in vitro de 18 s a 125 s, uniformidade de conteúdo de fármaco entre 98,12% e 100,03%, taxa de absorção de água de 67% a 87%, tempo de umidificaçãode 32 s a 64 s liberação do fármaco in vitro entre 53,92% e 98,82%, em 15 min. A análise no IV e de DSC mostrou que não houve interação de fármacos com os aditivos de formulação do comprimido e as formulações indicaram que não houve mudança significativa na dureza, friabilidade, s uniformidade de conteúdo de fármaco e na liberação do fármaco in vitro. Os comprimidos de liberação rápida apresentaram aumento na dissolução de tartarato metoprolol e conduzem à melhoria dabiodisponibilidade e à terapia eficaz.

Formulation and Characterization of Fast Disintegrating tablets of Amlodipine using Super-disintegrants.

Amlodipine besylate is a long‐acting calcium channel blocker used to treat chronic stable angina, vasospastic angina and hypertension. Amlodipine is a sparingly soluble orally administered drug and the rate of absorption is often controlled by the rate of dissolution. The rate of dissolution will increase by incorporating the drug in a fast dissolving dosage form. An attempt will be made to develop rapidly disintegrating oral tablets of Amlodipine Besylate by direct compression method. In this study, Fast Dissolving Tablet (FDT) was prepared using direct compression method using Crospovidone and Sodium starch glycolate as the super disintegrants. Amongst all formulations, formulation F3 prepared by a combination of both Crospovidone and Sodium starch glycolate showed least disintegrating time, and faster dissolution of 87%. Combination of super disintegrants were found to be better to formulate fast dissolving tablets of Amlodipine besylate.

Effect of superdisintegrants on formulation of taste masked fast disintegrating Ciprofloxacin tablets.

The present investigation deals with the formulation of taste masked fast disintegrating tablets of Ciprofloxacin that disintegrate in the oral cavity upon contact with saliva and thereby improve therapeutic efficacy. Ciprofloxacin is a synthetic chemotherapeutic antibiotic of the fluoroquinolone drug class. It is a second-generation fluoroquinolone antibacterial that kills bacteria by interfering with the enzymes that cause DNA to rewind after being copied, which stops synthesis of DNA and protein. It may also be used to prevent or slow anthrax after exposure. The influence of superdisintegrants, crospovidone and sodium starch glycolate on disintegration time, wetting time and water absorp-tion ratio were studied. Tablets were evaluation for weight and thickness variation, disintegration time, drug content, in vitro dissolution, wetting time and water absorption ratio. The in vitro disintegration time of the best fast disinte-gration tablets was found to be within 36 seconds. Tablets containing crospovidone (40%) exhibits quick disintegration time than tablets containing sodium starch glycolate. The fast disintegrating tablets of ciprofloxacin with shorter disintegration time, acceptable taste and sufficient hardness could be prepared using crospovidone and other excipients at optimum concentration.

Effect of superdisintegrants on formulation of taste masked fast disintegrating Ciprofloxacin tablets.

The present investigation deals with the formulation of taste masked fast disintegrating tablets of Ciprofloxacin that disintegrate in the oral cavity upon contact with saliva and thereby improve therapeutic efficacy. Ciprofloxacin is a synthetic chemotherapeutic antibiotic of the fluoroquinolone drug class. It is a second-generation fluoroquinolone antibacterial that kills bacteria by interfering with the enzymes that cause DNA to rewind after being copied, which stops synthesis of DNA and protein. It may also be used to prevent or slow anthrax after exposure. The influence of superdisintegrants, crospovidone and sodium starch glycolate on disintegration time, wetting time and water absorp-tion ratio were studied. Tablets were evaluation for weight and thickness variation, disintegration time, drug content, in vitro dissolution, wetting time and water absorption ratio. The in vitro disintegration time of the best fast disinte-gration tablets was found to be within 36 seconds. Tablets containing crospovidone (40%) exhibits quick disintegration time than tablets containing sodium starch glycolate. The fast disintegrating tablets of ciprofloxacin with shorter disintegration time, acceptable taste and sufficient hardness could be prepared using crospovidone and other excipients at optimum concentration.

Formulation and Evaluation of Oral disintegrated tablets of Alfuzosin Hydrochloride using superdisintegrants.

In the present work, orodispersible tablets of Alfuzosin Hcl were prepared by direct compression and sublimation methods with a view to enhance patient compliance. In these methods, varying concentrations of crospovidone, sodium starch glycolate and croscarmellose sodium of 3.3, 6.6 and 10% w/w were used, along with camphor used as subliming agent in sublimation method. The prepared batches of tablets were evaluated for hardness, friability, drug content, wetting time, dispersion time, disintegration time and dissolution studies. Based on disintegration time (approximately 13-18 seconds) all the promising formulations (from each method) were tested for in-vitro drug release pattern (in pH 6.8 phosphate buffer), drug-excipient interaction (FTIR spectroscopy) and short term stability studies. Among the promising formulations, the formulation F4 and F14 containing 10% w/w Crospovidone emerged as the overall best formulation (t50%1.79 and 1.21 minutes) based on drug release characteristic (in pH 6.8 phosphate buffer) compared to controlled formulation F1 (t50% >10 minutes).

Design and development of Orally Disintegrating Tablets of Famotidine Prepared by Direct Compression Method Using Different Superdisintegrants.

Orally disintegrating tablets (ODT) are gaining popularity over conventional tablets due to their convenience in administration and suitability for patients having dysphagia. Moreover no water is required for swallowing the tablets and hence suitable for geriatric, pediatric and traveling patients. Super disintegrants (such as Ac-Di-Sol, Crospovidone, sodium starch glycolate), Diluents (Dibasic calcium phosphate) along with sweetening agent (aspartame) were used in the formulation of tablets. The tablets were evaluated for hardness, friability, water absorption ratio, in-vitro disintegration time (DT), in-vitro disintegration time in oral cavity and in vitro drug release. Using the same excipients, the tablets were prepared by direct compression and were evaluated in the similar way. Maximum drug release and minimum DT were observed with Crospovidone excipient prepared by direct compression.

Superdisintegrant Selection for Tramadol Dispersible Tablets

The selection of a suitable superdisintegrant for a rapidly disintegrating dosage form is of the utmost importance, since disintegration time (DT) is a critical parameter. An experimental design was implemented, to find out the effects of superdisintegrants (sodium starch glycolate, crospovidone, croscarmellose sodium and methacrylic copolymer with divinyl benzene), at 2, 4, 6% w/w, on tablet hardness, with respect to DT. Methacrylic copolymer with divinyl benzene (at 4 wt%) was selected as the best superdisintegrant, adequate for the formulation of dispersible Tramadol tablets. With increasing hardness, there was a considerable increase in DT at all concentrations of superdisintegrants. A combination of crospovidone and methacrylic copolymer with divinyl benzene showed a remarkable drop in DT to 0.33 min. The stability of the batch with lowest DT was also tested under various conditions and the results suggested that there was no degradation over the test period.