A Novel Liposomal Bupivacaine Formulation to Produce Ultralong-Acting Analgesia

2004 ◽  
Vol 101 (1) ◽  
pp. 133-137 ◽  
Author(s):  
Gilbert J. Grant ◽  
Yechezkel Barenholz ◽  
Elijah M. Bolotin ◽  
Mylarrao Bansinath ◽  
Herman Turndorf ◽  
...  
Keyword(s):  
Ammonium Sulfate ◽  
In Vitro Release ◽  
Rank Test ◽  
Dependent Manner ◽  
Liposomal Bupivacaine ◽  
Freeze And Thaw ◽  
Phospholipid Ratio ◽  
Remote Loading ◽  
Vitro Release

Background Currently available local anesthetics have relatively brief durations of action. An ultralong-acting local anesthetic would benefit patients with acute and chronic pain. The authors prepared and characterized a novel liposomal bupivacaine formulation using remote loading of bupivacaine along an ammonium sulfate gradient and assessed its efficacy in humans. Methods A large multivesicular liposomal bupivacaine formulation was prepared by subjecting small unilamellar vesicles to successive freeze-and-thaw cycles. Bupivacaine hydrochloride was then remotely loaded into the liposomes along an ammonium sulfate gradient ([(NH4)2SO4)]intraliposome/[(NH4)2SO4)]medium > 1000). The liposomes were then characterized for size distribution; drug-to-phospholipid ratio; in vitro release profile at 4 degree, 21 degree C, and 37 degree C; sterility; and pyrogenicity. Six subjects each received six intradermal injections in the lower back with 0.5 ml of 0.5, 1.0, and 2% liposomal bupivacaine; 0.5% standard bupivacaine; saline; and "empty" liposomes. Duration of analgesia was assessed using pinprick testing of the skin directly over the injection sites. Results were compared using the log-rank test. Results The mean large multivesicular vesicle size was 2439 +/- 544 nm, with a drug-to-phospholipid ratio of 1.8, fivefold greater than results previously reported. In vitro release was slowest at 4 degree C. The median duration of analgesia with 0.5% standard bupivacaine was 1 h. The median durations of analgesia after 0.5, 1.0, and 2.0% liposomal bupivacaine were 19, 38, and 48 h, respectively. Neither saline nor "empty" liposomes produced analgesia. Conclusions This novel liposomal formulation had a favorable drug-to-phospholipid ratio and prolonged the duration of bupivacaine analgesia in a dose-dependent manner. If these results in healthy volunteers can be duplicated in the clinical setting, this formulation has the potential to significantly impact the management of pain.

Antral gland cell column: a method for studying release of gastric hormones

1983 ◽  
Vol 245 (4) ◽  
pp. G463-G469
Author(s):  
B. Richelsen ◽  
J. F. Rehfeld ◽  
L. I. Larsson
Keyword(s):  
In Vitro Release ◽  
Dependent Manner ◽  
Gastrin Release ◽  
Cell Column ◽  
Independent Manner ◽  
Response Characteristics ◽  
Dose Dependent ◽  
Vitro Release ◽  
Stimulation Of

A technique for studying in vitro release of gastric hormones has been developed. The system utilizes nonenzymatically isolated antropyloric glands from humans or rats, which are perifused in a Bio-Gel P-2 column. The system permits the study of kinetics and dose-response characteristics using the glands as their own control. The glands were stimulated with carbachol and bombesin, and the antral peptides gastrin and somatostatin were measured. Bombesin and carbachol both evoked a dose-dependent stimulation of gastrin release, beginning at below 10(-10) M (bombesin) and 10(-7) M (carbachol). Carbachol inhibited the release of somatostatin in a dose-dependent manner, being maximally effective at 10(-6) M and then producing 60% inhibition of somatostatin release. Bombesin was without effect on antropyloric somatostatin release. These data suggest that the gastrin-stimulating effect of carbachol is partially or totally due to inhibition of somatostatin release, whereas bombesinergic stimulation of gastrin release must work in an independent manner. In addition, data on the effects of these substances on the release of gastrin and ACTH-like peptides from human antropyloric glands are presented. Due to the absence of local neural reflexes, this system is a useful supplement to the isolated perfused stomach model.

Formulation and Evaluation of Teneligliptine Pellet

2019 ◽  
Vol 9 (01) ◽  
pp. 51-57
Author(s):  
Bodhle Priyanka Raju ◽  
Satish V Shirolkar
Keyword(s):  
Chemical Interaction ◽  
In Vitro Release ◽  
Angle Of Repose ◽  
Dependent Manner ◽  
32 Factorial Design ◽  
Formulation Parameters ◽  
Tapped Density ◽  
Vitro Release ◽  
Pellet Formulation

The present study is an attempt to formulate and evaluate Teneligliptin hydrobromide hydrate pellets. Teneligliptin is a potent, selective DPP-4 inhibitor, which is believed to exert its actions in diabetes mellitus patients. Teneligliptin increases insulin release and decreases glucagon levels in the circulation in a glucose dependent manner. The Teneligliptin pellets were prepared by using blend of MCC, Lactose, Crospovidone and PVP K-30. Pellet formulation was optimized for formulation parameters (concentration of Crosspovidone and PVP K-30) using 32 factorial design. FTIR studies showed absence of chemical interaction between the drug and polymer. The pellets were prepared and evaluated in terms of bulk density, tapped density, angle of repose and in-vitro release study. In-vitro release of drug was compared with in-vitro release of drug from marketed formulation (Dynaglipt Tablet).

Study on in vitro release patterns of fentanyl-loaded PLGA microspheres

2003 ◽  
Vol 20 (5) ◽  
pp. 569-579 ◽  
Author(s):  
S.-A. Seo ◽  
G. Khang ◽  
J. M. Rhee ◽  
J. Kim ◽  
H. B. Lee
Keyword(s):  
In Vitro Release ◽  
Plga Microspheres ◽  
Vitro Release

Reliability of a Single β-Thromboglobulin Measurement in a Diabetic Population : Importance of PGE1 in Anticoagulant Mixture

1987 ◽  
Vol 57 (02) ◽  
pp. 201-204 ◽  
Author(s):  
P Y Scarabin ◽  
L Strain ◽  
C A Ludlam ◽  
J Jones ◽  
E M Kohner
Keyword(s):  
In Vitro Release ◽  
Mean Value ◽  
Reliable Estimate ◽  
Diabetic Patients ◽  
Single Measurement ◽  
Diabetic Population ◽  
The Difference ◽  
Vitro Release

SummaryDuring the collection of samples for plasma β-thromboglobulin (β-TG) determination, it is well established that artificially high values can be observed due to in-vitro release. To estimate the reliability of a single β-TG measurement, blood samples were collected simultaneously from both arms on two separate occasions in 56 diabetic patients selected for a clinical trial. From each arm, blood was taken into two tubes containing an anticoagulant mixture with (tube A) and without (tube B) PGE!. The overall mean value of B-TG in tube B was 1.14 times higher than in tube A (p <0.01). The markedly large between-arms variation accounted for the most part of within-subject variation in both tubes and was significantly greater in tube B than in tube A. Based on the difference between B-TG values from both arms, the number of subjects with artifically high B-TG values was significantly higher in tube B than in tube A on each occasion (overall rate: 28% and 14% respectively). Estimate of between-occasions variation showed that B-TG levels were relatively stable for each subject between two occasions in each tube. It is concluded that the use of PGEi decreases falsely high B-TG levels, but a single measurement of B-TG does not provide a reliable estimate of the true B-TG value in vivo.

Preparation and In-vitro Evaluation of Fe3O4 Encapsulated by Chitosan Loaded Capecitabine Nanoparticles for the Treatment of Breast Cancer

2016 ◽  
Vol 6 (3) ◽  
Author(s):  
Shanmuganathan S. ◽  
Nigma S. ◽  
Anbarasan B. ◽  
Harika B.
Keyword(s):  
Fe3o4 Nanoparticles ◽  
Polymer Concentration ◽  
In Vitro Release ◽  
Entrapment Efficiency ◽  
In Vitro Evaluation ◽  
Sem Image ◽  
Therapeutic Molecules ◽  
Dialysis Method ◽  
Vitro Release

Nanoparticulate Carriers which is biodegradable, biocompatible and bio adhesive have significant feasible applications for administration of therapeutic molecules. The present study was aimed to formulate and optimise Capecitabine loaded Chitosan-Fe3O4 Nanoparticles and to study the in-vitro evaluation by sigma dialysis method. Capecitabine loaded chitosan – Fe3O4 nanoparticles batches with different ratios of drug: polymer (1:1, 1:2, 1:3, 1:4, 1:5, 1:6) were prepared by ionic gelation method. Increase in polymer concentration increases the nanoparticle drug content. Entrapment efficiency was 60.12% with drug to polymer ratio F3 (1:3). In-vitro release was found to be 65.20% for 12 hrs. Capecitabine from chitosanFe3O4 nanoparticles SEM image reveals discrete spherical structure and particles with size range of 100-500nm. FTIR studies represent the functional groups present with no characteristics change in formulations. Samples stored at refrigerator conditions showed better stability compared with samples kept at other conditions during 8 weeks of storage.

Formulation and In-vitro Evaluation of Chewable Tablets of Montelukast Sodium

2015 ◽  
Vol 5 (3) ◽  
Author(s):  
Laxman Devkota ◽  
Bhupendra Poudel ◽  
Junu Silwal
Keyword(s):  
In Vitro Release ◽  
Magnesium Stearate ◽  
Physical Parameters ◽  
Artificial Sweetener ◽  
Leukotriene Receptor Antagonist ◽  
Montelukast Sodium ◽  
Chewable Tablets ◽  
Leukotriene Receptor ◽  
Vitro Release

The objective of the present study is to develop chewable tablets containing different pharmaceutical compositions with simple manufacturing procedures using different excipients. Mannitols, L-HPC 11, Aspartame, Crospovidone, Crospovidone, Aerosil, and Magnesium Stearate are used as excipients for effective formulation of anti-asthmatic drug Montelukast. Montelukast is a selective, orally acting leukotriene receptor antagonist that is used for the treatment of asthma and seasonal allergic rhinitis. Montelukast chewable tablets were prepared by Direct Compression methods using suitable excipients. The chewable tablets were better presented using artificial sweetener Aspartame as flavouring agent. A total of forteen formulations were prepared and the granules were evaluated for pre-compression parameters. The formulated tablets were evaluated for post-compression parameters .The results showed that all the physical parameters were within the acceptable limits. The in vitro release study of all the formulations showed good release. The study concludes that aforementioned excipients can be used to design chewable montelukast sodium tablets.

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