scholarly journals Fabrication and Characterization of Lercanidipine Hydrochloride Solid Dispersions by Fusion Technique

2021 ◽  
Vol 11 (1) ◽  
Author(s):  
Reddy Nazemoon ◽  
Dugasani Swarnalatha ◽  
Nayakanti Devanna
Keyword(s):  
Solid Dispersion ◽  
Solid Dispersions ◽  
Compatibility Studies ◽  
Poloxamer 188 ◽  
Ftir Studies ◽  
Fabrication And Characterization ◽  
Lercanidipine Hydrochloride ◽  
Excipient Compatibility ◽  
Made In

The authors aimed to design solid dispersions with Lercanidipine Hydrochloride (LCD) with PVP K-30, Poloxamer-188, and HPMC K4M as carriers. Various mixtures of LCD and Polymers (PVP K-30, Poloxamer-188, and HPMC K4M) were made in 1:1, 1:3, 1:5 and 1:7 ratios, and the solid dispersion was prepared by melting tactic, later compressed into tablets. Drug excipient compatibility studies were examined by DSC and FTIR studies. LCD was found to compatible with carriers used. The LCD solid dispersion was measured for physicochemical quality both in solid dispersions SD, and tablet states. The LCD solid dispersions found to have excellent flow possessions and compression assets. The yield of prepared solid dispersion was observed to be more than 90%), and the formulation LPOX-3 has showed a good yield of 98.9±1.95%, The tablets which were compressed from solid dispersions were found to have a uniform in size, shape, color, and consistency. The tablets were observed to have a uniform in thickness, and weight and ranged from 300.2±1.64 to 301.7±1.64 mg. The loss on friability was less than 1%, and the hardness was more than 4 Kg/cm2 indicates significant mechanical strength and the LCD content was also found to be uniform (96.8±1.35 to 99.9±2.34). The solubility of LCD was found to be good in 0.1N HCl and diminished with an increase in pH of the buffer. LCD released from the tablets were firstly by eruption followed by zero order. The dissolution was found to be good in solid dispersions with LCD: Poloxamer-188 at the ratio of 1:5. The results obtained were satisfactory. The study concludes that LCD solid dispersions (LPOX-3) with 1:5 ratios of LCD and Poloxamer-188 was found to be a better carrier than PVP K-30, and HPMC K4M in increasing the solubility of LCD from the solid dispersions.

scholarly journals FABRICATION AND ASSESSMENT OF LERCANIDIPINE HYDROCHLORIDE SOLID DISPERSIONS FOR SOLUBILITY PREFERMENT USING POLYMER COMBINATION

2021 ◽  
pp. 77-81
Author(s):  
NAZEMOON REDDY ◽  
SWARNALATHA DUGASANI ◽  
DEVANNA NAYAKANTI
Keyword(s):  
Solid Dispersions ◽  
Methyl Cellulose ◽  
Solvent Evaporation ◽  
Vinyl Pyrrolidone ◽  
Melting Method ◽  
Poloxamer 188 ◽  
Model Drug ◽  
Poly Vinyl Pyrrolidone ◽  
Lercanidipine Hydrochloride ◽  
Made In

Objective: An attempt has made in fabricating solid dispersions (SDs) by taking lercanidipine hydrochloride (LCD) as a model drug. Methods: The SDs were made using a poly mix of poly vinyl pyrrolidone (PVP) K-30, Poloxamer-188, and hydroxy propyl methyl cellulose (HPMC) K4M. Different proportions of LCD: polymer mix in 1:1, 1:3, 1:5, and 1:7 ratios were fabricated as SDs by solvent evaporation and melting method, further compressed into tablets. The LCD SDs were assessed for physicochemical, and LCD release possessions. Results: The results were observed to be attractive with the increase in solubility LCD SD (F-3 and F-7) with 1:5 ratios of LCD. Conclusion: The study concludes that the poly mix of PVP K-30, Poloxamer-188, and HPMC K4M and was found to be a better combination for elevating the solubility and release of LCD from the SDs.

Development, Solubility Enhancement and Characterization of Nimodipine Solid Dispersions

2018 ◽  
Vol 11 (5) ◽  
pp. 4231-4239
Author(s):  
Bhikshapathi D. V. R. N. ◽  
Muralichand G
Keyword(s):  
Solid Dispersions ◽  
In Vitro Release ◽  
Solvent Evaporation Method ◽  
First Order ◽  
Ftir Studies ◽  
Release Data ◽  
Vitro Release ◽  
Excipient Compatibility

The main aim of this study was to formulate and characterize nimodipine solid dispersions using various novel polymers. Solid dispersions were prepared by solvent evaporation method in order to improve the solubility and overall bioavailability of nimodipine. Solubility and dissolution studies indicate that Kolliwax RH 40 is the most suitable polymer. The solubility studies was corresponded with dissolution data and the formulation SD15 was found to be having highest drug release of about 98.96 ± 5.15% in about 90 minutes. In vitro release data from several formulations containing Nimodipine was determined kinetically using different mathematical models like Zero order, First order, Higuchi, and Korsmeyer–Peppas model. XRD and SEM studies indicate no crystallinity in the optimized formulation SD15. FTIR studies suggested good drug excipient compatibility between all components of prepared formulation. These results confirm the viability of enhancing the solubility of nimodipine by formulating the drug as solid dispersions in Kolliwax. 

scholarly journals Design expert assisted mathematical optimization of solubility and study of fast disintegrating tablets of Lercanidipine Hydrochloride

2019 ◽  
Vol 9 (1-s) ◽  
pp. 172-180
Author(s):  
Seema Saini ◽  
Rajeev Garg
Keyword(s):  
Dissolution Rate ◽  
Solid Dispersion ◽  
Solid Dispersions ◽  
Mathematical Optimization ◽  
Statistical Design ◽  
In Vivo Studies ◽  
Dissolution Profile ◽  
Fast Disintegrating Tablets ◽  
Lercanidipine Hydrochloride

90% of drugs being researched today, posses poor solubility setback which inturn renders  the drug with slower rate of absorption from the buccal route; hence dissolution is the rate limiting step for such lipophilic drugs. So, there is a need to keep a check on the dissolution profile of these drugs to ensure maximum therapeutic utilization. The dissolution rate therefore becomes a primary factor which governs the rate and extent of its absorption. Enormous work is being performed in the field of enhancement of solubility and dissolution behaviour of such drugs. Advancements and innovations have developed solid dispersion (SD) technique as the novel method for the solubility enhancement. Precision of dosing and patient's compliance is a crucial prerequisite for the management of chronic Antihypertensive treatment, So there arised a need to formulate a system which should resolve the difficulties associated with conventional tablets. This issue can be better tackled with the formulation of orally fast disintegrating tablets. The aim of the present study was to improve the solubility and dissolution rate of Lercanidipine hydrochloride (LRH) by formulating a solid dispersion with Polyvinyl pyrollidine (PVP-K30) and Guargum. Full Factorial designs are exploited to learn and research the effects of different variables on the quality determinant parameters. An appropriate statistical model was selected for the scrutiny of the enhanced dissolution pattern. Finally, these solid dispersions were incorporated into fast disintegrating tablets. Keywords: Lercanidipine Hydrochloride, Solid dispersion, Statistical design approach, Melt fusion method, Fast disintegrating tablet, In vivo studies

Formulation Evaluation and Characterization of Fast Dissolving Tablets of Rofecoxib

2021 ◽  
pp. 60-64
Author(s):  
Preeti Mehra ◽  
Vishal Kapoor ◽  
Naveen Gupta ◽  
Dharmendra Singh Rajpoot ◽  
Neeraj Sharma
Keyword(s):  
Solid Dispersion ◽  
Water Solubility ◽  
Solid Dispersions ◽  
Amorphous State ◽  
Dissolution Profile ◽  
Major Drawback ◽  
Peg 4000 ◽  
Dissolution Efficiency ◽  
Pvp K30

Rofecoxib, a new non-steroidal anti-inflammatory agent mainly used for the treatment of osteoarthritis and rheumatoid arthritis. The major drawback of Rofecoxib is its very low water solubility, which results in poor bioavailability after oral administration. Hence, an attempt was made to formulate fast dissolving tablets of Rofecoxib. The solid dispersions of Rofecoxib were prepared with PEG-4000 and PVP K30 by solvent evaporation method. The characterization of prepared solid dispersions by FTIR, XRPD and DSC, which reveals lack of interaction with carriers and dictates amorphous state of solid dispersions. Solid dispersion of Rofecoxib with PVP K30 (1:6) showed maximum dissolution, therefore compressed into tablets by using microcrystalline cellulose, lactose and crosspovidone. The dissolution profile of developed fast dissolving tablets containing solid dispersion of Rofecoxib (1:6) was studied. The formulated formulations showed optimum dissolution efficiency.

scholarly journals DEVELOPMENT OF AMORPHOUS BINARY AND TERNARY SOLID DISPERSIONS OF NATEGLINIDE FOR IMPROVED SOLUBILITY AND DISSOLUTION

2020 ◽  
pp. 106-112
Author(s):  
SHRADHA S. TIWARI ◽  
SHAILESH J. WADHER ◽  
SURENDRA G. GATTANI
Keyword(s):  
Solid Dispersion ◽  
Water Solubility ◽  
Solid Dispersions ◽  
Physicochemical Characterization ◽  
Dissolution Behavior ◽  
Enhanced Solubility ◽  
Ft Ir ◽  
Ternary Solid Dispersion ◽  
Ternary Solid Dispersions

Objective: Nateglinide is a commonly used oral hypoglycemic, biopharmaceutical classification system Class II drug, which shows relatively poor water solubility and variable bioavailability. The objective of the present investigation was to develop the binary and ternary solid dispersions of nateglinide for improved solubility and dissolution. Methods: Nateglinide solid dispersions were prepared by a common solvent evaporation method. Polymers like soluplus, kolliphor P188, sylloid 244FP, gelucire 48/16, affinisol (HPMCAS), HPβCD, βCD were used in different combinations. The physicochemical characterization of the optimized ternary dispersion was studied by using FT-IR, DSC, and PXRD. Solubility and dissolution behavior of all dispersions were studied. Result: From all prepared ternary solid dispersions, nateglinide dissolution was significantly faster than pure nateglinide. With ternary solid dispersion of NTG, soluplus and kolliphor P188 there was a big improvement in solubility and dissolution. This combination enhanced the solubility of NTG by 23 folds. Another ternary dispersion of NTG with soluplus and gelucire 48/16 enhanced solubility by 25 fold. Conclusion: Ternary solid dispersion found superior over binary dispersions. For the ternary dispersions, showing the best solubility, tablets were prepared. Dissolution and drug release from the formulated tablet was as good as a marketed product.

scholarly journals STUDIES ON SOLID DISPERSIONS OF LEFLUNOMIDE

2020 ◽  
pp. 187-190
Author(s):  
MAHAPARALE PR ◽  
THORAT VP
Keyword(s):  
Drug Release ◽  
Solid Dispersion ◽  
Drug Carrier ◽  
Solid Dispersions ◽  
Solvent Evaporation ◽  
Water Soluble ◽  
Poloxamer 407 ◽  
Poloxamer 188 ◽  
Evaporation Method ◽  
Enhanced Solubility

Objective: Leflunomide is Non steroidal Anti-Inflammatory drug, which is poorly water soluble. In present study attempt has been made to prepare and characterize solid dispersions of leflunomide to increase solubility of drug.Method:  In Preparation of solid dispersion of leflunomide different polymer like PEG 4000, PEG 6000, Poloxamer 188 and Poloxamer 407 were used.  Effects of several variables such as type of carrier used, drug: carrier ratios, method of preparation were studied. The evaluation of solid dispersions was done by solubility study, dissolution study and X-ray diffractometry. Result: Improvement in dissolution of drug was observed in all solid dispersions as compared to pure drug alone. Solid dispersions prepared using Poloxamer 188 showed fastest in vitro drug release. Solid dispersions prepared using solvent evaporation method showed relatively faster drug release than melt evaporation method. XRD patterns indicated reduced crystallinity of drug particles, which suggests mechanism of enhanced solubility and dissolution of drug in solid dispersion systems.Conclusion:  A significant result obtained with the study indicated that solid dispersion by solvent evaporation can successfully be further explored and employed to improve solubility and dissolution characteristics of poorly soluble drugs.Keywords: Leflunomide, Solid dispersion, Carrier

scholarly journals ENHANCEMENT OF GLIBENCLAMIDE DISSOLUTION RATE BY SOLID DISPERSION METHOD USING HPMC AND PVP

2019 ◽  
pp. 19-24 ◽  
Author(s):  
ARIF BUDIMAN ◽  
IYAN SOPYAN ◽  
DENIA SEPTY RIYANDI
Keyword(s):  
Dissolution Rate ◽  
Solid Dispersion ◽  
Solid Dispersions ◽  
Hydroxypropyl Methylcellulose ◽  
X Ray Diffraction ◽  
Scanning Calorimetry ◽  
X Ray ◽  
Rate Test ◽  
Ft Ir

Objective: The aim of this study was to investigate the effects of changing in the proportions of the solid dispersion formula on the dissolution rate of glibenclamide. Methods: Solid dispersions were prepared by solvent evaporation method by using methanol as solvent, hydroxypropyl methylcellulose (HPMC) and polyvinyl pyrrolidone (PVP) as polymers. The prepared product was evaluated by the saturated solubility test and the dissolution rate test. The prepared product was characterized by Fourier transform infrared spectroscopy (FT-IR), differential scanning calorimetry (DSC), and powder X-ray diffraction (PXRD) and Scanning Electron Microscopy (SEM). Results: The result showed solid dispersion with a ratio of glibenclamide: PVP: HPMC (1: 3: 6) has the highest increase in solubility (20 fold) compared to pure glibenclamide. This formula also showed an improvement in dissolution rate from 19.9±1.19% (pure glibenclamide) to 99±1.60% in 60 min. Characterization of FT-IR showed that no chemical reaction occurred in solid dispersion of glibenclamide. The results of X-ray diffraction analysis showed an amorphous form in all solid dispersion formulas. The results of DSC analysis showed that endothermic peak melting point of solid dispersion occurred, and the morphology of solid dispersion was more irregular than pure glibenclamide based on SEM characterization Conclusion: The solid dispersion of glibenclamide using PVP: HPMC as carriers can increase the solubility and dissolution rate compared to pure glibenclamide.

scholarly journals PREPARATION AND CHARACTERIZATION OF SOLID DISPERSIONS OF CARVEDILOL WITH POLOXAMER 188

2013 ◽  
Vol 58 (1) ◽  
pp. 1553-1557 ◽  
Author(s):  
ANSHU SHARMA ◽  
CHANDRA PRAKASH JAIN ◽  
YUVERAJ SINGH TANWAR
Keyword(s):  
Solid Dispersions ◽  
Poloxamer 188
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